Integrin receptor antagonists

Abstract

This invention relates to novel heterocycles including 3-�1-�3-(imidazolin-2-ylamino)propyl!indazol-5-ylcarbonylamino!-2-(benzyloxycarbonylamino)propionic acid, which are useful as antagonists of the .alpha..sub.v .beta..sub.3 integrin and related cell surface adhesive protein receptors, to pharmaceutical compositions containing such compounds, processes for preparing such compounds, and to methods of using these compounds, alone or in combination with other therapeutic agents, for the inhibition of cell adhesion, the treatment of angiogenic disorders, inflammation, bone degradation, cancer metastasis, diabetic retinopathy, thrombosis, restenosis, macular degeneration, and other conditions mediated by cell adhesion and/or cell migration and/or angiogenesis.

Description

FIELD OF THE INVENTION

This application claims priority under 35 U.S.C. 119 (e) from provisional application Ser. No. 60/009,088, filed Dec. 22, 1995 and 60/025,699 filed Aug. 9, 1996.

This invention relates to novel heterocycles which are useful as antagonists of the .alpha..sub.v .beta..sub.3 integrin and related cell surface adhesive protein receptors, to pharmaceutical compositions containing such compounds, processes for preparing such compounds, and to methods of using these compounds, alone or in combination with other therapeutic agents, for the inhibition of cell adhesion, the treatment of angiogenic disorders, inflammation, bone degradation, cancer metastasis, diabetic retinopathy, thrombosis, restenosis, macular degeneration, and other conditions mediated by cell adhesion and/or cell migration and/or angiogenesis.

BACKGROUND OF THE INVENTION

Angiogenesis or neovascularization is critical for normal physiological processes such as embryonic development and wound repair (Folkman and Shing, J. Biol. Chem. 1992, 26:10931-10934; D'Amore and Thompson, Ann. Rev. Physiol. 1987, 49:453-464). However, angiogenesis also occurs pathologically, for example, in ocular neovascularization (leading to diabetic retinopathy, neovascular glaucoma, retinal vein occlusion and blindness), in rheumatoid arthritis and in solid tumors (Folkman and Shing, J. Biol. Chem., 1992, 267:10931-10934; Blood and Zetter, Biochim. Biophys. Acta., 1990, 1032:118-128).

Tumor dissemination, or metastasis, involves several distinct and complementary components, including the penetration and traversing of tumor cells through basement membranes and the establishment of self-sustaining tumor foci in diverse organ systems. To this end, angiogenesis is critical to tumor survival. Without neovascularization, tumor cells lack the nourishment to divide and will not be able to leave the primary tumor site (Folkman and Shing, J. Biol. Chem., 1992, 267:10931-10934).

Inhibition of angiogenesis in animal models of cancer has been shown to result in tumor growth suppression and prevention of metastatic growth (Herblin et al., Exp. Opin. Ther. Patents, 1994, 1-14). Many angiogenic inhibitors have been directed toward blocking initial cytokine-dependent induction of new vessel growth, e.g. antibodies to endothelial cell growth factors. However, these approaches are problematic because tumor and inflammatory cells can secrete multiple activators of angiogenesis (Brooks et al., Cell, 1994, 79:1157-1164). Therefore, a more general approach that would allow inhibition of angiogenesis due to a variety of stimuli would be of benefit.

The integrin .alpha..sub.v .beta..sub.3, sometimes called the vitronectin receptor, is preferentially expressed on angiogenic blood vessels in chick and man (Brooks et al., Science, 1994, 264:569-571; Enenstein and Kramer, J. Invest. Dermatol., 1994, 103:381-386). .alpha..sub.v .beta..sub.3 is the most promiscuous member of the integrin family, allowing endothelial cells to interact with a wide variety of extracellular matrix components (Hynes, Cell, 1992, 69:11-25). These adhesive interactions are considered to be critical for angiogenesis since vascular cells must ultimately be capable of invading virtually all tissues.

While integrin .alpha..sub.v .beta..sub.3 promotes adhesive events important for angiogenesis, this receptor also transmits signals from the extracellular environment to the intracellular compartment (Leavesley et al., J. Cell Biol., 1993, 121:163-170, 1993). For example, the interaction between the .alpha..sub.v .beta..sub.3 integrin and extracellular matrix components promotes a calcium signal required for cell motility.

During endothelium injury, the basement membrane zones of blood vessels express several adhesive proteins, including but not limited to von Willebrand factor, fibronectin, and fibrin. Additionally, several members of the integrin family of adhesion receptors are expressed on the surface of endothelial, smooth muscle and on other circulating cells. Among these integrins is .alpha..sub.v .beta..sub.3, the endothelial cell, fibroblast, and smooth muscle cell receptor for adhesive proteins including von Willebrand factor, fibrinogen (fibrin), vitronectin, thrombospondin, and osteopontin. These integrins initiate a calcium-dependent signaling pathway that can lead to endothelial cell and smooth muscle cell migration and, therefore, may play a fundamental role in vascular cell biology.

Recently, an antibody to the .alpha..sub.v .beta..sub.3 integrin has been developed that inhibits the interaction of this integrin with agonists such as vitronectin (Brooks et al., Science, 1994, 264:569-571). Application of this antibody has been shown to disrupt ongoing angiogenesis on the chick chorioallantoic membrane (CAM), leading to rapid regression of histologically distinct human tumor transplanted onto the CAM (Brooks et al., Cell, 1994, 79:1157-1164). In this model, antagonists of the .alpha..sub.v .beta..sub.3 integrin induced apoptosis of the proliferating angiogenic vascular cells, leaving pre-existing quiescent blood vessels unaffected. Thus, .alpha..sub.v .beta..sub.3 integrin antagonists have been shown to inhibit angiogenesis and are recognized as being useful as therapeutic agents for the treatment of human diseases such as cancer, restenosis, thromoembolic disorders, rheumatoid arthritis and ocular vasculopathies (Folkman and Shing, J. Biol. Chem., 1992, 267:10931-10934).

Increasing numbers of other cell surface receptors have been identified which bind to extracellular matrix ligands or other cell adhesion ligands thereby mediating cell-cell and cell-matrix adhesion processes. Like the .alpha..sub.v .beta..sub.3 integrin, these receptors belong to the integrin gene superfamily and are composed of heterodimeric transmembrane glycoproteins containing .alpha.- and .beta.-subunits. Integrin subfamilies contain a common .beta.-subunit combined with different .alpha.-subunits to form adhesion receptors with unique specificity. The genes for eight distinct .beta.-subunits have been cloned and sequenced to date.

The integrin .alpha..sub.v .beta..sub.3 is a member of the .beta..sub.3 integrin subfamily and has been described on platelets, endothelial cells, melanoma, smooth muscle cells, and osteoclasts (Horton and Davies, J. Bone Min. Res. 1989, 4:803-808; Davies et al., J. Cell. Biol. 1989, 109:1817-1826; Horton, Int. J. Exp. Pathol., 1990, 71:741-759). Like the major platelet integrin GPIIb/IIIa, the vitronectin receptor binds a variety of RGD-containing adhesive proteins such as vitronectin, fibronectin, von Willibrand factor, fibrinogen, osteopontin, bone sialoprotein II and thrombospondin in a manner mediated by the RGD sequence.

A key event in bone resorption is the adhesion of osteoclasts to the matrix of bone. Studies with monoclonal antibodies have implicated the .alpha..sub.v .beta..sub.3 receptor in this process and suggest that a selective .alpha..sub.v .beta..sub.3 antagonist would have utility in blocking bone resorption in diseases such as osteoporosis (Horton et al., J. Bone Miner. Res., 1993, 8:239-247; Helfrich et al., J. Bone Miner. Res., 1992, 7:335-343).

PCT Patent Application Publication Number WO94/08962, published Apr. 28, 1994 discloses fibrinogen receptor antagonists of the general formula shown below: ##STR1##

European Patent Application Publication Number 655,439, published May 31, 1995 discloses fibrinogen receptor antagonists of the general formula shown below: ##STR2##

PCT Patent Application Publication Number WO95/17397, published Jun. 29, 1995, discloses fibrinogen receptor antagonists of the general formula shown below: ##STR3##

PCT Patent Application Publication Number WO96/20192, published Jul. 4, 1996, discloses fibrinogen receptor antagonists of the general formula shown below: ##STR4##

Co-pending, commonly assigned U.S. patent application Ser. No. 08/455,768 filed May 31, 1995 discloses integrin inhibitors of the general formula shown below: ##STR5##

None of the above references discloses or suggests the compounds of the present invention which are described in detail below.

SUMMARY OF THE INVENTION

The present invention provides novel nonpeptide compounds which bind to integrin receptors thereby altering cell-matrix and cell-cell adhesion processes. The compounds of the present invention are useful for the inhibition of cell adhesion and the treatment (including prevention) of angiogenic disorders, inflammation, bone degradation, cancer metastases, diabetic retinopathy, thrombosis, restenosis, macular degeneration, and other conditions mediated by cell adhesion and/or cell migration and/or angiogenesis.

One aspect of this invention provides novel compounds of Formula Ia, Ib or Ic (described below) which are useful as antagonists of the .alpha..sub.v .beta..sub.3 integrin. The .alpha..sub.v .beta..sub.3 integrin is also referred to as the .alpha..sub.v .beta..sub.3 receptor or the vitronectin receptor. The compounds of the present invention inhibit the binding of vitronectin or other RGD-containing ligands to .alpha..sub.v .beta..sub.3 and inhibit cell adhesion. The present invention also includes pharmaceutical compositions containing such compounds, and methods of using such compounds for the inhibition of angiogenesis, and/or for the treatment of disorders mediated by angiogenesis.

Another aspect of the present invention comprises agents that inhibit the binding of vitronectin to the .alpha..sub.v .beta..sub.3 receptor for the treatment (including prevention) of thrombosis, which do not significantly alter hemostatic balance and do not significantly inhibit platelet aggregation and do not significantly inhibit coagulation. Also, the compounds of the current invention can be used for the treatment or prevention of restenosis.

The present invention also provides novel compounds, pharmaceutical compositions and methods which may be used in the treatment or prevention of other diseases which involve cell adhesion processes, including, but not limited to, rheumatoid arthritis, asthma, allergies, adult respiratory distress syndrome, graft versus host disease, organ transplantation, septic shock, psoriasis, eczema, contact dermatitis, osteoporosis, osteoarthritis, atherosclerosis, metastasis, wound healing, diabetic retinopathy, ocular vasculopathies, inflammatory bowel disease and other autoimmune diseases.

Also included in the present invention are pharmaceutical kits comprising one or more containers containing pharmaceutical dosage units comprising a compound of Formula Ia, Ib or Ic, for the therapeutic inhibition of cell adhesion, the treatment of angiogenic disorders, inflammation, bone degradation, cancer metastasis, diabetic retinopathy, thrombosis, restenosis, macular degeneration, and other conditions mediated by cell adhesion and/or cell migration and/or angiogenesis.

DETAILED DESCRIPTION OF THE INVENTION

The present invention provides novel compounds of Formula Ia, Ib or Ic (described below) which bind to integrin receptors thereby altering cell-matrix and cell-cell adhesion processes. The compounds of the present invention are useful for the inhibition of cell adhesion and the treatment of angiogenic disorders, inflammation, bone degradation, cancer metastases, diabetic retinopathy, thrombosis, restenosis, macular degeneration, and other conditions mediated by cell adhesion and/or cell migration and/or angiogenesis, in a mammal.

One aspect of this invention provides novel compounds of Formula Ia, Ib or Ic (described below) which are. useful as antagonists of the .alpha..sub.v .beta..sub.3 integrin. The .alpha..sub.v .beta..sub.3 integrin is also referred to as the .alpha..sub.v .beta..sub.3 receptor or the vitronectin receptor. The compounds of the present invention inhibit the binding of vitronectin or other RGD-containing ligands to .alpha..sub.v .beta..sub.3 and inhibit cell adhesion. The present invention also includes pharmaceutical compositions containing such compounds of Formula Ia, Ib or Ic, and methods of using such compounds for the inhibition of angiogenesis, and/or for the treatment of angiogenic disorders, inflammation, bone degradation, cancer metastases, diabetic retinopathy, thrombosis, restenosis, macular degeneration, and other conditions mediated by cell adhesion and/or cell migration and/or angiogenesis, in a mammal.

�1! One aspect of the present invention comprises compounds of Formula Ia: ##STR6## including stereoisomeric forms thereof, or mixtures of stereoisomeric forms thereof, or pharmaceutically acceptable salt or prodrug forms thereof, wherein:

X.sup.1, X.sup.2, X.sup.3, and X.sup.4 are independently selected from nitrogen or carbon provided that at least two of X.sup.1, X.sup.2, X.sup.3 and X.sup.4 are carbon; R.sup.1 is selected from: ##STR7## A and B are independently --CH.sub.2 --, --O--, --N(R.sup.2)--, or --C(.dbd.O)--; A.sup.1 and B.sup.1 are independently --CH.sub.2 -- or --N(R.sup.3)--; D is --N(R.sup.2)--, --O--, --S--, --C(.dbd.O)-- or --SO.sub.2 --; E--F is --C(R.sup.4).dbd.C(R.sup.5)--, --N.dbd.C(R.sup.4)--, --C(R.sup.4).dbd.N--, or --C(R.sup.4).sub.2 C(R.sup.5).sub.2 --; J, K, L and M are independently selected from --C(R.sup.4)--, --C(R.sup.5)-- or --N--, provided that at least one of J, K, L and M is not --N--; R.sup.2 is selected from: H, C.sub.1 -C.sub.6 alkyl, (C.sub.1 -C.sub.6 alkyl)carbonyl, (C.sub.1 -C.sub.6 alkoxy)carbonyl; (C.sub.1 -C.sub.6 alkyl)aminocarbonyl, C.sub.3 -C.sub.6 alkenyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.4 -C.sub.11 cycloalkylalkyl, aryl, heteroaryl(C.sub.1 -C.sub.6 alkyl)carbonyl, heteroarylcarbonyl, aryl(C.sub.1 -C.sub.6 alkyl)-, (C.sub.1 -C.sub.6 alkyl)carbonyl--, arylcarbonyl, C.sub.1 -C.sub.6 alkylsulfonyl, arylsulfonyl, aryl(C.sub.1 -C.sub.6 alkyl)sulfonyl, heteroarylsulfonyl, heteroaryl(C.sub.1 -C.sub.6 alkyl)sulfonyl, aryloxycarbonyl, or aryl(C.sub.1 -C.sub.6 alkoxy)carbonyl, wherein said aryl groups are substituted with 0-2 substituents selected from the group consisting of C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, halo, CF.sub.3, and nitro; R.sup.3 is selected from: H, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.4 -C.sub.11 cycloalkylalkyl, aryl, aryl(C.sub.1 -C.sub.6 alkyl)-, or heteroaryl(C.sub.1 -C.sub.6 alkyl)-; R.sup.4 and R.sup.5 are independently selected from: H, C.sub.1 -C.sub.4 alkoxy, NR.sup.2 R.sup.3, halogen, NO.sub.2, CN, CF.sub.3, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 alkenyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.4 -C.sub.11 cycloalkylalkyl, aryl, aryl(C.sub.1 -C.sub.6 alkyl)-, (C.sub.1 -C.sub.6 alkyl)carbonyl, (C.sub.1 -C.sub.6 alkoxy)carbonyl, arylcarbonyl, or alternatively, when substituents on adjacent atoms, R.sup.4 and R.sup.5 can be taken together with the carbon atoms to which they are attached to form a 5-7 membered carbocyclic or 5-7 membered heterocyclic aromatic or non-aromatic ring system, said carbocyclic or heterocyclic ring being optionally substituted with 0-2 groups selected from: C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, halo, cyano, amino, CF.sub.3, or NO.sub.2 ; U is selected from: --(CH.sub.2).sub.n --, --(CH.sub.2).sub.n (CR.sup.7 .dbd.CR.sup.8)(CH.sub.2).sub.m --, --(CH.sub.2).sub.n (C.tbd.C)(CH.sub.2).sub.m --, --(CH.sub.2).sub.t Q(CH.sub.2).sub.m --, --(CH.sub.2).sub.n O(CH.sub.2).sub.m --, --(CH.sub.2).sub.n N(R.sup.6)(CH.sub.2).sub.m --, --(CH.sub.2).sub.n C(.dbd.O)(CH.sub.2).sub.m --, --(CH.sub.2).sub.n (C.dbd.O)N(R.sup.6)(CH.sub.2).sub.m -- --(CH.sub.2).sub.n N(R.sup.6)(C.dbd.O)(CH.sup.2).sub.m --, or --(CH.sub.2).sub.n S(O).sub.p (CH.sub.2).sub.m --;

wherein one or more of the methylene groups in U is optionally substituted with R.sup.7 ;

Q is selected from 1,2-cycloalkylene, 1,2-phenylene, 1,3-phenylene, 1,4-phenylene, 2,3-pyridinylene, 3,4-pyridinylene, 2,4-pyridinylene, or 3,4-pyridazinylene; R.sup.6 is selected from: H, C.sub.1 -C.sub.4 alkyl, or benzyl; R.sup.7 and R.sup.8 are independently selected from: H, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.4 -C.sub.11 cycloalkylalkyl, aryl, aryl(C.sub.1 -C.sub.6 alkyl)-, or heteroaryl(C.sub.0 -C.sub.6 alkyl)-; R.sup.10 is selected from: H, C.sub.1 -C.sub.4 alkoxy substituted with 0-1 R.sup.21, N(R.sup.6).sub.2, halogen, NO.sub.2, CN, CF.sub.3, CO.sub.2 R.sup.17, C(.dbd.O)R.sup.17, CONR.sup.17 R.sup.20, --SO.sub.2 R.sup.17, --SO.sub.2 NR.sup.17 R.sup.20, C.sub.1 -C.sub.6 alkyl substituted with 0-1 R.sup.15 or 0-1 R.sup.21, C.sub.3 -C.sub.6 alkenyl substituted with 0-1 R.sup.15 or 0-1 R.sup.21, C.sub.3 -C.sub.7 cycloalkyl substituted with 0-1 R.sup.15 or 0-1 R.sup.21, C.sub.4 C.sub.11 cycloalkylalkyl substituted with 0-1 R.sup.15 or 0-1 R.sup.21, aryl substituted with 0-1 R.sup.15 or 0-2 R.sup.11 or 0-1 R.sup.21, or aryl(C.sub.1 -C.sub.6 alkyl)-substituted with 0-1 R.sup.15 or 0-2 R.sup.11 or 0-1 R.sup.21 ; R.sup.11 is selected from H, halogen, CF.sub.3, CN, NO.sub.2, hydroxy, NR.sup.2 R.sup.3, C.sub.1 -C.sub.4 alkyl substituted with 0-1 R.sup.21, C.sub.1 -C.sub.4 alkoxy substituted with 0-1 R.sup.21, aryl substituted with 0-1 R.sup.21, aryl(C.sub.1 -C.sub.6 alkyl)-substituted with 0-1 R.sup.21, (C.sub.1 -C.sub.4 alkoxy)carbonyl substituted with 0-1 R.sup.21, (C.sub.1 -C.sub.4 alkyl)carbonyl substituted with 0-1 R.sup.21, C.sub.1 -C.sub.4 alkylsulfonyl substituted with 0-1 R.sup.21, or C.sub.1 -C.sub.4 alkylaminosulfonyl substituted with 0-1 R.sup.21 ; W is selected from: --(C(R.sup.12).sub.2).sub.q C(.dbd.O)N(R.sup.13)--, or --C(.dbd.O)--N(R.sup.13)--(C(R.sup.12).sub.2).sub.q --; X is --C(R.sup.12)(R.sup.14)--C(R.sup.12)(R.sup.15)--; or alternatively, W and X can be taken together to be ##STR8## R.sup.12 is selected from H, halogen, C.sub.1 -C.sub.6 alkyl C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkynyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.4 -C.sub.10 cycloalkylalkyl, (C.sub.1 -C.sub.4 alkyl)carbonyl, aryl, or aryl(C.sub.1 -C.sub.6 alkyl)-; R.sup.13 is selected from H, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.7 cycloalkylmethyl, or aryl(C.sub.1 -C.sub.6 alkyl)-; R.sup.14 is selected from: H, C.sub.1 -C.sub.6 alkylthio (C.sub.1 -C.sub.6 alkyl)-, aryl(C.sub.1 -C.sub.10 alkylthioalkyl)-, aryl(C.sub.1 -C.sub.10 alkoxyalkyl)-, C.sub.1 -C.sub.10 alkyl, C.sub.1 -C.sub.10 alkoxyalkyl, C.sub.1 -C.sub.6 hydroxyalkyl, C.sub.2 -C.sub.10 alkenyl, C.sub.2 -C.sub.10 alkynyl, C.sub.3 -C.sub.10 cycloalkyl.sub.1 C.sub.3 -C.sub.10 cycloalkylalkyl, aryl(C.sub.1 -C.sub.6 alkyl)-, heteroaryl(C.sub.1 -C.sub.6 alkyl)-, aryl, heteroaryl, CO.sub.2 R.sup.17, C(.dbd.O) R.sup.17, or CONR.sup.17 R.sup.20, provided that any of the above alkyl, cycloalkyl, aryl or heteroaryl groups may be unsubstituted or substituted independently with 0-1 R.sup.16 or 0-2 R.sup.11 ; R.sup.15 is selected from: H, R.sup.16, C.sub.1 -C.sub.10 alkyl, C.sub.1 -C.sub.10 alkoxyalkyl, C.sub.1 -C.sub.10 alkylaminoalkyl, C.sub.1 -C.sub.10 dialkylaminoalkyl, (C.sub.1 -C.sub.10 alkyl)carbonyl, aryl(C.sub.0 -C.sub.6 alkyl)carbonyl, C.sub.1 -C.sub.10 alkenyl, C.sub.1 -C.sub.10 alkynyl, C.sub.3 -C.sub.10 cycloalkyl, C.sub.3 -C.sub.10 cycloalkylalkyl, aryl(C.sub.1 -C.sub.6 alkyl)-, heteroaryl(C.sub.1 -C.sub.6 alkyl)-, aryl, heteroaryl, CO.sub.2 R.sup.17, C(.dbd.O)R.sup.17, CONR.sup.17 R.sup.20, SO.sub.2 R.sup.17, or SO.sub.2 NR.sup.17 R.sup.20, provided that any of the above alkyl, cycloalkyl, aryl or heteroaryl groups may be unsubstituted or substituted independently with 0-2 R.sup.11 ; Y is selected from: --COR.sup.19, --SO.sub.3 H, --PO.sub.3 H, tetrazolyl, --CONHNHSO.sub.2 CF.sub.3, --CONHSO.sub.2 R.sup.17, --CONHSO.sub.2 NHR.sup.17, --NHCOCF.sub.3, --NHCONHSO.sub.2 R.sup.17, --NHSO.sub.2 R.sup.17, --OPO.sub.3 H.sub.2, --OSO.sub.3 H, --PO.sub.3 H.sub.2, --SO.sub.3 H, SO.sub.2 NHCOR.sup.17, --SO.sub.2 NHCO.sub.2 R.sup.17, ##STR9## R.sup.16 is selected from: --N(R.sup.20)--C(.dbd.O)--O--R.sup.17, --N(R.sup.20)--C(.dbd.O)--R.sup.17, --N(R.sup.20)--C(.dbd.O)--NH--R.sup.17, --N(R.sup.20)SO.sub.2 --R.sup.17, or --N(R.sup.20)SO.sub.2 --NR.sup.20 R.sup.17 ; R.sup.17 is selected from: --C.sub.1 -C.sub.10 alkyl, C.sub.3 -C.sub.11 cycloalkyl, aryl(C.sub.1 -C.sub.6 alkyl)-, (C.sub.1 -C.sub.6 alkyl)aryl, heteroaryl(C.sub.1 -C.sub.6 alkyl)-, (C.sub.1 -C.sub.6 alkyl)heteroaryl, biaryl(C.sub.1 -C.sub.6 alkyl)-, heteroaryl, or aryl, wherein said aryl or heteroaryl groups are optionally substituted with 0-3 substituents selected from the group consisting of: C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, aryl, heteroaryl, halo,cyano, amino, CF.sub.3, and NO.sub.2 ; R.sup.18 is selected from: H, --C(.dbd.O)--O--R.sup.17, --C(.dbd.O)--R.sup.17, --C(.dbd.O)--NH--R.sup.17, --SO.sub.2 --R.sup.17, or --SO.sub.2 --NR.sup.20 R.sup.17 ; R.sup.19 is selected from: hydroxy, C.sub.1 -C.sub.10 alkyloxy, C.sub.3 -C.sub.11 cycloalkyloxy, aryloxy, aryl(C.sub.1 -C.sub.6 alkoxy)- , C.sub.3 -C.sub.10 alkylcarbonyloxyalkyloxy, C.sub.3 -C.sub.10 alkoxycarbonyloxyalkyloxy, C.sub.2 -C.sub.10 alkoxycarbonylalkyloxy, C.sub.5 -C.sub.10 cycloalkylcarbonyloxyalkyloxy, C.sub.5 -C.sub.10 cycloalkoxycarbonyloxyalkyloxy, C.sub.5 -C.sub.10 cycloalkoxycarbonylalkyloxy, C.sub.7 -C.sub.11 aryloxycarbonylalkyloxy, C.sub.8 -C.sub.12 aryloxycarbonyloxyalkyloxy, C.sub.8 -C.sub.12 arylcarbonyloxyalkyloxy, C.sub.5 -C.sub.10 alkoxyalkylcarbonyloxyalkyloxy, C.sub.5 -C.sub.10 (5alkyl-1,3-dioxa-cyclopenten-2-one-yl)methyloxy, C.sub.10 -C.sub.14 (5-aryl-1,3-dioxa-cyclopenten-2-one-yl)methyloxy, or (R.sup.11)(R.sup.12)N--(C.sub.1 -C.sub.10 alkoxy)-; R.sup.20 is selected from: H, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.4 -C.sub.11 cycloalkylalkyl, aryl, aryl(C.sub.1 -C.sub.6 alkyl)-, or heteroaryl(C.sub.1 -C.sub.6 alkyl)-; R.sup.21 is selected from: COOH or NR.sup.6.sub.2 ; m is 0-4; n is 0-4; t is 0-4; p is 0-2; q is 0-2; and r is 0-2; with the following provisos: (1) t, n, m and q are chosen such that the number of atoms connecting R.sup.1 and Y is in the range of 10-14; and (2) n and m are chosen such that the value of n plus m is greater than one unless U is --(CH.sub.2).sub.t Q(CH.sub.2).sub.m --.

�2! Preferred compounds of the invention as described above are compounds of the Formula Ia: ##STR10## including stereoisomeric forms thereof, or mixtures of stereoisomeric forms thereof, or pharmaceutically acceptable salt or prodrug forms thereof, wherein:

X.sup.1, X.sup.2, X.sup.3, and X.sup.4 are independently selected from nitrogen or carbon provided that at least two of X.sup.1, X.sup.2, X.sup.3 and X.sup.4 are carbon; R.sup.1 is selected from: ##STR11## A and B are independently --CH.sub.2 --, --O--, --N(R.sup.2)--, or --C(.dbd.O)--; A.sup.1 and B.sup.1 are independently --CH.sub.2 -- or --N(R.sup.3)--; D is --N(R.sup.2)--, --O--, --S--, --C(.dbd.O)-- or --SO.sub.2 --; E--F is --C(R.sup.4).dbd.C(R.sup.5)--, --N.dbd.C(R.sup.4)--, --C(R.sup.4).dbd.N--, or --C(R.sup.4).sub.2 (R.sup.5).sub.2 --; J, K, L and M are independently selected from --C(R.sup.4)--, --C(R.sup.5)-- or --N--, provided that at least one of J, K, L and M is not --N--; R.sup.2 is selected from: H, C.sub.1 -C.sub.6 alkyl, (C.sub.1 -C.sub.6 alkyl)carbonyl, (C.sub.1 -C.sub.6 alkoxy)carbonyl, C.sub.1 -C.sub.6 alkylaminocarbonyl, C.sub.3 -C.sub.6 alkenyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.4 -C.sub.11 cycloalkylalkyl, aryl, heteroaryl(C.sub.l -C.sub.6 alkyl)carbonyl, heteroarylcarbonyl, aryl(C.sub.1 -C.sub.6 alkyl)-, (C.sub.1 -C.sub.6 alkyl)carbonyl, arylcarbonyl, alkylsulfonyl, arylsulfonyl, aryl(C.sub.1 -C.sub.6 alkyl)sulfonyl, heteroarylsulfonyl, heteroaryl(C.sub.1 -C.sub.6 alkyl)sulfonyl, aryloxycarbonyl, or aryl(C.sub.1 -C.sub.6 alkoxy)carbonyl, wherein said aryl groups are substituted with 0-2 substituents selected from the group consisting of C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, halo, CF.sub.3, and nitro; R.sup.3 is selected from: H, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.4 -C.sub.11 cycloalkylalkyl, aryl, aryl(C.sub.1 -C.sub.6 alkyl)-, or heteroaryl(C.sub.1 -C.sub.6 alkyl)-; R.sup.4 and R.sup.5 are independently selected from: H, C.sub.1 -C.sub.4 alkoxy, NR.sup.2 R.sup.3, halogen, NO.sub.2, CN, CF.sub.3, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 alkenyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.4 -C.sub.11 cycloalkylalkyl, aryl, aryl(C.sub.1 -C.sub.6 alkyl)-, C.sub.2 -C.sub.7 alkylcarbonyl, arylcarbonyl or alternatively, when substituents on adjacent atoms, R.sup.4 and R.sup.5 can be taken together with the carbon atoms to which they are attached to form a 5-7 membered carbocyclic or 5-7 membered heterocyclic aromatic or non-aromatic ring system, said carbocyclic or heterocyclic ring being optionally substituted with 0-2 groups selected from: C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, halo, cyano, amino, CF.sub.3, or NO.sub.2 ; U is selected from: --(CH.sub.2).sub.n --, --(CH.sub.2).sub.n (CR.sup.7 .dbd.CR.sup.8)(CH.sub.2).sub.m --, --(CH.sub.2).sub.t Q(CH.sub.2).sub.m --, --(CH.sub.2).sub.n O(CH.sub.2).sub.m --, --(CH.sub.2).sub.n N(R.sup.6)(CH.sub.2).sub.m --, --(CH.sub.2).sub.n C(.dbd.O)(CH.sub.2).sub.m --, or --(CH.sub.2).sub.n S(O).sub.p (CH.sub.2).sub.m --; wherein one or more of the methylene groups in U is optionally substituted with R.sup.7 ; Q is selected from 1,2-phenylene, 1,3-phenylene, 2,3-pyridinylene, 3,4-pyyrdinylene, or 2,4-pyridinylene; R.sup.6 is selected from: H, C.sub.1 -C.sub.4 alkyl, or benzyl; R.sup.7 and R.sup.8 are independently selected from: H, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.4 -C.sub.11 cycloalkylalkyl, aryl, aryl(C.sub.1 -C.sub.6 alkyl)-, or heteroaryl(C.sub.0 -C.sub.6 alkyl)-; R.sup.10 is selected from: H, C.sub.1 -C.sub.4 alkoxy substituted with 0-1 R.sup.21, N(R.sup.6).sub.2, halogen, NO.sub.2, CN, CF.sub.3, CO.sub.2 R.sup.17, C(.dbd.O)R.sup.17, CONR.sup.17 R.sup.20, --SO.sub.2 R.sup.17, --SO.sub.2 NR.sup.17 R.sup.20, C.sub.1 -C.sub.6 alkyl substituted with 0-1 R.sup.15 or 0-1 R.sup.21, C.sub.3 -C.sub.6 alkenyl substituted with 0-1 R.sup.15 or 0-1 R.sup.21 C.sub.3 -C.sub.7 cycloalkyl substituted with 0-1 R.sup.15 or 0-1 R.sup.21, C.sub.4 -C.sub.11 cycloalkylalkyl substituted with 0-1 R.sup.15 or 0-1 R.sup.21.sub.1 aryl substituted with 0-1 R.sup.15 or 0-2 R.sup.11 or 0-1 R.sup.21, or aryl(C.sub.1 -C.sub.6 alkyl)-substituted with 0-1 R.sup.15 or 0-2 R.sup.11 or 0-1 R.sup.21 ; R.sup.11 is selected from: H, halogen, CF.sub.3, CN, NO.sub.2, hydroxy, NR.sup.2 R.sup.3, C.sub.1 -C.sub.4 alkyl substituted with 0-1 R.sup.21, C.sub.1 -C.sub.4 alkoxy substituted with 0-1 R.sup.21, aryl substituted with 0-1 R.sup.21, aryl(C.sub.1 -C.sub.6 alkyl)-substituted with 0-1 R.sup.21, (C.sub.1 -C.sub.4 alkoxy)carbonyl substituted with 0-1 R.sup.21, (C.sub.1 -C.sub.4 alkyl)carbonyl substituted with 0-1 R.sup.21 C.sub.1 -C.sub.4 alkylsulfonyl substituted with 0-1 R.sup.21, or C.sub.1 -C.sub.4 alkylaminosulfonyl substituted with 0-1 R.sup.21 ; W is --C(.dbd.O)--N(R.sup.13)--(C(R.sup.12).sub.2).sub.q --; X is --C(R.sup.12)(R.sup.14)--C(R.sup.12)(R.sup.15)--; alternatively, W and X can be taken together to be ##STR12## R.sup.12 is H or C.sub.1 -C.sub.6 alkyl; R.sup.13 is selected from: H, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.7 cycloalkylmethyl, or aryl(C.sub.1 -C.sub.6 alkyl)-; R.sup.14 is selected from: H, C.sub.1 -C.sub.6 alkylthioalkyl, aryl(C.sub.1 -C.sub.10 alkylthioalkyl)-, aryl(C.sub.1 -C.sub.10 alkoxyalkyl)-, C.sub.1 -C.sub.10 alkyl, C.sub.1 -C.sub.10 alkoxyalkyl, C.sub.1 -C.sub.6 hydroxyalkyl, C.sub.2 -C.sub.10 alkenyl, C.sub.2 -C.sub.10 alkynyl, C.sub.3 -C.sub.10 cycloalkyl, C.sub.3 -C.sub.10 cycloalkylalkyl, aryl(C.sub.1 -C.sub.6 alkyl)-, heteroaryl(C.sub.1 -C.sub.6 alkyl)-, aryl, heteroaryl, CO.sub.2 R.sup.17, C(.dbd.O)R.sup.17, or CONR.sup.17 R.sup.20, or provided that any of the above alkyl, cycloalkyl, aryl or heteroaryl groups may be substituted independently with 0-1 R.sup.16 or 0-2 R.sup.11 ; R.sup.15 is selected from: H, R.sup.16, C.sub.1 -C.sub.10 alkyl, C.sub.1 -C.sub.10 alkoxyalkyl, C.sub.1 -C.sub.10 alkylaminoalkyl, C.sub.1 -C.sub.10 dialkylaminoalkyl, C.sub.1 -C.sub.10 alkylcarbonyl, aryl(C.sub.0 -C.sub.6 alkyl)carbonyl, C.sub.2 -C.sub.10 alkenyl, C.sub.2 -C.sub.10 alkynyl ,C.sub.3 -C.sub.10 cycloalkyl, C.sub.3 -C.sub.10 cycloalkylalkyl, aryl(C.sub.1 -C.sub.6 alkyl)-, heteroaryl(C.sub.1 -C.sub.6 alkyl)-, aryl, heteroaryl, CO.sub.2 R.sup.17, C(.dbd.O)R.sup.17, CONR.sup.17 R.sup.20, SO.sub.2 R.sup.17 or SO.sub.2 NR.sup.17 R.sup.20, provided that any of the above alkyl, cycloalkyl, aryl or heteroaryl groups may be substituted independently with 0-2 R.sup.11 ; Y is selected from: ##STR13## R.sup.16 is selected from: --N(R.sup.20)--C(.dbd.O)--O--R.sup.17, --N(R.sup.20)--C(.dbd.O)--R.sup.17, --N(R.sup.20)--C(.dbd.O)--NH--R.sup.17, --N(R.sup.20)SO.sub.2 --R.sup.17, or --N(R.sup.20)SO.sub.2 --NR.sup.20 R.sup.17 ; R.sup.17 is selected from: C.sub.1 -C.sub.10 alkyl, C.sub.3 -C.sub.11 cycloalkyl, aryl(C.sub.1 -C.sub.6 alkyl)-, (C.sub.1 -C.sub.6 alkyl)aryl, heteroaryl(C.sub.1 -C.sub.6 alkyl)-, (C.sub.1 -C.sub.6 alkyl)heteroaryl, biaryl(C.sub.1 -C.sub.6 alkyl)-, heteroaryl, or aryl, wherein said aryl or heteroaryl groups are optionally substituted with 0-3 substituents selected from the group consisting of: C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, aryl, heteroaryl, halo,cyano, amino, CF.sub.3, and NO.sub.2 ; R.sup.18 is selected from: H, --C(.dbd.O)--O--R.sup.17, --C(.dbd.O)--R.sup.17, --C(.dbd.O)--NH--R.sup.17, --SO.sub.2 --R.sup.17, or --SO.sub.2 --NR.sup.20 R.sup.17 ; R.sup.19 is selected from: hydroxy, C.sub.1 -C.sub.10 alkyloxy, C.sub.3 -C.sub.11 cycloalkyloxy, C.sub.6 -C.sub.10 aryloxy, C.sub.7 -C.sub.11 aralkyloxy, C.sub.3 -C.sub.10 alkylcarbonyloxyalkyloxy, C.sub.3 -C.sub.10 alkoxycarbonyloxyalkyloxy, C.sub.2 -C.sub.10 alkoxycarbonylalkyloxy, C.sub.5 -C.sub.10 cycloalkylcarbonyloxyalkyloxy, C.sub.5 -C.sub.10 cycloalkoxycarbonyloxyalkyloxy, C.sub.5 -C.sub.10 cycloalkoxycarbonylalkyloxy, C.sub.7 -C.sub.11 aryloxycarbonylalkyloxy, C.sub.8 -C.sub.12 aryloxycarbonyloxyalkyloxy, C.sub.8 -C.sub.12 arylcarbonyloxyalkyloxy, C.sub.5 -C.sub.10 alkoxyalkylcarbonyloxyalkyloxy, C.sub.5 -C.sub.10 (5-alkyl-1,3-dioxa-cyclopenten-2-one-yl)methyloxy, C.sub.10 -C.sub.14 (5-aryl-1,3-dioxa-cyclopenten-2-one-yl)methyloxy, or (R.sup.11)(R.sup.12)N--(C.sub.1 -C.sub.10 alkoxy)-; R.sup.20 selected from: H, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.4 -C.sub.11 cycloalkylalkyl, aryl(C.sub.1 -C.sub.6 alkyl)-, or heteroaryl(C.sub.1 -C.sub.6 alkyl)-; R.sup.21 is selected from COOH or NR.sup.6.sub.2 ; m is 0-4; n is 0-4; p is 0-2; q is 0-2; t is 0-4; and r is 0-2.

�3! Further preferred compounds of the invention as described above are compounds of the Formula IIa or IIb: ##STR14## including stereoisomeric forms thereof, or mixtures of stereoisomeric forms thereof, or pharmaceutically acceptable salt or prodrug forms thereof wherein:

X.sup.1 and X.sub.3 are independently selected from nitrogen or carbon; R.sup.1 is selected from: ##STR15## wherein the above heterocycles are optionally substituted with 0-2 substituents selected from the group consisting of: NH.sub.2, halogen, NO.sub.2, CN, CF.sub.3, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.6 alkyl, and C.sub.3 -C.sub.7 cycloalkyl; U is --(CH.sub.2).sub.n --, --(CH.sub.2).sub.t Q(CH.sub.2).sub.m -- or --C(.dbd.O)(CH.sub.2).sub.n-1 --, wherein one of the methylene groups is optionally substituted with R.sup.7 ; Q is selected from 1,2-phenylene, 1,3-phenylene, 2,3-pyridinylene, 3,4-pyrrdinylene, or 2,4-pyridinylene; R.sup.6 is selected from: H, C.sub.1 -C.sub.4 alkyl, or benzyl; R.sup.7 is selected from: C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.4 -C.sub.11 cycloalkylalkyl, aryl, aryl(C.sub.1 -C.sub.6 alkyl), heteroaryl, or heteroaryl(C.sub.1 -C.sub.6 alkyl); R.sup.10 is selected from: H, C.sub.1 -C.sub.4 alkoxy substituted with 0-1 R.sup.21, halogen, CO.sub.2 R.sup.17, CONR.sup.17 R.sup.20, C.sub.1 -C.sub.6 alkyl substituted with 0-1 R.sup.15 or 0-1 R.sup.21, C.sub.3 -C.sub.7 cycloalkyl substituted with 0-1 R.sup.15 or 0-1 R.sup.21, C.sub.4 -C.sub.11 cycloalkylalkyl substituted with 0-1 R.sup.15 or 0-1 R.sup.21, or aryl(C.sub.1 -C.sub.6 alkyl)-substituted with 0-1 R.sup.15 or 0-2 R.sup.11 or 0-1 R.sup.21 ; R.sup.11 is selected from: H, halogen, CF.sub.3, CN, NO.sub.2, hydroxy, NR.sup.2 R.sup.3, C.sub.1 -C.sub.4 alkyl substituted with 0-1 R.sup.21, C.sub.1 -C.sub.4 alkoxy substituted with 0-1 R.sup.21, aryl substituted with 0-1 R.sup.21, aryl(C.sub.1 -C.sub.6 alkyl)-substituted with 0-1 R.sup.21, (C.sub.1 -C.sub.4 alkoxy)carbonyl substituted with 0-1 R.sup.21, (C.sub.1 -C.sub.4 alkyl)carbonyl substituted with 0-1 R.sup.21, C.sub.1 -C.sub.4 alkylsulfonyl substituted with 0-1 R.sup.21, or C.sub.1 -C.sub.4 alkylaminosulfonyl substituted with 0-1 R.sup.21 ; W is --C(.dbd.O)--N(R.sup.13)--; X is --CH(R.sup.14)--CH(R.sup.15)--; R.sup.13 is H or CH.sub.3 ; R.sup.14 is selected from: H, C.sub.1 -C.sub.10 alkyl, aryl, or heteroaryl, wherein said aryl or heteroaryl groups are optionally substituted with 0-3 substituents selected from the group consisting of: C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, aryl, halo, cyano, amino, CF.sub.3, and NO.sub.2 ; R.sup.15 is H or R.sup.16 ; Y is --COR.sup.19 ; R.sup.16 is selected from: --NH (R.sup.20)--C(.dbd.O)--O--R.sup.17, --N(R.sup.20)--C(.dbd.O)--R.sup.17, --N(R.sup.20)--C(.dbd.O)--NH--R.sup.17, --N(R.sup.20)SO.sub.2 --R.sup.17, or --N(R.sup.20)SO.sub.2 --N(R.sup.20) R.sup.17 ; R.sup.17 is selected from: C.sub.1 -C.sub.10 alkyl, C.sub.3 -C.sub.11 cycloalkyl, aryl(C.sub.1 -C.sub.6 alkyl)-, (C.sub.1 -C.sub.6 alkyl)aryl, heteroaryl(C.sub.1 -C.sub.6 alkyl)-, (C.sub.1 -C.sub.6 alkyl)heteroaryl, biaryl(C.sub.1 -C.sub.6 alkyl)-, heteroaryl, or aryl, wherein said aryl or heteroaryl groups are optionally substituted with 0-3 substituents selected from the group consisting of: C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, aryl, heteroaryl, halo, cyano, amino, CF.sub.3, and NO.sub.2 ; R.sup.19 is selected from: hydroxy, C.sub.1 -C.sub.10 alkoxy, methylcarbonyloxymethoxy-, ethylcarbonyloxymethoxy-, t-butylcarbonyloxymethoxy-, cyclohexylcarbonyloxymethoxy-, 1-(methylcarbonyloxy)ethoxy-, 1-(ethylcarbonyloxy)ethoxy-, 1-(t-butylcarbonyloxy)ethoxy-, 1-(cyclohexylcarbonyloxy)ethoxy-, i-propyloxycarbonyloxymethoxy-, t-butyloxycarbonyloxymethoxy-, 1-(i-propyloxycarbonyloxy)ethoxy-, 1-(cyclohexyloxycarbonyloxy)ethoxy-, 1-(t-butyloxycarbonyloxy)ethoxy-, dimethylaminoethoxy-, diethylaminoethoxy-, (5-methyl-1,3-dioxacyclopenten-2-on-4-yl)methoxy-, (5-(t-butyl)-1,3-dioxacyclopenten-2-on-4-yl)methoxy-, (1,3-dioxa-5-phenyl-cyclopenten-2-on-4-yl)methoxy-, or 1-(2-(2-methoxypropyl)carbonyloxy)ethoxy-; R.sup.20 is H or CH.sub.3 ; R.sup.21 is selected from COOH or NR.sup.6.sub.2 ; m is 0 or 1; n is 1-4; and t is 0 or 1.

�4! Still further preferred compounds of the above invention are compounds of the Formula IIa or IIb: ##STR16## including stereoisomeric forms thereof, or mixtures of stereoisomeric forms thereof, or pharmaceutically acceptable salt or prodrug forms thereof wherein: X.sub.1 and X.sub.3 are independently selected from nitrogen or carbon, provided that at least one of X.sub.1 and X.sub.3 is carbon;

R.sup.1 is selected from: ##STR17## wherein the above heterocycles are optionally substituted with 0-2 substituents selected from the group consisting of: NH.sub.2, halogen, NO.sub.2, CN, CF.sub.3, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.6 alkyl, and C.sub.3 -C.sub.7 cycloalkyl; U is --(CH.sub.2).sub.n --, --(CH.sub.2).sub.t Q (CH.sub.2).sub.m -- or --C(.dbd.O)(CH.sub.2).sub.n-1 --, wherein one of the methylene groups is optionally substituted with R.sup.7 ; Q is selected from 1,2-phenylene, 1,3-phenylene, 2,3-pyridinylene, 3,4-pyridinylene, or 2,4-pyridinylene; R.sup.6 is selected from: H, C.sub.1 -C.sub.4 alkyl, or benzyl; R7 is selected from: C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.4 -C.sub.11 cycloalkylalkyl, aryl, aryl(C.sub.1 -C.sub.6 alkyl), heteroaryl, or heteroaryl(C.sub.1 -C.sub.6 alkyl); R.sup.10 is selected from: H, C.sub.1 -C.sub.4 alkoxy substituted with 0-1 R.sup.21, halogen, CO.sub.2 R.sup.17, CONR.sup.17 R.sup.20, C.sub.1 -C.sub.6 alkyl substituted with 0-1 R.sup.15 or 0-1 R.sup.21, C.sub.3 -C.sub.7 cycloalkyl substituted with 0-1 R.sup.15 or 0-1 R.sup.21, C.sub.4 -C.sub.11 cycloalkylalkyl substituted with 0-1 R.sup.15 or 0-1 R.sup.21, or aryl(C.sub.1 -C.sub.6 alkyl)-substituted with 0-1 R.sup.15 or 0-2 R.sup.11 or 0-1 R.sup.21 ; R.sup.11 is selected from: H, halogen, CF.sub.3, CN, NO.sub.2, hydroxy, NR.sup.2 R.sup.3, C.sub.1 -C.sub.4 alkyl substituted with 0-1 R.sup.21 C.sub.1 -C.sub.4 alkoxy substituted with 0-1 R.sup.21, aryl substituted with 0-1 R.sup.21, aryl(C.sub.1 -C.sub.6 alkyl)-substituted with 0-1 R.sup.21, (C.sub.1 -C.sub.4 alkoxy)carbonyl substituted with 0-1 R.sup.21, (C.sub.1 -C.sub.4 alkyl)carbonyl substituted with 0-1 R.sup.21, C.sub.1 -C.sub.4 alkylsulfonyl substituted with 0-1 R.sup.21, or C.sub.1 -C.sub.4 alkylaminosulfonyl substituted with 0-1 R.sup.21 ;W is --C(.dbd.O)--N(R.sup.13)--; W is --C(.dbd.O)-N(R.sup.13)--; X is --CH(R.sup.14)--CH(R.sup.15)--; R.sup.13 is H or CH.sub.3 ; R.sup.14 is selected from: H, C.sub.1 -C.sub.10 alkyl, aryl, or heteroaryl, wherein said aryl or heteroaryl groups are optionally substituted with 0-3 substituents selected from the group consisting of: C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, aryl, halo, cyano, amino, CF.sub.3, and NO.sub.2 ; R.sup.15 is H or R.sup.16 ; Y is --COR.sup.19 ; R.sup.16 is selected from: --N(R.sup.20)--C(.dbd.O)--O--R.sup.17, --N(R.sup.20)--C(.dbd.O)--R.sup.17, --N(R.sup.20)--C(.dbd.O)--NH--R.sup.17, --N(R.sup.20)SO.sub.2 --R.sup.17, or --N(R.sup.20)SO.sub.2 --NR.sup.20 R.sup.17 ; R.sup.17 is selected from: C.sub.1 -C.sub.10 alkyl, C.sub.3 -C.sub.11 cycloalkyl, aryl(C.sub.1 -C.sub.6 alkyl)-, (C.sub.1 -C.sub.6 alkyl)aryl, heteroaryl(C.sub.1 -C.sub.6 alkyl)-, (C.sub.1 -C.sub.6 alkyl)heteroaryl, biaryl(C.sub.1 -C.sub.6 alkyl)-, heteroaryl, or aryl, wherein said aryl or heteroaryl groups are optionally substituted with 0-3 substituents selected from the group consisting of: C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, aryl, heteroaryl, halo, cyano, amino, CF.sub.3, and NO.sub.2 ; R.sup.19 is selected from: hydroxy, C.sub.1 -C.sub.10 alkoxy, methylcarbonyloxymethoxy-, methylcarbonyloxymethoxy-, t-butylcarbonyloxymethoxy-, cyclohexylcarbonyloxymethoxy-, 1-(methylcarbonyloxy)ethoxy-, 1-(ethylcarbonyloxy)ethoxy-, 1-(t-butylcarbonyloxy)ethoxy-, 1-(cyclohexylcarbonyloxy)ethoxy-, i-propyloxycarbonyloxymethoxy-, t-butyloxycarbonyloxymethoxy-, 1-(i-propyloxycarbonyloxy)ethoxy-, 1-(cyclohexyloxycarbonyloxy)ethoxy-, 1-(t-butyloxycarbonyloxy)ethoxy-, dimethylaminoethoxy-, diethylaminoethoxy-, (5-methyl-1,3-dioxacyclopenten-2-on-4-yl)methoxy-, (5-(t-butyl)-1,3-dioxacyclopenten-2-on-4-yl)methoxy-, (1,3-dioxa-5-phenyl-cyclopenten-2-on-4-yl)methoxy-, or 1-(2-(2-methoxypropyl)carbonyloxy)ethoxy-; R.sup.20 is H or CH.sub.3 ; R.sup.21 is selected from COOH or NR.sup.6.sub.2 ; m is 0 or 1; n is 1-4; and t is 0 or 1.

�5! Specifically preferred compounds of the invention as described above are compounds of Formula Ia, including enantiomeric or diasteriomeric forms thereof, or mixtures of enantiomeric or diasteriomeric forms thereof, or pharmaceutically acceptable salt or prodrug forms thereof, selected from the group consisting of:

3-�1-�3-(imidazolin-2-ylamino)propyl!indazol-5-ylcarbonylamino!-2-(benzyloxycarbonylamino)-propionic acid, 3-�1-�3-(imidazolin-2-ylamino)propyl!indazol-5-ylcarbonylamino!-2-(2,4,6-trimethylbenzenesulfonylamino)propionic acid, 3-�1-�3-(imidazolin-2-ylamino)propyl!indazol-5-ylcarbonylamino!-2-(benzenesulfonylamino)propionic acid, 3-�1-�3-(imidazolin-2-ylamino)propyl!indazol-5-ylcarbonylamino!-2-(2,6-dichlorobenzenesulfonylamino)propionic acid, 3-�1-�3-(imidazolin-2-ylamino)propyl!indazol-5-ylcarbonylamino!-2-(3,5-dimethylisoxazol-4-ylsulfonylamino)propionic acid, 3-�1-�3-(imidazolin-2-ylamino)propyl!indazol-5-ylcarbonylamino!-2-(2,6-dimethylbenzenesulfonylamino)propionic acid, 3-�1-�3-(imidazolin-2-ylamino)propyl!indazol-5-ylcarbonylamino!-2-(2,6-dimethyl-4-phenylbenzenesulfonylamino)propionic acid, 3-�1-�3-(imidazolin-2-ylamino)propyl!indazol-5-ylcarbonylamino!-2-(4-phenylbenzenesulfonylamino)propionic acid, 3-�1-�3-(tetrahydropyrimid-2-ylamino)propyl!indazol-5-ylcarbonylamino!-2-(benzyloxycarbonylamino)propionic acid, 3-�1-�3-(tetrahydropyrimid-2-ylamino)propyl!indazol-5-ylcarbonylamino!-2-(2,4,6-trimethylbenzenesulfonylamino)propionic acid, 3-�1-�3-(tetrahydropyrimid-2-ylamino)propyl!indazol-5-ylcarbonylamino!-2-(benzenesulfonylamino)propionic acid, 3-�1-�3-(tetrahydropyrimid-2-ylamino)propyl!indazol-5-ylcarbonylamino!-2-(2,6-dichlorobenzenesulfonylamino)propionic acid, 3-�1-�3-(tetrahydropyrimid-2-ylamino)propyl!indazol-5-ylcarbonylamino!-2-(3,5-dimethylisoxazol-4-ylsulfonylamino)propionic acid, 3-�1-�3-(tetrahydropyrimid-2-ylamino)propyl!indazol-5-ylcarbonylamino!-2-(2,6-dimethylbenzenesulfonylamino)propionic acid, 3-�1-�3-(tetrahydropyrimid-2-ylamino)propyl!indazol-5-ylcarbonylamino!-2-(2,6-dimethyl-4-phenylbenzenesulfonylamino)propionic acid, 3-�1-�3-(tetrahydropyrimid-2-ylamino)propyl!indazol-5-ylcarbonylamino!-2-(4-phenylbenzenesulfonylamino)propionic acid, 3-�1-�3-(imidazol-2-ylamino)propyl!indazol-5-ylcarbonylamino!-2-(benzyloxycarbonylamino)propionic acid, 3-�1-�3-(imidazol-2-ylamino)propyl!indazol-5-ylcarbonylamino!-2-(2,4,6-trimethylbenzenesulfonylamino)propionic acid, 3-�1-�3-(imidazol-2-ylamino)propyl!indazol-5-ylcarbonylamino!-2-(benzenesulfonylamino)propionic acid, 3-�1-�3-(imidazol-2-ylamino)propyl!indazol-5-ylcarbonylamino!-2-(2,6-dichlorobenzenesulfonylamino)propionic acid, 3-�1-�3-(imidazol-2-ylamino)propyl!indazol-5-ylcarbonylamino!-2-(3,5-dimethylisoxazol-4-ylsulfonylamino)propionic acid, 3-�1-�3-(imidazol-2-ylamino)propyl!indazol-5-ylcarbonylamino!-2-(2,6-dimethylbenzenesulfonylamino)propionic acid, 3-�1-�3-(imidazol-2-ylamino)propyl!indazol-5-ylcarbonylamino!-2-(2,6-dimethyl-4-phenylbenzenesulfonylamino)propionic acid, 3-�1-�3-(imidazol-2-ylamino)propyl!indazol-5-ylcarbonylamino!-2-(4-phenylbenzenesulfonylamino)propionic acid, 3-�1-�3-(pyridin-2-ylamino)propyl!indazol-5-ylcarbonylamino!-2-(benzyloxycarbonylamino)propionic acid, 3-�1-�3-(pyridin-2-ylamino)propyl!indazol-5-ylcarbonylamino!-2-(2,4,6-trimethylbenzenesulfonylamino)propionic acid, 3-�1-�3-(pyridin-2-ylamino)propyl!indazol-5-ylcarbonylamino!-2-(benzenesulfonylamino)propionic acid, 3-�1-�3-(pyridin-2-ylamino)propyl!indazol-5-ylcarbonylamino!-2-(2,6-dichlorobenzenesulfonylamino)propionic acid, 3-�1-�3-(pyridin-2-ylamino)propyl!indazol-5-ylcarbonylamino!-2-(3,5-dimethylisoxazol-4-ylsulfonylamino)propionic acid, 3-�1-�3-(pyridin-2-ylamino)propyl!indazol-5-ylcarbonylamino!-2-(2,6-dimethylbenzenesulfonylamino)propionic acid, 3-�1-�3-(pyridin-2-ylamino)propyl!indazol-5-ylcarbonylamino!-2-(2,6-dimethyl-4-phenylbenzenesulfonylamino)propionic acid, 3-�1-�3-(pyridin-2-ylamino)propyl!indazol-5-ylcarbonylamino!-2-(4-phenylbenzenesulfonylamino)propionic acid, 3-�1-�3-(imidazolin-2-ylamino)propyl!indazol-4-ylcarbonylamino!-2-(benzyloxycarbonylamino)propionic acid, 3-�1-�3-(imidazolin-2-ylamino)propyl!indazol-4-ylcarbonylamino!-2-(2,4,6-trimethylbenzenesulfonylamino)propionic acid, 3-�1-�3-(imidazolin-2-ylamino)propyl!indazol-4-ylcarbonylamino!-2-(benzenesulfonylamino)propionic acid, 3-�1-�3-(imidazolin-2-ylamino)propyl!indazol-4-ylcarbonylamino!-2-(2,6-dichlorobenzenesulfonylamino)propionic acid, 3-�1-�3-(imidazolin-2-ylamino)propyl!indazol-4-ylcarbonylamino!-2-(3,5-dimethylisoxazol-4-ylsulfonylamino)propionic acid, 3-�1-�3-(imidazolin-2-ylamino)propyl!indazol-4-ylcarbonylamino!-2-(2,6-dimethylbenzenesulfonylamino)propionic acid, 3-�1-�3-(imidazolin-2-ylamino)propyl!indazol-4-ylcarbonylamino!-2-(2,6-dimethyl-4-phenylbenzenesulfonylamino)propionic acid, 3-�1-�3-(imidazolin-2-ylamino)propyl!indazol-4-ylcarbonylamino!-2-(4-phenylbenzenesulfonylamino)propionic acid, 3-�1-�3-(tetrahydropyrimid-2-ylamino)propyl!indazol-4-ylcarbonylamino!-2-(benzyloxycarbonylamino)propionic acid, 3-�1-�3-(tetrahydropyrimid-2-ylamino)propyl!indazol-4-ylcarbonylamino!-2-(2,4,6-trimethylbenzenesulfonylamino)propionic acid, 3-�1-�3-(tetrahydropyrimid-2-ylamino)propyl!indazol-4-ylcarbonylamino!-2-(benzenesulfonylamino)propionic acid, 3-�1-�3-(tetrahydropyrimid-2-ylamino)propyl!indazol-4-ylcarbonylamino!-2-(2,6-dichlorobenzenesulfonylamino)propionic acid, 3-�1-�3-(tetrahydropyrimid-2-ylamino)propyl!indazol-4-ylcarbonylamino!-2-(3,5-dimethylisoxazol-4-ylsulfonylamino)propionic acid, 3-�1-�3-(tetrahydropyrimid-2-ylamino)propyl!indazol-4-ylcarbonylamino!-2-(2,6-dimethylbenzenesulfonylamino)propionic acid, 3-�1-�3-(tetrahydropyrimid-2-ylamino)propyl!indazol-4-ylcarbonylamino!-2-(2,6-dimethyl-4-phenylbenzenesulfonylamino)propionic acid, 3-�1-�3-(tetrahydropyrimid-2-ylamino)propyl!indazol-4-ylcarbonylamino!-2-(4-phenylbenzenesulfonylamino)propionic acid, 3-�1-�3-(imidazol-2-ylamino)propyl!indazol-4-ylcarbonylamino!-2-(benzyloxycarbonylamino)propionic acid, 3-�1-�3-(imidazol-2-ylamino)propyl!indazol-4-ylcarbonylamino!-2-(2,4,6-trimethylbenzenesulfonylamino)propionic acid, 3-�1-�3-(imidazol-2-ylamino)propyl!indazol-4-ylcarbonylamino!-2-(benzenesulfonylamino)propionic acid, 3-�1-�3-(imidazol-2-ylamino)propyl!indazol-4-ylcarbonylamino!-2-(2,6-dichlorobenzenesulfonylamino)propionic acid, 3-�1-�3-(imidazol-2-ylamino)propyl!indazol-4-ylcarbonylamino!-2-(3,5-dimethylisoxazol-4-ylsulfonylamino)propionic acid, 3-�1-�3-(imidazol-2-ylamino)propyl!indazol-4-ylcarbonylamino!-2-(2,6-dimethylbenzenesulfonylamino)propionic acid, 3-�1-8 3-(imidazol-2-ylamino)propyl!indazol-4-ylcarbonylamino!-2-(2,6-dimethyl-4-phenylbenzenesulfonylamino)propionic acid, 3-�1-�3-(imidazol-2-ylamino)propyl!indazol-4-ylcarbonylamino!-2-(4-phenylbenzenesulfonylamino)propionic acid, 3-�1-�3-(pyridin-2-ylamino)propyl!indazol-4-ylcarbonylamino!-2-(benzyloxycarbonylamino)propionic acid, 3-�1-�3-(pyridin-2-ylamino)propyl!indazol-4-ylcarbonylamino!-2-(2,4,6-trimethylbenzenesulfonylamino)propionic acid, 3-�1-�3-(pyridin-2-ylamino)propyl!indazol-4-ylcarbonylamino!-2-(benzenesulfonylamino)propionic acid, 3-�1-�3-(pyridin-2-ylamino)propyl!indazol-4-ylcarbonylamino!-2-(2,6-dichlorobenzenesulfonylamino)propionic acid, 3-�1-�3-(pyridin-2-ylamino)propyl!indazol-4-ylcarbonylamino!-2-(3,5-dimethylisoxazol-4-ylsulfonylamino)propionic acid, 3-�1-�3-(pyridin-2-ylamino)propyl!indazol-4-ylcarbonylamino!-2-(2,6-dimethylbenzenesulfonylamino)propionic acid, 3-�1-�3-(pyridin-2-ylamino)propyl!indazol-4-ylcarbonylamino!-2-(2,6-dimethyl-4-phenylbenzenesulfonylamino)propionic acid, and 3-�1-�3-(pyridin-2-ylamino)propyl!indazol-4-ylcarbonylamino!-2-(4-phenylbenzenesulfonylamino)propionic acid.

Also specifically preferred are ester prodrugs of the specifically preferred compounds of Formula Ia, said esters being chosen from the group consisting of:

methyl, ethyl, isopropyl, n-butyl, isobutyl, benzyl, methylcarbonyloxymethyl, ethylcarbonyloxymethyl, tert-butylcarbonyloxymethyl, cyclohexylcarbonyloxymethyl, tert-butyloxycarbonyloxymethyl, dimethylaminoethyl, diethylaminoethyl, morpholinoethyl, pyrrolidinoethyl, and trimethylanimonioethyl.

�6! Another aspect of the present invention comprises compounds of Formula Ib: ##STR18## including stereoisomeric forms thereof, or mixtures of stereoisomeric forms thereof, or pharmaceutically acceptable salt or prodrug forms thereof, wherein:

X.sup.1, X.sup.2, X.sup.3, and X.sup.4 are independently selected from nitrogen or carbon provided that at least two of X.sup.1, X.sup.2, X.sup.3 and X.sup.4 are carbon; R.sup.1 is selected from: ##STR19## A and B are independently --CH.sub.2 --, --O--, --N(R.sup.2)--, or --C(.dbd.O)--; A.sup.1 and B.sup.1 are independently --CH.sub.2 -- or --N(R.sup.3)--; D is --N(R.sup.2)--, --O--, --S--, --C(.dbd.O)-- or --SO.sub.2 --; E--F is --C(R.sup.4).dbd.C(R.sup.5)--, --N.dbd.C(R.sup.4)--, --C(R.sup.4).dbd.N--, or --C(R.sup.4).sub.2 C(R.sup.5).sub.2 --; J, K, L and M are independently selected from: --C(R.sup.4)--, --C(R.sup.5)-- or --N--, provided that at least one of J, K, L and M is not --N--; R.sup.2 is selected from: H, C.sub.1 -C.sub.6 alkyl, (C.sub.1 -C.sub.6 alkyl)carbonyl, (C.sub.1 -C.sub.6 alkoxy)carbonyl; (C.sub.1 -C.sub.6 alkyl)aminocarbonyl, C.sub.3 -C.sub.6 alkenyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.4 -C.sub.11 cycloalkylalkyl, aryl, heteroaryl(C.sub.1 -C.sub.6 alkyl)carbonyl, heteroarylcarbonyl, aryl C.sub.1 -C.sub.6 alkyl, (C.sub.1 -C.sub.6 alkyl)carbonyl, or arylcarbonyl, C.sub.1 -C.sub.6 alkylsulfonyl, arylsulfonyl, aryl(C.sub.1 -C.sub.6 alkyl)sulfonyl, heteroarylsulfonyl, heteroaryl(C.sub.1 -C.sub.6 alkyl)sulfonyl, aryloxycarbonyl, or aryl(C.sub.1 -C.sub.6 alkoxy)carbonyl, wherein said aryl groups are substituted with 0-2 substituents selected from the group consisting of C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, halo, CF.sub.3, and nitro; R.sup.3 is selected from: H, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.4 -C.sub.11 cycloalkylalkyl, aryl, aryl(C.sub.1 -C.sub.6 alkyl)-, or heteroalry (C.sub.1 -C.sub.6 alkyl); R.sup.4 and R.sup.5 are independently selected from: H, C.sub.1 -C.sub.4 alkoxy, NR.sup.2 R.sup.3 halogen, NO.sub.2, CN, CF.sub.3, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 alkenyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.4 -C.sub.11 cycloalkylalkyl, aryl, aryl(C.sub.1 -C.sub.6 alkyl)(C.sub.1 -C.sub.6 alkyl)carbonyl, (C.sub.1 -C.sub.6 alkoxy)carbonyl, arylcarbonyl, or alternatively, when substituents on adjacent atoms, R.sup.4 and R.sup.5 can be taken together with the carbon atoms to which they are attached to form a 5-7 membered carbocyclic or 5-7 membered heterocyclic aromatic or non-aromatic ring system, said carbocyclic or heterocyclic ring being optionally substituted with 0-2 groups selected from: C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, halo, cyano, amino, CF.sub.3, or NO.sub.2 ; U is selected from: --(CH.sub.2).sub.n --, --(CH.sub.2).sub.n (CR.sup.7 .dbd.CR.sup.8)(CH.sub.2).sub.m -- --(CH.sub.2).sub.n (C.tbd.C)(CH.sub.2).sub.m -- --(CH.sub.2).sub.t Q(CH.sub.2).sub.m -- --(CH.sub.2).sub.n O(CH.sub.2).sub.m --, --(CH.sub.2).sub.n N(R.sup.6)(CH.sub.2).sub.m --, --(CH.sub.2).sub.n C(.dbd.O)(CH.sub.2).sub.m --, --(CH.sub.2).sub.n (C.dbd.O)N(R.sup.6)(CH.sub.2).sub.m -- --(CH.sub.2).sub.n N(R.sup.6)(C.dbd.O)(CH.sub.2).sub.m --, or --(CH.sub.2).sub.n S (O).sub.p (CH.sub.2).sub.m --; wherein one of the methylene groups is optionally substituted with R.sup.7 ; Q is selected from: 1,2-cycloalkylene, 1,2-phenylene, 1,3-phenylene, 1,4-phenylene, 2,3-pyridinylene, 3,4-pyridinylene, 2,4-pyridinylene, or 3,4-pyridazinylene; R.sup.6 is selected from: H, C.sub.1 -C.sub.4 alkyl, or benzyl; R.sup.7 and R.sup.8 are independently selected from: H, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.4 -C.sub.11 cycloalkylalkyl, aryl, aryl(C.sub.1 -C.sub.6 alkyl)-, or heteroaryl(C.sub.0 -C.sub.6 alkyl)-; R.sup.9 is selected from: H, CO.sub.2 R.sup.17, C(.dbd.O)R.sup.17, CONR.sup.17 R.sup.20, --SO.sub.2 R.sup.17, --SO.sub.2 NR.sup.17 R.sup.20, C.sub.1 -C.sub.6 alkyl substituted with 0-1 R.sup.15 or 0-1 R.sup.21, C.sub.3 -C.sub.6 alkenyl substituted with 0-1 R.sup.15 or 0-1 R.sup.21, C.sub.3 -C.sub.7 cycloalkyl substituted with 0-1 R.sup.15 or 0-1 R.sup.21, C.sub.4 -C.sub.11 cycloalkylalkyl substituted with 0-1 R.sup.15 or 0-1 R.sup.21, aryl substituted with 0-1 R.sup.15 or 0-2 R.sup.11 or 0-1 R.sup.21, or aryl(C.sub.1 -C.sub.6 alkyl)substituted with 0-1 R.sup.15 or 0-2 R.sup.11 or 0-1 R.sup.21 ; R.sup.11 is selected from H, halogen, CF.sub.3, CN, NO.sub.2, hydroxy, NR.sup.2 R.sup.3, C.sub.1 -C.sub.4 alkyl substituted with 0-1 R.sup.21, C.sub.1 -C.sub.4 alkoxy substituted with 0-1 R.sup.21, aryl substituted with 0-1 R.sup.21, aryl(C.sub.1 -C.sub.6 alkyl)substituted with 0-1 R.sup.21, (C.sub.1 -C.sub.4 alkoxy)carbonyl substituted with 0-1 R.sup.21, (C.sub.1 -C.sub.4 alkyl)carbonyl substituted with 0-1 R.sup.21, C.sub.1 -C.sub.4 alkylsulfonyl substituted with 0-1 R.sup.21, or C.sub.1 -C.sub.4 alkylaminosulfonyl substituted with 0-1 R.sup.21 ; W is selected from: --(C(R.sup.12).sub.2).sub.q C(.dbd.O)N(R.sup.13)--, or --C(.dbd.O)--N(R.sup.13)--(C(R.sup.12).sub.2).sub.q --; X is --C(R.sup.12)(R.sup.14)--C(R.sup.12)(R.sup.15)--; or alternatively, W and X can be taken together to be ##STR20## R.sup.12 is selected from: H, halogen, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkynyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.4 -C.sub.10 cycloalkylalkyl, (C.sub.1 -C.sub.4 alkyl)carbonyl, aryl, or aryl(C.sub.1 -C.sub.6 alkyl)-; R.sup.13 is selected from: H, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.7 cycloalkylmethyl, or aryl(C.sub.1 -C.sub.6 alkyl)-; R.sup.14 is selected from: H, C.sub.1 -C.sub.6 alkylthio(C.sub.1 -C.sub.6 alkyl)-, aryl(C.sub.1 -C.sub.10 alkylthioalkyl)-, aryl(C.sub.1 -C.sub.10 alkoxyalkyl)-, C.sub.1 -C.sub.10 alkyl, C.sub.1 -C.sub.10 alkoxyalkyl, C.sub.1 -C.sub.6 hydroxyalkyl, C.sub.2 -C.sub.10 alkenyl, C.sub.2 -C.sub.10 alkynyl, C.sub.3 -C.sub.10 cycloalkyl, C.sub.3 -C.sub.10 cycloalkylalkyl, aryl(C.sub.1 -C.sub.6 alkyl)-, heteroaryl(C.sub.1 -C.sub.6 alkyl)-, aryl, heteroaryl, CO.sub.2 R.sup.17, C(.dbd.O)R.sup.17, or CONR.sup.17 R.sup.20, provided that any of the above alkyl, cycloalkyl, aryl or heteroaryl groups may be unsubstituted or substituted independently with 0-1 R.sup.16 or 0-2 R.sup.11 ; R.sup.15 is selected from: H, R.sup.16 C.sub.1 -C.sub.10 alkyl, C.sub.1 -C.sub.10 alkoxyalkyl, C.sub.1 -C.sub.10 alkylaminoalkyl, C.sub.1 -C.sub.10 dialkylaminoalkyl, (C.sub.1 -C.sub.10 alkyl)carbonyl, aryl(C.sub.0 -C.sub.6 alkyl)carbonyl, C.sub.1 -C.sub.10 alkenyl, C.sub.1 -C.sub.10 alkynyl ,C.sub.3 -C.sub.10 cycloalkyl, C.sub.3 -C.sub.10 cycloalkylalkyl, aryl(C.sub.1 -C.sub.6 alkyl)-, heteroaryl(C.sub.1 -C.sub.6 alkyl)-, aryl, heteroaryl, CO.sub.2 R.sup.17, C(.dbd.O)R.sup.17, CONR.sup.17 R.sup.20, SO.sub.2 R.sup.17, or SO.sub.2 NR.sup.17 R.sup.20, provided that any of the above alkyl, cycloalkyl, aryl or heteroaryl groups may be unsubstituted or substituted independently with 0-2 R.sup.11 ; Y is selected from: --COR.sup.19, --SO.sub.3 H, --PO.sub.3 H, tetrazolyl, --CONHNHSO.sub.2 CF.sub.3, --CONHSO.sub.2 R.sup.17, --CONHSO.sub.2 NHR.sup.17, --NHCOCF.sub.3, --NHCONHSO.sub.2 R.sup.17, --NHSO.sub.2 R.sup.17, --OPO.sub.3 H.sub.2, --OSO.sub.3 H, --PO.sub.3 H.sub.2, --SO.sub.3 H, --SO.sub.2 NHCOR.sup.17, --SO.sub.2 NHCO.sub.2 R.sup.17, ##STR21## R.sup.16 is selected from: --N(R.sup.20)--C(.dbd.O)--O--R.sup.17, --N(R.sup.20)--C(.dbd.O)--R.sup.17, --N(R.sup.20)--C(.dbd.O)--NH--R.sup.17, --N(R.sup.20)SO.sub.2 --R.sup.17, or --N(R.sup.20)SO.sub.2 --NR.sup.20 R.sup.17 ; R.sup.17 is selected from: C.sub.1 -C.sub.10 alkyl, C.sub.3 -C.sub.11 cycloalkyl, aryl(C.sub.1 -C.sub.6 alkyl)-, (C.sub.1 -C.sub.6 alkyl)aryl, heteroaryl(C.sub.1 -C.sub.6 alkyl)-, (C.sub.1 -C.sub.6 alkyl)heteroaryl, biaryl(C.sub.1 -C.sub.6 alkyl)-, heteroaryl, or aryl, wherein said aryl or heteroaryl groups are optionally substituted with 0-3 substituents selected from the group consisting of: C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, aryl, heteroaryl, halo,cyano, amino, CF.sub.3, and NO.sub.2 ; R.sup.18 is selected from: H, --C(.dbd.O)--O--R.sup.17, --C(.dbd.O)--R.sup.17, --C(.dbd.O)--NH--R.sup.17, --SO.sub.2 --R.sup.17, or --SO.sub.2 --NR.sup.20 R.sup.17 ; R.sup.19 is selected from hydroxy, C.sub.1 -C.sub.10 alkyloxy, C.sub.3 -C.sub.11 cycloalkyloxy, aryloxy, aryl(C.sub.1 -C.sub.6 alkoxy)-, C.sub.3 -C.sub.10 alkylcarbonyloxyalkyloxy, C.sub.3 -C.sub.10 alkoxycarbonyloxyalkyloxy, C.sub.2 -C.sub.10 alkoxycarbonylalkyloxy, C.sub.5 -C.sub.10 cycloalkylcarbonyloxyalkyloxy, C.sub.5 -C.sub.10 cycloalkoxycarbonyloxyalkyloxy, C.sub.5 -C.sub.10 cycloalkoxycarbonylalkyloxy, C.sub.7 -C.sub.11 aryloxycarbonylalkyloxy, C.sub.8 -C.sub.12 aryloxycarbonyloxyalkyloxy, C.sub.8 -C.sub.12 arylcarbonyloxyalkyloxy, C.sub.5 -C.sub.10 alkoxyalkylcarbonyloxyalkyloxy, C.sub.5 -C.sub.10 (5-alkyl-1,3-dioxa-cyclopenten-2-one-yl)methyloxy, C.sub.10 -C.sub.14 (5-aryl-1,3-dioxa-cyclopenten-2-one-yl)methyloxy, or (R.sup.11)(R.sup.12)N-(C.sub.1 -C.sub.10 alkoxy)-; R.sup.20 is selected from: H, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.4 -C.sub.11 cycloalkylalkyl, aryl, aryl(C.sub.1 -C.sub.6 alkyl)-, or heteroaryl(C.sub.1 -C.sub.6 alkyl)-; R.sup.21 is selected from COOH or NR.sup.6.sub.2 ; m is 0-4; n is 0-4; t is 0-4; p is 0-2; q is 0-2; and r is 0-2; with the following provisos: (1) t, n, m and q are chosen such that the number of atoms connecting R.sup.1 and Y is in the range of 10-14; and (2) n and m are chosen such that the value of n plus m is greater than one unless U is --(CH.sub.2).sub.n Q(CH.sub.2).sub.m --.

�7! Preferred compounds of the invention as described above are compounds of the Formula Ib: ##STR22## including stereoisomeric forms thereof, or mixtures of stereoisomeric forms thereof, or pharmaceutically acceptable salt or prodrug forms thereof, wherein:

X.sup.1, X.sup.2, X.sup.3, and X.sup.4 are independently selected from nitrogen or carbon provided that at least two of X.sup.1, X.sup.2, X.sup.3 and X.sup.4 are carbon; R.sup.1 is selected from: ##STR23## A and B are independently --CH.sub.2 --, --O--, --N(R.sup.2)--, or --C(.dbd.O)--; A.sup.1 and B.sup.1 are independently --CH.sub.2 -- or --N(R.sup.3)--; D is --N(R.sup.2)--, --O--, --S--, --C(.dbd.O)-- or --SO.sub.2 --; E--F is --C(R.sup.4) .dbd.C(R.sup.5)--, -N.dbd.C(R.sup.4)--, --C(R.sup.4).dbd.N--, or --C(R.sup.4).sub.2 C(R.sup.5).sub.2 --; J, K, L and M are independently selected from --C(R.sup.4)--, --C(R.sup.5)-- or --N--, provided that at least one of J, K, L and M is not --N--; R.sup.2 is selected from: H, C.sub.1 -C.sub.6 alkyl, (C.sub.1 -C.sub.6 alkyl)carbonyl, (C.sub.1 -C.sub.6 alkoxy)carbonyl, C.sub.1 -C.sub.6 alkylaminocarbonyl, C.sub.3 -C.sub.6 alkenyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.4 -C.sub.11 cycloalkylalkyl, aryl, heteroaryl(C.sub.1 -C.sub.6 alkyl)carbonyl, heteroarylcarbonyl, aryl(C.sub.1 -C.sub.6 alkyl)-, (C.sub.1 -C.sub.6 alkyl)carbonyl, arylcarbonyl, alkylsulfonyl, arylsulfonyl, aryl(C.sub.1 -C.sub.6 alkyl)sulfonyl, heteroarylsulfonyl, heteroaryl(C.sub.1 -C.sub.6 alkyl)sulfonyl, aryloxycarbonyl, aryl(C.sub.1 -C.sub.6 alkoxy)carbonyl, wherein said aryl groups are substituted with 0-2 substituents selected from the group consisting of C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, halo, CF.sub.3, and nitro; R.sup.3 is selected from: H, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.4 -C.sub.11 cycloalkylalkyl, aryl, aryl(C.sub.1 -C.sub.6 alkyl)-, or heteroaryl(C.sub.1 -C.sub.6 alkyl)-; R.sup.4 and R.sup.5 are independently selected from: H, C.sub.1 -C.sub.4 alkoxy, NR.sup.2 R.sup.3, halogen, NO.sub.2, CN, CF.sub.3, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 alkenyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.4 -C.sub.11 cycloalkylalkyl, aryl, aryl(C.sub.1 -C.sub.6 alkyl)-, C.sub.2 -C.sub.7 alkylcarbonyl, arylcarbonyl or alternatively, when substituents on adjacent atoms, R.sup.4 and R.sup.5 can be taken together with the carbon atoms to which they are attached to form a 5-7 membered carbocyclic or 5-7 membered heterocyclic aromatic or non-aromatic ring system, said carbocyclic or heterocyclic ring being optionally substituted with 0-2 groups selected from: C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, halo, cyano, amino, CF.sub.3, or NO.sub.2 ; U is selected from: --(CH.sub.2).sub.n --, --(CH.sub.2).sub.n (CR.sup.7 .dbd.CR.sup.8)(CH.sub.2).sub.m -- --(CH.sub.2).sub.t Q(CH.sub.2).sub.m --, --(CH.sub.2).sub.n O(CH.sub.2).sub.m --, --(CH.sub.2).sub.n N(R.sup.6)(CH.sub.2).sub.m --, --(CH.sub.2).sub.n C(.dbd.O)(CH.sub.2).sub.m --, or --(CH.sub.2).sub.n S(O).sub.p (CH.sub.2).sub.m --; wherein one of the methylene groups is optionally substituted with R.sup.7 ; Q is selected from 1,2-phenylene, 1,3-phenylene, 2,3-pyridinylene, 3,4-pyridinylene, or 2,4-pyridinylene; R.sup.6 is selected from: H, C.sub.1 -C.sub.4 alkyl, or benzyl; R.sup.7 and R.sup.8 are independently selected from: H, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.4 -C.sub.11 cycloalkylalkyl, aryl, aryl(C.sub.1 -C.sub.6 alkyl)-, or heteroaryl(C.sub.0 -C.sub.6 alkyl)-; R.sup.9 is selected from: H, CO.sub.2 R.sup.17, C(.dbd.O)R.sup.17, CONR.sup.17 R.sup.20, --SO.sub.2 R.sup.17, --SO.sub.2 NR.sup.17 R.sup.20, C.sub.1 -C.sub.6 alkyl substituted with 0-1 R.sup.15 or 0-1 R.sup.21, C.sub.3 -C.sub.6 alkenyl substituted with 0-1 R.sup.15 or 0-1 R.sup.21, C.sub.3 -C.sub.7 cycloalkyl substituted with 0-1 R.sup.15 or 0-1 R.sup.21, C.sub.4 -C.sub.11 cycloalkylalkyl substituted with 0-1 R.sup.15 or 0-1 R.sup.21 aryl substituted with 0-1 R.sup.15 or 0-2 R.sup.11 or 0-1 R.sup.21, or aryl(C.sub.1 -C.sub.6 alkyl)substituted with 0-1 R.sup.15 or 0-2 R.sup.11 or 0-1 R.sup.21 ; R.sup.11 is selected from: H, halogen, CF.sub.3, CN, NO.sub.2, hydroxy, NR.sup.2 R.sup.3, C.sub.1 -C.sub.4 alkyl substituted with 0-1 R.sup.21, C.sub.1 -C.sub.4 alkoxy substituted with 0-1 R.sup.21, aryl substituted with 0-1 R.sup.21 aryl(C.sub.1 -C.sub.6 alkyl)-substituted with 0-1 R.sup.21, (C.sub.1 -C.sub.4 alkoxy)carbonyl substituted with 0-1 R.sup.21, (C.sub.1 -C.sub.4 alkyl)carbonyl substituted with 0-1 R.sup.21, C.sub.1 -C.sub.4 alkylsulfonyl substituted with 0-1 R.sup.21, or C.sub.1 -C.sub.4 alkylaminosulfonyl substituted with 0-1 R.sup.21 ; W is --C(.dbd.O)--N(R.sup.13)--(C(R.sup.12).sub.2).sub.q --; X is --C (R.sup.12)(R.sup.14)--C (R.sup.12)(R.sup.15)--; alternatively, W and X can be taken together to be ##STR24## R.sup.12 is H or C.sub.1 -C.sub.6 alkyl; R.sup.13 is selected from: H, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.7 cycloalkylmethyl, or aryl(C.sub.1 -C.sub.6 alkyl)-; R.sup.14 is selected from: H, C.sub.1 -C.sub.6 alkylthioalkyl, aryl(C.sub.1 -C.sub.10 alkylthioalkyl)-, aryl(C.sub.1 -C.sub.10 alkoxyalkyl)-, C.sub.1 -C.sub.10 alkyl, C.sub.1 -C.sub.10 alkoxyalkyl, C.sub.1 -C.sub.6 hydroxyalkyl, C.sub.2 -C.sub.10 alkenyl, C.sub.2 -C.sub.10 alkynyl, C.sub.3 -C.sub.10 cycloalkyl, C.sub.3 -C.sub.10 cycloalkylalkyl, aryl(C.sub.0 -C.sub.6 alkyl)-, heteroaryl(C.sub.1 -C.sub.6 alkyl)-, aryl, heteroaryl, CO.sub.2 R.sup.17, C(.dbd.O)R.sup.17 or CONR.sup.17 R.sup.20, provided that any of the above alkyl, cycloalkyl, aryl or heteroaryl groups may be unsubstituted or substituted independently with 0-1 R.sup.16 or 0-2 R.sup.11 ; R.sup.15 is selected from:

H, R.sup.16, C.sub.1 -C.sub.10 alkyl, C.sub.1 -C.sub.10 alkoxyalkyl, C.sub.1 -C.sub.10 alkylaminoalkyl, C.sub.1 -C.sub.10 dialkylaminoalkyl, C.sub.1 -C.sub.10 alkylcarbonyl, aryl(C.sub.0 -C.sub.6 alkyl)carbonyl, C.sub.2 -C.sub.10 alkenyl, C.sub.2 -C.sub.10 alkynyl ,C.sub.3 -C.sub.10 cycloalkyl, C.sub.3 -C.sub.10 cycloalkylalkyl, aryl(C.sub.1 -C.sub.6 alkyl)-, heteroaryl(C.sub.1 -C.sub.6 alkyl)-, aryl, heteroaryl, CO.sub.2 R.sup.17, C(.dbd.O)R.sup.17, CONR.sup.17 R.sup.20, SO.sub.2 R.sup.17, or SO.sub.2 NR.sup.17 R.sup.20, provided that any of the above alkyl, cycloalkyl, aryl or heteroaryl groups may be unsubstituted or substituted independently with 0-2 R.sup.11 ;

Y is selected from: ##STR25## R.sup.16 is selected from: --N(R.sup.20)--C(.dbd.O)--O--R.sup.17, --N(R.sup.20)--C(.dbd.O)--R.sup.17, --N(R.sup.20)--C(.dbd.O)--NH--R.sup.17, --N(R.sup.20)SO.sub.2 --R.sup.17 or --N(R.sup.20)SO.sub.2 --NR.sup.20 R.sup.17 ; R.sup.17 is selected from: C.sub.1 -C.sub.10 alkyl, C.sub.3 -C.sub.11 cycloalkyl, aryl(C.sub.1 -C.sub.6 alkyl)-, (C.sub.1 -C.sub.6 alkyl)aryl, heteroaryl(C.sub.1 -C.sub.6 alkyl)-, (C.sub.1 -C.sub.6 alkyl)heteroaryl, biaryl(C.sub.0 -C.sub.6 alkyl)-, heteroaryl, or aryl, wherein said aryl or heteroaryl groups are optionally substituted with 0-3 substituents selected from the group consisting of: C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, aryl, heteroaryl, halo,cyano, amino, CF.sub.3, and NO.sub.2 ; R.sup.18 is selected from: H, --C(.dbd.O)--O--R.sup.17, --C(.dbd.O)--R.sup.17, --C(.dbd.O)--NH--R.sup.17, --SO.sub.2 --R.sup.17, or --SO.sub.2 --NR.sup.20 R.sup.17 ; R.sup.19 is selected from hydroxy, C.sub.1 -C.sub.10 alkyloxy, C.sub.3 -C.sub.11 cycloalkyloxy, C.sub.6 -C.sub.10 aryloxy, C.sub.7 -C.sub.11 aralkyloxy, C.sub.3 -C.sub.10 alkylcarbonyloxyalkyloxy, C.sub.3 -C.sub.10 alkoxycarbonyloxyalkyloxy, C.sub.2 -C.sub.10 alkoxycarbonylalkyloxy, C.sub.5 -C.sub.10 cycloalkylcarbonyloxyalkyloxy, C.sub.5 -C.sub.10 cycloalkoxycarbonyloxyalkyloxy, C.sub.5 -C.sub.10 cycloalkoxycarbonylalkyloxy, C.sub.7 -C.sub.11 aryloxycarbonylalkyloxy, C.sub.8 -C.sub.12 aryloxycarbonyloxyalkyloxy, C.sub.8 -C.sub.12 arylcarbonyloxyalkyloxy, C.sub.5 -C.sub.10 alkoxyalkylcarbonyloxyalkyloxy, C.sub.5 -C.sub.10 (5-alkyl-1,3-dioxa-cyclopenten-2-one-yl)methyloxy, C.sub.10 -C.sub.14 (5-aryl-1,3-dioxa-cyclopenten-2-one-yl)methyloxy, or (R.sup.11)(R.sup.12)N--(C.sub.1 -C.sub.10 alkoxy)-; R.sup.20 selected from: H, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.4 -C.sub.11 cycloalkylalkyl, aryl(C.sub.1 -C.sub.6 alkyl)-, or heteroaryl(C.sub.1 -C.sub.6 alkyl)-; R.sup.21 is selected from COOH or NR.sup.6.sub.2 ; m is 0-4; n is 0-4; t is 0-4; p is 0-2; q is 0-2; and r is 0-2.

�8! Further preferred compounds of the invention as described above are compounds of the Formula IIc or IId: ##STR26## including stereoisomeric forms thereof, or mixtures of stereoisomeric forms thereof, or pharmaceutically acceptable salt or prodrug forms thereof, wherein:

X.sup.1 and X.sub.3 are independently selected from nitrogen or carbon; R.sup.1 is selected from: ##STR27## wherein the above heterocycles are optionally substituted with 0-2 substituents selected from the group consisting of: NH.sub.2, halogen, NO.sub.2, CN, CF.sub.3, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.6 alkyl, and C.sub.3 -C.sub.7 cycloalkyl; U is --(CH.sub.2).sub.n --, --(CH.sub.2).sub.t Q(CH.sub.2).sub.m -- or --C(.dbd.O)(CH.sub.2).sub.n-1 --, wherein one of the methylene groups is optionally substituted with R.sup.7 ; Q is selected from 1,2-phenylene, 1,3-phenylene, 2,3-pyridinylene, 3,4-pyrdinylene, or 2,4-pyridinylene; R.sup.6 is selected from: H, C.sub.1 -C.sub.4 alkyl, or benzyl; R.sup.7 is selected from: C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.4 -C.sub.11 cycloalkylalkyl, aryl, aryl(C.sub.1 -C.sub.6 alkyl), heteroaryl, or heteroaryl(C.sub.1 -C.sub.6 alkyl); R.sup.9 is selected from: H, --SO.sub.2 R.sup.17, --SO.sub.2 NR.sup.17 R.sup.20, C.sub.1 -C.sub.6 alkyl substituted with 0-1 R.sup.15 or 0-1 R.sup.21, C.sub.3 -C.sub.7 cycloalkyl substituted with 0-1 R.sup.15 or 0-1 R.sup.21, C.sub.4 -C.sub.11 cycloalkylalkyl substituted with 0-1 R.sup.15 or 0-1 R.sup.21, aryl substituted with 0-1 R.sup.15 or 0-2 R.sup.1 l or 0-1 R.sup.21, or aryl(C.sub.1 -C.sub.6 alkyl)-substituted with 0-1 R.sup.15 or 0-2 R.sup.11 or 0-1 R.sup.21 ; R.sup.11 is selected from: H, halogen, CF.sub.3, CN, NO.sub.2, hydroxy, NR.sup.2 R.sup.3, C.sub.1 -C.sub.4 alkyl substituted with 0-1 R.sup.21, C.sub.1 -C.sub.4 alkoxy substituted with 0-1 R.sup.21, aryl substituted with 0-1 R.sup.21, aryl(C.sub.1 -C.sub.6 alkyl)-substituted with 0-1 R.sup.21 (C.sub.1 -C.sub.4 alkoxy)carbonyl substituted with 0-1 R.sup.21 (C.sub.1 -C.sub.4 alkyl)carbonyl substituted with 0-1 R.sup.21, C.sub.1 -C.sub.4 alkylsulfonyl substituted with 0-1 R.sup.21, or C.sub.1 -C.sub.4 alkylaminosulfonyl substituted with 0-1 R.sup.21 ; W is --C(.dbd.O)--N(R.sup.13)--; X is --CH(R.sup.14)--CH(R.sup.15)--; R.sup.13 is H or CH.sub.3 ; R.sup.14 is selected from: H, C.sub.1 -C.sub.10 alkyl, aryl, or heteroaryl, wherein said aryl or heteroaryl groups are optionally substituted with 0-3 substituents selected from the group consisting of: C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, aryl, halo, cyano, amino, CF.sub.3, and NO.sub.2 ; R.sup.15 is H or R.sup.16 ; Y is --COR.sup.19 ; R.sup.16 is selected from: --NH(R.sup.20)--C(.dbd.O)--O--R.sup.17, --N(R.sup.20)--C(.dbd.O)--R.sup.17, --N(R.sup.20)--C(.dbd.O)--NH--R.sup.17, --N(R.sup.20)SO.sub.2 --R.sup.17, or --N(R.sup.20)SO.sub.2 --N(R.sup.20)R.sup.17 ; R.sup.17 is selected from: C.sub.1 -C.sub.10 alkyl, C.sub.3 -C.sub.11 cycloalkyl, aryl(C.sub.1 -C.sub.6 alkyl)-, (C.sub.1 -C.sub.6 alkyl)aryl, heteroaryl(C.sub.1 -C.sub.6 alkyl)-, (C.sub.1 -C.sub.6 alkyl)heteroaryl, biaryl(C.sub.1 -C.sub.6 alkyl)-, heteroaryl, or aryl, wherein said aryl or heteroaryl groups are optionally substituted with 0-3 substituents selected from the group consisting of: C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, aryl, heteroaryl, halo, cyano, amino, CF.sub.3, and NO.sub.2 ; R.sup.19 is selected from: hydroxy, C.sub.1 -C.sub.10 alkoxy, methylcarbonyloxymethoxy-, ethylcarbonyloxymethoxy-, t-butylcarbonyloxymethoxy-, cyclohexylcarbonyloxymethoxy-, 1-(methylcarbonyloxy)ethoxy-, 1-(ethylcarbonyloxy)ethoxy-, 1-(t-butylcarbonyloxy)ethoxy-, 1-(cyclohexylcarbonyloxy)ethoxy-, i-propyloxycarbonyloxymethoxy-, t-butyloxycarbonyloxymethoxy-, 1-(i-propyloxycarbonyloxy)ethoxy-, 1-(cyclohexyloxycarbonyloxy)ethoxy-, 1-(t-butyloxycarbonyloxy)ethoxy-, dimethylaminoethoxy-, diethylaminoethoxy-, (5-methyl-1,3-dioxacyclopenten-2-on-4-yl)methoxy-, (5-(t-butyl)-1,3-dioxacyclopenten-2-on-4-yl)methoxy-, (1,3-dioxa-5-phenyl-cyclopenten-2-on-4-yl)methoxy-, or 1-(2-(2-methoxypropyl)carbonyloxy)ethoxy-; R.sup.20 is H or CH.sub.3 ; R.sup.21 is selected from COOH or NR.sup.6.sub.2 ; and m is 0 or 1; n is 1-4; and t is 0 or 1.

�9! Still further preferred compounds of the above invention are compounds of the Formula IIc or IId: ##STR28## including stereoisomeric forms thereof, or mixtures of stereoisomeric forms thereof, or pharmaceutically acceptable salt or prodrug forms thereof, wherein:

X.sub.1 and X.sub.3 are independently selected from nitrogen or carbon, provided that at least one of X.sub.1 and X.sub.3 is carbon; R.sup.1 is selected from: ##STR29## wherein the above heterocycles are optionally substituted with 0-2 substituents selected from the group consisting of: NH.sub.2, halogen, NO.sub.2, CN, CF.sub.3, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.6 alkyl and C.sub.3 -C.sub.7 cycloalkyl: U is --(CH.sub.2).sub.n --, --(CH.sub.2).sub.t Q (CH.sub.2).sub.m -- or --C(.dbd.O)(CH.sub.2).sub.n-1 --, wherein one of the methylene groups is optionally substituted with R.sup.7 ; Q is selected from 1,2-phenylene, 1,3-phenylene, 2,3-pyridinylene, 3,4-pyridinylene, or 2,4-pyridinylene; R.sup.6 is selected from: H, C.sub.1 -C.sub.4 alkyl, or benzyl; R7 is selected from: C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.4 -C.sub.11 cycloalkylalkyl, aryl, aryl(C.sub.1 -C.sub.6 alkyl), heteroaryl, or heteroaryl(C.sub.1 -C.sub.6 alkyl); R.sup.9 is selected from: H, --SO.sub.2 R.sup.17, --SO.sub.2 NR.sup.17 R.sup.20, C.sub.1 -C.sub.6 alkyl substituted with 0-1 R.sup.15 or 0-1 R.sup.21, C.sub.3 -C.sub.7 cycloalkyl substituted with 0-1 R.sup.15 or 0-1 R.sup.21, C.sub.4 -C.sub.11 cycloalkylalkyl substituted with 0-1 R.sup.15 or 0-1 R.sup.21, aryl substituted with 0-1 R.sup.15 or 0-2 R.sup.11 or 0-1 R.sup.21, or aryl(C.sub.1 -C.sub.6 alkyl)-substituted with 0-1 R.sup.15 or 0-2 R.sup.11 or 0-1 R.sup.21 ; R.sup.11 is selected from H, halogen, CF.sub.3, CN, NO.sub.2, hydroxy, NR.sup.2 R.sup.3, C.sub.1 -C.sub.4 alkyl substituted with 0-1 R.sup.21, C.sub.1 -C.sub.4 alkoxy substituted with 0-1 R.sup.21, aryl substituted with 0-1 R.sup.21, aryl(C.sub.1 -C.sub.6 alkyl)-substituted with 0-1 R.sup.21, (C.sub.1 -C.sub.4 alkoxy)carbonyl substituted with 0-1 R.sup.21, (C.sub.1 -C.sub.4 alkyl)carbonyl substituted with 0-1 R.sup.21, C.sub.1 -C.sub.4 alkylsulfonyl substituted with 0-1 R.sup.21, or C.sub.1 -C.sub.4 alkylaminosulfonyl substituted with 0-1 R.sup.21 ; W is --C(.dbd.O)--N(R.sup.13)--; W is --C(.dbd.O)--N(R.sup.13)--; X is --CH(R.sup.14)--CH(R.sup.15)--; R.sup.13 is H or CH.sub.3 ; R.sup.14 is selected from: H, C.sub.1 -C.sub.10 alkyl, aryl, or heteroaryl, wherein said aryl or heteroaryl groups are optionally substituted with 0-3 substituents selected from the group consisting of: C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, aryl, halo, cyano, amino, CF.sub.3, and NO.sub.2 ; R.sup.15 is H or R.sup.16 ; Y is --COR.sup.19 ; R.sup.16 is selected from: --N(R.sup.20)--C(.dbd.O)--O--R.sup.17, --N(R.sup.20)--C(.dbd.O)--R.sup.17, --N(R.sup.20)--C(.dbd.O)--NH--R.sup.17, --N(R.sup.20)SO.sub.2 --R.sup.17, or --N(R.sup.20)SO.sub.2 --NR.sup.20 R.sup.17 ; R.sup.17 is selected from: C.sub.1 -C.sub.10 alkyl, C.sub.3 -C.sub.11 cycloalkyl, aryl(C.sub.1 -C.sub.6 alkyl)-, (C.sub.1 -C.sub.6 alkyl)aryl, heteroaryl(C.sub.1 -C.sub.6 alkyl)-, (C.sub.1 -C.sub.6 alkyl)heteroaryl, biaryl(C.sub.1 -C.sub.6 alkyl)-, heteroaryl, or aryl, wherein said aryl or heteroaryl groups are optionally substituted with 0-3 substituents selected from the group consisting of: C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, aryl, heteroaryl, halo, cyano, amino, CF.sub.3, and NO.sub.2 ; R.sup.19 is selected from: hydroxy, C.sub.1 -C.sub.10 alkoxy, methylcarbonyloxymethoxy-, ethylcarbonyloxymethoxy-, t-butylcarbonyloxymethoxy-, cyclohexylcarbonyloxymethoxy-, 1-(methylcarbonyloxy)ethoxy-, 1-(ethylcarbonyloxy)ethoxy-, 1-(t-butylcarbonyloxy)ethoxy-, 1-(cyclohexylcarbonyloxy)ethoxy-, i-propyloxycarbonyloxymethoxy-, t-butyloxycarbonyloxymethoxy-, 1-(i-propyloxycarbonyloxy)ethoxy-, 1-(cyclohexyloxycarbonyloxy)ethoxy-, 1-(t-butyloxycarbonyloxy)ethoxy-, dimethylaminoethoxy-, diethylaminoethoxy-, (5-methyl-1,3-dioxacyclopenten-2-on-4-yl)methoxy-, (5-(t-butyl)-1,3-dioxacyclopenten-2-on-4-yl)methoxy-, (1,3-dioxa-5-phenyl-cyclopenten-2-on-4-yl)methoxy-, or 1-(2-(2-methoxypropyl)carbonyloxy)ethoxy-; R.sup.20 is H or CH.sub.3 ; R.sup.21 is selected from COOH or NR.sup.6.sub.2 ; and m is 0 or 1; n is 1-4; and t is 0 or 1.

�10! Specifically preferred compounds of the invention as described above are compounds of Formula Ib, including enantiomeric or diasteriomeric forms thereof, or mixtures of enantiomeric or diasteriomeric forms thereof, or pharmaceutically acceptable salt or prodrug forms thereof, selected from the group consisting of:

3-�3-�3-(imidazolin-2-ylamino)propyl!indazol-6-ylcarbonylamino!-2-(benzyloxycarbonylamino)propionic acid, 3-�1-methyl-3-�3-(imidazolin-2-ylamino)propyl!-indazol-6-ylcarbonylamino!-2-(2,4,6-trimethylbenzenesulfonylamino)propionic acid, 3-�3-�3-(imidazolin-2-ylamino)propyl!indazol-6-ylcarbonylamino!-2-(benzenesulfonylamino)propionic acid, 3-�1-methyl-3-�3-(imidazolin-2-ylamino)propyl!indazol-6-ylcarbonylamino!-2-(2,6-dichlorobenzenesulfonylamino)propionic acid, 3-�3-�3-(imidazolin-2-ylamino)propyl!indazol-6-ylcarbonylamino!-2-(3,5-dimethylisoxazol-4-ylsulfonylamino)propionic acid, 3-�1-methyl-3-�3-(imidazolin-2-ylamino)propyl!indazol-6-ylcarbonylamino!-2-(2,6-dimethylbenzenesulfonylamino)propionic acid, 3-�3-�3-(imidazolin-2-ylamino)propyl!indazol-6-ylcarbonylamino!-2-(2,6-dimethyl-4-phenylbenzenesulfonylamino)propionic acid, 3-�1-methyl-3-�3-(imidazolin-2-ylamino)propyl!indazol-6-ylcarbonylamino!-2-(4-phenylbenzenesulfonylamino)propionic acid, 3-�3-�3-(tetrahydropyrimid-2-ylamino)propyl!indazol-6-ylcarbonylamino!-2-(benzyloxycarbonylamino)propionic acid, 3-�1-methyl-3-�3-(tetrahydropyrimid-2-ylamino)propyl!indazol-6-ylcarbonylamino!-2-(2,4,6-trimethylbenzenesulfonylamino)propionic acid, 3-�3-�3-(tetrahydropyrimid-2-ylamino)propyl!indazol-6-ylcarbonylamino!-2-(benzenesulfonylamino)propionic acid, 3-�1-methyl-3-�3-(tetrahydropyrimid-2-ylamino)propyl!indazol-6-ylcarbonylamino!-2-(2,6-dichlorobenzenesulfonylamino)propionic acid, 3-�3-�3-(tetrahydropyrimid-2-ylamino)propyl!indazol-6-ylcarbonylamino!-2-(3,5-dimethylisoxazol-4-ylsulfonylamino)propionic acid, 3-�1-methyl-3-�3-(tetrahydropyrimid-2-ylamino)propyl!indazol-6-ylcarbonylamino!-2-(2,6-dimethylbenzenesulfonylamino)propionic acid, 3-�3-�3-(tetrahydropyrimid-2-ylamino)propyl!indazol-6-ylcarbonylamino!-2-(2,6-dimethyl-4-phenylbenzenesulfonylamino)propionic acid, 3-�1-methyl-3-�3-(tetrahydropyrimid-2-ylamino)propyl!-indazol-6-ylcarbonylamino!-2-(4-phenylbenzenesulfonylamino)propionic acid, 3-�3-�3-(imidazol-2-ylamino)propyl!indazol-6-ylcarbonylamino!-2-(benzyloxycarbonylamino)propionic acid, 3-�1-methyl-3-�3-(imidazol-2-ylamino)propyl!indazol-6-ylcarbonylamino!-2-(2,4,6-trimethylbenzenesulfonylamino)propionic acid, 3-�3-�3-(imidazol-2-ylamino)propyl!indazol-6-ylcarbonylamino!-2-(benzenesulfonylamino)propionic acid, 3-�1-methyl-3-�3-(imidazol-2-ylamino)propyl!indazol-6-ylcarbonylamino!-2-(2,6-dichlorobenzenesulfonylamino)propionic acid, 3-�3-�3-(imidazol-2-ylamino)propyl!indazol-6-ylcarbonylamino!-2-(3,5-dimethylisoxazol-4-ylsulfonylamino)propionic acid, 3-�1-methyl-3-�3-(imidazol-2-ylamino)propyl!indazol-6-ylcarbonylamino!-2-(2,6-dimethylbenzenesulfonylamino)propionic acid, 3-�3-�3-(imidazol-2-ylamino)propyl!indazol-6-ylcarbonylamino!-2-(2,6-dimethyl-4-phenylbenzenesulfonylamino)propionic acid, 3-�1-methyl-3-�3-(imidazol-2-ylamino)propyl!indazol-6-ylcarbonylamino!-2-(4-phenylbenzenesulfonylamino)propionic acid, 3-�3-�3-(pyridin-2-ylamino)propyl!indazol-6-ylcarbonylamino!-2-(benzyloxycarbonylamino)propionic acid, 3-�1-methyl-3-�3-(pyridin-2-ylamino)propyl!indazol-6-ylcarbonylamino!-2-(2,4,6-trimethylbenzenesulfonylamino)propionic acid, 3-�3-�3-(pyridin-2-ylamino)propyl!indazol-6-ylcarbonylamino!-2-(benzenesulfonylamino)propionic acid, 3-�1-methyl-3-�3-(pyridin-2-ylamino)propyl!indazol-6-ylcarbonylamino!-2-(2,6-dichlorobenzenesulfonylamino)propionic acid, 3-�3-�3-(pyridin-2-ylamino)propyl!indazol-6-ylcarbonylamino!-2-(3,5-dimethylisoxazol-4-ylsulfonylamino)propionic acid, 3-�1-methyl-3-�3-(pyridin-2-ylamino)propyl!indazol-6-ylcarbonylamino!-2-(2,6-dimethylbenzenesulfonylamino)propionic acid, 3-�3-�3-(pyridin-2-ylamino)propyl!indazol-6-ylcarbonylamino!-2-(2,6-dimethyl-4-phenylbenzenesulfonylamino)propionic acid, 3-�1-methyl-3-�3-(pyridin-2-ylamino)propyl!indazol-6-ylcarbonylamino!-2-(4-phenylbenzenesulfonylamino)propionic acid, 3-�3-�3-(imidazolin-2-ylamino)propyl!indazol-7-ylcarbonylamino!-2-(benzyloxycarbonylamino)propionic acid, 3-�1-methyl-3-�3-(imidazolin-2-ylamino)propyl!indazol-7-ylcarbonylamino!-2-(2,4,6-trimethylbenzenesulfonylamino)propionic acid, 3-�3-�3-(imidazolin-2-ylamino)propyl!indazol-7-ylcarbonylamino!-2-(benzenesulfonylamino)propionic acid, 3-�1-methyl-3-�3-(imidazolin-2-ylamino)propyl!indazol-7-ylcarbonylamino!-2-(2,6-dichlorobenzenesulfonylamino)propionic acid, 3-�3-�3-(imidazolin-2-ylamino)propyl!indazol-7-ylcarbonylamino!-2-(3,5-dimethylisoxazol-4-ylsulfonylamino)propionic acid, 3-�1-methyl-3-�3-(imidazolin-2-ylamino)propyl!indazol-7-ylcarbonylamino!-2-(2,6-dimethylbenzenesulfonylamino)propionic acid, 3-�3-�3-(imidazolin-2-ylamino)propyl!indazol-7-ylcarbonylamino!-2-(2,6-dimethyl-4-phenylbenzenesulfonylamino)propionic acid, 3-�1-methyl-3-�3-(imidazolin-2-ylamino)propyl!indazol-7-ylcarbonylamino!-2-(4-phenylbenzenesulfonylamino)propionic acid, 3-�3-�3-(tetrahydropyrimid-2-ylamino)propyl!indazol-7-ylcarbonylamino!-2-(benzyloxycarbonylamino)propionic acid, 3-�1-methyl-3-�3-(tetrahydropyrimid-2-ylamino)propyl!indazol-7-ylcarbonylamino!-2-(2,4,6-trimethylbenzenesulfonylamino)propionic acid, 3-�3-�3-(tetrahydropyrimid-2-ylamino)propyl!indazol-7-ylcarbonylamino!-2-(benzenesulfonylamino)propionic acid, 3-�1-methyl-3-�3-(tetrahydropyrimid-2-ylamino)propyl!indazol-7-ylcarbonylamino!-2-(2,6-dichlorobenzenesulfonylamino)propionic acid, 3-�3-�3-(tetrahydropyrimid-2-ylamino)propyl!indazol-7-ylcarbonylamino!-2-(3,5-dimethylisoxazol-4-ylsulfonylamino)propionic acid, 3-�1-methyl-3-�3-(tetrahydropyrimid-2-ylamino)propyl!indazol-7-ylcarbonylamino!-2-(2,6-dimethylbenzenesulfonylamino)propionic acid, 3-�3-�3-(tetrahydropyrimid-2-ylamino)propyl!indazol-7-ylcarbonylamino!-2-(2,6-dimethyl-4-phenylbenzenesulfonylamino)propionic acid, 3-�1-methyl-3-�3-(tetrahydropyrimid-2-ylamino)propyl!indazol-7-ylcarbonylamino!-2-(4-phenylbenzenesulfonylamino)propionic acid, 3-�3-�3-(imidazol-2-ylamino)propyl!indazol-7-ylcarbonylamino!-2-(benzyloxycarbonylamino)propionic acid, 3-�1-methyl-3-�3-(imidazol-2-ylamino)propyl!indazol-7-ylcarbonylamino!-2-(2,4,6-trimethylbenzenesulfonylamino)propionic acid, 3-�3-�3-(imidazol-2-ylamino)propyl!indazol-7-ylcarbonylamino!-2-(benzenesulfonylamino)propionic acid, 3-�1-methyl-3-�3-(imidazol-2-ylamino)propyl!indazol-7-ylcarbonylamino!-2-(2,6-dichlorobenzenesulfonylamino)propionic acid, 3-�3-�3-(imidazol-2-ylamino)propyl!indazol-7-ylcarbonylamino!-2-(3,5-dimethylisoxazol-4-ylsulfonylamino)propionic acid, 3-�1-methyl-3-�3-(imidazol-2-ylamino)propyl!indazol-7-ylcarbonylamino!-2-(2,6-dimethylbenzenesulfonylamino)propionic acid, 3-�3-�3-(imidazol-2-ylamino)propyl!indazol-7-ylcarbonylamino!-2-(2,6-dimethyl-4-phenylbenzenesulfonylamino)propionic acid, 3-�1-methyl-3-�3-(imidazol-2-ylamino)propyl!indazol-7-ylcarbonylamino!-2-(4-phenylbenzenesulfonylamino)propionic acid, 3-�3-�3-(pyridin-2-ylamino)propyl!indazol-7-ylcarbonylamino!-2-(benzyloxycarbonylamino)propionic acid, 3-�1-methyl-3-�3-(pyridin-2-ylamino)propyl!indazol-7-ylcarbonylamino!-2-(2,4,6-trimethylbenzenesulfonylamino)propionic acid, 3-�3-�3-(pyridin-2-ylamino)propyl!indazol-7-ylcarbonylamino!-2-(benzenesulfonylamino)propionic acid, 3-�1-methyl-3-�3-(pyridin-2-ylamino)propyl!indazol-7-ylcarbonylamino!-2-(2,6-dichlorobenzenesulfonylamino)propionic acid, 3-�3-�3-(pyridin-2-ylamino)propyl!indazol-7-ylcarbonylamino!-2-(3,5-dimethylisoxazol-4-ylsulfonylamino)propionic acid, 3-�1-methyl-3-�3-(pyridin-2-ylamino)propyl!indazol-7-ylcarbonylamino!-2-(2,6-dimethylbenzenesulfonylamino)propionic acid, 3-�3-�3-(pyridin-2-ylamino)propyl!indazol-7-ylcarbonylamino!-2-(2,6-dimethyl-4-phenylbenzenesulfonylamino)propionic acid, and 3-�1-methyl-3-�3-(pyridin-2-ylamino)propyl!indazol-7-ylcarbonylamino!-2-(4-phenylbenzenesulfonylamino)propionic acid.

�11! Also specifically preferred are ester prodrugs of the specifically preferred compounds of Formula Ib, said esters being chosen from the group consisting of:

methyl, ethyl, isopropyl, n-butyl, isobutyl, benzyl, methylcarbonyloxymethyl, ethylcarbonyloxymethyl, tert-butylcarbonyloxymethyl, cyclohexylcarbonyloxymethyl, tert-butyloxycarbonyloxymethyl, dimethylaminoethyl, and diethylaminoethyl, pyrroldinoethyl, and trimethylanimonioethyl.

�12! Yet another aspect of the present invention comprises compounds of Formula Ic: ##STR30## including stereoisomeric forms thereof, or mixtures of stereoisomeric forms thereof, or pharmaceutically acceptable salt or prodrug forms, thereof wherein:

X.sup.1, X.sup.2, X.sup.3, and X.sup.4 are independently selected from nitrogen or carbon provided that at least two of X.sub.1, X.sup.2, X.sup.3 and X.sup.4 are carbon; R.sup.1 is selected from: ##STR31## A and B are independently --CH.sub.2 --, --O--, --N(R.sup.2)--, or --C(.dbd.O)--; A.sup.1 and B.sup.1 are independently --CH.sub.2 -- or --N(R.sup.3)--; D is --N(R.sup.2)--, --O--, --S--, --C(.dbd.O)-- or --SO.sub.2 --; E--F is --C(R.sup.4).dbd.C(R.sup.5)--, --N.dbd.C(R.sup.4)--, --C(R.sup.4).dbd.N--, or --C(R.sup.4).sub.2 C(R.sup.5).sub.2 --; J, K, L and M are independently selected from --C(R.sup.4)--, --C(R.sup.5)-- or --N--, provided that at least one of J, K, L and M is not --N--; R.sup.2 is selected from: H, C.sub.1 -C.sub.6 alkyl, (C.sub.1 -C.sub.6 alkyl)carbonyl, (C.sub.1 -C.sub.6 alkoxy)carbonyl; (C.sub.1 -C.sub.6 alkyl)aminocarbonyl, C.sub.3 -C.sub.6 alkenyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.4 -C.sub.11 cycloalkylalkyl, aryl, heteroaryl(C.sub.1 -C.sub.6 alkyl)carbonyl, heteroarylcarbonyl, aryl C.sub.1 -C.sub.6 alkyl, (C.sub.1 -C.sub.6 alkyl)carbonyl, or arylcarbonyl, C.sub.1 -C.sub.6 alkylsulfonyl, arylsulfonyl aryl(C.sub.1 -C.sub.6 alkyl)sulfonyl, heteroarylsulfonyl, heteroaryl(C.sub.1 -C.sub.6 alkyl)sulfonyl, aryloxycarbonyl, or aryl(C.sub.1 -C.sub.6 alkoxy)carbonyl, wherein said aryl groups are substituted with 0-2 substituents selected from the group consisting of C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, halo, CF.sub.3, and nitro; R.sup.3 is selected from: H, C.sub.1 -C.sub.6 alkyl, C.sub.3-C.sub.7 cycloalkyl, C.sub.4 -C.sub.11 cycloalkylalkyl, aryl, aryl(C.sub.1 -C.sub.6 alkyl)-, or heteroaryl(C.sub.1 -C.sub.6 alkyl)-; R.sup.4 and R.sup.5 are independently selected from: H, C.sub.1 -C.sub.4 alkoxy, NR.sup.2 R.sup.3, halogen, NO.sub.2, CN, CF.sub.3, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 alkenyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.4 -C.sub.11 cycloalkylalkyl, aryl, aryl(C.sub.1 -C.sub.6 alkyl)-, (C.sub.1 -C.sub.6 alkyl)carbonyl, (C.sub.1 -C.sub.6 alkoxy)carbonyl, arylcarbonyl, or alternatively, when substituents on adjacent atoms, R.sup.4 and R.sup.5 can be taken together with the carbon atoms to which they are attached to form a 5-7 membered carbocyclic or 5-7 membered heterocyclic aromatic or non-aromatic ring system, said carbocyclic or heterocyclic ring being optionally substituted with 0-2 groups selected from: C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, halo, cyano, amino, CF.sub.3, or NO.sub.2 ; U is selected from: --(CH.sub.2).sub.n --, --(CH.sub.2).sub.n (CR.sup.7 .dbd.CR.sup.8)(CH.sub.2).sub.m -- --(CH.sub.2).sub.n (C.tbd.C)(CH.sub.2).sub.m -- --(CH.sub.2).sub.t Q(CH.sub.2).sub.m -- --(CH.sub.2).sub.n O(CH.sub.2).sub.m --, --(CH.sub.2).sub.n N(R.sup.6)(CH.sub.2).sub.m --, --(CH.sub.2).sub.n C(.dbd.O)(CH.sub.2).sub.m --, --(CH.sub.2).sub.n (C.dbd.O)N(R.sup.6)(CH.sub.2).sub.m -- --(CH.sub.2).sub.n N(R.sup.6)(C.dbd.O)(CH.sub.2).sub.m --, or --(CH.sub.2).sub.n S(O).sub.p (CH.sub.2).sub.m --; wherein one of the methylene groups is optionally substituted with R.sup.7 ; Q is selected from 1,2-cycloalkylene, 1,2-phenylene, 1,3-phenylene, 1,4-phenylene, 2,3-pyridinylene, 3,4-pyridinylene, 2,4-pyridinylene, or 3,4-pyridazinylene; R.sup.6 is selected from: H, C.sub.1 -C.sub.4 alkyl, or benzyl; R.sup.7 and R.sup.8 are independently selected from: H, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.4 -C.sub.11 cycloalkylalkyl, aryl, aryl(C.sub.1 -C.sub.6 alkyl)-, or heteroaryl(C.sub.0 -C.sub.6 alkyl)-; R.sup.9 is selected from: H, CO.sub.2 R.sup.17, C(.dbd.O)R.sup.17, CONR.sup.17 R.sup.20, --SO.sub.2 R.sup.17, --SO.sub.2 NR.sup.17 R.sup.20, C.sub.1 -C.sub.6 alkyl substituted with 0-1 R.sup.15 or 0-1 R.sup.21, C.sub.3 -C.sub.6 alkenyl substituted with 0-1 R.sup.15 or 0-1 R.sup.21, C.sub.3 -C.sub.7 cycloalkyl substituted with 0-1 R.sup.15 or 0-1 R.sup.21, C.sub.4 -C.sub.11 cycloalkylalkyl substituted with 0-1 R.sup.15 or 0-1 R.sup.21, aryl substituted with 0-1 R.sup.15 or 0-2 R.sup.11 or 0-1 R.sup.21, or aryl(C.sub.1 -C.sub.6 alkyl)-substituted with 0-1 R.sup.15 or 0-2 R.sup.11 or 0-1 R.sup.21 ; R.sup.11 is selected from H, halogen, CF.sub.3, CN, NO.sub.2, hydroxy, NR.sup.2 R.sup.3, C.sub.1 -C.sub.4 alkyl substituted with 0-1 R.sup.21, C.sub.1 -C.sub.4 alkoxy substituted with 0-1 R.sup.21, aryl substituted with 0-1 R.sup.21, aryl(C.sub.1 -C.sub.6 alkyl)-substituted with 0-1 R.sup.21, (C.sub.1 -C.sub.4 alkoxy)carbonyl substituted with 0-1 R.sup.21, (C.sub.1 -C.sub.4 alkyl)carbonyl substituted with 0-1 R.sup.21, C.sub.1 -C.sub.4 alkylsulfonyl substituted with 0-1 R.sup.21, or C.sub.1 -C.sub.4 alkylaminosulfonyl substituted with 0-1 R.sup.21 ; W is selected from: --(C(R.sup.12).sub.2).sub.q C(.dbd.O)N(R.sup.13)--, or --C(.dbd.O)--N(R.sup.13)--(C(R.sup.12).sub.2).sub.q --; X is --C(R.sup.12)(R.sup.14)--C(R.sup.12)(R.sup.15)--; or alternatively, W and X can be taken together to be ##STR32## R.sup.12 is selected from: H, halogen, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkynyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.4 -C.sub.10 cycloalkylalkyl, (C.sub.1 -C.sub.4 alkyl)carbonyl, aryl, or aryl(C.sub.1 -C.sub.6 alkyl)-; R.sup.13 is selected from: H, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.7 cycloalkylmethyl, or aryl(C.sub.1 -C.sub.6 alkyl) R.sup.14 is selected from: H, C.sub.1 -C.sub.6 alkylthio(C.sub.1 -C.sub.6 alkyl)-, aryl(C.sub.1 -C.sub.10 alkylthioalkyl)-, aryl(C.sub.1 -C.sub.10 alkoxyalkyl)-, C.sub.1 -C.sub.10 alkyl, C.sub.1 -C.sub.10 alkoxyalkyl, C.sub.1 -C.sub.6 hydroxyalkyl, C.sub.2 -C.sub.10 alkenyl, C.sub.2 -C.sub.10 alkynyl, C.sub.3 -C.sub.10 cycloalkyl, C.sub.3 -C.sub.10 cycloalkylalkyl, aryl(C.sub.1 -C.sub.6 alkyl)-, heteroaryl(C.sub.1 -C.sub.6 alkyl)-, aryl, heteroaryl, CO.sub.2 R.sup.17, C(.dbd.O)R.sup.17, or CONR.sup.17 R.sup.20, provided that any of the above alkyl, cycloalkyl, aryl or heteroaryl groups may be unsubstituted or substituted independently with 0-1 R.sup.16 or 0-2 R.sup.11 ; R.sup.15 is selected from: H, R.sup.16, C.sub.1 -C.sub.10 alkyl, C.sub.1 -C.sub.10 alkoxyalkyl, C.sub.1 -C.sub.10 alkylaminoalkyl, C.sub.1 -C.sub.10 dialkylaminoalkyl, (C.sub.1 -C.sub.10 alkyl)carbonyl, aryl(C.sub.0 -C.sub.6 alkyl)carbonyl, C.sub.1 -C.sub.10 alkenyl, C.sub.1 -C.sub.10 alkynyl, C.sub.3 -C.sub.10 cycloalkyl, C.sub.3 -C.sub.10 cycloalkylalkyl, aryl(C.sub.1 -C.sub.6 alkyl)-, heteroaryl(C.sub.1 -C.sub.6 alkyl)-, aryl, heteroaryl, CO.sub.2 R.sup.17, C(.dbd.O)R.sup.17, CONR.sup.17 R.sup.20, SO.sub.2 R.sup.17, or SO.sub.2 NR.sup.17 R.sup.20, provided that any of the above alkyl, cycloalkyl, aryl or heteroaryl groups may be unsubstituted or substituted independently with 0-2 R.sup.11 ; Y is selected from: --COR.sup.19, --SO.sub.3 H, --PO.sub.3 H, tetrazolyl, --CONHNHSO.sub.2 CF.sub.3, --CONHSO.sub.2 R.sup.17, --CONHSO.sub.2 NHR.sup.17, --NHCOCF.sub.3, --NHCONHSO.sub.2 R.sup.17, --NHSO.sub.2 R.sup.17, --OPO.sub.3 H.sub.2, --OSO.sub.3 H, --PO.sub.3 H.sub.2, --SO.sub.3 H, --SO.sub.2 NHCOR.sup.17, --SO.sub.2 NHCO.sub.2 R.sup.17, ##STR33## R.sup.16 is selected from: --N(R.sup.20)--C(.dbd.O)--O--R.sup.17, --N(R.sup.20)--C(.dbd.O)--R.sup.17, --N(R.sup.20)--C(.dbd.O)--NH--R.sup.17, --N(R.sup.20)SO.sub.2 --R.sup.17, or --N(R.sup.20)SO.sub.2 --NR.sup.20 R.sup.17 ; R.sup.17 is selected from: C.sub.1 -C.sub.10 alkyl, C.sub.3 -C.sub.11 cycloalkyl, aryl(C.sub.1 -C.sub.6 alkyl)-, (C.sub.1 -C.sub.6 alkyl)aryl, heteroaryl(C.sub.1 -C.sub.6 alkyl)-, (C.sub.1 -C.sub.6 alkyl)heteroaryl, biaryl(C.sub.1 -C.sub.6 alkyl)-, heteroaryl, or aryl, wherein said aryl or heteroaryl groups are optionally substituted with 0-3 substituents selected from the group consisting of: C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, aryl, heteroaryl, halo, cyano, amino, CF.sub.3, and NO.sub.2 ; R.sup.18 is selected from: H, --C(.dbd.O)--O--R.sup.17, --C(.dbd.O)--R.sup.17, --C(.dbd.O)--NH--R.sup.17, --SO.sub.2 --R.sup.17, or --SO.sub.2 --NR.sup.20 R.sup.17 ; R.sup.19 is selected from hydroxy, C.sub.1 -C.sub.10 alkyloxy, C.sub.3 -C.sub.11 cycloalkyloxy, aryloxy, aryl(C.sub.1 -C.sub.6 alkoxy)-, C.sub.3 -C.sub.10 alkylcarbonyloxyalkyloxy, C.sub.3 -C.sub.10 alkoxycarbonyloxyalkyloxy, C.sub.2 -C.sub.10 alkoxycarbonylalkyloxy, C.sub.5 -C.sub.10 cycloalkylcarbonyloxyalkyloxy, C.sub.5 -C.sub.10 cycloalkoxycarbonyloxyalkyloxy, C.sub.5 -C.sub.10 cycloalkoxycarbonylalkyloxy, C.sub.7 -C.sub.11 aryloxycarbonylalkyloxy, C.sub.8 -C.sub.12 aryloxycarbonyloxyalkyloxy, C.sub.8 -C.sub.12 arylcarbonyloxyalkyloxy, C.sub.5 -C.sub.10 alkoxyalkylcarbonyloxyalkyloxy, C.sub.5 -C.sub.10 (5-alkyl-1,3-dioxa-cyclopenten-2-one-yl)methyloxy, C.sub.10 -C.sub.14 (5-aryl-1,3-dioxa-cyclopenten-2-one-yl)methyloxy, or (R.sup.11)(R.sup.12)N--(C.sub.1 -C.sub.10 alkoxy)-; R.sup.20 is selected from: H, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.4 -C.sub.11 cycloalkylalkyl, aryl, aryl(C.sub.1 -C.sub.6 alkyl)-, or heteroaryl(C.sub.1 -C.sub.6 alkyl)-; R.sup.21 is selected from COOH or NR.sup.6.sub.2 ; m is 0-4; n is 0-4; p is 0-2; q is 0-2; and r is 0-2; with the following provisos: (1) t, n, m and q are chosen such that the number of atoms connecting R.sup.1 and Y is in the range of 10-14; and (2) n and m are chosen such that the value of n plus m is greater than one unless U is --(CH.sub.2).sub.t Q(CH.sub.2).sub.m --.

�13! Preferred compounds of the invention as described above are compounds of the Formula Ic: ##STR34## including stereoisomeric forms thereof, or mixtures of stereoisomeric forms thereof, or pharmaceutically acceptable salt or prodrug forms thereof wherein:

X.sup.1, X.sup.2, X.sup.3, and X.sup.4 are independently selected from nitrogen or carbon provided that at least two of X.sup.1, X.sup.2, X.sup.3 and X.sup.4 are carbon; R.sup.1 is selected from: ##STR35## A and B are independently --CH.sub.2 --, --O--, --N(R.sup.2)--, or --C(.dbd.O)--; A.sup.1 and B.sup.1 are independently --CH.sub.2 -- or --N(R.sup.3)--; D is --N(R.sup.2)--, --O--, --S--, --C(.dbd.O)-- or --SO.sub.2 --; E-F is --C(R.sup.4).dbd.C(R.sup.5)--, --N.dbd.C(R.sup.4)--, --C(R.sup.4).dbd.N--, or --C(R.sup.4).sub.2 C(R.sup.5).sub.2 --; J, K, L and M are independently selected from: --C(R.sup.4)--, --C(R.sup.5)-- or --N--, provided that at least one of J, K, L and M is not --N--; R.sup.2 is selected from: H, C.sub.1 -C.sub.6 alkyl, (C.sub.1 -C.sub.6 alkyl)carbonyl, (C.sub.1 -C.sub.6 alkoxy)carbonyl, C.sub.1 -C.sub.6 alkylaminocarbonyl, C.sub.3 -C.sub.6 alkenyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.4 -C.sub.11 cycloalkylalkyl, aryl, heteroaryl(C.sub.1 -C.sub.6 alkyl)carbonyl, heteroarylcarbonyl, aryl(C.sub.1 -C.sub.6 alkyl)-, (C.sub.1 -C.sub.6 alkyl)carbonyl, arylcarbonyl, alkylsulfonyl, arylsulfonyl, aryl(C.sub.1 -C.sub.6 alkyl)sulfonyl, heteroarylsulfonyl, heteroaryl(C.sub.1 -C.sub.6 alkyl)sulfonyl, aryloxycarbonyl, aryl(C.sub.1 -C.sub.6 alkoxy)carbonyl, wherein said aryl groups are substituted with 0-2 substituents selected from the group consisting of C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, halo, CF.sub.3, and nitro; R.sup.3 is selected from: H, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.4 -C.sub.11 cycloalkylalkyl, aryl, aryl(C.sub.1 -C.sub.6 alkyl)-, or heteroaryl(C.sub.1 -C.sub.6 alkyl)-; R.sup.4 and R.sup.5 are independently selected from: H, C.sub.1 -C.sub.4 alkoxy, NR.sup.2 R.sup.3, halogen, NO.sub.2, CN, CF.sub.3, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 alkenyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.4 -C.sub.11 cycloalkylalkyl, aryl, aryl(C.sub.1 -C.sub.6 alkyl)-, C.sub.2 -C.sub.7 alkylcarbonyl, arylcarbonyl or alternatively, when substituents on adjacent atoms, R.sup.4 and R.sup.5 can be taken together with the carbon atoms to which they are attached to form a 5-7 membered carbocyclic or 5-7 membered heterocyclic aromatic or non-aromatic ring system, said carbocyclic or heterocyclic ring being optionally substituted with 0-2 groups selected from: C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, halo, cyano, amino, CF.sub.3, or NO.sub.2 ; U is selected from: --(CH.sub.2).sub.n --, --(CH.sub.2).sub.n (CR.sup.7 .dbd.CR.sup.8)(CH.sub.2).sub.m -- --(CH.sub.2).sub.t Q(CH.sub.2).sub.m --, --(CH.sub.2).sub.n O(CH.sub.2).sub.m --, --(CH.sub.2).sub.n N(R.sup.6)(CH.sub.2).sub.m --, --(CH.sub.2).sub.n C(.dbd.O)(CH.sub.2).sub.m --, or --(CH.sub.2).sub.n S(O).sub.p (CH.sub.2).sub.m --; wherein one of the methylene groups is optionally substituted with R.sup.7 ; Q is selected from 1,2-phenylene, 1,3-phenylene, 2,3-pyridinylene, 3,4-pyridinylene, or 2,4-pyridinylene; R.sup.6 is selected from: H, C.sub.1 -C.sub.4 alkyl, or benzyl; R.sup.7 and R.sup.8 are independently selected from: H, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.7 cylcloalkyl, C.sub.4 -C.sub.11 cycloalkylalkyl, aryl, aryl(C.sub.1 -C.sub.6 alkyl)-, or heteroaryl(C.sub.0 -C.sub.6 alkyl)-; R.sup.9 is selected from: H, CO.sub.2 R.sup.17, C(.dbd.O)R.sup.17, CONR.sup.17 R.sup.20, --SO.sub.2 R.sup.17, --SO.sub.2 NR.sup.17 R.sup.20, C.sub.1 -C.sub.6 alkyl substituted with 0-1 R.sup.15 or 0-1 R.sup.21, C.sub.3 -C.sub.6 alkenyl substituted with 0-1 R.sup.15 or 0-1 R.sup.21, C.sub.3 -C.sub.7 cycloalkyl substituted with 0-1 R.sup.15 or 0-1 R.sup.21, C.sub.4 -C.sub.11 cycloalkylalkyl substituted with 0-1 R.sup.15 or 0-1 R.sup.21, aryl substituted with 0-1 R.sup.15 or 0-2 R.sup.11 or 0-1 R.sup.21, or aryl(C.sub.1 -C.sub.6 alkyl)- substituted with 0-1 R.sup.15 or 0-2 R.sup.11 or 0-1 R.sup.21 ; R.sup.11 is selected from: H, halogen, CF.sub.3, CN, NO.sub.2, hydroxy, NR.sup.2 R.sup.3, C.sub.1 -C.sub.4 alkyl substituted with 0-1 R.sup.21, C.sub.1 -C.sub.4 alkoxy substituted with 0-1 R.sup.21, aryl substituted with 0-1 R.sup.21, aryl(C.sub.1 -C.sub.6 alkyl)- substituted with 0-1 R.sup.21, (C.sub.1 -C.sub.4 alkoxy)carbonyl substituted with 0-1 R.sup.21, (C.sub.1 -C.sub.4 alkyl)carbonyl substituted with 0-1 R.sup.21, C.sub.1 -C.sub.4 alkylsulfonyl substituted with 0-1 R.sup.21, or C.sub.1 -C.sub.4 alkylaminosulfonyl substituted with 0-1 R.sup.21 ; W is --C(.dbd.O)--N(R.sup.13)--(C(R.sup.12).sub.2).sub.q --; X is --C(R.sup.12)(R.sup.14)--C(R.sup.12)(R.sup.15)--; alternatively, W and X can be taken together to be ##STR36## R.sup.12 is H or C.sub.1 -C.sub.6 alkyl; R.sup.13 is selected from: H, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.7 cycloalkylmethyl, or aryl(C.sub.1 -C.sub.6 alkyl)-; R.sup.14 is selected from: H, C.sub.1 -C.sub.6 alkylthioalkyl, aryl(C.sub.1 -C.sub.10 alkylthioalkyl)-, aryl(C.sub.1 -C.sub.10 alkoxyalkyl)-, C.sub.1 -C.sub.10 alkyl, C.sub.1 -C.sub.10 alkoxyalkyl, C.sub.1 -C.sub.6 hydroxyalkyl, C.sub.2 -C.sub.10 alkenyl, C.sub.2 -C.sub.10 alkynyl, C.sub.3 -C.sub.10 cycloalkyl, C.sub.3 -C.sub.10 cycloalkylalkyl, aryl(C.sub.1 -C.sub.6 alkyl)-, heteroaryl(C.sub.1 -C.sub.6 alkyl)-, aryl, heteroaryl, CO.sub.2 R.sup.17, C(.dbd.O)R.sup.17, or CONR.sup.17 R.sup.20, provided that any of the above alkyl, cycloalkyl, aryl or heteroaryl groups may be unsubstituted or substituted independently with 0-1 R.sup.16 or 0-2 R.sup.11 ; R.sup.15 is selected from: H, R.sup.16, C.sub.1 -C.sub.10 alkyl, C.sub.1 -C.sub.10 alkoxyalkyl, C.sub.1 -C.sub.10 alkylaminoalkyl, C.sub.1 -C.sub.10 dialkylaminoalkyl, C.sub.1 -C.sub.10 alkylcarbonyl, aryl(C.sub.1 -C.sub.6 alkyl)carbonyl, C.sub.2 -C.sub.10 alkenyl, C.sub.2 -C.sub.10 alkynyl, C.sub.3 -C.sub.10 cycloalkyl, C.sub.3 -C.sub.10 cycloalkylalkyl, aryl(C.sub.1 -C.sub.6 alkyl)-, heteroaryl(C.sub.1 -C.sub.6 alkyl)-, aryl, heteroaryl, CO.sub.2 R.sup.17, C(.dbd.O)R.sup.17, CONR.sup.17 R.sup.20, SO.sub.2 R.sup.17, or SO.sub.2 NR.sup.17 R.sup.20, provided that any of the above alkyl, cycloalkyl, aryl or heteroaryl groups may be unsubstituted or substituted independently with 0-2 R.sup.11 ; Y is selected from: ##STR37## R.sup.16 is selected from: --N(R.sup.20)--C(.dbd.O)--O--R.sup.17, --N(R.sup.20)--C(.dbd.O)--R.sup.17, --N(R.sup.20)--C(.dbd.O)--NH--R.sup.17, --N(R.sup.20)SO.sub.2 --R.sup.17, or --N(R.sup.20)SO.sub.2 --NR.sup.20 R.sup.17 ; R.sup.17 is selected from: C.sub.1 -C.sub.10 alkyl, C.sub.3 -C.sub.11 cycloalkyl, aryl(C.sub.1 -C.sub.6 alkyl)-, (C.sub.1 -C.sub.6 alkyl)aryl, heteroaryl(C.sub.1 -C.sub.6 alkyl)-, (C.sub.1 -C.sub.6 alkyl)heteroaryl, biaryl(C.sub.1 -C.sub.6 alkyl)-, heteroaryl, or aryl, wherein said aryl or heteroaryl groups are optionally substituted with 0-3 substituents selected from the group consisting of: C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, aryl, heteroaryl, halo,cyano, amino, CF.sub.3, and NO.sub.2 ; R.sup.18 is selected from: H, --C(.dbd.O)--O--R.sup.17, --C(.dbd.O)--R.sup.17, --C(.dbd.O)--NH--R.sup.17, --SO.sub.2 --R.sup.17, or --SO.sub.2 --NR.sup.20 R.sup.17 ; R.sup.19 is selected from: hydroxy, C.sub.1 -C.sub.10 alkyloxy, C.sub.3 -C.sub.11 cycloalkyloxy, C.sub.6 -C.sub.10 aryloxy, C.sub.7 -C.sub.11 aralkyloxy, C.sub.3 -C.sub.10 alkylcarbonyloxyalkyloxy, C.sub.3 -C.sub.10 alkoxycarbonyloxyalkyloxy, C.sub.2 -C.sub.10 alkoxycarbonylalkyloxy, C.sub.5 -C.sub.10 cycloalkylcarbonyloxyalkyloxy, C.sub.5 -C.sub.10 cycloalkoxycarbonyloxyalkyloxy, C.sub.5 -C.sub.10 cycloalkoxycarbonylalkyloxy, C.sub.7 -C.sub.11 aryloxycarbonylalkyloxy, C.sub.8 -C.sub.12 aryloxycarbonyloxyalkyloxy, C.sub.8 -C.sub.12 arylcarbonyloxyalkyloxy, C.sub.5 -C.sub.10 alkoxyalkylcarbonyloxyalkyloxy, C.sub.5 -C.sub.10 (5-alkyl-1,3-dioxa-cyclopenten-2-one-yl)methyloxy, C.sub.10 -C.sub.14 (5-aryl-1,3-dioxa-cyclopenten-2-one-yl)methyloxy, or (R.sup.11)(R.sup.12)N--(C.sub.1 -C.sub.10 alkoxy)-; R.sup.20 selected from: H, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.4 -C.sub.11 cycloalkylalkyl, aryl(C.sub.1 -C.sub.6 alkyl)-, or heteroaryl(C.sub.1 -C.sub.6 alkyl)-; R.sup.21 is selected from COOH or NR.sup.6.sub.2 ; m is 0-4; n is 0-4; t is 0-4; p is 0-2; q is 0-2; and r is 0-2.

�14! Further preferred compounds of the invention as described above are compounds of the Formula IIe or IIf: ##STR38## including stereoisomeric forms thereof, or mixtures of stereoisomeric forms thereof, or pharmaceutically acceptable salt or prodrug forms thereof, wherein:

R.sup.1 is selected from: ##STR39## wherein the above heterocycles are optionally substituted with 0-2 substituents selected from the group consisting of: NH.sub.2, halogen, NO.sub.2, CN, CF.sub.3, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.6 alkyl, and C.sub.3 -C.sub.7 cycloalkyl; U is --(CH.sub.2).sub.n --, --(CH.sub.2).sub.t Q(CH.sub.2).sub.m -- or --C(.dbd.O)(CH.sub.2).sub.n-1 --, wherein one of the methylene groups is optionally substituted with R.sup.7 ; Q is selected from 1,2-phenylene, 1,3-phenylene, 2,3-pyridinylene, 3,4-pyrdinylene, or 2,4-pyridinylene; R.sup.6 is selected from: H, C.sub.1 -C.sub.4 alkyl, or benzyl; R7 is selected from: C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.4 -C.sub.11 cycloalkylalkyl, aryl, aryl(C.sub.1 -C.sub.6 alkyl), heteroaryl, or heteroaryl(C.sub.1 -C.sub.6 alkyl); R.sup.9 is selected from: H, --SO.sub.2 R.sup.17, --SO.sub.2 NR.sup.17 R.sup.20, C.sub.1 -C.sub.6 alkyl substituted with 0-1 R.sup.15 or 0-1 R.sup.21, C.sub.3 -C.sub.7 cycloalkyl substituted with 0-1 R.sup.15 or 0-1 R.sup.21, C.sub.4 -C.sub.11 cycloalkylalkyl substituted with 0-1 R.sup.15 or 0-1 R.sup.21 aryl substituted with 0-1 R.sup.15 or 0-2 R.sup.11 or 0-1 R.sup.21, or aryl(C.sub.1 -C.sub.6 alkyl)-substituted with 0-1 R.sup.15 or 0-2 R.sup.11 or 0-1 R.sup.21 ; R.sup.11 is selected from H, halogen, CF.sub.3, CN, NO.sub.2, hydroxy, NR.sup.2 R.sup.3, C.sub.1 -C.sub.4 alkyl substituted with 0-1 R.sup.21, C.sub.1 -C.sub.4 alkoxy substituted with 0-1 R.sup.21, aryl substituted with 0-1 R.sup.21.sub.1 aryl(C.sub.1 -C.sub.6 alkyl)-substituted with 0-1 R.sup.21, (C.sub.1 -C.sub.4 alkoxy)carbonyl substituted with 0-1 R.sup.21, (C.sub.1 -C.sub.4 alkyl)carbonyl substituted with 0-1 R.sup.21, C.sub.1 -C.sub.4 alkylsulfonyl substituted with 0-1 R.sup.21, or C.sub.1 -C.sub.4 alkylaminosulfonyl substituted with 0-1 R.sup.21 ; W is --C(.dbd.O)--N(R.sup.13)--; X is --CH(R.sup.14)--CH(R.sup.15)--; R.sup.13 is H or CH.sub.3 ; R.sup.14 is selected from: H, C.sub.1 -C.sub.10 alkyl, aryl, or heteroaryl, wherein said aryl or heteroaryl groups are optionally substituted with 0-3 substituents selected from the group consisting of: C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, aryl, halo, cyano, amino, CF.sub.3, and NO.sub.2 ; R.sup.15 is H or R.sup.16 ; Y is --COR.sup.19 ; R.sup.16 is selected from: --NH(R.sup.20)--C(.dbd.O)--O--R.sup.17, --N(R.sup.20)--C(.dbd.O)--R.sup.17, --N(R.sup.20)--C(.dbd.O)--NH--R.sup.17, --N(R.sup.20)SO.sub.2 --R.sup.17, or --N(R.sup.20)SO.sub.2 --N(R.sup.20)R.sup.17 ; R.sup.17 is selected from: C.sub.1 -C.sub.10 alkyl, C.sub.3 -C.sub.11 cycloalkyl, aryl(C.sub.1 -C.sub.6 alkyl)-, (C.sub.1 -C.sub.6 alkyl)aryl, heteroaryl(C.sub.1 -C.sub.6 alkyl)-, (C.sub.1 -C.sub.6 alkyl)heteroaryl, biaryl(C.sub.1 -C.sub.6 alkyl)-, heteroaryl, or aryl, wherein said aryl or heteroaryl groups are optionally substituted with 0-3 substituents selected from the group consisting of: C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, aryl, heteroaryl, halo, cyano, amino, CF.sub.3, and NO.sub.2 ; R.sup.19 is selected from: hydroxy, C.sub.1 -C.sub.10 alkoxy, methylcarbonyloxymethoxy-, ethylcarbonyloxymethoxy-, t-butylcarbonyloxymethoxy-, cyclohexylcarbonyloxymethoxy-, 1-(methylcarbonyloxy)ethoxy-, 1-(ethylcarbonyloxy)ethoxy-, 1-(t-butylcarbonyloxy)ethoxy-, 1-(cyclohexylcarbonyloxy)ethoxy-, i-propyloxycarbonyloxymethoxy-, t-butyloxycarbonyloxymethoxy-, 1-(i-propyloxycarbonyloxy)ethoxy-, 1-(cyclohexyloxycarbonyloxy)ethoxy-, 1-(t-butyloxycarbonyloxy)ethoxy-, dimethylaminoethoxy-, diethylaminoethoxy-, (5-methyl-1,3-dioxacyclopenten-2-on-4-yl)methoxy-, (5-(t-butyl)-1,3-dioxacyclopenten-2-on-4-yl)methoxy-, (1,3-dioxa-5-phenyl-cyclopenten-2-on-4-yl)methoxy-, or 1-(2-(2-methoxypropyl)carbonyloxy)ethoxy-; R.sup.20 is H or CH.sub.3 ; R.sup.21 is selected from COOH or NR.sup.6.sub.2 ; and m is 0 or 1; n is 1-4; and t is 0 or 1.

�15! Still further preferred compounds of the above described are compounds of the Formula IIe or IIf: ##STR40## including stereoisomeric forms thereof, or mixtures of stereoisomeric forms thereof, or pharmaceutically acceptable salt or prodrug forms thereof, wherein: R.sup.1 is selected from: ##STR41## wherein the above heterocycles are optionally substituted with 0-2 substituents selected from the group consisting of: NH.sub.2, halogen, NO.sub.2, CN, CF.sub.3, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.6 alkyl, and C.sub.3 -C.sub.7 cycloalkyl:

U is --(CH.sub.2).sub.n --, --(CH.sub.2).sub.t Q(CH.sub.2).sub.m -- or --C(.dbd.O)(CH.sub.2).sub.n-1 --, wherein one of the methylene groups is optionally substituted with R.sup.7 ; Q is selected from 1,2-phenylene, 1,3-phenylene, 2,3-pyridinylene, 3,4-pyridinylene, or 2,4-pyridinylene; R.sup.6 selected from: H, C.sub.1 -C.sub.4 alkyl, or benzyl; R7 is selected from C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.4 -C.sub.11 cycloalkylalkyl, aryl, aryl(C.sub.1 -C.sub.6 alkyl), heteroaryl, or heteroaryl(C.sub.1 -C.sub.6 alkyl); R.sup.9 is selected from: H, --SO.sub.2 R.sup.17, --SO.sub.2 NR.sup.17 R.sup.20, C.sub.1 -C.sub.6 alkyl substituted with 0-1 R.sup.15 or 0-1 R.sup.21, C.sub.3 -C.sub.7 cycloalkyl substituted with 0-1 R.sup.15 or 0-1 R.sup.21, C.sub.4 -C.sub.11 cycloalkylalkyl substituted with 0-1 R.sup.15 or 0-1 R.sup.21, aryl substituted with 0-1 R.sup.15 or 0-2 R.sup.11 or 0-1 R.sup.21, or aryl(C.sub.1 -C.sub.6 alkyl)-substituted with 0-1 R.sup.15 or 0-2 R.sup.11 or 0-1 R.sup.21 ; R.sup.11 is selected from H, halogen, CF.sub.3 CN, NO.sub.2, hydroxy, NR.sup.2 R.sup.3 C.sub.1 -C.sub.4 alkyl substituted with 0-1 R.sup.21 C.sub.1 -C.sub.4 alkoxy substituted with 0-1 R.sup.21, aryl substituted with 0-1 R.sup.21, aryl(C.sub.1 -C.sub.6 alkyl)-substituted with 0-1 R.sup.21 (C.sub.1 -C.sub.4 alkoxy)carbonyl substituted with 0-1 R.sup.21 (C.sub.1 -C.sub.4 alkyl)carbonyl substituted with 0-1 R.sup.21, C.sub.1 -C.sub.4 alkylsulfonyl substituted with 0-1 R.sup.21, or C.sub.1 -C.sub.4 alkylaminosulfonyl substituted with 0-1 R.sup.21 ;W is --C(.dbd.O)--N(R.sup.13)--; W is --C(.dbd.O)--N(R.sup.13)--; X is --CH(R.sup.14)--CH(R.sup.15) R.sup.13 is H or CH.sub.3 ; R.sup.14 is selected from: H, C.sub.1 -C.sub.10 alkyl, aryl, or heteroaryl, wherein said aryl or heteroaryl groups are optionally substituted with 0-3 substituents selected from the group consisting of: C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, aryl, halo, cyano, amino, CF.sub.3, and NO.sub.2 ; R.sup.15 is H or R.sup.16 ; Y is --COR.sup.19 ; R.sup.16 is selected from:. --NH(R.sup.20)--C(.dbd.O)--O--R.sup.17, --N(R.sup.20)--C(.dbd.O)--R.sup.17, --N(R.sup.20)--C(.dbd.O)--NH--R.sup.17, --N(R.sup.20)SO.sub.2 --R.sup.17, or --N(R.sup.20)SO.sub.2 --NR.sup.20 R.sup.17 ; R.sup.17 is selected from: C.sub.1 -C.sub.10 alkyl, C.sub.3 -C.sub.11 cycloalkyl, aryl(C.sub.1 -C.sub.6 alkyl)-, (C.sub.1 -C.sub.6 alkyl)aryl, heteroaryl(C.sub.1 -C.sub.6 alkyl)-, (C.sub.1 -C.sub.6 alkyl)heteroaryl, biaryl(C.sub.1 -C.sub.6 alkyl)-, heteroaryl, or aryl, wherein said aryl or heteroaryl groups are optionally substituted with 0-3 substituents selected from the group consisting of: C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, aryl, heteroaryl, halo, cyano, amino, CF.sub.3, and NO.sub.2 ; R.sup.19 is selected from: hydroxy, C.sub.1 -C.sub.10 alkoxy, methylcarbonyloxymethoxy-, ethylcarbonyloxymethoxy-, t-butylcarbonyloxymethoxy-, cyclohexylcarbonyloxymethoxy-, 1-(methylcarbonyloxy)ethoxy-, 1-(ethylcarbonyloxy)ethoxy-, 1-(t-butylcarbonyloxy)ethoxy-, 1-(cyclohexylcarbonyloxy)ethoxy-, i-propyloxycarbonyloxymethoxy-, t-butyloxycarbonyloxymethoxy-, 1-(i-propyloxycarbonyloxy)ethoxy-, 1-(cyclohexyloxycarbonyloxy)ethoxy-, 1-(t-butyloxycarbonyloxy)ethoxy-, dimethylaminoethoxy-, diethylaminoethoxy-, (5-methyl-1,3-dioxacyclopenten-2-on-4-yl)methoxy-, (5-(t-butyl)-1,3-dioxacyclopenten-2-on-4-yl)methoxy-, (1,3-dioxa-5-phenyl-cyclopenten-2-on-4-yl)methoxy-, or 1-(2-(2-methoxypropyl)carbonyloxy)ethoxy-; R.sup.20 is H or CH.sub.3 ; R.sup.21 is selected from COOH or NR.sup.6.sub.2 ; and m is 0 or 1; n is 1-4; and t is 0 or 1.

In the present invention it has been discovered that the compounds of Formula Ia, Ib or Ic above are useful as inhibitors of cell-matrix and cell-cell adhesion processes. The present invention includes novel compounds of Formula Ia, Ib or Ic and methods for using such compounds for the prevention or treatment of diseases resulting from abnormal cell adhesion to the extracellular matrix which comprises administering to a host in need of such treatment a therapeutically effective amount of such compound of Formula Ia, Ib or Ic.

In the present invention it has also been discovered that the compounds of Formula Ia, Ib or Ic above are useful as inhibitors of .alpha..sub.v .beta..sub.3. The compounds of the present invention inhibit the binding of vitronectin to .alpha..sub.v .beta..sub.3 and inhibit cell adhesion.

The present invention also provides pharmaceutical compositions comprising a compound of Formula Ia, Ib or Ic and a pharmaceutically acceptable carrier.

The compounds of Formula Ia, Ib or Ic of the present invention are useful for the treatment (including prevention) of angiogenic disorders, comprising administering to a mammal in need of such treatment a therapeutically effective amount of a compound of Formula Ia, Ib or Ic described above. The term "angiogenic disorders" as used herein includes conditions involving abnormal neovascularization, such as tumor metastasis and ocular neovascularization, including, for example, diabetic retinopathy, neovascular glaucoma, age-related macular degeneration, and retinal vein occlusion.

The compounds of Formula Ia, Ib or Ic of the present invention are also useful for the treatment (including prevention) of thromboembolic disorders, comprising administering to a mammal in need of such treatment a therapeutically effective amount of a compound of Formula Ia, Ib or Ic described above. The term "thromboembolic disorders" as used herein includes conditions involving platelet activation and aggregation, such as arterial or venous cardiovascular or cerebrovascular thromboembolic disorders, including, for example, thrombosis, unstable angina, first or recurrent myocardial infarction, ischemic sudden death, transient ischemic attack, stroke, atherosclerosis, venous thrombosis, deep vein thrombosis, thrombophlebitis, arterial embolism, coronary and cerebral arterial thrombosis, myocardial infarction, cerebral embolisms, kidney embolisms, pulmonary embolisms, or such disorders associated with diabetes.

The compounds of Formula Ia, Ib or Ic of the present invention may also be useful for the treatment or prevention of other diseases which involve cell adhesion processes, including, but not limited to, inflammation, bone degradation, restenosis, rheumatoid arthritis, asthma, allergies, adult respiratory distress syndrome, graft versus host disease, organ transplantation rejection, septic shock, psoriasis, eczema, contact dermatitis, osteoporosis, osteoarthritis, atherosclerosis, inflammatory bowel disease and other autoimmune diseases. The compounds of Formula Ia, Ib or Ic of the present invention may also be useful for wound healing.

The compounds of the present invention may be used for other ex vivo applications to prevent cellular adhesion in biological samples.

The compounds of the present invention can also be administered in combination with one or more additional therapeutic agents selected from: anti-coagulant or coagulation inhibitory agents, such as heparin or warfarin; anti-platelet or platelet inhibitory agents, such as aspirin, piroxicam, or ticlopidine; thrombin inhibitors such as boropeptides, hirudin or argatroban; or thrombolytic or fibrinolytic agents, such as plasminogen activators, anistreplase, urokinase, or streptokinase.

The compounds of Formula Ia, Ib or Ic of the present invention can be administered in combination with one or more of the foregoing additional therapeutic agents, thereby to reduce the doses of each drug required to achieve the desired therapeutic effect. Thus, the combination treatment of the present invention permits the use of lower doses of each component, with reduced adverse, toxic effects of each component. A lower dosage minimizes the potential of side effects of the compounds, thereby providing an increased margin of safety relative to the margin of safety for each component when used as a single agent. Such combination therapies may be employed to achieve synergistic or additive therapeutic effects for the treatment of thromboembolic or other disorders.

By "therapeutically effective amount" is meant an amount of a compound of Formula Ia, Ib or Ic that when administered alone or in combination with an additional therapeutic agent to a cell or mammal is effective to prevent or ameliorate the disease condition or the progression of the disease.

By "administered in combination" or "combination therapy" it is meant that the compound of Formula Ia, Ib or Ic and one or more additional therapeutic agents are administered concurrently to the mammal being treated. When administered in combination each component may be administered at the same time or sequentially in any order at different points in time. Thus, each component may be administered separately but sufficiently closely in time so as to provide the desired therapeutic effect.

The term anti-coagulant agents (or coagulation inhibitory agents), as used herein, denotes agents that inhibit blood coagulation. Such agents include warfarin sodium crystalline clathrate and heparin.

The term anti-platelet agents (or platelet inhibitory agents), as used herein, denotes agents that inhibit platelet function such as by inhibiting the aggregation, adhesion or granular secretion of platelets. Such agents include the various known non-steroidal anti-inflammatory drugs (NSAIDS) such as aspirin, ibuprofen, naproxen, sulindac, indomethacin, mefenamate, droxicam, diclofenac, sulfinpyrazone, and piroxicam, including pharmaceutically acceptable salts or prodrugs thereof. Other suitable anti-platelet agents include ticlopidine, including pharmaceutically acceptable salts or prodrugs thereof. Ticlopidine is also a preferred compound since it is known to be gentle on the gastrointestinal tract in use. Still other suitable platelet inhibitory agents include thromboxane-A.sub.2 -receptor antagonists and thromboxane-A.sub.2 -synthetase inhibitors, as well as pharmaceutically acceptable salts or prodrugs thereof.

The phrase thrombin inhibitors (or anti-thrombin agents), as used herein, denotes inhibitors of the serine protease thrombin. By inhibiting thrombin, various thrombin-mediated processes, such as thrombin-mediated platelet activation (that is, for example, the aggregation of platelets, and/or the granular secretion of plasminogen activator inhibitor-1 and/or serotonin) and/or fibrin formation are disrupted. Such inhibitors include boroarginine derivatives and boropeptides, hirudin and argatroban, including pharmaceutically acceptable salts and prodrugs thereof. Boroarginine derivatives and boropeptides include N-acetyl and peptide derivatives of boronic acid, such as C-terminal .alpha.-aminoboronic acid derivatives of lysine, ornithine, arginine, homoarginine and corresponding isothiouronium analogs thereof. The term hirudin, as used herein, includes suitable derivatives or analogs of hirudin, referred to herein as hirulogs, such as disulfatohirudin. Boropeptide thrombin inhibitors include compounds described in Kettner et al., U.S. Pat. No. 5,187,157 and European Patent Application Publication Number 293 881 A2, the disclosures of which are hereby incorporated herein by reference. Other suitable boroarginine derivatives and boropeptide thrombin inhibitors include those disclosed in PCT Application Publication Number 92/07869 and European Patent Application Publication Number 471 651 A2, the disclosures of which are hereby incorporated herein by reference, in their entirety.

The phrase thrombolytics (or fibrinolytic) agents (or thrombolytics or fibrinolytics), as used herein, denotes agents that lyse blood clots (thrombi). Such agents include tissue plasminogen activator, anistreplase, urokinase, retivase or streptokinase, including pharmaceutically acceptable salts or prodrugs thereof. Tissue plasminogen activator (tPA) is commercially available from Genentech Inc., South San Francisco, Calif. The term anistreplase, as used herein, refers to anisoylated plasminogen streptokinase activator complex, as described, for example, in European Patent Application No. 028,489, the disclosures of which are hereby incorporated herein by reference herein, in their entirety. The term urokinase, as used herein, is intended to denote both dual and single chain urokinase, the latter also being referred to herein as prourokinase.

The compounds of the present invention are also useful as standard or reference compounds, for example as a quality standard or control, in tests or assays involving the binding of vitronectin or fibrinogen to .alpha..sub.v .beta..sub.3. Such compounds may be provided in a commercial kit, for example, for use in pharmaceutical research involving .alpha..sub.v .beta..sub.3. The compounds of the present invention may also be used in diagnostic assays involving .alpha..sub.v .beta..sub.3.

The compounds herein described may have asymmetric centers. Unless otherwise indicated, all chiral, diastereomeric and racemic forms are included in the present invention. Many geometric isomers of olefins, C.dbd.N double bonds, and the like can also be present in the compounds described herein, and all such stable isomers are contemplated in the present invention. It will be appreciated that compounds of the present invention that contain asymmetrically substituted carbon atoms may be isolated in optically active or racemic forms. It is well known in the art how to prepare optically active forms, such as by resolution of racemic forms or by synthesis, from optically active starting materials. All chiral, diastereomeric, racemic forms and all geometric isomeric forms of a structure are intended, unless the specific stereochemistry or isomer form is specifically indicated.

When any variable (for example but not limited to, R.sup.2, R.sup.4, R.sup.6, R.sup.7, R.sup.8, R.sup.12,and R.sup.14, n, etc.) occurs more than one time in any constituent or in any formula, its definition on each occurrence is independent of its definition at every other occurrence. Thus, for example, if a group is shown to be substituted with 0-3 R.sup.4, then said group may optionally be substituted with up to three R.sup.4 and R.sup.4 at each occurrence is selected independently from the defined list of possible R.sup.4. Also, by way of example, for the group --N(R.sup.5a).sub.2, each of the two R.sup.5a substituents on N is independently selected from the defined list of possible R.sup.5a. Similarly, by way of example, for the group --C(R.sup.7).sub.2 --, each of the two R.sup.7 substituents on C is independently selected from the defined list of possible R.sup.7.

When a bond to a substituent is shown to cross the bond connecting two atoms in a ring, then such substituent may be bonded to any atom on the ring. When a bond joining a substituent to another group is not specifically shown or the atom in such other group to which the bond joins is not specifically shown, then such substituent may form a bond with any atom on such other group.

When a substituent is listed without indicating the atom via which such substituent is bonded to the rest of the compound of Formula Ia, Ib or Ic, then such substituent may be bonded via any atom in such substituent. For example, when the substituent is piperazinyl, piperidinyl, or tetrazolyl, unless specified otherwise, said piperazinyl, piperidinyl, tetrazolyl group may be bonded to the rest of the compound of Formula Ia, Ib or Ic via any atom in such piperazinyl, piperidinyl, tetrazolyl group.

Combinations of substituents and/or variables are permissible only if such combinations result in stable compounds. By stable compound or stable structure it is meant herein a compound that is sufficiently robust to survive isolation to a useful degree of purity from a reaction mixture, and formulation into an efficacious therapeutic agent.

The term "substituted", as used herein, means that any one or more hydrogen on the designated atom is replaced with a selection from the indicated group, provided that the designated atom's normal valency is not exceeded, and that the substitution results in a stable compound. When a substitent is keto (i.e., .dbd.O), then 2 hydrogens on the atom are replaced.

As used herein, "alkyl" is intended to include both branched and straight-chain saturated aliphatic hydrocarbon groups having the specified number of carbon atoms (for example, "C.sub.0 -C.sub.10 " denotes alkyl having 0 to 10 carbon atoms; C.sub.0 denotes a direct bond between the groups linked by the C.sub.0 group; also by way of example, "C.sub.1 to C.sub.4 " denotes methyl, ethyl, n-propyl, isopropyl, n-butyl, 2-methylpropyl, 1-methylpropyl, 1,1-dimethyl ethyl); "haloalkyl" is intended to include both branched and straight-chain saturated aliphatic hydrocarbon groups having the specified number of carbon atoms, substituted with 1 or more halogen (for example --C.sub.v F.sub.w where v=1 to 3 and w=1 to (2v+1)); "alkoxy" represents an alkyl group of indicated number of carbon atoms attached through an oxygen bridge; "cycloalkyl" is intended to include saturated ring groups, including mono-,bi- or poly-cyclic ring systems, such as cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, cyclooctyl, and adamantyl; and "biycloalkyl" is intended to include saturated bicyclic ring groups such as �3.3.0!bicyclooctane, �4.3.0!bicyclononane, �4.4.0!bicyclodecane (decalin), �2.2.2!bicyclooctane, and so forth. "Alkenyl" is intended to include hydrocarbon chains of either a straight or branched configuration and one or more unsaturated carbon-carbon bonds which may occur in any stable point along the chain, such as ethenyl, propenyl and the like; and "alkynyl" is intended to include hydrocarbon chains of either a straight or branched configuration and one or more triple carbon-carbon bonds which may occur in any stable point along the chain, such as ethynyl, propynyl and the like.

The terms "alkylene", "alkenylene", "phenylene", and the like, refer to alkyl, alkenyl, and phenyl groups, respectively, which are connected by two bonds to the rest of the structure of Formula Ia, Ib or Ic. Such "alkylene", "alkenylene", "phenylene", and the like, may alternatively and equivalently be denoted herein as "-(alkyl)-", "-(alkyenyl)-" and "-(phenyl)-", and the like.

"Halo" or "halogen" as used herein refers to fluoro, chloro, bromo and iodo; and "counterion" is used to represent a small, negatively charged species such as chloride, bromide, hydroxide, acetate, sulfate and the like.

As used herein, "aryl" or "aromatic residue" is intended to mean phenyl or naphthyl; the term "arylalkyl" represents an aryl group attached through an alkyl bridge.

As used herein, "carbocycle" or "carbocyclic residue" is intended to mean any stable 3- to 7-membered monocyclic or bicyclic or 7- to 14-membered bicyclic or tricyclic or an up to 26-membered polycyclic carbon ring, any of which may be saturated, partially unsaturated, or aromatic. Examples of such carbocyles include, but are not limited to, cyclopropyl, cyclopentyl, cyclohexyl, phenyl, biphenyl, naphthyl, indanyl, adamantyl, or tetrahydronaphthyl (tetralin).

As used herein, the term "heterocycle" or "heterocyclic" is intended to mean a stable 5- to 7-membered monocyclic or bicyclic or 7- to 10-membered bicyclic heterocyclic ring which may be saturated, partially unsaturated, or aromatic, and which consists of carbon atoms and from 1 to 4 heteroatoms independently selected from the group consisting of N, O and S and wherein the nitrogen and sulfur heteroatoms may optionally be oxidized, and the nitrogen may optionally be quaternized, and including any bicyclic group in which any of the above-defined heterocyclic rings is fused to a benzene ring. The heterocyclic ring may be attached to its pendant group at any heteroatom or carbon atom which results in a stable structure. The heterocyclic rings described herein may be substituted on carbon or on a nitrogen atom if the resulting compound is stable. Examples of such heterocycles include, but are not limited to, pyridyl (pyridinyl), pyrimidinyl, furanyl (furyl), thiazolyl, thienyl, pyrrolyl, pyrazolyl, imidazolyl, tetrazolyl, benzofuranyl, benzothiophenyl, indolyl, indolenyl, isoxazolinyl, isoxazolyl, quinolinyl, isoquinolinyl, benzimidazolyl, piperidinyl, 4-piperidonyl, pyrrolidinyl, 2-pyrrolidonyl, pyrrolinyl, tetrahydrofuranyl, tetrahydroquinolinyl, tetrahydroisoquinolinyl, decahydroquinolinyl or octahydroisoquinolinyl, azocinyl, triazinyl, 6H-1,2,5-thiadiazinyl, 2H,6H-1,5,2-dithiazinyl, thianthrenyl, pyranyl, isobenzofuranyl, chromenyl, xanthenyl, phenoxathiinyl, 2H-pyrrolyl, pyrrolyl, imidazolyl, pyrazolyl, isothiazolyl, isoxazolinyl, isoxazolyl, oxazolyl, pyridinyl, pyrazinyl, pyrimidinyl, pyridazinyl, indolizinyl, isoindolyl, 3H-indolyl, indolyl, 1H-indazolyl, purinyl, 4H-quinolizinyl, isoquinolinyl, quinolinyl, phthalazinyl, naphthyridinyl, quinoxalinyl, quinazolinyl, cinnolinyl, pteridinyl, 4aH-carbazole, carbazole, .beta.-carbolinyl, phenanthridinyl, acridinyl, perimidinyl, phenanthrolinyl, phenazinyl, phenarsazinyl, phenothiazinyl, furazanyl, phenoxazinyl, isochromanyl, chromanyl, pyrrolidinyl, pyrrolinyl, imidazolidinyl, imidazolinyl, pyrazolidinyl, pyrazolinyl, piperidinyl, piperazinyl, indolinyl, isoindolinyl, quinuclidinyl, morpholinyl or oxazolidinyl. Also included are fused ring and spiro compounds containing, for example, the above heterocycles.

As used herein, the term "heteroaryl" refers to aromatic heterocyclic groups. Such heteroaryl groups are preferably 5-6 membered monocyclic groups or 8-10 membered fused bicyclic groups. Examples of such heteroaryl groups include, but are not limited to pyridyl (pyridinyl), pyrimidinyl, furanyl (furyl), thiazolyl, thienyl, pyrrolyl, pyrazolyl, imidazolyl, indolyl, isoxazolyl, oxazolyl, pyrazinyl, pyrimidinyl, pyridazinyl, benzofuranyl, benzothienyl, benzimidazolyl, quinolinyl, or isoquinolinyl.

As used herein, "pharmaceutically acceptable salts" refer to derivatives of the disclosed compounds wherein the parent compound of Formula Ia, Ib or Ic is modified by making acid or base salts of the compound of Formula Ia, Ib or Ic. Examples of pharmaceutically acceptable salts include, but are not limited to, mineral or organic acid salts of basic residues such as amines; alkali or organic salts of acidic residues such as carboxylic acids; and the like.

"Prodrugs" are considered to be any covalently bonded carriers which release the active parent drug according to Formula Ia, Ib or Ic in vivo when such prodrug is administered to a mammalian subject. Prodrugs of the compounds of Formula Ia, Ib or Ic are prepared by modifying functional groups present in the compounds in such a way that the modifications are cleaved, either in routine manipulation or in vivo, to the parent compounds. Prodrugs include compounds of Formula Ia, Ib or Ic wherein hydroxyl, amino, sulfhydryl, or carboxyl groups are bonded to any group that, when administered to a mammalian subject, cleaves to form a free hydroxyl, amino, sulfhydryl, or carboxyl group respectively. Examples of prodrugs include, but are not limited to, acetate, formate and benzoate derivatives of alcohol and amine functional groups in the compounds of Formula Ia, Ib or Ic, and the like. Examples of representative carboxyl and amino prodrugs are included under the definition of R.sup.2, R.sup.3, and Y.

The pharmaceutically acceptable salts of the compounds of Formula Ia, Ib or Ic include the conventional non-toxic salts or the quaternary ammonium salts of the compounds of Formula Ia, Ib or Ic formed, for example, from non-toxic inorganic or organic acids. For example, such conventional non-toxic salts include those derived from inorganic acids such as hydrochloric, hydrobromic, sulfuric, sulfamic, phosphoric, nitric and the like; and the salts prepared from organic acids such as acetic, propionic, succinic, glycolic, stearic, lactic, malic, tartaric, citric, ascorbic, pamoic, maleic, hydroxymaleic, phenylacetic, glutamic, benzoic, salicylic, sulfanilic, 2-acetoxybenzoic, fumaric, toluenesulfonic, methanesulfonic, ethanesulfonic, ethanedisulfonic, oxalic, isethionic, and the like.

The pharmaceutically acceptable salts of the present invention can be synthesized from the compounds of Formula Ia, Ib or Ic which contain a basic or acidic moiety by conventional chemical methods. Generally, the salts are prepared by reacting the free base or acid with stoichiometric amounts or with an excess of the desired salt-forming inorganic or organic acid or base in a suitable solvent or various combinations of solvents.

The pharmaceutically acceptable salts of the acids of Formula Ia, Ib or Ic may be prepared by reacting the acid with an appropriate amount of a base, such as an alkali or alkaline earth metal hydroxide e.g. sodium, potassium, lithium, calcium, or magnesium, or an organic base such as an amine, e.g., dibenzylethylenediamine, trimethylamine, piperidine, pyrrolidine, benzylamine and the like, or a quaternary ammonium hydroxide such as tetramethylammonium hydroxide and the like.

As discussed above, pharmaceutically acceptable salts of the compounds of the invention can be prepared by reacting the free acid or base forms of these compounds with a stoichiometric amount of the appropriate base or acid, respectively, in water or in an organic solvent, or in a mixture of the two; generally, nonaqueous media like ether, ethyl acetate, methanol, ethanol, isopropanol, or acetonitrile are preferred. Lists of suitable salts are found in Remington's Pharmaceutical Sciences, 17th ed., Mack Publishing Company, Easton, Pa., 1985, p. 1418, the disclosure of which is hereby incorporated by reference.

The disclosures of all of the references cited herein are hereby incorporated herein by reference in their entirety.

Synthesis

The compounds of the present invention can be prepared in a number of ways well known to one skilled in the art of organic synthesis. The compounds of the present invention can be synthesized using the methods described below, together with synthetic methods known in the art of synthetic organic chemistry, or variations thereon as appreciated by those skilled in the art. Preferred methods include, but are not limited to, those described below. All references cited herein are hereby incorporated in their entirety herein by reference.

Compounds of Formula Ia, Ib or Ic wherein X.sup.1, X.sup.2, X.sup.3 and X.sup.4 are all carbon and W is C(.dbd.O)NH can be prepared from appropriately substituted 4-, 5-, 6-, or 7-alkoxycarbonyl indazoles, IIIa, wherein R is an alkyl group such as methyl, ethyl or tert-butyl. ##STR42##

The requisite indazoles can be conveniently prepared from the commercially available nitrotoluic acids according to the example shown in Scheme 1. Conversion of the acid 1a to a suitable ester, such as the ethyl ester 1b, may be carried out by one of many methods well-known to one skilled in the art of organic synthesis, for example treatment with a suitable base, such as sodium bicarbonate, in a suitable solvent, such as N,N-dimethylformamide, followed by treatment with an alkyl halide, such as iodoethane. Reduction of the nitro group of 1b can be effected in a number of ways known to one skilled in the art of organic synthesis, including treatment with tin(II) chloride in ethanol. The resulting aniline derivative can be converted to the desired substituted indazole IIIa according to the method of Bartsch and Yang (J. Heterocycl. Chem. 1984, 21(4): 1063-1064). A variation of the conversion of the aniline 1c to the indazole IIIa proceeds through an N-acylated intermediate 1d followed by cyclization and deacetylation, according to the method reported by Ruchardt and Hassmann (Liebigs Ann. Chem. 1980, 908-927).

The order of the esterification and reduction steps may be reversed, such that the nitrotoluic acid is first converted to an aminotoluic acid, which is then esterified. In some cases other intermediates related to those shown in Scheme 1 are commercially available or may be prepared using methods described in the literature of organic chemistry; in these cases transformations similar to those shown in Scheme 1 may be used to prepare the desired compounds IIIa. For example, commercially available methyl 3-amino-4-methylbenzoate may be directly transformed into 6-methoxycarbonylindazole. ##STR43##

Compounds of Formula Ia or Ib wherein one or more of X.sup.1, X.sup.2, X.sup.3 or X.sup.4 are nitrogen may be prepared from the corresponding alkoxycarbonylindazoles IIIb in which the appropriate carbon atom or atoms have been replaced by nitrogen. These may in turn be prepared by substitution of the appropriately substituted heterocycle for the nitrotoluic acids, nitrotoluic acid esters, or aminotoluic acid esters in Scheme 1 above. The starting heterocycles could be obtained by following the procedures and methods in references outlined below, along with implementation of standard functional group transformations well known to one skilled in the art. ##STR44##

Functionalized pyrazines could be prepared according to procedures outlined in The Chemistry of Heterocyclic Compounds: The Pyrazines, Vol. 41 (Arnold Weissberger and Edward C. Taylor, Eds.),. John Wiley and Sons (New York: 1982). Preparation of appropriately functionalized pyridazines could be achieved using the methods described in The Chemistry of Heterocyclic Compounds: Condensed Pyridazines Including Cinnolines and Phthalazines, Vol. 27 (Arnold Weissberger and Edward C. Taylor, Eds.), John Wiley and Sons (New York: 1973) and The Chemistry of Heterocyclic Compounds: Pyridazines, Vol. 28 (Arnold Weissberger and Edward C. Taylor, Eds.), John Wiley and Sons (New York: 1973). For the synthesis of functionalized pyrimidines one could follow procedures in The Chemistry of Heterocyclic Compounds: The Pyrimidines, (Arnold Weissberger, Consulting Ed.) John Wiley and Sons (New York: 1962), The Chemistry of Heterocyclic Compounds: The Pyrimidines, Supplement I, (Arnold Weissberger and Edward C. Taylor, Consulting Eds.) John Wiley and Sons (New York: 1970), and The Chemistry of Heterocyclic Compounds: The Pyrimidines, Supplement II, Vol. 16 (Arnold Weissberger and Edward C. Taylor, Consulting Eds.) John Wiley and Sons (New York: 1985). Functionalized pyridines which can serve as starting materials in Scheme 1 could be made by the methods described in The Chemistry of Heterocyclic Compounds: Pyridine and Its Derivatives, Part Four, (Arnold Weissberger, Consulting Ed.) John Wiley and Sons (New York: 1964), The Chemistry of Heterocyclic Compounds: Pyridine and Its Derivatives, Supplement Part Two, (Arnold Weissberger and Edward C. Taylor, Consulting Eds.) John Wiley and Sons (New York: 1974), The Chemistry of Heterocyclic Compounds: pyridine and Its Derivatives, Supplement Part Three, Vol. 14 (Arnold Weissberger and Edward C. Taylor, Consulting Eds.) John Wiley and Sons (New York: 1974), The Chemistry of Heterocyclic Compounds: Pyridine and Its Derivatives, Supplement Part Four, Vol. 14 (Arnold Weissberger and Edward C. Taylor, Consulting Eds.) John Wiley and Sons (New York: 1975), and The Chemistry of Heterocyclic Compounds: Pyridine and Its Derivatives, Part Five, Vol. 14 (Arnold Weissberger and Edward C. Taylor, Consulting Eds.) John Wiley and Sons (New York: 1984). One example of the preparation of an appropriately substituted pyridine starting material is the preparation of 2-methyl-3-aminopyridine-5-carboxylic acid half-sulfate salt, as described by Argoudelis and Kummerow (J. Org. Chem. 1961, 26: 3420-3422).

Compounds of Formula Ia wherein R.sup.10 is not hydrogen may be prepared from appropriately substituted alkoxycarbonylindazoles. Some such substituted alkoxycarbonylindazoles may be prepared using the method outlined in Scheme 1. For example, methyl 4-amino-3-ethylbenzoate may be prepared as described by Witte and BoekeOheide (J. Org. Chem. 1972, 37 (18): 2849-2853) This compound may be converted to the diazonium fluoroborate and cyclized to 3-methyl-2-methoxycarbonylindazole using the method outlined in Scheme 1. This compound may be used as a starting material for preparation of the corresponding compounds of Formula Ia wherein R.sup.10 is methyl.

Other substituted alkoxycarbonylindazoles may be prepared from unsubstituted alkoxycarbonylindazoles using the methods outlined in Scheme 2. For example, an ethoxycarbonylindazole may be brominated by treatment with bromine in a suitable solvent, such as acetic acid, to provide the corresponding 3-bromo-ethoxycarbonyl-indazole IIIc. This compound may be coupled with a suitable reagent, alternatively followed by additional synthetic manipulations, to provide the desired 3-substituted-ethoxycarbonylindazole. For example, coupling with phenylboronic acid in the presence of tetrakis-(triphenylphosphine)palladium and triethylamine in N,N-dimethylformamide, using the method of Miyaura, Suginome and Suzuki (Tetrahedron 1983, 2: 3271) provides the corresponding 3-phenyl-ethoxycarbonylindazole IIId. Similar methods, starting from compounds of Formula IIIb, may be used to prepare the corresponding compounds wherein one or more of the ring carbons (corresponding to those designated X.sup.1, X.sup.2, X.sup.3 and X.sup.4 in Formula Ia) are replaced by nitrogen. ##STR45##

As another example, also shown in Scheme 2, coupling of IIIc with phenylacetylene in the presence of bis-(triphenylphosphine)palladium(II) chloride, copper(I) chloride, and triethylamine in pyridine according to the method of Melissaris and Litt (J. Org. Chem. 1992, 57: 6998-6999) provides the corresponding 3-(2-phenylethynyl)-ethoxycarbonylindazole IIIe, which may be reduced using hydrogen in the presence of palladium on charcoal to provide the corresponding 3-(2-phenyl-ethyl)ethoxycarbonylindazole IIIf. Similar methods, starting from compounds of Formula IIIb, may be used to prepare the corresponding compounds wherein one or more of the ring carbons (corresponding to those designated X.sup.1, X.sup.2, X.sup.3 and X.sup.4 in Formula Ia) are replaced by nitrogen.

Compounds IIIc, IIId, IIIe and IIIf may be used in the preparation of compounds of Formula Ia in which R.sup.10 is phenyl, 2-phenylethynyl, or 2-phenylethyl, respectively. Alternatively, further manipulations of the substituent may be accomplished at a later stage in the synthesis of the compound of Formula Ia. For example, the 2-phenylethynyl indazoles IIIe may be used in a synthetic sequence during the course of which the acetylene will be reduced, providing ultimately compounds of Formula Ia in which R.sup.10 is 2-phenylethyl.

Other appropriately substituted alkoxycarbonylindazoles, for use in the preparation of compounds of Formula Ia wherein R.sup.10 is not hydrogen, may be prepared using other methods known in the art of organic synthesis, such as those outlined in The Chemistry of Heterocyclic Compounds: Pyrazoles, Pyrazolines, Pyrazolidines, Indazoles and Condensed Rings, Vol. 22 (Arnold Weissberger, Ed.), John Wiley and Sons (New York: 1967), Chapter 10.

Hereinafter, unless otherwise specified, phrases such as "indazoles III" and "indazoles of Formula III" are meant to include simple indazoles IIIa, mono- or diazaindazoles IIIb, and substituted indazoles such as but not restricted to IIIc, IIId, IIIe and IIIf. Substituted mono- and diazaindazoles such as but not restricted to mono- and diaza analogs of IIIc, IIId, IIIe and IIIf are also included.

Compounds of Formula Ia may be prepared from indazoles III as outlined in Scheme 3. Alkylation of the indazoles of Formula III with a suitably functionalized alkyl halide can be effected in a variety of ways known to one skilled in the art. For example, using a method similar to that described by Granger et al. (Chim. Ther. 1970, 5: 24), an indazole of Formula III is treated with a suitable base, such as potassium bis(trimethylsilyl) amide, followed by addition of the alkyl halide, for example, 3-bromopropylphthalimide. Alternately, the alkylation can be carried out utilizing Mitsunobu conditions (Mitsunobu, Synthesis, 1981, 1-28) by addition of the corresponding alcohol, 3-hydroxypropylphthalimide, to a mixture of diethyl azodicarboxylate and triphenylphosphine in a suitable solvent, usually dry tetrahydrofuran, followed by addition of the indazole III. Separation, if necessary, of the mixture of 1- and 2-substituted isomers by chromatography provides the desired 1-alkylated product 3a. Removal of the phthalimide may be achieved by treatment with anhydrous hydrazine to give the primary amine 3b. ##STR46##

As further shown in Scheme 3,2-imidazolinyl-aminoalkylindazoles may be prepared by treatment of the amine 3b with a suitable reagent such as 2-methylthio-4,5-dihydroimidazolium iodide. Hydrolysis of the ester, using conventional methods known to one skilled in the art of organic synthesis, may be followed by coupling of the resulting acid to an appropriately substituted .alpha.- or .beta.-amino ester such as a compound of Formula IV, to provide an intermediate which, after deprotection, affords compounds of Formula Ia wherein R.sup.1 is 2-imidazolinylaminoalkyl. The coupling may be carried out using any of the many methods for the formation of amide bonds known to one skilled in the art of organic synthesis. Those methods include, but are not limited to, use of standard coupling procedures such as the azide method, mixed carbonic acid anhydride (isobutyl chloroformate) method, carbodiimide (dicyclohexylcarbodiimide, diisopropylcarbodiimide, or water-soluble carbodiimides (WSCDI)) method, active ester (p-nitrophenyl ester, N-hydroxysuccinic imido ester) method, or by the use of one of many other known coupling reagent such as BOP-Cl. Some of these methods (especially the carbodiimide method) can be enhanced by the addition of 1-hydroxybenzotriazole to the reaction mixture.

An alternative method for preparing amines 3b wherein n=3 is outlined in Scheme 4. Alkylation of the indazole III may be achieved by treatment with an optionally substituted acrylonitrile in the presence of a catalytic amount of a base such as sodium ethoxide or sodium bis(trimethylsilyl)amide, in a suitable solvent such as ethanol, to provide the intermediate nitrile 4a. This may be converted to the amine 3b by reduction using any of a number of methods known to one skilled in the art of organic synthesis, such as by treatment with hydrogen in the presence of a catalyst such as palladium on charcoal. An acid such as aqueous hydrochloric acid may be added to the reaction mixture to minimize side reactions during the reduction. ##STR47##

Appropriately substituted racemic .beta.-amino acids IV (used in Scheme 3) may be purchased commercially or, as is shown in Scheme 5, Method 1, prepared from the appropiate aldehyde, malonic acid and ammonium acetate according to the procedure of Johnson and Livak (J. Am. Chem. Soc., 1936, 58, 299). Racemic .beta.-substituted-.beta.-amino esters may be prepared through the reaction of dialkylcuprates or alkyllithiums with 4-benzoyloxy-2-azetidinone followed by treatment with anhydrous ethanol (Scheme 5, Method 2) or by reductive amination of .beta.-keto esters as is described in WO93/16038 (also see Rico et al., J. Org. Chem., 1993, 58, 7948-51). Enantiomerically pure .beta.-substituted-.beta.-amino acids can be obtained through the optical resolution of the racemic mixture or can be prepared using numerous methods, including: Arndt-Eistert homologation of the corresponding .beta.-amino acids as shown in Scheme 5, Method 3 (see Meier and Zeller, Angew. Chem. Int. Ed. Engl., 1975 14, 32; Rodriguez et al., Tetrahedron Lett., 1990, (31), 5153; Greenlee, J. Med. Chem. 1985, 28, 434 and references cited within); and through an enantioselective hydrogenation of a dehydroamino acid as is shown in Scheme 5, Method 4 (see Asymmetric Synthesis, Vol. 5, (Morrison, ed.) Academic Press, New York: 1985). A comprehensive treatise on the preparation of .beta.-amino acid derivatives may be found in patent application WO 93/07867, the disclosure of which is hereby incorporated by reference. ##STR48##

The synthesis of N.sup.2 -substituted diaminopropionic acid derivatives IV can be carried out via Hoffmann rearrangement of a wide variety of asparagine derivatives as described, for example, by Waki et al. (Synthesis 1981, 266-267) or by Moore et al. (J. Med. Chem. 1976, 19(6), 766-772). An example is shown in Scheme 6, Method 1. They may also be prepared by manipulations, which will be familiar to one skilled in the art of organic synthesis, of the commercially available 3-amino-2-benzyloxycarbonylaminopropionic acid. An example is shown in Scheme 6, Method 2. ##STR49##

Compounds of Formula Ia above wherein R.sup.1 is 2-pyridinylaminoalkyl may be prepared by the method outlined in Scheme 7. Treatment of the intermediate aminoalkylindazole 3b from Scheme 3 (or the corresponding salt from Scheme 4) with 2-chloropyridine N-oxide hydrochloride, using a modification of the method described by Misra, et al. (Bioorg. and Med. Chem. Letters, 1994, 4, 2165-2170), and subsequent reduction of the resulting N-oxide derivative 7a provides a 2-pyridinylaminoalkyl intermediate 7b. This reduction may be performed using a number of methods known to one skilled in the art of organic synthesis, such as that using ammonium formate in the presence of 10% palladium on charcoal in refluxing ethanol, as described by Balicki (Synthesis, 1989, 645-646), or by reduction with hydrogen in the presence of a catalyst such as palladium on charcoal or Raney nickel, or by treatment with triphenylphosphine. The resulting 2-aminopyridine moiety of 7b may be optionally protected, for example by treatment with di-t-butyldicarbonate in dry tetrahydrofuran in the presence of a suitable base, such as triethylamine or N,N-dimethylaminopyridine, using the method of Iwanowicz (Synth. Commun., 1993, 23(10), 1443-1445), to provide intermediate 7c. Ester hydrolysis, coupling and deprotection as outlined in Scheme 3 can then provide the desired compounds of Formula Ia. ##STR50##

An alternative route to 1-(heteroarylaminoalkyl)indazoles of Formula Ia is outlined in Scheme 8. A suitable indazole III can be alkylated with an alkyl halide bearing a protected aldehyde, such as a 1,3-dioxolane, using conditions described above (see Scheme 3) to provide 8a. Deprotection to the aldehyde 8b, for example by treatment with aqueous acid, may be followed by reductive amination with a heteroarylamine such as 2-aminopyridine or a suitably protected 2-aminoimidazole, such as 1-triphenylmethyl-2-aminoimidazole, in the presence of a reducing agent such as sodium triacetoxyborohydride or sodium cyanoborohydride, to provide the 1-(heteroarylaminoalkyl)indazole 8c. The intermediates 8c can then be elaborated to the corresponding compounds of Formula Ia, for example as described in Scheme 3. ##STR51##

A route to 1-(heteroarylaminocarbonylethyl) 10 indazoles of Formula Ia is outlined in Scheme 9. A suitable indazole III can be alkylated by treatment with an acrylic acid ester such as tert-butyl acrylate, using a method such as that described in Scheme 4. Removal of the ester of 9a may be followed by conversion to a heteroaryl amide by treatment with a heteroaryl amine using any of a number of methods well known to one skilled in the art of organic synthesis. The resulting 1-(heteroarylaminocarbonylethyl)indazole 9b can then be elaborated to the corresponding compounds of Formula Ia, for example as described in Scheme 3. ##STR52##

Compounds of Formula Ib may be prepared according to the method outlined in Scheme 10. Thus, the appropriate indazole III may be alkylated by treatment with a suitable base, for example sodium hydride, followed by addition of a suitable alkylating agent such as an alkyl halide R.sup.9 -Br or R.sup.9 -I. Bromination of the intermediate 10a using, for example, bromine in acetic acid, provides the corresponding 3-bromo derivative 10b. (The order of these two synthetic steps may also be reversed. That is, the indazole III may be brominated, and resulting bromoindazole may be alkylated, to provide similar products 10b.) Coupling of 10b with, for example, 3,3-diethoxy-1-propyne, under conditions similar to those described by Sakamoto et al. (Synthesis 1992, 746-748) provides a functionallzed alkynyl derivative 10c. Reduction of the acetylenic bond of 10c using, for example, hydrogen in the presence of a catalyst such as palladium on charcoal, followed by hydrolysis of the acetal with aqueous acid provides an aldehyde intermediate 10d which, using methods analogous to those outlined in Scheme 8, may be elaborated to an intermediate 10e containing a heteroarylaminoalkyl substituent at the 3-position. This intermediate may then in turn be elaborated to the desired compounds of Formula Ib, for example using methods described in Scheme 3. ##STR53##

Compounds of Formula Ib may alternatively be prepared from the intermediate 10b to the method described in Scheme 11. Thus,coupling of 10b under conditions similar to those described by Murakami et al. (Heterocycles, 1990, 31(8), 1505-11) can provide a 3-allyl derivative 11a. Hydroboration as described by Brown and Subba Rao (J. Am. Chem. Soc. 81, 6428-6433) can provide the alcohol 11b, which may be subjected to the Mitsunobu reaction (vide supra) with phthalimide followed by deprotection to provide an amine intermediate 11c which, analogously to the method shown in Schemes 10 and 3, can be elaborated to the desired compounds of Formula Ib. Alternatively, the intermediate 11b may be prepared by reduction of the aldehyde 10d shown in Scheme 10. Other methods can be used for the conversion of intermediates 10d and 11b to the primary amine 10c which are known to those skilled in the art of organic synthesis. ##STR54##

Compounds of Formula Ic may be prepared according to methods outlined in Scheme 12. Treatment of the appropriate indazole starting material 12a with zinc bromide and vinylmagnesium bromide followed by dichloro�1,1'-bis(diphenylphosphino)ferrocene! palladium (II), using a procedure similar to that described by Brown, et al. (U.S. Pat. No. 4,898,863), can provide the desired 3-vinyl derivative 12b. Treatment of this compound with ozone (F. J. Brown, et al. Ibid.), can provide an aldehyde 12c. Oxidation using silver(I) oxide, as described by Campaigne and LeSuer (Organic Syntheses, 1963, Coll. Vol. 4, 919), can provide the desired carboxylic acid 12d. Esterification and deprotection of the ether oxygen of 12e using boron tribromide, by a method analogous to that detailed by Manson and Musgrave (J. Chem. Soc. 1011 (1963)), can provide the hydroxy intermediate 12f. Mitsunobu coupling, (vide supra), followed by further transformations of 12g similar to those shown in Scheme 3, can provide compounds of Formula Ic. ##STR55##

Additional alcohols useful for the preparation of compounds of Formula Ia, Ib and Ic through the Mitsunobu reaction described in the above schemes may be prepared as described in Scheme 13. ##STR56##

Various compounds of Formula Ia, Ib or Ic may be prepared from a common derivative of the corresponding compounds of Formula Ia, Ib or Ic by functional group manipulations familiar to one skilled in the art of organic synthesis. As one example, preparation of compounds of Formula Ia having different sulfonamide substituents at R.sup.16 may be achieved as outlined in Scheme 14. Thus, the compound of Formula Ia having a benzyloxycarbonylamino group at R.sup.16 (14a) may be hydrogenolyzed using, for example, hydrogen in the presence of a catalyst such as palladium on charcoal to provide the primary amine derivative 14b. This may be reacted with a sulfonylating agent such as R.sup.17 SO.sub.2 Cl in the presence of an amine such as triethylamine to provide, after deprotection of the ester, the desired compound of Formula Ia. In place of the sulfonyl chloride, use of a carboxylic acid, acid chloride or acid anhydride can provide the corresponding amide derivative, use of a chloroformate can provide the corresponding carbamate derivative, use of a sulfamoyl chloride can provide the corresponding sulfamide derivative, and use of an isocyanate can provide the corresponding urea derivative. ##STR57##

As another example, compounds of Formula Ia with different variations in R.sup.1 may be prepared from a common precursor as outlined in Scheme 15. Thus, the amine intermediate 3b may be reacted, for example, with benzyl chloroformate to provide the benzyl carbamate. Hydrolysis of the ester, for example with lithium hydroxide, can provide the acid intermediate 15a. Using methods described earlier, 15a may be reacted with, for example, a suitable beta-amino ester, followed by removal of the benzyl carbamate, for example by hydrogenolysis, to provide the amine intermediate 15b. Using, for example, steps analogous to those shown in Schemes 3 or 7, the amine may be converted to an aminoheterocyclic group. After deprotection of the ester, the desired compound of Formula Ia may be obtained. ##STR58##

The example outlined in Scheme 15 will also serve to demonstrate that the order in which the different substituents are elaborated to give the compounds of Formula Ia, Ib and Ic may be varied from that in the examples shown in Schemes 1 through 14. This example will also serve to demonstrate the use of protecting groups to temporarily protect a functional group in the course of a synthetic sequence when that functional group is not compatible with one or more of the synthetic transformations that are to be accomplished. Such use of protecting groups, while not always explicitly shown in Schemes 1 through 15, is well known to one skilled in the art of organic synthesis. Many examples of protecting groups may be found, for example, in Greene, "Protective Groups in Organic Syntheses", Wiley (New York), 1981.

The detailed processes for preparing the compounds of Formula Ia, Ib or Ic are illustrated by the following Examples. It is, however, understood that this invention is not limited to the specific details of these examples. Reactions were run under an atmosphere of nitrogen unless otherwise indicated. Solvent removal from reaction mixtures, extracts, and the like was performed under vacuum on a rotary evaporator. Flash chromatography refers to the medium-pressure column chromatography method described by Still et al. (J. Org. Chem. 1978, 43(14), 2923-2925). Melting points (mp) are uncorrected. Proton nuclear magnetic resonance spectra (NMR) were measured in chloroform-d (CDCl.sub.3), dimethyl sulfoxide-d.sub.6 (DMSO-d.sub.6) or methanol-d.sub.4 (MeOH-d.sub.4) and the peaks are reported in parts per million downfield from tetramethylsilane (.delta.). The coupling patterns are reported as follows: s, singlet; d, doublet; t, triplet; q, quartet; m, multiplet; b, broad. Mass spectra were measured using electrospray ionization (ESI),. ammonia chemical ionization (NH.sub.3 --CI), fast-atom bombardment from a glycol matrix (FAB), or electron impact ionization (EI).

EXAMPLE 1035b

3-�1-�3-(N-imidazol-2-ylamino)propyl!-indazol-5-ylcarbonyl-amino!-2(S)-(2 6-dimethyl-4-phenylbenzene-sulfonylamino)-propionic acid trifluoroacetate

A. tert-Butyl 3-�1-�3-(N-(1-triphenylmethylimidazol-2-yl)-amino)propyl!-indazol-5-ylcarbonylamino!-2(S)-(2,4,6-trimethylbenzenesulfonylamino)propionate

A mixture of the product prepared according to Example 1050e Part K (215 mg, 407 .mu.mol, the product prepared according to Example 1178b Part E (140 mg, 407 .mu.mol), 1-hydroxybenzotriazole hydrate (57 mg, 407 .mu.mol) and N, N-dimethylformamide (5 .mu.L) was treated with dicyclohexylcarbodiimide (870 mg, 407 .mu.mol) and stirred at room temperature for 24 h. The mixture was poured into water (75 mL) and extracted with ethyl acetate (3.times.50 mL) The organic phase was drIed (MgSO.sub.4) and concentrated under vacum. The residue was flash chromatographed (toluene:ethyl acetate, step gradient from 50:50 to 10:90) to provide the title product (262 mg, 75%) as a colorless glassy foam: .sup.1 H NMR (CDCl.sub.3).delta.8.17 (s, 1H), 7.97 (d, 1H), 7.73 (dd, 1H), 7.4-7.1 (15H), 6.99 (d, 1H), 6.94 (s, 2H), 6.85 (bt, 1H), 6.68 (d, 1H), 6.42 (d, 1H) 5.82 (bd, 1H), 4.07 (t, 2H), 3.93 (m, 1H), 3.83 (m, 1H), 3.62 (m, 1H), 3.04 (m, 1H), 2.97 (m, 2H), 2.65 (s, 6H), 2.26 (s, 3H) 1.82 (m, 2H), 1.32 (s, 9H); Mass spectrum (ESI) m/z 852.4 (100%, M+H.sup.+).

Alternatively, a solution of the product prepared according to Example 1050e Part K (1.108 g, 2.1 mmol) in N,N-dimethylformamide (15 mL) was treated with the product prepared according to Example 1178b Part E (719 mg, 2.1 mmol), BOP reagent (975 mg, 2.2 mmol and diisopropylethyl-amine (543 mg, 4.2 mmol) and the mixture was stirred at room temperature overnight. The mixture was concentrated under vacuum and the residue was partitioned between ethyl acetate (100 mL) and water (25 mL). The aqueous phase was extracted with additional ethyl acetate (3.times.25 mL) and the combined organic phases were washed with hydrochloric acid (1.0N; 10 mL), water (2.times.10 mL), saturated aqueous sodium bicarbonate (10 mL) and brine (2.times.10 mL) then were dried (MgSO.sub.4) and concentrated wider vacuum. This material was combined with the crude product from another run, starting from 10.8 g of the product prepared according to Example 1050e Part K (20.5 mmol), to provide the title product as a crude material; (23.0 g) which was used in the next step without purification.

B. tert-Butyl 3-�1-�3-(N-imidazol-2-ylamino)propyl!-indazol-5-ylcarbonylamino!-2(S)-(2,6-dimethyl-4-phenylbenzene-sulfonylamino)propionate

The product prepared according to Example 1035b Part A (3.3 g, 3.9 mmol) was combined with methanol (100 mL) and acetic acid (10 mL) and the mixture was heated at reflux overnight. The mixture was concentrated under vacuum, and the residue was flash chromatographed (chloroform: methanol:aqueous ammonia 100:10:1) to provide the product as a glassy foam. This was combined with the product from another run, starting from 19.0 g of the product prepared according to Example 1035b Part A (22.3 mmol), to provide the title product (4.5 g). Impure material from the column was re-chromatographed (chloroform: methanol:aqueous ammonia 100:5:0.5) to provide additional pure title product (6.5 g; total combined yield 81%): .sup.1 H NMR (MeOH-d.sub.4) .delta. 8.17 (d, 1H), 8.13 (d, 1H), 7.76 (dd, 1H), 7.57 (d, 1H), 6.85 (s, 2H), 6.51 (s, 2H), 4.53 (t, 2H), 4.06 (dd, 1H), 3.70 (dd, 1H), 3.50 (dd, 1H), 3.17 (t, 2H), 2.59 (S, 6H), 2.16 (m, 2H), 2.10 (s, 3H), 1.22 (s, 9H).

C. 3-�1-�3-(N-imidazol-2-ylamino)propyl!-indazol-5-yl-carbonylamino!-2(S)-(2,6-dimethyl-4-phenylbenzenesulfonyl-amino)propionic acid trifluoroacetate

A solution of the product prepared according to Example 1035b Part B (480 mg, 788 .mu.mol) in dichloromethane (30 mL) was treated with trifluoroacetic acid (5 mL) and stirred for 1 h at room temperature. The solution was concentrated under vacuum, and the residue was dissolved in methanol (3 mL) and purified by preparative reverse-phase HPLC to provide, after lyophilization, the title product (432 mg, 82%) as an amorphous white solid: HPLC T.sub.R 12.33 min (95%); .sup.1 H NMR (MeOH-d.sub.4) .delta. 8.12 (s, 2H), 7.72 (dd, 1H), 7.54 (d, 1H), 6.76 (s, 2H), 6.73 (s, 2H), 4.53 (t, 2H), 4.16 (dd, 1H), 3.76 (dd, 1H), 3.49 (dd, 1H), 3.23 (t, 2H), 2.56 (s, 6H), 2.22 (m, 2H), 1.98 (s, 3H); High resolution mass spectrum (FAB) calculated (M+H.sup.+) 554.2186, found 554.2196.

Alternatively, a solution of the product prepared according to Example 1035b Part A (249 mg, 292 .mu.mol) in trifluoroacetic acid (2.5 mL) was heated at reflux for 60 min. The mixture was as cooled and concentrated, and the residue was purified by preparative reverse-phase HPLC to provide, after lyophilization, the title product (153 mg, 78%) as a white powder.

EXAMPLE 1050e

3-�1-�3-(N-imidazol-2-ylamino)propyl!indazol-5-ylcarbonylamino!-2(S)-(2,6-dimethyl-4-phenylbenzenesulfonylamino)propionic acid trifluoroacetate

A. Ethyl 3-methyl-4-nitrobenzoate

A mixture of 3-methyl-4-nitrobenzoic acid (1) (362.3 g, 2.0 mol), N,N-dimethylformamide (2000 mL), sodium bicarbonate (200 g, 2.38 mol) and iodoethane (623.9 g, 4.0 mol) was stirred at 70.degree. C. for 18 h. The mixture was allowed to cool to room temperature and poured into water (2000 mL. The resulting solid was collected by filtration, washed with water and dried. The solid was washed further with hexane and dried to provide the title product (382.1 g, 91%) as an off-white solid: mp 51.degree.-52.5.degree. C.; .sup.1 H NMR (CDCl.sub.3) .delta. 8.04-7.98 (m, 3H), 4.42 (q, 2H), 2.63 (s, 3H), 1.42 (t, 3H); Mass spectrum (NH.sub.3 --CI) m/z 210 (100%, M+H.sup.+).

B. Ethyl 3-methyl-4-aminobenzoate

A mixture of the product prepared accordIng to Example 1050e Part A (183.96 g, 880 mol), tin (II) chloride hydrate (1025 g, 4.54 mol) and ethanol (3500 mL) was heated at reflux for 2 h. The mixture was cooled and diluted with water (3500 mL) and the pH was adjusted to 8.5. The mixture was diluted further with additional water, and extracted with ethyl acetate. The organic extracts were dried (MgSO.sub.4), filtered and concentrated to provide the title product (136.62 g, 87%) as an off-white solid: mp 76.degree.-78.degree. C.; .sup.1 H NMR (CDCl.sub.3) .delta. 7.78 (s, 1H), 7.76 (d, 1H), 6.63 (d, 1H), 4,31 (q, 2H), 3.99 (bs, 2H), 2.19 (s, 3H), 1.38 (t, 3H); High resolution mass spectrum (NH.sub.3 --CI) calculated (M+H.sup.+) 180.1025, found 180.1023.

C. 5-Ethoxycarbonylindazole

A mixture of the product prepared according to Example 1050e Part B (250.55 g, 1.4 mol, potassium acetate (143.3 g, 1.46 mol), acetic anhydride 285.9 g, 2.8 mol) and chloroform (ethanol free; 2700 mL) was stirred at room temperature. The temperature rose to 40.degree. C., then started to decline, at which time no starting material was detected by TLC. A mixture of 18-crown-6(75 g, 280 mmol) and n-amyl nitrite (364.5 g, 3.1 mol) was added and the mixture was heated at reflux overnight. The cooled mixture was washed with saturated aqueous sodium bicarbonate, then with water, and was dried (MgSO.sub.4), filtered and concentrated under vacuum. The residue was combined with that from another batch (711.3 g) and distilled through a 10 cm vigreax column under vacuum to provide 1-Acetyl-5-ethoxcarbonyl-indazole (576 g, 82%), bp 115.degree.-165.degree. C. (1.0 Torr). This intermediate was combined with hydrochloric acid (6N; 2000 mL) and ethanol (2000 mL), and the mixture was stirred overnight at room temperature. The mixture was concentrated under vacuum and the solid was combined with water. The PH of the mixture was adjusted to 8 with aqueous ammonia, and the mixture was extracted with dichloromethane. The organic phase was concentrated to provide a solid (460 g). This was recrystallized from acetonitrile (1000 mL), and the crystals were washed with ethanol, then hexane, and dried to provide 5 (281 g, 60%) as a tan solid: mp 122.degree.-124.degree. C.; .sup.1 H NMR (CDCl.sub.3) .delta. 10.23 (bs, 1H), 8.57 (s, 1H), 8.20 (s, 1H), 8.10 (d, 1H), 7.53 (d, 1H), 4.42 (q, 2H), 1.42 (t, 3H); High resolution mass spectrum (NH.sub.3 --CI) calculated (M+H.sup.+); 191.0821, found 191.0838.

D. 1-(2-(1,3dioxolan-2-yl)ethyl)-5-ethoxycarbonylindazole

A solution of the product prepared according to Example 1050e Part C (74.5 g, 397 mol: in anhydrous tetrahydrofuran (1000 mL) was treated sequentially with sodium bis(trimethylsilyl)amide (1.0M in tetrahydrofuran; 430 mL, 430 mmol), 18-crown-6 (1.5 g) and 2(2bromoethyl)-1,3-dioxolane (90 g, 496 mmol). The solution was heated at reflux for 20 h, then was cooled to room temperature. The solvent was removed under vacuum, and the residue partitioned between toluene (2000 mL) and water (1000 mL). The aqueous phase was further extracted with toluene (3.times.200 mL), and the combined organic phases were washed with water (3.times.200 mL) and brine (2.times.200 mL). The organic phase was dried (MgSO.sub.4) and concentrated under vacuum. The resulting oil was chromatographed with toluene, then with 185:15 toluene-ethyl acetate, to provide the title product (71.0 g, 55%): .sup.1 H NMR (CDCl.sub.3) .delta. 8.49 (s, 1H), 8.10 (s, 1H), 8.06 (d, 1H), 7.46 (d, 1H), 4.84 (t, 1H), 4.55 (t, 2H), 4.41 (q, 2H), 3.90 (m, 4H), 2.31 (m, 2H), 1.42 (t, 3H); High resolution mass spectrum (NH.sub.3 --CI) calculated (M+H.sup.+) 291.1345, found 291.1328.

E. 1-(3-oxopropyl) -5-ethoxycarbonylindazole

A mixture of the product prepared according to Example 1050e Part D (73.0 g, 256 mmol), acetic acid (365 g) and water (1020 mL) was heated at 70.degree. C. for 20 h. The mixture was cooled to room temperature, extracted with dichloromethane (5.times.550 mL), and the combined organic layers were washed cautiously with saturated aqueous sodium bicarbonate (until no more gases were evolved), then with water (2.times.250 mL) and brine (2.times.250 mL). The organic layer was dried (MgSO.sub.4), filtered and concentrated under vacuum to provide the title product (60.9 g, 98%) as a light yellow solid: .sup.1 H NMR (CDCl.sub.3) .delta. 9.87 (s, 1H), 8.50 (s, 1H), 8.10 (s+d, 2H), 7.51 (d, 1H), 4.70 (t, 2H), 4.41 (q, 2H), 3.19 (t, 2H), 1.42 (t, 3H); High resolution mass spectrum (NH.sub.3 --CI) calculated (M+H.sup.+) 247.1083, found 247.1068.

F. 2-Aminoimidazole

2Aminoimidazole sulfate (50 g, 378 mmol) was dissolved in methanol (1500 mL) and cooled to -78.degree. C. Sodium methoxide (20.44 g, 378 mmol) was added portionwise over 60 min. The mixture stirred at -78.degree. C. for 30 min, then at room temperature for 2.5 h. The solution was filtered through Celite.RTM. and concentrated under vacuum to provide 2-aminoimidazole as a semi-solid (32.5 g) which was used directly without further purification: .sup.1 H NMR (DMSO-d.sub.6) .delta. 6.32 (s, 2H), 5.0 (bs, 2H).

G. 2-Phthalimidoimidazole

A mixture of phthalic anhydride (57.3 g, 387.mmol) and the product prepared according to Example 1050e Part F (32.5 g, 387 mmol) was heated with mechanical stirring to 190.degree.-200.degree. C. for 20 min, then was placed under vacuum for 10 min. The mixture was cooled to room temperature and dried under vacuum for 24 h. This material (80 g, 99%) was used without further purification. It could be purified by flash chromatography (chloroform:methanol gradient from 95:5 to 80:20): .sup.1 H NMR (DMSO-d.sub.6) .delta. 12.35 (bs, 1H), 7.94-8.06 (m, 4H), 7.16 (bs, 2H); Mass spectrum (ESI) m/z 214.2 (100%, M+H.sup.+).

H. 1Triphenylmethyl-2-phthalimidoimidazole

A solution of the product prepared according to Example 1050e Part G (80 g, 375 mmol) in dichloromethane (200 mL) was treated with triphenylmethyl chloride (314 g, 1.126 mol) and triethylamine (151.8 g, 1.5 mol). The mixture was heated at reflux for 5.5 h, then cooled to room temperature and concentrated under vacuum. The residue was extracted several times with hexane/ethyl acetate (70:30). The residual solid was dissolved in dichloromethane and washed several times with water, dried (MgSO.sub.4) and concentrated. The residual solid was boiled in hexane, filtered, and the solid was washed several times with hot hexane until no trityl chloride was present by TLC. This provided the title product (119 g, 70%): .sup.1 H NMR (CDCl.sub.3) .delta. 7.64 (s, 4H), 7.28 (d, 6H), 7.17 (m, 7H), 7.06 (t, 3H),6.80 (d, 1H); Mass spectrum (NH.sub.3 --CI) m/z 456 (100%, M+H.sup.+).

I. 1-Triphenylmethyl-2aminoimidazole

A mixture of the product prepared according to Example 1050e Part H (114 g, 250 mmol), hydrazine (78. mL, 2.50 mol) and ethanol (3500 mL) was heated at reflux for 2 h. The mixture was cooled and the solvent was removed under vacuum. The solid residue was partitioned between water (500 mL) and chloroform (500 mL and the aqueous phase was extracted further with chloroform (3.times.200 mL). The combined organic layers were washed with water (2.times.200 mL), dried (MgSO.sub.4) and concentrated to provide a sticky solid. This was heated with hexane and filtered to provide the title product (65 g, 80%) as a granular solid: .sup.1 H NMR (DMSO-d.sub.6) .delta. 7.33-7.44 (m, 9H), 7.13 (d, 6H), 6.51 (d, 1H), 6.26 (d, 1H); Mass spectrum (NH.sub.3 --CI) 326 (100%, M+H.sup.+).

J. 1-�3-�N-(1-Triphenylmethylimidazol-2yl)amino!-propyl!-5-ethoxycarbonylindazole

A mixture of the product prepared according to Example 1050e Part E (10.0 g, 40.6 mmol), the product prepared according to Example 1050e Part I (13.2 g, 40.6 mmol) and toluene (500 mL) was heated at reflux under a Dean-Stark trap. Toluene (3.times.100 mL) was removed while adding fresh dry toluene. The mixture fleas then heated further for 20 h, when NMR analysis of an aliquot showed the absence of aldehyde. The mixture was cooled to room temperature and sodium triacetoxyborohydride (34.42 g, 162.4 mmol) was added. The mixture was stirred at room temperature for 20 h, then was poured into water (500 mL). The layers were separated and the aqueous phase was extracted with ethyl acetate (3.times.100 mL). The combined organics were washed with saturated aqueous sodium bicarbonate (2.times.100 mL), water (2.times.100 mL) and brine (2.times.100 mL), then were dried (MgSO.sub.4), fIltered and concentrated under vacuum to provide a crude product (25.0 g). This was combined with the crude product from another run (starting from 7.77 g of the product prepared according to Example 1050e Part E and 10.28 g of the product prepared according to Example 1050e Part I) and was purified by flash chromatography (toluene:ethyl acetate step gradient from 90:10 to 50:50) to provide the title product (21.0 g, 52%) as an oil which slowly solidified: .sup.1 H NMR (CDCl.sub.3) .delta. 8.45 (s, 1H), 7.97 (s, 1H) , 7.93 (d, 1H), 7.33 (m, 9H), 7.21 (m, 6H), 6.99 (d, 1H), 6.67 (d, 1H), 6.41 (d, 1H), 4.41 (q, 2H), 4.06 (t, 2H), 2.98 (m, 3H), 1.81 (m, 2H), 1.42 (t, 3H); High resolution mass spectrum (FAB) calculated (M+H.sup.+) 556.2713, found 556.2725.

K. 1-�3-�N-(1Triphenylmethylimidazol-2yl)amino!propylyl!-5-carboxyindazole

A mixture of the product prepared according to Example 1050e Part J (21.0 g, 37.8 mmol), ethanol (600 mL) and aqueous sodium hydroxide (1.0M; 209 mL, 209 mmol) was heated at reflux for 4 h. The mixture was cooled to room temperature and concentrated under vacuum to remove the ethanol. The pH of the residue was adjusted to 4, and the mixture was extracted with dichloromethane and the combined organic phases were dried (Na.sub.2 SO.sub.4). The mixture was filtered and the solids were washed with N,N-dimethylformamide to recover precipitated product. The combined filtrates were concentrated under vacuum and the residue was washed with ethanol and dried to provide the title product (16.9 g, 85%, as a white solid: .sup.1 H NMR (DMSO-d.sub.6) .delta. 8.39 (s, 1H), 8.13 (s, 1H), 7.87 (d, 1H), 7.36 (m, 10H), 7.12 (d, 6H), 6.51 (d, 1H), 6.28 (d, 1H), 4.05 (t, 2H), 2.84 (m, 2H), 1.63 (m, 2H); High resolution mass spectrum (FAB) calculated (M+H.sup.+) 528.2400, found 528.2418.

L. Methyl 3-�1-�3(N-(1-triphenylmethylimidazol-2-yl)amino)propyl!indazol-5-ylcarbonylamino!-2(S)-(2,6-dimethyl-4-phenylbenzenesulfonylamino)propionate

A mixture of the product prepared according to Example 1050e Part K (293 mg, 566 .mu.mol), methyl 3amino-2(S)-(2,6-dimethyl-4-phenylbenzenesulfonyl)aminopropionate hydrochloride (prepared according to the method of Example 3093 Parts J and K described below; 290 mg, 727 .mu.mol), N,N-dimethylformamide (7 mL), dicyclohexylcarbodiimide (115 mg, 557 .mu.mol), 1-hydroxybenzotriazole hydrate (76 mg, 562 .mu.mol) and triethylamine (230 .mu.L, 1.65 mmol) was stirred at room temperature for 42 h. The mixture was concentrated under vacuum and the residue was purified by flash chromatography (ethyl acetate) to provide the title product (507 mg) contaminated with dicyclohexylurea, which was used in the subsequent reaction without further purification: .sup.1 H NMR (CDCl.sub.3) .delta. 8.13 (s, 1H), 8.02 (s, 1H), 7.70 (d, 1H), 7.60-7.15 (22H), 6.98 (d, 1H), 6.87 (t, 1H), 6.67 (d, 1H), 6.41 (d, 1H), 6.08 (bs, 1H), 4.05 (t, 2H), 3.95 (m, 1H), 3.75 (m, 1H), 3.65 (s, 3H), 3.47 (m, 1H), 2.95 (m, 2H), 2.75 (s, 6H), 1.79 (m, 2H); High resolution mass spectrum (FAB) calculated (M+H.sup.+) 872.3594, found 872.3593.

M. 3-�1-�3-(N-imidazol-2-ylamino)propyl!-indazol-5-ylcarbonylamino!-2(S)-(2,6-dimethyl-4-phenylbenzene-sulfonylamino) propionic acid trifluoroacetate

A mixture of the product prepared according to Example 1050e Part L (469 mg, 540 .mu.mol), ethanol (13 mL) and aqueous sodium hydroxide (1.0M; 2.7 mL, 2.7 mmol) was heated at reflux for 90 min. The mixture was cooled to room temperature and concentrated, and the residue was taken up in trifluoroacetic acid (6 mL) and heated at reflux for 90 min. The mixture was cooled to room temperature and concentrated. The residue was purified by preparative reverse phase high pressure liquid chromatography (acetonitrile:water containing 0.05% trifluoroacetic acid; gradient from 10:90 to 90:10) to provide the title product (218 mg, 55%) as a white solid: .sup.1 H NMR (MeOH-d.sub.4) .delta. 8.06 (s, 1H), 7.95 (s, 1H), 7.63 (d, 1H), 7.34 (d, 1H), 7.28 (m, 5H), 7.09 (s, 2H), 6.75 (s, 2H), 4.34 (t, 2H), 4.27 (dd, 2H), 3.77 (dd, 1H), 3.47 (dd, 1H), 3.17 (t, 2H), 2.66 (s, 6H), 2.12 (m, 2H); High resolution mass spectrum (FAB) calculated (M+H.sup.+) 616.2342, found 616.2324.

EXAMPLE 1081

3-�1-�3-(N-pyridin-2-ylamino)propyl!indazol-5-ylcarbonylamino!-2(S)-(benzyloxycarbonylamino)propionic acid trifluoroacetate

A. 1-�3-(N-phthalimido)-propyl!-5-ethoxycarbonylindazole

A mixture of tetrahydrofuran (50 mL) and 18-crown-6 (100 mg) was stirred at room temperature. Potassium bis(trimethylsilyl)amide (0.5M in toluene; 46.6 mL, 23.3 mmol) was added, followed by the product prepared according to Example 1050e Part C (4.43 g, 23.3 mmol) dissolved in dry tetrahydrofuran (50 mL). Then N-(3-bromopropyl)phthalimide (6.24 g, 23.3 mmol) dissolved in dry tetrahydrofuran (50 mL) was added. The mixture was heated at reflux for 16 h. The mixture was allowed to cool to room temperature and poured into water (200 mL). The layers were separated and the aqueous layer was extracted with ethyl acetate. The organic layers were combined, dried over anhydrous magnesium sulfate, filtered and concentrated under vacuum. The residue was purified by flash chromatography (hexanes:ethyl acetate 50:50) to provide the title product (4.25 g, 48%) as a yellow solid: mp 122.degree.-124.degree. C.; .sup.1 H NMR (CDCl.sub.3) .delta. 8.48 (s, 1H), 8.06 (s, 1H), 8.04 (d, 1H), 7.82 (m, 2H), 7.71 (m, 2H), 7.42 (d, 1H), 4.44 (t, 2H), 4.40 (q, 2H), 3.80 (t, 2H), 2.40 (m, 2H), 1.42 (t, 3H); High resolution mass spectrum (NH.sub.3 --CI) calculated (M+H.sup.+) 378.1454, found 378.1430. Also obtained (as a more polar fraction) was 2-�3-(N-phthalimido)propyl!-5-ethoxycarbonylindazole (2,75 g, 31%) as a yellow solid: mp 133.degree.-135.degree. C.; .sup.1 H NMR (CDCl.sub.3) .delta. 8.48 (s, 1H), 8.25 (s, 1H), 7.85 (d, 1H), 7.81 (m, 2H), 7.70 (m, 2H), 7.61 (d, 1H), 4.50 (t, 2H), 4.40 (q, 2H), 3.78 (t, 2H), 2.47 (m, 2H), 1.43 (t, 3H); High resolution mass spectrum (NH.sub.3 --CI) calculated (M+H.sup.+) 378.1454, found 378.1430.

B. 1-(3-aminopropyl)-5-ethoxycarbonylindazole

A mixture of the product prepared according to Example 1081 Part A (2.10 g, 5.6 mmol), ethanol (35 mL), anhydrous tetrahydrofuran (35 mL) and anhydrous hydrazine (0.75 mL) was stirred at room temperature for 16 h. Dry tetrahydrofuran (100 mL) was added and the mixture was filtered. The filtrate was concentrated under vacuum. The residue was purified by flash chromatography (dichloromethane:methanol 90:10 containing 1% triethylamine) to provide the title product (1.25 g, 91%) as an orange syrup: .sup.1 H NMR (CDCl.sub.3) .delta. 8.51 (s, 1H), 8.10 (s, 1H), 8.06 (d, 1H), 7.46 (d, 1H), 4.52 (t, 2H), 4.41 (q, 2H), 2.68 (t, 2H), 2.06 (m, 2H), 1.47 (bs, 2H), 1.43 (t, 3H); High resolution mass spectrum (NH.sub.3 --CI) calculated (M+H.sup.+) 248.1399, found 248.1392.

C. 1-�3-�N-(1-oxido)pyridin-2-ylamino!propyl!-5-ethoxycarbonylindazole

A mixture of the product prepared according to Example 1081 Part B (600 mg, 2.4 mmol), 2-chloropyridine-N-oxide hydrochloride (806 mg, 4.9 mmol), sodium bicarbonate (816 mg, 9.7 mmol) and n-butanol (7 mL) was stirred at 100.degree. C. for 21 h. The mixture was allowed to cool to room temperature and was filtered. The filtrate was concentrated under vacuum. The residue was purified by flash chromatography (dichloromethane:methanol 95:5) to provide the title product (675 mg, 81%) as a pale yellow solid, mp 87.degree.-89.degree. C.: .sup.1 H NMR (CDCl.sub.3) .delta. 8.52 (s, 1H), 8.15 (s, 1H), 8.13 (d, 1H), 8.03 (d, 1H), 7.39 (d, 1H), 7.10 (t, 1H), 6.93 (bt, 1H), 6.56 (t, 1H), 6.41 (d, 1H), 4.57 (t, 2H), 4.40 (q, 2H), 3.24 (q, 2H), 2.38 (m, 2H), 1.40 (t, 3H); High resolution mass spectrum (NH.sub.3 --CI) calculated (M+H.sup.+) 341.1614, found 341.1622.

D. 1-�3-(N-pyridin-2-ylamino)propyl!-5-ethoxycarbonylindazole

A mixture of the product prepared according to Example 1081 Part C (62 mg, 182 .mu.mol), 10% palladium on charcoal (8 mg) and ethanol (0.5 mL) was stirred at room temperature. Ammonium formate (63 mg, 1.0 mmol) was added and the mixture heated to reflux for 30 min. Additional 10% palladium on charcoal (8 mg) and 6ammonium formate (63 mg, 1.0 mmol) were added and the reaction was continued at reflux for 4 h. The mixture was allowed to cool to room temperature, filtered through Celite.RTM. and the solids were rinsed with ethanol. The solvent was evaporated from the filtrate under vacuum. The residue was purified by flash chromatography (dichloromethane:methanol 95:5) to provide the title product (31 mg, 52%) as a glass: .sup.1 H NMR (CDCl.sub.3) .delta. 8.52 (s, 1H), 8.12 (s, 1H), 8.06 (m, 2H), 7.38 (m, 2H), 6.55 (dd, 1H), 6.32 (d, 1H), 4.70 (bm, 1H), 4.53 (t, 2H), 4.40 (q, 2H), 3.30 (q, 2H), 2.24 (m, 2H), 1.42 (t, 3H); High resolution mass spectrum (NH3--CI) calculated (M+H.sup.+); 325.1665, found 325.1659.

E. 1-�3-(N-tert-butyloxycarbonyl-N-pyridin-2-ylamino)-propyl!-5-ethoxycarbonylindazole

A mixture of the product prepared according to Example 1081 Part D (80 mg, 246 mol), dry tetrahydrofuran (4 mL), triethylamine (0.3 mL) and N,N-dimethylaminopyridine (5 mg) was stirred at 0.degree. C. Di-tert-butyldicarbonate (130 mg, 2.4 equiv.) was added and the mixture was stirred for 30 min. The ice bath was removed and the mixture was stirred at room temperature for 16 h. Additional di-tert-butyldicarbonate (130 mg, 2.4 equiv.) and N,N-dimethylaminopyridine (5 mg) were added and the mixture was stirred at room temperature for 72 h. The solvent was evaporated under vacuum and the residue was purified by flash chromatography (hexanes:ethyl acetate 65:35) to provide the title product (70 mg, 66%) as a clear oil: .sup.1 H NMR (CDCl.sub.3) .delta. 8.50 (s, 1H), 8.28 (m, 1H), 8.08 (s, 1H), 8.04 (d, 1H), 7.60 (m, 2H), 7.37 (d, 1H), 6.99 (m, 1H), 4.46 (t, 2H), 4.41 (q, 2H), 4.02 (t, 2H), 2.34 (m, 2H), 1.42 (t+s, 12H); High resolution mass spectrum (NH.sub.3 --CI) calculated (M+H.sup.+); 425.2189, found 425.2193.

F. 1-�3-(N-tert-butyloxycarbonyl-N-pyridin-2-ylamino)propyl!-5-carboxyindazole

A mixture of the product prepared according to Example 1081 Part E (7.9 g, 18.6 mmol), water (100 mL), ethanol (100 mL) and aqueous sodium hydroxide (1.0M; 40 ml, 40 mmol) was stirred at reflux for 16 h. The mixture was allowed to cool to room temperature and aqueous hydrochloric acid (1.0M; 43 mL, 43 mmol) was added. The solvent was decanted and the resulting gum was triturated several times with hexane to provide the title product (5.56 g, 75%) as a solid: mp 129.degree.-131.degree. C.; .sup.1 H NMR (CDCl.sub.3) .delta. 8.59 (s, 1H), 8.30 (m, 1H), 8.12 (s, 1H), 8.07 (d, 1H), 7.61 (m, 2H), 7.41 (d, 1H), 7.00 (m, 1H), 4.46 (t, 2H), 4.01 (t, 2H), 2.34 (m, 2H), 1.42 (s, 9H); High resolution mass spectrum (NH.sub.3 --CI) calculated (M+H.sup.+); 397.1876, found 397.1878.

G. tert-Butyl 3-�1-�3-(N-(tert-butyloxycarbonyl-N-pyridin-2-ylamino)propyl!indazol-5-ylcarbonylamino!-2(S)-(benzyloxycarbonylamino)propionate

A mixture of the product prepared according to the procedure of Example 1081 Part F (1.19 g, 3.0 mmol), tert-butyl 3-amino-2(S)-(benzyloxycarbonylamino)propionate (prepared according to Mokotoff and Logue, J. Med. Chem. 1981, 24, 554; 880 mg, 3.0 mmol), 1-hydroxybenzotriazole hydrate (410 mg, 3.0 mmol), and anhydrous tetrahydrofuran (20 mL) was stirred at room temperature. The mixture was treated with dicyclohexylcarbodiimide (660 mg, 3.2 mmol) and stirred for 24 h. The mixture was filtered and solvent was removed under vacuum. The residue was purified by flash chromatography (hexanes:ethyl acetate 50:50) to provide the title product (1.81 g, 89%) as a glass: .sup.1 H NMR (CDCl.sub.3) .delta. 8.28 (d, 1H), 8.17 (s, 1H), 8.04 (s, 1H), 7.77 (d, 1H), 7.60 (d, 2H), 7.4-7.25 (m, 6H), 6.98 (m, 2H), 5.88 (bd, 1H), 5.13 (s, 2H), 4.47 (bm, 1H), 4.46 (t, 2H), 4.01 (t, 2H), 3.87 (m, 2H), 2.31 (m, 2H), 1.48 (s, 9H), 1.43 (s, 9H); High resolution mass spectrum (NH.sub.3 --CI) calculated (M+H.sup.+) 673.3350, found 673.3324.

H. 3-�1-�3-(N-pyridin-2ylamino)propyl!indazol-5-ylcarbonylamino!-2(S)-(benzyloxycarbonylamino)propionic acid trifluoroacetate

A mixture of the product prepared according to Example 1081 Part G (32 mg, 47 .mu.mol), dichloromethane (5 mL) and trifluoroacetic acid (300 .mu.L) was stirred at room temperature for 16 h. The mixture was concentrated under vacuum and toluene was added. The solvent was evaporated and the residue was triturated with ether. The solvent was removed by decantation, and the residue was dried to constant weight under vacuum to provide the desired product (25 mg, 83%) as a hygroscopic white solid: .sup.1 H NMR (DMSO-d.sub.6) .delta. 8.57 (bm, 1H), 8.53 (bt, 1H), 8.26 (s, 1H), 8.21 (s, 1H), 7.82 (m, 3H), 7.69 (d, 1H), 7.59 (d, 1H), 7.28 (m, 5H), 6.93 (d, 1H), 6.78 (t, 1H), 4.99 (s, 2H), 4.52 (t, 2H), 4.23 (m, 1H), 3.60 (m, 2H), 3.24 (m, 2H), 2.15 (m, 2H); High resolution mass spectrum (FAB) calculated (M+H.sup.+) 517.2199, found 517.2213.

EXAMPLE 1094

3-�1-�3-(N-pyridin-2ylamino)propyl!indazol-5-yl-carbonylamino!-2(S)-(isobutyloxycarbonylamino)propionic acid trifluoroacetate

A. tert-Butyl 3-�1-�3-(N-tert-butyloxycarbonyl-N-pyridin-2-ylamino)-propyl!indazol-5-ylcarbonylamino!-2(S)-aminopropionate

A mixture of the product prepared according to the procedure of Example 1081 Part G (1.60 g, 2.33 mmol), 10% palladium on charcoal (160 mg) and ethanol (30 mL) was placed in a pressure bottle and stirred at room temperature under an atmosphere of hydrogen (1 atmosphere pressure). After 5 h, the mixture was filtered through Celite.RTM., the solids were rinsed with ethanol, and the filtrate was concentrated under vacuum to provide the title product (1.24 g, 97%) as a glass: .sup.1 H NMR (CDCl.sub.3) .delta. 8.28 (d, 1H), 8.20 (s, 1H), 7.82 (d, 1H), 7.60 (m, 2H), 7.38 (d, 1H), 6.98 (m, 1H), 6.93 (bt, 1H), 4.45 (t, 2H), 4.00 (t, 2H), 3.88 (m, 1H), 3.66 (m, 1H), 3.56 (m, 1H), 2.51 (m, 2H), 2.05 (bs, ca. 2H), 1.48 (s, 9H), 1.42 (s, 9H); High resolution mass spectrum (NH.sub.3 --CI) calculated (M+H.sup.+) 539.2982, found 539.2998.

B. tert-Butyl 3-�1-�3-(N-tert-butyloxycarbonyl-N-pyridin-2ylamino)-propyl!indazol-5-ylcarbonylamino-!2(S)-(isobutyloxycarbonylamino)propionate

A solution of the product prepared according to Example 1094 Part A (100 mg, 186 .mu.mol) in N,N-dimethylformamide (5 mL) was treated with isobutyl chloroformate (27 .mu.L, 205 .mu.mol), 4-(N,N-dimethylamino)pyridine (10 mg) and pyridine (15 .mu.L, 205 .mu.mol). The solution was stirred at room temperature for 16 h, then was concentrated under vacuum. The residue was purified by flash chromatography (dichloromethane:ethyl acetate 97:3) to provide the title product (106 mg, 89%) as a gum: .sup.1 H NMR (DMSO-d.sub.6) .delta. 8.51 (m, 1H), 8.28 (m, 2H), 8.22 (s, 1H), 7.96 (s, 1H), 7.9-7.50 (m, 3H), 7.53 (d, 1H), 7.11 (m, 1H), 4.46 (t, 2H), 4.21 (m, 1H), 3.84 (m, 2H), 3.75 (d, 2H), 3.69 (m, 1H), 3.56 (m, 1H), 2.13 (m, 2H), 1.83 (m, 1H), 1.33 (s, 9H), 1.30 (s, 9H), 0.88 (d, 6H); High resolution mass spectrum (FAB) calculated (M+H.sup.+) calculated 639.3480, found 639.3506.

C. 3-�1-�3(N-pyridin-2ylamino)propyl!indazol-5-yl-carbonylamino!-2(S)-(isobutyloxycarbonylamino)propionic acid trifluoroacetate

Using the procedure of Example 1081 Part H, the product prepared according to Example 1094 Part B (106 mg, 166 .mu.mol) was converted to the title product (76 mg, 76%) as a solid: .sup.1 H NMR (DMSO-d.sub.6) .delta. 8.56 (m, 2H), 8.30 (s, 1H), 8.25 (s, 1H), 7.90-7.75 (m, 3H), 7.72 (d, 1H), 7.44 (d, 1H), 6.96 (d, 1H), 6.80 (t, 1H), 4.56 (t, 2H), 4.24 (m, 1H), 3.73 (d, 2H), 3.62 (m, 2H), 3.28 (m, 2H), 2.17 (m, 2H), 1.82 (m, 1H), 0.85 (d, 6H); High resolution mass spectrum (NH.sub.3 --CI) calculated (M+H.sup.+) calculated 483.2348, found 483.2356.

EXAMPLE 1099b

3-�1-�3(N-pyridin-2ylamino)propyl!indazol-5-yl-carbonylamino!-2-(S)-(E-�phenylethenyl!carbonylamino)-propionic acid trifluoroacetate

A. tert-Butyl 3-�1-�3-(N-tert-butyloxycarbonyl-N-pyridin-2-ylamino)propyl!indazol-5-ylcarbonylamino-2(S)-(E-�phenylethenyl!carbonylamino)propionate

A solution of the product prepared according to Example 1094 Part A (100 mg, 186 .mu.mol) in tetrahydrofuran (3 mL) was treated with trans-cinnamic acid (28 mg, 186 .mu.mol), 1-hydroxybenzotriazole hydrate (25 mg, 186 .mu.mol) and dicyclohexylcarbodiimide (39 mg, 186 .mu.mol). The mixture was stirred at room temperature for 18 h, then was concentrated under vacuum. The residue was purified by flash chromatography (hexanes:ethyl acetate 70:30) to provide the title product (108 mg, 87%) as a gummy white solid: .sup.1 H NMR (CDCl.sub.3) .delta. 8.27 (d, 1H), 8.24 (s, 1H), 8.06 (s, 1H), 7.83 (d, 1H), 7.67 (d, J=17 Hz, 1H), 7.59 (m, 1H), 7.55-7.35 (m, 6H), 6.97 (m, 1H), 6.88 (d, 1H), 6.70 (d, J=17 Hz, 1H), 4.85 (m, 1H), 4.44 (t, 2H), 4.02 (m, 3H), 3.47 (m, 2H), 2.31 (m, 2H), 1.52 (s, 9H), 1.40 (s, 9H); High resolution mass spectrum (FAB) calculated (M+H.sup.+) 669.3401, found 669.3389.

B. 3-�1-�3-(N-pyridin-2-ylamino)propyl!indazol-5-yl-carbonylamino!-2(S)-(E-�phenylethenyl!carbonylamino)propionate acid trifluoroacetate

Using the procedure of Example 1081 Part H, the product prepared according to Example 1099b Part A (100 mg, 150 .mu.mol) was converted to the title product (90 mg, 96%) as a white solid: .sup.1 H NMR (DMSO-d.sub.6) .delta. 8.64 (t, 1H), 8.47 (d, 1H), 8.31 (s, 1H), 8.04 (s, 1H), 7.90-7.80 (m, 3H), 7.73 (d, 1H), 7.58 (d, 1H), 7.50-7.35 (m, 6H), 6.98 (d, 1H), 6.82 (t, 1H), 6.74 (d, J=17 Hz, 1H), 4.63 (m, 1H), 4.55 (t, 2H), 3.75-3.55 (m, 2H), 3.27 (m, 2H), 2.18 (m, 2H); High resolution mass spectrum (FAB) calculated (M+H.sup.+) 513.2250, found 513.2239.

EXAMPLE 1108b

3-1-�3-(N-pyridin-2-ylamino)propyl!indazol-5-yl-carbonylamino!-2(S)-(cyclohexylcarbonylamino)propionic acid trifluoroacetate

A. 1-�3(pyridin-2-ylamino)propyl!-5-carboxyindazole

A mixture of the product prepared according to Example 1081 Part D (1.04 g, 3.19 mmol), ethanol (16 mL) and aqueous sodium hydroxide (1.0M; 16 ml, 16 mmol) was stirred at reflux for 20 h. The mixture was allowed to cool to room temperature and aqueous hydrochloric acid (1.0M; 16 mL, 16 mmol) was added. The resulting solid was collected by filtration, washed with water and dried to provide the title product: .sup.1 H NMR (DMSO-d.sub.6) .delta. 8.42 (s, 1H), 8.22 (s, 1H), 7.90 (m, 2H), 7.76 (d, 1H), 7.38 (m, 1H), 6.58 (t, 1H), 6.42 (m, 2H), 4.52 (t, 2H), 3.20 (q, 2H), 2.08 (m, 2H); Mass spectrum (ESI) m/z 297.3 (100%, M+H.sup.+).

B. tert-Butyl 3-�1-�3-(pyridin-2-ylamino)propyl!indazol-5-ylcarbonylamino!-2(S)-(benzyloxycarbonylamino)propionate

Using the procedure of 1081 Part G, the product prepared according to the procedure of Example 1108b Part A (740 mg, 2.5 .mu.mmol) was converted to the title product (700 mg, 56%): .sup.1 H NMR (CDCl.sub.3) .delta. 8.19 (s, 1H), 8.08 (s, 1H), 8.06 (m, 1H), 7.79 (d, 1H), 7.45-7.25 (m, 7H), 7.02 (bm, 1H), 6.56 (m, 1H), 6.32 (d, 1H), 5.90 (bm, 1H), 5.13 (s, 2H), 4.52 (t, 2H), 4.05 (bm, 1H), 3.87 (m, 2H), 3.47 (m, 1H), 3.28 (m, 2H), 2.26 (m, 2H), 1.48 (s, 9H); Mass spectrum (ESI) m/z 573.4 (22%, M+H.sup.+).

C. tert-Butyl 3-1-�3-(pyridin-2-ylamino)propyl!indazol-5-ylcarbonylamino!-2(S)-aminopropionate

Using the procedure of 1094 Part A, the product prepared according to the procedure of Example 1108b Part B (700 mg, 1.22 mmol) was converted to the title product (500 mg, 93%) as a gummy solid: .sup.1 H NMR (CDCl.sub.3) .delta. 8.24 (s, 1H), 8.09 (s, 1H), 8.01 (d, 1H), 7.84 (d, 1H), 7.47 (d, 1H), 7.40 (t, 1H), 7.10 (bm, 1H), 6.56 (t, 1H), 6.33 (d, 1H), 4.54 (t, 2H), 4.11 (m, 1H), 3.86 (m, 1H), 3.59 (m, 1H), 3.25 (m, 2H), 2.27 (m, 2H), 1.49 (s, 9H); Mass spectrum (ESI) m/z 439.3 (100%, M+H.sup.+).

D. tert-Butyl 3-�1-�3-(pyridin-2-ylamino)propyl!indazol-5-ylcarbonylamino!-2(S)-(cyclohexylcarbonylamino)propionate

Using the procedure of 1094 Part B, the product prepared according to the procedure of Example 1108b Part C (100 mg, 230 .mu.mol) and cyclohexylcarbonyl chloride (31 .mu.L, 230 .mu.mol) were converted to the title product (60 mg, 50%): .sup.1 H NMR (CDCl.sub.3) .delta. 8.22 (s, 1H), 8.10 (s, 1H), 7.91 (d, 1H), 7.80 (d, 1H), 7.54 (d, 1H), 7.45 (m, 2H), 6.72 (d, 1H), 6.57 (t, 1H), 6.32 (d, 1H), 4.72 (m, 1H), 4.58 (t, 2H), 3.89 (m, 1H), 3.76 (m, 1H), 3.19 (t, 2H), 2.30 (m, 3H), 2.19 (m, 1H), 2.0-1.2 (m, 10H); Mass spectrum (ESI) m/z 549.5 (100%, M+H.sup.+).

E. 3-�1-�3-(N-pyridin-2-ylamino)propyl!indazol-5-yl-carbonylamino!-2(S)-(cyclohexylcarbonylamino)propionic acid trifluoroacetate

Using the procedure of Example 1081 Part H, the product prepared according to Example title product: .sup.1 H NMR (DMSO-d.sub.6) .delta. 8.54 (m, 1H), 8.28 (s, 1H), 8.25 (s, 1H), 8.02 (d, 1H), 7.9-7.7 (m, 4H), 6.90 (m, 1H), 6.77 (m, 1H), 4.55 (t, 2H), 4.44 (m, 1H), 3.61 (m, 2H), 3.26 (m, 2H), 2.16 (m, 3H), 2.0-1.0 (m, 10H); High resolution mass spectrum (NH.sub.3 --CI) calculated (M+H.sup.+) 493.2563, found 493.2559.

EXAMPLE 1110a

3-�1-�3-(N-pyridin-2-ylamino)propyl!indazol-5-ylcarbonylamino!-2(S)-(phenylaminocarbonylamino)propionic acid trifluoroacetate

A. tert-Butyl 3-�1-�3-(N-tert-butyloxycarbonyl-N-pyridin-2-ylamino)propyl!indazol-5-ylcarbonylamino!-2(S)-(phenylaminocarbonylamino)propionate

A solution of the product prepared according to Example 1094 Part A (105 mg, 195 .mu.mol) in dichloromethane (5 mL) was treated sequentially with diisopropylethylamine (69 .mu.L, 385 .mu.mol) and phenyl isocyanate (49 .mu.l, 448 .mu.mol). The solution was stirred at room temperature for 1 h, then was concentrated under vacuum. The residue was purified by flash chromatography (hexanes:ethyl acetate, 50:50) to provide the title product (72 mg, 56%): .sup.1 H NMR (CDCl.sub.3) .delta. 8.25 (d, 1H), 8.18 (s, 1H), 7.95 (m, 1H), 7.86 (s, 1H), 7.75 (d, 1H), 7.70 (bm, 1H), 7.57 (m, 2H), 7.17 (m, 3H), 7.10 (m, 2H), 6.95 (m, 1H), 6.92 (m, 1H), 6.63 (m, 1H), 4.79 (m, 1H), 4.34 (t, 2H), 3.96 (m, 2H), 3.86 (m, 2H), 2.25 (m, 2H), 1.46 (s, 9H), 1.41 (s, 9H); High resolution mass spectrum (FAB) calculated (M+H.sup.+) 658.3353, found 658.3342.

B. 3-�1-�3-(N-pyridin-2-ylamino)propyl!indazol-5-yl-carbonylamino!-2(S)-(phenylaminocarbonylamino)propionic acid trifluoroacetate

Using the procedure of Example 1081 Part H, the product prepared according to Example 1110a Part A (68 mg, 104 .mu.mol) was converted to the title product (44 mg, 68%) as a white solid after preparative reverse phase high pressure liquid chromatography (acetonitrile:water containing 0.05% trifluoroacetic acid, gradient from 1:9 to 9:1): .sup.1 H NMR (MeOH-d.sub.4) .delta. 8.24 (s, 1H), 8.09 (s, 1H), 7.85-7.70 (m, 2H), 7.68 (d, 1H), 7.55 (d, 1H), 7.29 (m, 2H), 7.17 (t, 2H), 6.91 (m, 2H), 6.79 (t, 1H), 4.66 (m, 1H), 4.54 (t, 2H), 3.88 (dd, 1H), 3.77 (dd, 1H), 3.27 (m, 2H), 2.28 (m, 2H); High resolution mass spectrum (FAB) calculated (M+H.sup.+) 502.2203, found 502.2196.

EXAMPLE 1129

3-�1-�3-(N-pyridin-2-ylamino)propyl!indazol-5-yl-carbonylamino!-2(S)-(1-naphthalene-sulfonylamino)-propionic acid trifluoroacetate

A. 1-(2-cyanoethyl)-5-ethoxycarbonylindazole

A mixture of the product prepared according to Example 1050e Part C (3.80 g, 20 mmol), acrylonitrile (7.9 mL, 120 mmol), sodium bis-(trimethylsilyl)amide (1.0M in tetrahydrofuran; 1.0 mL, 1.0 mmol) and ethanol (40 mL) was heated to reflux. After 2 h, the solution was cooled to room temperature and treated with aqueous hydrochloric acid (1.0M; 1.5 mL, 1.5 mmol). After the mixture was partially concentrated under vacuum, a solid formed. Water (100 mL) was added and the mixture was stirred briefly. The resulting solid was collected by filtration, rinsed with water and dried to provide the title product (4.38 g, 90%) as a pale yellow fluffy solid: mp 106.degree.-109.degree. C.; .sup.1 H NMR (CDCl.sub.3) .delta. 8.54 (s, 1H), 8.16 (s, 1H), 8.13 (d, 1H), 7.48 (d, 1H), 4.70 (t, 2H), 4.42 (q, 2H), 3.03 (t, 2H), 1.43 (t, 3H); High resolution mass spectrum (NH.sub.3 --CI) calculated (M+H.sup.+) 244.1086, found 244.1070.

B. 1-(3-aminopropyl)-5-ethoxycarbonylindazole hydrochloride

A mixture of the product prepared according to Example 1129 Part A (60 g, 260 mmol), platinum oxide (6.0 g), ethanol (1600 mL) and chloroform (200 mL) was placed in a pressure bottle and agitated under an atmosphere of hydrogen (40 psig) for 19 h. The mixture was filtered through Celite.RTM. and the solids were washed with ethanol. The filtrate was concentrated under vacuum and the residue was dissolved in aqueous sodium bicarbonate and washed with ethyl acetate. The aqueous phase was acidified with hydrochloric acid and concentrated to a solid. This was dissolved in hot ethanol, filtered, and the filtrate cooled. The resulting crystals were collected by filtration to provide the title product. Repeating the reaction twice more starting with 57 g of the nitrile provided a total of 115 g (57%) of the title product as a white solid: mp 198.degree.-200.degree. C.; .sup.1 H NMR (DMSO-d.sub.6) .delta. 8.49 (s, 1H), 8.32 (s, 1H), 8.07 (bs, 3H), 7.98 (d, 1H), 7.85 (d, 1H), 4.58 (t, 2H), 4.34 (q, 2H), 2.80 (bm, 2H), 2.14 (m, 2H), 1.34 (t, 3H); High resolution mass spectrum (NH.sub.3 --CI) calculated (M+H.sup.+) 248.1399, found 248.1396.

C. 1-�3-�N-(1-oxido)pyridin-2-ylamino!propyl!-5-ethoxycarbonylindazole

Using the procedure of Example 1081 Part C, the product prepared according to Example 1129 Part B (566 mg, 2.0 mmol) was converted to the title product (470 mg, 69%). This product is the same as the product of Example 1081 Part C.

D. 1-�3-�N-(1-oxido)pyridin-2-ylamino!propyl!-5-carboxyindazole

A mixture of the product prepared according to Example 1129 Part C (470 mg, 1.3 mmol), aqueous sodium hydroxide (1.0M; 4.0 moL, 4.0 mmol), water (10 mL) and ethanol (10 mL) was heated to reflux. After 30 h, additional aqueous sodium hydroxide (1.0M; 2.0 mL) was added and heating was continued. After 48 h more, the mixture was cooled to room temperature and treated with aqueous hydrochloric acid (1.0M; 6.0 mL) to give a precipitate. The solid was collected by filtration, rinsed with water and dried to provide the title product (369 mg, 91%) as a white solid: .sup.1 H NMR (DMSO-d.sub.6) .delta. 12.70 (bs, 1H), 8.45 (s, 1H), 8.27 (s, 1H), 8.11 (d, 1H), 7.92 (d, 1H), 7.73 (d, 1H), 7.32 (bt, 1H), 7.16 (t, 1H), 6.70 (d, 1H), 6.59 (t, 1H), 4.53 (t, 2H), 3.24 (q, 2H), 2.14 (m, 2H); High resolution mass spectrum (NH.sub.3 --CI) calculated (M+H.sup.+) 313.1301, found 313.1299.

E. tert-Butyl 3-�1-�3-(N-(1-oxido)pyridin-2-ylamino)-propyl!indazol-5-ylcarbonylamino!-2-(S)-(benzyloxy-carbonylamino)propionate

A mixture of the product prepared according to Example 1129 Part D (312 mg, 1.0 mmol), tert-butyl 3-amino-2(S)-benzyloxycarbonylaminopropionate (prepared according to Mokitoff and Logue, J. Med. Chem. 1981, 24, 554; 294 mg, 1.0 mmol), 1-hydroxybenzotriazole hydrate (135 mg, 1.0 mmol), tetrahydrofuran (4 mL) and dry N,N-dimethylformamide (1 mL) was stirred on an ice bath. Dicyclohexylcarbodiimide (227 mg, 1.1 mmol) was added, and the mixture was stirred for 1 h. The ice bath was removed and stirring was continued for 3.5 h more. The mixture was filtered, and the solid was rinsed with tetrahydrofuran. The filtrate was concentrated under vacuum, and the residue was taken up in ethyl acetate. The solution was washed with water, dried over anhydrous sodium sulfate, filtered and concentrated under vacuum. The residue was purified by flash chromatography (dichloromethane/methanol; 96:4, then 94:6) to provide the title product (304 mg, 52%) as an off-white glass: .sup.1 H NMR (CDCl.sub.3) .delta. 8.00 (s, 1H), 8.11 (d, 1H), 8.07 (s, 1H), 7.76 (d, 1H), 7.4-7.2 (m, 6H), 7.18 (bt, 1H), 7.12 (t, 1H), 6.95 (bt, 1H), 6.53 (t, 1H), 6.39 (d, 1H), 6.10 (d, 1H), 5.11 (s, 2H), 4.50 (t, 3H),3.88 (m, 2H), 3.21 (q, 2H), 2.31 (m, 2H), 1.48 (s, 9H); High resolution mass spectrum (FAB) calculated (M+H.sup.+) 589.2775, found 589.2804.

F. tert-Butyl 3-�1-�3-(N-pyridin-2ylamino)-propyl!-indazol-5-ylcarbonylamino!-2-(S)-aminopropionate

A mixture of the product prepared according to Example 1129 Part E (266 mg, 452 mol) and 10% palladium on charcoal (65 mg) in ethanol (20 mL) was placed in a pressure bottle and agitated under an atmosphere of hydrogen (55 psig) for 100 h. The mixture was filtered through Celite.RTM. and the solids were rinsed with ethanol. The filtrate was concentrated under vacuum, and the residue was purified by flash chromatography (dichloromethane:methanol, step gradient from 96:4, to 92.5:7.5) to provide the title product (100 mg, 50%) as a colorless glass: .sup.1 H NMR (CDCl.sub.3) .delta. 8.21 (s, 1H), 8.10 (s, 1H), 8.07 (d, 1H), 7.80 (d, 1H), 7.42 (d, 1H), 7.39 (t, 1H), 6.88 (bt, 1H), 6.56 (t, 1H), 6.33 (d, 1H), 4.90 (bt, 1H), 4.53 (t, 2H), 3.86 (m, 1H), 3.63 (m,1H), 3.52 (m, 1H), 3.28 (q, 2H), 2.26 (m, 2H), 1.90 (b, 2H), 1.48 (s, 9H); High resolution mass spectrum (NH.sub.3 --CI) calculated (M+H.sup.+) 439.2458, found 439.2457.

G. tert-Butyl 3-�1-�3-(N-pyridin-2-ylamino)-propyl!-indazol-5-ylcarbonylamino!-2-(S)-(1-naphthalenesulfonylamino)propionate

A solution of the product prepared according to Example 1129 Part F (77 mg, 176 .mu.mol) in dry tetrahydrofuran (2 mL) was treated with 4-(N,N- dimethylamino)pyridine (24 mg, 193 .mu.mol), 1-naphthalenesulfonyl chloride (44 mg, 193 .mu.mol) and pyridine (16 .mu.L, 193 .mu.mol). The mixture was stirred at room temperature for 20 h, then was concentrated under vacuum. The residue was purified by flash chromatography (dichloromethane-methanol, 96:4) and rotary thin-layer chromatography (dichloromethane-methanol, 96:4) to provide the title product (90 mg, 82%) as a colorless glass: .sup.1 H NMR (CDCl.sub.3) .delta. 8.67 (d, 1H), 8.26 (d, 1H), 8.1-8.0 (m, 4H), 7.88 (d, 1H), 7.70 (m, 2H), 7.56 (m, 2H), 7.20 (m, 2H), 6.60 (m, 2H), 6.34 (d, 1H), 6.10 (bs, 1H), 5.35 (bs, 1H), 4.53 (t, 2H), 3.95 (b, 1H), 3.80 (m, 1H), 3.63 (m, 1H), 3.28 (q, 2H), 2.28 (m, 2H), 1.12 (s, 9H); High resolution mass spectrum (FAB) calculated (M+H.sup.+) 629.2546, found 629.2526.

H. 3-�1-�3-(N-pyridin-2-ylamino)-propyl!indazol-5-ylcarbonylamino!-2-(S)-(1-naphthalenesulfonylamino)propionic acid trifluoroacetate

A solution of the product prepared according to Example 1129 Part G (77 mg, 122 .mu.mol) in dichloromethane (2 mL) was treated with trifluoroacetic acid (1 mL) and stirred at room temperature for 3 h. The solution was concentrated under vacuum, toluene was added, and the solvent was again removed under vacuum. The residue was triturated in ether, and the resulting solid was collected by filtration to provide the title product (81 mg, 96%) as a white powder: .sup.1 H NMR (DMSO-d.sub.6) .delta. 8.60 (m, 3H), 8.39 (bt, 1H), 8.21 (s, 1H), 8.09 (d, 2H), 8.05 (s, 1H), 7.90 (t, 2H), 7.83 (t, 1H), 7.67 (m, 3H), 7.55 (m, 2H), 6.97 (d, 1H), 6.81 (t, 1H), 4.56 (t, 2H), 4.08 (q, 1H), 3.53 (m, 1H), 3.30 (m, 3H), 2.18 (m, 2H); High resolution mass spectrum (FAB) calculated (M+H.sup.+) 573.1947, found 573.1928.

EXAMPLE 1129a

3-�1-�3-(N-pyridin-2ylamino)propyl!indazol-5-ylcarbonylamino!-2(S)-(4-phenylbenzenesulfonylamino)propionic acid trifluoroacetate

A. tert-Butyl 3-�1-�3-(N-tert-butyloxycarbonyl-N-pyridin-2ylamino)propyl!indazol-5-ylcarbonylamino!-2(S)-(4-phenylbenzenesulfonylamino)propionate

Using the procedure of Example 1129 Part G, the product prepared according to Example 1094 Part A (86 mg, 159 .mu.mol) and 4-phenylbenzenesulfonyl chloride were converted to the title product (116 mg, 97%): .sup.1 H NMR (CDCl.sub.3) .delta. 8.28 (m, 1H), 8.23 (2, 1H), 8.06 (s, 1H), 7.92 (d, 2H), 7.81 (d, 1H), 7.68 (d, 2H), 7.60 (m, 2H), 7.53 (m, 2H), 7.45 (m, 3H), 7.37 (d, 1H), 6.99 (m, 1H), 6.88 (bt, 1H), 5.75 (d, 1H), 4.45 (t, 2H), 4.01 (m, 4H), 3.62 (m, 1H), 2.31 (m, 2H), 1.43 (s, 9H), 1.30 (s, 9H); High resolution mass spectrum (FAB) calculated (M+H.sup.+) 755.3227, found 755.3200.

B. 3-�1-�3-(N-pyridin-2ylamino)propyl!indazol-5-yl-carbonylamino!-2(S)-(4-phenylbenzenesulfonylamino)propionic acid trifluoroacetate

Using the procedure of Example 1129 Part H, the product prepared according to Example 1129 a Part A (108 mg, 143 .mu.mol) was converted to the title product: .sup.1 H NMR (MeOH-d.sub.4) .delta. 8.16 (s, 1H), 8.08 (s, 1H), 7.85 (d, 2H), 7.8-7.7 (m, 4H), 7.58 (d, 2H), 7.5-7.3 (m, 6H), 6.9-6.75 (m, 2H), 4.48 (t, 2H), 4.23 (m, 1H), 3.78 (dd, 1H), 3.50 (dd, 1H), 3.26 (m, 2H), 2.26 (m, 2H); High resolution mass spectrum (FAB) calculated (M+H.sup.+) 599.2077, found 599.2062.

EXAMPLE 1155

3-�1-�3-(N-pyridin-2-ylamino)propyl!indazol-5-yl-carbonylamino!-2(S)-(benzylaminiosulfonylamino)propionic acid trifluoroacetate

A. tert-Butyl 3-�1-�3-(N-(tert-butyloxycarbonyl-N-pyridin-2-ylamino)propyl!indazol-5-ylcarbonylamino!-2(S)-(benzylaminosulfonylamino)propionate

A solution of the product prepared according to Example 1094 Part A (101 mg, 188 .mu.mol) in anhydrous tetrahydrofuran (5 mL) was treated with N-benzylsulfamoyl chloride (prepared according to the procedures of Audrieth and Sveda, J. Org. Chem. 1944, 9, 89-101, and Kloeck and Leschinsky, J. Org. Chem. 1976, 41, 4028-4029; 51 mg, 248 .mu.mol), then with 4-(N,N-dimethylamino)pyridine (37 mg, 193 .mu.mol) and pyridine (19 .mu.L, 252 .mu.mol). The resulting mixture was stirred at room temperature for 24 h, then was concentrated under vacuum. The residue was purified by flash chromatography (hexanes:ethyl acetate 45:55) to provide the title product (92 mg, 70%) as a white solid: .sup.1 H NMR (CDCl.sub.3) .delta. 8.27 (m, 1H), 8.18 (s, 1H), 8.04 (s, 1H), 7.78 (d, 1H), 7.60 (m, 2H), 7.36 (d, 1H), 7.29 (m, 5H), 6.99 (m, 1H), 6.79 (bt, 1H), 5.62 (d, 1H), 4.75 (t, 1H), 4.44 (t, 2H), 4.23 (t, 2H), 4.15 (m, 1H), 4.00 (m, 2H), 3.95 (m, 1H), 3.76 (m, 1H), 2.31 (m, 2H), 1.48 (s, 9H), 1.43 (s, 9H); High resolution mass spectrum (FAB) calculated (M+H.sup.+) 708.3179, found 708.3205

B. 3-�1-�3-(N-pyridin-2yl)aminoproply!indazol-5-yl!-carbonylamino-2(S)-benzylaminosulfonylaminopropionic acid trifluoroacetate

Using the procedure of Example 1129 Part H, the product prepared according to Example 1155 Part A (21 mg, 30 .mu.mol) was converted to the title product (19 mg, 96%): .sup.1 H NMR (DMSO-d.sub.6) .delta. 8.56 (m, 2H), 8.33 (s, 1H), 8.24 (s, 1H), 7.90-7.70 (m, 4H), 7.49 (d, 1H), 7.43 (t, 1H), 7.23 (m, 5H), 6.96 (d, 1H), 6.80 (t, 1H), 4.56 (t, 2H), 4.20-3.60 (m, 5H), 3.59 (m, 2H), 2.18 (t, 2H); High resolution mass spectrum (FAB) calculated (M+H.sup.+) 552.2029, found 552.2042.

EXAMPLE 1178b

3-�1-�3-(N-3 4,5,6-Tetrahydropyrimidin-2-ylamino)propyl!indazol-5-ylcarbonylamino!-2(S)-(2,4,6-trimethylbenzenesulfonylamino)propionic acid trifluoroacetate

A. 1-(3-Benzyloxycarbonylaminopropyl)-5-ethoxycarbonylindazole

A mixture of the product prepared according to Example 1129 Part B (5.0 g, 18 mmol) and triethylamine (7.5 mL, 19 mmol) in dichloromethane (100 mL) was cooled on an ice bath and treated with benzyl chloroformate (2.7 mL, 19 mmol). The mixture was stirred at room temperature for 16 h, then was concentrated under vacuum. The residue was dissolved in dichloromethane and washed with water several times, then was dried over anhydrous magnesium sulfate, filtered and concentrated to provide the title product (3.4 g, 49%) as a white solid. While this material was suitable for further use, it could be purified by flash chromatography (dichloromethane:methanol 95:5): .sup.1 H NMR (CDCl.sub.3) .delta. 8.50 (s, 1H), 8.06 (m, 2H), 7.38 (m, 6H), 5.20 (bm, 1H), 5.02 (s, 2H), 4.42 (m, 4H), 3.18 (m, 2H), 2.18 (m, 2H), 1.40 (m, 3H); Mass spectrum (ESI) m/z 382.5 (100%, M+H.sup.+).

B. 1-(3-Benzyloxycarbonylaminopropyl)-5-carboxyindazole

A mixture of the product prepared according to Example 1178b Part A (3.08 g, 8.07 mmol), lithium hydroxide hydrate (678 mg, 16.2 mmol), ethanol (160 mL) and water (40 mL) was stirred at room temperature. Tetrahydrofuran was added until the mixture was homogeneous, then stirring was continued for 5 days. The solution was concentrated, and the residue was taken up in water. The mixture was washed with ethyl acetate, and the aqueous phase was acidified to pH 4-5 with aqueous hydrochloric acid (1.0M). This mixture was then extracted with ethyl acetate. The extract was dried over anhydrous magnesium sulfate, filtered and concentrated to provide the title product (1.6 g, 56%) as a sticky solid: .sup.1 H NMR (DMSO-d.sub.6) .delta. 8.44 (s, 1H), 8.26 (s, 1H), 7.93 (d, 1H), 7.72 (d, 1H), 7.35 (m, 5H), 5.00 (s, 2H), 4.46 (t, 2H), 3.01 (m, 2H), 1.98 (m, 2H).

C. N.sup.2 -(2,4,6 trimethylbenzenesulfonyl)-L-asparagine

L- Asparagine (20.0 g, 0.15 mol) was suspended in a mixture of tetrahydrofuran (130 mL) and water (250 mL). Triethylamine (68 mL, 0.48 mol) was added, followed by mesitylenesulfonyl chloride (49.7 g, 0.23 mol) added over 20 min. The reaction mixture became slightly warmer and the solids dissolved to yield a yellow solution. The reaction mixture was stirred for 3 h at room temperature, then washed twice with ether, and twice with dichloromethane. The aqueous layer was acidified to pH 1.5 with concentrated aqueous HCl, during which time a thick precipitate formed. After being stirred for 30 min the solid was collected by filtration, washed with water and dried to yield the title product (34.1 g, 72%) as a white solid: m.p. 193.5.degree.-195.degree. C.; .sup.1 H NMR (DMSO-d.sub.6) .delta.12.58 (bs, 1H), 7.82 (d, 1H), 7.32 (bs, 1H), 6.99 (s, 2H), 6.88 (bs, 1H) 3.98 (m, 1H), 2.55 (s, 6H), 2.45 (dd, 1H), 2.28 (dd, 1H), 2.24 (s, 3H); Mass spectrum (ESI) m/z 315.2, (100%, M+H.sup.+).

D. 3-Amino-2-(S)-(2,4,6-trimethylbenzenesulfonylamino)propionic acid

Sodium hydroxide (32 g, 0.80 mol), was dissolved in water (200 mL) and cooled in an ice bath.

Bromine (6.2 mL, 0.12 mol) was added dropwise over 5 min and the mixture was allowed to stir for 15 min. The product prepared according to Example 1178b Part C (31.44 g, 0.10 mol) was added in several portions over a period of ca. 10 min, during which time the yellow color faded. After stirring for 15 min more, the reaction mixture was heated rapidly to an internal temperature of ca. 85.degree. C. After 1 h, the reaction mixture was allowed to cool to room temperature, then cooled in an ice bath. The reaction mixture was cautiously acidified to pH 6 with concentrated aqueous HCl, during which time a solid formed and gas was evolved. The solid was collected by filtration, washed with cold water, and allowed to dry overnight to provide the title product (23.9 g, 83%) as a white solid: .sup.1 H NMR (DMSO-d.sub.6) .delta. 7.06 (s, 2H), 3.07 (dd, 1H), 3.35 (broad), 2.94 (dd, 1H), 2.80 (dd, 1H), 2.59 (s, 6H), 2.26 (s, 3H); Mass spectrum (ESI) m/z 287.2 (100%, M+H.sup.+).

E. tert-Butyl 3-amino-2-(S)-(2,4,6-trimethylbenzenesulfonylamino)propionate

The product prepared according to Example 1178b Part D (11.45 g, 0.04 mol) was placed in a pressure bottle and dissolved in dioxane (170 mL). Concentrated sulfuric acid (11 mL) was added and the reaction mixture was cooled in a dry ice-acetone bath. Liquid isobutylene (ca. 185 mL) was added, and the bottle was sealed and agitated for 114 h. The bottle was de-pressurized, then purged with nitrogen for a brief time. The reaction mixture was poured into a rapidly stirred mixture of water (225 mL) containing sodium hydroxide (17 g) and ether (600 mL) which had been pre-cooled in an ice bath. The layers were separated, and the aqueous layer was extracted with additional ether. These organic extracts were discarded. The pH of the aqueous layer was carefully adjusted with concentrated aqueous HCl to pH 11.0 and extracted four times with ether. The organic layers from the pH 11 extraction were combined, dried with anhydrous sodium sulfate, filtered and concentrated to yield the title product (8.64 g, 63%) as a viscous oil which gradually solidified: .sup.1 H NMR (CDCl.sub.3) .delta. 6.95 (s, 2H), 3.69 (m, 1H), 2.93 (m, 2H), 2.67 (s, 6H), 2.28 (s, 3H), 1.28 (s, 9H); Mass spectrum (ESI) m/z 343.3 (100%, M+H.sup.+).

F. tert-Butyl 3-�1-(3-benzyloxycarbonylaminopropyl)indazol-5-ylcarbonylamino!-2(S)-(2,4,6-trimethylbenzenesulfonylamino)propionate

Using the procedure of Example 1129 Part E, the product prepared according to Example 1178b Part B (100 mg, 283 .mu.mol) and the product prepared according to Example 1178b Part E (107 mg, 283 .mu.mol) were converted to the title product (130 mg, 68%) as a yellowish solid: .sup.1 H NMR (CDCl.sub.3) .delta. 8.24 (s, 1H), 8.09 (s, 1H), 7.85 (d, 1H), 7.42 (d, 1H), 7.36 (m, 5H), 6.93 (s, 2H), 6.83 (m, 1H), 5.78 (d, 1H), 5.09 (s, 2H), 4.47 (t, 2H), 4.02 (m, 1H), 3.84 (m, 1H), 3.7-3.4 (m, 2H), 3.18 (m, 2H), 2.66 (s, 6H), 2.26 (s, 3H), 2.15 (m, 2H), 1.21 (s, 9H); Mass spectrum (ESI) m/z 678.4 (41%, M+H.sup.+).

G. tert-Butyl 3-�1-(3-aminopropyl)-indazol-5-yl-carbonylamino!-2(S)-(2,4,6-trimethylbenzenesulfonylamino)propionate

A mixture of the product prepared according to Example 1178b Part F (50 mg, 74 .mu.mol), palladium hydroxide on charcoal (Pearlman's catalyst; 15 mg), 1,4-cyclohexa-diene (1 mL) and methanol (2 mL) was heated at reflux. After 4 h, the mixture was cooled and filtered through Celite.RTM., and the solids were rinsed with methanol. The filtrate was concentrated under vacuum to provide the title product (34 mg, 85%) as a solid which was used in subsequent reactions without further purification: .sup.1 H NMR (CDCl.sub.3) .delta. 8.03 (s, 1H), 7.80-7.65 (m, 3H), 7.31 (d, 1H), 6.84 (s,H), 4.40 (m, 2H), 4.02 (m, 1H), 3.78 (m, 2H), 3.06 (m, 2H), 2.63 (m, 1H), 2.59 (s, 6H), 2.27 (m, 2H), 2.19 (s, 3H), 1.23 (s, 9H); Mass spectrum (ESI) m/z 544.5 (100%, M+H.sup.+).

H. tert-Butyl 3-�1-�3-(N-3,4,5,6-tetrahydropyrimidin-2-ylamino)propyl!-indazol-5-ylcarbonylamino!-2(S)-(2,4,6-trimethylbenzenesulfonylamino)propionate hydriodide

A mixture of the product prepared according to Example 1178b Part G (100 mg, 184 .mu.mol) and 2methylthio-3,4,5,6-tetrahydropyrimidine hydriodide (57 mg, 221 .mu.mol) in pyridine (5 mL) was heated at 120.degree. C. After 16 h, the mixture was cooled to room temperature and concentrated under vacuum. The residue was purified by flash chromatography (dichloromethane:methanol, step gradient from 95:5 to 90:10) to provide the title product (37 mg, 27%): .sup.1 H NMR (CDCl.sub.3) .delta. 8.30 (s, 1H), 8.10 (bm, 1H), 8.08 (s, 1H), 7.92 (d, 1H), 7.85 (t, 1H), 7.51 (d, 1H), 7.10 (bt, 1H), 6.95 (s, 2H), 4.47 (m, 2H), 3.95 (m, 1H), 3.85 (m, 1H), 3.61 (m, 1H), 3.44 (m, 4H), 3.27 (m, 2H), 2.64 (s, 6H), 2.28 (s, 3H), 2.15 (m, 2H), 2.00 (m, 2H), 1.30 (s, 9H); Mass spectrum (ESI) m/z 626.5 (100%, M+H.sup.+).

I. 3-�1-�3-(N-3,4,5,6-Tetrahydropyrimidin-2ylamino)propyl!indazol-5-ylcarbonylamino!-2(S)-(2,4,6-trimethylbenzenesulfonylamino)propionic acid trifluoroacetate

Using the procedure of Example 1129 Part H, the product prepared according to Example 1178b Part H was converted to the title product: .sup.1 H NMR (DMSO-d.sub.6) .delta. 8.46 (bt, 1H), 8.24 (s, 1H), 8.19 (s, 1H), 8.07 (d, 1H), 7.79 (d, 1H), 7.32 (bt, 1H), 6.84 (s, 2H), 4.47 (t, 2H), 4.02 (m, 1H), 3.6-3.4 (m, 2H), 3.21 (m, 4H), 3.03 (m, 2H), 2.52 (s, 6H), 2.07 (s, 3H), 2.05 (m, 2H), 1.78 (m, 2H); Mass spectrum (ESI) m/z 570.5 (100%, M+H.sup.+).

EXAMPLE 1198

3-�1-�3-(N-4,5-Dihydroimidazol-2-ylamino)propyl!indazol-5-ylcarbonylamino!-2(S)-(benzyloxycarbonylamino)propionic acid trifluoroacetate

A. 1-(3-aminoproply)-5-ethoxycarbonylindazole

A mixture of the product prepared according to Example 1081 Part A (4.20 g, 11.1 mmol), ethanol (75 mL), dry tetrahydrofuran (75 mL) and anhydrous hydrazine (1.5 mL) was stirred at room temperature for 16 h. Dry tetrahydrofuran (100 mL) was added, the mixture was filtered and the filtrate was concentrated to provide the title product, which was used directly in the subsequent reaction without purification: .sup.1 H NMR (CDCl.sub.3) .delta. 8.51 (s, 1H), 8.10 (s, 1H), 8.06 (d, 1H), 7.46 (d, 1H), 4.52 (t, 2H), 4.41 (q, 2H), 2.68 (t, 2H), 2.06 (m, 2H), 1.72 (bs, 2H), 1.43 (t, 3H).

B. 1-�3-(N-4,5-Dihydroimidazol-2-ylamino)propyl!-5-ethoxycarbonylindazole hydriodide

The crude product of Example 1198 Part A was combined with 2-methylthio-4,5-dihydroimidazole hydriodide (2.71 g, 11.1 mmol) and pyridine (125 mL), and the mixture was heated at 80.degree. C. for 5 h. The mixture was allowed to cool to room temperature and concentrated under vacuum. The residue was purified by flash chromatography (dichloromethane:methanol 80:20) to provide the title product (3.73 g, 75%) as a gum: .sup.1 H NMR (DMSO-d.sub.6) .delta. 8.50 (s, 1H), 8.30 (s, 1H), 8.24 (bs, 1H), 7.98 (d, 1H), 7.75 (d, 1H), 4.49 (t, 2H), 4.34 (q, 2H), 3.57 (s, 4H), 3.13 (m, 2H), 2.05 (m, 2H), 1.35 (t, 3H); High resolution mass spectrum (NH.sub.3 --CI) calculated (M+H.sup.+) 316.1774, found 316.1765.

C. tert-Butyl 3-�1-�3-(N-4,5-Dihydroimidazol-2yl-amino)-propyl!indazol-5-ylcarbonylamino!-2(S)-(benzyloxycarbonylamino)propionate hydrochloride

A mixture of the product prepared according to Example 1198 Part B (3.39 g, 7.64 mmol), aqueous sodium hydroxide (1.0M; 16 mL, 16 mmol) and ethanol (35 mL) was stirred at reflux for 16 h. The mixture was allowed to cool to room temperature and was treated with aqueous hydrochloric acid (1.0M; 16 mL, 16 mmol). The solvent was evaporated under vacuum, benzene was added and solvent was again evaporated. A portion of the resulting residue (77 mg, 240 .mu.mol) was combined with tert-butyl 3-amino-2(S)-benzyloxycarbonylamino)propionate (prepared according to Mokotoff and Logue, J. Med. Chem. 1981, 24, 554; 70 mg, 240 .mu.mol), 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide hydrochloride (60 mg, 313 .mu.mol), 1-hydroxybenzotriazole hydrate (10 mg), dry N,N-dimethylformamide (5 mL) and triethylamine (0.1 mL), and the resulting mixture was stirred at room temperature for 16 h. The mixture was concentrated under vacuum and benzene (20 mL) was added. The solvent was evaporated and the residue was purified by flash chromatography (dichloromethane:methanol 90:10) to provide the title product (122 mg, 85%) as a yellow gum: .sup.1 H NMR (DMSO-d.sub.6) .delta. 8.53 (bt, 1H), 8.30 (s, 1H), 8.24 (s+m, 2H), 7.88 (d, 1H), 7.71 (d, 1H), 7.70 (m, 1H), 7.34 (m, 5H), 5.04 (s, 2H), 4.47 (t, 2H), 4.23 (m, 1H), 3.75-3.50 (m, 2H), 3.55 (s, 4H), 3.12 (q, 2H), 2.06 (m, 2H), 1.33 (s, 9H); High resolution mass spectrum (NH.sub.3 --CI) calculated (M+H.sup.+) 564.2934, found 564.2959.

D. 3-�1-�3-(N-4,5-Dihydroimidazol-2-ylamino)propyl!indazol-5-ylcarbonylamino)-2(S)-(benzyloxycarbonylamino)propionic acid trifluoroacetate

Using the procedure of Example 1081 Part H, the product prepared according to Example 1198 Part C (108 mg, 180 .mu.mol) was converted to the title product (74 mg, 75%) as a hygroscopic, off-white solid: .sup.1 H NMR (DMSO-d.sub.6) .delta. 8.57 (bt, 1H), 8.31 (s, 1H), 8.28 (m, 1H), 8.24 (s, 1H), 7.88 (d, 1H), 7.72 (d, 1H), 7.62 (m, 1H), 7.32 (m, 5H), 5.02 (s, 2H), 4.47 (t, 2H), 4.29 (m, 1H), 3.65 (m, 2H), 3.55 (s, 4H), 3.11 (q, 2H), 2.06 (m, 2H); High resolution mass spectrum (FAB) calculated (M+H.sup.+) 508.2308, found 508.2323.

EXAMPLE 1213

3-�1-�3-(N-4,5-Dihydroimidazol-2-ylamino)-propyl!indazol-5-ylcarbonylamino!-2(S)-(benzenesulfonylamino)propionic acid trifluoroacetate

A. tert-Butyl 3-�1-�3-(N-4,5-dihydroimidazol-2yl-amino)propyl!indazol-5-ylcarbonylamino!-2(S)-(benzenesulfonylamino)propionate hydrochloride

A mixture of tert-butyl 3-benzyloxycarbonylamino-2-(S)-benzenesulfonylamino)propionate (200 mg, 460 .mu.mol), methanol (15 mL) and 10% palladium on charcoal (25 mg) was stirred at room temperature. Hydrogen gas was bubbled through the solution for 5 minutes, and a hydrogen-filled balloon was then placed on the reaction flask. The mixture was stirred at room temperature for 3 h, then was filtered through Celite.RTM.. The solids were washed with methanol and the filtrate was concentrated. The residue was mixed with a portion of the intermediate residue obtained in Example 1198 Part C (149 mg, 460 .mu.mol), 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide hydrochloride (120 mg, 626 .mu.mol), 1-hydroxybenzotriazole hydrate (20 mg), dry N,N-dimethylformamide (10 mL) and triethylamine (0.2 mL). The mixture was stirred at room temperature for 16 h. The solvent was removed under vacuum and the residue was purified by flash chromatography (dichloromethane:ethanol 75:25) to provide the title product (220 mg, 78%) as a gum: .sup.1 H NMR (CDCl.sub.3) .delta. 8.66-7.04 (m, 13H), 5.99 (bs, 1H), 4.52-1.98 (m, 15H), 1.30 (s, 9H); High resolution mass spectrum calculated (M+H.sup.+) 570.2499, found 570.2503.

B. 3-�1-�3-(N-4,5-Dihydroimidazol-2-ylamino)propyl!-indazol-5-ylcarbonylamino!-2(S)-(benzenesulfonylamino)propionic acid trifluoroacetate

Using the procedure of Example 1081 Part H, the product prepared according to Example 1213 Part A (202 mg, 333 .mu.mol) was converted to the title product (151 mg, 82%) as a hygroscopic solid: .sup.1 H NMR (DMSO-d.sub.6) .delta. 8.56-7.08 (m, 15H), 4.54-2.01 (m, 13H); High resolution mass spectrum calculated (M+H.sup.+) 514.1873, found 514.1879.

EXAMPLE 1216b

3-�1-�3-(N-4,5-Dihydroimidazol-2-ylamino)propyl!indazol-5-ylcarbonylamino!-2(S)-(2,4,6-trimethylbenzenesulfonylamino)propionic acid trifluoroacetate

A. tert-Butyl 3-�1-�3-(N-4,5-dihydroimidazol-2-yl-amino)propyl!indazol-5-ylcarbonylamino-2(S)-(2,4,6-trimethylbenzenesulfonylamino)propionate hydriodide

A mixture of the product prepared according to Example 1178b Part G (60 mg, 110 .mu.mol), 2-methylthioimidazoline hydriodide (32 mg, 130 .mu.mol) and pyridine (5 mL) was heated on an oil bath at 120.degree. C. After 16 h, the mixture was cooled to room temperature and concentrated under vacuum. The residue was purified by flash chromatography (dichloromethane:methanol, step gradient from 98:2 to 90:10) to provide the title product (30 mg, 37%): .sup.1 H NMR (CDCl.sub.3) .delta. 8.03 (s, 1H), 7.82 (s, 1H), 7.73 (d, 1H), 7.70 (bm, 1H), 7.31 (d, 1H), 6.84 (s, 1H), 4.39 (m, 2H), 3.99 (m, 1H), 3.78 (m, 2H), 3.48 (s, 4H), 3.01 (m, 2H), 2.60 (s, 6H), 2.21 (m, 2H), 2.17 (s, 3H), 1.24 (s, 9H); High resolution mass spectrum (FAB) calculated (M+H.sup.+) 612.2968, found 612.2975.

B. 3-�1-�3-(N-4,5-Dihydroimidazol-2-ylamino)propyl!indazol-5-ylcarbonylamino!-2(S)-(2,4,6-trimethylbenzenesulfonylamino)propionic acid trifluoroacetate

Using the procedure of Example 1129 Part H, followed by purification by preparative reverse phase high pressure liquid chromatography (acetonitrile:water containing 0.05% trifluoroacetic acid; gradient from 10:90 to 90:10), the product prepared according to Example 1216b Part A was converted to the title product (15 mg, 48%): .sup.1 H NMR (MeOH-d.sub.4) .delta. 8.16 (s, 2H), 7.79 (d, 1H), 7.59 (d, 1H), 6.76 (s, 2H), 4.52 (t, 2H), 4.16 (dd, 1H), 3.77 (dd, 1H), 3.59 (s, 4H), 3.47 (dd, 1H), 3.16 (m, 2H), 2.57 (s, 6H), 2.18 (m, 2H), 2.02 (s, 3H); High resolution mass spectrum (FAB) calculated (M+H.sup.+) 556.2372, found 556.2342.

EXAMPLE 1326b

3-�1-�1-(RS)-Methyl-3-(N-pyridin-2ylamino)propyl!indazol-5-ylcarbonylamino!-2(S)-(2,4,6-trimethylbenzenesulfonylamino)propionic acid trifluoroacetate

A. 1-(1-(RS)-methyl-2-cyanoethyl)-5-ethoxycarbonylindazole

A mixture of the product prepared according to Example 1050e Part C (1.90 g, 10 mmol), crotononitrile (4.9 mL, 60 mmol), sodium bis(trimethylsilyl)amide (1.0M in tetrahydrofuran; 0.5 mL, 0.5 mmol) and ethanol (20 mL) was heated at reflux for 18 h. The solution was cooled to room temperature and treated with aqueous hydrochloric acid (1.0M; 0.5 mL). The solvent was removed under vacuum, and the residue was taken up in dichloromethane and washed with water. The organic phase was dried over anhydrous magnesium sulfate, filtered, and concentrated under vacuum. The residue was purified by flash chromatography (hexanes:ethyl acetate 60:40) to provide the title product (2.49 g, 96%) as a viscous syrup which gradually solidified on standing: .sup.1 H NMR (CDCl.sub.3) .delta. 8.53 (s, 1H), 8.17 (s, 1H), 8.11 (d, 1H), 7.45 (d, 1H), 5.03 (m, 1H), 4.41 (q, 2H), 3.05 (m, 2H), 1.74 (d, 3H), 1.43 (t, 3H); High resolution mass spectrum (NH.sub.3 --CI) calculated (M+H.sup.+) 258.1243, found 258.1248.

B. 1-(1-(RS)-methyl-3-aminopropyl)-5-ethoxycarbonylindazole hydrochloride

Using the procedure of Example 1129 Part B, the product prepared according to Example 1326b Part A (2.0 g, 7.8 mmol) was converted into the title product (2.22 g, 96%) as a pale yellow, hygroscopic glass: .sup.1 H NMR (DMSO-d.sub.6) .delta. 8.48 (s, 1H), 8.33 (s, 1H), 8.10 (bs, 3H), 7.96 (d, 1H), 7.88 (d, 1H), 5.11 (m, 1H), 4.34 (q, 2H), 2.75 (bm, 1H), 2.45 (bm, 1H), 2.30 (bm, 1H), 2.15 (bm, 1H), 1.49 (d, 3H), 1.35 (t, 3H); high resolution mass spectrum (NH.sub.3 --CI) calculated (M+H.sup.+) 262.1556, found 262.1561.

C. 1-(1-(RS)-methyl-3-�N-(1-oxido)pyridin-2-ylamino!propyl)-5-ethoxycarbonylindazole. Using the procedure of Example 1081 Part C, the product prepared according to Example 1326b Part B (596 mg, 2.0 mmol) was converted into the title product (312 mg, 44%) as a tan glass: .sup.1 H NMR (CDCl.sub.3 ) .delta. 8.52 (s, 1H), 8.18 (s, 1H), 8.09 (d, 1H), 7.98 (d, 1H), 7.38 (d, 1H), 6.99 (t, 1H), 6.82 (bt, 1H), 6.51 (d, 1H), 4.90 (m, 1H), 4.41 (q, 2H), 3.12 (m, 1H), 2.95 (m, 1H), 2.61 (m, 1H), 2.22 (m, 1H), 1.62 (d, 3H), 1.42 (t, 3H); High resolution mass spectrum (NH.sub.3 --CI) calculated (M+H.sup.+) 355.1770, found 355.1771. D. 1-(1-(RS)-methyl-3-�N-pyridin-2-ylamino!propyl)-5-ethoxycarbonylindazole

A mixture of the product prepared according to Example 1326b Part C (292 mg, 824 .mu.mol), polymer-supported triphenylphosphine (550 mg, ca. 1.65 mmol) and N,N-dimethylformamide (5 mL) was heated on an oil bath at 160.degree. C. After 18.5 h, an additional aliquot of polymer-supported triphenylphosphine (550 mg) was added, and the reaction was heated for 24 h more. The mixture was cooled to room temperature and filtered. The solid was washed with N,N-dimethylformamide, and the filtrate was concentrated under vacuum. The residue was purified by flash chromatography (dichloromethane:methanol 96:4) and rotary thin-layer chromatography (dichloromethane:methanol 97:3) to provide the title product (189 mg, 67%) as a pale yellow gum which gradually solidified on standing: .sup.1 H NMR (CDCl.sub.3) .delta. 8.52 (s, 1H), 8.16 (s, 1H), 8.05-8.00 (m, 2H), 7.41 (d, 1H), 7.33 (t, 1H), 6.54 (t, 1H), 6.19 (d, 1H), 4.87 (m, 1H), 4.50-4.30 (m, 3H), 3.16 (m, 1H), 3.05 (m, 1H), 2.45 (m, 1H), 2.23 (m, 1H), 1.61 (d, 3H), 1.42 (t, 3H); High resolution mass spectrum (NH.sub.3 --CI) calculated (M+H.sup.+) 339.1821, found 339.1832.

E. 1-(1-(RS)-methyl-3-�N-pyridin-2-ylamino!propyl)-5-carboxyindazole

A mixture of the product prepared according to Example 1326b Part D (180 mg, 532 .mu.mol), aqueous sodium hydroxide (1.0M; 2.13 mL, 2.13 mmol) and ethanol (4 mL) was heated to reflux. After 4.25 h, the solution was cooled to room temperature and concentrated under vacuum. The residue was used directly in the next reaction without purification or characterization.

F. tert-Butyl 3-�1-�1-(RS)-methyl-3-(N-pyridin-2-ylamino)propyl!indazol-5-ylcarbonylamino!-2-(S)-(2,4,6-trimethylbenzenesulfonylamino)propionate

The product of Example 1326b Part E was combined with the product prepared according to Example 1178b Part E (183 mg, 535 .mu.mol), 1-hydroxybenzotriazole hydrate (72 mg, 535 .mu.mol), N,N-dimethylformamide (8 mL), and triethylamine (1 drop), and the mixture was treated with dicyclohexylcarbodiimide (121 mg, 589 .mu.mol) and stirred at room temperature. After 21.75 h, the mixture was diluted with ethyl acetate and filtered. The filtrate was concentrated under vacuum, and the residue was purified by flash chromatography (dichloromethane:methanol 97:3) to provide the title product (286 mg, 85%) as a colorless glass: .sup.1 H NMR (CDCl.sub.3) .delta. 8.21 (s, 1H), 8.12 (s, 1H), 8.04 (dd, 1H), 7.77 (dt, 1H), 7.40 (d, 1H), 7.33 (t, 1H), 6.93 (s, 2H), 6.87 (bt, 1H), 6.53 (dd, 1H), 6.18 (d, 1H), 6.01 (bs, 1H), 4.86 (bm, 1H), 4.51 (m, 1H), 4.0-3.8 (m, 2H), 3.65 (m, 1H), 3.15 (m, 1H), 3.03 (m, 1H), 2.66 (s, 6H), 2.44 (m, 1H), 2.26 (s, 3H), 2.22 (m, 1H) 1.61 (d, 3H), 1.30 (s, 9H); High resolution mass spectrum (FAB) calculated (M+H.sup.+) 635.3016, found 635.3019.

G. 3-�1-�1-(RS)-Methyl-3-(N-pyridin-2-ylamino)propyl!indazol-5-ylcarbonylamino!-2(S)-(2,4,6-trimethylbenzenesulfonyl)aminopropionic acid trifluoroacetate

Using the procedure of Example 1129 Part H, the product prepared according to Example 1326b Part F (109 mg, 172 .mu.mol) was converted to the title product (92 mg, 77%) as a white powder: .sup.1 H NMR (DMSO-d.sub.6) .delta. 8.43 (bt, 2H), 8.27 (s, 1H), 8.17 (s, 1H), 8.06 (d, 1H), 7.8-7.6 (m, 4H), 6.87 (d, 1H), 6.82 (d, 2H), 6.74 (t, 1H), 5.02 (m, 1H), 4.02 (q, 1H), 3.57 (m, 1H), 3.40 (m, 1H), 3.07 (m, 2H), 2.53 (s, 6H), 2.37 (m, 1H), 2.21 (m, 1H), 2.05 (s, 3H), 1.52 (d, 3H); High resolution mass spectrum (FAB) calculated (M+H.sup.+) 579.2390, found 579.2405.

EXAMPLE 1326f

3-�1-�3-(N-pyridin-2ylamino)propyl!-3-phenylindazol-5-ylcarbonylamino!-2(S)-(2,4,6-trimethylbenzenesulfonylamino)propionic acid trifluoroacetate

A. 3-Bromo-5-ethoxycarbonylindazole

A solution of the product prepared according to Example 1050e Part C (3.80 g, 20 mmol) in acetic acid (120 mL) was stirred at room temperature and treated with bromine (1.55 mL, 30 mmol). The mixture was stirred in the dark for 51 h, then was poured into water (600 mL). The resulting slurry was stirred at room temperature and treated with small portions of solid sodium bisulfite, whereupon the original orange color faded to almost white. After stirring 20 min more, the solid was collected by filtration, rinsed with water and dried to provide the title product (5.14 g, 96%) as a white solid. While pure enough for use in subsequent reactions, this material could be purified further by flash chromatography (hexanes:ethyl acetate 70:30): .sup.1 H NMR (DMSO-d.sub.6) .delta. 13.80 (bs, 1H), 8.20 (d, 1H), 8.01 (dd, 1H), 7.69 (d, 1H), 4.36 (q, 2H), 1.37 (t, 3H); Mass spectrum (NH.sub.3 --CI) m/z 269 (100%), 271 (95%) (M+H.sup.+).

B. 3-Phenyl-5-ethoxycarbonylindazole

A mixture of the product prepared according to Example 1326f Part A (2.69 g, 10.0 mmol), phenylboronic acid (1.71 g, 14.0 mmol), triethylamine (5.6 mL, 40.0 mmol), and N,N-dimethylformamide (20 mL) was purged of oxygen by bubbling with nitrogen for 20 min. Tetrakis(triphenylphosphine)palladium (580 mg, 500 .mu.mol) was added, and the mixture was heated on an oil bath at 110.degree. C. under nitrogen. After 48 h, the mixture was cooled to room temperature and diluted with water. The mixture was extracted with ethyl acetate, and the organic phase was dried over anhydrous magnesium sulfate, filtered and concentrated under vacuum. The residue was purified by flash chromatography (hexanes:ethyl acetate 80:20) to provide the title product (542 mg, 20 %) as a white solid: .sup.1 H NMR (CDCl.sub.3 ) .delta. 11.44 (bs, 1H), 8.78 (s, 1H), 8.06 (d, 1H), 8.01 (d, 2H), 7.57 (t, 2H), 7.49 (t, 1H), 7.30 (d, 1H), 4.44 (q, 2H), 1.43 (t, 3H); High resolution mass spectrum (NH.sub.3 --CI) calculated (M+H.sup.+) 267.1134, found 267.1132.

C. 1-(2-Cyanoethyl)-3-phenyl-5-ethoxycarbonylindazole

Using the procedure of Example 1129 Part A, followed by purification by flash chromatography (hexanes:ethyl acetate 70:30),the product prepared according to Example 1326f Part B (266 mg, 1.0 mmol) was converted to the title product (263 mg, 82%) as a white solid: mp 99.degree.-102.degree. C.; .sup.1 H NMR (CDCl.sub.3) .delta. 8.77 (s, 1H), 8.16 (d, 1H), 7.96 (m, 2H), 7.60-7.40 (m, 4H), 4.73 (t, 2H), 4.43 (q, 2H), 3.10 (t, 2H), 1.44 (t, 3H); High resolution mass spectrum (NH.sub.3 --CI) calculated (M+H.sup.+) 320.1399, found 320.1386.

D. 1-(3-aminopropyl)-3-phenyl-5-ethoxycarbonylindazole hydrochloride

Using the procedure of Example 1129 Part B, the product prepared according to Example 1326f Part C (214 mg, 670 .mu.mol) was converted to the title product (260 mg, >100%) as a tan solid which was not purified, but was used directly in subsequent reactions: .sup.1 H NMR (DMSO-d.sub.6) .delta. 8.64 (s, 1H), 8.05 (d, 1H), 8.0-7.9 (m), 7.60 (t, 2H), 7.49 (m, 1H), 4.63 (t, 2H), 4.37 (q, 2H), 2.90 (m, 2H), 2.18 (m, 2H), 1.36 (t, 3H); High resolution mass spectrum (ESI) calculated (M+H.sup.+) 323.1634, found 323.1645.

E. 1-�3-(N-(1-oxido)pyridin-2-ylamino)propyl!-3phenyl-5-ethoxycarbonylindazole

Using the procedure of Example 1081 Part C, the crude product of Example 1326f Part D was converted into the title product (122 mg, 43%) as a tan glass: .sup.1 H NMR (CDCl.sub.3) .delta. 8.78 (s, 1H), 8.13 (d, 1H), 8.07 (d, 1H), 7.99 (d, 2H), 7.55 (t, 2H), 7.47 (d, 1H), 7.42 (d, 1H), 7.09 (t, 1H), 6.97 (bt, 1H), 6.56 (t, 1H), 6.47 (d, 1H), 4.59 (t, 2H), 4.43 (q, 2H), 3.32 (q, 2H), 2.41 (m, 2H), 1.43 (t, 3H); High resolution mass spectrum (NH.sub.3 --CI) calculated (M+H.sup.+) 417.1927, found 417.1918.

F. 1-�3-(N-pyridin-2-ylamino)propyl!-3-phenyl-5-ethoxycarbonylindazole

Using the procedure of Example 1129 Part F, the product prepared according to Example 1326f Part E (106 mg, 255 .mu.mol) was converted to the title product (39 mg, 38%) as a glass: .sup.1 HNMR (CDCl.sub.3) .delta. 8.77 (s, 1H), 8.08 (m, 2H), 7.98 (d, 2H), 7.54 (t, 2H), 7.5-7.3 (m, 3H), 6.56 (t, 1H), 6.32 (d, 1H), 4.77 (bt, 1H), 4.55 (t, 2H), 4.42 (q, 2H), 3.35 (q, 2H), 2.30 (m, 2H), 1.43 (t, 3H); High resolution mass spectrum (NH.sub.3 --CI) calculated (M+H.sup.+) 401.1978, found 401.1977.

G. tert-Butyl 3-�1-�3-(N-pyridin-2-ylamino)propyl!-3-phenylindazol-5-ylcarbonylamino!-2(S)-(2,4,6-trimethylbenzenesulfonylamino)propionate

Using the procedures of Example 1326b Parts E and F, the product prepared according to Example 1326f Part F (38 mg, 95 .mu.mol) was converted to the title product (59 mg, 89%) as a glass: .sup.1 H NMR (CDCl.sub.3) .delta. 8.57 (s, 1H), 8.08 (d, 1H), 8.01 (d, 2H), 7.85 (d, 1H), 7.53 (t, 2H), 7.5-7.4 (m, 3H), 6.97 (m, 1H), 6.92 (s, 2H), 6.57 (dd, 1H), 6.33 (d, 1H), 5.86 (d, 1H), 4.57 (t, 2H), 3.98 (m, 1H), 3.83 (m, 1H), 3.53 (m, 1H), 3.35 (q, 2H), 2.65 (s, 6H), 2.31 (m, 2H), 2.24 (s, 3H), 1.31 (s, 9H); High resolution mass spectrum (FAB) calculated (M+H.sup.+) 697.3172, found 692.3184.

H. 3-�1-�3-(N-pyridin-2-yl)aminopropyl!3-phenylindazol-5-yl!carbonylamino-2(S)-(2,4,6-trimethylbenzenesulfonyl)aminopropionic acid trifluoroacetate

Using the procedure of Example 1129 Part H. the product prepared according to Example 1326f Part G (44 mg, 63 .mu.mol) was converted to the title product (32 mg, 80%) as an off-white powder: .sup.1 H NMR (DMSO-d.sub.6) .delta. 8.61 (bt, 1H), 8.38 (s, 1H), 8.08 (d, 1H), 8.01 (d, 2H), 7.88 (d, 1H), 7.82 (d, 1H), 7.75 (d, 1H), 7.71 (bm, 1H), 7.57 (t, 2H), 7.47 (t, 1H), 6.86 (bd, 1H), 6.72 (bt, 1H), 6.70 (s, 2H), 4.61 (t, 2H), 4.07 (in, 1H), 3.58 (m, 1H), 3.5-3.3 (m, 3H), 2.51 (s, 6H), 2.23 (in, 2H), 1.92 (s, 3H); High resolution mass spectrum (FAB) calculated (M+H.sup.+) 641.2546, found 641.2569.

EXAMPLE 1326g

3-�1-�3-(N-pyridin-2-ylamino)propyl!-3-(2-phenylethyl)indazol-5-ylcarbonylamino!-2(S)-(2,4,6-trimethylbenzenesulfonylamino)propionic acid trifluoroacetate

A. 3-Phenylethynyl-5-ethoxycarbonylindazole

A mixture of the product prepared according to Example 1326f Part A (269 mg, 1.0 mmol), triphenylphosphine (21 mg, 80 .mu.mol), copper(I) iodide (8 mg, 40 .mu.mol), phenylacetylene (165 .mu.L, 1.5 mmol) and diethylamine (5 mL) was purged of oxygen by bubbling with nitrogen for 35 min. Bis(triphenylphosphine)palladium(II) chloride (14 mg, 20 .mu.mol) was then added, and the mixture was heated to reflux under nitrogen. After 16.5 h, the mixture was cooled to room temperature and concentrated under vacuum. The residue was purified by flash chromatography (hexanes:ethyl acetate 80:20) to provide the title product (227 mg, 78%) as a yellowish solid: .sup.1 H NMR (CDCl.sub.3) .delta. 8.66 (s, 1H), 8.13 (d, 1H), 7.68 (m, 2H), 7.55 (d, 1H), 7.42 (m, 3H), 4.45 (q, 2H), 1.45 (t, 3H); High resolution mass spectrum (NH.sub.3 --CI) calculated (M+H.sup.+) 291.1134, found 291.1111.

B. 1-(2-Cyanoethyl)-3-(2-phenylethynyl)-5-ethoxycarbonylindazole

Using the procedure of Example 1129 Part A, the product prepared according to Example 1326g Part A (278 mg, 958 .mu.mol) was converted to the title product (254 mg, 77%) as a tan solid: mp 90.degree.-94.degree. C.; .sup.1 H NMR (CDCl.sub.3) .delta. 8.63 (s, 1H), 8.17 (d, 1H), 7.67 (m, 2H), 7.52 (d, 1H), 7.42 (m, 3H), 4.70 (t, 2H), 4.45 (q, 2H), 3.09 (t, 2H), 1.46 (t, 3H); High resolution mass spectrum (NH.sub.3 --CI) calculated (M+H.sup.+) 344.1399, found 344.1391.

C. 1-(3-Aminopropyl)-3-(2-phenylethyl)-5-ethoxycarbonylindazole hydrochloride

Using the procedure of Example 1129 Part B. the product prepared according to Example 1326g Part B (240 mg, 699 .mu.mol) was converted to the title product (277 mg, >100%) as a pale yellow solid which was not purified, but was used directly in subsequent reactions: .sup.1 H NMR (DMSO-d.sub.6) .delta. 4.50 (m, 2H), 3.28 (t, 2H), 3.05 (t, 2H), 2.80 (m, 2H), 2.10 (m, 2H).

D. 1-�3-�N-(1-oxido)pyridin-2-ylamino!propyl!-3-(2-phenylethyl)-5-ethoxycarbonylindazole

Using the procedure of Example 1081 Part C, the crude product of Example 1326g Part C was converted into the title product (145 mg, 46%) as a pale yellow glass which was not purified but was used in subsequent reactions: Mass spectrum (ESI) m/z 445.4 (100%, M+H.sup.+).

E. 1-�3-�N-pyridin-2-ylamino!propyl!-3-(2phenylethyl)-5-ethoxycarbonylindazole

Using the procedure of Example 1326b Part D, the impure product of Example 1326g Part D was converted to the title product (90 mg, 70%) as a yellow gum, which impure but was used in subsequent reactions without further purification.

F. tert-Butyl 3-�1-�3-(N-pyridin-2-ylamino)propyl!-3-(2-phenylethyl)indazol-5-ylcarbonylamino!-2(S)-(2,4,6-trimethylbenzenesulfonylamino)propionate

Using the procedures of Example 1326b Parts E and F, the impure product of Example 1326g Part E was converted to the title product (98 mg, 64%) as a glass, which was impure but was used without further purification in the subsequent reaction.

G. 3-�1-�3-(N-pyridin-2-ylamino)propyl!-3-(2phenylethyl)indazol-5-ylcarbonylamino!-2(S)-(2,4,6-trimethylbenzenesulfonylamino)propionic acid trifluoroacetate

Using the procedure of Example 1129 Part H, the impure product of Example 1326g Part F was converted to the title product. The crude material was purified by preparative reverse-phase high pressure liquid chromatography (acetonitrile-water containing 0.05% trifluoroacetic acid, gradient from 10:90 to 90:10) to provide the title product (20 mg, 20 %) as an off-white powder: High resolution mass spectrum (FAB) calculated (M+H.sup.+) 669.2859, found 669.2881.

EXAMPLE 1327b

3-�1-�2-(N-Imidazol-2-ylaminocarbonyl)ethyl!indazol-5-ylcarbonylamino!-2(S)-(2,4,6-trimethylbenzenesulfonylamino)propionic acid trifluoroacetate

A. 1-(2-tert-Butyloxycarbonylethyl)-5-ethoxycarbonylindazole

A mixture of the product prepared according to Example 1050e Part C (2.0 g, 10.5 mmol), tert-butyl acrylate (9.3 mL, 63.5 mmol) and ethanol (21 mL) was treated with sodium bis(trimethylsilyl)amide (1.0M in tetrahydrofuran; 530 .mu.L, 530 .mu.mol). The resulting solution was heated at reflux for 3 h, then was cooled to room temperature. Aqueous hydrochloric acid (1.0M; 550 .mu.L, 550 .mu.mol) was added, and the mixture was concentrated. The residue was partitioned between ether and water, and the aqueous phase was extracted further with ether. The combined organic phases were dried over anhydrous sodium sulfate, filtered and concentrated under vacuum. The residue was purified by flash chromatography (hexanes:ethyl acetate 85:15) to provide the title product (830 mg, 25%): .sup.1 H NMR (CDCl.sub.3) .delta. 8.49 (s, 1H), 8.10 (s, 1H), 8.07 (d, 1H), 7.50 (d, 1H), 4.64 (t, 2H), 4.41 (q, 2H), 2.91 (t, 2H), 1.42 (t, 3H), 1.33 (s, 9H); high resolution mass spectrum (NH.sub.3 --CI) calculated (M+H.sup.+) 319.1658, found 319.1655.

B. 1-(2-Carboxyethyl)-5-ethoxycarbonylindazole

A solution of the product prepared according to Example 1327b Part A (791 mg, 2.49 mmol) in dichloromethane (28 mL) was treated with trifluoroacetic acid (6 mL). The mixture was stirred at room temperature for 16 h, then was concentrated under vacuum. Addition of ether to the residue produced, after filtering and drying, the title product (571 mg, 88%) as a white solid: .sup.1 H NMR (CDCl.sub.3) .delta. 8.52 (s, 1H), 8.12 (s, 1H), 8.09 (d, 1H), 7.49 (d, 1H), 4.67 (t, 2H), 4.41 (q, 2H), 3.07 (t, 2H), 1.42 (t, 3H); Mass spectrum (ESI) m/z 263.3 (100%, M+H.sup.+).

C. 1-(2-(N-imidazol-2-ylaminocarbonyl)ethyl)-5-ethoxycarbonylindazole

A mixture of the product prepared according to Example 1327b Part B (352 mg, 1.34 mmol), 2-aminoimidazole sulfate (0.55 g, 4.15 mmol), diisopropylethylamine (1.17 mL, 6.7 mL) and N,N-dimethylformamide (7 mL) was treated with benzotriazol-1-yloxy-tris(dimethylamino)phosphonium hexafluorophosphonate (BOP Reagent; 891 mg, 2.0 mmol) and warmed to 70.degree. C. on an oil bath. The mixture was stirred at this temperature for 18 h, then was cooled to room temperature and diluted with water (75 mL). The resulting precipitate was collected by filtration to provide the title product (310 mg, 71%) which was used in subsequent reactions without further purification: .sup.1 H NMR (CDCl.sub.3) .delta. 8.49 (s, 1H), 8.11 (s, 1H), 8.07 (d, 1H), 7.88 (b, 1H), 7.55 (d, 1H), 7.40 (b, 1H), 4.75 (t, 2H), 4.41 (q, 2H), 3.01 (t, 2H), 1.42 (t, 3H); high resolution mass spectrum (NH.sub.3 --CI) calculated (M+H.sup.+) 328.1046, found 328.1031.

D. 1-(2-(N-imidazol-2-ylaminocarbonyl)ethyl)-5-carboxyindazole

A mixture of the product of Example 1327b Part C (145 mg, 443 .mu.mol), tetrahydrofuran (2 mL) and water (2 mL) was treated with aqueous lithium hydroxide (1.0 M; 0.56 mL, 560 .mu.mol) and stirred at room temperature for 21 h. The reaction was incomplete by thin-layer chromatography, so additional lithium hydroxide solution (a total of 1.35 mL) was added in four portions over the next 8 h. After stirring for 16 h more, the reaction was acidified with aqueous hydrochloric acid (1.0M) and concentrated under vacuum. The residue was partitioned between water and dichloromethane, and the organic phase was dried over anhydrous magnesium sulfate, filtered and concentrated to provide the title product (49 mg, 37%): .sup.1 H NMR (DMSO-d.sub.6) .delta. 8.41 (s, 1H), 8.24 (s, 1H), 7.94 (d, 1H), 7.76 (d, 1H), 6.67 (s, 2H), 4.73 (t, 2H), 3.00 (t, 2H); High resolution mass spectrum (NH.sub.3 --CI) calculated (M+H.sup.+) 300.1097, found 300.1097.

E. tert-Butyl 3-�1-�2-(N-imidazol-2ylaminocarbonyl)ethyl!indazol-5-ylcarbonylamino!-2-(S)-(2,4,6-trimethylbenzenesulfonylamino)propionate

Using the procedure of Example 1326b Part F, the product prepared according to Example 1327b Part D (48 mg, 160 .mu.mol) was converted to the title product (32 mg, 32%): Mass spectrum (ESI) m/z 624.4 (100%, M+H.sup.+).

F. 3-�1-�2-(N-imidazol-2-ylaminocarbonyl)ethyl!indazol-5-ylcarbonylamino!-2(S)-(2,4,6-trimethylbenzenesulfonylamino)propionic acid trifluoroacetate

Using the procedure of Example 1081 Part H followed by purification by preparative reverse phase high pressure liquid chromatography (acetonitrile:water containing 0.05% trifluoroacetic acid, gradient from 10:90 to 90:10), the product prepared according to Example 1327b Part E (32 mg, 52 .mu.mol) was converted to the title product (28 mg, 95%) as a white powder after lyophilization: .sup.1 H NMR (MeOH-d.sub.4) .delta. 8.11 (s, 1H), 8.09 (s, 1H), 7.77 (d, 1H), 7.68 (d, 1H), 7.10 (s, 2H), 6.73 (s, 2H), 4.81 (t, 2H), 4.14 (dd, 1H), 3.75 (dd, 1H), 3.47 (dd, 1H), 3.19 (t, 1H), 2.56 (s, 6H), 1.97 (s, 3H); high resolution mass spectrum (FAB) calculated (M+H.sup.+) 568.1978, found 568.1972.

EXAMPLE 2328

3-�1-�4-(N-4,5-Dihydroimidazol-2-ylamino)butyl!indazol-4-ylcarbonylamino!-2(S)-(benzyloxycarbonylamino)propionic acid trifluoroacetate

A. Methyl 2-methyl-3-aminobenzoate

A mixture of methyl 2-methyl-3-nitrobenzoate (30 g, 154 mmol), 10% palladium on charcoal (3.0 g) and ethanol (350 mL) was shaken under hydrogen at 50 psig. After 4 h, the mixture was filtered through Celite.RTM. and the solids were washed with additional ethanol. The filtrate was concentrated to provide the title product (24.4 g, 96%) as a tan oil: .sup.1 H NMR (CDCl.sub.3) .delta. 7.18 (m, 1H), 7.06 (m, 1H), 6.78 (m, 1H), 3.85 (s, 3H), 2.34 (s, 3H); high resolution mass spectrum (NH.sub.3 --CI) calculated (M+H.sup.+) 166.0868, found 166.0866.

B. 4-Methoxycarbonylindazole

The product prepared according to Example 2328 Part A (24.25 g, 147 mmol) was combined with concentrated hydrochloric acid (30.1 mL) and water (170 mL). Ammonium tetrafluoroborate (20.62 g, 197 mmol) was added and the mixture was stirred at 0.degree. C. A solution of sodium nitrite (10.14 g, 147 mmol) in water (25 mL) was added dropwise, and the mixture was stirred for 40 min after addition was complete. The white precipitate was collected by filtration and washed with water (3.times.80 mL), then with methanol (80 mL) and finally with ether (3.times.60 mL). The resulting solid was added to a stirred mixture of potassium acetate (17.89 g, 182 mmol), 18-crown-6 (1.20 g, 4.5 mmol) and chloroform (360 mL) at room temperature. The resulting mixture was stirred for 50 min, then water (250 mL) was added and the layers were separated. The organic phase was washed with water (250 mL) and brine (300 mL), and drIed over anhydrous magnesium sulfate, filtered and concentrated under reduced pressure. The residue was triturated with hexanes and filtered to provide after drying the title product (16.96 g, 62%) as an orange solid: .sup.1 H NMR (CDCl.sub.3) .delta. 8.60 (s, 1H), 7.98 (d, 1H), 7.74 (d, 1H), 7.42 (t, 1H), 4.01 (s, 3H); High resolution mass spectrum (NH.sub.3 --CI) calculated (M+H.sup.+) 177.0664, found 177.0669.

C. 1-�4-(N-phthalimido)butyl!-4-methoxycarbonylindazole

Following the procedure of Example 1081 Part A, the product prepared according to Example 2328 Part B (2.97 g, 16.9 mmol) and N-(4-bromobutyl)phthalimide (4.99 g, 16.9 mmol) were converted to the title product (1.88 g, 29%) as an orange oil: .sup.1 H NMR (CDCl.sub.3) .delta. 8.45 (s, 1H), 7.91 (d, 1H), 7.82 (m, 2H), 7.72 (m, 2H), 7.66 (d, 1H), 7.43 (t, 1H), 4.46 (t, 2H), 4.02 (t, 3H), 3.75 (t, 2H), 1.99 (m, 2H), 1.72 (m, 2H); Mass spectrum (NH.sub.3 --CI) m/z 378.0 (100%, M+H.sup.+).

D. 1-�4-(Aminobutyl)-4-methoxycarbonylindazole

Using the procedure of Example 1081 Part B, the product prepared according to Example 2328 Part C (1.81 g, 4.8 mmol) was converted to the title product (0.72 g, 60%) as a yellow oil: .sup.1 H NMR (CDCl.sub.3) .delta. 8.48 (s, 1H), 7.93 (d, 1H), 7.64 (d, 1H), 7.44 (t, 1H), 4.44 (t, 2H), 4.02 (s, 3H), 2.74 (t, 2H), 2.00 (m, 2H), 1.84 (bs, 2H), 1.47 (m, 2H); High resolution mass spectrum (NH.sub.3 --CI) calculated (M+H.sup.+); 248.1399, found 248.1391.

E. 1-�4-(N-4,5-Dihydroimidazol-2ylamino)butyl!-4-methoxycarbonylindazole hydriodide

Using the procedure of Example 1198 Part B, the product prepared according to Example 2328 Part D (247 mg, 1.0 mmol) was converted to the title product (223 mg, 50%) as a gum. .sup.1 H NMR (DMSO-d.sub.6) .delta. 8.37 (s, 1H), 8.11 (bs, 1H), 8.01 (d, 1H), 7.82 (d, 1H), 7.51 (t, 1H), 4.46 (t, 2H), 3.90 (s, 3H), 3.53 (s, 4H), 3.08 (m, 2H), 1.81 (m, 2H), 1.38 (m, 2H); High resolution mass spectrum (NH.sub.3 --CI) calculated (M+H.sup.+) 316.1774, found 316.1772.

F. tert-Butyl 3-�1-�4-(N-4,5-dihydroimidazol-2-yl-amino)butyl!indazol-4-ylcarbonylamino!-2(S)-(benzyloxycarbonylamino)propionate hydrochloride

Using the procedure of Example 1198 Part C, the product prepared according to Example 2328 Part E (215 mg, 485 .mu.mol) was converted to the title product (178 mg, 59%) as a clear gum: .sup.1 H NMR (DMSO-d.sub.6) .delta. 8.52 (m, 1H), 8.32 (s, 1H), 8.13 (bm, 1H), 7.85 (d, 1H), 7.69 (d, 1H), 7.50 (t, 2H), 7.45 (m, 1H), 7.30 (m, 5H), 5.01 (s, 2H), 4.44 (t, 2H), 4,24 (m, 1H), 3.75-3.50 (m, 2H), 3.50 (s, 4H), 3.19 (m, 2H), 1.80 (m, 2H), 1.37 (m, 2H), 1.31 (s, 9H); High resolution mass spectrum (FAB) calculated (M+H.sup.+); 578.3091, found 578.3119.

G. 3-�1-�4-(N-4,5-Dihydroimidazol-2-ylamino)butyl!indazol-4-ylcarbonylamino!-2(S)-(benzyloxycarbonylamino)propionic acid hydrochloride

Using the procedure of Example 1081 Part H, the product prepared according to Example 2328 Part F (121 mg, 197 .mu.mol) was converted to the title product (88 mg, 80%) as a hygroscopic white solid: .sup.1 H NMR (DMSO-d.sub.6) .delta. 8.57 (m, 1H), 8.31 (s, 1H), 8.18 (bm, 1H), 7.86 (d, 1H), 7.63 (d, 1H), 7.50-7.35 (m, 3H), 7.30 (m, 5H), 5.00 (s, 2H), 4.43 (t, 2H), 4,28 (m, 1H), 3.75-3.40 (m, 6H), 3.07 (m, 2H), 1.78 (m, 2H), 1.38 (m, 2H); High resolution mass spectrum (FAB) calculated (M+H.sup.+); 522.2465, found 522.2484.

EXAMPLE 3093

3-�1-Methyl-3-�3-(N-imidazol-2-ylamino)propyl!indazol-6-ylcarbonylamino!-2(S)-(2,6-dimethylbenzenesulfonylamino)propionic acid trifluoroacetate

A. 6-Methoxycarbonylindazol

Using the procedure of Example 2328 Part B, methyl 3amino-4-methylbenzoate (12.39 g, 75 mmol) was converted to the title product (8.85 g, 67%) which could be recrystallized from acetonitrile to give pale orange crystals: mp 142.degree.-144.degree. C.; .sup.1 H NMR (CDCl.sub.3) .delta. 11.17 (bs, 1H), 8.30 (s, 1H), 8.18 (s, 1H), 7.83 (m, 2H), 3.97 (s, 3H); Mass spectrum (NH.sub.3 --CI) m/z 177 (100%, M+H.sup.+).

B. 3-Bromo-6-methoxycarbonylindazole

Using the procedure of Example 1326f Part A, the product prepared according to Example 3093 Part A (3.52 g, 20 mmol) was converted to the title product (4.46 g, 87%) as a light yellow powder: mp 186.degree.-189.degree. C.; .sup.1 H NMR (CDCl.sub.3) .delta. 8.24 (s, 1H), 7.91 (d, 1H), 7.70 (d, 1H), 3.92 (s, 3H); Mass spectrum (NH.sub.3 --CI) m/z 255 (100%), 257 (96%) (M+H.sup.+); High resolution mass spectrum (EI) calculated (M.sup.+) 253.9691, found 253.9694.

C. 1-Methyl-3-bromo-6-methoxycarbonylindazole

Sodium hydride (60% in mineral oil; 600 mg, 15 mmol) was placed in a dry flask under nitrogen and suspended in dry N,N-dimethylformamide (20 mL). The suspension was stirred on an ice bath and treated with a solution of the product prepared according to Example 3093 Part B (2.55 g, 10 mmol) in dry N,N-dimethylformamide (20 mL) over ca. 3 min. The resulting yellow solution was stirred for 10 min more, then was treated with iodomethane (0.7 mL, 11 mmol). The mixture was stirred at room temperature for 22.5 h, then was poured into water (ca. 600 mL). After being stirred for 10 min, the suspension was filtered, and the solid was washed with water and dried to provide the title product (2.57 g, 95%) as a yellow solid, which could be recrystallized from ethanol: mp 122.degree.-125.degree. C.; .sup.1 H NMR (CDCl.sub.3) .delta. 8.16 (s, 1H), 7.87 (d, 1H), 7.65 (d, 1H), 4.13 (s, 3H), 3.99 (s, 3H); Mass spectrum (NH.sub.3 --CI) m/z 269 (100%), 271 (92%) (M+H.sup.+); High resolution mass spectrum (NH.sub.3 --CI) calculated 268.9926, found 268.9914.

D. 1-Methyl-3-(3,3diethylpropyl)-6-methoxycarbonylindazole

A mixture of the product prepared according to Example 3093 Part C (1.93 g, 7.2 mmol), 3,3-diethoxypropyne (1.65 mL, 11.5 mmol), triphenylphosphine (190 mg, 720 .mu.mol), copper(I) iodide (68 mg, 360 .mu.mol) and triethylamine (60 mL) was purged of oxygen by bubbling with nitrogen for 25 min. Bis(triphenylphosphine)palladium(II) chloride (126 mg, 180 .mu.mol) was added, and the mixture was heated at 100.degree. C. After 14 h, the mixture was concentrated under a nitrogen stream and cooled to room temperature. The residue was purified by flash chromatography (hexanes:ethyl acetate 85:15) to provide an orange, sticky solid. This was recrystallized (methanol) to provide the title product (1.26 g, 56%) as light yellow fibrous needles: mp 91.degree.-93.degree. C.; .sup.1 H NMR (CDCl.sub.3) .delta. 8.18 (s, 1H), 7.88 (d, 1H), 7.83 (d, 1H), 5.59 (s, 1H), 4.14 (s, 3H), 3.98 (s, 3H), 3.89 (m, 2H), 3.72 (m, 2H), 1.30 (t, 6H); Mass spectrum (ESI) m/z 317.4 (100%, M+H.sup.+).

E. 1-Methyl-3-(3,3diethoxypropyl)-6-methoxycarbonylindazole

A mixture of the product prepared according to Example 3093 Part D (1.24 g, 3.92 mmol), 10% palladium, on charcoal (130 mg), methanol (40 mL) and tetrahydrofuran (60 mL) was placed in a pressure bottle and shaken under an atmosphere of hydrogen (60 psig). After 60 min, the bottle was vented and the mixture was filtered through Celite..RTM. The solids were rinsed with methanol and tetrahydrofuran, and the filtrate was concentrated under vacuum to provide the title product (1.31 g, >100%) as a slightly cloudy oil which was not purified further: .sup.1 H NMR (CDCl.sub.3) .delta. 8.11 (s, 1H), 7.77 (d, 1H), 7.72 (d, 1H), 4.57 (t, 1H), 4.08 (s, 3H), 3.97 (s, 3H), 3.69 (m, 2H), 3.52 (m, 2H), 3.06 (t, 2H), 2.13 (m, 2H), 1.22 (t, 6H); High resolution mass spectrum (NH.sub.3 --CI) calculated (M+H.sup.+) 321,1814, found 321.1830.

F. 1-Methyl-3-(3-oxopropyl)-6-methoxycarbonylindazole

A mixture of the product prepared according to Example 3093 Part E (1.29 g, 4.0 mmol), acetic acid (20 mL) and water (30 mL) was heated on an oil bath at 80.degree. C. After 30 min, the solvent was removed under vacuum, and the residue-was dissolved in ethyl acetate. The solution was washed with saturated aqueous sodium bicarbonate, dried over anhydrous magnesium sulfate, filtered and concentrated under vacuum to provide a light brown oil. On further concentration under vacuum, a tan solid slowly formed, which was the title product (982 mg, 98%): mp 80.degree.-83.degree. C.; .sup.1 H NMR (CDCl.sub.3) .delta. 9.92 (s, 1H), 8.11 (s, 1H), 7.79 (d, 1H), 7.71 (d, 1H), 4.07 (s, 3H), 3.98 (s, 3H), 3.31 (t, 2H), 3.03 (t, 2H); High resolution mass spectrum (NH.sub.3 --CI) calculated (M+H.sup.+) 247.1083, found 247.1077.

G. 1-Methyl-3-�3-�N-(1-triphenylmethylimidazol-2yl-amino)propyl!-6-methoxycarbonylindazole

A solution of the product prepared according to Example 3093 Part F (900 mg, 3.65 mmol) and the product prepared according to Example 1050e Part I (1.19 g, 3.65 mmol) in toluene (130 mL) was heated at reflux under an empty Dean-Stark water trap. After 22.5 h, additional toluene (ca. 40 mL) was removed by distillation, and the solution was cooled to room temperature under a nitrogen atmosphere. The solution was then cooled on an ice bath and treated with sodium triacetoxyborohydride (3.09 g, 14.6 mmol) and the mixture was stirred at room temperature for 21.75 h. Water (ca. 4 mL) was added cautiously and the mixture was stirred for 15 min. Additional water (75 mL) was added, and the layers were separated. The aqueous phase was extracted with ethyl acetate, and the combined organic phases were dried over anhydrous magnesium sulfate, filtered and concentrated under vacuum. The residue was purified by flash chromatography (toluene:ethyl acetate 50:50) to provide the title product (1.56 g, 77 %) as a pale tan glass: .sup.1 H NMR (CDCl.sub.3) .delta. 8.07 (s, 1H), 7.72 (d, 1H), 7.43 (d, 1H), 7.30 (m, 9H), 7.20 (m, 6H), 6.68 (d, 1H), 6.38 (d, 1H), 4.01 (s, 3H), 3.97 (s, 3H), 3.13 (q, 2H), 2.96 (t, 1H), 2.61 (t, 2H), 1.61 (m, 2H); High resolution mass spectrum (NH.sub.3 --CI) calculated (M+H.sup.+) 556.2713, found 556.2732.

H. Methyl 3-amino-2-(S)-benzoyloxycarbonyl)aminopropionate, hydrochloride salt

A suspension of 3-amino-2-(S)-N-benzyloxycarbonyl)aminopropionic acid (11.0 g, 46.2 mmol) in methanol (165 mL) was stirred on an ice/acetone bath until the internal temperature was below 0.degree. C. Thionyl chloride (3.7 mL, 50.8 mmol) was added dropwise over 10 min. The mixture was stirred for an additional 10 min at 0.degree. C., then for 17.25 h at room temperature. The mixture was concentrated under vacuum and the gummy residue was stirred in ether (300 mL) to provide a white solid. This was collected by filtration, rinsed with additional ether and dried to provide the title product (12.9 g, 97%) as a white powder: .sup.1 H NMR (DMSO-d.sub.6) .delta. 8.32 (bs, 3H), 7.94 (d, 1H), 7.37 (5H), 5.07 (s, 2H), 4.45 (m, 1H), 3.68 (s, 3H), 3.22 (m, 1H), 3.07 (m, 1H).

I. Methyl 3-(tert-butyloxycarbonylamino)-2-(benzyloxycarbonylamino)propionate

A suspension of the product prepared according to Example 3093 Part H (8.00 g, 27.7 mmol) in dichloromethane (140 mL) and saturated aqueous sodium bicarbonate (85 mL) was stirred at room temperature and treated with di-tert-butyldicarbonate (6.11 g, 28 mmol). The mixture was stirred at room temperature for 16.5 h, then filtered and the layers were separated. The aqueous layer was extracted with additional dichloromethane, and the combined organics were washed with brine, dried over magnesium sulfate, and concentrated under vacuum. The resulting viscous oil was stirred in hexane (ca. 200 mL) overnight. The resulting solid was collected by filtration, washed with hexane and dried to provide the title product (7.66 g, 78%) as a white powder: .sup.1 H NMR (CDCl.sub.3) .delta. 7.36 (5H), 5.80 (bd, 1H), 5.12 (s, 2H), 4.84 (b, 1H), 4.41 (b, 1H), 3.77 (s, 3H), 3.55 (b, 2H), 1.42 (s, 9H).

J. Methyl 3-(tert-butyloxycarbonylamino)-2-aminopropionate.

A solution of the product prepared according to Example 3093 Part I (7.50 g, 21.3 mmol) in ethanol (200 mL) was treated with 10% palladium on charcoal (0.75 g) and stirred under hydrogen (1 atmosphere) for 8.5 h. The mixture was filtered through Celite.RTM. and the solids were rinsed with additional ethanol. The filtrate was concentrated to provide the title product (4.65 g, 100%) as a viscous oil: .sup.1 H NMR (CDCl.sub.3) .delta. 5.02 (bs, 1H), 3.75 (s, 3H), 3.59 (t, 1H), 3.50 (m, 1H), 3.27 (m, 1H), 1.67 (bs, 2H), 1.44 (s, 9H).

K. Methyl 3-(tert-butyloxycarbonylamino)-2-(S)-(2,6-dimethylbenzenesulfonylamino)propionate

A solution of the product prepared according to Example 3093 Part J (6.24 g, 24.5 mmol), and diisopropylamine (6.34 g, 49 mmol) in dichloromethane (25 mL) was cooled on an ice bath. A solution of 2,6-dimethylbenzenesulfonyl chloride (prepared according to Wagenaar and Engberts, J. Royal Neth. Chem. Soc. 1982, 101(5), 91-94; 5.01 g, 24.5 mmol) in dichloromethane (75 mL) was added over 15 min. The ice bath was removed and the mixture was stirred at room temperature for 18 h. Additional dichloromethane was added and the solution was washed with water. The organic phase was dried over anhydrous magnesium sulfate, filtered and concentrated under vacuum. The residue was purified by flash chromatography (hexanes:ethyl acetate, step gradient from 80:20 to 60:40) to provide the title product (7.25 g, 76%) as a colorless gum: .sup.1 H NMR (CDCl.sub.3) .delta. 7.29 (t, 1H), 7.14 (d, 2H), 5.78 (bd, 1H), 4.89 (bt, 1H), 3.92 (m, 1H), 3.55 (s, 3H), 3.47 (m, 2H), 2.68 (s, 6H), 1.42 (s, 9H).

L. Methyl 3-amino-2-(S)-(2,6-dimethylbenzenesulfonylamino)propionate (+)-camphorsulfonate

The product prepared according to Example 3093, Part K (7.25 g, 18.8 mmol) was dissolved in HCl/dioxane (4.0M; 50 mL) and the solution was stirred at room temperature for 18 h. The mixture was concentrated under vacuum to yield a hygroscopic solid (6.63 g) which was dissolved in tetrahydrofuran and treated with triethylamine (1.0 equiv.). The resulting solid was removed by filtration, and the filtrate was treated with (+)-camphorsulfonic acid (1.0 equiv.). The mixture was stirred at room temperature for 15 min, and the resulting solid was collected by filtration, rinsed with tetrahydrofuran, and dried to provide the title product (6.63 g, 68%) as a white solid: .sup.1 H NMR (DMSO-d.sub.6) .delta. 8.30 (bs, 1H), 7.94 (bs, 3H), 7.33 (t, 1H), 7.19 (d, 2H), 4.09 (bt, 1H), 3.21 (s, 3H), 3.10 (dd, 1H), 2.93 (dd, 1H), 2.83 (d, 1H), 2.64 (t, 1H), 2.56 (s, 6H), 2.34 (d, 1H), 2.20 (dm, 1H), 1.90 (m, 2H), 1.80 (d, 1H), 1.24 (dd, 2H), 1.01 (s, 3H), 0.70 (s, 3H).

M. Methyl 3-�1-methyl-3-�3-(N-(1-triphenylmethylimidazol-2-ylamino)propyl!indazol-5-ylcarbonylamino!-2(S)-(2,6-dimethylbenzenesulfonylamino)propionate

A mixture of the product prepared according to Example 3093 Part G (1.43 g, 2.57 mmol), aqueous sodium hydroxide (1.0M; 13 mL, 13 mmol) and ethanol (32 mL) was heated at reflux. After 80 min, the mixture was cooled to room temperature and aqueous hydrochloric acid (1.0M; 13 mL, 13 mmol) was added. The mixture was concentrated under vacuum and dried. A portion of this material (which contains sodium chloride; 77 mg, 92 .mu.mol) was combined with the product prepared according to Example 3093 Part L (52 mg, 101 .mu.mol), 1-hydroxybenzotriazole hydrate (13 mg, 92 .mu.mol), and triethylamine (25 .mu.L, 184 .mu.mol) in N,N-dimethylformamide (5 mL) and treated with dicyclohexylcarbodiimide (19 mg, 92 .mu.mol). The mixture was stirred at room temperature for 2.5 days, then was concentrated under vacuum. The residue was partially purified by flash chromatography (dichloromethane:methanol 95:5) to provide the title product (75 mg, 100%) which was impure but was used directly in the subsequent reaction.

N. 3-�1-Methyl-3-�3-(N-imidazol-2-ylamino)propyl!indazol-5-ylcarbonylamino!-2(S)-(2,6-dimethylbenzenesulfonylamino)propionic acid trifluoroacetate

Using the procedure of Example 1050e Part M, the product prepared according to Example 3093 Part M (75 mg, 92 .mu.mol) was converted to the title product as a white powder (after lyophilization): .sup.1 H NMR (MeOH-d.sub.4) .delta. 7.90 (s, 1H), 7.76 (d, 1H), 7.47 (d, 1H), 7.09 (m, 1H), 7.01 (m, 2H), 6.81 (s, 2H), 4.16 (m, 1H), 4.04 (s, 3H), 3.78 (dd, 1H), 3.52 (dd, 1H), 3.34 (t, 2H), 3.09 (t, 2H), 2.62 (s, 6H), 2.14 (m, 2H); High resolution mass spectrum (FAB) calculated (M+H.sup.+) 554.2186, found 554.2184.

EXAMPLE 3142

3-�1-Methyl-3-�3-(N-pyridin-2-ylamino)propyl!indazol-6-ylcarbonylamino!-2(S)-(2,4,6-trimethylbenzenesulfonylamino)propionic acid trifluoroacetate

A. 1-Methyl-3-�3-�N-pyridin-2-ylamino)propyl!-6-methoxycarbonylindazole

A solution of the product prepared according to Example 3093 Part F (201 mg, 816 .mu.mol) and 2aminopyridine (154 mg, 1.63 mmol) in dichloroethane (4 mL) was stirred at room temperature and treated with sodium triacetoxyborohydride (346 mg, 1.63 mmol). After 16.5 h, the mixture was diluted with water (ca. 5 mL) and saturated aqueous sodium bicarbonate (ca. 2 mL) and stirred for 15 min. The mixture was extracted three times with dichloromethane, and the combined organic phases were dried over anhydrous magnesium sulfate, filtered and concentrated under vacuum. The residue was purified by flash chromatography (dichloromethane:isopropanol 95:5) to provide the title product (214 mg 81%) as a white solid: mp 101.degree.-104.degree. C.; .sup.1 H NMR (CDCl.sub.3) .delta. 8.13 (s, 1H), 8.07 (d, 1H), 7.76 (d, 1H), 7.67 (d, 1H), 7.39 (t, 1H), 6.56 (dd, 1H), 6.36 (d, 1H), 4.65 (bt, 1H), 4.08 (s, 3H), 3.98 (s, 3H), 3.38 (q, 2H), 3.10 (t, 3H), 2.16 (m, 2H); High resolution mass spectrum (NH.sub.3 --CI) calculated (M+H.sup.+) 325.1665, found 325.1653.

B. tert-Butyl 3-�1-methyl-3-�3-(N-pyridin-2-ylamino)propyl!indazol-6-ylcarbonylamino!-2(S)-(2,4,6-trimethylbenzenesulfonyl)aminopropionate

Using the procedures of Example 1326b Parts E and F, the product prepared according to Example 3142 Part A (59 mg, 182 .mu.mol) was converted to the title product (108 mg, 93%) as a colorless glass: .sup.1 H NMR (CDCl.sub.3) .delta. 8.08 (d, 1H), 7.95 (s, 1H), 7.70 (d, 1H), 7.46 (d, 1H), 7.40 (m, 1H), 6.94 (s, 2H), 6.92 (m, 1H), 6.56 (m, 1H), 6.37 (d, 1H), 5.79 (d, 1H), 4.67 (m, 1H), 4.08 (s, 3H), 3.95 (m, 1H), 3.83 (m, 1H), 3.61 (m, 1H), 3.38 (q, 2H), 3.10 (t, 2H), 2.66 (s, 6H), 2.27 (s, 3H), 2.16 (m, 2H), 1.32 (s, 9H); High resolution mass spectrum (FAB) calculated (M+H.sup.+) 635.3016, found 635.3028.

C. 3-�1-Methyl-3-�3-(N-pyridin-2-ylamino)propyl!-indazol-6-ylcarbonylamino!-2(S)-(2,4,6-trimethylbenzenesulfonylamino)propionic acid trifluoroacetate

Using the procedure of Example 1129 Part H, the product prepared according to Example 3142 Part B (100 mg, 158 .mu.mol) was converted to the title product (84 mg, 77%) as a white powder: .sup.1 H NMR (DMSO-d.sub.6) .delta. 8.52 (m, 2H), 8.08 (d, 1H), 7.95 (s, 1H), 7.90 (d, 1H), 7.82 (t, 1H), 7.77 (d, 1H), 7.46 (d, 1H), 6.97 (d, 1H), 6.79 (s+m, 3H), 4.05 (m, 1H), 4.01 (s, 3H), 3.59 (m, 2H), 3.39 (m, 2H), 3.03 (t, 2H), 2.52 (s, 6H), 2.07 (m, 2H), 2.00 (s, 3H); High resolution mass spectrum (FAB) calculated (M+H.sup.+) 579.2390, found 579.2400.

EXAMPLE 3339

3-�1-Benzyl-3-�3-(N-pyridin-2-ylamino)propyl!indazol-6-ylcarbonylamino!-2(S)-(2,4,6-trimethylbenzenesulfonylamino)propionic acid trifluoroacetate

A. 3-(3,3-Diethoxypropynyl)-6-methoxycarbonylindazole

Using the procedure of Example 3093 Part D, the product prepared according to Example 3093 Part B (2.55 g, 10 mmol) was converted to the title product (1.49 g, 49%) as a brown gum: .sup.1 H NMR (CDCl.sub.3) .delta. 8.28 (s, 1H), 7.90 (d, 1H), 7.85 (d, 1H), 5.61 (s, 1H), 3.98 (s, 3H), 3.88 (m, 2H), 3.75 (m, 2H), 1.31 (t, 6H); Mass spectrum (NH.sub.3 --CI) m/z 257 (100%, (M+H-EtOH).sup.+).

B. 3-(3,3-Diethoxypropynyl)-6-methoxycarbonylindazole

Using the procedure of Example 3093 Part E, the product prepared according to Example 3339 Part A (263 mg, 870 .mu.mol) was converted to the title product (106 mg, 40%) as an orange oil, which contained a contaminant but was used directly in the subsequent reaction: .sup.1 H NMR (CDCl.sub.3) .delta. 8.20 (s, 1H), 7.81 (d, 1H), 7.76 (d, 1H), 4.60 (t, 1H), 3.96 (s, 3H), 3.68 (m, 2H), 3.51 (m, 2H), 3.09 (m, 2H), 2.17 (m, 2H), 1.22 (t, 6H); High resolution mass spectrum (NH.sub.3 --CI) calculated (M+H.sup.+) 307.1658, found 307.1636.

C. 1-Benzyl-3-(3,3-diethoxypropyl)-6-methoxycarbonylindazole

A solution of the product prepared according to Example 3339 Part B (230 mg, 750 .mu.mol) and benzyl chloride (95 .mu.L, 826 .mu.mol) in dry N,N-dimethylformamide (4 mL) was stirred on an ice bath and treated with sodium hydride (60% in mineral oil; 36 mg, 900 .mu.mol).

The mixture was stirred 10 min, then was allowed to warm to room temperature and stirred for 23 h. The mixture was diluted with water and extracted three times with ethyl acetate. The combined organic phases were washed twice with water, then dried over magnesium sulfate, filtered and concentrated under vacuum. The residue was purified by flash chromatography (hexanes:ethyl acetate 85:15) to provide the title product (152 mg, 51%) as an oil, which was impure but was used directly in the subsequent reaction: .sup.1 H NMR (CDCl.sub.3) .delta. 8.08 (s, 1H), 7.75 (m, 2H), 7.25 (m, 3H), 7.17 (m, 2H), 5.59 (s, 2H), 4.56 (t, 1H), 3.94 (s, 3H), 3.67 (m, 2H), 3.50 (m, 2H), 3.08 (m, 2H), 2.2-2.05 (m, 2H), 1.22 (t, 6H); Mass spectrum (NH.sub.3 --CI) m/z 397.5 (10%, M+H.sup.+), 351 (100%, (M+H-EtOH).sup.+).

D. 1-Benzyl-3-(3-oxopropyl)-6-methoxycarbonylindazole

Using the procedure of Example 3093 Part F, the product of Example 3339 Part C (115 mg, 567 .mu.mol) was converted to the title product (110 mg, 60%) as an oil which solidified on standing: .sup.1 H NMR (CDCl.sub.3) .delta. 9.91 (s, 1H), 8.08 (s, 1H), 7.78 (d, 1H), 7.72 (d, 1H), 7.27 (m, 3H), 7.16 (m, 2H), 5.57 (s, 2H), 3.93 (s, 3H), 3.33 (t, 2H), 3.05 (t, 2H); Mass spectrum (ESI) m/z 323.4 (24%, M+H.sup.+).

E. 1-Benzyl-3-�3-(N-pyridin-2-ylamino)propyl!-6-methoxycarbonylindazole

Using the procedure of Example 3142 Part A, the product prepared according to Example 3339 Part D (91 mg, 282 .mu.mol) was converted to the title product (90 mg, 80%) as a viscous oil which solidified on standing. This material contained a contaminant but was used directly in the subsequent reaction: .sup.1 H NMR (CDCl.sub.3) .delta. 8.08 (m, 2H), 7.77 (d, 1H), 7.70 (d, 1H), 7.36 (m, 1H), 7.3-7.2 (m, 3H), 7.17 (m, 2H), 6.54 (dd, 1H), 6.30 (d, 1H), 5.60 (s, 2H), 4.65 (bt, 1H), 3.93 (s, 3H), 3.37 (q, 2H), 3.13 (t, 2H), 2.16 (m, 2H); High resolution mass spectrum (FAB) calculated (M+H.sup.+) 401.1978, found 401.1982.

F. tert-Butyl 3-�1-benzyl-3-�3-(N-pyridin-2-ylamino)propyl!indazol-6-ylcarbonylamino!-2(S)-(2,4,6-trimethylbenzenesulfonyl)aminopropionate

Using the procedure of Example 1326b Parts E and F, the product prepared according to Example 3339 Part E (81 mg, 202 .mu.mol) was converted to the title product (162 mg, >100%) as a colorless glass which contained a contaminant but was used directly in the subsequent reaction: .sup.1 H NMR (CDCl.sub.3) .delta. 8.07 (m, 1H), 7.94 (s, 1H), 7.71 (d, 1H), 7.47 (d, 1H), 7.38 (m, 1H), 7.26 (m, 5H), 6.92 (s+bm, 3H), 6.55 (m, 1H), 6.33 (d, 1H), 5.81 (d, 1H), 5.59 (s, 2H), 4.69 (bt, 1H), 3.94 (m, 1H), 3.81 (m, 1H), 3.56 (m, 1H), 3.38 (q, 2H), 3.13 (t, 2H), 2.63 (s, 6H), 2.26 (s, 3H), 2.17 (m, 2H), 1.29 (s, 9H); High resolution mass spectrum (FAB) calculated (M+H.sup.+) 711.3329, found 711.3341.

G. 3-�1-Benzyl-3-�3-(N-pyridin-2-ylamino)propyl!indazol-6-ylcarbonylamino!-2(S)-(2,4,6-trimethylbenzenesulfonylamino)propionic acid trifluoroacetate

Using the procedure of Example 1129 Part H, the product prepared according to Example 3339 Part F (136 mg, 191 .mu.mol) was converted to the title product (110 mg, 75%) as a white powder: .sup.1 H NMR (DMSO-d.sub.6) .delta. 8.49 (t, 1H), 8.07 (d, 1H), 8.05 (s, 1H), 7.92 (d, 1H), 7.81 (d, 1H), 7.72 (m, 1H), 7.45 (d, 1H), 7.35-17.20 (m, 5H), 6.88 (d, 1H), 6.73 (s+m, 3H), 5.62 (s, 2H), 4.05 (m, 1H), 3.58 (m, 1H), 3.5-3.3 (m, 3H), 3.05 (t, 2H), 2.52 (s, 6H), 2.07 (m, 2H), 1.95 (s, 3H); High resolution mass spectrum (FAB) calculated (M+H.sup.+) 655.2703, found 655.2701.

Using the methods described above and modifications thereof known to one skilled in the art of organic synthesis, the following additional examples in Tables 1-8 can be prepared.

UTILITY

The compounds of Formula Ia, Ib or Ic of the present invention possess activity as antagonists of integrins such as, for example, the .alpha..sub.v .beta..sub.3 or vitronectin receptor, .alpha..sub.v .beta..sub.5 or .alpha..sub.5 .beta..sub.1, and as such have utility in the treatment and diagnosis of cell adhesion, angiogenic disorders, inflammation, bone degradation, cancer metastases, diabetic retinopathy, thrombosis, restenosis, macular degeneration, and other conditions mediated by cell adhesion and/or cell migration and/or angiogenesis. The integrin antagonist activity of the compounds of the present invention is demonstrated using assays which measure the binding of a specific integrin to a native ligand, for example, using the ELISA assay described below for the binding of vitronectin to the .alpha..sub.v .beta..sub.3 receptor.

The compounds of the present invention possess selectivity for the .alpha..sub.v .beta..sub.3 receptor relative to the GPIIb/IIIa receptor as demonstrated by their reduced activity in standard assays of platelet aggregation, such as the platelet aggregation assay described below.

One of the major roles of integrins in vivo is to mediate cellular interactions with adjacent cells. Cell based adhesion assays can be used to mimic these interactions in vitro. A cell based assay is more representative of the in vivo situation than an ELISA since the receptor is maintained in membranes in the native state. The compounds of the present invention have activity in cell-based assays of adhesion, for example as demonstrated in using the cell adhesion assays described below.

The compounds of Formula Ia, Ib or Ic of the present invention may be useful for the treatment or prevention of other diseases which involve cell adhesion processes, including, but not limited to, osteoporosis, rheumatoid arthritis, autoimmune disorders, bone degradation, rheumatoid arthritis, asthma, allergies, adult respiratory distress syndrome, graft versus host disease, organ transplantation, septic shock, psoriasis, eczema, contact dermatitis, osteoarthritis, atherosclerosis, metastasis, wound healing, inflammatory bowel disease and other angiogenic disorders.

The compounds of Formula Ia, Ib or Ic have the ability to suppress/inhibit angiogenesis in vivo, for example, as demonstrated using animal models of ocular neovascularization.

The compounds provided by this invention are also useful as standards and reagents in determining the ability of a potential pharmaceutical to inhibit integrin-ligand binding. These may be provided in a commercial kit comprising a compound of this invention.

As used herein ".mu.g" denotes microgram, "mg" denotes milligram, "g" denotes gram, ".mu.L" denotes microliter, "mL" denotes milliliter, "L" denotes liter, "nM" denotes nanomolar, ".mu.M" denotes micromolar, "mM" denotes millimolar, "M" denotes molar and "nm" denotes nanometer. "Sigma" stands for the Sigma-Aldrich Corp. of St. Louis, Mo.

The utility of the compounds of the present invention may be assessed by testing in one or more of the following assays as described in detail below: Purified .alpha..sub.v .beta..sub.3 (human placenta)--Vitronectin ELISA, .alpha..sub.v .beta..sub.3 -Vitronectin Binding Assay, Human Aortic Smooth Muscle Cell Migration Assay, In Vivo Angiogenesis Model, Pig Restenosis Model, Mouse Retinopathy Model. A compound of the present invention is considered to be active if it has an IC.sub.50 or K.sub.i value of less than about 10 .mu.M for the inhibition of .alpha..sub.v .beta..sub.3 -Vitronectin Binding Assay, with compounds preferably having K.sub.i values of less than about 0.1 .mu.M. Tested compounds of the present invention are active in the .alpha..sub.v .beta..sub.3 -Vitronectin Binding Assay.

Purified .alpha..sub.v .beta..sub.3 (human placenta)--Vitronectin ELISA

The .alpha..sub.v .beta..sub.3 receptor was isolated from human placental extracts prepared using octylglucoside. The extracts were passed over an affinity column composed of anti-.alpha..sub.v .beta..sub.3 monoclonal antibody (LM609) bound to Affigel. The column was subsequently washed extensively at pH 7 and pH 4.5 followed by elution at pH 3. The resulting sample was concentrated by wheat germ agglutinin chromatography to provide two bands by SDS gel electrophoresis which were confirmed as .alpha..sub.v .beta..sub.3 by western blotting.

Affinity purified protein was diluted at different levels and plated to 96 well plates. ELISA was performed using fixed concentration of biotinylated vitronectin (approximately 80 nM/well). This receptor preparation contains the .alpha..sub.v .beta..sub.3 with no detectable levels of .alpha..sub.v .beta..sub.5 according to the gel and according to effects of blocking antibodies for the .alpha..sub.v .beta..sub.3 or .alpha..sub.v .beta..sub.5 integrins in the ELISA.

A submaximal concentration of biotinylated vitronectin was selected based on a concentration response curve with fixed receptor concentration and variable concentrations of biotinylated vitronectin.

.alpha..sub.v .beta..sub.3 -Vitronectin Binding Assay

The purified receptor is diluted with coating buffer (20 mM Tris HCl, 150 mM NaCl, 2.0 mM CaCl.sub.2, 1.0 mM MgCl.sub.2.6H.sub.2 O, 1.0 mM MnCl.sub.2.4H.sub.2 O) and coated (100 .mu.L/well) on Costar (3590) high capacity binding plates overnight at 4.degree. C. The coating solution is discarded and the plates washed once with blocking/binding buffer (B/B buffer, 50 mM Tris HCl, 100 mM NaCl, 2.0 mM CaCl.sub.2, 1.0 mM MgCl.sub.2.6H.sub.2 O, 1.0 mM MnCl.sub.2.4H.sub.2 O). Receptor is then blocked (200 .mu.L/well) with 3.5% BSA in B/B buffer for 2 hours at room temperature. After washing once with 1.0 % BSA in B/B buffer, biotinylated vitronectin (100 .mu.L) and either inhibitor (11 .mu.L) or B/B buffer w/1.0% BSA (11 .mu.L) is added to each well. The plates are incubated 2 hours at room temperature. The plates are washed twice with B/B buffer and incubated 1 hour at room temperature with anti-biotin alkaline phosphatase (100 .mu.L/well) in B/B buffer containing 1.0 % BSA. The plates are washed twice with B/B buffer and alkaline phosphatase substrate (100 .mu.L) is added. Color is developed at room temperature. Color development is stopped by addition of 2N NaOH (25 .mu.L/well) and absorbance is read at 405 nm. The IC.sub.50 is the concentration of test substance needed to block 50% of the vitronectin binding to the receptor.

Integrin Cell-Based Adhesion Assays

In the adhesion assays, a 96 well plate was coated with the ligand (i.e., fibrinogen) and incubated overnight at 4.degree. C. The following day, the cells were harvested, washed and loaded with a fluorescent dye. Test compounds and cells were added together and then were immediately added to the coated plate. After incubation, loose cells are removed from the plate, and the plate (with adherent cells) is counted on a fluorometer. The ability of test compounds to inhibit cell adhesion by 50% is given by the IC.sub.50 value and represents a measure of potency of inhibition of integrin mediated binding. Compounds were tested for their ability to block cell adhesion using assays specific for .alpha..sub.v .beta..sub.3, .alpha..sub.v .beta..sub.5 and .alpha..sub.v .beta..sub.1 integrin interactions.

Platelet Aggregation Assay

Venous blood was obtained from anesthetized mongrel dogs or from healthy human donors who were drug- and aspirin-free for at least two weeks prior to blood collection. Blood was collected into citrated Vacutainer tubes. The blood was centrifuged for 15 minutes at 150.times.g (850 RPM in a Sorvall RT6000 Tabletop Centrifuge with H-1000 B rotor) at room temperature, and platelet-rich plasma (PRP) was removed. The remaining blood was centrifuged for 15 minutes at 1500.times.g (26,780 RPM) at room temperature, and platelet-poor plasma (PPP) was removed. Samples were assayed on a PAP-4 Platelet Aggregation Profiler, using PPP as the blank (100% transmittance). 200 .mu.L of PRP (5.times.10.sup.8 platelets/mL) were added to each micro test tube, and transmittance was set to 0%. 20 .mu.L of ADP (10 .mu.M) was added to each tube, and the aggregation profiles were plotted (% transmittance versus time). Test agent (20 .mu.L) was added at different concentrations prior to the addition of the platelet agonist. Results are expressed as % inhibition of agonist-induced platelet aggregation.

Human Aortic Smooth Muscle Cell Migration Assay

A method for assessing .alpha..sub.v .beta..sub.3 -mediated smooth muscle cell migration and agents which inhibit .alpha..sub.v .beta..sub.3 -mediated smooth muscle cell migration is described in Liaw et al., J. Clin. Invest. (1995) 95: 713-724).

In Vivo Angiogenesis Model

A quantitative method for assessing angiogenesis and antiangiogenic agents is described in Passaniti et al., Laboratory Investigation (1992) 67: 519-528

Pig Restenosis Model

A method for assessing restenosis and agents which inhibit restenosis is described in Schwartz et al., J. Am. College of Cardiology (1992) 19: 267-274.

Mouse Retinopathy Model

A method for assessing retinopathy and agents which inhibit retinopathy is described in Smith et al., Invest. Ophthal. & Visual Science (1994) 35: 101-111.

Dosage and Formulation

The compounds of this invention can be administered by any means that produces contact of the active agent with the agent's site of action, the .alpha..sub.v .beta..sub.3 integrin, in the body of a mammal. They can be administered by any conventional means available for use in conjunction with pharmaceuticals, either as individual therapeutic agents or in a combination of therapeutic agents, such as a antiplatelet agent such as aspirin, piroxicam, or ticlopidine which are agonist-specific, or an anti-coagulant such as warfarin or heparin, or a thrombin inhibitor such as a boropeptide, hirudin or argatroban, or a thrombolytic agent such as tissue plasminogen activator, anistreplase, urokinase or streptokinase, or combinations thereof. The compounds of the invention, or compounds of the invention in combination with other therapeutic agents, can be administered alone, but generally administered with a pharmaceutical carrier selected on the basis of the chosen route of administration and standard pharmaceutical practice.

The dosage of the novel compounds of this invention administered will, of course, vary depending upon known factors, such as the pharmacodynamic characteristics of the particular agent and its mode and route of administration; the age, health and weight of the recipient; the nature and extent of the symptoms; the kind of concurrent treatment; the frequency of treatment; and the effect desired. A daily dosage of active ingredient can be expected to be about 0.001 to 10 milligrams per kilogram of body weight.

Dosage forms (compositions suitable for administration) contain from about 0.1 milligram to about 100 milligrams of active ingredient per unit. In these pharmaceutical compositions the active ingredient will ordinarily be present in an amount of about 0.5-95% by weight based on the total weight of the composition.

The active ingredient can be administered orally in solid dosage forms, such as capsules, tablets, and powders, or in liquid dosage forms, such as elixirs, syrups, and suspensions. It can also be administered by injection, in sterile liquid dosage forms.

Gelatin capsules contain the active ingredient and powdered carriers, such as lactose, starch, cellulose derivatives, magnesium stearate, stearic acid, and the like. Similar diluents can be used to make compressed tablets. Both tablets and capsules can be manufactured as sustained release products to provide for continuous release of medication over a period of hours. Compressed tablets can be sugar coated or film coated to mask any unpleasant taste and protect the tablet from the atmosphere, or enteric coated for selective disintegration in the gastrointestinal tract.

Liquid dosage forms for oral administration can contain coloring and flavoring to increase patient acceptance.

In general, water, a suitable oil, saline, aqueous dextrose (glucose), and related sugar solutions and glycols such as propylene glycol or polyethylene glycols are suitable carriers for parenteral solutions. Solutions for parenteral administration preferably contain a water soluble salt of the active ingredient, suitable stabilizing agents, and if necessary, buffer substances. Antioxidizing agents such as sodium bisulfite, sodium sulfite, or ascorbic acid, either alone or combined, are suitable stabilizing agents. Also used are citric acid and its salts and sodium EDTA. In addition, parenteral solutions can contain preservatives, such as benzalkonium chloride, methyl- or propyl-paraben, and chlorobutanol.

Suitable pharmaceutical carriers are described in Remington's Pharmaceutical Sciences, Mack Publishing Company, a standard reference text in this field.

Useful pharmaceutical dosage-forms for administration of the compounds of this invention can be illustrated as follows:

Capsules

A large number of unit capsules are prepared by filling standard two-piece hard gelatin capsules each with 10 milligrams of powdered active ingredient, 150 milligrams of lactose, 50 milligrams of cellulose, and 6 milligrams magnesium stearate.

Soft Gelatin Capsules

A mixture of active ingredient in a digestable oil such as soybean oil, cottonseed oil or olive oil is prepared and injected by means of a positive displacement pump into gelatin to form soft gelatin capsules containing 10 milligrams of the active ingredient. The capsules are washed and dried.

Tablets

A large number of tablets are prepared by conventional procedures so that the dosage unit was 10 milligrams of active ingredient, 0.2 milligrams of colloidal silicon dioxide, 5 milligrams of magnesium stearate, 275 milligrams of microcrystalline cellulose, 11 milligrams of starch and 98.8 milligrams of lactose. Appropriate coatings may be applied to increase palatability or delay absorption.

The combination products of this invention, such as the novel .alpha..sub.v .beta..sub.3 antagonist compounds of this invention in combination with an anti-coagulant agent such as warfarin or heparin, or an anti-platelet agent such as aspirin, piroxicam or ticlopidine, or a thrombin inhibitor such as a boropeptide, hirudin or argatroban, or a thrombolytic agent such as tissue plasminogen activator, anistreplase, urokinase or streptokinase, or combinations thereof, can be in any dosage form, such as those described above, and can also be administered in various ways, as described above.

In a preferred embodiment, the combination products of the invention are formulated together, in a single dosage form (that is, combined together in one capsule, tablet, powder, or liquid, etc.). When the combination products are not formulated together in a single dosage form, the .alpha..sub.v .beta..sub.3 antagonist compounds of this invention and the anti-coagulant agent, anti-platelet agent, thrombin inhibitor, and/or thrombolytic agent may be administered at the same time (that is, together), or in any order, for example the compounds of this invention are administered first, followed by administration of the anti-coagulant agent, anti-platelet agent, thrombin inhibitor, and/or thrombolytic agent. When not administered at the same time, preferably the administration of the compound of this invention and any anti-coagulant agent, anti-platelet agent, thrombin inhibitor, and/or thrombolytic agent occurs less than about one hour apart, more preferably less than about 30 minutes apart, even more preferably less than about 15 minutes apart, and most preferably less than about 5 minutes apart. Preferably, administration of the combination products of the invention is oral. The terms oral agent, oral inhibitor, oral compound, or the like, as used herein, denote compounds which may be orally administered. Although it is preferable that the .alpha..sub.v .beta..sub.3 antagonist compounds of this invention and the anti-coagulant agent, anti-platelet agent, thrombin inhibitor, and/or thrombolytic agent are both administered in the same fashion (that is, for example, both orally), if desired, they may each be administered in different fashions (that is, for example, one component of the combination product may be administered orally, and another component may be administered intravenously). The dosage of the combination products of the invention may vary depending upon various factors such as the pharmacodynamic characteristics of the particular agent and its mode and route of administration, the age, health and weight of the recipient, the nature and extent of the symptoms, the kind of concurrent treatment, the frequency of treatment, and the effect desired, as described above.

As discussed above, where two or more of the foregoing therapeutic agents are combined or co-administered with the compounds of this invention, generally the amount of each component in a typical daily dosage and typical dosage form may be reduced relative to the usual dosage of the agent when administered alone, in view of the additive or synergistic effect which would be obtained as a result of addition of further agents in accordance with the present invention.

Particularly when provided as a single dosage form, the potential exists for a chemical interaction between the combined active ingredients (for example, a novel compound of this invention and an anti-coagulant such as warfarin or heparin, or a novel compound of this invention and an anti-platelet agent such as aspirin, piroxicam or ticlopidine, or a novel compound of this invention and a thrombin inhibitor such as a boropeptide, hirudin or argatroban, or a novel compound of this invention and a thrombolytic agent such as tissue plasminogen activator, anistreplase, urokinase or streptokinase, or combinations thereof). For this reason, the preferred dosage forms of the combination products of this invention are formulated such that although the active ingredients are combined in a single dosage form, the physical contact between the active ingredients is minimized (that is, reduced).

In order to minimize contact, one embodiment of this invention where the product is orally administered provides for a combination product wherein one active ingredient is enteric coated. By enteric coating one of the active ingredients, it is possible not only to minimize the contact between the combined active ingredients, but also, it is possible to control the release of one of these components in the gastrointestinal tract such that one of these components is not released in the stomach but rather is released in the intestines. Another embodiment of this invention where oral administration is desired provides for a combination product wherein one of the active ingredients is coated with a sustained-release material which effects a sustained-release throughout the gastrointestinal tract and also serves to minimize physical contact between the combined active ingredients. Furthermore, the sustained-released component can be additionally enteric coated such that the release of this component occurs only in the intestine. Still another approach would involve the formulation of a combination product in which the one component is coated with a sustained and/or enteric release polymer, and the other component is also coated with a polymer such as a low viscosity grade of hydroxypropyl methylcellulose (HPMC) or other appropriate materials as known in the art, in order to further separate the active components. The polymer coating serves to form an additional barrier to interaction with the other component.

Dosage forms of the combination products of the present invention wherein one active ingredient is enteric coated can be in the form of tablets such that the enteric coated component and the other active ingredient are blended together and then compressed into a tablet or such that the enteric coated component is compressed into one tablet layer and the other active ingredient is compressed into an additional layer. Optionally, in order to further separate the two layers, one or more placebo layers may be present such that the placebo layer is between the layers of active ingredients. In addition, dosage forms of the present invention can be in the form of capsules wherein one active ingredient is compressed into a tablet or in the form of a plurality of microtablets, particles, granules or non-perils, which are then enteric coated. These enteric coated microtablets, particles, granules or non-perils are then placed into a capsule or compressed into a capsule along with a granulation of the other active ingredient.

These as well as other ways of minimizing contact between the components of combination products of the present invention, whether administered in a single dosage form or administered in separate forms but at the same time by the same manner, will be readily apparent to those skilled in the art, once armed with the present disclosure.

Pharmaceutical kits useful in, for example, the inhibition of thrombus formation, the prevention of blood clots, and/or the treatment of thromboembolic disorders, which comprise a therapeutically effective amount of a compound according to the method of the present invention along with a therapeutically effective amount of an anti-coagulant agent such as warfarin or heparin, or an antiplatelet agent such as aspirin, piroxicam or ticlopidine, or a thrombin inhibitor such as a boropeptide, hirudin or argatroban, or a thrombolytic agent such as tissue plasminogen activator, anistreplase, urokinase or streptokinase, or combinations thereof, in one or more sterile containers, are also within the ambit of the present invention. Sterilization of the container may be carried out using conventional sterilization methodology well known to those skilled in the art. The sterile containers of materials may comprise separate containers, or one or more multi-part containers, as exemplified by the UNIVIALTM.TM. two-part container (available from Abbott Labs, Chicago, Illinois), as desired. The compounds according to the method of the invention and the anti-coagulant agent, anti-platelet agent, thrombin inhibitor, thrombolytic agent, and/or combinations thereof, may be separate, or combined into a single dosage form as described above. Such kits may further include, if desired, one or more of various conventional pharmaceutical kit components, such as for example, one or more pharmaceutically acceptable carriers, additional vials for mixing the components, etc., as will be readily apparent to those skilled in the art. Instructions, either as inserts or as labels, indicating quantities of the components to be administered, guidelines for administration, and/or guidelines for mixing the components, may also be included in the kit.

TABLE 1__________________________________________________________________________ ##STR59##Ex.No. R.sup.1 R.sup.10 R.sup.13 R.sup.14 R.sup.15 MS__________________________________________________________________________1001 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H H1002 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHCO.sub.2 CH.sub.2 Ph1003 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHCO.sub.2 CH.sub.2 C.sub.6 H.sub.4 -(2-CH.sub.3)1004 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHCO.sub.2 CH.sub.2 C.sub.6 H.sub.4 -(3-CH.sub.3)1005 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHCO.sub.2 CH.sub.2 C.sub.6 H.sub.4 -(4-CH.sub.3)1006 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHCO.sub.2 CH.sub.2 (2-pyridinyl)1007 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHCO.sub.2 CH.sub.2 (3-pyridinyl)1008 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHCO.sub.2 CH.sub.2 (4-pyridinyl)1009 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHCO.sub.2 CH.sub.2 (2-thiazolyl)1010 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHCO.sub.2 CH.sub.2 (4-thiazolyl)1011 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHCO.sub.2 CH.sub.2 (5-thiazolyl)1012 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHCO.sub.2 CH.sub.2 (4-isoxazolyl) 21013 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHCO.sub.2 CH.sub.2 (2-thienyl)1014 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHCO.sub.2 CH.sub.2 (5-isoxazolyl) 41015 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHCO.sub.2 n-Bu1016 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHCO.sub.2 i-Bu1017 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHCO.sub.2 t-Bu1017a imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHCOPh1018 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHCOCH.sub.2 Ph1019 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHCOCH.sub.2 C.sub.6 H.sub.4 -(2-CH.sub.3)1020 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHCOCH.sub.2 C.sub.6 H.sub.4 -(3-CH.sub.3)1021 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHCOCH.sub.2 C.sub.6 H.sub.4 -(4-CH.sub.3)1021a imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHCOCH.sub.2 CH.sub.2 Ph1021b imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHCOCHCHPh1022 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHCOCH.sub.2 (2-pyridinyl)1023 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHCOCH.sub.2 (3-pyridinyl)1024 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHCOCH.sub.2 (4-pyridinyl)1025 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHCOCH.sub.2 (2-thiazolyl)1026 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHCOCH.sub.2 (4-thiazolyl)1027 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHCOCH.sub.2 (5-thiazolyl)1028 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHCOCH.sub.2 (4-isoxazol)1029 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHCOCH.sub.2 (2-thienyl)1029a imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHCOCH.sub.2 (cyclohexyl)1029b imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHCO-cyclohexyl1030 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHCOn-Bu1031 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHCOt-Bu1031a imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHCONHPh1031b imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHCONHCH.sub.2 Ph1032 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 Ph 512.31033 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.4 -(2-CH.sub.3)1034 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.4 -(3-CH.sub.3)1035 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.4 -(4-CH.sub.3)1035a imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.3 -(2,6-CH.sub.3).sub.2 540.41035b imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.2 -(2,4,6-CH.sub.3).sub.3 554.41036 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 (2-pyridyl)1037 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 (3-pyridyl)1038 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 (4-pyridyl)1038a imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 (2-thienyl)1038b imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 -�3-(2,5- dichloro)thienyl!1039 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 (2-thiaz-olyl)1040 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 (3-thiazolyl)1040a imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 -�5-(4-methyl-2- amino)thiazolyl!1041 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 (4-isoxazolyl)1042 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 �4-(3,5- dimethyl)isoxazolyl!1043 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.4 -(2-Br)1044 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.4 -(3-Br)1045 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.4 -(4-Br)1046 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.4 -(2-F)1047 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.4 -(3-F)1048 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.4 -(4-F)1048a imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.3 -(2,6-Cl.sub.2) 580.21049 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 (2-naphthyl)1050 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 (1-naphthyl) 562.41050a imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.4 -(4-Ph) 588.41050b imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.4 -4-(4- pyridyl)1050c imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.4 -4-(2- oxazolyl)1050d imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.4 -4-(3- pyrazolyl)1050e imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.2 -4-Ph-2,6- 616.3 dimethyl1050f imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.2 -4-(3- pyridyl)-2,6-dimethyl1050g imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.2 -4-(2-oxa- zolyl)-2,6-dimethyl1050h imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.2 -4-(3-pyra- zolyl)-2,6-dimethyl1050i imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.2 -4-Ph-2,6- dichloro1050j imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.4 -4-(2-furyl) 578.31050k imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.2 -4-(3-furyl)1050l imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.2 -4-(3- pyridyl)1050m imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.2 -4-(4- pyridyl)-2,6-dimethyl1050n imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.2 -4-(3-furyl)- 2,6-dimethyl1050o imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.2 -4-(2-furyl)- 2,6-dichloro1051 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 CHCHPh1052 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 CH.sub.2 Ph1053 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 CH.sub.2 CHCHPh1054 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 -n-Bu1055 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 -i-Bu1056 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 -t-Bu1057 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NHPh1058 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NHC.sub.6 H.sub.4 -(2-CH.sub.3)1059 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NHC.sub.6 H.sub.4 -(3-CH.sub.3)1060 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NHC.sub.6 H.sub.4 -(4-CH.sub.3)1060a imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NHC.sub.6 C.sub.3 -(2,6-Me.sub.2)1060b imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NHC.sub.6 C.sub.2 -(2,4,6- Me.sub.3)1061 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NH(2-pyridyl)1062 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NH(3-pyridyl)1063 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NH(4-pyridyl)1064 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NH(2-thiazolyl)1065 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NH(4-thiazolyl)1066 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NH(4-isoxazolyl)1067 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 �4-(3,5- dimethyl)isoxazolyl!1068 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NHC.sub.6 H.sub.4 -(2-Br)1069 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NHC.sub.6 H.sub.4 -(3-Br)1070 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NHC.sub.6 H.sub.4 -(4-Br)1071 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NHC.sub.6 H.sub.4 -(3-F)1072 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NHC.sub.6 H.sub.4 -(4-F)1073 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NH(2-naphthyl)1074 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NH(1-naphthyl)1074a imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NHC.sub.6 H.sub.4 -(4-Ph)1074b imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NHC.sub.6 H.sub.2 -(4-Ph-2,6- dimethyl)1074c imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NHC.sub.6 H.sub.2 -(4-Ph-2,6- dichloro)1075 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NHCHCHPh1076 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NHCH.sub.2 Ph1077 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NHCH.sub.2 CHCHPh1077a imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NH-cyclohexyl1078 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NH-n-Bu1079 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NH-i-Bu1080 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NH-t-Bu1081 pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHCO.sub.2 CH.sub.2 Ph 517.31082 pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHCO.sub.2 CH.sub.2 C.sub.6 H.sub.4 -(2-CH.sub.3)1083 pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHCO.sub.2 CH.sub.2 C.sub.6 H.sub.4 -(3-CH.sub.3)1084 pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHCO.sub.2 CH.sub.2 C.sub.6 H.sub.4 -(4-CH.sub.3)1085 pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHCO.sub.2 CH.sub.2 (2-pyridinyl)1086 pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHCO.sub.2 CH.sub.2 (3-pyridinyl)1087 pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHCO.sub.2 CH.sub.2 (4-pyridinyl)1088 pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHCO.sub.2 CH.sub.2 (2-thiazolyl)1089 pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHCO.sub.2 CH.sub.2 (4-thiazolyl)1090 pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHCO.sub.2 CH.sub.2 (5-thiazolyl)1091 pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHCO.sub.2 CH.sub.2 (4-isoxazolyl) 11092 pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHCO.sub.2 CH.sub.2 (2-thienyl)1093 pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHCO.sub.2 n-Bu1094 pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHCO.sub.2 i-Bu 483.51095 pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHCO.sub.2 t-Bu1095a pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHCOPh 487.31096 pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHCOCH.sub.2 Ph 501.41097 pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHCOCH.sub.2 C.sub.6 H.sub.4 -(2-CH.sub.3)1098 pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHCOCH.sub.2 C.sub.6 H.sub.4 -(3-CH.sub.3)1099 pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHCOCH.sub.2 C.sub.6 H.sub.4 -(4-CH.sub.3)1099a pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHCOCH.sub.2 CH.sub.2 Ph 515.41099b pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHCOCHCHPh 513.31100 pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHCOCH.sub.2 (2-pyridinyl)1101 pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHCOCH.sub.2 (3-pyridinyl)1102 pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHCOCH.sub.2 (4-pyridinyl)1103 pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHCOCH.sub.2 (2-thiazolyl)1104 pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHCOCH.sub.2 (4-thiazolyl)1105 pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHCOCH.sub.2 (5-thiazolyl)1106 pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHCOCH.sub.2 CH.sub.2 CH(CH.sub.3) .sub.2 481.41107 pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHCOCH.sub.2 (4-isoxazolyl)1108 pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHCOCH.sub.2 (2-thienyl)1108a pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHCOCH.sub.2 (cyclohexyl) 507.31108b pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHCO-cyclohexyl 493.41109 pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHCOn-Bu1110 pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHCOt-Bu1110a pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHCONHPh 502.41110b pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHCONHCH.sub.2 Ph 516.51111 pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 Ph 523.21112 pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.4 -(2-CH.sub.3)1113 pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.4 -(3-CH.sub.3)1114 pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.4 -(4-CH.sub.3)1114a pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.3 -(2,6-CH.sub.3).sub.21114b pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.2 -(2,4,6-CH.sub.3).sub.3 565.21115 pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 (2-pyridyl)1116 pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 (3-pyridyl)1117 pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 (4-pyridyl)1117a pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 (2-thienyl) 529.21117b pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 -�3-(2,5- 597.1 dichloro)thienyl!1118 pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 (2-thiazolyl)1119 pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 (4-thiazolyl)1119a pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 -�5-(4-methyl-2- 559.2 amino)thiazolyl!1120 pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 (4-isoxazolyl)1121 pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 -�4-(3,5- 542.2 dimethyl)isoxazolyl!1122 pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.4 -(2-Br)1123 pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.4 -(3-Br)1124 pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.4 -(4-Br)1125 pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.4 -(2-F)1126 pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.4 -(3-F)1127 pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.4 -(4-F)1127a pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.3 -(2,6-Cl.sub.2) 591.31128 pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 (2-naphthyl) 573.41129 pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 (1-naphthyl) 573.21129a pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.4 -(4-Ph) 599.41129b pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.4 -4-(4- pyridyl)1129c pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.4 -4-(2- oxazolyl)1129d pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.4 -4-(3- pyrazolyl)1129e pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.2 -4-Ph-2,6- dimethyl1129f pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.2 -4-(3- pyridyl)-2,6-dimethyl1129g pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.2 -4-(2-oxa- zolyl)-2,6-dimethyl1129h pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.2 -4-(3-pyra- zolyl)-2,6-dimethyl1129i pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.2 -4-Ph-2,6- dichloro1129j pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.4 -4-(2-furyl)1129k pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.2 -4-(3-furyl)1129l pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.2 -4-(3- pyridyl)1129m pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.2 -4-(4- pyridyl)-2,6-dimethyl1129n pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.2 -4-(3-furyl)- 2,6-dimethyl1129o pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.2 -4-(2-furyl)- 2,6-dichloro1130 pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 CHCHPh1131 pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 CH.sub.2 Ph 537.41132 pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 CH.sub.2 CHCHPh1133 pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 -n-Bu 503.31134 pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 -i-Bu1135 pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 -t-Bu1136 pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NHPh1137 pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NHC.sub.6 H.sub.4 -(2-CH.sub.3)1138 pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NHC.sub.6 H.sub.4 -(3-CH.sub.3)1139 pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NHC.sub.6 H.sub.4 -(4-CH.sub.3)1139a pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NHC.sub.6 C.sub.3 -(2,6-Me.sub.2)1139b pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NHC.sub.6 C.sub.2 -(2,4,6- 580.3 Me.sub.3)1140 pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NH(2-pyridyl)1141 pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NH(3-pyridyl)1142 pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NH(4-pyridyl)1143 pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NH(2-thiazolyl)1144 pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NH-(4-thiazolyl)1145 pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NH(4-isoxazolyl)1146 pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 -�4-(3,5- dimethyl)isoxazolyl!1147 pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NHC.sub.6 H.sub.4 -(2-Br)1148 pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NHC.sub.6 H.sub.4 -(3-Br)1149 pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NHC.sub.6 H.sub.4 -(4-Br)1150 pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NHC.sub.6 H.sub.4 -(3-F)1151 pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NHC.sub.6 H.sub.4 -(4-F)1152 pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NH(2-naphthyl)1153 pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NH)1-naphthyl)1153a pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NHC.sub.6 H.sub.4 -(4-Ph)1153b pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NHC.sub.6 H.sub.2 -(4-Ph-2,6- dimethyl)1153c pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NHC.sub.6 H.sub.2 -(4-Ph-2,6- dichloro)1154 pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NHCHCHPh1155 pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NHCH.sub.2 Ph 552.41156 pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NHCH.sub.2 CHCHPh1156a pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHSONH-cyclohexyl 544.41157 pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NH-n-Bu1158 pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NH-i-Bu 518.41159 pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NH-t-Bu1160 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H H H NHCOOCH.sub.2 Ph1161 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H H H NHCO.sub.2 CH.sub.2 C.sub.6 H.sub.4 -(2-CH.sub.3)1162 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H H H NHCO.sub.2 CH.sub.2 C.sub.6 H.sub.4 -(3-CH.sub.3)1163 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H H H NHCO.sub.2 CH.sub.2 C.sub.6 H.sub.4 -(4-CH.sub.3)1164 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H H H NHCO.sub.2 CH.sub.2 (2-pyridinyl)1165 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H H H NHCO.sub.2 CH.sub.2 (3-pyridinyl)1166 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H H H NHCO.sub.2 CH.sub.2 (4-pyridinyl)1167 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H H H NHCO.sub.2 CH.sub.2 (2-thiazolyl)1168 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H H H NHCO.sub.2 CH.sub.2 (4-thiazolyl)1169 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H H, H NHCO.sub.2 CH.sub.2 (5-thiazolyl)1170 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H H H NHCO.sub.2 CH.sub.2 (4-isoxazolyl)1171 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H H H NHCO.sub.2 CH.sub.2 (2-thienyl)1172 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H H H NHCO.sub.2 n-Bu1173 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H H H NHCO.sub.2 i-Bu1174 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H H H NHCO.sub.2 t-Bu1175 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 Ph1176 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.4 -(2-CH.sub.3)1177 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.4 -(3-CH.sub.3)1178 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.4 -(4-CH.sub.3)1178a tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.3 -(2,6-Me.sub.2)1178b tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.2 -(2,4,6-Me.sub.3) 570.51179 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 (2-pyridyl)1180 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 (3-pyridyl)1181 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 (4-pyridyl)1181a tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 (2-thienyl)1181b tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 -�3-(2,5- dichloro)thienyl!1182 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 (2-thiazolyl)1183 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 (4-thiazolyl)1184 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 (4-isoxazolyl)1185 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 -�4-(3,5- dimethyl)isoxazolyl!1186 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.4 -(2-Br)1187 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.4 -(3-Br)1188 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.4 -(2-F)1189 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.4 -(3-F)1190 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.4 -(4-F)1190a tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.3 -(2,6-Cl.sub.2)1191 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 (2-naphthyl)1192 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 (1-naphthyl)1192a tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.4 -(4-Ph)1192b tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.4 -4-(4- pyridyl)1192c tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.4 -4-(2- oxazolyl)1192d tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.4 -4-(3- pyrazolyl)1192e tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.2 -4-Ph-2,6- dimethyl1192f tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.2 -4-(3- pyridyl)-2,6-dimethyl1192g tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.2 -4-(2-oxa- zolyl)-2,6-dimethyl1192h tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.2 -4-(3-pyra- zolyl)-2,6-dimethyl1192i tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.2 -4-Ph-2,6- dichloro1192j tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.4 -4-(2-furyl)1192k tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.2 -4-(3-furyl)1192l tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.2 -4-(3- pyridyl)1192m tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.2 -4-(4- pyridyl)-2,6-dimethyl1192n tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.2 -4-(3-furyl)- 2,6-dimethyl1192o tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.2 -4-(2-furyl)- 2,6-dichloro1193 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 CHCHPh1194 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 CH.sub.2 Ph1195 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 CH.sub.2 CHCHPh1196 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 -n-Bu1197 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 -i-Bu1197a tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NHPh1197b tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NHC.sub.6 H.sub.4 -(2-CH.sub.3)1197c tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NHC.sub.6 H.sub.4 -(3-CH.sub.3)1197d tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NHC.sub.6 H.sub.4 -(4-CH.sub.3)1197e tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NHC.sub.6 C.sub.3 -(2,6-Me.sub.2)1197f tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NHC.sub.6 C.sub.2 -(2,4,6- Me.sub.3)1197g tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 �4-(3,5- dimethyl)isoxazolyl!1197h tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NH(2-naphthyl)1197j tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NH(1-naphthyl)1197k tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NHC.sub.6 H.sub.4 -(4-Ph)1197m tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NHC.sub.6 H.sub.2 -(4-Ph-2,6- dimethyl)1197n tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NHC.sub.6 H.sub.2 -(4-Ph-2,6- dichloro)1197p tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NHCH.sub.2 Ph1198 imidazolin-2-ylamino-(CH.sub.2).sub.3 H H H NHCOOCH.sub.2 Ph 508.61199 imidazolin-2-ylamino-(CH.sub.2).sub.3 H H H NHCO.sub.2 CH.sub.2 C.sub.6 H.sub.4 -(2-CH.sub.3)1200 imidazolin-2-ylamino-(CH.sub.2).sub.3 H H H NHCO.sub.2 CH.sub.2 C.sub.6 H.sub.4 -(3-CH.sub.3)1201 imidazolin-2-ylamino-(CH.sub.2).sub.3 H H H NHCO.sub.2 CH.sub.2 C.sub.6 H.sub.4 -(4-CH.sub.3)1202 imidazolin-2-ylamino-(CH.sub.2).sub.3 H H H NHCO.sub.2 CH.sub.2 (2-pyridinyl)1203 imidazolin-2-ylamino-(CH.sub.2).sub.3 H H H NHCO.sub.2 CH.sub.2 (3-pyridinyl)1204 imidazolin-2-ylamino-(CH.sub.2).sub.3 H H H NHCO.sub.2 CH.sub.2 (4-pyridinyl)1205 imidazolin-2-ylamino-(CH.sub.2).sub.3 H H H NHCO.sub.2 CH.sub.2 (2-thiazolyl)1206 imidazolin-2-ylamino-(CH.sub.2).sub.3 H H H NHCO.sub.2 CH.sub.2 (4-thiazolyl)1207 imidazolin-2-ylamino-(CH.sub.2).sub.3 H H H NHCO.sub.2 CH.sub.2 (5-thiazolyl)1208 imidazolin-2-ylamino-(CH.sub.2).sub.3 H H H NHCO.sub.2 CH.sub.2 (4-isoxazolyl)1209 imidazolin-2-ylamino-(CH.sub.2).sub.3 H H H NHCO.sub.2 CH.sub.2 (2-thienyl)1210 imidazolin-2-ylamino-(CH.sub.2).sub.3 H H H NHCO.sub.2 n-Bu1211 imidazolin-2-ylamino-(CH.sub.2).sub.3 H H H NHCO.sub.2 i-Bu1212 imidazolin-2-ylamino-(CH.sub.2).sub.3 H H H NHCO.sub.2 t-Bu1213 imidazolin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 Ph 514.31214 imidazolin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.4 -(2-CH.sub.3)1215 imidazolin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.4 -(3-CH.sub.3)1216 imidazolin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.4 -(4-CH.sub.3)1216a imidazolin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.3 -(2,6-Me.sub.2)1216b imidazolin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.2 -(2,4,6-Me.sub.3) 556.41217 imidazolin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 (2-pyridyl)1218 imidazolin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 (3-pyridyl)1219 imidazolin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 (4-pyridyl)1219a imidazolin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 (2-thienyl)1219b imidazolin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 -�3-(2,5- dichloro)thienyl!1220 imidazolin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 (2-thiazolyl)1220a imidazolin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 -�5-(4-methyl-2- amino)thiazolyl!1221 imidazolin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 (4-isoxazolyl)1222 imidazolin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 -�4-(3,5- dimethyl)isoxazolyl!1223 imidazolin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.4 -(2-Br)1224 imidazolin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.4 -(3-Br)1225 imidazolin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.4 -(2-F)1226 imidazolin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.4 -(3-F)1227 imidazolin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.4 -(4-F)1227a imidazolin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.3 -(2,6-Cl.sub.2)1228 imidazolin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 (2-naphthyl)1229 imidazolin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 (1-naphthyl)1229a imidazolin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.4 -(4-Ph)1229b imidazolin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.4 -4-(4- pyridyl)1229c imidazolin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.4 -4-(2- oxazolyl)1229d imidazolin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.4 -4-(3- pyrazolyl)1229e imidazolin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.2 -4-Ph-2,6- dimethyl1229f imidazolin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.2 -4-(3- pyridyl)-2,6-dimethyl1229g imidazolin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.2 -4-(2-oxa- zolyl)-2,6-dimethyl1229h imidazolin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.2 -4-(3-pyra- zolyl)-2,6-dimethyl1229i imidazolin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.2 -4-Ph-2,6- dichloro1229j imidazolin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.4 -4-(2-furyl)1229k imidazolin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.2 -4-(3-furyl)1229l imidazolin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.2 -4-(3- pyridyl)1229m imidazolin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.2 -4-(4- pyridyl)-2,6-dimethyl1229n imidazolin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.2 -4-(3-furyl)- 2,6-dimethyl1229o imidazolin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.2 -4-(2-furyl)- 2,6-dichloro1230 imidazolin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 CHCHPh1231 imidazolin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 CH.sub.2 Ph1232 imidazolin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 CH.sub.2 CHCHPh1233 imidazolin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 -n-Bu1234 imidazolin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 -i-Bu1234a imidazolin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NHPh1234b imidazolin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NHC.sub.6 H.sub.4 -(2-CH.sub.3)1234c imidazolin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NHC.sub.6 H.sub.4 -(3-CH.sub.3)1234d imidazolin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NHC.sub.6 H.sub.4 -(4-CH.sub.3)1234e imidazolin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NHC.sub.6 C.sub.3 -(2,6-Me.sub.2)1234f imidazolin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NHC.sub.6 C.sub.2 -(2,4,6- Me.sub.3)1234g imidazolin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NH(2-naphthyl)1234h imidazolin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NH)1-naphthyl)1234j imidazolin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NHC.sub.6 H.sub.4 -(4-Ph)1234m imidazolin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NHC.sub.6 H.sub.2 -(4-Ph-2,6- dimethyl)1234n imidazolin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NHC.sub.6 H.sub.2 -(4-Ph-2,6- dichloro)1234p imidazolin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NHCH.sub.2 Ph1235 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 Ph1236 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.4 -(2-CH.sub.3)1237 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.4 -(3-CH.sub.3)1238 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.4 -(4-CH.sub.3)1238a benzimidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.3 -(2,6-Me.sub.2)1238b benzimidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.2 -(2,4,6-Me.sub.3)1239 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 (2-pyridyl)1240 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 (3-pyridyl)1241 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 (4-pyridyl)1241a benzimidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 (2-thienyl)1241b benzimidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 -�3-(2,5- dichloro)thienyl!1242 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 (2-thiazolyl)1242a benzimidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 -�5-(4-methyl-2- amino)thiazolyl!1243 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 (4-isoxazolyl)1244 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 -�4-(3,5- dimethyl)isoxazolyl!1245 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.4 -(2-Br)1246 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.4 -(3-Br)1247 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.4 -(2-F)1248 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.4 -(3-F)1249 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.4 -(4-F)1249a benzimidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.3 -(2,6-Cl.sub.2)1249b benzimidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 (2-naphthyl)1249c benzimidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 (1-naphthyl)1249d benzimidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.4 -(4-Ph)1249e benzimidazol-2-ylamino(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.2 -(4-Ph-2,6- dimethyl)1249f benzimidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.2 -(4-Ph-2,6- dichloro)1249g benzimidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 CHCHPh1249h benzimidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 CH.sub.2 Ph1249j benzimidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 CH.sub.2 CHCHPh1249k benzimidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 -n-Bu1249m benzimidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 -i-Bu1249n benzimidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NHPh1249p benzimidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NHC.sub.6 H.sub.4 -(2-CH.sub.3)1249q benzimidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NHC.sub.6 H.sub.4 -(3-CH.sub.3)1249r benzimidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NHC.sub.6 H.sub.4 -(4-CH.sub.3)1249s benzimidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NHC.sub.6 C.sub.3 -(2,6-Me.sub.2)1249t benzimidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NHC.sub.6 C.sub.2 -(2,4,6- Me.sub.3)1249u benzimidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NH(2-naphthyl)1249v benzimidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NH)1-naphthyl)1249w benzimidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NHC.sub.6 H.sub.4 -(4-Ph)1249x benzimidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NHC.sub.6 H.sub.2 -(4-Ph-2,6- dimethyl)1249y benzimidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NHC.sub.6 H.sub.2 -(4-Ph-2,6- dichloro)1249z benzimidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NHCH.sub.2 Ph1250 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHCO.sub.2 CH.sub.2 Ph1251 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHCO.sub.2 n-Bu1252 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHCO.sub.2 i-Bu1253 2-aminopyridin-6-yl-(CH.sub.2).sub.3 H H H NHSO.sub.2 Ph1254 2-aminopyridin-6-yl-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.4 -(2-CH.sub.3)1255 2-aminopyridin-6-yl-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.4 -(3-CH.sub.3)1256 2-aminopyridin-6-yl-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.4 -(4-CH.sub.3)1256a 2-aminopyridin-6-yl-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.3 -(2,6-Me.sub.2)1256b 2-aminopyridin-6-yl-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.2 -(2,4,6-Me.sub.3)1257 2-aminopyridin-6-yl-(CH.sub.2).sub.3 H H H NHSO.sub.2 (2-pyridyl)1258 2-aminopyridin-6-yl-(CH.sub.2).sub.3 H H W NHSO.sub.2 (3-pyridyl)1259 2-aminopyridin-6-yl-(CH.sub.2).sub.3 H H H NHSO.sub.2 (4-pyridyl)1260 2-aminopyridin-6-yl-(CH.sub.2).sub.3 H H H NHSO.sub.2 (2-thiazolyl)1261 2-aminopyridin-6-yl-(CH.sub.2).sub.3 H H H NHSO.sub.2 (4-isoxazolyl)1262 2-aminopyridin-6-yl-(CH.sub.2).sub.3 H H H NHSO.sub.2 -�4-(3,5- dimethyl)isoxazolyl!1263 2-aminopyridin-6-yl-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.4 -(2-Br)1264 2-aminopyridin-6-yl-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.4 -(3-Br)1265 2-aminopyridin-6-yl-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.4 -(2-F)1266 2-aminopyridin-6-yl-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.4 -(3-F)1267 2-aminopyridin-6-yl-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.4 -(4-F)1267a 2-aminopyridin-6-yl-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.3 -(2,6-Cl.sub.2)1267b 2-aminopyridin-6-yl-(CH.sub.2).sub.3 H H H NHSO.sub.2 (2-naphthyl)1267c 2-aminopyridin-6-yl-(CH.sub.2).sub.3 H H H NHSO.sub.2 (1-naphthyl)1267d 2-aminopyridin-6-yl-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.4 -(4-Ph)1267e 2-aminopyridin-6-yl-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.2 -(4-Ph-2,6- dimethyl)1267f 2-aminopyridin-6-yl-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.2 -(4-Ph-2,6- dichloro)1267g 2-aminopyridin-6-yl-(CH.sub.2).sub.3 H H H NHSO.sub.2 CHCHPh1267h 2-aminopyridin-6-yl-(CH.sub.2).sub.3 H H H NHSO.sub.2 CH.sub.2 Ph1267j 2-aminopyridin-6-yl-(CH.sub.2).sub.3 H H H NHSO.sub.2 CH.sub.2 CHCHPh1267k 2-aminopyridin-6-yl-(CH.sub.2).sub.3 H H H NHSO.sub.2 -n-Bu1267m 2-aminopyridin-6-yl-(CH.sub.2).sub.3 H H H NHSO.sub.2 -i-Bu1267n 2-aminopyridin-6-yl-(CH.sub.2).sub.3 H H H NHSO.sub.2 NHPh1267p 2-aminopyridin-6-yl-(CH.sub.2).sub.3 H H H NHSO.sub.2 NHC.sub.6 H.sub.4 -(2-CH.sub.3)1267q 2-aminopyridin-6-yl-(CH.sub.2).sub.3 H H H NHSO.sub.2 NHC.sub.6 H.sub.4 -(3-CH.sub.3)1267r 2-aminopyridin-6-yl-(CH.sub.2).sub.3 H H H NHSO.sub.2 NHC.sub.6 H.sub.4 -(4-CH.sub.3)1267s 2-aminopyridin-6-yl-(CH.sub.2).sub.3 H H H NHSO.sub.2 NHC.sub.6 C.sub.3 -(2,6-Me.sub.2)1267t 2-aminopyridin-6-yl-(CH.sub.2).sub.3 H H H NHSO.sub.2 NHC.sub.6 C.sub.2 -(2,4,6- Me.sub.3)1267u 2-aminopyridin-6-yl-(CH.sub.2).sub.3 H H H NHSO.sub.2 NH(2-naphthyl)1267v 2-aminopyridin-6-yl-(CH.sub.2).sub.3 H H H NHSO.sub.2 NH)1-naphthyl)1267w 2-aminopyridin-6-yl-(CH.sub.2).sub.3 H H H NHSO.sub.2 NHC.sub.6 H.sub.4 -(4-Ph)1267x 2-aminopyridin-6-yl-(CH.sub.2).sub.3 H H H NHSO.sub.2 NHC.sub.6 H.sub.2 -(4-Ph-2,6- dimethyl)1267y 2-aminopyridin-6-yl-(CH.sub.2).sub.3 H H H NHSO.sub.2 NHC.sub.6 H.sub.2 -(4-Ph-2,6- dichloro)1268 2-aminopyridin-6-yl-(CH.sub.2).sub.3 H H H NHCO.sub.2 CH.sub.2 Ph1269 2-aminopyridin-6-yl-(CH.sub.2).sub.3 H H H NHCO.sub.2 n-Bu1270 2-aminopyridin-6-yl-(CH.sub.2).sub.3 H H H NHCO.sub.2 i-Bu1271 2-iminoazepin-7-yl-(CH.sub.2).sub.3 H H H NHSO.sub.2 Ph1274 imidazol-4-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 Ph1279 2-iminoazepin-7-yl-(CH.sub.2).sub.3 H H H NHSO.sub.2 (4-isoxazolyl)1282 imidazol-4-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 (4-isoxazolyl)1287 2-iminoazepin-7-yl-(CH.sub.2).sub.3 H H H NHSO.sub.2 -�4-(3,5- dimethyl)isoxazolyl!1290 imidazol-4-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 -�4-(3,5- dimethyl)isoxazolyl!1295 imidazol-2-ylamino-(CH.sub.2).sub.3 H H 3-pyridinyl H1296 pyridin-2-ylamino-(CH.sub.2).sub.3 H H 3-pyridinyl H1297 imidazolin-2-ylamino-(CH.sub.2).sub.3 H H 3-pyridinyl H1298 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H H 3-pyridinyl H1299 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H H 3-pyridinyl H1300 2-aminopyridin-6-yl-(CH.sub.2).sub.3 H H 3-pyridinyl H1301 2-iminoazepin-7-yl-(CH.sub.2).sub.3 H H 3-pyridinyl H1304 imidazol-4-ylamino-(CH.sub.2).sub.3 H H 3-pyridinyl H1309 imidazol-2-ylamino-(CH.sub.2).sub.3 H H (3,4-methylene- H dioxy)phenyl1310 pyridin-2-ylamino-(CH.sub.2).sub.3 H H (3,4-methylene- H dioxy)phenyl1311 imidazolin-2-ylamino-(CH.sub.2).sub.3 H H (3,4-methylene- H dioxy)phenyl1312 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H H (3,4-methylene- H dioxy)phenyl1313 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H H (3,4-methylene- H dioxy)phenyl1314 2-aminopyridin-6-yl-(CH.sub.2).sub.3 H H (3,4-methylene- H dioxy)phenyl1315 2-iminoazepin-7-yl-(CH.sub.2).sub.3 H H (3,4-methylene- H dioxy)phenyl1318 imidazol-4-ylamino-(CH.sub.2).sub.3 H H (3,4-methylene- H dioxy)phenyl1323 imidazol-2-ylamino-(CH.sub.2).sub.3 H H 3-pyridinyl NHSO.sub.2 Ph1324 pyridin-2-ylamino-(CH.sub.2).sub.3 H H 3-pyridinyl NHSO.sub.2 Ph1325 imidazol-2-ylamino-(CH.sub.2).sub.3 H H (3,4-methylene- NHSO.sub.2 Ph dioxy)phenyl1326 pyridin-2-ylamino-(CH.sub.2).sub.3 H H (3,4-methylene- NHSO.sub.2 Ph dioxy)phenyl1326a pyridinyl-2-ylamino(CH.sub.2).sub.2 CH(Ph) H H H NHSO.sub.2 C.sub.6 H.sub.2 -(2,4,6-CH.sub.3).sub.3 641.41326b pyridin-2-ylamino-(CH.sub.2).sub.2 CH(CH.sub.3) H H H NHSO.sub.2 C.sub.6 H.sub.2 -(2,4,6-CH.sub.3).sub.3 579.41326c pyridin-2-ylamino-CH.sub.2 CH(CH.sub.3)CH.sub.2 H H H NHSO.sub.2 C.sub.6 H.sub.2 -(2,4,6-CH.sub.3).sub.3 579.51326d pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H H NHSO.sub.2 C.sub.6 H.sub.2 -(2,4,6-CH.sub.3).sub.31326e pyridin-2-ylamino-(CH.sub.2).sub.3 C.sub.2 H.sub.5 H H NHSO.sub.2 C.sub.6 H.sub.2 -(2,4,6-CH.sub.3).sub.31326f pyridin-2-ylamino-(CH.sub.2).sub.3 Ph H H NHSO.sub.2 C.sub.6 H.sub.2 -(2,4,6-CH.sub.3).sub.3 641.41326g pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.2 CH.sub.2 Ph H H NHSO.sub.2 C.sub.6 H.sub.2 -(2,4,6-CH.sub.3).sub.3 669.51326h pyridin-2-ylamino-(CH.sub.2).sub.3 H CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.2 -(2,4,6-CH.sub.3).sub.3 579.41326i imidazol-2-ylamino-(CH.sub.2).sub.2 H H Me NHSO.sub.2 C.sub.6 H.sub.2 -(2,4,6-CH.sub.3).sub.3 568.31327 imidazol-2-ylamino-(CH.sub.2).sub.2 H H H NHSO.sub.2 Ph1327a imidazol-2-ylamino-(CH.sub.2).sub.2 H H H NHCO.sub.2 CH.sub.2 Ph1327b imidazol-2-ylamino-carbonyl-(CH.sub.2).sub.2 H H H NHSO.sub.2 C.sub.6 H.sub.2 -(2,4,6-CH.sub.3).sub.3 568.51328 pyridin-2-ylamino-(CH.sub.2).sub.2 H H H NHSO.sub.2 Ph1328a pyridin-2-ylamino-(CH.sub.2).sub.2 H H H NHCO.sub.2 CH.sub.2 Ph1328b pyridin-2-ylamino-carbonyl-(CH.sub.2).sub.2 H H H NHSO.sub.2 C.sub.6 H.sub.2 -(2,4,6-CH.sub.3).sub.31329 imidazolin-2-ylamino-(CH.sub.2).sub.2 H H H NHSO.sub.2 Ph1329a imidazolin-2-ylamino-(CH.sub.2).sub.2 H H H NHCO.sub.2 CH.sub.2 Ph 494.31330 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.2 H H H NHSO.sub.2 Ph1330a tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.2 H H H NHCO.sub.2 CH.sub.2 Ph1331 benzimidazol-2-ylamino-(CH.sub.2).sub.2 H H H NHSO.sub.2 Ph1331a benzimidazol-2-ylamino-(CH.sub.2).sub.2 H H H NHCO.sub.2 CH.sub.2 Ph1331b benzimidazol-2-ylamino-carbonyl- H H H NHSO.sub.2 C.sub.6 H.sub.2 -(2,4,6-CH.sub.3).sub.3 (CH.sub.2).sub.21332 2-aminopyridin-6-yl-(CH.sub.2).sub.2 H H H NHSO.sub.2 Ph1332a 2-aminopyridin-6-yl-(CH.sub.2).sub.2 H H H NHCO.sub.2 CH.sub.2 Ph1333 2-iminoazepin-7-yl-(CH.sub.2).sub.2 H H H NHSO.sub.2 Ph1333a 2-iminoazepin-7-yl-(CH.sub.2).sub.2 H H H NHCO.sub.2 CH.sub.2 Ph1336 imidazol-4-ylamino-(CH.sub.2).sub.2 H H H NHSO.sub.2 Ph1336a imidazol-4-ylamino-(CH.sub.2).sub.2 H H H NHCO.sub.2 CH.sub.2 Ph1341 imidazol-2-ylamino-(CH.sub.2).sub.4 H H H NHSO.sub.2 Ph1341a imidazol-2-ylamino-(CH.sub.2).sub.4 H H H NHCO.sub.2 CH.sub.2 Ph1342 pyridin-2-ylamino-(CH.sub.2).sub.4 H H H NHSO.sub.2 Ph1342a pyridin-2-ylamino-(CH.sub.2).sub.4 H H H NHCO.sub.2 CH.sub.2 Ph1343 imidazolin-2-ylamino-(CH.sub.2).sub.4 H H H NHSO.sub.2 Ph1343a imidazolin-2-ylamino-(CH.sub.2).sub.4 H H H NHCO.sub.2 CH.sub.2 Ph 522.31344 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.4 H H H NHSO.sub.2 Ph1344a tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.4 H H H NHCO.sub.2 CH.sub.2 Ph1345 benzimidazol-2-ylamino-(CH.sub.2).sub.4 H H H NHSO.sub.2 Ph1345a benzimidazol-2-ylamino-(CH.sub.2).sub.4 H H H NHCO.sub.2 CH.sub.2 Ph1346 2-aminopyridin-6-yl-(CH.sub.2).sub.4 H H H NHSO.sub.2 Ph1346a 2-aminopyridin-6-yl-(CH.sub.2).sub.4 H H H NHCO.sub.2 CH.sub.2 Ph1347 2-iminoazepin-7-yl-(CH.sub.2).sub.4 H H H NHSO.sub.2 Ph1347a 2-iminoazepin-7-yl-(CH.sub.2).sub.4 H H H NHCO.sub.2 CH.sub.2 Ph1350 imidazol-4-ylamino-(CH.sub.2).sub.4 H H H NHSO.sub.2 Ph1350a imidazol-4-ylamino-(CH.sub.2).sub.4 H H H NHCO.sub.2 CH.sub.2 Ph1351 imidazol-2-ylamino-CH.sub.2 (o-C.sub.6 H.sub.4)CH.sub.2 H H H NHSO.sub.2 -(1-naphthyl)1352 imidazol-2-ylamino-CH.sub.2 (o-C.sub.6 H.sub.4)CH.sub.2 H H H NHCO.sub.2 CH.sub.2 Ph1353 imidazol-2-ylamino-CH.sub.2 (o-C.sub.6 H.sub.4)CH.sub.2 H H H NHSO.sub.2 C.sub.6 C.sub.2 -(2,4,6-Me.sub.3)1354 pyridin-2-ylamino-CH.sub.2 (o-C.sub.6 H.sub.4)CH.sub.2 H H H NHSO.sub.2 -(1-naphthyl)1355 pyridin-2-ylamino-CH.sub.2 (o-C.sub.6 H.sub.4)CH.sub.2 H H H NHCO.sub.2 CH.sub.2 Ph1356 pyridin-2-ylamino-CH.sub.2 (o-C.sub.6 H.sub.4)CH.sub.2 H H H NHSO.sub.2 C.sub.6 C.sub.2 -(2,4,6-Me.sub.3)1357 imidazolin-2-ylamino-CH.sub.2 (o-C.sub.6 H.sub.4)CH.sub.2 H H H NHSO.sub.2 -(1-naphthyl)1358 imidazolin-2-ylamino-CH.sub.2 (o-C.sub.6 H.sub.4)CH.sub.2 H H H NHCO.sub.2 CH.sub.2 Ph1359 imidazolin-2-ylamino-CH.sub.2 (o-C.sub.6 H.sub.4)CH.sub.2 H H H NHSO.sub.2 C.sub.6 C.sub.2 -(2,4,6-Me.sub.3)1360 imidazolin-2-ylamino-(o-C.sub.6 H.sub.4)CH.sub.2 H H H NHSO.sub.2 -(1-naphthyl)1361 imidazolin-2-ylamino-(o-C.sub.6 H.sub.4)CH.sub.2 H H H NHCO.sub.2 CH.sub.2 Ph1362 imidazolin-2-ylamino-(o-C.sub.6 H.sub.4)CH.sub.2 H H H NHSO.sub.2 C.sub.6 H.sub.2 -(2,4,6-Me.sub.3)__________________________________________________________________________ TABLE 2__________________________________________________________________________ ##STR60##Ex.No. R.sup.1a R.sup.10 R.sup.13 R.sup.14 R.sup.15 MS__________________________________________________________________________2001 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H H2002 pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHCOOCH.sub.2 Ph2003 imidazolin-2-yl amino-(CH.sub.2).sub.3 H H H NHCO.sub.2 CH.sub.2 C.sub.6 H.sub.4 -(2-CH.sub.3)2004 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H H H NHCO.sub.2 CH.sub.2 C.sub.6 H.sub.4 -(3-CH.sub.3)2005 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHCO.sub.2 CH.sub.2 C.sub.6 H.sub.4 -(4-CH.sub.3)2006 2-aminopyridin-6-yl-(CH.sub.2).sub.3 H H H NHCO.sub.2 CH.sub.2 (2-pyridinyl)2007 2-iminoazepin-7-yl-(CH.sub.2).sub.3 H H H NHCO.sub.2 CH.sub.2 (3-pyridinyl)2010 imidazol-4-ylamino-(CH.sub.2).sub.3 H H H NHCO.sub.2 CH.sub.2 (2-thiazolyl)2015 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHCO.sub.2 CH.sub.2 (4-isoxazolyl)2016 pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHCO.sub.2 CH.sub.2 (2-thienyl)2017 imidazolin-2-ylamino-(CH.sub.2).sub.3 H H H NHCO.sub.2 n-Bu2018 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H H H NHCO.sub.2 i-Bu2019 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHCO.sub.2 t-Bu2020 2-aminopyridin-6-yl-(CH.sub.2).sub.3 H H H NHSO.sub.2 Ph2021 2-iminoazepin-7-yl-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.4 -(2-CH.sub .3)2024 imidazol-4-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 (2-pyridyl)2029 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 (4-isoxazolyl)2030 pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 -�4-(3,5-dim- ethyl)isoxazolyl!2031 imidazolin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.4 -(2-Br)2032 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.4 -(3-Br)2033 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.4 -(4-Br)2034 2-aminopyridin-6-yl-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.4 -(2-F)2035 2-iminoazepin-7-yl-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.4 -(3-F)2038 imidazol-4-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 (1-naphthyl)2043 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 -i-Bu2044 pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 -t-Bu2045 imidazol-2-ylamino-(CH.sub.2).sub.3 H H (3,4- H methylenedioxy) phenyl2046 pyridin-2-ylamino-(CH.sub.2).sub.3 H H (3,4- H methylenedioxy) phenyl2047 imidazolin-2-ylamino-(CH.sub.2).sub.3 H H (3,4- H methylenedioxy) phenyl2048 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H H (3,4- H methylenedioxy) phenyl2049 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H H (3,4- H methylenedioxy) phenyl2050 2-aminopyridin-6-yl-(CH.sub.2).sub.3 H H (3,4- H methylenedioxy) phenyl2051 2-iminoazepin-7-yl-(CH.sub.2).sub.3 H H (3,4- methylenedioxy) phenyl2054 imidazol-4-ylamino-(CH.sub.2).sub.3 H H (3,4- H methylenedioxy) phenyl2059 imidazol-2-ylamino-(CH.sub.2).sub.3 H H 3-pyridinyl H2060 pyridin-2-ylamino-(CH.sub.2).sub.3 H H 3-pyridinyl H2061 imidazolin-2-ylamino-(CH.sub.2).sub.3 H H 3-pyridinyl H2062 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H H 3-pyridinyl H2063 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H H 3-pyridinyl H2064 2-aminopyridin-6-yl-(CH.sub.2).sub.3 H H 3-pyridinyl H2065 2-iminoazepin-7-yl-(CH.sub.2).sub.3 H H 3-pyridinyl H2068 imidazol-4-ylamino-(CH.sub.2).sub.3 H H 3-pyridinyl H2073 imidazolin-2-ylamino-(CH.sub.2).sub.3 H H H NHCOOCH.sub.2 Ph 508.32075 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHCO.sub.2 CH.sub.2 Ph2076 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHCO.sub.2 CH.sub.2 C.sub.6 H.sub.4 -(3-CH.sub.3)2077 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHCO.sub.2 CH.sub.2 (3 -pyridinyl)2078 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHCO.sub.2 CH.sub.2 (2-thiazolyl)2079 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHCO.sub.2 CH.sub.2 (2-thienyl)2080 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHCO.sub.2 CH.sub.2 (5-isoxazolyl)2081 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHCO.sub.2 n-Bu2082 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHCOPh2083 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHCOCH.sub.2 Ph2084 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHCOCH.sub.2 CH.sub.2 Ph2085 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHCOCHCHPh2086 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHCOCH.sub.2 (3-pyridinyl)2087 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHCOCH.sub.2 (2-thienyl)2088 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHCOCH.sub.2 (cyclohexyl)2089 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHCOn-Bu2090 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHCONHCH.sub.2 Ph2091 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 Ph2092 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.4 -(4-CH.sub .3)2093 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.3 -(2,6-CH.s ub.3).sub.2 540.32094 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.2 -(2,4,6-CH .sub.3).sub.3 554.42095 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 (3-pyridyl)2096 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 (2-thienyl)2097 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 (2-thiazolyl)2098 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 �4-(3,5- dimethyl)isoxazolyl!2099 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.4 -(4-Br)2100 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.4 -(4-F)2101 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.3 -(2,6-Cl.s ub.2)2102 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 (2-naphthyl)2103 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 (1-naphthyl) 562.42104 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.4 -4-Ph 588.42104a imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.4 -4-(4- pyridyl)2104b imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.4 -4-(2- oxazolyl)2104c imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.4 -4-(3- pyrazolyl)2105 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.2 -4-Ph-2,6- 616.3 dimethyl2105a imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.2 -4-(3- pyridyl)-2,6-dimethyl2105b imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.2 -4-(2-oxa- zolyl)-2,6-dimethyl2105c imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.2 -4-(3-pyra - zolyl)-2,6-dimethyl2106 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.2 -4-Ph-2,6- dichloro2107 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H-4-Ph-2,6- dimethyl-3-chloro2108 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 CH.sub.2 Ph2109 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 -n-Bu2110 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NHPh2111 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NHC.sub.6 H.sub.4 -(4-CH.sub.3)2112 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NHC.sub.6 C.sub.3 -(2,6-Me.sub.2)2113 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NHC.sub.6 C.sub.2 -(2,4,6- Me.sub.3)2114 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NH(3-pyridyl)2115 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 �4-(3,5- dimethyl)isoxazolyl!2116 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NHC.sub.6 H.sub.4 -(4-Br)2117 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NHC.sub.6 H.sub.4 -(4-F)2118 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NH(2-naphthyl)2119 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NH(1-naphthyl)2120 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NHC.sub.6 H.sub.4 -(4-Ph)2121 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NHC.sub.6 H.sub.2 -(4-Ph-2,6- dimethyl)2122 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NHC.sub.6 H.sub.2 -(4-Ph-2,6- dichloro)2123 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NHCH.sub.2 Ph2124 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NH-n-Bu2125 pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHCO.sub.2 CH.sub.2 C.sub.6 H.sub.4 -(3-CH.sub.3)2126 pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHCO.sub.2 CH.sub.2 (3-pyridinyl)2127 pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHCO.sub.2 CH.sub.2 (2-thiazolyl)2128 pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHCO.sub.2 CH.sub.2 (4-isoxazolyl)2129 pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHCO.sub.2 i-Bu2130 pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHCOPh2131 pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHCOCH.sub.2 Ph2132 pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHCOCH.sub.2 CH.sub.2 Ph2133 pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHCOCHCHPh2134 pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHCOCH.sub.2 (3-pyridinyl)2135 pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHCOCH.sub.2 (2-thienyl)2136 pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHCOCH.sub.2 (cyclohexyl)2137 pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHCOn-Bu2138 pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHCONHCH.sub.2 Ph2139 pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 Ph2140 pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.4 -(4-CH.sub .3)2141 pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.3 -(2,6-CH.s ub.3).sub.22142 pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.2 -(2,4,6-CH .sub.3).sub.3 565.42143 pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 (3-pyridyl)2144 pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 (2-thienyl)2145 pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 (2-thiazolyl)2146 pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.4 -(4-Br)2147 pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.4 -(4-F)2148 pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.3 -(2,6-Cl.s ub.2)2149 pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 (2-naphthyl)2150 pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 (1-naphthyl)2151 pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.4 -(4-Ph)2151a pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.4 -4-(4- pyridyl)2151b pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.4 -4-(2- oxazolyl)2151c pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.4 -4-(3- pyrazolyl)2152 pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.2 -4-Ph-2,6- dimethyl2152a pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.2 -4-(3- pyridyl)-2,6-dimethyl2152b pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.2 -4-(2-oxa- zolyl)-2,6-dimethyl2152c pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.2 -4-(3-pyra - zolyl)-2,6-dimethyl2153 pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.2 -4-Ph-2,6- dichloro2154 pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 CH.sub.2 Ph2155 pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 -n-Bu2156 pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NHPh2157 pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NHC.sub.6 H.sub.4 -(4-CH.sub.3)2158 pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NHC.sub.6 C.sub.3 -(2,6-Me.sub.2)2159 pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NHC.sub.6 C.sub.2 -(2,4,6- Me.sub.3)2160 pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NH(3-pyridyl)2161 pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 -�4-(3,5- dimethyl)isoxazolyl!2162 pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NHC.sub.6 H.sub.4 -(4-Br)2163 pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NHC.sub.6 H.sub.4 -(4-F)2164 pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NH(2-naphthyl)2165 pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NH)1-naphthyl)2166 pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NHC.sub.6 H.sub.4 -(4-Ph)2167 pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NHC.sub.6 H.sub.2 -(4-Ph-2,6- dimethyl)2168 pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NHC.sub.6 H.sub.2 -(4-Ph-2,6- dichloro)2169 pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NHCH.sub.2 Ph2170 pyridin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NH-n-Bu2171 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H H H NHCOOCH.sub.2 Ph2172 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H H H NHCO.sub.2 CH.sub.2 C.sub.6 H.sub.4 -(4-CH.sub.3)2173 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H H H NHCO.sub.2 CH.sub.2 (3-pyridinyl)2173 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H H H NHCO.sub.2 CH.sub.2 (2-thiazolyl)2175 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H H H NHCO.sub.2 CH.sub.2 (2-thienyl)2176 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H H H NHCO.sub.2 n-Bu2177 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 Ph2178 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.4 -(4-CH.sub .3)2179 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.3 -(2,6-Me.s ub.2)2180 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.2 -(2,4,6-Me .sub.3)2181 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 (3-pyridyl)2182 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 (2-thienyl)2183 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 (2-thiazolyl)2184 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.4 -(2-Br)2185 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.4 -(4-F)2186 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.3 -(2,6-Cl.s ub.2)2187 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 (2-naphthyl)2188 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 (1-naphthyl)2189 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.4 -(4-Ph)2189a tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.4 -4-(4- pyridyl)2189b tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.4 -4-(2- oxazolyl)2189c tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.4 -4-(3- pyrazolyl)2190 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.2 -4-Ph-2,6- dimethyl2190a tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.2 -4-(3- pyridyl)-2,6-dimethyl2190b tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.2 -4-(2-oxa- zolyl)-2,6-dimethyl2190c tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.2 -4-(3-pyra - zolyl)-2,6-dimethyl2191 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.2 -4-Ph-2,6- dichloro2192 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 CH.sub.2 Ph2193 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 -n-Bu2194 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NHPh2195 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NHC.sub.6 H.sub.4 -(4-CH.sub.3)2196 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NHC.sub.6 C.sub.3 -(2,6-Me.sub.2)2197 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NHC.sub.6 C.sub.2 -(2,4,6- Me.sub.3)2198 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 �4-(3,5- dimethyl)isoxazolyl!2199 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NH(2-naphthyl)2200 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NH(1-naphthyl)2201 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NHC.sub.6 H.sub.4 -(4-Ph)2202 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NHC.sub.6 H.sub.2 -(4-Ph-2,6- dimethyl)2203 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NHC.sub.6 H.sub.2 -(4-Ph-2,6- dichloro)2204 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NHCH.sub.2 Ph2205 imidazolin-2-ylamino-(CH.sub.2).sub.3 H H H NHCO.sub.2 CH.sub.2 C.sub.6 H.sub.4 -(4-CH.sub.3)2206 imidazolin-2-ylamino-(CH.sub.2).sub.3 H H H NHCO.sub.2 CH.sub.2 (3-pyridinyl)2207 imidazolin-2-ylamino-(CH.sub.2).sub.3 H H H NHCO.sub.2 CH.sub.2 (2-thiazolyl)2208 imidazolin-2-ylamino-(CH.sub.2).sub.3 H H H NHCO.sub.2 CH.sub.2 (2-thienyl)2209 imidazolin-2-ylamino-(CH.sub.2).sub.3 H H H NHCO.sub.2 i-Bu2210 imidazolin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 Ph2211 imidazolin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.4 -(3-CH.sub .3)2212 imidazolin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.3 -(2,6-Me.s ub.2)2213 imidazolin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.2 -(2,4,6-Me .sub.3)2214 imidazolin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 (3-pyridyl)2215 imidazolin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 (2-thienyl)2216 imidazolin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 (2-thiazolyl)2217 imidazolin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 -�4-(3,5- dimethyl)isoxazolyl!2218 imidazolin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.4 -(3-Br)2218 imidazolin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.4 -(4-F)2219 imidazolin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.3 -(2,6-Cl.s ub.2)2220 imidazolin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 (2-naphthyl)2221 imidazolin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 (1-naphthyl)2222 imidazolin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.4 -(4-Ph)2222a imidazolin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.4 -4-(4- pyridyl)2222b imidazolin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.4 -4-(2- oxazolyl)2222c imidazolin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.4 -4-(3- pyrazolyl)2223 imidazolin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.2 -4-Ph-2,6- dimethyl2223a imidazolin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.2 -4-(3- pyridyl)-2,6-dimethyl2223b imidazolin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.2 -4-(2-oxa- zolyl)-2,6-dimethyl2223c imidazolin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.2 -4-(3-pyra - zolyl)-2,6-dimethyl2224 imidazolin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.2 -4-Ph-2,6- dichloro2225 imidazolin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 CH.sub.2 Ph2226 imidazolin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 -n-Bu2227 imidazolin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NHPh2228 imidazolin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NHC.sub.6 H.sub.4 -(4-CH.sub.3)2229 imidazolin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NHC.sub.6 C.sub.3 -(2,6-Me.sub.2)2230 imidazolin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NHC.sub.6 C.sub.2 -(2,4,6- Me.sub.3)2231 imidazolin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NH(2-naphthyl)2232 imidazolin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NH)1-naphthyl)2233 imidazolin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NHC.sub.6 H.sub.4 -(4-Ph)2234 imidazolin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NHC.sub.6 H.sub.2 -4-Ph-2,6- dimethyl2235 imidazolin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NHC.sub.6 H.sub.2 -4-Ph-2,6- dichloro2236 imidazolin-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NHCH.sub.2 Ph2237 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 Ph2238 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.4 -(3-CH.sub .3)2239 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.3 -(2,6-Me.s ub.2)2240 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.2 -(2,4,6-Me .sub.3)2241 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 (4-pyridyl)2242 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 (2-thienyl)2243 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 (2-thiazolyl)2244 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 -�4-(3,5- dimethyl)isoxazolyl!2245 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.4 -(3-Br)2246 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.4 -(3-F)2247 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.3 -(2,6-Cl.s ub.2)2248 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 (2-naphthyl)2249 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 (1-naphthyl)2250 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.4 -(4-Ph)2251 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.2 -4-Ph-2,6- dimethyl2252 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.2 -4-Ph-2,6- dichloro2253 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 CH.sub.2 Ph2254 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 -i-Bu2255 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NHPh2256 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NHC.sub.6 H.sub.4 -(4-CH.sub.3)2257 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NHC.sub.6 C.sub.3 -(2,6-Me.sub.2)2258 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NHC.sub.6 C.sub.2 -(2,4,6- Me.sub.3)2259 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NH(2-naphthyl)2260 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NH)1-naphthyl)2261 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NHC.sub.6 H.sub.4 -(4-Ph)2262 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NHC.sub.6 H.sub.2 -4-Ph-2,6- dimethyl2263 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NHC.sub.6 H.sub.2 -4-Ph-2,6- dichloro2264 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 NHCH.sub.2 Ph2265 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHCO.sub.2 CH.sub.2 Ph2266 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H H H NHCO.sub.2 i-Bu2267 2-aminopyridin-6-yl-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.4 -(4-CH.sub .3)2268 2-aminopyridin-6-yl-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.3 -(2,6-Me.s ub.2)2269 2-aminopyridin-6-yl-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.2 -(2,4,6-Me .sub.3)2270 2-aminopyridin-6-yl-(CH.sub.2).sub.3 H H H NHSO.sub.2 (3-pyridyl)2271 2-aminopyridin-6-yl-(CH.sub.2).sub.3 H H H NHSO.sub.2 (2-thiazolyl)2272 2-aminopyridin-6-yl-(CH.sub.2).sub.3 H H H NHSO.sub.2 (4-isoxazolyl)2273 2-aminopyridin-6-yl-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.4 -(3-Br)2274 2-aminopyridin-6-yl-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.4 -(3-F)2275 2-aminopyridin-6-yl-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.3 -(2,6-Cl.s ub.2)2276 2-aminopyridin-6-yl-(CH.sub.2).sub.3 H H H NHSO.sub.2 (2-naphthyl)2277 2-aminopyridin-6-yl-(CH.sub.2).sub.3 H H H NHSO.sub.2 (1-naphthyl)2278 2-aminopyridin-6-yl-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.4 -(4-Ph)2279 2-aminopyridin-6-yl-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.2 -4-Ph-2,6- dimethyl2280 2-aminopyridin-6-yl-(CH.sub.2).sub.3 H H H NHSO.sub.2 C.sub.6 H.sub.2 -4-Ph-2,6- dichloro2281 2-aminopyridin-6-yl-(CH.sub.2).sub.3 H H H NHSO.sub.2 CH.sub.2 Ph2282 2-aminopyridin-6-yl-(CH.sub.2).sub.3 H H H NHSO.sub.2 -i-Bu2283 2-aminopyridin-6-yl-(CH.sub.2).sub.3 H H H NHSO.sub.2 NHPh2284 2-aminopyridin-6-yl-(CH.sub.2).sub.3 H H H NHSO.sub.2 NHC.sub.6 H.sub.4 -(4-CH.sub.3)2285 2-aminopyridin-6-yl-(CH.sub.2).sub.3 H H H NHSO.sub.2 NHC.sub.6 C.sub.3 -(2,6-Me.sub.2)2286 2-aminopyridin-6-yl-(CH.sub.2).sub.3 H H H NHSO.sub.2 NHC.sub.6 C.sub.2 -(2,4,6- Me.sub.3)2287 2-aminopyridin-6-yl-(CH.sub.2).sub.3 H H H NHSO.sub.2 NH(2-naphthyl)2288 2-aminopyridin-6-yl-(CH.sub.2).sub.3 H H H NHSO.sub.2 NH)1-naphthyl)2289 2-aminopyridin-6-yl-(CH.sub.2).sub.3 H H H NHSO.sub.2 NHC.sub.6 H.sub.4 -(4-Ph)2290 2-aminopyridin-6-yl-(CH.sub.2).sub.3 H H H NHSO.sub.2 NHC.sub.6 H.sub.2 -4-Ph-2,6- dimethyl2291 2-aminopyridin-6-yl-(CH.sub.2).sub.3 H H H NHSO.sub.2 NHC.sub.6 H.sub.2 -4-Ph-2,6- dichloro2292 2-aminopyridin-6-yl-(CH.sub.2).sub.3 H H H NHCO.sub.2 n-Bu2293 2-aminopyridin-6-yl-(CH.sub.2).sub.3 H H H NHCO.sub.2 i-Bu2294 2-iminoazepin-7-yl-(CH.sub.2).sub.3 H H H NHSO.sub.2 Ph2295 imidazol-4-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 Ph2296 2-iminoazepin-7-yl-(CH.sub.2).sub.3 H H H NHSO.sub.2 (4-isoxazolyl)2297 imidazol-4-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 (4-isoxazolyl)2298 2-iminoazepin-7-yl-(CH.sub.2).sub.3 H H H NHSO.sub.2 -�4-(3,5- dimethyl)isoxazolyl!2299 imidazol-4-ylamino-(CH.sub.2).sub.3 H H H NHSO.sub.2 -�4-(3,5- dimethyl)isoxazolyl!2300 imidazol-2-ylamino-(CH.sub.2).sub.3 H H 3-pyridinyl NHSO.sub.2 Ph2301 pyridin-2-ylamino-(CH.sub.2).sub.3 H H 3-pyridinyl NHSO.sub.2 Ph2302 imidazol-2-ylamino-(CH.sub.2).sub.3 H H (3,4-methylene- NHSO.sub.2 Ph dioxy)phenyl2303 pyridin-2-ylamino-(CH.sub.2).sub.3 H H (3,4-methylene- NHSO.sub.2 Ph dioxy)phenyl2304 imidazol-2-ylamino-(CH.sub.2).sub.2 H H H NHSO.sub.2 Ph2305 imidazol-2-ylamino-(CH.sub.2).sub.2 H H H NHCO.sub.2 CH.sub.2 Ph2306 imidazol-2-ylamino-carbonyl-(CH.sub.2).sub.2 H H H NHSO.sub.2 C.sub.6 H.sub.2 -(2,4,6-CH .sub.3).sub.32307 pyridin-2-ylamino-(CH.sub.2).sub.2 H H H NHSO.sub.2 Ph2308 pyridin-2-ylamino-(CH.sub.2).sub.2 H H H NHCO.sub.2 CH.sub.2 Ph2309 pyridin-2-ylamino-carbonyl-(CH.sub.2).sub.2 H H H NHSO.sub.2 C.sub.6 H.sub.2 -(2,4,6-CH .sub.3).sub.32310 imidazolin-2-ylamino-(CH.sub.2).sub.2 H H H NHSO.sub.2 Ph2311 imidazolin-2-ylamino-(CH.sub.2).sub.2 H H H NHCO.sub.2 CH.sub.2 Ph2312 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.2 H H H NHSO.sub.2 Ph2313 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.2 H H H NHCO.sub.2 CH.sub.2 Ph2314 benzimidazol-2-ylamino-(CH.sub.2).sub.2 H H H NHSO.sub.2 Ph2315 benzimidazol-2-ylamino-(CH.sub.2).sub.2 H H H NHCO.sub.2 CH.sub.2 Ph2316 benzimidazol-2-ylamino-carbonyl-(CH.sub.2).sub.2 H H H NHSO.sub.2 C.sub.6 H.sub.2 -(2,4,6-CH .sub.3).sub.32317 2-aminopyridin-6-yl-(CH.sub.2).sub.2 H H H NHSO.sub.2 Ph2318 2-aminopyridin-6-yl-(CH.sub.2).sub.2 H H H NHCO.sub.2 CH.sub.2 Ph2319 2-iminoazepin-7-yl-(CH.sub.2).sub.2 H H H NHSO.sub.2 Ph2320 2-iminoazepin-7-yl-(CH.sub.2).sub.2 H H H NHCO.sub.2 CH.sub.2 Ph2321 imidazol-4-ylamino-(CH.sub.2).sub.2 H H H NHSO.sub.2 Ph2322 imidazol-4-ylamino-(CH.sub.2).sub.2 H H H NHCO.sub.2 CH.sub.2 Ph2323 imidazol-2-ylamino-(CH.sub.2).sub.4 H H H NHSO.sub.2 Ph2324 imidazol-2-ylamino-(CH.sub.2).sub.4 H H H NHCO.sub.2 CH.sub.2 Ph2325 pyridin-2-ylamino-(CH.sub.2).sub.4 H H H NHSO.sub.2 Ph2326 pyridin-2-ylamino-(CH.sub.2).sub.4 H H H NHCO.sub.2 CH.sub.2 Ph2327 imidazolin-2-ylamino-(CH.sub.2).sub.4 H H H NHSO.sub.2 Ph2328 imidazolin-2-ylamino-(CH.sub.2).sub.4 H H H NHCO.sub.2 CH.sub.2 Ph 522.32329 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.4 H H H NHSO.sub.2 Ph2330 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.4 H H H NHCO.sub.2 CH.sub.2 Ph2331 benzimidazol-2-ylamino-(CH.sub.2).sub.4 H H H NHSO.sub.2 Ph2332 benzimidazol-2-ylamino-(CH.sub.2).sub.4 H H H NHCO.sub.2 CH.sub.2 Ph2333 2-aminopyridin-6-yl-(CH.sub.2).sub.4 H H H NHSO.sub.2 Ph2334 2-aminopyridin-6-yl-(CH.sub.2).sub.4 H H H NHCO.sub.2 CH.sub.2 Ph2335 2-iminoazepin-7-yl-(CH.sub.2).sub.4 H H H NHSO.sub.2 Ph2336 2-iminoazepin-7-yl-(CH.sub.2).sub.4 H H H NHCO.sub.2 CH.sub.2 Ph2337 imidazol-4-ylamino-(CH.sub.2).sub.4 H H H NHSO.sub.2 Ph2338 imidazol-4-ylamino-(CH.sub.2).sub.4 H H H NHCO.sub.2 CH.sub.2 Ph2339 imidazol-2-ylamino-CH.sub.2 (o-C.sub.6 H.sub.4)CH.sub.2 H H H NHSO.sub.2 -(1-naphthyl)2340 imidazol-2-ylamino-CH.sub.2 (o-C.sub.6 H.sub.4)CH.sub.2 H H H NHCO.sub.2 CH.sub.2 Ph2341 imidazol-2-ylamino-CH.sub.2 (o-C.sub.6 H.sub.4)CH.sub.2 H H H NHSO.sub.2 C.sub.6 C.sub.2 -(2,4,6-Me .sub.3)2342 pyridin-2-ylamino-CH.sub.2 (o-C.sub.6 H.sub.4)CH.sub.2 H H H NHSO.sub.2 -(1-naphthyl)2343 pyridin-2-ylamino-CH.sub.2 (o-C.sub.6 H.sub.4)CH.sub.2 H H H NHCO.sub.2 CH.sub.2 Ph2344 pyridin-2-ylamino-CH.sub.2 (o-C.sub.6 H.sub.4)CH.sub.2 H H H NHSO.sub.2 C.sub.6 C.sub.2 -(2,4,6-Me .sub.3)2345 imidazolin-2-ylamino-CH.sub.2 (o-C.sub.6 H.sub.4)CH.sub.2 H H H NHSO.sub.2 -(1-naphthyl)2346 imidazolin-2-ylamino-CH.sub.2 (o-C.sub.6 H.sub.4)CH.sub.2 H H H NHCO.sub.2 CH.sub.2 Ph2347 imidazolin-2-ylamino-CH.sub.2 (o-C.sub.6 H.sub.4)CH.sub.2 H H H NHSO.sub.2 C.sub.6 C.sub.2 -(2,4,6-Me .sub.3)2348 imidazolin-2-ylamino-(o-C.sub.6 H.sub.4)CH.sub.2 H H H NHSO.sub.2 -(1-naphthyl)2349 imidazolin-2-ylamino-(o-C.sub.6 H.sub.4)CH.sub.2 H H H NHCO.sub.2 CH.sub.2 Ph2350 imidazolin-2-ylamino-(o-C.sub.6 H.sub.4)CH.sub.2 H H H NHSO.sub.2 C.sub.6 C.sub.2 -(2,4,6-Me .sub.3)__________________________________________________________________________ TABLE 3__________________________________________________________________________ ##STR61##Ex. No. R.sup.1 R.sup.9 R.sup.14 R.sup.15 MS__________________________________________________________________________3001 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H3002 pyridin-2-ylamino-(CH.sub.2).sub.3 H H NHCOOCH.sub.2 Ph3002a imidazolin-2-ylamino-(CH.sub.2).sub.3 H H NHCOOCH.sub.2 Ph3002b tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H H NHCO.sub.2 CH.sub.2 Ph3002c imidazol-2-ylamino-(CH.sub.2).sub.3 H H NHCO.sub.2 CH.sub.2 Ph3003 imidazolin-2-ylamino-(CH.sub.2).sub.3 H H NHCO.sub.2 CH.sub.2 C.sub.6 H.sub.4 -(2-CH.sub.3)3004 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H H NHCO.sub.2 CH.sub.2 C.sub.6 H.sub.4 -(3-CH.sub.3)3005 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H H NHCO.sub.2 CH.sub.2 C.sub.6 H.sub.4 -(4-CH.sub.3)3006 2-aminopyridin-6-yl-(CH.sub.2).sub.3 H H NHCO.sub.2 CH.sub.2 (2-pyridinyl )3007 2-iminoazepin-7-yl-(CH.sub.2).sub.3 H H NHCO.sub.2 CH.sub.2 (3-pyridinyl )3010 imidazol-4-ylamino-(CH.sub.2).sub.3 H H NHCO.sub.2 CH.sub.2 (2-thiazolyl )3015 imidazol-2-ylamino-(CH.sub.2).sub.3 H H NHCO.sub.2 CH.sub.2 (4-isoxazoly l)3016 pyridin-2-ylamino-(CH.sub.2).sub.3 H H NHCO.sub.2 CH.sub.2 (2-thienyl)3017 imidazolin-2-ylamino-(CH.sub.2).sub.3 H H NHCO.sub.2 n-Bu3018 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H H NHCO.sub.2 i-Bu3019 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H H NHCO.sub.2 t-Bu3020 2-aminopyridin-6-yl-(CH.sub.2).sub.3 H H NHSO.sub.2 Ph3020a pyridin-2-ylamino-(CH.sub.2).sub.3 H H NHSO.sub.2 Ph3020b imidazolin-2-ylamino-(CH.sub.2).sub.3 H H NHSO.sub.2 Ph3020c tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H H NHSO.sub.2 Ph3020d imidazol-2-ylamino-(CH.sub.2).sub.3 H H NHSO.sub.2 Ph3021 2-iminoazepin-7-yl-(CH.sub.2).sub.3 H H NHSO.sub.2 C.sub.6 H.sub.4 -(2-CH.sub.3)3021a imidazol-2-ylamino-(CH.sub.2).sub.3 H H NHSO.sub.2 C.sub.6 H.sub.3 -(2,6-Me.sub.2)3021b imidazol-2-ylamino-(CH.sub.2).sub.3 H H NHSO.sub.2 C.sub.6 H.sub.2 -(2,4,6-Me.sub.3)3021c imidazo1-2-ylamino-(CH.sub.2).sub.3 H H NHSO.sub.2 C.sub.6 H.sub.2 -(2,6-Me.sub.2 -4-Ph)3021d pyridin-2-ylamino-(CH.sub.2).sub.3 H H NHSO.sub.2 C.sub.6 H.sub.2 -(2,6-Me.sub.2 -4-Ph)3021e imidazolin-2-ylamino-(CH.sub.2).sub.3 H H NHSO.sub.2 C.sub.6 H.sub.2 -(2,6-Me.sub.2 -4-Ph)3021f tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H H NHSO.sub.2 C.sub.6 H.sub.2 -(2,6-Me.sub.2 -4-Ph)3021g imidazol-2-ylamino-(CH.sub.2).sub.3 H H NHSO.sub.2 C.sub.6 H.sub.2 -(2,6-Me.sub.2 -4-(3-pyridyl)3021h imidazol-2-ylamino-(CH.sub.2).sub.3 H H NHSO.sub.2 C.sub.6 H.sub.2 -(2,6-Me.sub.2 -4-(4-pyridyl)3021i imidazol-2-ylamino-(CH.sub.2).sub.3 H H NHSO.sub.2 C.sub.6 H.sub.2 -(2,6-Me.sub.2 -4-(2-furyl)3021j imidazol-2-ylamino-(CH.sub.2).sub.3 H H NHSO.sub.2 C.sub.6 H.sub.2 -(2,6-Me.sub.2 -4-(3-furyl)3021k imidazol-2-ylamino-(CH.sub.2).sub.3 H H NHSO.sub.2 C.sub.6 H.sub.2 -(2,6-Me.sub.2 -4-(5-pyrazolyl))3021l pyridin-2-ylamino-(CH.sub.2).sub.3 H H NHSO.sub.2 C.sub.6 H.sub.2 -(2,4,6-Me.sub.3)3021m pyridin-2-ylamino-(CH.sub.2).sub.3 H H NHSO.sub.2 C.sub.6 H.sub.2 -(2,6-Me.sub.2 -4-(3-pyridyl))3021n pyridin-2-ylamino-(CH.sub.2).sub.3 H H NHSO.sub.2 C.sub.6 H.sub.2 -(2,6-Me.sub.2 -4-(4-pyridyl))3021o pyridin-2-ylamino-(CH.sub.2).sub.3 H H NHSO.sub.2 C.sub.6 H.sub.2 (2,6-Me.sub.2 -4-(2-furyl))3021p pyridin-2-ylamino-(CH.sub.2).sub.3 H H NHSO.sub.2 C.sub.6 H.sub.2 -(2,6-Me.sub.2 -4-(3-furyl))3021q pyridin-2-ylamino-(CH.sub.2).sub.3 H H NHSO.sub.2 C.sub.6 H.sub.2 -(2,6-Me.sub.2 -4-(5-pyrazolyl))3021r imidazolin-2-ylamino-(CH.sub.2).sub.3 H H NHSO.sub.2 C.sub.6 H.sub.2 -(2,4,6-Me.sub.3)3021s imidazolin-2-ylamino-(CH.sub.2).sub.3 H H NHSO.sub.2 C.sub.6 H.sub.2 -(2,6-Me.sub.2 -4-(3-pyridyl))3021t imidazolin-2-ylamino-(CH.sub.2).sub.3 H H NHSO.sub.2 C.sub.6 H.sub.2 - (2,6-Me.sub.2 -4-(4-pyridyl))3021u imidazolin-2-ylamino-(CH.sub.2).sub.3 H H NHSO.sub.2 C.sub.6 H.sub.2 -(2,6-Me.sub.2 -4-(2-furyl))3021v imidazolin-2-ylamino-(CH.sub.2).sub.3 H H NHSO.sub.2 C.sub.6 H.sub.2 -(2,6-Me.sub.2 -4-(3-furyl))3021w imidazolin-2-ylamino-(CH.sub.2).sub.3 H H NHSO.sub.2 C.sub.6 H.sub.2 -(2,6-Me.sub.2 -4-(5-pyrazolyl))3024 imidazol-4-ylamino-(CH.sub.2).sub.3 H H. NHSO.sub.2 (2-pyridyl)3029 imidazol-2-ylamino-(CH.sub.2).sub.3 H H NHSO.sub.2 (4-isoxazolyl)3030 pyridin-2-ylamino-(CH.sub.2).sub.3 H H NHSO.sub.2 -�4-(3,5-dimethyl)iso xazolyl!3030a imidazolin-2-ylamino-(CH.sub.2).sub.3 H H NHSO.sub.2 -�4-(3,5-dimethyl)iso xazolyl!3030b tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H H NHSO.sub.2 -�4-(3,5 dimethyl)isoxazolyl!3030c imidazol-2-ylamino-(CH.sub.2).sub.3 H H NHSO.sub.2 -�4-(3,5-dimethyl)iso xazolyl!3031 imidazolin-2-ylamino-(CH.sub.2).sub.3 H H NHSO.sub.2 C.sub.6 H.sub.4 -(2-Br)3032 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H H NHSO.sub.2 C.sub.6 H.sub.4 -(3-Br)3033 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H H NHSO.sub.2 C.sub.6 H.sub.4 -(4-Br)3034 2-aminopyridin-6-yl-(CH.sub.2).sub.3 H H NHSO.sub.2 C.sub.6 H.sub.4 -(2-F)3035 2-iminoazepin-7-yl-(CH.sub.2).sub.3 H H NHSO.sub.2 C.sub.6 H.sub.4 -(3-F)3038 imidazol-2-ylamino-(CH.sub.2).sub.3 H H NHSO.sub.2 (1-naphthyl)3038a imidazol-2-ylamino-(CH.sub.2).sub.3 H H NHSO.sub.2 C.sub.6 H.sub.3 -(2,6-Cl.sub.2)3038b imidazol-2-ylamino-(CH.sub.2).sub.3 H H NHSO.sub.2 C.sub.6 H.sub.2 -(2,6-Cl.sub.2 -4-Ph)3043 imidazol-2-ylamino-(CH.sub.2).sub.3 H H NHSO.sub.2 -i-Bu3044 pyridin-2-ylamino-(CH.sub.2)3 H H NHSO.sub.2 -t-Bu3045 imidazol-2-ylamino-(CH.sub.2).sub.3 H (3,4-methylenedioxy)phenyl3046 pyridin-2-ylamino-(CH.sub.2).sub.3 H (3,4-methylenedioxy)phenyl H3047 imidazolin-2-ylamino-(CH.sub.2).sub.3 H (3,4-methylenedioxy)phenyl H3048 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H (3,4-methylenedioxy)phenyl H3049 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H (3,4-methylenedioxy)phenyl H3050 2-aminopyridin-6-yl-(CH.sub.2).sub.3 H (3,4-methylenedioxy)phenyl H3051 2-iminoazepin-7-yl-(CH.sub.2).sub.3 H (3,4-methylenedioxy)phenyl H3054 imidazol-4-ylamino-(CH.sub.2).sub.3 H (3,4-methylenedioxy)phenyl H3059 imidazol-2-ylamino-(CH.sub.2).sub.3 H 3-pyridinyl H3060 pyridin-2-ylamino-(CH.sub.2).sub.3 H 3-pyridinyl H3061 imidazolin-2-ylamino-(CH.sub.2).sub.3 H 3-pyridinyl H3062 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H 3-pyridinyl H3063 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H 3-pyridinyl H3064 2-aminopyridin-6-yl-(CH.sub.2).sub.3 H 3-pyridinyl H3065 2-iminoazepin-7-yl-(CH.sub.2).sub.3 H 3-pyridinyl H3068 imidazol-4-ylamino-(CH.sub.2).sub.3 H 3-pyridinyl H3068a imidazol-2-ylamino-CH.sub.2 (o-C.sub.6 H.sub.4) H H NHSO.sub.2 -(1-naphthyl)3068b imidazol-2-ylamino-CH.sub.2 (o-C.sub.6 H.sub.4) H H NHCO.sub.2 CH.sub.2 Ph3068c imidazol-2-ylamino-CH.sub.2 (o-C.sub.6 H.sub.4) H H NHSO.sub.2 C.sub.6 C.sub.2 -(2,4,6-Me.sub.3)3068d pyridin-2-ylamino-CH.sub.2 (o-C.sub.6 H.sub.4) H H NHSO.sub.2 -(1-naphthyl)3068e pyridin-2-ylamino-CH.sub.2 (o-C.sub.6 H.sub.4) H H NHCO.sub.2 CH.sub.2 Ph3068f pyridin-2-ylamino-CH.sub.2 (o-C.sub.6 H.sub.4) H H NHSO.sub.2 C.sub.6 C.sub.2 -(2,4,6-Me.sub.3)3068g imidazolin-2-ylamino-CH.sub.2 (o-C.sub.6 H.sub.4) H H NHSO.sub.2 -(1-naphthyl)3068h imidazolin-2-ylamino-CH.sub.2 (6-C.sub.6 H.sub.4) H H NHCO.sub.2 CH.sub.2 Ph3068i imidazolin-2-ylamino-CH.sub.2 (o-C.sub.6 H.sub.4) H H NHSO.sub.2 C.sub.6 C.sub.2 -(2,4,6-Me.sub.3)3068j imidazolin-2-ylamino-(m-C.sub.6 H.sub.4) H H NHSO.sub.2 -(1-naphthyl)3068k imidazolin-2-ylamino-(m-C.sub.6 H.sub.4) H H NHCO.sub.2 CH.sub.2 Ph3068l imidazolin-2-ylamino-(m-C.sub.6 H.sub.4) H H NHSO.sub.2 C.sub.6 C.sub.2 -(2,4,6-Me.sub.3)3075 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHCO.sub.2 CH.sub.2 Ph3076 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHCO.sub.2 CH.sub.2 C.sub.6 H.sub.4 -(3-CH.sub.3)3077 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHCO.sub.2 CH.sub.2 (3-pyridinyl )3078 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHCO.sub.2 CH.sub.2 (2-thiazolyl )3079 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHCO.sub.2 CH.sub.2 (2-thienyl)3080 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHCO.sub.2 CH.sub.2 (5-isoxazoly l)3081 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHCO.sub.2 n-Bu3082 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHCOPh3083 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHCOCH.sub.2 Ph *3084 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHCOCH.sub.2 CH.sub.2 Ph3085 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHCOCH.dbd.CHPh3086 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHCOCH.sub.2 (3-pyridinyl)3087 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHCOCH.sub.2 (2-thienyl)3088 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHCOCH.sub.2 (cyclohexyl)3089 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHCOn-Bu3090 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHCONHCH.sub.2 Ph3091 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 Ph3092 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.4 -(4-CH.sub.3)3093 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.3 -(2,6-CH.sub.3).sub.2 554.43094 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.2 -(2,4,6-CH.sub.3).sub.3 568.43095 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 (3-pyridyl)3096 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 (2-thienyl)3097 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 (2-thiazolyl)3098 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 �4-(3,5-dimethyl)isox azolyl!3099 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.4 -(4-Br)3100 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.4 -(4-F)3101 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.3 -(2,6-Cl.sub.2) 594.33102 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 (2-naphthyl)3103 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 (1-naphthyl)3104 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.4 -(4-Ph)3104a imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.4 -4-(4-pyridyl)3104b imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.4 -4-(2-oxazolyl)3104c imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.4 -4-(3-pyrazolyl)3105 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.2 -(4-Ph-2,6-dimethyl) 630.33105a imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.2 -4-(3-pyridyl)-2,6-dimethyl3105b imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.2 -4-(2-oxazolyl)-2,6-dimethyl3105c imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.2 -4-(3-pyrazolyl)-2,6-dimethyl3105d imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.2 -4-(4-pyridyl)-2,6-dimethyl3105e imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.2 -4-(2-furyl)-2,6-dimethyl3105f imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.2 -4-(3-furyl)-2,6-dimethyl3106 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.2 -(4-Ph-2,6-dichloro) 670.33107 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H-(4-Ph-2,6-d imethyl-3-chloro)3108 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 CH.sub.2 Ph3109 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 -n-Bu3110 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NHPh3111 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NHC.sub.6 H.sub.4 -(4-CH.sub.3)3112 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NHC.sub.6 C.sub.3 -(2,6-Me.sub.2)3113 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NHC.sub.6 C.sub.2 -(2,4,6-Me.sub.3)3114 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NH(3-pyridyl)3115 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 �4-(3,5-dimethyl)isox azolyl!3116 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NHC.sub.6 H.sub.4 -(4-Br)3117 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NHC.sub.6 H.sub.4 -(4-F)3118 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NH(2-naphthyl)3119 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NH(1-naphthyl)3120 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NHC.sub.6 H.sub.4 -(4-Ph)3121 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NHC.sub.6 H.sub.2 -(4-Ph-2,6-dimethyl)3122 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NHC.sub.6 H.sub.2 -(4-Ph-2,6-dichloro)3123 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NHCH.sub.2 Ph3124 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NH-n-Bu3125 pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHCO.sub.2 CH.sub.2 C.sub.6 H.sub.4 -(3-CH.sub.3)3126 pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHCO.sub.2 CH.sub.2 (3-pyridinyl )3127 pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHCO.sub.2 CH.sub.2 (2-thiazolyl )3128 pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHCO.sub.2 CH.sub.2 (4-isoxazoly l)3129 pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHCO.sub.2 i-Bu3130 pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHCOPh3131 pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHCOCH.sub.2 Ph3132 pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHCOCH.sub.2 CH.sub.2 Ph3133 pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHCOCH.dbd.CHPh3134 pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHCOCH.sub.2 (3-pyridinyl)3135 pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHCOCH.sub.2 (2-thienyl)3136 pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHCOCH.sub.2 (cyclohexyl)3137 pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHCOn-Bu3138 pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHCONHCH.sub.2 Ph3139 pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 Ph3140 pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.4 -(4-CH.sub.3)3141 pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.3 -(2,6-CH.sub.3).sub.23142 pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.2 -(2,4,6-CH.sub.3).sub.3 579.43143 pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 (3-pyridyl)3144 pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 (2-thienyl)3145 pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 (2-thiazolyl)3146 pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.4 -(4-Br)3147 pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.4 -(4-F)3148 pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.3 -(2,6-Cl.sub.2)3149 pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 (2-naphthyl)3150 pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 (1-naphthyl)3151 pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.4 -(4-Ph)3151a pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.4 -4-(4-pyridyl)3151b pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.4 -4-(2-oxazolyl)3151c pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.4 -4-(3-pyrazolyl)3152 pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.2 -(4-Ph-2,6-dimethyl)3152a pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.2 -4-(3-pyridyl)-2,6-dimethyl3152b pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.2 -4-(2-oxazolyl)-2,6-dimethyl3152c pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.2 -4-(3-pyrazolyl)-2,6-dimethyl3152d pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.2 -4-(4-pyridyl)-2,6-dimethyl3152e pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.2 -4-(2-furyl)-2,6-dimethyl3152f pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.2 -4-(3-furyl)-2,6-dimethyl3153 pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.2 -(4-Ph-2,6-dichloro)3154 pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 CH.sub.2 Ph3155 pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 -n-Bu3156 pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NHPh3157 pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NHC.sub.6 H.sub.4 -(4-CH.sub.3)3158 pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NHC.sub.6 C.sub.3 -(2,6-Me.sub.2)3159 pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NHC.sub.6 C.sub.2 -(2,4,6-Me.sub.3)3160 pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NH(3-pyridyl)3161 pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 -�4-(3,5-dimethyl)iso xazolyl!3162 pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NHC.sub.6 H.sub.4 -(4-Br)3163 pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NHC.sub.6 H.sub.4 -(4-F)3164 pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NH(2-naphthyl)3165 pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NH)1-naphthyl)3166 pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NHC.sub.6 H.sub.4 -(4-Ph)3167 pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NHC.sub.6 H.sub.2 -(4-Ph-2,6-dimethyl)3168 pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NHC.sub.6 H.sub.2 -(4-Ph-2,6-dichloro)3169 pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NHCH.sub.2 Ph3170 pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NH-n-Bu3171 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHCOOCH.sub.2 Ph3172 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHCO.sub.2 CH.sub.2 C.sub.6 H.sub.4 -(4-CH.sub.3)3173 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHCO.sub.2 CH.sub.2 (3-pyridinyl )3173 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHCO.sub.2 CH.sub.2 (2-thiazolyl )3175 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHCO.sub.2 CH.sub.2 (2-thienyl)3176 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHCO.sub.2 n-Bu3177 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 Ph3178 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.4 -(4-CH.sub.3)3179 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.3 -(2,6-Me.sub.2)3180 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.2 -(2,4,6-Me.sub.3)3181 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 (3-pyridyl)3182 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 (2-thienyl)3183 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 (2-thiazolyl)3184 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.4 -(2-Br)3185 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.4 -(4-F)3186 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.3 -(2,6-Cl.sub.2)3187 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 (2-naphthyl)3188 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 (1-naphthyl)3189 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.4 -(4-Ph)3189a tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.4 -4-(4-pyridyl)3189b tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.4 -4-(2-oxazolyl)3189c tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.4 -4-(3-pyrazolyl)3190 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.2 -(4-Ph-2,6-dimethyl)3190a tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.2 -4-(3-pyridyl)-2,6-dimethyl3190b tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.2 -4-(2-oxazolyl)-2,6-dimethyl3190c tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.2 -4-(3-pyrazolyl)-2,6-dimethyl3190d tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.2 -4-(4-pyridyl)-2,6-dimethyl3190e tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.2 -4-(2-furyl)-2,6-dimethyl3190f tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.2 -4-(3-furyl)-2,6-dimethyl3191 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.2 -(4-Ph-2,6-dichloro)3192 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 CH.sub.2 Ph3193 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 -n-Bu3194 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NHPh3195 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NHC.sub.6 H.sub.4 -(4-CH.sub.3)3196 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NHC.sub.6 C.sub.3 -(2,6-Me.sub.2)3197 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NHC.sub.6 C.sub.2 -(2,4,6-Me.sub.3)3198 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 �4-(3,5-dimethyl)isox azolyl!3199 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NH(2-naphthyl)3200 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NH(1-naphthyl)3201 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NHC.sub.6 H.sub.4 -(4-Ph)3202 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NHC.sub.6 H.sub.2 -(4-Ph-2,6-dimethyl)3203 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NHC.sub.6 H.sub.2 -(4-Ph-2,6-dichloro)3204 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NHCH.sub.2 Ph3205 imidazolin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHCO.sub.2 CH.sub.2 C.sub.6 H.sub.4 -(4-CH.sub.3)3206 imidazolin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHCO.sub.2 CH.sub.2 (3-pyridinyl )3207 imidazolin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHCO.sub.2 CH.sub.2 (2-thiazolyl )3208 imidazolin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHCO.sub.2 CH.sub.2 (2-thienyl)3209 imidazolin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHCO.sub.2 i-Bu3210 imidazolin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 Ph3211 imidazolin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.4 -(3-CH.sub.3)3212 imidazolin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.3 -(2,6-Me.sub.2)3213 imidazolin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.2 -(2,4,6-Me.sub.3)3214 imidazolin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 (3-pyridyl)3215 imidazolin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 (2-thienyl)3216 imidazolin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 (2-thiazolyl)3217 imidazolin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 -�4-(3,5-dimethyl)iso xazolyl!3218 imidazolin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.4 -(3-Br)3218a imidazolin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.4 -(4-F)3219 imidazolin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.3 -(2,6-Cl.sub.2)3220 imidazolin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 (2-naphthyl)3221 imidazolin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 (1-naphthyl)3222 imidazolin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.4 -(4-Ph)3222a imidazolin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.4 -4-(4-pyridyl)3222b imidazolin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.4 -4-(2-oxazolyl)3222c imidazolin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.4 -4-(3-pyrazolyl)3223 imidazolin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.2 -(4-Ph-2,6-dimethyl)3223a imidazolin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.2 -4-(3-pyridyl)-2,6-dimethyl3223b imidazolin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.2 -4-(2-oxazolyl)-2,6-dimethyl3223c imidazolin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.2 -4-(3-pyrazolyl)-2,6-dimethyl3223d imidazolin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.2 -4-(4-pyridyl)-2,6-dimethyl3223e imidazolin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.2 -4-(2-furyl)-2,6-dimethyl3223f imidazolin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.2 -4-(3-furyl)-2,6-dimethyl3224 imidazolin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.2 -(4-Ph-2,6-dichloro)3225 imidazolin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 CH.sub.2 Ph3226 imidazolin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 -n-Bu3227 imidazolin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NHPh3228 imidazolin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NHC.sub.6 H.sub.4 -(4-CH.sub.3)3229 imidazolin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NHC.sub.6 C.sub.3 -(2,6-Me.sub.2)3230 imidazolin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NHC.sub.6 C.sub.2 -(2,4,6-Me.sub.3)3231 imidazolin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NH(2-naphthyl)3232 imidazolin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NH)1-naphthyl)3233 imidazolin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NHC.sub.6 H.sub.4 -(4-Ph)3234 imidazolin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NHC.sub.6 H.sub.2 -(4-Ph-2,6-dimethyl)3235 imidazolin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NHC.sub.6 H.sub.2 -(4-Ph-2,6-dichloro)3236 imidazolin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NHCH.sub.2 Ph3237 benzimidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 Ph3238 benzimidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.4 -(3-CH.sub.3)3239 benzimidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.3 -(2,6-Me.sub.2)3240 benzimidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.2 -(2,4,6-Me.sub.3)3241 benzimidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 (4-pyridyl)3242 benzimidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 (2-thienyl)3243 benzimidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 (2-thiazolyl)3244 benzimidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 -�4-(3,5-dimethyl)iso xazolyl!3245 benzimidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.4 -(3-Br)3246 benzimidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.4 -(3-F)3247 benzimidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.3 -(2,6-Cl.sub.2)3248 benzimidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 (2-naphthyl)3249 benzimidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 (1-naphthyl)3250 benzimidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.4 -(4-Ph)3251 benzimidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.2 -(4-Ph-2,6-dimethyl)3252 benzimidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.2 -(4-Ph-2,6-dichloro)3253 benzimidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 CH.sub.2 Ph3254 benzimidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 -i-Bu3255 benzimidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NHPh3256 benzimidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NHC.sub.6 H.sub.4 -(4-CH.sub.3)3257 benzimidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NHC.sub.6 C.sub.3 -(2,6-Me.sub.2)3258 benzimidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NHC.sub.6 C.sub.2 -(2,4,6-Me.sub.3)3259 benzimidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NH(2-naphthyl)3260 benzimidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NH)1-naphthyl)3261 benzimidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NHC.sub.6 H.sub.4 -(4-Ph)3262 benzimidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NHC.sub.6 H.sub.2 -(4-Ph-2,6-dimethyl)3263 benzimidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NHC.sub.6 H.sub.2 -(4-Ph-2,6-dichloro)3264 benzimidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NHCH.sub.2 Ph3265 benzimidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHCO.sub.2 CH.sub.2 Ph3266 benzimidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHCO.sub.2 i-Bu3267 2-aminopyridin-6-yl-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.4 -(4-CH.sub.3)3268 2-aminopyridin-6-yl-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.3 -(2,6-Me.sub.2)3269 2-aminopyridin-6-yl-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.2 -(2,4,6-Me.sub.3)3270 2-aminopyridin-6-yl-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 (3-pyridyl)3271 2-aminopyridin-6-yl-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 (2-thiazolyl)3272 2-aminopyridin-6-yl-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 (4-isoxazolyl)3273 2-aminopyridin-6-yl-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.4 -(3-Br)3274 2-aminopyridin-6-yl-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.4 -(3-F)3275 2-aminopyridin-6-yl-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.3 -(2,6-Cl.sub.2)3276 2-aminopyridin-6-yl-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 (2-naphthyl)3277 2-aminopyridin-6-yl-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 (1-naphthyl)3278 2-aminopyridin-6-yl-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.4 -(4-Ph)3279 2-aminopyridin-6-yl-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.2 -(4-Ph-2,6-dimethyl)3280 2-aminopyridin-6-yl-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.2 -(4-Ph-2,6-dichloro)3281 2-aminopyridin-6-yl-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 CH.sub.2 Ph3282 2-aminopyridin-6-yl-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 -i-Bu3283 2-aminopyridin-6-yl-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NHPh3284 2-aminopyridin-6-yl-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NHC.sub.6 H.sub.4 -(4-CH.sub.3)3285 2-aminopyridin-6-yl-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NHC.sub.6 C.sub.3 -(2,6-Me.sub.2)3286 2-aminopyridin-6-yl-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NHC.sub.6 C.sub.2 -(2,4,6-Me.sub.3)3287 2-aminopyridin-6-yl-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NH(2-naphthyl)3288 2-aminopyridin-6-yl-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NH)1-naphthyl)3289 2-aminopyridin-6-yl-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NHC.sub.6 H.sub.4 -(4-Ph)3290 2-aminopyridin-6-yl-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NHC.sub.6 H.sub.2 -(4-Ph-2,6-dimethyl)3291 2-aminopyridin-6-yl-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NHC.sub.6 H.sub.2 -(4-Ph-2,6-dichloro)3292 2-aminopyridin-6-yl-(CH.sub.2).sub.3 CH.sub.3 H NHCO.sub.2 n-Bu3293 2-aminopyridin-6-yl-(CH.sub.2).sub.3 CH.sub.3 H NHCO.sub.2 i-Bu3294 2-iminoazepin-7-yl-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 Ph3295 imidazol-4-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 Ph3296 2-iminoazepin-7-yl-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 (4-isoxazolyl)3297 imidazol-4-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 (4-isoxazolyl)3298 2-iminoazepin-7-yl-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 -�4-(3,5-dimethyl)iso xazolyl!3299 imidazol-4-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 -�4-(3,5-dimethyl)iso xazolyl!3300 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 3-pyridinyl NHSO.sub.2 Ph3301 pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 3-pyridinyl NHSO.sub.2 Ph3302 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 (3,4-methylenedioxy)phenyl NHSO.sub.2 Ph3303 pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 (3,4-methylenedioxy)phenyl NHSO.sub.2 Ph3304 imidazol-2-ylamino-(CH.sub.2).sub.2 CH.sub.3 H NHSO.sub.2 Ph3305 imidazol-2-ylamino-(CH.sub.2).sub.2 CH.sub.3 H NHCO.sub.2 CH.sub.2 Ph3306 imidazol-2-ylamino-carbonyl-(CH.sub.2).sub.2 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.2 -(2,4,6-CH.sub.3).sub.33307 pyridin-2-ylamino-(CH.sub.2).sub.2 CH.sub.3 H NHSO.sub.2 Ph3308 pyridin-2-ylamino-(CH.sub.2).sub.2 CH.sub.3 H NHCO.sub.2 CH.sub.2 Ph3309 pyridin-2-ylamino-carbonyl-(CH.sub.2).sub.2 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.2 -(2,4,6-CH.sub.3).sub.33310 imidazolin-2-ylamino-(CH.sub.2).sub.2 CH.sub.3 H NHSO.sub.2 Ph3311 imidazolin-2-ylamino-(CH.sub.2).sub.2 CH.sub.3 H NHCO.sub.2 CH.sub.2 Ph3312 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.2 CH.sub.3 H NHSO.sub.2 Ph3313 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.2 CH.sub.3 H NHCO.sub.2 CH.sub.2 Ph3314 benzimidazol-2-ylamino-(CH.sub.2).sub.2 CH.sub.3 H NHSO.sub.2 Ph3315 benzimidazol-2-ylamino-(CH.sub.2).sub.2 CH.sub.3 H NHCO.sub.2 CH.sub.2 Ph3316 benzimidazol-2-ylamino-carbonyl-(CH.sub.2).sub.2 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.2 -(2,4,6-CH.sub.3).sub.33317 2-aminopyridin-6-yl-(CH.sub.2).sub.2 CH.sub.3 H NHSO.sub.2 Ph3318 2-aminopyridin-6-yl-(CH.sub.2).sub.2 CH.sub.3 H NHCO.sub.2 CH.sub.2 Ph3319 2-iminoazepin-7-yl-(CH.sub.2).sub.2 CH.sub.3 H NHSO.sub.2 Ph3320 2-iminoazepin-7-yl-(CH.sub.2).sub.2 CH.sub.3 H NHCO.sub.2 CH.sub.2 Ph3321 imidazol-4-ylamino-(CH.sub.2).sub.2 CH.sub.3 H NHSO.sub.2 Ph3322 imidazol-4-ylamino-(CH.sub.2).sub.2 CH.sub.3 H NHCO.sub.2 CH.sub.2 Ph3323 imidazol-2-ylamino-(CH.sub.2).sub.4 CH.sub.3 H NHSO.sub.2 Ph3324 imidazol-2-ylamino-(CH.sub.2).sub.4 CH.sub.3 H NHCO.sub.2 CH.sub.2 Ph3325 pyridin-2-ylamino-(CH.sub.2).sub.4 CH.sub.3 H NHSO.sub.2 Ph3326 pyridin-2-ylamino-(CH.sub.2).sub.4 CH.sub.3 H NHCO.sub.2 CH.sub.2 Ph3327 imidazolin-2-ylamino-(CH.sub.2).sub.4 CH.sub.3 H NHSO.sub.2 Ph3328 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.4 CH.sub.3 H NHSO.sub.2 Ph3329 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.4 CH.sub.3 H NHCO.sub.2 CH.sub.2 Ph3330 benzimidazol-2-ylamino-(CH.sub.2).sub.4 CH.sub.3 H NHSO.sub.2 Ph3331 benzimidazol-2-ylamino-(CH.sub.2).sub.4 CH.sub.3 H NHCO.sub.2 CH.sub.2 Ph3332 2-aminopyridin-6-yl-(CH.sub.2).sub.4 CH.sub.3 H NHSO.sub.2 Ph3333 2-aminopyridin-6-yl-(CH.sub.2).sub.4 CH.sub.3 H NHCO.sub.2 CH.sub.2 Ph3334 2-iminoazepin-7-yl-(CH.sub.2).sub.4 CH.sub.3 H NHSO.sub.2 Ph3335 2-iminoazepin-7-yl-(CH.sub.2).sub.4 CH.sub.3 H NHCO.sub.2 CH.sub.2 Ph3336 imidazol-4-ylamino-(CH.sub.2).sub.4 CH.sub.3 H NHSO.sub.2 Ph3337 imidazol-4-ylamino-(CH.sub.2).sub.4 CH.sub.3 H NHCO.sub.2 CH.sub.2 Ph3338 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.2 Ph H NHSO.sub.2 C.sub.6 H.sub.2 -(2,4,6-CH.sub.3).sub.33339 pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.2 Ph H NHSO.sub.2 C.sub.6 H.sub.2 -(2,4,6-CH.sub.3).sub.33340 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.2 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.2 -(2,4,6-CH.sub.3).sub.33341 imidazol-2-ylamino-(CH.sub.2).sub.3 CH(CH.sub.3).sub.2 H NHSO.sub.2 C.sub.6 H.sub.2 -(2,4,6-CH.sub.3).sub.33342 imidazol-2-ylamino-(CH.sub.2).sub.3 cyclopropyl H NHSO.sub.2 C.sub.6 H.sub.2 -(2,4,6-CH.sub.3).sub.33343 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.2 - H NHSO.sub.2 C.sub.6 H.sub.2 -(2,4,6-CH.sub.3).sub.3 cyclopropyl3344 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.2 COOH H NHSO.sub.2 C.sub.6 H.sub.2 -(2,4,6-CH.sub.3).sub.33345 imidazol-2-ylamino-(CH.sub.2).sub.3 (CH.sub.2).sub.2 NMe.sub.2 H NHSO.sub.2 C.sub.6 H.sub.2 -(2,4,6-CH.sub.3).sub.33346 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.2 CH.sub.2 OMe H NHSO.sub.2 C.sub.6 H.sub.2 -(2,4,6-CH.sub.3).sub.33347 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.2 CH.sub.2 Ph H NHSO.sub.2 C.sub.6 H.sub.2 -(2,4,6-CH.sub.3).sub.33348 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.2 CH.sub.2 OH H NHSO.sub.2 C.sub.6 H.sub.2 -(2,4,6-CH.sub.3).sub.33349 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.2 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.2 -(2,6-CH.sub.3).sub.2 -4-Ph3350 imidazol-2-ylamino-(CH.sub.2).sub.3 CH(CH.sub.3).sub.2 H NHSO.sub.2 C.sub.6 H.sub.2 -(2,6-CH.sub.3).sub.2 -4-Ph3351 imidazol-2-ylamino-(CH.sub.2).sub.3 cyclopropyl H NHSO.sub.2 C.sub.6 H.sub.2 -(2,6-CH.sub.3).sub.2 -4-Ph3352 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.2 - H NHSO.sub.2 C.sub.6 H.sub.2 -(2,6-CH.sub.3).sub.2 -4-Ph cyclopropyl3353 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.2 COOH H NHSO.sub.2 C.sub.6 H.sub.2 -(2,6-CH.sub.3).sub.2 -4-Ph3354 imidazol-2-ylamino-(CH.sub.2).sub.3 (CH.sub.2).sub.2 NMe.sub.2 H NHSO.sub.2 C.sub.6 H.sub.2 -(2,6-CH.sub.3).sub.2 -4-Ph3355 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.2 CH.sub.2 OMe H NHSO.sub.2 C.sub.6 H.sub.2 -(2,6-CH.sub.3).sub.2 -4-Ph3356 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.2 CH.sub.2 Ph H NHSO.sub.2 C.sub.6 H.sub.2 -(2,6-CH.sub.3).sub.2 -4-Ph3357 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.2 CH.sub.2 OH H NHSO.sub.2 C.sub.6 H.sub.2 -(2,6-CH.sub.3).sub.2 -4-Ph3358 imidazol-2-ylamino-CH.sub.2 (o-C.sub.6 H.sub.4) CH.sub.3 H NHSO.sub.2 -(1-naphthyl)3359 imidazol-2-ylamino-CH.sub.2 (o-C.sub.6 H.sub.4) CH.sub.3 H NHCO.sub.2 CH.sub.2 Ph3360 imidazol-2-ylamino-CH.sub.2 (o-C.sub.6 H.sub.4) CH.sub.3 H NHSO.sub.2 C.sub.6 C.sub.2 -(2,4,6-Me.sub.3)3361 pyridin-2-ylamino-CH.sub.2 (o-C.sub.6 H.sub.4) CH.sub.3 H NHSO.sub.2 -(1-naphthyl)3362 pyridin-2-ylamino-CH.sub.2 (o-C.sub.6 H.sub.4) CH.sub.3 H NHCO.sub.2 CH.sub.2 Ph3363 pyridin-2-ylamino-CH.sub.2 (o-C.sub.6 H.sub.4) CH.sub.3 H NHSO.sub.2 C.sub.6 C.sub.2 -(2,4,6-Me.sub.3)3364 imidazolin-2-ylamino-CH.sub.2 (o-C.sub.6 H.sub.4) CH.sub.3 H NHSO.sub.2 -(1-naphthyl)3365 imidazolin-2-ylamino-CH.sub.2 (o-C.sub.6 H.sub.4) CH.sub.3 H NHCO.sub.2 CH.sub.2 Ph3366 imidazolin-2-ylamino-CH.sub.2 (o-C.sub.6 H.sub.4) CH.sub.3 H NHSO.sub.2 C.sub.6 C.sub.2 -(2,4,6-Me.sub.3)3367 imidazolin-2-ylamino-(m-C.sub.6 H.sub.4) CH.sub.3 H NHSO.sub.2 -(1-naphthyl)3368 imidazolin-2-ylamino-(m-C.sub.6 H.sub.4) CH.sub.3 H NHCO.sub.2 CH.sub.2 Ph3369 imidazolin-2-ylamino-(m-C.sub.6 H.sub.4) CH.sub.3 H NHSO.sub.2 C.sub.6 C.sub.2 -(2,4,6-Me.sub.3)__________________________________________________________________________ TABLE 4__________________________________________________________________________ ##STR62##Ex. No. R.sup.1 R.sup.9 R.sup.14 R.sup.15 MS__________________________________________________________________________4001 imidazol-2-ylamino-(CH.sub.2).sub.3 H H H4002 pyridin-2-ylamino-(CH.sub.2).sub.3 H H NHCOOCH.sub.2 Ph4002a imidazolin-2-ylamino-(CH.sub.2).sub.3 H H NHCOOCH.sub.2 Ph4002b tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H H NHCO.sub.2 CH.sub.2 Ph4002c imidazol-2-ylamino-(CH.sub.2).sub.3 H H NHCO.sub.2 CH.sub.2 Ph4003 imidazolin-2-ylamino-(CH.sub.2).sub.3 H H NHCO.sub.2 CH.sub.2 C.sub.6 H.sub.4 -(2-CH.sub.3)4004 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H H NHCO.sub.2 CH.sub.2 C.sub.6 H.sub.4 -(3-CH.sub.3)4005 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H H NHCO.sub.2 CH.sub.2 C.sub.6 H.sub.4 -(4-CH.sub.3)4006 2-aminopyridin-6-yl-(CH.sub.2).sub.3 H H NHCO.sub.2 CH.sub.2 (2-pyridinyl )4007 2-iminoazepin-7-yl-(CH.sub.2).sub.3 H H NHCO.sub.2 CH.sub.3 (3-pyridinyl )4010 imidazol-4-ylamino-(CH.sub.2).sub.3 H H NHCO.sub.2 CH.sub.2 (2-thiazolyl )4015 imidazol-2-ylamino-(CH.sub.2).sub.3 H H NHCO.sub.2 CH.sub.2 (4-isoxazoly l)4016 pyridin-2-ylamino-(CH.sub.2).sub.3 H H NHCO.sub.2 CH.sub.2 (2-thienyl)4017 imidazolin-2-ylamino-(CH.sub.2).sub.3 H H NHCO.sub.2 n-Bu4018 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H H NHCO.sub.2 i-Bu4019 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H H NHCO.sub.2 t-Bu4020 2-aminopyridin-6-yl-(CH.sub.2).sub.3 H H NHSO.sub.2 Ph4020a pyridin-2-ylamino-(CH.sub.2).sub.3 H H NHSO.sub.2 Ph4020b imidazolin-2-ylamino-(CH.sub.2).sub.3 H H NHSO.sub.2 Ph4020c tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H H NHSO.sub.2 Ph4020d imidazol-2-ylamino-(CH.sub.2).sub.3 H H NHSO.sub.2 Ph4021 2-iminoazepin-7-yl-(CH.sub.2).sub.3 H H NHSO.sub.2 C.sub.6 H.sub.4 -(2-CH.sub.3)4021a imidazol-2-ylamino-(CH.sub.2).sub.3 H H NHSO.sub.2 C.sub.6 H.sub.3 -(2,6-Me.sub.2)4021b imidazol-2-ylamino-(CH.sub.2).sub.3 H H NHSO.sub.2 C.sub.6 H.sub.2 -(2,4,6-Me.sub.3)4021c imidazol-2-ylamino-(CH.sub.2).sub.3 H H NHSO.sub.2 C.sub.6 H.sub.2 -(2,6-Me.sub.2 -4-Ph)4021d pyridin-2-ylamino-(CH.sub.2).sub.3 H H NHSO.sub.2 C.sub.6 H.sub.2 -(2,6-Me.sub.2 -4-Ph)4021e imidazolin-2-ylamino-(CH.sub.2).sub.3 H H NHSO.sub.2 C.sub.6 H.sub.2 -(2,6-Me.sub.2 -4-Ph)4021f tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H H NHSO.sub.2 C.sub.6 H.sub.2 -(2,6-Me.sub.2 -4-Ph)4024 imidazol-4-ylamino-(CH.sub.2).sub.3 H H NHSO.sub.2 (2-pyridyl)4029 imidazol-2-ylamino-(CH.sub.2).sub.3 H H NHSO.sub.2 (4-isoxazolyl)4030 pyridin-2-ylamino-(CH.sub.2).sub.3 H H NHSO.sub.2 -�4-(3,5-dimethyl)iso xazolyl!4030a imidazolin-2-ylamino-(CH.sub.2).sub.3 H H NHSO.sub.2 -�4-(3,5-dimethyl)iso xazolyl!4030b tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H H NHSO.sub.2 -�4-(3,5-dimethyl)iso xazolyl!4030c imidazol-2-ylamino-(CH.sub.2).sub.3 H H NHSO.sub.2 -�4-(3,5-dimethyl)iso xazolyl!4031 imidazolin-2-ylamino-(CH.sub.2).sub.3 H H NHSO.sub.2 C.sub.6 H.sub.4 -(2-Br)4032 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H H NHSO.sub.2 C.sub.6 H.sub.4 -(3-Br)4033 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H H NHSO.sub.2 C.sub.6 H.sub.4 -(4-Br)4034 2-aminopyridin-6-yl-(CH.sub.2).sub.3 H H NHSO.sub.2 C.sub.6 H.sub.4 -(2-F)4035 2-iminoazepin-7-yl-(CH.sub.2).sub.3 H H NHSO.sub.2 C.sub.6 H.sub.4 -(3-F)4038 imidazol-2-ylamino-(CH.sub.2).sub.3 H H NHSO.sub.2 (1-naphthyl)4038a imidazol-2-ylamino-(CH.sub.2).sub.3 H H NHSO.sub.2 C.sub.6 H.sub.3 -(2,6-Cl.sub.2)4038b imidazol-2-ylamino-(CH.sub.2).sub.3 H H NHSO.sub.2 C.sub.6 H.sub.2 -(2,6-Cl.sub.2 -4-Ph)4043 imidazol-2-ylamino-(CH.sub.2).sub.3 H H NHSO.sub.2 -i-Bu4044 pyridin-2-ylamino-(CH.sub.2).sub.3 H H NHSO.sub.2 -t-Bu4045 imidazol-2-ylamino-(CH.sub.2).sub.3 H (3,4-methylenedioxy)phenyl H4046 pyridin-2-ylamino-(CH.sub.2).sub.3 H (3,4-methylenedioxy)phenyl H4047 imidazolin-2-ylamino-(CH.sub.2).sub.3 H (3,4-methylenedioxy)phenyl H4048 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H (3,4-methylenedioxy)phenyl H4049 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H (3,4-methylenedioxy)phenyl H4050 2-aminopyridin-6-yl-(CH.sub.2).sub.3 H (3,4-methylenedioxy)phenyl H4051 2-iminoazepin-7-yl-(CH.sub.2).sub.3 H (3,4-methylenedioxy)phenyl H4054 imidazol-4-ylamino-(CH.sub.2).sub.3 H (3,4-methylenedioxy)phenyl H4059 imidazol-2-ylamino-(CH.sub.2).sub.3 H 3-pyridinyl H4060 pyridin-2-ylamino-(CH.sub.2).sub.3 H 3-pyridinyl H4061 imidazolin-2-ylamino-(CH.sub.2).sub.3 H 3-pyridinyl H4062 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H 3-pyridinyl H4063 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H 3-pyridinyl H4064 2-aminopyridin-6-yl-(CH.sub.2).sub.3 H 3-pyridinyl H4065 2-iminoazepin-7-yl-(CH.sub.2).sub.3 H 3-pyridinyl H4068 imidazol-4-ylamino-(CH.sub.2).sub.3 H 3-pyridinyl H4068a imidazol-2-ylamino-CH.sub.2 (o-C.sub.6 H.sub.4) H H NHSO.sub.2 -(1-naphthyl)4068b imidazol-2-ylamino-CH.sub.2 (o-C.sub.6 H.sub.4) H H NHCO.sub.2 CH.sub.2 Ph4068c imidazol-2-ylamino-CH.sub.2 (o-C.sub.6 H.sub.4) H H NHSO.sub.2 C.sub.6 C.sub.2 -(2,4,6-Me.sub.3)4068d pyridin-2-ylamino-CH.sub.2 (o-C.sub.6 H.sub.4) H H NHSO.sub.2 -(1-naphthyl)4068e pyridin-2-ylamino-CH.sub.2 (o-C.sub.6 H.sub.4) H H NHCO.sub.2 CH.sub.2 Ph4068f pyridin-2-ylamino-CH.sub.2 (o-C.sub.6 H.sub.4) H H NHSO.sub.2 C.sub.6 C.sub.2 -(2,4,6-Me.sub.3)4068g imidazolin-2-ylamino-CH.sub.2 (o-C.sub.6 H.sub.4) H H NHSO.sub.2 -(1-naphthyl)4068h imidazolin-2-ylamino-CH.sub.2 (o-C.sub.6 H.sub.4) H H NHCO.sub.2 CH.sub.2 Ph4068i imidazolin-2-ylamino-CH.sub.2 (o-C.sub.6 H.sub.4) H H NHSO.sub.2 C.sub.6 C.sub.2 -(2,4,6-Me.sub.3)4068j imidazolin-2-ylamino-(m-C.sub.6 H.sub.4) H H NHSO.sub.2 -(1-naphthyl)4068k imidazolin-2-ylamino-(m-C.sub.6 H.sub.4) H H NHCO.sub.2 CH.sub.2 Ph4068l imidazolin-2-ylamino-(m-C.sub.6 H.sub.4) H H NHSO.sub.2 C.sub.6 C.sub.2 -(2,4,6-Me.sub.3)4075 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHCO.sub.2 CH.sub.2 Ph4076 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHCO.sub.2 CH.sub.2 C.sub.6 H.sub.4 -(3-CH.sub.3)4077 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHCO.sub.2 CH.sub.2 (3-pyridinyl )4078 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHCO.sub.2 CH.sub.2 (2-thiazolyl )4079 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHCO.sub.2 CH.sub.2 (2-thienyl) O4080 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHCO.sub.2 CH.sub.2 (5-isoxazoly l)4081 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHCO.sub.2 n-Bu4082 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHCOPh4083 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHCOCH.sub.2 Ph4084 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHCOCH.sub.2 CH.sub.2 Ph4085 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHCOCH.dbd.CHPh4086 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHCOCH.sub.2 (3-pyridinyl)4087 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHCOCH.sub.2 (2-thienyl)4088 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHCOCH.sub.2 (cyclohexyl)4089 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHCOn-Bu4090 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHCONHCH.sub.2 Ph4091 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 Ph4092 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.4 -(4-CH.sub.3)4093 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.3 -(2,6-CH.sub.3).sub.24094 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.2 -(2,4,6-CH.sub.3).sub.34095 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 (3-pyridyl)4096 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 (2-thienyl)4097 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 (2-thiazolyl)4098 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 �4-(3,5-dimethyl)isox azolyl!4099 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.4 -(4-Br)4100 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.4 -(4-F)4101 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.3 -(2,6-Cl.sub.2)4102 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 (2-naphthyl)4103 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 (1-naphthyl)4104 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.4 -(4-Ph)4104a imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.4 -4-(4-pyridyl)4104b imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.4 -4-(2-oxazolyl)4104c imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.4 -4-(3-pyrazolyl)4105 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.2 -(4-Ph-2,6-dimethyl)4105a imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.2 -4-(3-pyridyl)-2,6-dimethyl4105b imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.2 -4-(2-oxazolyl)-2,6-dimethyl4105c imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.2 -4-(3-pyrazolyl)-2,6-dimethyl4106 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.2 -(4-Ph-2,6-dichloro)4107 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H-(4-Ph-2,6-d imethyl-3-chloro)4108 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 CH.sub.2 Ph4109 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 -n-Bu4110 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NHPh4111 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NHC.sub.6 H.sub.4 -(4-CH.sub.3)4112 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NHC.sub.6 C.sub.3 -(2,6-Me.sub.2)4113 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NHC.sub.6 C.sub.2 -(2,4,6-Me.sub.3)4114 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NH(3-pyridyl)4115 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 �4-(3,5-dimethyl)isox azolyl!4116 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NHC.sub.6 H.sub.4 -(4-Br)4117 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NHC.sub.6 H.sub.4 -(4-F)4118 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NH(2-naphthyl)4119 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NH(1-naphthyl)4120 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NHC.sub.6 H.sub.4 -(4-Ph)4121 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NHC.sub.6 H.sub.2 -(4-Ph-2,6-dimethyl)4122 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NHC.sub.6 H.sub.2 -(4-Ph-2,6-dichloro)4123 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NHCH.sub.2 Ph4124 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NH-n-Bu4125 pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHCO.sub.2 CH.sub.2 C.sub.6 H.sub.4 -(3-CH.sub.3)4126 pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHCO.sub.2 CH.sub.2 (3-pyridinyl )4127 pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHCO.sub.2 CH.sub.2 (2-thiazolyl )4128 pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHCO.sub.2 CH.sub.2 (4-isoxazoly l)4129 pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHCO.sub.2 i-Bu4130 pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHCOPh4131 pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHCOCH.sub.2 Ph4132 pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHCOCH.sub.2 CH.sub.2 Ph4133 pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHCOCH.dbd.CHPh4134 pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHCOCH.sub.2 (3-pyridinyl)4135 pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHCOCH.sub.2 (2-thienyl)4136 pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHCOCH.sub.2 (cyclohexyl)4137 pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHCOn-Bu4138 pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHCONHCH.sub.2 Ph4139 pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 Ph4140 pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.4 -(4-CH.sub.3)4141 pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.3 -(2,6-CH.sub.3).sub.24142 pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.2 -(2,4,6-CH.sub.3).sub.34143 pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 (3-pyridyl)4144 pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 (2-thienyl)4145 pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 (2-thiazolyl)4146 pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.4 -(4-Br)4147 pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.4 -(4-F)4148 pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.3 -(2,6-Cl.sub.2)4149 pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 (2-naphthyl)4150 pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 (1-naphthyl)4151 pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.4 -(4-Ph)4151a pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.4 -4-(4-pyridyl)4151b pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.4 -4-(2-oxazolyl)4151c pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.4 -4-(3-pyrazolyl)4152 pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.2 -(4-Ph-2,6-dimethyl)4152a pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.2 -4-(3-pyridyl)-2,6-dimethyl4152b pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.2 -4-(2-oxazolyl)-2,6-dimethyl4152c pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.2 -4-(3-pyrazolyl)-2,6-dimethyl4153 pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.2 -(4-Ph-2,6-dichloro)4154 pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 CH.sub.2 Ph4155 pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 -n-Bu4156 pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NHPh4157 pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NHC.sub.6 H.sub.4 -(4-CH.sub.3)4158 pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NHC.sub.6 C.sub.3 -(2,6-Me.sub.2)4159 pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NHC.sub.6 C.sub.2 -(2,4,6-Me.sub.3)4160 pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NH(3-pyridyl)4161 pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 -�4-(3,5-dimethyl)iso xazolyl!4162 pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NHC.sub.6 H.sub.4 -(4-Br)4163 pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NHC.sub.6 H.sub.4 -(4-F)4164 pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NH(2-naphthyl)4165 pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NH)1-naphthyl)4166 pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NHC.sub.6 H.sub.4 -(4-Ph)4167 pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NHC.sub.6 H.sub.2 -(4-Ph-2,6-dimethyl)4168 pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NHC.sub.6 H.sub.2 -(4-Ph-2,6-dichloro)4169 pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NHCH.sub.2 Ph4170 pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NH-n-Bu4171 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHCOOCH.sub.2 Ph4172 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHCO.sub.2 CH.sub.2 C.sub.6 H.sub.4 -(4-CH.sub.3)4173 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHCO.sub.2 CH.sub.3 (3-pyridinyl )4173 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHCO.sub.2 CH.sub.2 (2-thiazolyl )4175 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHCO.sub.2 CH.sub.2 (2-thienyl) O4176 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHCO.sub.2 n-Bu4177 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 Ph4178 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.4 -(4-CH.sub.3)4179 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.3 -(2,6-Me.sub.2)4180 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.2 -(2,4,6-Me.sub.3)4181 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 (3-pyridyl)4182 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 (2-thienyl)4183 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 (2-thiazolyl)4184 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.4 -(2-Br)4185 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.4 -(4-F)4186 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.3 -(2,6-Cl.sub.2)4187 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 (2-naphthyl)4188 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 (1-naphthyl)4189 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.4 -(4-Ph)4189a tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.4 -4-(4-pyridyl)4189b tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.4 -4-(2-oxazolyl)4189c tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.4 -4-(3-pyrazolyl)4190 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.2 -(4-Ph-2-6-dimethyl)4190a tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.2 -4-(3-pyridyl)-2,6-dimethyl4190b tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.2 -4-(2-oxazolyl)-2,6-dimethyl4190c tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.2 -4-(3-pyrazolyl)-2,6-dimethyl4191 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.2 -(4-Ph-2,6-dichloro)4192 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 CH.sub.2 Ph4193 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 -n-Bu4194 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NHPh4195 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NHC.sub.6 H.sub.4 -(4-CH.sub.3)4196 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NHC.sub.6 C.sub.3 -(2,6-Me.sub.2)4197 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NHC.sub.6 C.sub.2 -(2,4,6-Me.sub.3)4198 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 �4-(3,5-dimethyl)isox azolyl!4199 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NH(2-naphthyl)4200 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NH(1-naphthyl)4201 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NHC.sub.6 H.sub.4 -(4-Ph)4202 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NHC.sub.6 H.sub.2 -(4-Ph-2,6-dimethyl)4203 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NHC.sub.6 H.sub.2 -(4-Ph-2,6-dichloro)4204 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NHCH.sub.2 Ph4205 imidazolin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHCO.sub.2 CH.sub.2 C.sub.6 H.sub.4 -(4-CH.sub.3)4206 imidazolin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHCO.sub.2 CH.sub.2 (3-pyridinyl )4207 imidazolin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHCO.sub.2 CH.sub.2 (2-thiazolyl )4208 imidazolin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHCO.sub.2 CH.sub.2 (2-thienyl)4209 imidazolin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHCO.sub.2 i-Bu4210 imidazolin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 Ph4211 imidazolin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.4 -(3-CH.sub.3)4212 imidazolin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.3 -(2,6-Me.sub.2)4213 imidazolin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.2 -(2,4,6-Me.sub.3)4214 imidazolin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 (3-pyridyl)4215 imidazolin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 (2-thienyl)4216 imidazolin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 (2-thiazolyl)4217 imidazolin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 -�4-(3,5-dimethyl)iso xazolyl!4218 imidazolin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.4 -(3-Br)4218a imidazolin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.4 -(4-F)4219 imidazolin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.3 -(2,6-Cl.sub.2)4220 imidazolin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 (2-naphthyl)4221 imidazolin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 (1-naphthyl)4222 imidazolin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.4 -(4-Ph)4223 imidazolin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.2 -(4-Ph-2,6-dimethyl)4224 imidazolin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.2 -(4-Ph-2,6-dichloro)4225 imidazolin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 CH.sub.2 Ph4226 imidazolin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 -n-Bu4227 imidazolin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NHPh4228 imidazolin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NHC.sub.6 H.sub.4 -(4-CH.sub.3)4229 imidazolin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NHC.sub.6 C.sub.3 -(2,6-Me.sub.2)4230 imidazolin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NHC.sub.6 C.sub.2 -(2,4,6-Me.sub.3)4231 imidazolin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NH(2-naphthyl)4232 imidazolin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NH)1-naphthyl)4233 imidazolin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NHC.sub.6 H.sub.4 -(4-Ph)4234 imidazolin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NHC.sub.6 H.sub.2 -(4-Ph-2,6-dimethyl)4235 imidazolin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NHC.sub.6 H.sub.2 -(4-Ph-2,6-dichloro)4236 imidazolin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NHCH.sub.2 Ph4237 benzimidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 Ph4238 benzimidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.4 -(3-CH.sub.3)4239 benzimidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.3 -(2,6-Me.sub.2)4240 benzimidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.2 -(2,4,6-Me.sub.3)4241 benzimidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 (4-pyridyl)4242 benzimidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 (2-thienyl)4243 benzimidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 (2-thiazolyl)4244 benzimidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 -�4-(3,5-dimethyl)iso xazolyl!4245 benzimidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.4 -(3-Br)4246 benzimidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.4 -(3-F)4247 benzimidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.3 -(2,6-Cl.sub.2)4248 benzimidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 (2-naphthyl)4249 benzimidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 (1-naphthyl)4250 benzimidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.4 -(4-Ph)4250a benzimidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.4 -4-(4-pyridyl)4250b benzimidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.4 -4-(2-oxazolyl)4250c benzimidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.4 -4-(3-pyrazolyl)4251 benzimidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.2 -(4-Ph-2,6-dimethyl)4251a benzimidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.2 -4-(3-pyridyl)-2,6-dimethyl)4251b benzimidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.2 -4-(2-oxazolyl)-2,6-dimethyl)4251c benzimidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.2 -4-(2-pyrazolyl)-2,6-dimethyl)4252 benzimidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.2 -(4-Ph-2,6-dichloro)4253 benzimidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 CH.sub.2 Ph4254 benzimidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 -i-Bu4255 benzimidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NHPh4256 benzimidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NHC.sub.6 H.sub.4 -(4-CH.sub.3)4257 benzimidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NHC.sub.6 C.sub.3 -(2,6-Me.sub.2)4258 benzimidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NHC.sub.6 C.sub.2 -(2,4,6-Me.sub.3)4259 benzimidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NH(2-naphthyl)4260 benzimidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NH)1-naphthyl)4261 benzimidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NHC.sub.6 H.sub.4 -(4-Ph)4262 benzimidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NHC.sub.6 H.sub.4 -(4-Ph-2,6-dimethyl)4263 benzimidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NHC.sub.6 H.sub.4 -(4-Ph-2,6-dichloro)4264 benzimidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NHCH.sub.2 Ph4265 benzimidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHCO.sub.2 CH.sub.2 Ph4266 benzimidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHCO.sub.2 i-Bu4267 2-aminopyridin-6-yl-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.4 -(4-CH.sub.3)4268 2-aminopyridin-6-yl-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.3 -(2,6-Me.sub.2)4269 2-aminopyridin-6-yl-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.2 -(2,4,6-Me.sub.3)4270 2-aminopyridin-6-yl-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 (3-pyridyl)4271 2-aminopyridin-6-yl-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 (2-thiazolyl)4272 2-aminopyridin-6-yl-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 (4-isoxazolyl)4273 2-aminopyridin-6-yl-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.4 -(3-Br)4274 2-aminopyridin-6-yl-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.4 -(3-F)4275 2-aminopyridin-6-yl-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.3 -(2,6-Cl.sub.2)4276 2-aminopyridin-6-yl-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 (2-naphthyl)4277 2-aminopyridin-6-yl-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 (1-naphthyl)4278 2-aminopyridin-6-yl-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.4 -(4-Ph)4279 2-aminopyridin-6-yl-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.2 -(4-Ph-2,6-dimethyl)4280 2-aminopyridin-6-yl-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.2 -(4-Ph-2,6-dichloro)4281 2-aminopyridin-6-yl-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 CH.sub.2 Ph4282 2-aminopyridin-6-yl-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 -i-Bu4283 2-aminopyridin-6-yl-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NHPh4284 2-aminopyridin-6-yl-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NHC.sub.6 H.sub.4 -(4-CH.sub.3)4285 2-aminopyridin-6-yl-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NHC.sub.6 C.sub.3 -(2,6-Me.sub.2)4286 2-aminopyridin-6-yl-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NHC.sub.6 C.sub.2 -(2,4,6-Me.sub.3)4287 2-aminopyridin-6-yl-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NH(2-naphthyl)4288 2-aminopyridin-6-yl-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NH)1-naphthyl)4289 2-aminopyridin-6-yl-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NHC.sub.6 H.sub.4 -(4-Ph)4290 2-aminopyridin-6-yl-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NHC.sub.6 H.sub.2 -(4-Ph-2,6-dimethyl)4291 2-aminopyridin-6-yl-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 NHC.sub.6 H.sub.2 -(4-Ph-2,6-dichloro)4292 2-aminopyridin-6-yl-(CH.sub.2).sub.3 CH.sub.3 H NHCO.sub.2 n-Bu4293 2-aminopyridin-6-yl-(CH.sub.2).sub.3 CH.sub.3 H NHCO.sub.2 i-Bu4294 2-iminoazepin-7-yl-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 Ph4295 imidazol-4-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 Ph4296 2-iminoazepin-7-yl-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 (4-isoxazolyl)4297 imidazol-4-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 (4-isoxazolyl)4298 2-iminoazepin-7-yl-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 -�4-(3,5-dimethyl)iso xazolyl!4299 imidazol-4-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 -�4-(3,5-dimethyl)iso xazolyl!4300 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 3-pyridinyl NHSO.sub.2 Ph4301 pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 3-pyridinyl NHSO.sub.2 Ph4302 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 (3,4-methylenedioxy)phenyl NHSO.sub.2 Ph4303 pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 (3,4-methylenedioxy)phenyl NHSO.sub.2 Ph4304 imidazol-2-ylamino-(CH.sub.2).sub.2 CH.sub.3 H NHSO.sub.2 Ph4305 imidazol-2-ylamino-(CH.sub.2).sub.2 CH.sub.3 H NHCO.sub.2 CH.sub.2 Ph4306 imidazol-2-ylamino-carbonyl-(CH.sub.2).sub.2 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.2 -(2,4,6-CH.sub.3)4307 pyridin-2-ylamino-(CH.sub.2).sub.2 CH.sub.3 H NHSO.sub.2 Ph4308 pyridin-2-ylamino-(CH.sub.2).sub.2 CH.sub.3 H NHCO.sub.2 CH.sub.2 Ph4309 pyridin-2-ylamino-carbonyl-(CH.sub.2).sub.2 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.2 -(2,4,6-CH.sub.3).sub.34310 imidazolin-2-ylamino-(CH.sub.2).sub.2 CH.sub.3 H NHSO.sub.2 Ph4311 imidazolin-2-ylamino-(CH.sub.2).sub.2 CH.sub.3 H NHCO.sub.2 CH.sub.2 Ph4312 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.2 CH.sub.3 H NHSO.sub.2 Ph4313 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.2 CH.sub.3 H NHCO.sub.2 CH.sub.2 Ph4314 benzimidazol-2-ylamino-(CH.sub.2).sub.2 CH.sub.3 H NHSO.sub.2 Ph4315 benzimidazol-2-ylamino-(CH.sub.2).sub.2 CH.sub.3 H NHCO.sub.2 CH.sub.2 Ph4316 benzimidazol-2-ylamino-carbonyl-(CH.sub.2).sub.2 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.2 -(2,4,6-CH.sub.3).sub.34317 2-aminopyridin-6-yl-(CH.sub.2).sub.2 CH.sub.3 H NHSO.sub.2 Ph4318 2-aminopyridin-6-yl-(CH.sub.2).sub.2 CH.sub.3 H NHCO.sub.2 CH.sub.2 Ph4319 2-iminoazepin-7-yl-(CH.sub.2).sub.2 CH.sub.3 H NHSO.sub.2 Ph4320 2-iminoazepin-7-yl-(CH.sub.2).sub.2 CH.sub.3 H NHCO.sub.2 CH.sub.2 Ph4321 imidazol-4-ylamino-(CH.sub.2).sub.2 CH.sub.3 H NHSO.sub.2 Ph4322 imidazol-4-ylamino-(CH.sub.2).sub.2 CH.sub.3 H NHCO.sub.2 CH.sub.2 Ph4323 imidazol-2-ylamino-(CH.sub.2).sub.4 CH.sub.3 H NHSO.sub.2 Ph4324 imidazol-2-ylamino-(CH.sub.2).sub.4 CH.sub.3 H NHCO.sub.2 CH.sub.2 Ph4325 pyridin-2-ylamino-(CH.sub.2).sub.4 CH.sub.3 H NHSO.sub.2 Ph4326 pyridin-2-ylamino-(CH.sub.2).sub.4 CH.sub.3 H NHCO.sub.2 CH.sub.2 Ph4327 imidazolin-2-ylamino-(CH.sub.2).sub.4 CH.sub.3 H NHSO.sub.2 Ph4328 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.4 CH.sub.3 H NHSO.sub.2 Ph4329 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.4 CH.sub.3 H NHCO.sub.2 CH.sub.2 Ph4330 benzimidazol-2-ylamino-(CH.sub.2).sub.4 CH.sub.3 H NHSO.sub.2 Ph4331 benzimidazol-2-ylamino-(CH.sub.2).sub.4 CH.sub.3 H NHCO.sub.2 CH.sub.2 Ph4332 2-aminopyridin-6-yl-(CH.sub.2).sub.4 CH.sub.3 H NHSO.sub.2 Ph4333 2-aminopyridin-6-yl-(CH.sub.2).sub.4 CH.sub.3 H NHCO.sub.2 CH.sub.2 Ph4334 2-iminoazepin-7-yl-(CH.sub.2).sub.4 CH.sub.3 H NHSO.sub.2 Ph4335 2-iminoazepin-7-yl-(CH.sub.2).sub.4 CH.sub.3 H NHCO.sub.2 CH.sub.2 Ph4336 imidazol-4-ylamino-(CH.sub.2).sub.4 CH.sub.3 H NHSO.sub.2 Ph4337 imidazol-4-ylamino-(CH.sub.2).sub.4 CH.sub.3 H NHCO.sub.2 CH.sub.2 Ph4338 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.2 Ph H NHSO.sub.2 C.sub.6 H.sub.2 -(2,4,6-CH.sub.3)4339 pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.2 Ph H NHSO.sub.2 C.sub.6 H.sub.2 -(2,4,6-CH.sub.3)4340 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.2 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.2 -(2,4,6-CH.sub.3)4341 imidazol-2-ylamino-(CH.sub.2).sub.3 CH(CH.sub.3).sub.2 H NHSO.sub.2 C.sub.6 H.sub.2 -(2,4,6-CH.sub.3)4342 imidazol-2-ylamino-(CH.sub.2).sub.3 cyclopropyl H NHSO.sub.2 C.sub.6 H.sub.2 -(2,4,6-CH.sub.3)4343 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.2 - H NHSO.sub.2 C.sub.6 H.sub.2 -(2,4,6-CH.sub.3) cyclopropyl4344 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.2 COOH H NHSO.sub.2 C.sub.6 H.sub.2 -(2,4,6-CH.sub.3)4345 imidazol-2-ylamino-(CH.sub.2).sub.3 (CH.sub.2).sub.2 NMe.sub.2 H NHSO.sub.2 C.sub.6 H.sub.2 -(2,4,6-CH.sub.3)4346 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.2 CH.sub.2 OMe H NHSO.sub.2 C.sub.6 H.sub.2 -(2,4,6-CH.sub.3)4347 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.2 CH.sub.2 Ph H NHSO.sub.2 C.sub.6 H.sub.2 -(2,4,6-CH.sub.3)4348 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.2 CH.sub.2 OH H NHSO.sub.2 C.sub.6 H.sub.2 -(2,4,6-CH.sub.3)4349 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.2 CH.sub.3 H NHSO.sub.2 C.sub.6 H.sub.2 -(2,6-CH.sub.3).sub.2 -4-Ph4350 imidazol-2-ylamino-(CH.sub.2).sub.3 CH(CH.sub.3).sub.2 H NHSO.sub.2 C.sub.6 H.sub.2 -(2,6-CH.sub.3).sub.2 -4-Ph4351 imidazol-2-ylamino-(CH.sub.2).sub.3 cyclopropyl H NHSO.sub.2 C.sub.6 H.sub.2 -(2,6-CH.sub.3).sub.2 -4-Ph4352 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.2 - H NHSO.sub.2 C.sub.6 H.sub.2 -(2,6-CH.sub.3).sub.2 -4-Ph cyclopropyl4353 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.2 COOH H NHSO.sub.2 C.sub.6 H.sub.2 -(2,6-CH.sub.3).sub.2 -4-Ph4354 imidazol-2-ylamino-(CH.sub.2).sub.3 (CH.sub.2).sub.2 NMe.sub.2 H NHSO.sub.2 C.sub.6 H.sub.2 -(2,6-CH.sub.3).sub.2 -4-Ph4355 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.2 CH.sub.2 OMe H NHSO.sub.2 C.sub.6 H.sub.2 -(2,6-CH.sub.3).sub.2 -4-Ph4356 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.2 CH.sub.2 Ph H NHSO.sub.2 C.sub.6 H.sub.2 -(2,6-CH.sub.3).sub.2 -4-Ph4357 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.2 CH.sub.2 OH H NHSO.sub.2 C.sub.6 H.sub.2 -(2,6-CH.sub.3).sub.2 -4-Ph4358 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 -(1-naphthyl)4359 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHCO.sub.2 CH.sub.2 Ph4360 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 H NHSO.sub.2 C.sub.6 C.sub.2 -(2,4,6-Me.sub.3)4361 pyridin-2-ylamino-CH.sub.2 (o-C.sub.6 H.sub.4) CH.sub.3 H NHSO.sub.2 -(1-naphthyl)4362 pyridin-2-ylamino-CH.sub.2 (o-C.sub.6 H.sub.4) CH.sub.3 H NHCO.sub.2 CH.sub.2 Ph4363 pyridin-2-ylamino-CH.sub.2 (o-C.sub.6 H.sub.4) CH.sub.3 H NHSO.sub.2 C.sub.6 C.sub.2 -(2,4,6-Me.sub.3)4364 imidazolin-2-ylamino-CH.sub.2 (o-C.sub.6 H.sub.4) CH.sub.3 H NHSO.sub.2 -(1-naphthyl)4365 imidazolin-2-ylamino-CH.sub.2 (o-C.sub.6 H.sub.4) CH.sub.3 H NHCO.sub.2 CH.sub.2 Ph4366 imidazolin-2-ylamino-CH.sub.2 (o-C.sub.6 H.sub.4) CH.sub.3 H NHSO.sub.2 C.sub.6 C.sub.2 -(2,4,6-Me.sub.3)4367 imidazolin-2-ylamino-(m-C.sub.6 H.sub.4) CH.sub.3 H NHSO.sub.2 -(1-naphthyl)4368 imidazolin-2-ylamino-(m-C.sub.6 H.sub.4) CH.sub.3 H NHCO.sub.2 CH.sub.2 Ph4369 imidazolin-2-ylamino-(m-C.sub.6 H.sub.4) CH.sub.3 H NHSO.sub.2 C.sub.6 C.sub.2 -(2,4,6-Me.sub.3)__________________________________________________________________________ TABLE 5__________________________________________________________________________ ##STR63##Ex. No. R.sup.1 R.sup.14 R.sup.15 MS__________________________________________________________________________5001 imidazol-2-ylamino-(CH.sub.2).sub.3 H H5002 pyridin-2-ylamino-(CH.sub.2).sub.3 H NHCOOCH.sub.2 Ph5003 imidazolin-2-yl amino-(CH.sub.2).sub.3 H NHCO.sub.2 CH.sub.2 C.sub.6 H.sub.4 -(2-CH.sub.3)5004 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H NHCO.sub.2 CH.sub.2 C.sub.6 H.sub.4 -(3-CH.sub.3)5005 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H NHCO.sub.2 CH.sub.2 C.sub.6 H.sub.4 -(4-CH.sub.3)5006 2-aminopyridin-6-yl-(CH.sub.2).sub.3 H NHCO.sub.2 CH.sub.2 (2-pyridinyl)5007 2-iminoazepin-7-yl-(CH.sub.2).sub.3 H NHCO.sub.2 CH.sub.2 (3-pyridinyl)5010 imidazol-4-ylamino-(CH.sub.2).sub.3 H NHCO.sub.2 CH.sub.2 (2-thiazolyl)5015 imidazol-2-ylamino-(CH.sub.2).sub.3 H NHCO.sub.2 CH.sub.2 (4-isoxazolyl)5016 pyridin-2-ylamino-(CH.sub.2).sub.3 H NHCO.sub.2 CH.sub.2 (2-thienyl)5017 imidazolin-2-ylamino-(CH.sub.2).sub.3 H NHCO.sub.2 n-Bu5018 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H NHCO.sub.2 i-Bu5019 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H NHCO.sub.2 t-Bu5020 2-aminopyridin-6-yl-(CH.sub.2).sub.3 H NHSO.sub.2 Ph5021 2-iminoazepin-7-yl-(CH.sub.2).sub.3 H NHSO.sub.2 C.sub.6 H.sub.4 -(2-CH.sub.3) N5024 imidazol-4-ylamino-(CH.sub.2).sub.3 H NHSO.sub.2 (2-pyridyl)5029 imidazol-2-ylamino-(CH.sub.2).sub.3 H NHSO.sub.2 (4-isoxazolyl)5030 pyridin-2-ylamino-(CH.sub.2).sub.3 H NHSO.sub.2 -�4-(3,5-dimethyl)isoxazolyl! O5031 imidazolin-2-ylamino-(CH.sub.2).sub.3 H NHSO.sub.2 C.sub.6 H.sub.4 -(2-Br)5032 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H NHSO.sub.2 C.sub.6 H.sub.4 -(3-Br)5033 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H NHSO.sub.2 C.sub.6 H.sub.4 -(4-Br)5034 2-aminopyridin-6-yl-(CH.sub.2).sub.3 H NHSO.sub.2 C.sub.6 H.sub.4 -(2-F)5035 2-iminoazepin-7-yl-(CH.sub.2).sub.3 H NHSO.sub.2 C.sub.6 H.sub.4 -(3-F)5038 imidazol-4-ylamino-(CH.sub.2).sub.3 H NHSO.sub.2 (1-naphthyl)5043 imidazol-2-ylamino-(CH.sub.2).sub.3 H NHSO.sub.2 -i-Bu5044 pyridin-2-ylamino-(CH.sub.2).sub.3 H NHSO.sub.2 -t-Bu5045 imidazol-2-ylamino-(CH.sub.2).sub.3 (3,4-methylenedioxy)phenyl H5046 pyridin-2-ylamino-(CH.sub.2).sub.3 (3,4-methylenedioxy)phenyl H5047 imidazolin-2-ylamino-(CH.sub.2).sub.3 (3,4-methylenedioxy)phenyl H5048 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 (3,4-methylenedioxy)phenyl H5049 benzimidazol-2-ylamino-(CH.sub.2).sub.3 (3,4-methylenedioxy)phenyl H5050 2-aminopyridin-6-yl-(CH.sub.2).sub.3 (3,4-methylenedioxy)phenyl H5051 2-iminoazepin-7-yl-(CH.sub.2).sub.3 (3,4-methylenedioxy)phenyl H5054 imidazol-4-ylamino-(CH.sub.2).sub.3 (3,4-methylenedioxy)phenyl H5059 imidazol-2-ylamino-(CH.sub.2).sub.3 3-pyridinyl H5060 pyridin-2-ylamino-(CH.sub.2).sub.3 3-pyridinyl H5061 imidazolin-2-ylamino-(CH.sub.2).sub.3 3-pyridinyl H5062 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 3-pyridinyl H5063 benzimidazol-2-ylamino-(CH.sub.2).sub.3 3-pyridinyl H5064 2-aminopyridin-6-yl-(CH.sub.2).sub.3 3-pyridinyl H5065 2-iminoazepin-7-yl-(CH.sub.2).sub.3 3-pyridinyl H5068 imidazol-4-ylamino-(CH.sub.2).sub.3 3-pyridinyl H5069 imidazol-2-ylamino-CH.sub.2 (o-C.sub.6 H.sub.4) H NHSO.sub.2 -(1-naphthyl)5070 imidazol-2-ylamino-CH.sub.2 (o-C.sub.6 H.sub.4) H NHCO.sub.2 CH.sub.2 Ph5071 imidazol-2-ylamino-CH.sub.2 (o-C.sub.6 H.sub.4) H NHSO.sub.2 C.sub.6 C.sub.2 -(2,4,6-Me.su b.3)5072 pyridin-2-ylamino-CH.sub.2 (o-C.sub.6 H.sub.4) H NHSO.sub.2 -(1-naphthyl)5073 pyridin-2-ylamino-CH.sub.2 (o-C.sub.6 H.sub.4) H NHCO.sub.2 CH.sub.2 Ph5074 pyridin-2-ylamino-CH.sub.2 (o-C.sub.6 H.sub.4) H NHSO.sub.2 C.sub.6 C.sub.2 -(2,4,6-Me.su b.3)5075 imidazolin-2-ylamino-CH.sub.2 (o-C.sub.6 H.sub.4) H NHSO.sub.2 -(1-naphthyl)5076 imidazolin-2-ylamino-CH.sub.2 (o-C.sub.6 H.sub.4) H NHCO.sub.2 CH.sub.2 Ph5077 imidazolin-2-ylamino-CH.sub.2 (o-C.sub.6 H.sub.4) H NHSO.sub.2 C.sub.6 C.sub.2 -(2,4,6-Me.su b.3)5078 imidazolin-2-ylamino-(m-C.sub.6 H.sub.4) H NHSO.sub.2 -(1-naphthyl)5079 imidazolin-2-ylamino-(m-C.sub.6 H.sub.4) H NHCO.sub.2 CH.sub.2 Ph5080 imidazolin-2-ylamino-(m-C.sub.6 H.sub.4) H NHSO.sub.2 C.sub.6 C.sub.2 -(2,4,6-Me.su b.3)__________________________________________________________________________ TABLE 6__________________________________________________________________________ ##STR64##Ex. No. R.sup.1 R.sup.14 R.sup.15 MS__________________________________________________________________________6001 imidazol-2-ylamino-(CH.sub.2).sub.3 H H6002 pyridin-2-ylamino-(CH.sub.2).sub.3 H NHCOOCH.sub.2 Ph6003 imidazolin-2-yl amino-(CH.sub.2).sub.3 H NHCO.sub.2 CH.sub.2 C.sub.6 H.sub.4 -(2-CH.sub.3)6004 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H NHCO.sub.2 CH.sub.2 C.sub.6 H.sub.4 -(3-CH.sub.3)6005 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H NHCO.sub.2 CH.sub.2 C.sub.6 H.sub.4 -(4-CH.sub.3)6006 2-aminopyridin-6-yl-(CH.sub.2).sub.3 H NHCO.sub.2 CH.sub.2 (2-pyridinyl)6007 2-iminoazepin-7-yl-(CH.sub.2).sub.3 H NHCO.sub.2 CH.sub.2 (3-pyridinyl)6010 imidazol-4-ylamino-(CH.sub.2).sub.3 H NHCO.sub.2 CH.sub.2 (2-thiazolyl)6015 imidazol-2-ylamino-(CH.sub.2).sub.3 H NHCO.sub.2 CH.sub.2 (4-isoxazolyl)6016 pyridin-2-ylamino-(CH.sub.2).sub.3 H NHCO.sub.2 CH.sub.2 (2-thienyl)6017 imidazolin-2-ylamino-(CH.sub.2).sub.3 H NHCO.sub.2 n-Bu6018 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H NHCO.sub.2 i-Bu6019 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H NHCO.sub.2 t-Bu6020 2-aminopyridin-6-yl-(CH.sub.2).sub.3 H NHSO.sub.2 Ph6021 2-iminoazepin-7-yl-(CH.sub.2).sub.3 H NHSO.sub.2 C.sub.6 H.sub.4 -(2-CH.sub.3) N6024 imidazol-4-ylamino-(CH.sub.2).sub.3 H NHSO.sub.2 (2-pyridyl)6029 imidazol-2-ylamino-(CH.sub.2).sub.3 H NHSO.sub.2 (4-isoxazolyl)6030 pyridin-2-ylamino-(CH.sub.2).sub.3 H NHSO.sub.2 -�4-(3,5-dimethyl)isoxazolyl! O6031 imidazolin-2-ylamino-(CH.sub.2).sub.3 H NHSO.sub.2 C.sub.6 H.sub.4 -(2-Br)6032 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H NHSO.sub.2 C.sub.6 H.sub.4 -(3-Br)6033 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H NHSO.sub.2 C.sub.6 H.sub.4 -(4-Br)6034 2-aminopyridin-6-yl-(CH.sub.2).sub.3 H NHSO.sub.2 C.sub.6 H.sub.4 -(2-F)6035 2-iminoazepin-7-yl-(CH.sub.2).sub.3 H NHSO.sub.2 C.sub.6 H.sub.4 -(3-F)6038 imidazol-4-ylamino-(CH.sub.2).sub.3 H NHSO.sub.2 (1-naphthyl)6043 imidazol-2-ylamino-(CH.sub.2).sub.3 H NHSO.sub.2 -i-Bu6044 pyridin-2-ylamino-(CH.sub.2).sub.3 H NHSO.sub.2 -t-Bu6045 imidazol-2-ylamino-(CH.sub.2).sub.3 (3,4-methylenedioxy)phenyl H6046 pyridin-2-ylamino-(CH.sub.2).sub.3 (3,4-methylenedioxy)phenyl H6047 imidazolin-2-ylamino-(CH.sub.2).sub.3 (3,4-methylenedioxy)phenyl H6048 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 (3,4-methylenedioxy)phenyl H6049 benzimidazol-2-ylamino-(CH.sub.2).sub.3 (3,4-methylenedioxy)phenyl H6050 2-aminopyridin-6-yl-(CH.sub.2).sub.3 (3,4-methylenedioxy)phenyl H6051 2-iminoazepin-7-yl-(CH.sub.2).sub.3 (3,4-methylenedioxy)phenyl H6054 imidazol-4-ylamino-(CH.sub.2).sub.3 (3,4-methylenedioxy)phenyl H6059 imidazol-2-ylamino-(CH.sub.2).sub.3 3-pyridinyl H6060 pyridin-2-ylamino-(CH.sub.2).sub.3 3-pyridinyl H6061 imidazolin-2-ylamino-(CH.sub.2).sub.3 3-pyridinyl H6062 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 3-pyridinyl H6063 benzimidazol-2-ylamino-(CH.sub.2).sub.3 3-pyridinyl H6064 2-aminopyridin-6-yl-(CH.sub.2).sub.3 3-pyridinyl H6065 2-iminoazepin-7-yl-(CH.sub.2).sub.3 3-pyridinyl H6068 imidazol-4-ylamino-(CH.sub.2).sub.3 3-pyridinyl H6069 imidazol-2-ylamino-CH.sub.2 (o-C.sub.6 H.sub.4) H NHSO.sub.2 -(1-naphthyl)6070 imidazol-2-ylamino-CH.sub.2 (o-C.sub.6 H.sub.4) H NHCO.sub.2 CH.sub.2 Ph6071 imidazol-2-ylamino-CH.sub.2 (o-C.sub.6 H.sub.4) H NHSO.sub.2 C.sub.6 C.sub.2 -(2,4,6-Me.su b.3)6072 pyridin-2-ylamino-CH.sub.2 (o-C.sub.6 H.sub.4) H NHSO.sub.2 -(1-naphthyl)6073 pyridin-2-ylamino-CH.sub.2 (o-C.sub.6 H.sub.4) H NHCO.sub.2 CH.sub.2 Ph6074 pyridin-2-ylamino-CH.sub.2 (o-C.sub.6 H.sub.4) H NHSO.sub.2 C.sub.6 C.sub.2 -(2,4,6-Me.su b.3)6075 imidazolin-2-ylamino-CH.sub.2 (o-C.sub.6 H.sub.4) H NHSO.sub.2 -(1-naphthyl)6076 imidazolin-2-ylamino-CH.sub.2 (o-C.sub.6 H.sub.4) H NHCO.sub.2 CH.sub.2 Ph6077 imidazolin-2-ylamino-CH.sub.2 (o-C.sub.6 H.sub.4) H NHSO.sub.2 C.sub.6 C.sub.2 -(2,4,6-Me.su b.3)6078 imidazolin-2-ylamino-(m-C.sub.6 H.sub.4) H NHSO.sub.2 -(1-naphthyl)6079 imidazolin-2-ylamino-(m-C.sub.6 H.sub.4) H NHCO.sub.2 CH.sub.2 Ph6080 imidazolin-2-ylamino-(m-C.sub.6 H.sub.4) H NHSO.sub.2 C.sub.6 C.sub.2 -(2,4,6-Me.su b.3)__________________________________________________________________________ TABLE 7__________________________________________________________________________ ##STR65##Ex. No. R.sup.1 R.sup.10 X.sup.1 X.sup.3 X.sup.4 R.sup.15 MS__________________________________________________________________________7001 imidazol-2-ylamino-(CH.sub.2).sub.3 H N CH CH NHCO.sub.2 CH.sub.2 Ph7002 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 CH N CH NHCO.sub.2 n-Bu7003 imidazol-2-ylamino-(CH.sub.2).sub.3 H N CH CH NHCO.sub.2 i-Bu7004 imidazol-2-ylamino-(CH.sub.2).sub.3 H CH N CH NHCOPh7005 imidazol-2-ylamino-(CH.sub.2).sub.3 H CH CH N NHCOCH.sub.2 Ph7006 imidazol-2-ylamino-(CH.sub.2).sub.3 H N N CH NHCOCH.sub.2 CH.sub.2 Ph7007 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 N CH CH NHCOCH.dbd.CHPh7008 imidazol-2-ylamino-(CH.sub.2).sub.3 H CH N CH NHCOn-Bu7009 imidazol-2-ylamino-(CH.sub.2).sub.3 H N CH CH NHSO.sub.2 Ph7010 imidazol-2-ylamino-(CH.sub.2).sub.3 H CH N CH NHSO.sub.2 C.sub.6 H.sub.4 -(2-CH.sub.3)7011 imidazol-2-ylamino-(CH.sub.2).sub.3 H CH CH N NHSO.sub.2 C.sub.6 H.sub.4 -(3-CH.sub.3)7012 imidazol-2-ylamino-(CH.sub.2).sub.3 H N N CH NHSO.sub.2 C.sub.6 H.sub.4 -(4-CH.sub.3)7013 imidazol-2-ylamino-(CH.sub.2).sub.3 H N CH CH NHSO.sub.2 C.sub.6 H.sub.3 -(2,6-CH.sub.3) .sub.27014 imidazol-2-ylamino-(CH.sub.2).sub.3 H CH N CH NHSO.sub.2 C.sub.6 H.sub.2 -(2,4,6-CH.sub. 3).sub.37015 imidazol-2-ylamino-(CH.sub.2).sub.3 H N CH CH NHSO.sub.2 (2-pyridyl)7016 imidazol-2-ylamino-(CH.sub.2).sub.3 H CH N CH NHSO.sub.2 (3-pyridyl)7017 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 CH CH N NHSO.sub.2 (4-pyridyl)7018 imidazol-2-ylamino-(CH.sub.2).sub.3 H N N CH NHSO.sub.2 (2-thienyl)7019 imidazol-2-ylamino-(CH.sub.2).sub.3 H N CH CH NHSO.sub.2 �4-(3,5-dimethyl)isoxazolyl!7020 imidazol-2-ylamino-(CH.sub.2).sub.3 H CH N CH NHSO.sub.2 C.sub.6 H.sub.3 -(2,6-Cl.sub.2)7021 imidazol-2-ylamino-(CH.sub.2).sub.3 H N CH CH NHSO.sub.2 (2-naphthyl)7022 imidazol-2-ylamino-(CH.sub.2).sub.3 H CH N CH NHSO.sub.2 (1-naphthyl)7023 imidazol-2-ylamino-(CH.sub.2).sub.3 H N CH CH NHSO.sub.2 C.sub.6 H.sub.4 -(4-Ph)7024 imidazol-2-ylamino-(CH.sub.2).sub.3 H CH N CH NHSO.sub.2 C.sub.6 H.sub.2 -(4-Ph-2,6-dime thyl)7025 imidazol-2-ylamino-(CH.sub.2).sub.3 H N CH CH NHSO.sub.2 C.sub.6 H.sub.2 -(4-Ph-2,6-dich loro)7026 imidazol-2-ylamino-(CH.sub.2).sub.3 H CH N CH NHSO.sub.2 C.sub.6 H.sub.4 -4-(4-pyridyl)7027 imidazol-2-ylamino-(CH.sub.2).sub.3 H N CH CH NHSO.sub.2 C.sub.6 H.sub.4 -4-(4-pyridyl)- 2,6-dimethyl7028 imidazol-2-ylamino-(CH.sub.2).sub.3 H CH N CH NHSO.sub.2 C.sub.6 H.sub.4 -4-(4-pyridyl)- 2,6-dichloro7029 imidazol-2-ylamino-(CH.sub.2).sub.3 H CH N CH NHSO.sub.2 C.sub.6 H.sub.4 -4-(2-oxazolyl) O7030 imidazol-2-ylamino-(CH.sub.2).sub.3 H CH N CH NHSO.sub.2 C.sub.6 H.sub.4 -4-(2-oxazolyl) -2,6-dimethyl7031 imidazol-2-ylamino-(CH.sub.2).sub.3 H N CH CH NHSO.sub.2 C.sub.6 H.sub.4 -4-(2-oxazolyl) -2,6-dichloro7031a imidazol-2-ylamino-(CH.sub.2).sub.3 H N CH CH NHSO.sub.2 C.sub.6 H.sub.4 -4-(2-pyridyl)- 2,6-dimethyl7031b imidazol-2-ylamino-(CH.sub.2).sub.3 H N CH CH NHSO.sub.2 C.sub.6 H.sub.4 -4-(2-furyl)-2, 6-dimethyl7031c imidazol-2-ylamino-(CH.sub.2).sub.3 H N CH CH NHSO.sub.2 C.sub.6 H.sub.4 -4-(3-furyl)2,6 -dimethyl7031d imidazol-2-ylamino-(CH.sub.2).sub.3 H N CH CH NHSO.sub.2 C.sub.6 H.sub.4 -4-(5-pyrazolyl )-2,6-dimethyl7032 imidazol-2-ylamino-(CH.sub.2).sub.3 H CH N CH NHSO.sub.2 CH.sub.2 Ph7033 imidazol-2-ylamino-(CH.sub.2).sub.3 H N CH CH NHSO.sub.2 -n-Bu7034 imidazol-2-ylamino-(CH.sub.2).sub.3 H CH N CH NHSO.sub.2 NHPh7035 imidazol-2-ylamino-(CH.sub.2).sub.3 H CH CH N NHSO.sub.2 NHC.sub.6 H.sub.3 -(2,6-Me.sub. 2)7036 imidazol-2-ylamino-(CH.sub.2).sub.3 H N N CH NHSO.sub.2 NHC.sub.6 H.sub.2 -(2,4,6-Me.su b.3)7037 imidazol-2-ylamino-(CH.sub.2).sub.3 H N CH CH NHSO.sub.2 NH(2-naphthyl)7038 imidazol-2-ylamino-(CH.sub.2).sub.3 H CH N CH NHSO.sub.2 NH(1-naphthyl)7039 imidazol-2-ylamino-(CH.sub.2).sub.3 H N CH CH NHSO.sub.2 NHC.sub.6 H.sub.4 -(4-Ph)7040 imidazol-2-ylamino-(CH.sub.2).sub.3 H CH N CH NHSO.sub.2 NHC.sub.6 H.sub.2 -(4-Ph-2,6-di methyl)7041 imidazol-2-ylamino-(CH.sub.2).sub.3 H CH CH N NHSO.sub.2 C.sub.6 H.sub.2 -(4-Ph-2,6-dich loro)7042 imidazol-2-ylamino-(CH.sub.2).sub.3 H N N CH NHSO.sub.2 NHCH.sub.2 Ph7043 imidazol-2-ylamino-(CH.sub.2).sub.3 H N CH CH NHSO.sub.2 NH-n-Bu7044 imidazol-2-ylamino-(CH.sub.2).sub.3 H CH N CH NHSO.sub.2 NH-i-Bu7045 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 N CH CH NHSO.sub.2 NH-t-Bu7046 pyridin-2-ylamino-(CH.sub.2).sub.3 H CH N CH NHCO.sub.2 CH.sub.2 Ph7047 pyridin-2-ylamino-(CH.sub.2).sub.3 H CH CH N NHCO.sub.2 n-Bu7048 pyridin-2-ylamino-(CH.sub.2).sub.3 H N N CH NHCO.sub.2 i-Bu7049 pyridin-2-ylamino-(CH.sub.2).sub.3 H N CH CH NHCOPh7050 pyridin-2-ylamino-(CH.sub.2).sub.3 H CH N CH NHCOCH.sub.2 Ph7051 pyridin-2-ylamino-(CH.sub.2).sub.3 H N CH CH NHCOCH.sub.2 CH.sub.2 Ph7052 pyridin-2-ylamino-(CH.sub.2).sub.3 H CH N CH NHCOCH.dbd.CHPh7053 pyridin-2-ylamino-(CH.sub.2).sub.3 H CH CH N NHCOn-Bu7054 pyridin-2-ylamino-(CH.sub.2).sub.3 H N CH CH NHSO.sub.2 Ph7055 pyridin-2-ylamino-(CH.sub.2).sub.3 H CH N CH NHSO.sub.2 C.sub.6 H.sub.4 -(2-CH.sub.3)7056 pyridin-2-ylamino-(CH.sub.2).sub.3 H CH CH N NHSO.sub.2 C.sub.6 H.sub.4 -(3-CH.sub.3)7057 pyridin-2-ylamino-(CH.sub.2).sub.3 H N N CH NHSO.sub.2 C.sub.6 H.sub.4 -(4-CH.sub.3)7058 pyridin-2-ylamino-(CH.sub.2).sub.3 H N CH CH NHSO.sub.2 C.sub.6 H.sub.3 -(2,6-CH.sub.3) .sub.27059 pyridin-2-ylamino-(CH.sub.2).sub.3 H CH N CH NHSO.sub.2 C.sub.6 H.sub.2 -(2,4,6-CH.sub. 3).sub.37060 pyridin-2-ylamino-(CH.sub.2).sub.3 H N CH CH NHSO.sub.2 (2-pyridyl)7061 pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 CH N CH NHSO.sub.2 (3-pyridyl)7062 pyridin-2-ylamino-(CH.sub.2).sub.3 H CH CH N NHSO.sub.2 (4-pyridyl)7063 pyridin-2-ylamino-(CH.sub.2).sub.3 H N N CH NHSO.sub.2 (2-thienyl)7064 pyridin-2-ylamino-(CH.sub.2).sub.3 H N CH CH NHSO.sub.2 �4-(3,5-dimethyl)isoxazolyl!7065 pyridin-2-ylamino-(CH.sub.2).sub.3 H CH N CH NHSO.sub.2 C.sub.6 H.sub.3 -(2,6-Cl.sub.2) A7066 pyridin-2-ylamino-(CH.sub.2).sub.3 H N CH CH NHSO.sub.2 (2-naphthyl)7067 pyridin-2-ylamino-(CH.sub.2).sub.3 H CH N CH NHSO.sub.2 (1-naphthyl)7068 pyridin-2-ylamino-(CH.sub.2).sub.3 H N CH CH NHSO.sub.2 C.sub.6 H.sub.4 -(4-Ph)7069 pyridin-2-ylamino-(CH.sub.2).sub.3 H CH N CH NHSO.sub.2 C.sub.6 H.sub.4 -(4-Ph-2,6-dime thyl)7070 pyridin-2-ylamino-(CH.sub.2).sub.3 H N CH CH NHSO.sub.2 C.sub.6 H.sub.4 -(4-Ph-2,6-dich loro)7071 pyridin-2-ylamino-(CH.sub.2).sub.3 H CH N CH NHSO.sub.2 C.sub.6 H.sub.4 -4-(4-pyridyl) B7072 pyridin-2-ylamino-(CH.sub.2).sub.3 H N CH CH NHSO.sub.2 C.sub.6 H.sub.4 -4-(4-pyridyl)- 2,6-dimethyl7073 pyridin-2-ylamino-(CH.sub.2).sub.3 H CH N CH NHSO.sub.2 C.sub.6 H.sub.4 -4-(4-pyridyl)- 2,6-dichloro7074 pyridin-2-ylamino-(CH.sub.2).sub.3 H CH N CH NHSO.sub.2 C.sub.6 H.sub.4 -4-(2-oxazolyl)7075 pyridin-2-ylamino-(CH.sub.2).sub.3 H CH N CH NHSO.sub.2 C.sub.6 H.sub.4 -4-(2-oxazolyl) -2,6-dimethyl7076 pyridin-2-ylamino-(CH.sub.2).sub.3 H N CH CH NHSO.sub.2 C.sub.6 H.sub.4 -4-(2-oxazolyl) -2,6-dichloro7076a pyridin-2-ylamino-(CH.sub.2).sub.3 H N CH CH NHSO.sub.2 C.sub.6 H.sub.4 -4-(3-pyridyl)- 2,6-dimethyl7076b pyridin-2-ylamino-(CH.sub.2).sub.3 H N CH CH NHSO.sub.2 C.sub.6 H.sub.4 -4-(2-furyl)-2, 6-dimethyl7076c pyridin-2-ylamino-(CH.sub.2).sub.3 H N CH CH NHSO.sub.2 C.sub.6 H.sub.4 -4-(3-furyl)-2, 6-dimethyl7076d pyridin-2-ylamino-(CH.sub.2).sub.3 H N CH CH NHSO.sub.2 C.sub.6 H.sub.4 -4-(5-pyrazolyl )-2,6-dimethyl7077 pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 CH CH N NHSO.sub.2 CH.sub.2 Ph7078 pyridin-2-ylamino-(CH.sub.2).sub.3 H N N CH NHSO.sub.2 -n-Bu7079 pyridin-2-ylamino-(CH.sub.2).sub.3 H N CH CH NHSO.sub.2 NHPh7080 pyridin-2-ylamino-(CH.sub.2).sub.3 H CH N CH NHSO.sub.2 NHC.sub.6 H.sub.3 -(2,6-Me.sub. 2)7081 pyridin-2-ylamino-(CH.sub.2).sub.3 H N CH CH NHSO.sub.2 NHC.sub.6 H.sub.2 -(2,4,6-Me.su b.3)7082 pyridin-2-ylamino-(CH.sub.2).sub.3 H CH N CH NHSO.sub.2 NH(2-naphthyl)7083 pyridin-2-ylamino-(CH.sub.2).sub.3 H CH CH N NHSO.sub.2 NH(1-naphthyl)7084 pyridin-2-ylamino-(CH.sub.2).sub.3 H N N CH NHSO.sub.2 NHC.sub.6 H.sub.4 -(4-Ph)7085 pyridin-2-ylamino-(CH.sub.2).sub.3 H N CH CH NHSO.sub.2 NHC.sub.6 H.sub.2 -(4-Ph-2,6-di methyl)7086 pyridin-2-ylamino-(CH.sub.2).sub.3 H CH N CH NHSO.sub.2 NHC.sub.6 H.sub.2 -(4-Ph-2,6-di chloro)7087 pyridin-2-ylamino-(CH.sub.2).sub.3 H N CH CH NHSO.sub.2 NHCH.sub.2 Ph7088 pyridin-2-ylamino-(CH.sub.2).sub.3 H CH N CH NHSO.sub.2 NH-n-Bu7089 pyridin-2-ylamino-(CH.sub.2).sub.3 H CH CH N NHSO.sub.2 NH-i-Bu7090 pyridin-2-ylamino-(CH.sub.2).sub.3 H N N CH NHSO.sub.2 NH-t-Bu7091 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 C.sub.2 H.sub.5 N CH CH NHCO.sub.2 CH.sub.2 Ph7092 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H CH N CH NHCO.sub.2 n-Bu7093 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H N CH CH NHCO.sub.2 i-Bu7094 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H CH N CH NHCOPh7095 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H CH CH N NHCOCH.sub.2 Ph7096 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H N N CH NHCOCH.sub.2 CH.sub.2 Ph7097 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H N CH CH NHCOCH.dbd.CHPh7098 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H CH N CH NHCOn-Bu7099 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H N CH CH NHSO.sub.2 Ph7100 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H CH N CH NHSO.sub.2 C.sub.6 H.sub.4 -(2-CH.sub.3)7101 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H CH CH N NHSO.sub.2 C.sub.6 H.sub.4 -(3-CH.sub.3)7102 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H N N CH NHSO.sub.2 C.sub.6 H.sub.4 -(4-CH.sub.3)7103 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H N CH CH NHSO.sub.2 C.sub.6 H.sub.3 -(2,6-CH.sub.3) .sub.27104 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H CH N CH NHSO.sub.2 C.sub.6 H.sub.2 -(2,4,6-CH.sub. 3).sub.37105 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H N CH CH NHSO.sub.2 (2-pyridyl)7106 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H CH N CH NHSO.sub.2 (3-pyridyl)7107 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H CH CH N NHSO.sub.2 (4-pyridyl)7108 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 N N CH NHSO.sub.2 (2-thienyl)7109 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H N CH CH NHSO.sub.2 �4-(3,5-dimethyl)isoxazolyl!7110 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H CH N CH NHSO.sub.2 C.sub.6 H.sub.3 -(2,6-Cl.sub.2)7111 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H N CH CH NHSO.sub.2 (2-naphthyl)7112 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H CH N CH NHSO.sub.2 (1-naphthyl)7113 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H N CH CH NHSO.sub.2 C.sub.6 H.sub.4 -(4-Ph)7114 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H CH N CH NHSO.sub.2 C.sub.6 H.sub.2 -(4-Ph-2,6-dime thyl)7115 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H N CH CH NHSO.sub.2 C.sub.6 H.sub.2 -(4-Ph-2,6-dich loro)7116 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H CH N CH NHSO.sub.2 C.sub.6 H.sub.4 -4-(4-pyridyl) 27117 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H N CH CH NHSO.sub.2 C.sub.6 H.sub.4 -4-(4-pyridyl)- 2,6-dimethyl7118 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H CH N CH NHSO.sub.2 C.sub.6 H.sub.4 -4-(4-pyridyl)- 2,6-dichloro7119 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H CH N CH NHSO.sub.2 C.sub.6 H.sub.4 -4-(2-oxazolyl)7120 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H CH N CH NHSO.sub.2 C.sub.6 H.sub.4 -4-(2-oxazolyl) -2,6-dimethyl7121 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H N CH CH NHSO.sub.2 C.sub.6 H.sub.4 -4-(2-oxazolyl) -2,6-dichloro7121a tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H N CH CH NHSO.sub.2 C.sub.6 H.sub.4 -4-(3-pyridyl)- 2,6-dimethyl7121b tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H N CH CH NHSO.sub.2 C.sub.6 H.sub.4 -4-(2-furyl)-2, 6-dimethyl7121c tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H N CH CH NHSO.sub.2 C.sub.6 H.sub.4 -4-(3-furyl)-2, 6-dimethyl7121d tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H N CH CH NHSO.sub.2 C.sub.6 H.sub.4 -4-(5-pyrazolyl )-2,6-dimethyl7122 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 CH N CH NHSO.sub.2 CH.sub.2 Ph7123 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H N CH CH NHSO.sub.2 -n-Bu7124 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H CH N CH NHSO.sub.2 NHPh7125 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H CH CH N NHSO.sub.2 NHC.sub.6 H.sub.3 -(2,6-Me.sub. 2)7126 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H N N CH NHSO.sub.2 NHC.sub.6 H.sub.2 -(2,4,6-Me.su b.3)7127 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H N CH CH NHSO.sub.2 NH(2-naphthyl)7128 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H CH N CH NHSO.sub.2 NH(1-naphthyl)7129 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H N CH CH NHSO.sub.2 NHC.sub.6 H.sub.4 -(4-Ph)7130 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H CH N CH NHSO.sub.2 NHC.sub.6 H.sub.2 -(4-Ph-2,6-di methyl)7131 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H CH CH N NHSO.sub.2 NHC.sub.6 H.sub.2 -(4-Ph-2,6-di chloro)7132 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H N N CH NHSO.sub.2 NHCH.sub.2 Ph7133 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H N CH CH NHSO.sub.2 NH-n-Bu7134 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H CH N CH NHSO.sub.2 NH-i-Bu7135 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H N CH CH NHSO.sub.2 NH-t-Bu7136 imidazolin-2-ylamino-(CH.sub.2).sub.3 H CH N CH NHCO.sub.2 CH.sub.2 Ph7137 imidazolin-2-ylamino-(CH.sub.2).sub.3 H CH CH N NHCO.sub.2 n-Bu7138 imidazolin-2-ylamino-(CH.sub.2).sub.3 H N N CH NHCO.sub.2 i-Bu7139 imidazolin-2-ylamino-(CH.sub.2).sub.3 H N CH CH NHCOPh7140 imidazolin-2-ylamino-(CH.sub.2).sub.3 H CH N CH NHCOCH.sub.2 Ph7141 imidazolin-2-ylamino-(CH.sub.2).sub.3 H N CH CH NHCOCH.sub.2 CH.sub.2 Ph7142 imidazolin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 CH N CH NHCOCH.dbd.CHPh7143 imidazolin-2-ylamino-(CH.sub.2).sub.3 H CH CH N NHCOn-Bu7144 imidazolin-2-ylamino-(CH.sub.2).sub.3 H N CH CH NHSO.sub.2 Ph7145 imidazolin-2-ylamino-(CH.sub.2).sub.3 H CH N CH NHSO.sub.2 C.sub.6 H.sub.4 -(2-CH.sub.3)7146 imidazolin-2-ylamino-(CH.sub.2).sub.3 H CH CH N NHSO.sub.2 C.sub.6 H.sub.4 -(3-CH.sub.3)7147 imidazolin-2-ylamino-(CH.sub.2).sub.3 H N N CH NHSO.sub.2 C.sub.6 H.sub.4 -(4-CH.sub.3)7148 imidazolin-2-ylamino-(CH.sub.2).sub.3 H N CH CH NHSO.sub.2 C.sub.6 H.sub.3 -(2,6-CH.sub.3) .sub.27149 imidazolin-2-ylamino-(CH.sub.2).sub.3 H CH N CH NHSO.sub.2 C.sub.6 H.sub.2 -(2,4,6-CH.sub. 3).sub.37150 imidazolin-2-ylamino-(CH.sub.2).sub.3 H N CH CH NHSO.sub.2 (2-pyridyl)7151 imidazolin-2-ylamino-(CH.sub.2).sub.3 H CH N CH NHSO.sub.2 (3-pyridyl)7152 imidazolin-2-ylamino-(CH.sub.2).sub.3 H CH CH N NHSO.sub.2 (4-pyridyl)7153 imidazolin-2-ylamino-(CH.sub.2).sub.3 H N N CH NHSO.sub.2 (2-thienyl)7154 imidazolin-2-ylamino-(CH.sub.2).sub.3 H N CH CH NHSO.sub.2 �4-(3,5-dimethyl)isoxazolyl!7155 imidazolin-2-ylamino-(CH.sub.2).sub.3 H CH N CH NHSO.sub.2 C.sub.6 H.sub.3 -(2,6-Cl.sub.2)7156 imidazolin-2-ylamino-(CH.sub.2).sub.3 H N CH CH NHSO.sub.2 (2-naphthyl)7157 imidazolin-2-ylamino-(CH.sub.2).sub.3 H CH N CH NHSO.sub.2 (1-naphthyl)7158 imidazolin-2-ylamino-(CH.sub.2).sub.3 H N CH CH NHSO.sub.2 C.sub.6 H.sub.4 -(4-Ph)7159 imidazolin-2-ylamino-(CH.sub.2).sub.3 H CH N CH NHSO.sub.2 C.sub.6 H.sub.2 -(4-Ph-2,6-dime thyl)7160 imidazolin-2-ylamino-(CH.sub.2).sub.3 H N CH CH NHSO.sub.2 C.sub.6 H.sub.2 -(4-Ph-2,6-dich loro)7161 imidazolin-2-ylamino-(CH.sub.2).sub.3 H CH N CH NHSO.sub.2 C.sub.6 H.sub.4 -4-(4-pyridyl) N7162 imidazolin-2-ylamino-(CH.sub.2).sub.3 H N CH CH NHSO.sub.2 C.sub.6 H.sub.4 -4-(4-pyridyl)- 2,6-dimethyl7163 imidazolin-2-ylamino-(CH.sub.2).sub.3 H CH N CH NHSO.sub.2 C.sub.6 H.sub.4 -4-(4-pyridyl)- 2,6-dichloro7164 imidazolin-2-ylamino-(CH.sub.2).sub.3 H CH N CH NHSO.sub.2 C.sub.6 H.sub.4 -4-(2-oxazolyl)7165 imidazolin-2-ylamino-(CH.sub.2).sub.3 H CH N CH NHSO.sub.2 C.sub.6 H.sub.4 -4-(2-oxazolyl) -2,6-dimethyl7166 imidazolin-2-ylamino-(CH.sub.2).sub.3 H N CH CH NHSO.sub.2 C.sub.6 H.sub.4 -4-(2-oxazolyl) -2,6-dichloro7166a imidazolin-2-ylamino-(CH.sub.2).sub.3 H N CH CH NHSO.sub.2 C.sub.6 H.sub.4 -4-(3-pyridyl)- 2,6-dimethyl7166b imidazolin-2-ylamino-(CH.sub.2).sub.3 H N CH CH NHSO.sub.2 C.sub.6 H.sub.4 -4-(2-furyl)-2, 6-dimethyl7166c imidazolin-2-ylamino-(CH.sub.2).sub.3 H N CH CH NHSO.sub.2 C.sub.6 H.sub.4 -4-(3-furyl)-2, 6-dimethyl7166d imidazolin-2-ylamino-(CH.sub.2).sub.3 H N CH CH NHSO.sub.2 C.sub.6 H.sub.4 -4-(5-pyrazolyl )-2,6-dimethyl7167 imidazolin-2-ylamino-(CH.sub.2).sub.3 H CH CH N NHSO.sub.2 CH.sub.2 Ph7168 imidazolin-2-ylamino-(CH.sub.2).sub.3 H N N CH NHSO.sub.2 -n-Bu7169 imidazolin-2-ylamino-(CH.sub.2).sub.3 Br N CH CH NHSO.sub.2 NHPh7170 imidazolin-2-ylamino-(CH.sub.2).sub.3 H CH N CH NHSO.sub.2 NHC.sub.6 H.sub.3 -(2,6-Me.sub. 2)7171 imidazolin-2-ylamino-(CH.sub.2).sub.3 H N CH CH NHSO.sub.2 NHC.sub.6 H.sub.2 -(2,4,6-Me.su b.3)7172 imidazolin-2-ylamino-(CH.sub.2).sub.3 H CH N CH NHSO.sub.2 NH(2-naphthyl)7173 imidazolin-2-ylamino-(CH.sub.2).sub.3 H CH CH N NHSO.sub.2 NH(1-naphthyl)7174 imidazolin-2-ylamino-(CH.sub.2).sub.3 H N N CH NHSO.sub.2 NHC.sub.6 H.sub.4 -(4-Ph)7175 imidazolin-2-ylamino-(CH.sub.2).sub.3 H N CH CH NHSO.sub.2 NHC.sub.6 H.sub.2 -(4-Ph-2,6-di methyl)7176 imidazolin-2-ylamino-(CH.sub.2).sub.3 H CH N CH NHSO.sub.2 NHC.sub.6 H.sub.2 -(4-Ph-2,6-di chloro)7177 imidazolin-2-ylamino-(CH.sub.2).sub.3 H N CH CH NHSO.sub.2 NHCH.sub.2 Ph7178 imidazolin-2-ylamino-(CH.sub.2).sub.3 H CH N CH NHSO.sub.2 NH-n-Bu7179 imidazolin-2-ylamino-(CH.sub.2).sub.3 H CH CH N NHSO.sub.2 NH-i-Bu7180 imidazolin-2-ylamino-(CH.sub.2).sub.3 H N N CH NHSO.sub.2 NH-t-Bu7181 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H N CH CH NHCO.sub.2 CH.sub.2 Ph7182 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H CH N CH NHCO.sub.2 n-Bu7183 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H N CH CH NHCO.sub.2 i-Bu7184 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H CH N CH NHCOPh7185 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H CH CH N NHCOCH.sub.2 Ph7186 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H N N CH NHCOCH.sub.2 CH.sub.2 Ph7187 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H N CH CH NHCOCH.dbd.CHPh7188 benzimidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 CH N CH NHCOn-Bu7189 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H N CH CH NHSO.sub.2 Ph7190 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H CH N CH NHSO.sub.2 C.sub.6 H.sub.4 -(2-CH.sub.3)7191 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H CH CH N NHSO.sub.2 C.sub.6 H.sub.4 -(3-CH.sub.3)7192 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H N N CH NHSO.sub.2 C.sub.6 H.sub.4 -(4-CH.sub.3)7193 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H N CH CH NHSO.sub.2 C.sub.6 H.sub.3 -(2,6-CH.sub.3) .sub.27194 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H CH N CH NHSO.sub.2 C.sub.6 H.sub.2 -(2,4,6-CH.sub. 3).sub.37195 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H N CH CH NHSO.sub.2 (2-pyridyl)7196 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H CH N CH NHSO.sub.2 (3-pyridyl)7197 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H CH CH N NHSO.sub.2 (4-pyridyl)7198 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H N N CH NHSO.sub.2 (2-thienyl)7199 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H N CH CH NHSO.sub.2 �4-(3,5-dimethyl)isoxazolyl!7200 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H CH N CH NHSO.sub.2 C.sub.6 H.sub.3 -(2,6-Cl.sub.2) 17201 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H N CH CH NHSO.sub.2 (2-naphthyl)7202 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H CH N CH NHSO.sub.2 (1-naphthyl)7203 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H N CH CH NHSO.sub.2 C.sub.6 H.sub.4 -(4-Ph)7204 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H CH N CH NHSO.sub.2 C.sub.6 H.sub.2 -(4-Ph-2,6-dime thyl)7205 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H N CH CH NHSO.sub.2 C.sub.6 H.sub.2 -(4-Ph-2,6-dich loro)7206 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H CH N CH NHSO.sub.2 C.sub.6 H.sub.4 -4-(4-pyridyl) 57207 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H N CH CH NHSO.sub.2 C.sub.6 H.sub.4 -4-(4-pyridyl)- 2,6-dimethyl7208 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H CH N CH NHSO.sub.2 C.sub.6 H.sub.4 -4-(4-pyridyl)- 2,6-dichloro7209 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H CH N CH NHSO.sub.2 C.sub.6 H.sub.4 -4-(2-oxazolyl)7210 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H CH N CH NHSO.sub.2 C.sub.6 H.sub.4 -4-(2-oxazolyl) -2,6-dimethyl7211 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H N CH CH NHSO.sub.2 C.sub.6 H.sub.4 -4-(2-oxazolyl) -2,6-dichloro7211a benzimidazol-2-ylamino-(CH.sub.2).sub.3 H N CH CH NHSO.sub.2 C.sub.6 H.sub.4 -4-(3-pyridyl)- 2,6-dimethyl7211b benzimidazol-2-ylamino-(CH.sub.2).sub.3 H N CH CH NHSO.sub.2 C.sub.6 H.sub.4 -4-(2-furyl)-2, 6-dimethyl7211c benzimidazol-2-ylamino-(CH.sub.2).sub.3 H N CH CH NHSO.sub.2 C.sub.6 H.sub.4 -4-(3-furyl)-2, 6-dimethyl7211d benzimidazol-2-ylamino-(CH.sub.2).sub.3 H N CH CH NHSO.sub.2 C.sub.6 H.sub.4 -4-(5-pyrazolyl )-2,6-dimethyl7212 benzimidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 CH N CH NHSO.sub.2 CH.sub.2 Ph7213 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H N CH CH NHSO.sub.2 -n-Bu7214 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H CH N CH NHSO.sub.2 NHPh7215 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H CH CH N NHSO.sub.2 NHC.sub.6 H.sub.3 -(2,6-Me.sub. 2)7216 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H N N CH NHSO.sub.2 NHC.sub.6 H.sub.2 -(2,4,6-Me.su b.3)7217 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H N CH CH NHSO.sub.2 NH(2-naphthyl)7218 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H CH N CH NHSO.sub.2 NH(1-naphthyl)7219 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H N CH CH NHSO.sub.2 NHC.sub.6 H.sub.4 -(4-Ph)7220 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H CH N CH NHSO.sub.2 NHC.sub.6 H.sub.2 -(4-Ph-2,6-di methyl)7221 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H CH CH N NHSO.sub.2 NHC.sub.6 H.sub.2 -(4-Ph-2,6-di chloro)7222 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H N N CH NHSO.sub.2 NHCH.sub.2 Ph7223 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H N CH CH NHSO.sub.2 NH-n-Bu7224 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H CH N CH NHSO.sub.2 NH-i-Bu7225 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H N CH CH NHSO.sub.2 NH-t-Bu7226 2-aminopyridin-6-yl-(CH.sub.2).sub.2 H CH N CH NHSO.sub.2 CH.sub.2 Ph7227 2-aminopyridin-6-yl-(CH.sub.2).sub.2 H CH CH N NHCO.sub.2 n-Bu7228 2-aminopyridin-6-yl-(CH.sub.2).sub.2 H N N CH NHCO.sub.2 i-Bu7229 2-aminopyridin-6-yl-(CH.sub.2).sub.2 H N CH CH NHCOPh7230 2-aminopyridin-6-yl-(CH.sub.2).sub.2 H CH N CH NHCOCH.sub.2 Ph7231 2-aminopyridin-6-yl-(CH.sub.2).sub.2 H N CH CH NHCOCH.sub.2 CH.sub.2 Ph7232 2-aminopyridin-6-yl-(CH.sub.2).sub.2 H CH N CH NHCOCH.dbd.CHPh7233 2-aminopyridin-6-yl-(CH.sub.2).sub.2 H CH CH N NHCOn-Bu7234 2-aminopyridin-6-yl-(CH.sub.2).sub.2 H N CH CH NHSO.sub.2 Ph7235 2-aminopyridin-6-yl-(CH.sub.2).sub.2 H CH N CH NHSO.sub.2 C.sub.6 H.sub.4 -(2-CH.sub.3)7236 2-aminopyridin-6-yl-(CH.sub.2).sub.2 H CH CH N NHSO.sub.2 C.sub.6 H.sub.4 -(3-CH.sub.3)7237 2-aminopyridin-6-yl-(CH.sub.2).sub.2 H N N CH NHSO.sub.2 C.sub.6 H.sub.4 -(4-CH.sub.3)7238 2-aminopyridin-6-yl-(CH.sub.2).sub.2 H N CH CH NHSO.sub.2 C.sub.6 H.sub.3 -(2,6-CH.sub.3) .sub.27239 2-aminopyridin-6-yl-(CH.sub.2).sub.2 H CH N CH NHSO.sub.2 C.sub.6 H.sub.2 -(2,4,6-CH.sub. 3).sub.37240 2-aminopyridin-6-yl-(CH.sub.2).sub.2 H N CH CH NHSO.sub.2 (2-pyridyl)7241 2-aminopyridin-6-yl-(CH.sub.2).sub.2 H CH N CH NHSO.sub.2 (3-pyridyl)7242 2-aminopyridin-6-yl-(CH.sub.2).sub.2 H CH CH N NHSO.sub.2 (4-pyridyl)7243 2-aminopyridin-6-yl-(CH.sub.2).sub.2 H N N CH NHSO.sub.2 (2-thienyl)7244 2-aminopyridin-6-yl-(CH.sub.2).sub.2 CH.sub.3 N CH CH NHSO.sub.2 �4-(3,5-dimethyl)isoxazolyl!7245 2-aminopyridin-6-yl-(CH.sub.2).sub.2 H CH N CH NHSO.sub.2 C.sub.6 H.sub.3 -(2,6-Cl.sub.2) M7246 2-aminopyridin-6-yl-(CH.sub.2).sub.2 H N CH CH NHSO.sub.2 (2-naphthyl)7247 2-aminopyridin-6-yl-(CH.sub.2).sub.2 H CH N CH NHSO.sub.2 (1-naphthyl)7248 2-aminopyridin-6-yl-(CH.sub.2).sub.2 H N CH CH NHSO.sub.2 C.sub.6 H.sub.4 -(4-Ph)7249 2-aminopyridin-6-yl-(CH.sub.2).sub.2 H CH N CH NHSO.sub.2 C.sub.6 H.sub.2 -(4-Ph-2,6-dime thyl)7250 2-aminopyridin-6-yl-(CH.sub.2).sub.2 H N CH CH NHSO.sub.2 C.sub.6 H.sub.2 -(4-Ph-2,6-dich loro)7251 2-aminopyridin-6-yl-(CH.sub.2).sub.2 H CH N CH NHSO.sub.2 C.sub.6 H.sub.4 -4-(4-pyridyl) O7252 2-aminopyridin-6-yl-(CH.sub.2).sub.2 H N CH CH NHSO.sub.2 C.sub.6 H.sub.4 -4-(4-pyridyl)- 2,6-dimethyl7253 2-aminopyridin-6-yl-(CH.sub.2).sub.2 H CH N CH NHSO.sub.2 C.sub.6 H.sub.4 -4-(4-pyridyl)- 2,6-dichloro7254 2-aminopyridin-6-yl-(CH.sub.2).sub.2 H CH N CH NHSO.sub.2 C.sub.6 H.sub.4 -4-(2-oxazolyl) 37255 2-aminopyridin-6-yl-(CH.sub.2).sub.2 H CH N CH NHSO.sub.2 C.sub.6 H.sub.4 -4-(2-oxazolyl) -2,6-dimethyl7256 2-aminopyridin-6-yl-(CH.sub.2).sub.2 H N CH CH NHSO.sub.2 C.sub.6 H.sub.4 -4-(2-oxazolyl) -2,6-dichloro7256a 2-aminopyridin-6-yl-(CH.sub.2).sub.2 H N CH CH NHSO.sub.2 C.sub.6 H.sub.4 -4-(3-pyridyl)- 2,6-dimethyl7256b 2-aminopyridin-6-yl-(CH.sub.2).sub.2 H N CH CH NHSO.sub.2 C.sub.6 H.sub.4 -4-(2-furyl)-2, 6-dimethyl7256c 2-aminopyridin-6-yl-(CH.sub.2).sub.2 H N CH CH NHSO.sub.2 C.sub.6 H.sub.4 -4-(3-furyl)-2, 6-dimethyl7256d 2-aminopyridin-6-yl-(CH.sub.2).sub.2 H N CH CH NHSO.sub.2 C.sub.6 H.sub.4 -4-(5-pyrazolyl )-2,6-dimethyl7257 2-aminopyridin-6-yl-(CH.sub.2).sub.2 H CH CH N NHSO.sub.2 CH.sub.2 Ph7258 2-aminopyridin-6-yl-(CH.sub.2).sub.2 H N N CH NHSO.sub.2 -n-Bu7259 2-aminopyridin-6-yl-(CH.sub.2).sub.2 H N CH CH NHSO.sub.2 NHPh7260 2-aminopyridin-6-yl-(CH.sub.2).sub.2 H CH N CH NHSO.sub.2 NHC.sub.6 H.sub.3 -(2,6-Me.sub. 2)7261 2-aminopyridin-6-yl-(CH.sub.2).sub.2 H N CH CH NHSO.sub.2 NHC.sub.6 H.sub.2 -(2,4,6-Me.su b.3)7262 2-aminopyridin-6-yl-(CH.sub.2).sub.2 H CH N CH NHSO.sub.2 NH(2-naphthyl)7263 2-aminopyridin-6-yl-(CH.sub.2).sub.2 H CH CH N NHSO.sub.2 NH(1-naphthyl)7264 2-aminopyridin-6-yl-(CH.sub.2).sub.2 H N N CH NHSO.sub.2 NHC.sub.6 H.sub.4 -(4-Ph)7265 2-aminopyridin-6-yl-(CH.sub.2).sub.2 H N CH CH NHSO.sub.2 NHC.sub.6 H.sub.2 -(4-Ph-2,6-di methyl)7266 2-aminopyridin-6-yl-(CH.sub.2).sub.2 H CH N CH NHSO.sub.2 NHC.sub.6 H.sub.2 -(4-Ph-2,6-di chloro)7267 2-aminopyridin-6-yl-(CH.sub.2).sub.2 H N CH CH NHSO.sub.2 NHCH.sub.2 Ph7268 2-aminopyridin-6-yl-(CH.sub.2).sub.2 H CH N CH NHSO.sub.2 NH-n-Bu7269 2-aminopyridin-6-yl-(CH.sub.2).sub.2 H CH CH N NHSO.sub.2 NH-i-Bu7270 2-aminopyridin-6-yl-(CH.sub.2).sub.2 H N N CH NHSO.sub.2 NH-t-Bu7271 imidazol-2-ylamino-CH.sub.2 (o-C.sub.6 H.sub.4)-CH.sub.2 H N CH CH NHSO.sub.2 -(1-naphthyl)7272 imidazol-2-ylamino-CH.sub.2 (o-C.sub.6 H.sub.4)-CH.sub.2 H N CH CH NHCO.sub.2 CH.sub.2 Ph7273 imidazol-2-ylamino-CH.sub.2 (o-C.sub.6 H.sub.4)-CH.sub.2 H N CH CH NHSO.sub.2 C.sub.6 C.sub.2 -(2,4,6-Me.sub. 3)7274 pyridin-2-ylamino-CH.sub.2 (o-C.sub.6 H.sub.4)-CH.sub.2 H N CH CH NHSO.sub.2 -(1-naphthyl)7275 pyridin-2-ylamino-CH.sub.2 (o-C.sub.6 H.sub.4)-CH.sub.2 H N CH CH NHCO.sub.2 CH.sub.2 Ph7276 pyridin-2-ylamino-CH.sub.2 (o-C.sub.6 H.sub.4)-CH.sub.2 H N CH CH NHSO.sub.2 C.sub.6 C.sub.2 -(2,4,6-Me.sub. 3)7277 imidazolin-2-ylamino-CH.sub.2 (o-C.sub.6 H.sub.4)-CH.sub.2 H N CH CH NHSO.sub.2 -(1-naphthyl)7278 imidazolin-2-ylamino-CH.sub.2 (o-C.sub.6 H.sub.4)-CH.sub.2 H N CH CH NHCO.sub.2 CH.sub.2 Ph7279 imidazolin-2-ylamino-CH.sub.2 (o-C.sub.6 H.sub.4)-CH.sub.2 H N CH CH NHSO.sub.2 C.sub.6 C.sub.2 -(2,4,6-Me.sub. 3)7280 imidazolin-2-ylamino-(o-C.sub.6 H.sub.4)-CH.sub.2 H N CH CH NHSO.sub.2 -(1-naphthyl)7281 imidazolin-2-ylamino-(o-C.sub.6 H.sub.4)-CH.sub.2 H N CH CH NHCO.sub.2 CH.sub.2 Ph7282 imidazolin-2-ylamino-(o-C.sub.6 H.sub.4)-CH.sub.2 H N CH CH NHSO.sub.2 C.sub.6 C.sub.2 -(2,4,6-Me.sub. 3)__________________________________________________________________________ TABLE 8__________________________________________________________________________ ##STR66##Ex.No. R.sup.1 R.sup.9 X.sup.1 X.sup.3 X.sup.4 R.sup.15 MS__________________________________________________________________________8001 imidazol-2-ylamino-(CH.sub.2).sub.3 H CH CH N NHCO.sub.2 CH.sub.2 Ph8002 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 CH N CH NHCO.sub.2 n-Bu8003 imidazol-2-ylamino-(CH.sub.2).sub.3 H CH CH N NHCO.sub.2 i-Bu8004 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 N CH CH NHCOPh8005 imidazol-2-ylamino-(CH.sub.2).sub.3 H CH CH N NHCOCH.sub.2 Ph8006 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 N N CH NHCOCH.sub.2 CH.sub.2 Ph8007 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 CH CH N NHCOCHCHPh8008 imidazol-2-ylamino-(CH.sub.2).sub.3 H CH N CH NHCOn-Bu8009 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 CH CH N NHSO.sub.2 Ph8010 imidazol-2-ylamino-(CH.sub.2).sub.3 H N CH CH NHSO.sub.2 C.sub.6 H.sub.4 -(2-CH.sub.3)8011 imidazol-2-ylamino-(CH.sub.2).sub.3 H CH CH N NHSO.sub.2 C.sub.6 H.sub.4 -(3-CH.sub.3)8012 imidazol-2-ylamino-(CH.sub.2).sub.3 H N N CH NHSO.sub.2 C.sub.6 H.sub.4 -(4-CH.sub.3)8013 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 CH CH N NHSO.sub.2 C.sub.6 H.sub.3 -(2,6-CH.sub.3 ).sub.28014 imidazol-2-ylamino-(CH.sub.2).sub.3 H CH CH N NHSO.sub.2 C.sub.6 H.sub.2 -(2,4,6-CH.sub .3).sub.38015 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 CH CH N NHSO.sub.2 (2-pyridyl)8016 imidazol-2-ylamino-(CH.sub.2).sub.3 H N CH CH NHSO.sub.2 (3-pyridyl)8017 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 CH CH N NHSO.sub.2 (4-pyridyl)8018 imidazol-2-ylamino-(CH.sub.2).sub.3 H N N CH NHSO.sub.2 (2-thienyl)8019 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 CH CH N NHSO.sub.2 �4-(3,5- dimethyl)isoxazolyl!8020 imidazol-2-ylamino-(CH.sub.2).sub.3 H CH CH N NHSO.sub.2 C.sub.6 H.sub.3 -(2,6-Cl.sub.2 )8021 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 CH CH N NHSO.sub.2 (2-naphthyl)8022 imidazol-2-ylamino-(CH.sub.2).sub.3 H CH CH N NHSO.sub.2 (1-naphthyl)8023 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 CH CH N NHSO.sub.2 C.sub.6 H.sub.4 -(4-Ph)8024 imidazol-2-ylamino-(CH.sub.2).sub.3 H CH CH N NHSO.sub.2 C.sub.6 H.sub.2 -(4-Ph-2,6- dimethyl)8025 imidazol-2-ylamino-(CH.sub.2).sub.3 H CH CH N NHSO.sub.2 C.sub.6 H.sub.2 -(4-Ph-2,6- dichloro)8026 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 CH CH N NHSO.sub.2 C.sub.6 H.sub.4 -4-(4-pyridyl) J8027 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 CH CH N NHSO.sub.2 C.sub.6 H.sub.4 -4-(4-pyridyl) - 2,6-dimethyl8028 imidazol-2-ylamino-(CH.sub.2).sub.3 H N CH CH NHSO.sub.2 C.sub.6 H.sub.4 -4-(4-pyridyl) - 2,6-dichloro8029 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 CH CH N NHSO.sub.2 C.sub.6 H.sub.4 -4-(2-oxazolyl )8030 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 CH CH N NHSO.sub.2 C.sub.6 H.sub.4 -4-(2-oxazolyl )- 2,6-dimethyl8031 imidazol-2-ylamino-(CH.sub.2).sub.3 H CH CH N NHSO.sub.2 C.sub.6 H.sub.4 -4-(2-oxazolyl )- 2,6-dichloro8031a imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 CH CH N NHSO.sub.2 C.sub.6 H.sub.4 -4-(3-pyridyl) - 2,6-dimethyl8031b imidazol-2-ylamino-(CH.sub.2).sub.3 H CH CH N NHSO.sub.2 C.sub.6 H.sub.4 -4-(2-furyl)-2 ,6- dimethyl8031c imidazol-2-ylamino-(CH.sub.2).sub.3 H CH CH N NHSO.sub.2 C.sub.6 H.sub.4 -4-(3-furyl)-2 ,6- dimethyl8031d imidazol-2-ylamino-(CH.sub.2)3 CH.sub.3 CH CH N NHSO.sub.2 C.sub.6 H.sub.4 -4-(5-pyrazoly l)- 2,6-dimethyl8032 imidazol-2-ylamino-(CH.sub.2).sub.3 H CH N CH NHSO.sub.2 CH.sub.2 Ph8033 imidazol-2-ylamino-(CH.sub.2).sub.3 H CH CH N NHSO.sub.2 -n-Bu8034 imidazol-2-ylamino-(CH.sub.2).sub.3 H N CH CH NHSO.sub.2 NHPh8035 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 CH CH N NHSO.sub.2 NHC.sub.6 H.sub.3 -(2,6-Me.sub .2)8036 imidazol-2-ylamino-(CH.sub.2).sub.3 H N N CH NHSO.sub.2 NHC.sub.6 H.sub.2 -(2,4,6-Me.s ub.3)8037 imidazol-2-ylamino-(CH.sub.2).sub.3 H CH CH N NHSO.sub.2 NH(2-naphthyl)8038 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 CH N CH NHSO.sub.2 NH(1-naphthyl)8039 imidazol-2-ylamino-(CH.sub.2).sub.3 H CH CH N NHSO.sub.2 NHC.sub.6 H.sub.4 -(4-Ph)8040 imidazol-2-ylamino-(CH.sub.2).sub.3 H N CH CH NHSO.sub.2 NHC.sub.6 H.sub.2 -(4-Ph-2,6- dimethyl)8041 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 CH CH N NHSO.sub.2 NHC.sub.6 H.sub.2 -(4-Ph-2,6- dichloro)8042 imidazol-2-ylamino-(CH.sub.2).sub.3 H N N CH NHSO.sub.2 NHCH.sub.2 Ph8043 imidazol-2-ylamino-(CH.sub.2).sub.3 H CH CH N NHSO.sub.2 NH-n-Bu8044 imidazol-2-ylamino-(CH.sub.2).sub.3 H CH N CH NHSO.sub.2 NH-i-Bu8045 imidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 CH CH N NHSO.sub.2 NH-t-Bu8046 pyridin-2-ylamino-(CH.sub.2).sub.3 H N CH CH NHCO.sub.2 CH.sub.2 Ph8047 pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 CH CH N NHCO.sub.2 n-Bu8048 pyridin-2-ylamino-(CH.sub.2).sub.3 H N N CH NHCO.sub.2 i-Bu8049 pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 CH CH N NHCOPh8050 pyridin-2-ylamino-(CH.sub.2).sub.3 H CH N CH NHCOCH.sub.2 Ph8051 pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 CH CH N NHCOCH.sub.2 CH.sub.2 Ph8052 pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 N CH CH NHCOCHCHPh8053 pyridin-2-ylamino-(CH.sub.2).sub.3 H CH CH N NHCOn-Bu8054 pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 CH CH N NHSO.sub.2 Ph8055 pyridin-2-ylamino-(CH.sub.2).sub.3 H N CH CH NHSO.sub.2 C.sub.6 H.sub.4 -(2-CH.sub.3)8056 pyridin-2-ylamino-(CH.sub.2).sub.3 H CH CH N NHSO.sub.2 C.sub.6 H.sub.4 -(3-CH.sub.3)8057 pyridin-2-ylamino-(CH.sub.2).sub.3 H N N CH NHSO.sub.2 C.sub.6 H.sub.4 -(4-CH.sub.3)8058 pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 CH CH N NHSO.sub.2 C.sub.6 H.sub.3 -(2,6-CH.sub.3 ).sub.28059 pyridin-2-ylamino-(CH.sub.2).sub.3 H CH CH N NHSO.sub.2 C.sub.6 H.sub.2 -(2,4,6-CH.sub .3).sub.38060 pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 CH CH N NHSO.sub.2 (2-pyridyl)8061 pyridin-2-ylamino-(CH.sub.2).sub.3 H N CH CH NHSO.sub.2 (3-pyridyl)8062 pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 CH CH N NHSO.sub.2 (4-pyridyl)8063 pyridin-2-ylamino-(CH.sub.2).sub.3 H N N CH NHSO.sub.2 (2-thienyl)8064 pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 CH CH N NHSO.sub.2 �4-(3,5- dimethyl)isoxazolyl!8065 pyridin-2-ylamino-(CH.sub.2).sub.3 H CH CH N NHSO.sub.2 C.sub.6 H.sub.3 -(2,6-Cl.sub.2 )8066 pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 CH CH N NHSO.sub.2 (2-naphthyl)8067 pyridin-2-ylamino-(CH.sub.2).sub.3 H CH CH N NHSO.sub.2 (1-naphthyl)8068 pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 CH CH N NHSO.sub.2 C.sub.6 H.sub.4 -(4-Ph)8069 pyridin-2-ylamino-(CH.sub.2).sub.3 H CH CH N NHSO.sub.2 C.sub.6 H.sub.2 -(4-Ph-2,6- dimethyl)8070 pyridin-2-ylamino-(CH.sub.2).sub.3 H CH CH N NHSO.sub.2 C.sub.6 H.sub.2 -(4-Ph-2,6- dichloro)8071 pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 CH CH N NHSO.sub.2 C.sub.6 H.sub.4 -4-(4-pyridyl) N8072 pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 CH CH N NHSO.sub.2 C.sub.6 H.sub.4 -4-(4-pyridyl) - 2,6-dimethyl8073 pyridin-2-ylamino-(CH.sub.2).sub.3 H N CH CH NHSO.sub.2 C.sub.6 H.sub.4 -4-(4-pyridyl) - 2,6-dichloro8074 pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 CH CH N NHSO.sub.2 C.sub.6 H.sub.4 -4-(2-oxazolyl )8075 pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 CH CH N NHSO.sub.2 C.sub.6 H.sub.4 -4-(2-oxazolyl )- 2,6-dimethyl8076 pyridin-2-ylamino-(CH.sub.2).sub.3 H CH CH N NHSO.sub.2 C.sub.6 H.sub.4 -4-(2-oxazolyl )- 2,6-dichloro8076a pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 CH CH N NHSO.sub.2 C.sub.6 H.sub.4 -4-(3-pyridyl) - 2,6-dimethyl8076b pyridin-2-ylamino-(CH.sub.2).sub.3 H CH CH N NHSO.sub.2 C.sub.6 H.sub.4 -4-(2-furyl)-2 ,6- dimethyl8076c pyridin-2-ylamino-(CH.sub.2).sub.3 H CH CH N NHSO.sub.2 C.sub.6 H.sub.4 -4-(3-furyl)-2 ,6- dimethyl8076d pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 CH CH N NHSO.sub.2 C.sub.6 H.sub.4 -4-(5-pyrazoly l)- 2,6-dimethyl8077 pyridin-2-ylamino-(CH.sub.2).sub.3 H CH CH N NHSO.sub.2 CH.sub.2 Ph8078 pyridin-2-ylamino-(CH.sub.2).sub.3 H N N CH NHSO.sub.2 -n-Bu8079 pyridin-2-ylamino-(CH.sub.2).sub.3 H CH CH N NHSO.sub.2 NHPh8080 pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 CH N CH NHSO.sub.2 NHC.sub.6 H.sub.3 -(2,6-Me.sub .2)8081 pyridin-2-ylamino-(CH.sub.2).sub.3 H CH CH N NHSO.sub.2 NHC.sub.6 H.sub.2 -(2,4,6-Me.s ub.3)8082 pyridin-2-ylamino-(CH.sub.2).sub.3 H N CH CH NHSO.sub.2 NH(2-naphthyl)8083 pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 CH CH N NHSO.sub.2 NH(1-naphthyl)8084 pyridin-2-ylamino-(CH.sub.2).sub.3 H N N CH NHSO.sub.2 NHC.sub.6 H.sub.4 -(4-Ph)8085 pyridin-2-ylamino-(CH.sub.2).sub.3 H CH CH N NHSO.sub.2 NHC.sub.6 H.sub.2 -(4-Ph-2,6- dimethyl)8086 pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 CH N CH NHSO.sub.2 NHC.sub.6 H.sub.2 -(4-Ph-2,6- dichloro)8087 pyridin-2-ylamino-(CH.sub.2).sub.3 H CH CH N NHSO.sub.2 NHCH.sub.2 Ph8088 pyridin-2-ylamino-(CH.sub.2).sub.3 H N CH CH NHSO.sub.2 NH-n-Bu8089 pyridin-2-ylamino-(CH.sub.2).sub.3 H CH CH N NHSO.sub.2 NH-i-Bu8090 pyridin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 N N CH NHSO.sub.2 NH-t-Bu8091 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H CH CH N NHCO.sub.2 CH.sub.2 Ph8092 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 CH N CH NHCO.sub.2 n-Bu8093 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H CH CH N NHCO.sub.2 i-Bu8094 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 N CH CH NHCOPh8095 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H CH CH N NHCOCH.sub.2 Ph8096 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 N N CH NHCOCH.sub.2 CH.sub.2 Ph8097 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 CH CH N NHCOCHCHPh8098 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H CH N CH NHCOn-Bu8099 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 CH CH N NHSO.sub.2 Ph8100 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H N CH CH NHSO.sub.2 C.sub.6 H.sub.4 -(2-CH.sub.3)8101 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H CH CH N NHSO.sub.2 C.sub.6 H.sub.4 -(3-CH.sub.3)8102 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H N N CH NHSO.sub.2 C.sub.6 H.sub.4 -(4-CH.sub.3)8103 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 CH CH N NHSO.sub.2 C.sub.6 H.sub.3 -(2,6-CH.sub.3 ).sub.28104 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H CH CH N NHSO.sub.2 C.sub.6 H.sub.2 -(2,4,6-CH.sub .3).sub.38105 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 CH CH N NHSO.sub.2 (2-pyridyl)8106 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H N CH CH NHSO.sub.2 (3-pyridyl)8107 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 CH CH N NHSO.sub.2 (4-pyridyl)8108 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H N N CH NHSO.sub.2 (2-thienyl)8109 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 CH CH N NHSO.sub.2 �4-(3,5- dimethyl)isoxazolyl!8110 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H CH CH N NHSO.sub.2 C.sub.6 H.sub.3 -(2,6-Cl.sub.2 )8111 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 CH CH N NHSO.sub.2 (2-naphthyl)8112 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H CH CH N NHSO.sub.2 (1-naphthyl)8113 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 CH CH N NHSO.sub.2 C.sub.6 H.sub.4 -(4-Ph)8114 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H CH CH N NHSO.sub.2 C.sub.6 H.sub.2 -(4-Ph-2,6- dimethyl)8115 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H CH CH N NHSO.sub.2 C.sub.6 H.sub.2 -(4-Ph-2,6- dichloro)8116 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 CH CH N NHSO.sub.2 C.sub.6 H.sub.4 -4-(4-pyridyl) 18117 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 CH CH N NHSO.sub.2 C.sub.6 H.sub.4 -4-(4-pyridyl) - 2,6-dimethyl8118 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H N CH CH NHSO.sub.2 C.sub.6 H.sub.4 -4-(4-pyridyl) - 2,6-dichloro8119 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 CH CH N NHSO.sub.2 C.sub.6 H.sub.4 -4-(2-oxazolyl )8120 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 CH CH N NHSO.sub.2 C.sub.6 H.sub.4 -4-(2-oxazolyl )- 2,6-dimethyl8121 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H CH CH N NHSO.sub.2 C.sub.6 H.sub.4 -4-(2-oxazolyl )- 2,6-dichloro8121a tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 CH CH N NHSO.sub.2 C.sub.6 H.sub.4 -4-(3-pyridyl) - 2,6-dimethyl8121b tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H CH CH N NHSO.sub.2 C.sub.6 H.sub.4 -4-(2-furyl)-2 ,6- dimethyl8121c tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H CH CH N NHSO.sub.2 C.sub.6 H.sub.4 -4-(3-furyl)-2 ,6- dimethyl8121d tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 CH CH N NHSO.sub.2 C.sub.6 H.sub.4 -4-(5-pyrazoly l)- 2,6-dimethyl8122 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H CH N CH NHSO.sub.2 CH.sub.2 Ph8123 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H CH CH N NHSO.sub.2 -n-Bu8124 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H N CH CH NHSO.sub.2 NHPh8125 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 CH CH N NHSO.sub.2 NHC.sub.6 H.sub.3 -(2,6-Me.sub .2)8126 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H N N CH NHSO.sub.2 NHC.sub.6 H.sub.2 -(2,4,6-Me.s ub.3)8127 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H CH CH N NHSO.sub.2 NH(2-naphthyl)8128 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 CH N CH NHSO.sub.2 NH(1-naphthyl)8129 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H CH CH N NHSO.sub.2 NHC.sub.6 H.sub.4 -(4-Ph)8130 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H N CH CH NHSO.sub.2 NHC.sub.6 H.sub.2 -(4-Ph-2,6- dimethyl)8131 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 CH CH N NHSO.sub.2 NHC.sub.6 H.sub.2 -(4-Ph-2,6- dichloro)8132 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H N N CH NHSO.sub.2 NHCH.sub.2 Ph8133 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H CH CH N NHSO.sub.2 NH-n-Bu8134 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 H CH N CH NHSO.sub.2 NH-i-Bu8135 tetrahydropyrimidin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 CH CH N NHSO.sub.2 NH-t-Bu8136 imidazolin-2-ylamino-(CH.sub.2).sub.3 H N CH CH NHCO.sub.2 CH.sub.2 Ph8137 imidazolin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 CH CH N NHCO.sub.2 n-Bu8138 imidazolin-2-ylamino-(CH.sub.2).sub.3 H N N CH NHCO.sub.2 i-Bu8139 imidazolin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 CH CH N NHCOPh8140 imidazolin-2-ylamino-(CH.sub.2).sub.3 H CH N CH NHCOCH.sub.2 Ph8141 imidazolin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 CH CH N NHCOCH.sub.2 CH.sub.2 Ph8142 imidazolin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 N CH CH NHCOCHCHPh8143 imidazolin-2-ylamino-(CH.sub.2).sub.3 H CH CH N NHCOn-Bu8144 imidazolin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 CH CH N NHSO.sub.2 Ph8145 imidazolin-2-ylamino-(CH.sub.2).sub.3 H N CH CH NHSO.sub.2 C.sub.6 H.sub.4 -(2-CH.sub.3)8146 imidazolin-2-ylamino-(CH.sub.2).sub.3 H CH CH N NHSO.sub.2 C.sub.6 H.sub.4 -(3-CH.sub.3)8147 imidazolin-2-ylamino-(CH.sub.2).sub.3 H N N CH NHSO.sub.2 C.sub.6 H.sub.4 -(4-CH.sub.3)8148 imidazolin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 CH CH N NHSO.sub.2 C.sub.6 H.sub.3 -(2,6-CH.sub.3 ).sub.28149 imidazolin-2-ylamino-(CH.sub.2).sub.3 H CH CH N NHSO.sub.2 C.sub.6 H.sub.2 -(2,4,6-CH.sub .3).sub.38150 imidazolin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 CH CH N NHSO.sub.2 (2-pyridyl)8151 imidazolin-2-ylamino-(CH.sub.2).sub.3 H N CH CH NHSO.sub.2 (3-pyridyl)8152 imidazolin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 CH CH N NHSO.sub.2 (4-pyridyl)8153 imidazolin-2-ylamino-(CH.sub.2).sub.3 H N N CH NHSO.sub.2 (2-thienyl)8154 imidazolin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 CH CH N NHSO.sub.2 �4-(3,5- dimethyl)isoxazolyl!8155 imidazolin-2-ylamino-(CH.sub.2).sub.3 H CH CH N NHSO.sub.2 C.sub.6 H.sub.3 -(2,6-Cl.sub.2 )8156 imidazolin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 CH CH N NHSO.sub.2 (2-naphthyl)8157 imidazolin-2-ylamino-(CH.sub.2).sub.3 H CH CH N NHSO.sub.2 (1-naphthyl)8158 imidazolin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 CH CH N NHSO.sub.2 C.sub.6 H.sub.4 -(4-Ph)8159 imidazolin-2-ylamino-(CH.sub.2).sub.3 H CH CH N NHSO.sub.2 C.sub.6 H.sub.2 -(4-Ph-2,6- dimethyl)8160 imidazolin-2-ylamino-(CH.sub.2).sub.3 H CH CH N NHSO.sub.2 C.sub.6 H.sub.2 -(4-Ph-2,6- dichloro)8161 imidazolin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 CH CH N NHSO.sub.2 C.sub.6 H.sub.4 -4-(4-pyridyl) 18162 imidazolin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 CH CH N NHSO.sub.2 C.sub.6 H.sub.4 -4-(4-pyridyl) - 2,6-dimethyl8163 imidazolin-2-ylamino-(CH.sub.2).sub.3 H N CH CH NHSO.sub.2 C.sub.6 H.sub.4 -4-(4-pyridyl) - 2,6-dichloro8164 imidazolin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 CH CH N NHSO.sub.2 C.sub.6 H.sub.4 -4-(2-oxazolyl )8165 imidazolin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 CH CH N NHSO.sub.2 C.sub.6 H.sub.4 -4-(2-oxazolyl )- 2,6-dimethyl8166 imidazolin-2-ylamino-(CH.sub.2).sub.3 H CH CH N NHSO.sub.2 C.sub.6 H.sub.4 -4-(2-oxazolyl )- 2,6-dichloro8166a imidazolin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 CH CH N NHSO.sub.2 C.sub.6 H.sub.4 -4-(3-pyridyl) - 2,6-dimethyl8166b imidazolin-2-ylamino-(CH.sub.2).sub.3 H CH CH N NHSO.sub.2 C.sub.6 H.sub.4 -4-(2-furyl)-2 ,6- dimethyl8166c imidazolin-2-ylamino-(CH.sub.2).sub.3 H CH CH N NHSO.sub.2 C.sub.6 H.sub.4 -4-(3-furyl)-2 ,6- dimethyl8166d imidazolin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 CH CH N NHSO.sub.2 C.sub.6 H.sub.4 -4-(5-pyrazoly l)- 2,6-dimethyl8167 imidazolin-2-ylamino-(CH.sub.2).sub.3 H CH CH N NHSO.sub.2 CH.sub.2 Ph8168 imidazolin-2-ylamino-(CH.sub.2).sub.3 H N N CH NHSO.sub.2 -n-Bu8169 imidazolin-2-ylamino-(CH.sub.2).sub.3 H CH CH N NHSO.sub.2 NHPh8170 imidazolin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 CH N CH NHSO.sub.2 NHC.sub.6 H.sub.3 -(2,6-Me.sub .2)8171 imidazolin-2-ylamino-(CH.sub.2).sub.3 H CH CH N NHSO.sub.2 NHC.sub.6 H.sub.2 -(2,4,6-Me.s ub.3)8172 imidazolin-2-ylamino-(CH.sub.2).sub.3 H N CH CH NHSO.sub.2 NH(2-naphthyl)8173 imidazolin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 CH CH N NHSO.sub.2 NH(1-naphthyl)8174 imidazolin-2-ylamino-(CH.sub.2).sub.3 H N N CH NHSO.sub.2 NHC.sub.6 H.sub.4 -(4-Ph)8175 imidazolin-2-ylamino-(CH.sub.2).sub.3 H CH CH N NHSO.sub.2 NHC.sub.6 H.sub.2 -(4-Ph-2,6- dimethyl)8176 imidazolin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 CH N CH NHSO.sub.2 NHC.sub.6 H.sub.2 -(4-Ph-2,6- dichloro)8177 imidazolin-2-ylamino-(CH.sub.2).sub.3 H CH CH N NHSO.sub.2 NHCH.sub.2 Ph8178 imidazolin-2-ylamino-(CH.sub.2).sub.3 H N CH CH NHSO.sub.2 NH-n-Bu8179 imidazolin-2-ylamino-(CH.sub.2).sub.3 H CH CH N NHSO.sub.2 NH-i-Bu8180 imidazolin-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 N N CH NHSO.sub.2 NH-t-Bu8181 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H CH CH N NHCO.sub.2 CH.sub.2 Ph8182 benzimidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 CH N CH NHCO.sub.2 n-Bu8183 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H CH CH N NHCO.sub.2 i-Bu8184 benzimidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 N CH CH NHCOPh8185 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H CH CH N NHCOCH.sub.2 Ph8186 benzimidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 N N CH NHCOCH.sub.2 CH.sub.2 Ph8187 benzimidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 CH CH N NHCOCHCHPh8188 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H CH N CH NHCOn-Bu8189 benzimidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 CH CH N NHSO.sub.2 Ph8190 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H N CH CH NHSO.sub.2 C.sub.6 H.sub.4 -(2-CH.sub.3)8191 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H CH CH N NHSO.sub.2 C.sub.6 H.sub.4 -(3-CH.sub.3)8192 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H N N CH NHSO.sub.2 C.sub.6 H.sub.4 -(4-CH.sub.3)8193 benzimidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 CH CH N NHSO.sub.2 C.sub.6 H.sub.3 -(2,6-CH.sub.3 ).sub.28194 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H CH CH N NHSO.sub.2 C.sub.6 H.sub.2 -(2,4,6-CH.sub .3).sub.38195 benzimidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 CH CH N NHSO.sub.2 (2-pyridyl)8196 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H N CH CH NHSO.sub.2 (3-pyridyl)8197 benzimidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 CH CH N NHSO.sub.2 (4-pyridyl)8198 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H N N CH NHSO.sub.2 (2-thienyl)8199 benzimidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 CH CH N NHSO.sub.2 �4-(3,5- dimethyl)isoxazolyl!8200 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H CH CH N NHSO.sub.2 C.sub.6 H.sub.3 -(2,6-Cl.sub.2 )8201 benzimidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 CH CH N NHSO.sub.2 (2-naphthyl)8202 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H CH CH N NHSO.sub.2 (1-naphthyl)8203 benzimidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 CH CH N NHSO.sub.2 C.sub.6 H.sub.4 -(4-Ph)8204 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H CH CH N NHSO.sub.2 C.sub.6 H.sub.2 -(4-Ph-2,6- dimethyl)8205 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H CH CH N NHSO.sub.2 C.sub.6 H.sub.2 -(4-Ph-2,6- dichloro)8206 benzimidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 CH CH N NHSO.sub.2 C.sub.6 H.sub.4 -4-(4-pyridyl) r8207 benzimidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 CH CH N NHSO.sub.2 C.sub.6 H.sub.4 -4-(4-pyridyl) - 2,6-dimethyl8208 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H N CH CH NHSO.sub.2 C.sub.6 H.sub.4 -4-(4-pyridyl) - 2,6-dichloro8209 benzimidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 CH CH N NHSO.sub.2 C.sub.6 H.sub.4 -4-(2-oxazolyl )8210 benzimidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 CH CH N NHSO.sub.2 C.sub.6 H.sub.4 -4-(2-oxazolyl )- 2,6-dimethyl8211 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H CH CH N NHSO.sub.2 C.sub.6 H.sub.4 -4-(2-oxazolyl )- 2,6-dichloro8211a benzimidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 CH CH N NHSO.sub.2 C.sub.6 H.sub.4 -4-(3-pyridyl) - 2,6-dimethyl8211b benzimidazol-2-ylamino-(CH.sub.2).sub.3 H CH CH N NHSO.sub.2 C.sub.6 H.sub.4 -4-(2-furyl)-2 ,6- dimethyl8211c benzimidazol-2-ylamino-(CH.sub.2).sub.3 H CH CH N NHSO.sub.2 C.sub.6 H.sub.4 -4-(3-furyl)-2 ,6- dimethyl8211d benzimidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 CH CH N NHSO.sub.2 C.sub.6 H.sub.4 -4-(5-pyrazoly l)- 2,6-dimethyl8212 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H CH N CH NHSO.sub.2 CH.sub.2 Ph8213 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H CH CH N NHSO.sub.2 -n-Bu8214 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H N CH CH NHSO.sub.2 NHPh8215 benzimidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 CH CH N NHSO.sub.2 NHC.sub.6 H.sub.3 -(2,6-Me.sub .2)8216 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H N N CH NHSO.sub.2 NHC.sub.6 H.sub.2 -(2,4,6-Me.s ub.3)8217 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H CH CH N NHSO.sub.2 NH(2-naphthyl)8218 benzimidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 CH N CH NHSO.sub.2 NH(1-naphthyl)8219 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H CH CH N NHSO.sub.2 NHC.sub.6 H.sub.4 -(4-Ph)8220 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H N CH CH NHSO.sub.2 NHC.sub.6 H.sub.2 -(4-Ph-2,6- dimethyl)8221 benzimidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 CH CH N NHSO.sub.2 NHC.sub.6 H.sub.2 -(4-Ph-2,6- dichloro)8222 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H N N CH NHSO.sub.2 NHCH.sub.2 Ph8223 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H CH CH N NHSO.sub.2 NH-n-Bu8224 benzimidazol-2-ylamino-(CH.sub.2).sub.3 H CH N CH NHSO.sub.2 NH-i-Bu8225 benzimidazol-2-ylamino-(CH.sub.2).sub.3 CH.sub.3 CH CH N NHSO.sub.2 NH-t-Bu8226 2-aminopyridin-6-yl-(CH.sub.2).sub.2 H N CH CH NHCO.sub.2 CH.sub.2 Ph8227 2-aminopyridin-6-yl-(CH.sub.2).sub.2 CH.sub.3 CH CH N NHCO.sub.2 n-Bu8228 2-aminopyridin-6-yl-(CH.sub.2).sub.2 H N N CH NHCO.sub.2 i-Bu8229 2-aminopyridin-6-yl-(CH.sub.2).sub.2 CH.sub.3 CH CH N NHCOPh8230 2-aminopyridin-6-yl-(CH.sub.2).sub.2 H CH N CH NHCOCH.sub.2 Ph8231 2-aminopyridin-6-yl-(CH.sub.2).sub.2 CH.sub.3 CH CH N NHCOCH.sub.2 CH.sub.2 Ph8232 2-aminopyridin-6-yl-(CH.sub.2).sub.2 CH.sub.3 N CH CH NHCOCHCHPh8233 2-aminopyridin-6-yl-(CH.sub.2).sub.2 H CH CH N NHCOn-Bu8234 2-aminopyridin-6-yl-(CH.sub.2).sub.2 CH.sub.3 CH CH N NHSO.sub.2 Ph8235 2-aminopyridin-6-yl-(CH.sub.2).sub.2 H N CH CH NHSO.sub.2 C.sub.6 H.sub.4 -(2-CH.sub.3)8236 2-aminopyridin-6-yl-(CH.sub.2).sub.2 H CH CH N NHSO.sub.2 C.sub.6 H.sub.4 -(3-CH.sub.3)8237 2-aminopyridin-6-yl-(CH.sub.2).sub.2 H N N CH NHSO.sub.2 C.sub.6 H.sub.4 -(4-CH.sub.3)8238 2-aminopyridin-6-yl-(CH.sub.2).sub.2 CH.sub.3 CH CH N NHSO.sub.2 C.sub.6 H.sub.3 -(2,6-CH.sub.3 ).sub.28239 2-aminopyridin-6-yl-(CH.sub.2).sub.2 H CH CH N NHSO.sub.2 C.sub.6 H.sub.2 -(2,4,6-CH.sub .3).sub.38240 2-aminopyridin-6-yl-(CH.sub.2).sub.2 CH.sub.3 CH CH N NHSO.sub.2 (2-pyridyl)8241 2-aminopyridin-6-yl-(CH.sub.2).sub.2 H N CH CH NHSO.sub.2 (3-pyridyl)8242 2-aminopyridin-6-yl-(CH.sub.2).sub.2 CH.sub.3 CH CH N NHSO.sub.2 (4-pyridyl)8243 2-aminopyridin-6-yl-(CH.sub.2).sub.2 H N N CH NHSO.sub.2 (2-thienyl)8244 2-aminopyridin-6-yl-(CH.sub.2).sub.2 CH.sub.3 CH CH N NHSO.sub.2 �4-(3,5- dimethyl)isoxazolyl!8245 2-aminopyridin-6-yl-(CH.sub.2).sub.2 H CH CH N NHSO.sub.2 C.sub.6 H.sub.3 -(2,6-Cl.sub.2 )8246 2-aminopyridin-6-yl-(CH.sub.2).sub.2 CH.sub.3 CH CH N NHSO.sub.2 (2-naphthyl)8247 2-aminopyridin-6-yl-(CH.sub.2).sub.2 H CH CH N NHSO.sub.2 (1-naphthyl)8248 2-aminopyridin-6-yl-(CH.sub.2).sub.2 CH.sub.3 CH CH N NHSO.sub.2 C.sub.6 H.sub.4 -(4-Ph)8249 2-aminopyridin-6-yl-(CH.sub.2).sub.2 H CH CH N NHSO.sub.2 C.sub.6 H.sub.2 -(4-Ph-2,6- dimethyl)8250 2-aminopyridin-6-yl-(CH.sub.2).sub.2 H CH CH N NHSO.sub.2 C.sub.6 H.sub.2 -(4-Ph-2,6- dichloro)8251 2-aminopyridin-6-yl-(CH.sub.2).sub.2 CH.sub.3 CH CH N NHSO.sub.2 C.sub.6 H.sub.4 -4-(4-pyridyl) O8252 2-aminopyridin-6-yl-(CH.sub.2).sub.2 CH.sub.3 CH CH N NHSO.sub.2 C.sub.6 H.sub.4 -4-(4-pyridyl) - 2,6-dimethyl8253 2-aminopyridin-6-yl-(CH.sub.2).sub.2 H N CH CH NHSO.sub.2 C.sub.6 H.sub.4 -4-(4-pyridyl) - 2,6-dichloro8254 2-aminopyridin-6-yl-(CH.sub.2).sub.2 CH.sub.3 CH CH N NHSO.sub.2 C.sub.6 H.sub.4 -4-(2-oxazolyl )8255 2-aminopyridin-6-yl-(CH.sub.2).sub.2 CH.sub.3 CH CH N NHSO.sub.2 C.sub.6 H.sub.4 -4-(2-oxazolyl )- 2,6-dimethyl8256 2-aminopyridin-6-yl-(CH.sub.2).sub.2 H CH CH N NHSO.sub.2 C.sub.6 H.sub.4 -4-(2-oxazolyl )- 2,6-dichloro8256a 2-aminopyridin-6-yl-(CH.sub.2).sub.2 CH.sub.3 CH CH N NHSO.sub.2 C.sub.6 H.sub.4 -4-(3-pyridyl) - 2,6-dimethyl8256b 2-aminopyridin-6-yl-(CH.sub.2).sub.2 H CH CH N NHSO.sub.2 C.sub.6 H.sub.4 -4-(2-furyl)-2 ,6- dimethyl8256c 2-aminopyridin-6-yl-(CH.sub.2).sub.2 H CH CH N NHSO.sub.2 C.sub.6 H.sub.4 -4-(3-furyl)-2 ,6- dimethyl8256d 2-aminopyridin-6-yl-(CH.sub.2).sub.2 CH.sub.3 CH CH N NHSO.sub.2 C.sub.6 H.sub.4 -4-(5-pyrazoly l)- 2,6-dimethyl8257 2-aminopyridin-6-yl-(CH.sub.2).sub.2 H CH CH N NHSO.sub.2 CH.sub.2 Ph8258 2-aminopyridin-6-yl-(CH.sub.2).sub.2 H N N CH NHSO.sub.2 -n-Bu8259 2-aminopyridin-6-yl-(CH.sub.2).sub.2 H CH CH N NHSO.sub.2 NHPh8260 2-aminopyridin-6-yl-(CH.sub.2).sub.2 CH.sub.3 CH N CH NHSO.sub.2 NHC.sub.6 H.sub.3 -(2,6-Me.sub .2)8261 2-aminopyridin-6-yl-(CH.sub.2).sub.2 H CH CH N NHSO.sub.2 NHC.sub.6 H.sub.2 -(2,4,6-Me.s ub.3)8262 2-aminopyridin-6-yl-(CH.sub.2).sub.2 H N CH CH NHSO.sub.2 NH(2-naphthyl)8263 2-aminopyridin-6-yl-(CH.sub.2).sub.2 CH.sub.3 CH CH N NHSO.sub.2 NH(1-naphthyl)8264 2-aminopyridin-6-yl-(CH.sub.2).sub.2 H N N CH NHSO.sub.2 NHC.sub.6 H.sub.4 -(4-Ph)8265 2-aminopyridin-6-yl-(CH.sub.2).sub.2 H CH CH N NHSO.sub.2 NHC.sub.6 H.sub.2 -(4-Ph-2,6- dimethyl)8266 2-aminopyridin-6-yl-(CH.sub.2).sub.2 CH.sub.3 CH N CH NHSO.sub.2 NHC.sub.6 H.sub.2 -(4-Ph-2,6- dichloro)8267 2-aminopyridin-6-yl-(CH.sub.2).sub.2 H CH CH N NHSO.sub.2 NHCH.sub.2 Ph8268 2-aminopyridin-6-yl-(CH.sub.2).sub.2 H N CH CH NHSO.sub.2 NH-n-Bu8269 2-aminopyridin-6-yl-(CH.sub.2).sub.2 H CH CH N NHSO.sub.2 NH-i-Bu8270 2-aminopyridin-6-yl-(CH.sub.2).sub.2 CH.sub.3 N N CH NHSO.sub.2 NH-t-Bu8271 imidazol-2-ylamino-CH.sub.2 (o-C.sub.6 H.sub.4) H CH CH N NHSO.sub.2 -(1-naphthyl)8272 imidazol-2-ylamino-CH.sub.2 (o-C.sub.6 H.sub.4) H CH CH N NHCO.sub.2 CH.sub.2 Ph8273 imidazol-2-ylamino-CH.sub.2 (o-C.sub.6 H.sub.4) H CH CH N NHSO.sub.2 C.sub.6 C.sub.2 -(2,4,6-Me.sub .3)8274 pyridin-2-ylamino-CH.sub.2 (o-C.sub.6 H.sub.4) H CH CH N NHSO.sub.2 -(1-naphthyl)8275 pyridin-2-ylamino-CH.sub.2 (o-C.sub.6 H.sub.4) H CH CH N NHCO.sub.2 CH.sub.2 Ph8276 pyridin-2-ylamino-CH.sub.2 (o-C.sub.6 H.sub.4) H CH CH N NHSO.sub.2 C.sub.6 H.sub.2 -(2,4,6-Me.sub .3)8277 imidazolin-2-ylamino-CH.sub.2 (o-C.sub.6 H.sub.4) H CH CH N NHSO.sub.2 -(1-naphthyl)8278 imidazolin-2-ylamino-CH.sub.2 (o-C.sub.6 H.sub.4) H CH CH N NHCO.sub.2 CH.sub.2 Ph8279 imidazolin-2-ylamino-CH.sub.2 (o-C.sub.6 H.sub.4) H CH CH N NHSO.sub.2 C.sub.6 C.sub.2 -(2,4,6-Me.sub .3)8280 imidazolin-2-ylamino-(m-C.sub.6 H.sub.4) H CH CH N NHSO.sub.2 -(1-naphthyl)8281 imidazolin-2-ylamino-(m-C.sub.6 H.sub.4) H CH CH N NHCO.sub.2 CH.sub.2 Ph8282 imidazolin-2-ylamino-(m-C.sub.6 H.sub.4) H CH CH N NHSO.sub.2 C.sub.6 C.sub.2 -(2,4,6-Me.sub .3)__________________________________________________________________________

Claims

1. A compound of Formula Ia: ##STR67## and pharmaceutically acceptable salt forms thereof, wherein: X.sup.1, X.sup.2, X.sup.3, and X.sup.4 are independently selected from nitrogen or carbon provided that at least two of X.sup.1, X.sup.2, X.sup.3 and X.sup.4 are carbon;

R.sup.1 is selected from: ##STR68## A and B are independently --CH.sub.2 --, --O--, --N(R.sup.2)--, or --C(.dbd.O)--;

A.sup.1 and B.sup.1 are independently --CH.sub.2 -- or --N(R.sup.3)--;

D is --N(R.sup.2)--, --O--, --S--, --C(.dbd.O)-- or --SO.sub.2 --;

E--F is --C(R.sup.4).dbd.C(R.sup.5)--, --N.dbd.C(R.sup.4)--, --C(R.sup.4).dbd.N--, or --C(R.sup.4).sub.2 C(R.sup.5).sub.2 --;

J, K, L and M are independently selected from --C(R.sup.4)--, --C(R.sup.5)-- or --N--, provided that at least one of J, K, L and M is not --N--;

R.sup.2 is selected from: H, C.sub.1 -C.sub.6 alkyl, (C.sub.1 -C.sub.6 alkyl)carbonyl, (C.sub.1 -C.sub.6 alkoxy)carbonyl; (C.sub.1 -C.sub.6 alkyl)aminocarbonyl, C.sub.3 -C.sub.6 alkenyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.4 -C.sub.11 cycloalkylalkyl, aryl, heteroaryl(C.sub.1 -C.sub.6 alkyl)carbonyl, heteroarylcarbonyl, aryl(C.sub.1 -C.sub.6 alkyl)-, (C.sub.1 -C.sub.6 alkyl)darbonyl-, arylcarbonyl, C.sub.1 -C.sub.6 alkylsulfonyl, arylsulfonyl, aryl(C.sub.1 -C.sub.6 alkyl)sulfonyl, heteroarylsulfonyl, heteroaryl(C.sub.1 -C.sub.6 alkyl)sulfonyl, aryloxycarbonyl, or aryl(C.sub.1 -C.sub.6 alkoxy)carbonyl, wherein said aryl groups are substituted with 0-2 substituents selected from the group consisting of C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, halo, CF.sub.3, and nitro;

R.sup.3 is selected from: H, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.4 -C.sub.11 cycloalkylalkyl, aryl, aryl(C.sub.1 -C.sub.6 alkyl)-, or heteroaryl(C.sub.1 -C.sub.6 alkyl)-;

R.sup.4 and R.sup.5 are independently selected from: H, C.sub.1 -C.sub.4 alkoxy, NR.sup.2 R.sup.3, halogen, NO.sub.2, CN, CF.sub.3, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 alkenyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.4 -C.sub.11 cycloalkylalkyl, aryl, aryl (C.sub.1 -C.sub.6 alkyl)-, (C.sub.1 -C.sub.6 alkyl)carbonyl, (C.sub.1 -C.sub.6 alkoxy)carbonyl, arylcarbonyl, or

alternatively, when substituents on adjacent atoms, R.sup.4 and R.sup.5 can be taken together with the carbon atoms to which they are attached to form a 5-7 membered carbocyclic or 5-7 membered heterocyclic aromatic or non-aromatic ring system, said carbocyclic or heterocyclic ring being optionally substituted with 0-2 groups selected from: C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, halo, cyano, amino, CF.sub.3, or NO.sub.2 ;

U is selected from:

--(CH.sub.2).sub.n --,

--(CH.sub.2).sub.n (CR.sup.7 .dbd.CR.sup.8) (CH.sub.2).sub.m --,

--(CH.sub.2).sub.n (C.tbd.C) (CH.sub.2).sub.m --,

--(CH.sub.2).sub.t Q(CH.sub.2).sub.m --,

--(CH.sub.2).sub.n O(CH.sub.2).sub.m --,

--CH.sub.2).sub.n N(R.sup.6)(CH.sub.2).sub.m --,

--(CH.sub.2).sub.n C(.dbd.O)(CH.sub.2).sub.m --,

--(CH.sub.2).sub.n (C.dbd.O)N(R.sup.6)(CH.sub.2).sub.m--

--(CH.sub.2).sub.n N(R.sup.6)(C.dbd.O)(CH.sub.2).sub.m --, or

--(CH.sub.2).sub.n S(O).sub.p (CH.sub.2).sub.m --;

wherein one or more of the methylene groups in U is optionally substituted with R.sup.7 ;

Q is selected from 1,2-cycloalkylene, 1,2-phenylene, 1,3-phenylene, 1,4-phenylene, 2,3-pyridinylene, 3,4-pyridinylene, 2,4-pyridinylene, or 3,4-pyridazinylene;

R.sup.6 is selected from: H, C.sub.1 -C.sub.4 alkyl, or benzyl;

R.sup.7 and R.sup.8 are independently selected from: H, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.4 -C.sub.11 cycloalkylalkyl, aryl, aryl(C.sub.1 -C.sub.6 alkyl)-, or heteroaryl(C.sub.0 -C.sub.6 alkyl)-;

R.sup.10 is selected from: H, C.sub.1 -C.sub.4 alkoxy substituted with 0-1 R.sup.21, N(R.sup.6).sub.2, halogen, NO.sub.2, CN, CF.sub.3, CO.sub.2 R.sup.17, C(.dbd.O)R.sup.17, CONR.sup.17 R.sup.20, --SO.sub.2 R.sup.17, --SO.sub.2 NR.sup.17 R.sup.20, C.sub.1 -C.sub.6 alkyl substituted with 0-1 R.sup.15 or 0-1 R.sup.21, C.sub.3 -C.sub.6 alkenyl substituted with 0-1 R.sup.15 or 0-1 R.sup.21, C.sub.3 -C.sub.7 cycloalkyl substituted with 0-1 R.sup.15 or 0-1 R.sup.21, C.sub.1 -C.sub.11 cycloalkylalkyl substituted with 0-1 R.sup.15 or 0-1 R.sup.21, aryl substituted with 0-1 R.sup.15 or 0-2 R.sup.11 or 0-1 R.sup.21, or aryl(C.sub.1 -C.sub.6 alkyl)- substituted with 0-1 R.sup.15 or 0-2 R.sup.11 or 0-1 R.sup.21 ;

R.sup.11 is selected from H, halogen, CF.sub.3, CN, NO.sub.2, hydroxy, NR.sup.2 R.sup.3, C.sub.1 -C.sub.4 alkyl substituted with 0-1 R.sup.21, C.sub.1 -C.sub.4 alkoxy substituted with 0-1 R.sup.21, aryl substituted with 0-1 R.sup.21, aryl(C.sub.1 -C.sub.6 alkyl)- substituted with 0-1 R.sup.21, (C.sub.1 -C.sub.4 alkoxy)carbonyl substituted with 0-1 R.sup.21, (C.sub.1 -C.sub.4 alkyl)carbonyl substituted with 0-1 R.sup.21, C.sub.1 -C.sub.4 alkylsulfonyl substituted with 0-1 R.sup.21, or C.sub.1 -C.sub.4 alkylaminosulfonyl substituted with 0-1 R.sup.21 ;

W is selected from:

--(C(R.sup.12).sub.2).sub.q C(.dbd.O)N(R.sup.13)--, or

C(.dbd.O)--N(R.sup.13)--(C(R.sup.12).sub.2).sub.q --;

X is --C(R.sup.12)(R.sup.14)--C(R.sup.12)(R.sup.15)--; or

alternatively, W and X can be taken together to be ##STR69## R.sup.12 is selected from H, halogen, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkynyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.4 -C.sub.10 cycloalkylalkyl, (C.sub.1 -C.sub.4 alkyl)carbonyl, aryl, or aryl(C.sub.1 -C.sub.6 alkyl)-;

R.sup.13 is selected from H, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.7 cycloalkylmethyl, or aryl(C.sub.1 -C.sub.6 alkyl)-;

R.sup.14 is selected from:

H, C.sub.1 -C.sub.6 alkylthio(C.sub.1 -C.sub.6 alkyl)-, aryl(C.sub.1 -C.sub.10 alkylthioalkyl)-, aryl(C.sub.1 -C.sub.10 alkoxyalkyl)-, C.sub.1 -C.sub.10 alkyl, C.sub.1 -C.sub.10 alkoxyalkyl, C.sub.1 -C.sub.6 hydroxyalkyl, C.sub.2 -C.sub.10 alkenyl, C.sub.2 -C.sub.10 alkynyl, C.sub.3 -C.sub.10 cycloalkyl, C.sub.3 -C.sub.10 cycloalkylalkyl, aryl(C.sub.1 -C.sub.6 alkyl)-, heteroaryl(C.sub.1 -C.sub.6 alkyl)-, aryl, heteroaryl, CO.sub.2 R.sup.17, C(.dbd.O)R.sup.17, or CONR.sup.17 R.sup.20, provided that any of the above alkyl, cycloalkyl, aryl or heteroaryl groups may be unsubstituted or substituted independently with 0-1 R.sup.16 or 0-2 R.sup.11 ;

R.sup.15 is selected from:

H, R.sup.16, C.sub.1 -C.sub.10 alkyl, C.sub.1 -C.sub.10 alkoxyalkyl, C.sub.1 -C.sub.10 alkylaminoalkyl, C.sub.1 -C.sub.10 dialkylaminoalkyl, (C.sub.1 -C.sub.10 alkyl)carbonyl, aryl(C.sub.0 -C.sub.6 alkyl)carbonyl, C.sub.1 -C.sub.10 alkenyl, C.sub.1 -C.sub.10 alkynyl, C.sub.3 -C.sub.10 cycloalkyl, C.sub.3 -C.sub.10 cycloalkylalkyl, aryl(C.sub.1 -C.sub.6 alkyl)-, heteroaryl(C.sub.1 -C.sub.6 alkyl)-, aryl, heteroaryl, CO.sub.2 R.sup.17, C(.dbd.O)R.sup.17, CONR.sup.17 R.sup.20, SO.sub.2 R.sup.17, or SO.sub.2 NR.sup.17 R.sup.20, provided that any of the above alkyl, cycloalkyl, aryl or heteroaryl groups may be unsubstituted or substituted independently with 0-2 R.sup.11 ;

Y is selected from:

--COR.sup.19, --SO.sub.3 H, --PO.sub.3 H, tetrazolyl, --CONHNHSO.sub.2 CF.sub.3, --CONHSO.sub.2 R.sup.17, --CONHSO.sub.2 NHR.sup.17, --NHCOCF.sub.3, --NHCONHSO.sub.2 R.sup.17, --NHSO.sub.2 R.sup.17, --OP).sub.3 H.sub.2, --OSO.sub.3 H, --PO.sub.3 H.sub.2, --SO.sub.3 H, --SO.sub.2 NHCOR.sup.17, --SO.sub.2 NHCO.sub.2 R.sup.17, ##STR70## R.sup.16 is selected from: --N(R.sup.20)--C(.dbd.O)--O--R.sup.17,

--N(R.sup.20)--C(.dbd.O)--R.sup.17,

--N(R.sup.20)--C(.dbd.O)--NH--R.sup.17,

--N(R.sup.20)SO.sub.2 --R--R.sup.17, or

--N(R.sup.20)SO.sub.2 --NR.sup.20 R.sup.17 ;

R.sup.17 is selected from:

C.sub.1 -C.sub.10 alkyl, C.sub.3 -C.sub.11 cycloalkyl, aryl(C.sub.1 -C.sub.6 alkyl)-, (C.sub.1 -C.sub.6 alkyl)aryl, heteroaryl(C.sub.1 -C.sub.6 alkyl)-, (C.sub.1 -C.sub.6 alkyl)heteroaryl, biaryl(C.sub.1 -C.sub.6 alkyl)-, heteroaryl, or aryl, wherein said aryl or heteroaryl groups are optionally substituted with 0-3 substituents selected from the group consisting of: C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, aryl, heteroaryl, halo, cyano, amino, CF.sub.3, and NO.sub.2 ;

R.sup.18 is selected from:

H,

--C(.dbd.O)--O--R.sup.17,

--C(.dbd.O)--R.sup.17,

--C(.dbd.O)--NH--R.sup.17,

--SO.sub.2 --R.sup.17, or

--SO.sub.2 --NR.sup.20 R.sup.17 ;

R.sup.19 is selected from: hydroxy, C.sub.1 -C.sub.10 alkyloxy, C.sub.3 -C.sub.11 cycloalkyloxy, aryloxy, aryl(C.sub.1 -C.sub.6 alkoxy)-, C.sub.3 -C.sub.10 alkylcarbonyloxyalkyloxy, C.sub.3 -C.sub.10 alkoxycarbonyloxyalkyloxy, C.sub.2 -C.sub.10 alkoxycarbonylalkyloxy, C.sub.5 -C.sub.10 cycloalkylcarbonyloxyalkyloxy, C.sub.5 -C.sub.10 cycloalkoxycarbonyloxyalkyloxy, C.sub.5 -C.sub.10 cycloalkoxycarbonylalkyloxy, C.sub.7 -C.sub.11 aryloxycarbonylalkyloxy, C.sub.8 -C.sub.12 aryloxycarbonyloxyalkyloxy, C.sub.8 -C.sub.12 arylcarbonyloxyalkyloxy, C.sub.5 -C.sub.10 alkoxyalkylcarbonyloxyalkyloxy, C.sub.5 -C.sub.10 (5-alkyl-1,3-dioxa-cyclopenten-2-one-yl)methyloxy, C.sub.10 -C.sub.14 (5-aryl-1,3-dioxa-cyclopenten-2-one-yl)methyloxy, or (R.sup.11)(R.sup.12)N--(C.sub.1 -C.sub.10 alkoxy)-;

R.sup.20 is selected from: H, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.4 -C.sub.11 cycloalkylalkyl, aryl, aryl(C.sub.1 -C.sub.6 alkyl)-, or heteroaryl (C.sub.1 -C.sub.6 alkyl)-;

R.sup.21 is selected from: COOH or NR.sup.6.sub.2 ;

m is 0-4;

n is 0-4;

t is 0-4;

p is 0-2;

q is 0-2; and

r is 0-2;

with the following provisos:

(1) t, n, m and q are chosen such that the number of atoms connecting R.sup.1 and Y is in the range of 10-14; and

(2) n and m are chosen such that the value of n plus m is greater than one unless U is --(CH.sub.2).sub.t Q(CH.sub.2).sub.m --.

2. A compound of claim 1 of the Formula Ia: ##STR71## and pharmaceutically acceptable salt forms thereof, wherein: X.sup.1, X.sup.2, X.sup.3, and X.sup.4 are independently selected from nitrogen or carbon provided that at least two of X.sup.1, X.sup.2, X.sup.3 and X.sup.4 are carbon;

R.sup.1 is selected from: ##STR72## A and B are independently --CH.sub.2 --, --O--, --N(R.sup.2)--, or --C(.dbd.O)--;

A.sup.1 and B.sup.1 are independently --CH.sub.2 -- or --N(R.sup.3)--;

D is --N(R.sup.2)--, --O--, --S--, --C(.dbd.)-- or --SO.sub.2 --;

E--F is --C(R.sup.4).dbd.C(R.sup.5)--, --N.dbd.C(R.sup.4)--, --C(R.sup.4).dbd.N--, or --C(R.sup.4).sub.2 C(R.sup.5).sub.2 --;

J, K, L and M are independently selected from --C(R.sup.4)--, --C(R.sup.5)-- or --N--, provided that at least one of J, K, L and M is not --N--;

R.sup.2 is selected from: H, C.sub.1 -C.sub.6 alkyl, (C.sub.1 -C.sub.6 alkyl)carbonyl, (C.sub.1 -C.sub.6 alkoxy)carbonyl, C.sub.1 -C.sub.6 alkylaminocarbonyl, C.sub.3 -C.sub.6 alkenyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.4 -C.sub.11 cycloalkylalkyl, aryl, heteroaryl(C.sub.1 -C.sub.6 alkyl)carbonyl, heteroarylcarbonyl, aryl(C.sub.1 -C.sub.6 alkyl)-, (C.sub.1 -C.sub.6 alkyl)carbonyl, arylcarbonyl, alkylsulfonyl, arylsulfonyl, aryl(C.sub.1 -C.sub.6 alkyl)sulfonyl, heteroarylsulfonyl, heteroaryl(C.sub.1 -C.sub.6 alkyl)sulfonyl, aryloxycarbonyl, or aryl(C.sub.1 -C.sub.6 alkoxy)carbonyl, wherein said aryl groups are substituted with 0-2 substituents selected from the group consisting of C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, halo, CF.sub.3, and nitro;

R.sup.3 is selected from: H, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.4 -C.sub.11 cycloalkylalkyl, aryl, aryl (C.sub.1 -C.sub.6 alkyl)-, or heteroaryl(C.sub.1 -C.sub.6 alkyl)-;

R.sup.4 and R.sup.5 are independently selected from: H, C.sub.1 -C.sub.4 alkoxy, NR.sup.2 R.sup.3, halogen, NO.sub.2, CN, CF.sub.3, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 alkenyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.4 -C.sub.11 cycloalkylalkyl, aryl, aryl(C.sub.1 -C.sub.6 alkyl)-, C.sub.2 -C.sub.7 alkylcarbonyl, arylcarbonyl or

alternatively, when substituents on adjacent atoms, R.sup.4 and R.sup.5 can be taken together with the carbon atoms to which they are attached to form a 5-7 membered carbocyclic or 5-7 membered heterocyclic aromatic or non-aromatic ring system, said carbocyclic or heterocyclic ring being optionally substituted with 0-2 groups selected from: C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, halo, cyano, amino, CF.sub.3, or NO.sub.2 ;

U is selected from:

--(CH.sub.2).sub.n --,

--(CH.sub.2).sub.n (CR.sup.7 .dbd.CR.sup.8)(CH.sub.2).sub.m --,

--(CH.sub.2).sub.t Q(CH.sub.2).sub.m --,

--(CH.sub.2).sub.n O(CH.sub.2).sub.m --,

--(CH.sub.2).sub.n N(R.sup.6)(CH.sub.2).sub.m --,

--(CH.sub.2).sub.n C(.dbd.O)(CH.sub.2).sub.m --, or

--(CH.sub.2).sub.n S(O).sub.p (CH.sub.2).sub.m --;

wherein one or more of the methylene groups in U is optionally substituted with R.sup.7 ;

Q is selected from 1,2-phenylene, 1,3-phenylene, 2,3-pyridinylene, 3,4-pyridinylene, or 2,4-pyridinylene;

R.sup.6 is selected from: H, C.sub.1 -C.sub.4 alkyl, or benzyl;

R.sup.7 and R.sup.8 are independently selected from: H, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.1 -C.sub.11 cycloalkylalkyl, aryl, aryl(C.sub.1 -C.sub.6 alkyl)-, or heteroaryl(C.sub.0 -C.sub.6 alkyl)-;

R.sup.10 is selected from: H, C.sub.1 -C.sub.4 alkoxy substituted with 0-1 R.sup.21, N(R.sup.6).sub.2, halogen, NO.sub.2, CN, CF.sub.3, CO.sub.2 R.sup.17, C(.dbd.O)R.sup.17, CONR.sup.17 R.sup.20, --SO.sub.2 R.sup.17, --SO.sub.2 NR.sup.17 R.sup.20, C.sub.1 -C.sub.6 alkyl substituted with 0-1 R.sup.15 or 0-1 R.sup.21, C.sub.3 -C.sub.6 alkenyl substituted with 0-1 R.sup.15 or 0-1 R.sup.21, C.sub.3 -C.sub.7 cycloalkyl substituted with 0-1 R.sup.15 or 0-1 R.sup.21, C.sub.4 -C.sub.11 cycloalkylalkyl substituted with 0-1 R.sup.15 or 0-1 R.sup.21, aryl substituted with 0-1 R.sup.15 or 0-2 R.sup.11 or 0-1 R.sup.21, or aryl(C.sub.1 -C.sub.6 alkyl)- substituted with 0-1

R.sup.15 or 0-2 R.sup.11 or 0-1 R.sup.21 ;

R.sup.11 is selected from: H, halogen, CF.sub.3, CN, NO.sub.2 , hydroxy, NR.sup.2 R.sup.3, C.sub.1 -C.sub.4 alkyl substituted with 0-1 R.sup.21, C.sub.1 -C.sub.4 alkoxy substituted with 0-1 R.sup.21, aryl substituted with 0-1 R.sup.21, aryl(C.sub.1 -C.sub.6 alkyl)- substituted with 0-1 R.sup.21, (C.sub.1 -C.sub.4 alkoxy)carbonyl substituted with 0-1 R.sup.21, (C.sub.1 -C.sub.4 alkyl)carbonyl substituted with 0-1 R.sup.21, C.sub.1 -C.sub.4 alkylsulfonyl substituted with 0-1 R.sup.21, or C.sub.1 -C.sub.4 alkylaminosulfonyl substituted with 0-1 R.sup.21 ;

W is --C(.dbd.O)--N(R.sup.13)--(C(R.sup.12).sub.2).sub.2).sub.q --;

X is --C(R.sup.12)(R.sup.14)--C(R.sup.12)(R.sup.15)--;

alternatively, W and X can be taken together to be ##STR73## R.sup.12 is H or C.sub.1 -C.sub.6 alkyl; R.sup.13 is selected from: H, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.7 cycloalkylmethyl, or aryl(C.sub.1 -C.sub.6 alkyl)-;

R.sup.14 is selected from:

H, C.sub.1 -C.sub.6 alkylthioalkyl, aryl(C.sub.1 -C.sub.10 alkylthioalkyl)-, aryl(C.sub.1 -C.sub.10 alkoxyalkyl)-, C.sub.1 -C.sub.10 alkyl, C.sub.1 -C.sub.10 alkoxyalkyl, C.sub.1 -C.sub.6 hydroxyalkyl, C.sub.2 -C.sub.10 alkenyl, C.sub.2 -C.sub.10 alkynyl, C.sub.3 -C.sub.10 cycloalkyl, C.sub.3 -C.sub.10 cycloalkylalkyl, aryl(C.sub.1 -C.sub.6 alkyl)-, heteroaryl(C.sub.1 -C.sub.6 alkyl)-, aryl, heteroaryl, CO.sub.2 R.sup.17, C(.dbd.O)R.sup.17, or CONR.sup.17 R.sup.20, provided that any of the above alkyl, cycloalkyl, aryl or heteroaryl groups may be substituted independently with 0-1 R.sup.16 or 0-2 R.sup.11 ;

R.sup.15 is selected from:

H, R.sup.16, C.sub.1 -C.sub.10 alkyl, C.sub.1 -C.sub.10 alkoxyalkyl, C.sub.1 -C.sub.10 alkylaminoalkyl, C.sub.1 -C.sub.10 dialkylaminoalkyl, C.sub.1 -C.sub.10 alkylcarbonyl, aryl(C.sub.0 -C.sub.6 alkyl)carbonyl, C.sub.2 -C.sub.10 alkenyl, C.sub.2 -C.sub.10 alkynyl, C.sub.3 -C.sub.10 cycloalkyl, C.sub.3 -C.sub.10 cycloalkylalkyl, aryl(C.sub.1 -C.sub.6 alkyl)-, heteroaryl(C.sub.1 -C.sub.6 alkyl)-, aryl, heteroaryl, CO.sub.2 R.sup.17, C(.dbd.O)R.sup.17, CONR.sup.17 R.sup.20, SO.sub.2 R.sup.17 or SO.sub.2 NR.sup.17 R.sup.20, provided that any of the above alkyl, cycloalkyl, aryl or heteroaryl groups may be substituted independently with 0-2 R.sup.11 ;

Y is selected from: ##STR74## R.sup.16 is selected from: --N(R.sup.20)--C(.dbd.O)--O--R.sup.17,

--N(R.sup.20)--C(.dbd.O)--R.sup.17,

--N(R.sup.20)--C(.dbd.O)--NH--R.sup.17,

--N(R.sup.20)SO.sub.2 --R.sup.17, or

--N(R.sup.20)SO.sub.2 --NR.sup.20 R.sup.17 ;

R.sup.17 is selected from:

C.sub.1 -C.sub.10 alkyl, C.sub.3 -C.sub.11 cycloalkyl, aryl(C.sub.1 -C.sub.6 alkyl)-, (C.sub.1 -C.sub.6 alkyl)aryl, heteroaryl(C.sub.1 -C.sub.6 alkyl)-, (C.sub.1 -C.sub.6 alkyl)heteroaryl, biaryl(C.sub.1 -C.sub.6 alkyl)-, heteroaryl, or aryl, wherein said aryl or heteroaryl groups are optionally substituted with 0-3 substituents selected from the group consisting of: C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, aryl, heteroaryl, halo, cyano, amino, CF.sub.3, and NO.sub.2 ;

R.sup.18 is selected from:

H,

--C(.dbd.O)--O--R.sup.17,

--C(.dbd.O)--R.sup.17,

--C(.dbd.O)--NH--R.sup.17,

--SO.sub.2 --R.sup.17, or

--SO.sub.2 --NR.sup.20 R.sup.17 ;

R.sup.19 is selected from: hydroxy, C.sub.1 -C.sub.10 alkyloxy, C.sub.3 -C.sub.11 cycloalkyloxy, C.sub.6 -C.sub.10 aryloxy, C.sub.7 -C.sub.11 aralkyloxy, C.sub.3 -C.sub.10 alkylcarbonyloxyalkyloxy, C.sub.3 -C.sub.10 alkoxycarbonyloxyalkyloxy, C.sub.2 -C.sub.10 alkoxycarbonylalkyloxy, C.sub.5 -C.sub.10 cycloalkylcarbonyloxyalkyloxy, C.sub.5 -C.sub.10 cycloalkoxycarbonyloxyalkyloxy, C.sub.5 -C.sub.10 cycloalkoxycarbonylalkyloxy, C.sub.7 -C.sub.11 aryloxycarbonylalkyloxy, C.sub.8 -C.sub.12 aryloxycarbonyloxyalkyloxy, C.sub.8 -C.sub.12 arylcarbonyloxyalkyloxy, C.sub.5 -C.sub.10 alkoxyalkylcarbonyloxyalkyloxy, C.sub.5 -C.sub.10 (5-alkyl-1,3-dioxa-cyclopenten-2-one-yl)methyloxy, C.sub.10 -C.sub.14 (5-aryl-1,3-dioxa-cyclopenten-2-one-yl)methyloxy, or (R.sup.11)(R.sup.12)N--(C.sub.0 -C.sub.10 alkoxy)-;

R.sup.20 selected from: H, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.4 -C.sub.11 cycloalkylalkyl, aryl(C.sub.1 -C.sub.6 alkyl)-, or heteroaryl(C.sub.1 -C.sub.6 alkyl)-;

R.sup.21 is selected from COOH or NR.sup.6.sub.2 ;

m is 0-4;

n is 0-4;

p is 0-2;

q is 0-2;

t is 0-4; and

r is 0-2.

3. A compound of claim 1 of the Formula IIa or IIb: ##STR75## and pharmaceutically acceptable salt forms thereof wherein: X.sub.1 and X.sub.3 are independently selected from nitrogen or carbon;

R.sup.1 is selected from: ##STR76## wherein the above heterocycles are optionally substituted with 0-2 substituents selected from the group consisting of: NH.sub.2, halogen, NO.sub.2, CN, CF.sub.3, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.6 alkyl, and C.sub.3 -C.sub.7 cycloalkyl;

U is --(CH.sub.2).sub.n --, --(CH.sub.2).sub.t Q(CH.sub.2).sub.m -- or --C(.dbd.O)(CH.sub.2).sub.n-1 --, wherein one of the methylene groups is optionally substituted with R.sup.7 ;

Q is selected from 1,2-phenylene, 1,3-phenylene, 2,3-pyridinylene, 3,4-pyridinylene, or 2,4-pyridinylene;

R.sup.6 is selected from: H, C.sub.1 -C.sub.4 alkyl, or benzyl;

R.sup.7 is selected from: C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.4 -C.sub.11 cycloalkylalkyl, aryl, aryl(C.sub.1 -C.sub.6 alkyl), heteroaryl, or heteroaryl(C.sub.1 -C.sub.6 alkyl);

R.sup.10 is selected from: H, C.sub.1 -C.sub.4 alkoxy substituted with 0-1 R.sup.21, halogen, CO.sub.2 R.sup.17, CONR.sup.17 R.sup.20, C.sub.1 -C.sub.6 alkyl substituted with 0-1 R.sup.15 or 0-1 R.sup.21, C.sub.3 -C.sub.7 cycloalkyl substituted with 0-1 R.sup.15 or 0-1 R.sup.21, C.sub.4 -C.sub.11 cycloalkylalkyl substituted with 0-1 R.sup.15 or 0-1 R.sup.21, or aryl(C.sub.1 -C.sub.6 alkyl)- substituted with 0-1 R.sup.15 or 0-2 R.sup.11 or 0-1 R.sup.21 ;

R.sup.11 is selected from: H, halogen, CF.sub.3, CN, NO.sub.2, hydroxy, NR.sup.2 R.sup.3, C.sub.1 -C.sub.4 alkyl substituted with 0-1 R.sup.21, C.sub.1 -C.sub.4 alkoxy substituted with 0-1 R.sup.21 aryl substituted with 0-1 R.sup.21, aryl(C.sub.1 -C.sub.6 alkyl)- substituted with 0-1 R.sup.21, (C.sub.1 -C.sub.4 alkoxy)carbonyl substituted with 0-1 R.sup.21, (C.sub.1 -C.sub.4 alkyl)carbonyl substituted with 0-1 R.sup.21, C.sub.1 -C.sub.4 alkylsulfonyl substituted with 0-1 R.sup.21, or C.sub.1 -C.sub.4 alkylaminosulfonyl substituted with 0-1 R.sup.21 ;

W is --C(.dbd.O)--N(R.sup.13)--;

X is --CH(R.sup.14)--CH(R.sup.15)--;

R.sup.13 is H or CH.sub.3 ;

R.sup.14 is selected from:

H, C.sub.1 -C.sub.10 alkyl, aryl, or heteroaryl, wherein said aryl or heteroaryl groups are optionally substituted with 0-3 substituents selected from the group consisting of: C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, aryl, halo, cyano, amino, CF.sub.3, and NO.sub.2 ;

R.sup.15 is H or R.sup.16 ;

Y is --COR.sup.19 ;

R.sup.16 is selected from:

--NH(R.sup.20)--C(.dbd.O)--O--R.sup.17,

--N(R.sup.20)--C(.dbd.O)--R.sup.17,

--N(R.sup.20)--C(.dbd.O)--NH--R.sup.17,

--N(R.sup.20)SO.sub.2 --R.sup.17, or

--N(R.sup.20)SO.sub.2 --N(R.sup.20)R.sup.17 ;

R.sup.17 is selected from:

C.sub.1 -C.sub.10 alkyl, C.sub.3 -C.sub.11 cycloalkyl, aryl(C.sub.1 -C.sub.6 alkyl)-, (C.sub.1 -C.sub.6 alkyl)aryl, heteroaryl(C.sub.1 -C.sub.6 alkyl)-, (C.sub.1 -C.sub.6 alkyl)heteroaryl, biaryl(C.sub.1 -C.sub.6 alkyl)-, heteroaryl, or aryl, wherein said aryl or heteroaryl groups are optionally substituted with 0-3 substituents selected from the group consisting of: C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, aryl, heteroaryl, halo, cyano, amino, CF.sub.3, and NO.sub.2 ;

R.sup.19 is selected from:

hydroxy, C.sub.1 -C.sub.10 alkoxy,

methylcarbonyloxymethoxy-,

ethylcarbonyloxymethoxy-,

t-butylcarbonyloxymethoxy-,

cyclohexylcarbonyloxymethoxy-,

1-(methylcarbonyloxy)ethoxy-,

1-(ethylcarbonyloxy)ethoxy-,

1-(t-butylcarbonyloxy)ethoxy-,

1-(cyclohexylcarbonyloxy)ethoxy-,

i-propyloxycarbonyloxymethoxy-,

t-butyloxycarbonyloxymethoxy-,

1-(i-propyloxycarbonyloxy)ethoxy-,

1-(cyclohexyloxycarbonyloxy)ethoxy-,

1-(t-butyloxycarbonyloxy)ethoxy-,

dimethylaminoethoxy-,

diethylaminoethoxy-,

(5-methyl-1,3-dioxacyclopenten-2-on-4-yl)methoxy-,

(5-(t-butyl)-1,3-dioxacyclopenten-2-on-4-yl)methoxy-,

(1,3-dioxa-5-phenyl-cyclopenten-2-on-4-yl)methoxy-, or

1-(2-(2-methoxypropyl)carbonyloxy)ethoxy-;

R.sup.20 is H or CH.sub.3 ;

R.sup.21 is selected from COOH or NR.sup.6.sub.2 ;

m is 0 or 1;

n is 1-4; and

t is 0 or 1.

4. A compound of claim 1 of the Formula IIa or IIb: ##STR77## and pharmaceutically acceptable salt forms thereof wherein: X.sub.1 and X.sub.3 are independently selected from nitrogen or carbon, provided that at least one of X.sub.1 and X.sub.3 is carbon;

R.sup.1 is selected from: ##STR78## wherein the above heterocycles are optionally substituted with 0-2 substituents selected from the group consisting of: NH.sub.2, halogen, NO.sub.2, CN, CF.sub.3, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.6 alkyl, and C.sub.3 -C.sub.7 cycloalkyl;

U is --(CH.sub.2).sub.n --, --(CH.sub.2).sub.t Q(CH.sub.2).sub.m -- or --C(.dbd.O)(CH.sub.2).sub.n-1, wherein one of the methylene groups is optionally substituted with R.sup.7 ;

Q is selected from 1,2-phenylene, 1,3-phenylene, 2,3-pyridinylene, 3 4-pyridinylene, or 2,4-pyridinylene;

R.sup.6 is selected from: H, C.sub.1 -C.sub.4 alkyl, or benzyl;

R.sup.7 is selected from: C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.4 -C.sub.11 cycloalkylalkyl, aryl, aryl(C.sub.1 -C.sub.6 alkyl), heteroaryl, or heteroaryl(C.sub.1 -C.sub.6 alkyl);

R.sup.10 is selected from: H, C.sub.1 -C.sub.4 alkoxy substituted with 0-1 R.sup.21, halogen, CO.sub.2 R.sup.17, CONR.sup.17 R.sup.20, C.sub.1 -C.sub.6 alkyl substituted with 0-1 R.sup.15 or 0-1 R.sup.21, C.sub.3 -C.sub.7 cycloalkyl substituted with 0-1 R.sup.15 or 0-1 R.sup.21, C.sub.4 -C.sub.11 cycloalkylalkyl substituted with 0-1 R.sup.15 or 0-1 R.sup.21, or aryl(C.sub.1 -C.sub.6 alkyl)- substituted with 0-1 R.sup.15 or 0-2 R.sup.11 or 0-1 R.sup.21 ;

R.sup.11 is selected from: H, halogen, CF.sub.3, CN, NO.sub.2, hydroxy, NR.sup.2 R.sup.3, C.sub.1 -C.sub.4 alkyl substituted with 0-1 R.sup.21, C.sub.1 -C.sub.4 alkoxy substituted with 0-1 R.sup.21, aryl substituted with 0-1 R.sup.21 aryl(C.sub.1 -C.sub.6 alkyl)- substituted with 0-1 R.sup.21, (C.sub.1 -C.sub.4 alkoxy)carbonyl substituted with 0-1 R.sup.21, (C.sub.1 -C.sub.4 alkyl)carbonyl substituted with 0-1 R.sup.21, C.sub.1 -C.sub.4 alkylsulfonyl substituted with 0-1 R.sup.21, or C.sub.1 -C.sub.4 alkylaminosulfonyl substituted with 0-1 R.sup.21 ; W is --C(.dbd.O)--N(R.sup.13)--;

W is --C(.dbd.O)--N(R.sup.13)--;

X is --CH(R.sup.14)--CH(R.sup.15)--;

R.sup.13 is H or CH.sub.3 ;

R.sup.14 is selected from:

H, C.sub.1 -C.sub.10 alkyl, aryl, or heteroaryl, wherein said aryl or heteroaryl groups are optionally substituted with 0-3 substituents selected from the group consisting of: C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, aryl, halo, cyano, amino, CF.sub.3, and NO.sub.2 ;

R.sup.15 is H or R.sup.16 ;

Y is --COR.sup.19 ;

R.sup.16 is selected from:

--N(R.sup.20)--C(.dbd.O)--O--R.sup.17,

--N(R.sup.20)--C(.dbd.O)--R.sup.17,

--N(R.sup.20)--C(.dbd.O)--NH--R.sup.17,

--N(R.sup.20)SO.sub.2 --R.sup.17, or

--N(R.sup.20)SO.sub.2 --NR.sup.20 R.sup.17 ;

R.sup.17 is selected from:

C.sub.1 -C.sub.10 alkyl, C.sub.3 -C.sub.11 cycloalkyl, aryl(C.sub.1 -C.sub.6 alkyl)-, (C.sub.1 -C.sub.6 alkyl)aryl, heteroaryl(C.sub.1 -C.sub.6 alkyl)-, (C.sub.1 -C.sub.6 alkyl)heteroaryl, biaryl(C.sub.1 -C.sub.6 alkyl)-, heteroaryl, or aryl, wherein said aryl or heteroaryl groups are optionally substituted with 0-3 substituents selected from the group consisting of: C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, aryl, heteroaryl, halo, cyano, amino, CF.sub.3, and NO.sub.2 ;

R.sup.19 is selected from:

hydroxy, C.sub.1 -C.sub.10 alkoxy,

methylcarbonyloxymethoxy-,

ethylcarbonyloxymethoxy-,

t-butylcarbonyloxymethoxy-,

cyclohexylcarbonyloxymethoxy-,

1-(methylcarbonyloxy)ethoxy-,

1-(ethylcarbonyloxy)ethoxy-,

1-(t-butylcarbonyloxy)ethoxy-,

1-(cyclohexylcarbonyloxy)ethoxy-,

i-propyloxycarbonyloxymethoxy-,

t-butyloxycarbonyloxymethoxy-,

1-(i-propyloxycarbonyloxy)ethoxy-,

1-(cyclohexyloxycarbonyloxy)ethoxy-,

1-(t-butyloxycarbonyloxy)ethoxy-,

dimethylaminoethoxy-,

diethylaminoethoxy-,

(5-methyl-1,3-dioxacyclopenten-2-on-4-yl)methoxy-,

(5-(t-butyl)-1,3-dioxacyclopenten-2-on-4-yl)methoxy-,

(1,3-dioxa-5-phenyl-cyclopenten-2-on-4-yl)methoxy-, or

1-(2-(2-methoxypropyl)carbonyloxy)ethoxy-;

R.sup.20 is H or CH.sub.3 ;

R.sup.21 is selected from COOH or NR.sup.6.sub.2 ;

m is 0 or 1;

n is 1-4; and

t is 0 or 1.

5. A compound of claim 1 of Formula Ia and enantiomeric or diasteriomeric forms thereof, and mixtures of enantiomeric or diasteriomeric forms thereof, and pharmaceutically acceptable salt forms thereof, selected from the group consisting of:

3-�1-�3-(imidazolin-2-ylamino)propyl!indazol-5-ylcarbonylamino!-2-(benzyloxycarbonylamino)propionic acid,

3-�1-�3-(imidazolin-2-ylamino)propyl!indazol-5-ylcarbonylamino!-2-(2,4,6-trimethylbenzenesulfonylamino)propionic acid,

3-�1-�3-(imidazolin-2-ylamino)propyl!indazol-5-ylcarbonylamino!-2-(benzenesulfonylamino)propionic acid,

3-�1-�3-(imidazolin-2-ylamino)propyl!indazol-5-ylcarbonylamino!-2-(2,6-dichlorobenzenesulfonylamino)propionic acid,

3-�1-�3-(imidazolin-2-ylamino)propyl!indazol-5-ylcarbonylamino!-2-(3,5-dimethylisoxazol-4-ylsulfonylamino)propionic acid,

3-�1-�3-(imidazolin-2-ylamino)propyl!indazol-5-ylcarbonylamino!-2-(2,6-dimethylbenzenesulfonylamino)propionic acid,

3-�1-�3-(imidazolin-2-ylamino)propyl!indazol-5-ylcarbonylamino!-2-(2,6-dimethyl-4-phenylbenzenesulfonylamino)propionic acid,

3-�1-�3-(imidazolin-2-ylamino)propyl!indazol-5-ylcarbonylamino!-2-(4-phenylbenzenesulfonylamino)propionic acid,

3-�1-�3-(tetrahydropyrimid-2-ylamino)propyl!indazol-5-ylcarbonylamino!-2-(benzyloxycarbonylamino)propionic acid,

3-�1-�3-(tetrahydropyrimid-2-ylamino)propyl!indazol-5-ylcarbonylamino!-2-(2,4,6-trimethylbenzenesulfonylamino)propionic acid,

3-�1-�3-(tetrahydropyrimid-2-ylamino)propyl!indazol-5-ylcarbonylamino!-2-(benzenesulfonylamino)propionic acid,

3-�1-�3-(tetrahydropyrimid-2-ylamino)propyl!indazol-5-ylcarbonylamino!-2-(2,6-dichlorobenzenesulfonylamino)propionic acid,

3-�1-�3-(tetrahydropyrimid-2-ylamino)propyl!indazol-5-ylcarbonylamino!-2-(3,5-dimethylisoxazol-4-ylsulfonylamino)propionic acid,

3-�1-�3-(tetrahydropyrimid-2-ylamino)propyl!indazol-5-ylcarbonylamino!-2-(2,6-dimethylbenzenesulfonylamino)propionic acid,

3-�1-�3-(tetrahydropyrimid-2-ylamino)propyl!indazol-5-ylcarbonylamino!-2-(2,6-dimethyl-4-phenylbenzenesulfonylamino)propionic acid,

3-�1-�3-(tetrahydropyrimid-2-ylamino)propyl!indazol-5-ylcarbonylamino!-2-(4-phenylbenzenesulfonylamino)propionic acid,

3-�1-�3-(imidazol-2-ylamino)propyl!indazol-5-ylcarbonylamino!-2-(benzyloxycarbonylamino)propionic acid,

3-�1-�3-(imidazol-2-ylamino)propyl!indazol-5-ylcarbonylamino!-2-(2,4,6-trimethylbenzenesulfonylamino)propionic acid,

3-�1-�3-(imidazol-2-ylamino)propyl!indazol-5-ylcarbonylamino!-2-(benzenesulfonylamino)propionic acid,

3-�1-�3-(imidazol-2-ylamino)propyl!indazol-5-ylcarbonylamino!-2-(2,6-dichlorobenzenesulfonylamino)propionic acid,

3-�1-�3-(imidazol-2-ylamino)propyl!indazol-5-ylcarbonylamino!-2-(3,5-dimethylisoxazol-4-ylsulfonylamino)propionic acid,

3-�1-�3-(imidazol-2-ylamino)propyl!indazol-5-ylcarbonylamino!-2-(2,6-dimethylbenzenesulfonylamino)propionic acid,

3-�1-�3-(imidazol-2-ylamino)propyl!indazol-5-ylcarbonylamino!-2-(2,6-dimethyl-4-phenylbenzenesulfonylamino)propionic acid,

3-�1-�3-(imidazol-2-ylamino)propyl!indazol-5-ylcarbonylamino!-2-(4-phenylbenzenesulfonylamino)propionic acid,

3-�1-�3-(pyridin-2-ylamino)propyl!indazol-5-ylcarbonylamino!-2-(benzyloxycarbonylamino)propionic acid,

3-�1-�3-(pyridin-2-ylamino)propyl!indazol-5-ylcarbonylamino!-2-(2,4,6-trimethylbenzenesulfonylamino)propionic acid,

3-�1-�3-(pyridin-2-ylamino)propyl!indazol-5-ylcarbonylamino!-2-(benzenesulfonylamino)propionic acid,

3-�1-�3-(pyridin-2-ylamino)propyl!indazol-5-ylcarbonylamino!-2-(2,6-dichlorobenzenesulfonylamino)propionic acid,

3-�1-�3-(pyridin-2-ylamino)propyl!indazol-5-ylcarbonylamino!-2-(3,5-dimethylisoxazol-4-ylsulfonylamino)propionic acid,

3-�1-�3-(pyridin-2-ylamino)propyl!indazol-5-ylcarbonylamino!-2-(2,6-dimethylbenzenesulfonylamino)propionic acid,

3-�1-�3-(pyridin-2-ylamino)propyl!indazol-5-ylcarbonylamino!-2-(2,6-dimethyl-4-phenylbenzenesulfonylamino)propionic acid,

3-�1-�3-(pyridin-2-ylamino)propyl!indazol-5-ylcarbonylamino!-2-(4-phenylbenzenesulfonylamino)propionic acid,

3-�1-�3-(imidazolin-2-ylamino)propyl!indazol-4-ylcarbonylamino!-2-(benzyloxycarbonylamino)propionic acid,

3-�1-�3-(imidazolin-2-ylamino)propyl!indazol-4-ylcarbonylamino!-2-(2,4,6-trimethylbenzenesulfonylamino)propionic acid,

3-�1-�3-(imidazolin-2-ylamino)propyl!indazol-4-ylcarbonylamino!-2-(benzenesulfonylamino)propionic acid,

3-�1-�3-(imidazolin-2-ylamino)propyl!indazol-4-ylcarbonylamino!-2-(2,6-dichlorobenzenesulfonylamino)propionic acid,

3-�1-�3-(imidazolin-2-ylamino)propyl!indazol-4-ylcarbonylamino!-2-(3,5-dimethylisoxazol-4-ylsulfonylamino)propionic acid,

3-�1-�3-(imidazolin-2-ylamino)propyl!indazol-4-ylcarbonylamino!-2-(2,6-dimethylbenzenesulfonylamino)propionic acid,

3-�1-�3-(imidazolin-2-ylamino)propyl!indazol-4-ylcarbonylamino!-2-(2,6-dimethyl-4-phenylbenzenesulfonylamino)propionic acid,

3-�1-�3-(imidazolin-2-ylamino)propyl!indazol-4-ylcarbonylamino!-2-(4-phenylbenzenesulfonylamino)propionic acid,

3-�1-�3-(tetrahydropyrimid-2-ylamino)propyl!indazol-4-ylcarbonylamino!-2-(benzyloxycarbonylamino)propionic acid,

3-�1-�3-(tetrahydropyrimid-2-ylamino)propyl!indazol-4-ylcarbonylamino!-2-(2,4,6-trimethylbenzenesulfonylamino)propionic acid,

3-�1-�3-(tetrahydropyrimid-2-ylamino)propyl!indazol-4-ylcarbonylamino!-2-(benzenesulfonylamino)propionic acid,

3-�1-�3-(tetrahydropyrimid-2-ylamino)propyl!indazol-4-ylcarbonylamino!-2-(2,6-dichlorobenzenesulfonylamino)propionic acid,

3-�1-�3-(tetrahydropyrimid-2-ylamino)propyl!indazol-4-ylcarbonylamino!-2-(3,5-dimethylisoxazol-4-ylsulfonylamino)propionic acid,

3-�1-�3-(tetrahydropyrimid-2-ylamino)propyl!indazol-4-ylcarbonylamino!-2-(2,6-dimethylbenzenesulfonylamino)propionic acid,

3-�1-�3-(tetrahydropyrimid-2-ylamino)propyl!indazol-4-ylcarbonylamino!-2-(2,6-dimethyl-4-phenylbenzenesulfonylamino)propionic acid,

3-�1-�3-(tetrahydropyrimid-2-ylamino)propyl!indazol-4-ylcarbonylamino!-2-(4-phenylbenzenesulfonylamino)propionic acid,

3-1-�3-(imidazol-2-ylamino)propyl!indazol-4-ylcarbonylamino!-2-(benzyloxycarbonylamino)propionic acid,

3-�1-�3-(imidazol-2-ylamino)propyl!indazol-4-ylcarbonylamino!-2-(2,4,6-trimethylbenzenesulfonylamino)propionic acid,

3-1-�3-(imidazol-2-ylamino)propyl!indazol-4-ylcarbonylamino!-2-(benzenesulfonylamino)propionic acid,

3-1-�3-(imidazol-2-ylamino)propyl!indazol-4-ylcarbonylamino!-2-(2,6-dichlorobenzenesulfonylamino)propionic acid,

3-�1-�3-(imidazol-2-ylamino)propyl!indazol-4-ylcarbonylamino!-2-(3,5-dimethylisoxazol-4-ylsulfonylamino)propionic acid,

3-�1-�3-(imidazol-2-ylamino)propyl!indazol-4-ylcarbonylamino!-2-(2,6-dimethylbenzenesulfonylamino)propionic acid,

3-�1-�3-(imidazol-2-ylamino)propyl!indazol-4-ylcarbonylamino!-2-(2,6-dimethyl-4-phenylbenzenesulfonylamino)propionic acid,

3-�1-�3-(imidazol-2-ylamino)propyl!indazol-4-ylcarbonylamino!-2-(4-phenylbenzenesulfonylamino)propionic acid,

3-�1-�3-(pyridin-2-ylamino)propyl!indazol-4-ylcarbonylamino!-2-(benzyloxycarbonylamino)propionic acid,

3-�1-�3-(pyridin-2-ylamino)propyl!indazol-4-ylcarbonylamino!-2-(2,4,6-trimethylbenzenesulfonylamino)propionic acid,

3-�1-�3-(pyridin-2-ylamino)propyl!indazol-4-ylcarbonylamino!-2-(benzenesulfonylamino)propionic acid,

3-�1-�3-(pyridin-2-ylamino)propyl!indazol-4-ylcarbonylamino!-2-(2,6-dichlorobenzenesulfonylamino)propionic acid,

3-�1-�3-(pyridin-2-ylamino)propyl!indazol-4-ylcarbonylamino!-2-(3,5-dimethylisoxazol-4-ylsulfonylamino)propionic acid,

3-�1-�3-(pyridin-2-ylamino)propyl!indazol-4-ylcarbonylamino!-2-(2,6-dimethylbenzenesulfonylamino)propionic acid,

3-�1-�3-(pyridin-2-ylamino)propyl!indazol-4-ylcarbonylamino!-2-(2,6-dimethyl-4-phenylbenzenesulfonylamino)propionic acid, and

3-�1-�3-(pyridin-2-ylamino)propyl!indazol-4-ylcarbonylamino!-2-(4-phenylbenzenesulfonylamino)propionic acid; and ester forms thereof, said ester being selected from the group consisting of:

methyl,

ethyl,

isopropyl,

n-butyl,

isobutyl,

benzyl,

methylcarbonyloxymethyl,

ethylcarbonyloxymethyl,

tert-butylcarbonyloxymethyl,

cyclohexylcarbonyloxymethyl,

tert-butyloxycarbonyloxymethyl,

dimethylaminoethyl,

diethylaminoethyl,

morpholinoethyl,

pyrrolidinoethyl, and

trimethylammonioethyl.

6. A compound of Formula Ib: ##STR79## and pharmaceutically acceptable salt forms thereof, wherein: X.sup.1, X.sup.2, X.sup.3, and X.sup.4 are independently selected from nitrogen or carbon provided that at least two of X.sup.1, X.sup.2, X.sup.3 and X.sup.4 are carbon;

R.sup.1 is selected from: ##STR80## A and B are independently --CH.sub.2 --, --O--, --N(R.sup.2)--, or --C(.dbd.O)--;

A.sup.1 and B.sup.1 are independently --CH.sub.2 -- or --N(R.sup.3)--;

D is --N(R.sup.2)--, --O--, --S--, --C(.dbd.O)-- or --SO.sub.2 --;

E--F is --C(R.sup.4).dbd.C(R.sup.5)--, --N.dbd.C(R.sup.4)--, --C(R.sup.4).dbd.N--, or --C(R.sup.4).sub.2 C(R.sup.5).sub.2 --;

J, K, L and M are independently selected from: --C(R.sup.4)--, --C(R.sup.5)-- or --N--, provided that at least one of J, K, L and M is not --N--;

R.sup.2 is selected from: H, C.sub.1 -C.sub.6 alkyl, (C.sub.1 -C.sub.6 alkyl)carbonyl, (C.sub.1 -C.sub.6 alkoxy)carbonyl; (C.sub.1 -C.sub.6 alkyl)aminocarbonyl, C.sub.3 -C.sub.6 alkenyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.4 -C.sub.11 cycloalkylalkyl, aryl, heteroaryl(C.sub.1 -C.sub.6 alkyl)carbonyl, heteroarylcarbonyl, aryl C.sub.1 -C.sub.6 alkyl, (C.sub.1 -C.sub.6 alkyl)carbonyl, or arylcarbonyl, C.sub.1 -C.sub.6 alkylsulfonyl, arylsulfonyl, aryl(C.sub.1 -C.sub.6 alkyl)sulfonyl, heteroarylsulfonyl, heteroaryl(C.sub.1 -C.sub.6 alkyl)sulfonyl, aryloxycarbonyl, or aryl(C.sub.1 -C.sub.6 alkoxy)carbonyl, wherein said aryl groups are substituted with 0-2 substituents selected from the group consisting of C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, halo, CF.sub.3, and nitro;

R.sup.3 is selected from: H, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.4 -C.sub.11 cycloalkylalkyl, aryl, aryl(C.sub.1 -C.sub.6 alkyl)-, or heteroaryl(C.sub.1 -C.sub.6 alkyl)-;

R.sup.4 and R.sup.5 are independently selected from: H, C.sub.1 -C.sub.4 alkoxy, NR.sup.2 R.sup.3, halogen, NO.sub.2, CN, CF.sub.3, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 alkenyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.1 -C.sub.11 cycloalkylalkyl, aryl, aryl(C.sub.1 -C.sub.6 alkyl)-, (C.sub.1 -C.sub.6 alkyl)carbonyl, (C.sub.1 -C.sub.6 alkoxy)carbonyl, arylcarbonyl, or

alternatively, when substituents on adjacent atoms, R.sup.4 and R.sup.5 can be taken together with the carbon atoms to which they are attached to form a 5-7 membered carbocyclic or 5-7 membered heterocyclic aromatic or non-aromatic ring system, said carbocyclic or heterocyclic ring being optionally substituted with 0-2 groups selected from: C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, halo, cyano, amino, CF.sub.3, or NO.sub.2 ;

U is selected from:

--(CH.sub.2).sub.n --,

--(CH.sub.2).sub.n (CR.sup.7 .dbd.CR.sup.8)(CH.sub.2).sub.m --

--(CH.sub.2).sub.n (C.tbd.C)(CH.sub.2).sub.m --

--(CH.sub.2).sub.t Q(CH.sub.2).sub.m --

--(CH.sub.2).sub.n O(CH.sub.2).sub.m --,

--(CH.sub.2).sub.n N(R.sup.6)(CH.sub.2).sub.m --,

--(CH.sub.2).sub.n C(.dbd.O)(CH.sub.2).sub.m --,

--(CH.sub.2).sub.n (C.dbd.O)N(R.sup.6)(CH.sub.2).sub.m --

--(CH.sub.2).sub.n N(R.sup.6)(C.dbd.O)(CH.sub.2).sub.m --, or

--(CH.sub.2).sub.n S(O).sub.p (CH.sub.2).sub.m --;

wherein one of the methylene groups is optionally substituted with R.sup.7 ;

Q is selected from: 1,2-cycloalkylene, 1,2-phenylene, 1,3-phenylene, 1,4-phenylene, 2,3-pyridinylene, 3,4-pyridinylene, 2,4-pyridinylene, or 3,4-pyridazinylene;

R.sup.6 is selected from: H, C.sub.1 -C.sub.4 alkyl, or benzyl;

R.sup.7 and R.sup.8 are independently selected from: H, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.4 -C.sub.11 cycloalkylalkyl, aryl, aryl(C.sub.1 -C.sub.6 alkyl)-, or heteroaryl(C.sub.0 -C.sub.6 alkyl)-;

R.sup.9 is selected from: H, CO.sub.2 R.sup.17, C(.dbd.O)R.sup.17, CONR.sup.17 R.sup.20, --SO.sub.2 R.sup.17, --SO.sub.2 NR.sup.17 R.sup.20, C.sub.1 -C.sub.6 alkyl substituted with 0-1 R.sup.15 or 0-1 R.sup.21, C.sub.3 -C.sub.6 alkenyl substituted with 0-1 R.sup.15 or 0-1 R.sup.21, C.sub.3 -C.sub.7 cycloalkyl substituted with 0-1 R.sup.15 or 0-1 R.sup.21, C.sub.4 -C.sub.11 cycloalkylalkyl substituted with 0-1 R.sup.15 or 0-1 R.sup.21, aryl substituted with 0-1 R.sup.15 or 0-2 R.sup.11 or 0-1 R.sup.21, or aryl(C.sub.1 -C.sub.6 alkyl)- substituted with 0-1 R.sup.15 or 0-2 R.sup.11 or 0-1 R.sup.21 ;

R.sup.11 is selected from H, halogen, CF.sub.3, CN, N).sub.2, hydroxy, NR.sup.2 R.sup.3, C.sub.1 -C.sub.4 alkyl substituted with 0-1 R.sup.21, C.sub.1 -C.sub.4 alkoxy substituted with 0-1 R.sup.21, aryl substituted with 0-1 R.sup.21, aryl(C.sub.1 -C.sub.6 alkyl)- substituted with 0-1 R.sup.21, (C.sub.1 -C.sub.4 alkoxy)carbonyl substituted with 0-1 R.sup.21, (C.sub.1 -C.sub.4 alkyl)carbonyl substituted with 0-1 R.sup.21, C.sub.1 -C.sub.4 alkylsulfonyl substituted with 0-1 R.sup.21, or C.sub.1 -C.sub.4 alkylaminosulfonyl substituted with 0-1 R.sup.21 ;

W is selected from:

--(C(R.sup.12).sub.2).sub.q C(.dbd.O)N(R.sup.13)--, or --C(.dbd.O)--N(R.sup.13)--(C(R.sup.12).sub.2).sub.q --;

X is --C(R.sup.12)(R.sup.14)--C(R.sup.12)(R.sup.15)--; or

alternatively, W and X can be taken together to be ##STR81## R.sup.12 is selected from: H, halogen, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkynyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.4 -C.sub.10 cycloalkylalkyl, (C.sub.1 -C.sub.4 alkyl)carbonyl, aryl, or aryl(C.sub.1 -C.sub.6 alkyl)-;

R.sup.13 is selected from: H, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.7 cycloalkylmethyl, or aryl(C.sub.1 -C.sub.6 alkyl)-;

R.sup.14 is selected from:

H, C.sub.1 -C.sub.6 alkylthio(C.sub.1 -C.sub.6 alkyl)-, aryl(C.sub.1 -C.sub.10 alkylthioalkyl)-, aryl(C.sub.1 -C.sub.10 alkoxyalkyl)-, C.sub.1 -C.sub.10 alkyl, C.sub.1 -C.sub.10 alkoxyalkyl, C.sub.1 -C.sub.6 hydroxyalkyl, C.sub.2 -C.sub.10 alkenyl, C.sub.2 -C.sub.10 alkynyl, C.sub.3 -C.sub.10 cycloalkyl, C.sub.3 -C.sub.10 cycloalkylalkyl, aryl(C.sub.1 -C.sub.6 alkyl)-, heteroaryl(C.sub.1 -C.sub.6 alkyl)-, aryl, heteroaryl, CO.sub.2 R.sup.17, C(.dbd.O)R.sup.17, or CONR.sup.17 R.sup.20, provided that any of the above alkyl, cycloalkyl, aryl or heteroaryl groups may be unsubstituted or substituted independently with 0-1 R.sup.16 or 0-2 R.sup.11 ;

R.sup.15 is selected from:

H, R.sup.16, C.sub.1 -C.sub.10 alkyl, C.sub.1 -C.sub.10 alkoxyalkyl, C.sub.1 -C.sub.10 alkylaminoalkyl, C.sub.1 -C.sub.10 dialkylaminoalkyl, (C.sub.1 -C.sub.10 alkyl)carbonyl, aryl(C.sub.0 -C.sub.6 alkyl)carbonyl, C.sub.1 -C.sub.10 alkenyl, C.sub.1 -C.sub.10 alkynyl ,C.sub.3 -C.sub.10 cycloalkyl, C.sub.3 -C.sub.10 cycloalkylalkyl, aryl(C.sub.1 -C.sub.6 alkyl)-, heteroaryl(C.sub.1 -C.sub.6 alkyl)-, aryl, heteroaryl, CO.sub.2 R.sup.17 C(.dbd.O)R.sup.17, CONR.sup.17 R.sup.20, SO.sub.2 R.sup.17, or SO.sub.2 NR.sup.17 R.sup.20, provided that any of the above alkyl, cycloalkyl, aryl or heteroaryl groups may be unsubstituted or substituted independently with 0-2 R.sup.11 ;

Y is selected from:

--COR.sup.19, --SO.sub.3 H, --PO.sub.3 H, tetrazolyl, --CONHNHSO.sub.2 CF.sub.3, --CONHSO.sub.2 R.sup.17, --CONHSO.sub.2 NHR.sup.17, --NHCOCF.sub.3, --NHCONHSO.sub.2 R.sup.17, --NHSO.sub.2 R.sup.17, --OPO.sub.3 H.sub.2, --OSO.sub.3 H, --PO.sub.3 H.sub.2, --SO.sub.3 H, --SO.sub.2 NHCOR.sup.17, --SO.sub.2 NHCO.sub.2 R.sup.17 ##STR82## R.sup.16 is selected from: --N(R.sup.20)--C(.dbd.O)--O--R.sup.17,

--N(R.sup.20)--C(.dbd.O)--R.sup.17,

--N(R.sup.20)--C(.dbd.O)--NH--R.sup.17,

--N(R.sup.20)SO.sub.2 --R.sup.17, or

--N(R.sup.20)SO.sub.2 --NR.sup.20 R.sup.17 ;

R.sup.17 is selected from:

C.sub.1 -C.sub.10 alkyl, C.sub.3 -C.sub.11 cycloalkyl, aryl(C.sub.1 -C.sub.6 alkyl)-, (C.sub.1 -C.sub.6 alkyl)aryl, heteroaryl(C.sub.1 -C.sub.6 alkyl)-, (C.sub.1 -C.sub.6 alkyl)heteroaryl, biaryl(C.sub.1 -C.sub.6 alkyl)-, heteroaryl, or aryl, wherein said aryl or heteroaryl groups are optionally substituted with 0-3 substituents selected from the group consisting of: C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, aryl, heteroaryl, halo, cyano, amino, CF.sub.3, and NO.sub.2 ;

R.sup.18 is selected from:

H,

--C(.dbd.O)--O--R.sup.17,

--C(.dbd.0)--R.sup.17,

--C(.dbd.O)--NH--R.sup.17,

--SO.sub.2 --R.sup.17, or

--SO.sub.2 --NR.sup.20 R.sup.17 ;

R.sup.19 is selected from hydroxy, C.sub.1 -C.sub.10 alkyloxy, C.sub.3 -C.sub.11 cycloalkyloxy, aryloxy, aryl(C.sub.1 -C.sub.6 alkoxy)-, C.sub.3 -C.sub.10 alkylcarbonyloxyalkyloxy, C.sub.3 -C.sub.10 alkoxycarbonyloxyalkyloxy, C.sub.2 -C.sub.10 alkoxycarbonylalkyloxy, C.sub.5 -C.sub.10 cycloalkylcarbonyloxyalkyloxy, C.sub.5 -C.sub.10 cycloalkoxycarbonyloxyalkyloxy, C.sub.5 -C.sub.10 cycloalkoxycarbonylalkyloxy, C.sub.7 -C.sub.11 aryloxycarbonylalkyloxy, C.sub.8 -C.sub.12 aryloxycarbonyloxyalkyloxy, C.sub.8 -C.sub.12 arylcarbonyloxyalkyloxy, C.sub.5 -C.sub.10 alkoxyalkylcarbonyloxyalkyloxy, C.sub.5 -C.sub.10 (5-alkyl-1,3-dioxa-cyclopenten-2-one-yl)methyloxy, C.sub.10 -C.sub.14 (5-aryl-1,3-dioxa-cyclopenten-2-one-yl)methyloxy, or (R.sup.11)(R.sup.12)N--(C.sub.1 -C.sub.10 alkoxy)-;

R.sup.20 is selected from: H, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.4 -C.sub.11 cycloalkylalkyl, aryl, aryl(C.sub.1 -C.sub.6 alkyl)-, or heteroaryl(C.sub.1 -C.sub.6 alkyl)-;

R.sup.21 is selected from COOH or NR.sup.6.sub.2 ;

m is 0-4;

n is 0-4;

t is 0-4;

p is 0-2;

q is 0-2; and

r is 0-2;

with the following provisos:

(1) t, n, m and q are chosen such that the number of atoms connecting R.sup.1 and Y is in the range of 10-14; and

(2) n and m are chosen such that the value of n plus m is greater than one unless U is --(CH.sub.2).sub.t Q(CH.sub.2).sub.m --.

7. A compound of claim 6 of Formula Ib: ##STR83## and pharmaceutically acceptable salt forms thereof, wherein: X.sup.1, X.sup.2, X.sup.3, and X.sup.4 are independently selected from nitrogen or carbon provided that at least two of X.sup.1, X.sup.2, X.sup.3 and X.sup.4 are carbon;

R.sup.1 is selected from: ##STR84## A and B are independently --CH.sub.2 --, --O--, --N(R.sup.2)--, or --C(.dbd.O)--;

A.sup.1 and B.sup.1 are independently --CH.sub.2 -- or --N(R.sup.3)--;

D is --N(R.sup.2)--, --O--, --S--, --C(.dbd.O)-- or --SO.sub.2 --;

E--F is --C(R.sup.4).dbd.C(R.sup.5)--, --N.dbd.C(R.sup.4)--, --C(R.sup.4).dbd.N--, or --C(R.sup.4).sub.2 C(R.sup.5).sub.2 --;

J, K, L and M are independently selected from --C(R.sup.4)--, --C(R.sup.5)-- or --N--, provided that at least one of J, K, L and M is not --N--;

R.sup.2 is selected from: H, C.sub.1 -C.sub.6 alkyl, (C.sub.1 -C.sub.6 alkyl)carbonyl, (C.sub.1 -C.sub.6 alkoxy)carbonyl, C.sub.1 -C.sub.6 alkylaminocarbonyl, C.sub.3 -C.sub.6 alkenyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.4 -C.sub.11 cycloalkylalkyl, aryl, heteroaryl(C.sub.1 -C.sub.6 alkyl)carbonyl, heteroarylcarbonyl, aryl(C.sub.1 -C.sub.6 alkyl)-, (C.sub.1 -C.sub.6 alkyl)carbonyl, arylcarbonyl, alkylsulfonyl, arylsulfonyl, aryl(C.sub.1 -C.sub.6 alkyl)sulfonyl, heteroarylsulfonyl, heteroaryl(C.sub.1 -C.sub.6 alkyl)sulfonyl, aryloxycarbonyl, aryl(C.sub.1 -C.sub.6 alkoxy)carbonyl, wherein said aryl groups are substituted with 0-2 substituents selected from the group consisting of C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, halo, CF.sub.3, and nitro;

R.sup.3 is selected from: H, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.4 -C.sub.11 cycloalkylalkyl, aryl, aryl(C.sub.1 -C.sub.6 alkyl)-, or heteroaryl(C.sub.1 -C.sub.6 alkyl)-;

R.sup.4 and R.sup.5 are independently selected from: H, C.sub.1 -C.sub.4 alkoxy, NR.sup.2 R.sup.3, halogen, NO.sub.2, CN, CF.sub.3, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 alkenyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.4 -C.sub.11 cycloalkylalkyl, aryl, aryl(C.sub.1 -C.sub.6 alkyl)-, C.sub.2 -C.sub.7 alkylcarbonyl, arylcarbonyl or

alternatively, when substituents on adjacent atoms, R.sup.4 and R.sup.5 can be taken together with the carbon atoms to which they are attached to form a 5-7 membered carbocyclic or 5-7 membered heterocyclic aromatic or non-aromatic ring system, said carbocyclic or heterocyclic ring being optionally substituted with 0-2 groups selected from: C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, halo, cyano, amino, CF.sub.3, or NO.sub.2 ;

U is selected from:

--(CH.sub.2).sub.n --,

--(CH.sub.2).sub.n (CR.sup.7 .dbd.CR.sup.8)(CH.sub.2).sub.m --

--(CH.sub.2).sub.t Q(CH.sub.2).sub.m --,

--(CH.sub.2).sub.n O(CH.sub.2).sub.m --,

--(CH.sub.2).sub.n N(R.sup.6)(CH.sub.2).sub.m --,

--(CH.sub.2).sub.n C(.dbd.O)(CH.sub.2).sub.m --, or

--(CH.sub.2).sub.n S(O).sub.p (CH.sub.2).sub.m --;

wherein one of the methylene groups is optionally substituted with R.sup.7 ;

Q is selected from 1,2-phenylene, 1,3-phenylene, 2,3-pyridinylene, 3,4-pyridinylene, or 2,4-pyridinylene;

R.sup.6 is selected from: H, C.sub.1 -C.sub.4 alkyl, or benzyl;

R.sup.7 and R.sup.8 are independently selected from: H, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.1 -C.sub.11 cycloalkylalkyl, aryl, aryl(C.sub.1 -C.sub.6 alkyl)-, or heteroaryl(C.sub.0 -C.sub.6 alkyl)-;

R.sup.9 is selected from: H, CO.sub.2 R.sup.17 C(.dbd.O)R.sup.17, CONR.sup.17 R.sup.20, --SO.sub.2 R.sup.17, --SO.sub.2 NR.sup.17 R.sup.20, C.sub.1 -C.sub.6 alkyl substituted with 0-1 R.sup.15 or 0-1 R.sup.21, C.sub.3 -C.sub.6 alkenyl substituted with 0-1 R.sup.15 or 0-1 R.sup.21, C.sub.3 -C.sub.7 cycloalkyl substituted with 0-1 R.sup.15 or 0-1 R.sup.21, C.sub.4 -C.sub.11 cycloalkylalkyl substituted with 0-1 R.sup.15 or 0-1 R.sup.21, aryl substituted with 0-1 R.sup.15 or 0-2 R.sup.11 or 0-1 R.sup.21, or aryl(C.sub.1 -C.sub.6 alkyl)- substituted with 0-1 R.sup.15 or 0-2 R.sup.11 or 0-1 R.sup.21 ;

R.sup.11 is selected from: H, halogen, CF.sub.3, CN, NO.sub.2, hydroxy, NR.sup.2 R.sup.3, C.sub.1 -C.sub.4 alkyl substituted with 0-1 R.sup.21, C.sub.1 -C.sub.4 alkoxy substituted with 0-1 R.sup.21, aryl substituted with 0-1 R.sup.21, aryl(C.sub.1 -C.sub.6 alkyl)- substituted with 0-1 R.sup.21, (C.sub.1 -C.sub.4 alkoxy)carbonyl substituted with 0-1 R.sup.21, (C.sub.1 -C.sub.4 alkyl)carbonyl substituted with 0-1 R.sup.21, C.sub.1 -C.sub.4 alkylsulfonyl substituted with 0-1 R.sup.21, or C.sub.1 -C.sub.4 alkylaminosulfonyl substituted with 0-1 R.sup.21 ;

W is --C(.dbd.O)--N(R.sup.13)--(C(R.sup.12).sub.2).sub.q --;

X is --C(R.sup.12)(R.sup.14)--C(R.sup.12)(R.sup.15)--;

alternatively, W and X can be taken together to be ##STR85## R.sup.12 is H or C.sub.1 -C.sub.6 alkyl; R.sup.13 is selected from: H, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.7 cycloalkylmethyl, or aryl(C.sub.1 -C.sub.6 alkyl)-;

R.sup.14 is selected from:

H, C.sub.1 -C.sub.6 alkylthioalkyl, aryl(C.sub.1 -C.sub.10 alkylthioalkyl)-, aryl(C.sub.1 -C.sub.10 alkoxyalkyl)-, C.sub.1 -C.sub.10 alkyl, C.sub.1 -C.sub.10 alkoxyalkyl, C.sub.1 -C.sub.6 hydroxyalkyl, C.sub.2 -C.sub.10 alkenyl, C.sub.2 -C.sub.10 alkynyl, C.sub.3 -C.sub.10 cycloalkyl, C.sub.3 -C.sub.10 cycloalkylalkyl, aryl(C.sub.1 -C.sub.6 alkyl)-, heteroaryl(C.sub.1 -C.sub.6 alkyl)-, aryl, heteroaryl, CO.sub.2 R.sup.17, C(.dbd.O)R.sup.17, or CONR.sup.17 R.sup.20, provided that any of the above alkyl, cycloalkyl, aryl or heteroaryl groups may be unsubstituted or substituted independently with 0-1 R.sup.16 or 0-2 R.sup.11 ;

R.sup.15 is selected from:

H, R.sup.16, C.sub.1 -C.sub.10 alkyl, C.sub.1 -C.sub.10 alkoxyalkyl, C.sub.1 -C.sub.10 alkylaminoalkyl, C.sub.1 -C.sub.10 dialkylaminoalkyl, C.sub.1 -C.sub.10 alkylcarbonyl, aryl(C.sub.0 -C.sub.6 alkyl)carbonyl, C.sub.2 -C.sub.10 alkenyl, C.sub.2 -C.sub.10 alkynyl, C.sub.3 -C.sub.10 cycloalkyl, C.sub.3 -C.sub.10 cycloalkylalkyl, aryl(C.sub.1 -C.sub.6 alkyl)-, heteroaryl(C.sub.1 -C.sub.6 alkyl)-, aryl, heteroaryl, CO.sub.2 R.sup.17, C(.dbd.O)R.sup.17, CONR.sup.17 R.sup.20, SO.sub.2 R.sup.17, or SO.sub.2 NR.sup.17 R.sup.20, provided that any of the above alkyl, cycloalkyl, aryl or heteroaryl groups may be unsubstituted or substituted independently with 0-2 R.sup.11 ;

Y is selected from: ##STR86## R.sup.16 is selected from: --N(R.sup.20)--C(.dbd.O)--O--R.sup.17,

--N(R.sup.20)--C(.dbd.O)--R.sup.17,

--N(R.sup.20)--C(.dbd.O)--NH--R.sup.17,

--N(R.sup.20)SO.sub.2 --R.sup.17, or

--N(R.sup.20)SO.sub.2 --NR.sup.20 R.sup.17 ;

R.sup.17 is selected from:

C.sub.1 -C.sub.10 alkyl, C.sub.3 -C.sub.11 cycloalkyl, aryl(C.sub.1 -C.sub.6 alkyl)-, (C.sub.1 -C.sub.6 alkyl)aryl, heteroaryl(C.sub.1 -C.sub.6 alkyl)-, (C.sub.1 -C.sub.6 alkyl)heteroaryl, biaryl(C.sub.1 -C.sub.6 alkyl)-, heteroaryl, or aryl, wherein said aryl or heteroaryl groups are optionally substituted with 0-3 substituents selected from the group consisting of: C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, aryl, heteroaryl, halo, cyano, amino, CF.sub.3, and NO.sub.2 ;

R.sup.18 is selected from:

H,

--C(.dbd.O)--O--R.sup.17,

--C(.dbd.O)--R.sup.17,

--C(.dbd.O)--NH--R.sup.17,

--SO.sub.2 --R.sup.17, or

--SO.sub.2 --NR.sup.20 R.sup.17 ;

R.sup.19 is selected from hydroxy, C.sub.1 -C.sub.10 alkyloxy, C.sub.3 -C.sub.11 cycloalkyloxy, C.sub.6 -C.sub.10 aryloxy, C.sub.7 -C.sub.11 aralkyloxy, C.sub.3 -C.sub.10 alkylcarbonyloxyalkyloxy, C.sub.3 -C.sub.10 alkoxycarbonyloxyalkyloxy, C.sub.2 -C.sub.10 alkoxycarbonylalkyloxy, C.sub.5 -C.sub.10 cycloalkylcarbonyloxyalkyloxy, C.sub.5 -C.sub.10 cycloalkoxycarbonyloxyalkyloxy, C.sub.5 -C.sub.10 cycloalkoxycarbonylalkyloxy, C.sub.7 -C.sub.11 aryloxycarbonylalkyloxy, C.sub.8 -C.sub.12 aryloxycarbonyloxyalkyloxy, C.sub.8 -C.sub.12 arylcarbonyloxyalkyloxy, C.sub.5 -C.sub.10 alkoxyalkylcarbonyloxyalkyloxy, C.sub.5 -C.sub.10 (5-alkyl-1,3-dioxa-cyclopenten-2-one-yl)methyloxy, C.sub.10 -C.sub.14 (5-aryl-1,3-dioxa-cyclopenten-2-one-yl)methyloxy, or (R.sup.11)(R.sup.12)N-(C.sub.1 -C.sub.10 alkoxy)-;

R.sup.20 selected from: H, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.4 -C.sub.11 cycloalkylalkyl, aryl(C.sub.1 -C.sub.6 alkyl)-, or heteroaryl(C.sub.1 -C.sub.6 alkyl)-;

R.sup.21 is selected from COOH or NR.sup.6.sub.2 ;

m is 0-4;

n is 0-4;

t is 0-4;

p is 0-2;

q is 0-2; and

r is 0-2.

8. A compound of claim 6 of the Formula IIc or IId: ##STR87## and pharmaceutically acceptable salt forms thereof, wherein: X.sub.1 and X.sub.3 are independently selected from nitrogen or carbon;

R.sup.1 is selected from: ##STR88## wherein the above heterocycles are optionally substituted with 0-2 substituents selected from the group consisting of: NH.sub.2, halogen, NO.sub.2, CN, CF.sub.3, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.6 alkyl, and C.sub.3 -C.sub.7 cycloalkyl;

U is --(CH.sub.2).sub.n --, --(CH.sub.2).sub.t Q(CH.sub.2).sub.m -- or --C(.dbd.O)(CH.sub.2).sub.n-1 --, wherein one of the methylene groups is optionally substituted with R.sup.7 ;

Q is selected from 1,2-phenylene, 1,3-phenylene, 2,3-pyridinylene, 3,4-pyridinylene, or 2,4-pyridinylene;

R.sup.6 is selected from: H, C.sub.1 -C.sub.4 alkyl, or benzyl;

R.sup.7 is selected from: C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.4 -C.sub.11 cycloalkylalkyl, aryl, aryl(C.sub.1 -C.sub.6 alkyl), heteroaryl, or heteroaryl(C.sub.1 .C.sub.6 alkyl);

R.sup.9 is selected from: H, --SO.sub.2 R.sup.17, --SO.sub.2 NR.sup.17 R.sup.20, C.sub.1 -C.sub.6 alkyl substituted with 0-1 R.sup.15 or 0-1 R.sup.21, C.sub.3 -C.sub.7 cycloalkyl substituted with 0-1 R.sup.15 or 0-1 R.sup.21, C.sub.4 -C.sub.11 cycloalkylalkyl substituted with 0-1 R.sup.15 or 0-1 R.sup.21, aryl substituted with 0-1 R.sup.15 or 0-2 R.sup.11 or 0-1 R.sup.21, or aryl(C.sub.1 -C.sub.6 alkyl)- substituted with 0-1 R.sup.15 or 0-2 R.sup.11 or 0-1 R.sup.21 ;

R.sup.11 is selected from: H, halogen, CF.sub.3, CN, NO.sub.2 , hydroxy, NR.sup.2 R.sup.3, C.sub.1 -C.sub.4 alkyl substituted with 0-1 R.sup.21, C.sub.1 -C.sub.4 alkoxy substituted with 0-1 R.sup.21, aryl substituted with 0-1 R.sup.21, aryl(C.sub.1 -C.sub.6 alkyl)- substituted with 0-1 R.sup.21, (C.sub.1 -C.sub.4 alkoxy)carbonyl substituted with 0-1 R.sup.21, (C.sub.1 -C.sub.4 alkyl)carbonyl substituted with 0-1 R.sup.21, C.sub.1 -C.sub.4 alkylsulfonyl substituted with 0-1 R.sup.21, or C.sub.1 -C.sub.4 alkylaminosulfonyl substituted with 0-1 R.sup.21 ;

W is --C(.dbd.O)--N(R.sup.13)--;

X is --CH(R.sup.14)--CH(R.sup.15)--;

R.sup.13 is H or CH.sub.3 ;

R.sup.14 is selected from:

H, C.sub.1 -C.sub.10 alkyl, aryl, or heteroaryl, wherein said aryl or heteroaryl groups are optionally substituted with 0-3 substituents selected from the group consisting of: C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, aryl, halo, cyano, amino, CF.sub.3, and NO.sub.2 ;

R.sup.15 is H or R.sup.16 ;

Y is --COR.sup.19 ;

R.sup.16 is selected from:

--NH(R.sup.20)--C(.dbd.O)--O--R.sup.17,

--N(R.sup.20)--C(.dbd.O)--R.sup.17,

--N(R.sup.20)--C(.dbd.O)--NH--R.sup.17,

--N(R.sup.20)SO.sub.2 --R.sup.17, or

--N(R.sup.20)SO.sub.2 --N(R.sup.20)R.sup.17 ;

R.sup.17 is selected from:

C.sub.1 -C.sub.10 alkyl, C.sub.3 -C.sub.11 cycloalkyl, aryl(C.sub.1 -C.sub.6 alkyl)-, (C.sub.1 -C.sub.6 alkyl)aryl, heteroaryl(C.sub.1 -C.sub.6 alkyl)-, (C.sub.1 -C.sub.6 alkyl)heteroaryl, biaryl(C.sub.1 -C.sub.6 alkyl)-, heteroaryl, or aryl, wherein said aryl or heteroaryl groups are optionally substituted with 0-3 substituents selected from the group consisting of: C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, aryl, heteroaryl, halo, cyano, amino, CF.sub.3, and NO.sub.2 ;

R.sup.19 is selected from:

hydroxy, C.sub.1 -C.sub.10 alkoxy,

methylcarbonyloxymethoxy-,

ethylcarbonyloxymethoxy-,

t-butylcarbonyloxymethoxy-,

cyclohexylcarbonyloxymethoxy-,

1-(methylcarbonyloxy)ethoxy-,

1-(ethylcarbonyloxy)ethoxy-,

1-(t-butylcarbonyloxy)ethoxy-,

1-(cyclohexylcarbonyloxy)ethoxy-,

i-propyloxycarbonyloxymethoxy-,

t-butyloxycarbonyloxymethoxy-,

1-(i-propyloxycarbonyloxy)ethoxy-,

1-(cyclohexyloxycarbonyloxy)ethoxy-,

1-(t-butyloxycarbonyloxy)ethoxy-,

dimethylaminoethoxy-,

diethylaminoethoxy-,

(5-methyl-1,3-dioxacyclopenten-2-on-4-yl)methoxy-,

(5-(t-butyl)-1,3-dioxacyclopenten-2-on-4-yl)methoxy-,

(1,3-dioxa-5-phenyl-cyclopenten-2-on-4-yl)methoxy-, or

1-(2-(2-methoxypropyl)carbonyloxy)ethoxy-;

R.sup.20 is H or CH.sub.3 ;

R.sup.21 is selected from COOH or NR.sup.6.sub.2 ; and

m is 0 or 1;

n is 1-4; and

t is 0 or 1.

9. A compound of claim 6 of the Formula IIc or IId: ##STR89## and pharmaceutically acceptable salt forms thereof, wherein: X.sub.1 and X.sub.3 are independently selected from nitrogen or carbon, provided that at least one of X.sub.1 and X.sub.3 is carbon;

R.sup.1 is selected from: ##STR90## wherein the above heterocycles are optionally substituted with 0-2 substituents selected from the group consisting of: NH.sub.2, halogen, NO.sub.2, CN, CF.sub.3, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.6 alkyl, and C.sub.3 -C.sub.7 cycloalkyl:

U is --(CH.sub.2).sub.n --, --(CH.sub.2).sub.t Q(CH.sub.2).sub.m -- or --C(.dbd.O)(CH.sub.2).sub.n-1 --, wherein one of the methylene groups is optionally substituted with R.sup.7 ;

Q is selected from 1,2-phenylene, 1,3-phenlylene, 2,3-pyridinylene, 3,4-pyridinylene, or 2,4-pyridinylene;

R.sup.6 is selected from: H, C.sub.1 -C.sub.4 alkyl, or benzyl;

R.sup.7 is selected from: C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.4 -C.sub.11 cycloalkylalkyl, aryl, aryl(C.sub.1 -C.sub.6 alkyl), heteroaryl, or heteroaryl(C.sub.1 -C.sub.6 alkyl);

R.sup.9 is selected from: H, --SO.sub.2 R.sup.17, --SO.sub.2 NR.sup.17 R.sup.20, C.sub.1 -C.sub.6 alkyl substituted with 0-1 R.sup.15 or 0-1 R.sup.21, C.sub.3 -C.sub.7 cycloalkyl substituted with 0-1 R.sup.15 or 0-1 R.sup.21, C.sub.4 -C.sub.11 cycloalkylalkyl substituted with 0-1 R.sup.15 or 0-1 R.sup.21, aryl substituted with 0-1 R.sup.15 or 0-2 R.sup.11 or 0-1 R.sup.21, or aryl(C.sub.1 -C.sub.6 alkyl)- substituted with 0-1 R.sup.15 or 0-2 R.sup.11 or 0-1 R.sup.21 ;

R.sup.11 is selected from H, halogen, CF.sub.3, CN, NO.sub.2, hydroxy, NR.sup.2 R.sup.3, C.sub.1 -C.sub.4 alkyl substituted with 0-1 R.sup.21, C.sub.1 -C.sub.4 alkoxy substituted with 0-1 R.sup.21, aryl substituted with 0-1 R.sup.21, aryl(C.sub.1 -C.sub.6 alkyl)- substituted with 0-1 R.sup.21, (C.sub.1 -C.sub.4 alkoxy)carbonyl substituted with 0-1 R.sup.21, (C.sub.1 -C.sub.4 alkyl)carbonyl substituted with 0-1 R.sup.21, C.sub.1 -C.sub.4 alkylsulfonyl substituted with 0-1 R.sup.21, or C.sub.1 -C.sub.4 alkylaminosulfonyl substituted with 0-1 R.sup.21 ;W is --C(.dbd.O)--N(R.sup.13)--;

W is --C(.dbd.O)--N(R.sup.13)--;

X is --CH(R.sup.14)--CH(R.sup.15);

R.sup.13 is H or CH.sub.3 ;

R.sup.14 is selected from:

H, C.sub.1 -C.sub.10 alkyl, aryl, or heteroaryl, wherein said aryl or heteroaryl groups are optionally substituted with 0-3 substituents selected from the group consisting of: C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, aryl, halo, cyano, amino, CF.sub.3, and NO.sub.2 ;

R.sup.15 is H or R.sup.16 ;

Y is --COR.sup.19 ;

R.sup.16 is selected from:

--N(R.sup.20)--C(.dbd.O)--O--R.sup.17,

--N(R.sup.20)--C(.dbd.O)--R.sup.17,

--N(R.sup.20)--C(.dbd.0)--NH--R.sup.17,

--N(R.sup.20)SO.sub.2 --R.sup.17, or

--N(R.sup.20)SO.sub.2 --NR.sup.20 R.sup.17 ;

R.sup.17 is selected from:

C.sub.1 -C.sub.10 alkyl, C.sub.3 -C.sub.11 cycloalkyl, aryl(C.sub.1 -C.sub.6 alkyl)-, (C.sub.1 -C.sub.6 alkyl)aryl, heteroaryl(C.sub.1 -C.sub.6 alkyl)-, (C.sub.1 -C.sub.6 alkyl)heteroaryl, biaryl(C.sub.1 -C.sub.6 alkyl)-, heteroaryl, or aryl, wherein said aryl or heteroaryl groups are optionally substituted with 0-3 substituents selected from the group consisting of: C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, aryl, heteroaryl, halo, cyano, amino, CF.sub.3, and NO.sub.2 ;

R.sup.19 is selected from:

hydroxy, C.sub.1 -C.sub.10 alkoxy,

methylcarbonyloxymethoxy-,

ethylcarbonyloxymethoxy-,

t-butylcarbonyloxymethoxy-,

cyclohexylcarbonyloxymethoxy-,

1-(methylcarbonyloxy)ethoxy-,

1-(ethylcarbonyloxy)ethoxy-,

1-(t-butylcarbonyloxy)ethoxy-,

1-(cyclohexylcarbonyloxy)ethoxy-,

i-propyloxycarbonyloxymethoxy-,

t-butyloxycarbonyloxymethoxy-,

1-(i-propyloxycarbonyloxy)ethoxy-,

1-(cyclohexyloxycarbonyloxy)ethoxy-,

1-(t-butyloxycarbonyloxy)ethoxy-,

dimethylaminoethoxy-,

diethylaminoethoxy-,

(5-methyl-1,3-dioxacyclopenten-2-on-4-yl)methoxy-,

(5-(t-butyl)-1,3-dioxacyclopenten-2-on-4-yl)methoxy-,

(1,3-dioxa-5-phenyl-cyclopenten-2-on-4-yl)methoxy-, or

1-(2-(2-methoxypropyl)carbonyloxy)ethoxy-;

R.sup.20 is H or CH.sub.3 ;

R.sup.21 is selected from COOH or NR.sup.6.sub.2 ; and

m is 0 or n 1;

n is 1-4; and

t is 0 or 1.

10. A compound of claim 6 of Formula Ib and enantiomeric or diasteriomeric forms thereof, and mixtures of enantiomeric or diasteriomeric forms thereof, and pharmaceutically acceptable salt forms thereof, selected from the group consisting of:

3-�3-�3-(imidazolin-2-ylamino)propyl!indazol-6-ylcarbonylamino!-2-(benzyloxycarbonylamino)propionic acid,

3-�1-methyl-3-�3-(imidazolin-2-ylamino)propyl!indazol-6-ylcarbonylamino!-2-(2,4,6-trimethylbenzenesulfonylamino)propionic acid,

3-�3-�3-(imidazolin-2-ylamino)propyl!indazol-6-ylcarbonylamino!-2-(benzenesulfonylamino)propionic acid,

3-�1-methyl-3-�3-(imidazolin-2-ylamino)propyl!indazol-6-ylcarbonylamino!-2-(2,6-dichlorobenzenesulfonylamino)propionic acid,

3-�3-�3-(imidazolin-2-ylamino)propyl!indazol-6-ylcarbonylamino!-2-(3,5-dimethylisoxazol-4-ylsulfonylamino)propionic acid,

3-�1-methyl-3-�3-(imidazolin-2-ylamino)propyl!indazol-6-ylcarbonylamino!-2-(2,6-dimethylbenzenesulfonylamino)propionic acid,

3-�3-�3-(imidazolin-2-ylamino)propyl!indazol-6-ylcarbonylamino!-2-(2,6-dimethyl-4-phenylbenzenesulfonylamino)propionic acid,

3-�1-methyl-3-�3-(imidazolin-2-ylamino)propyl!indazol-6-ylcarbonylamino!-2-(4-phenylbenzenesulfonylamino)propionic acid,

3-�3-�3-(tetrahydropyrimid-2-ylamino)propyl!indazol-6-ylcarbonylamino!-2-(benzyloxycarbonylamino)propionic acid,

3-�1-methyl-3-�3-(tetrahydropyrimid-2-ylamino)propyl!indazol-6-ylcarbonylamino!-2-(2,4,6-trimethylbenzenesulfonylamino)propionic acid,

3-�3-�3-(tetrahydropyrimid-2-ylamino)propyl!indazol-6-ylcarbonylamino!-2-(benzenesulfonylamino)propionic acid,

3-�1-methyl-3-�3-(tetrahydropyrimid-2-ylamino)propyl!indazol-6-ylcarbonylamino!-2-(2,6-dichlorobenzenesulfonylamino)propionic acid,

3-�3-�3-(tetrahydropyrimid-2-ylamino)propyl!indazol-6-ylcarbonylamino!-2-(3,5-dimethylisoxazol-4-ylsulfonylamino)propionic acid,

3-�1-methyl-3-�3-(tetrahydropyrimid-2-ylamino)propyl!indazol-6-ylcarbonylamino!-2-(2,6-dimethylbenzenesulfonylamino)propionic acid,

3-�3-�3-(tetrahydropyrimid-2-ylamino)propyl!indazol-6-ylcarbonylamino!-2-(2,6-dimethyl-4-phenylbenzenesulfonylamino)propionic acid,

3-�1-methyl-3-�3-(tetrahydropyrimid-2-ylamino)propyl!-indazol-6-ylcarbonylamino!-2-(4-phenylbenzenesulfonylamino)propionic acid,

3-�3-�3-(imidazol-2-ylamino)propyl!indazol-6-ylcarbonylamino!-2-(benzyloxycarbonylamino)propionic acid,

3-�1-methyl-3-�3-(imidazol-2-ylamino)propyl!indazol-6-ylcarbonylamino!-2-(2,4,6-trimethylbenzenesulfonylamino)propionic acid,

3-�3-�3-(imidazol-2-ylamino)propyl!indazol-6-ylcarbonylamino!-2-(benzenesulfonylamino)propionic acid,

3-�1-methyl-3-�3-(imidazol-2-ylamino)propyl!indazol-6-ylcarbonylamino!-2-(2,6-dichlorobenzenesulfonylamino)propionic acid,

3-�3-�3-imidazol-2-ylamino)propyl!indazol-6-ylcarbonylamino!-2-(3,5-dimethylisoxazol-4-ylsulfonylamino)propionic acid,

3-�1-methyl-3-�3-(imidazol-2-ylamino)propyl!indazol-6-ylcarbonylamino!-2-(2,6-dimethylbenzenesulfonylamino)propionic acid,

3-�3-�3-(imidazol-2-ylamino)propyl!indazol-6-ylcarbonylamino!-2-(2,6-dimethyl-4-phenylbenzenesulfonylamino)propionic acid,

3-�1-methyl-3-�3-(imidazol-2-ylamino)propyl!indazol-6-ylcarbonylamino!-2-(4-phenylbenzenesulfonylamino)propionic acid,

3-�3-�3-(pyridin-2-ylamino)propyl!indazol-6-ylcarbonylamino!-2-(benzyloxycarbonylamino)propionic acid,

3-�1-methyl-3-�3-(pyridin-2-ylamino)propyl!indazol-6-ylcarbonylamino!-2-(2,4,6-trimethylbenzenesulfonylamino)propionic acid,

3-�3-�3-(pyridin-2-ylamino)propyl!indazol-6-ylcarbonylamino!-2-(benzenesulfonylamino)propionic acid,

3-�1-methyl-3-�3-(pyridin-2-ylamino)propyl!indazol-6-ylcarbonylamino!-2-(2,6-dichlorobenzenesulfonylamino)propionic acid,

3-�3-�3-(pyridin-2-ylamino)propyl!indazol-6-ylcarbonylamino!-2-(3,5-dimethylisoxazol-4-ylsulfonylamino)propionic acid,

3-�1-methyl-3-�3-(pyridin-2-ylamino)propyl!indazol-6-ylcarbonylamino!-2-(2,6-dimethylbenzenesulfonylamino)propionic acid,

3-�3-�3-(pyridin-2-ylamino)propyl!indazol-6-ylcarbonylamino!-2-(2,6-dimethyl-4-phenylbenzenesulfonylamino)propionic acid,

3-�1-methyl-3-�3-(pyridin-2-ylamino)propyl!indazol-6-ylcarbonylamino!-2-(4-phenylbenzenesulfonylamino)propionic acid,

3-�3-�3-(imidazolin-2-ylamino)propyl!indazol-7-ylcarbonylamino!-2-(benzyloxycarbonylamino)propionic acid,

3-�1-methyl-3-(3-(imidazolin-2-ylamino)propyl!indazol-7-ylcarbonylamino!-2-(2,4,6-trimethylbenzenesulfonylamino)propionic acid,

3-�3-�3-(imidazolin-2-ylamino)propyl!indazol-7-ylcarbonylamino!-2-(benzenesulfonylamino)propionic acid,

3-(1-methyl-3-�3-(imidazolin-2-ylamino)propyl!indazol-7-ylcarbonylamino!-2-(2,6-dichlorobenzenesulfonylamino)propionic acid,

3-�3-�3-(imidazolin-2-ylamino)propyl!indazol-7-ylcarbonylamino!-2-(3,5-dimethylisoxazol-4-ylsulfonylamino)propionic acid,

3-�1-methyl-3-�3-(imidazolin-2-ylamino)propyl!indazol-7-ylcarbonylamino!-2-(2,6-dimethylbenzenesulfonylamino)propionic acid,

3-�3-�3-(imidazolin-2-ylamino)propyl!indazol-7-ylcarbonylamino!-2-(2,6-dimethyl-4-phenylbenzenesulfonylamino)propionic acid,

3-�1-methyl-3-(3-(imidazolin-2-ylamino)propyl!indazol-7-ylcarbonylamino!-2-(4-phenylbenzenesulfonylamino)propionic acid,

3-�3-�3-(tetrahydropyrimid-2-ylamino)propyl!indazol-7-ylcarbonylamino!-2-(benzyloxycarbonylamino)propionic acid,

3-�1-methyl-3-�3-(tetrahydropyrimid-2-ylamino)propyl!indazol-7-ylcarbonylamino!-2-(2,4,6-trimethylbenzenesulfonylamino)propionic acid,

3-�3-�3-(tetrahydropyrimid-2-ylamino)propyl!indazol-7-ylcarbonylamino!-2-(benzenesulfonylamino)propionic acid,

3-�1-methyl-3-�3-(tetrahydropyrimid-2-ylamino)propyl!indazol-7-ylcarbonylamino!-2-(2,6-dichlorobenzenesulfonylamino)propionic acid,

3-�3-�3-(tetrahydropyrimid-2-ylamino)propyl!indazol-7-ylcarbonylamino!-2-(3,5-dimethylisoxazol-4-ylsulfonylamino)propionic acid,

3-�1-methyl-3-�3-(tetrahydropyrimid-2-ylamino)propyl!indazol-7-ylcarbonylamino!-2-(2,6-dimethylbenzenesulfonylamino)propionic acid,

3-�3-�3-(tetrahydropyrimid-2-ylamino)propyl!indazol-7-ylcarbonylamino!-2-(2,6-dimethyl-4phenylbenzenesulfonylamino)propionic acid,

3-�1-methyl-3-�3-(tetrahydropyrimid-2-ylamino)propyl!indazol-7-ylcarbonylamino!-2-(4-phenylbenzenesulfonylamino)propionic acid,

3-�3-�3-(imidazol-2-ylamino)propyl!indazol-7-ylcarbonylamino!-2-(benzyloxycarbonylamino)propionic acid,

3-�1-methyl-3-�3-(imidazol-2-ylamino)propyl!indazol-7-ylcarbonylamino!-2-(2,4,6-trimethylbenzenesulfonylamino)propionic acid,

3-�3-�3-(imidazol-2-ylamino)propyl!indazol-7-ylcarbonylamino!-2-(benzenesulfonylamino)propionic acid,

3-�1-methyl-3-�3-(imidazol-2-ylamino)propyl!indazol-7-ylcarbonylamino!-2-(2,6-dichlorobenzenesulfonylamino)propionic acid,

3-�3-�3-(imidazol-2-ylamino)propyl!indazol-7-ylcarbonylamino!-2-(3,5-dimethylisoxazol-4-ylsulfonylamino)propionic acid,

3-�1-methyl-3-�3-(imidazol-2-ylamino)propyl!indazol-7-ylcarbonylamino!-2-(2,6-dimethylbenzenesulfonylamino)propionic acid,

3-�3-�3-(imidazol-2-ylamino)propyl!indazol-7-ylcarbonylamino!-2-(2,6-dimethyl-4-phenylbenzenesulfonylamino)propionic acid,

3-�1-methyl-3-�3-(imidazol-2-ylamino)propyl!indazol-7-ylcarbonylamino!-2-(4-phenylbenzenesulfonylamino)propionic acid,

3-�3-�3-(pyridin-2-ylamino)propyl!indazol-7-ylcarbonylamino!-2-(benzyloxycarbonylamino)propionic acid,

3-�1-methyl-3-�3-(pyridin-2-ylamino)propyl!indazol-7-ylcarbonylamino!-2-(2,4,6-trimethylbenzenesulfonylamino)propionic acid,

3-�3-�3-(pyridin-2-ylamino)propyl!indazol-7-ylcarbonylamino!-2-(benzenesulfonylamino)propionic acid,

3-�1-methyl-3-�3-(pyridin-2-ylamino)propyl!indazol-7-ylcarbonylamino!-2-(2,6-dichlorobenzenesulfonylamino)propionic acid,

3-�3-�3-(pyridin-2-ylamino)propyl!indazol-7-ylcarbonylamino!-2-(3,5-dimethylisoxazol-4-ylsulfonylamino)propionic acid,

3-�1-methyl-3-�3-(pyridin-2-ylamino)propyl!indazol-7-ylcarbonylamino!-2-(2,6-dimethylbenzenesulfonylamino)propionic acid,

3-�3-�3-(pyridin-2-ylamino)propyl!indazol-7-ylcarbonylamino!-2-(2,6-dimethyl-4-phenylbenzenesulfonylamino)propionic acid, and

3-�1-methyl-3-�3-(pyridin-2-ylamino)propyl!indazol-7-ylcarbonylamino!-2-(4-phenylbenzenesulfonylamino)propionic acid;

and ester forms thereof, said esters being chosen from the group consisting of:

methyl,

ethyl,

isopropyl,

n-butyl,

isobutyl,

benzyl,

methylcarbonyloxymethyl,

ethylcarbonyloxymethyl,

tert-butylcarbonyloxymethyl,

cyclohexylcarbonyloxymethyl,

tert-butyloxycarbonyloxymethyl,

dimethylaminoethyl, and

diethylaminoethyl.

11. A compound of Formula Ic: ##STR91## and pharmaceutically acceptable salt forms thereof, wherein: X.sup.1, X.sup.2, X.sup.3, and X.sup.4 are independently selected from nitrogen or carbon provided that at least two of X.sup.1, X.sup.2, X.sup.3 and X.sup.4 are carbon;

R.sup.1 is selected from: ##STR92## A and B are independently --CH.sub.2 --, --O--, --N(R.sup.2)--, or --C(.dbd.O)--;

A.sup.1 and B.sup.1 are independently --CH.sub.2 -- or --N(R.sup.3)--;

D is --N(R.sup.2)--, --O--, --S--, --C(.dbd.O)-- or --SO.sub.2 --;

E--F is --C(R.sup.4).dbd.C(R.sup.5)--, --N.dbd.C(R.sup.4)--, --C(R.sup.4).dbd.N--, or --C(R.sup.4).sub.2 C(R.sup.5).sub.2 --;

J, K, L and M are independently selected from --C(R.sup.4)--, --C(R.sup.5)-- or --N--, provided that at least one of J, K, L and M is not --N--;

R.sup.2 is selected from: H, C.sub.1 -C.sub.6 alkyl, (C.sub.1 -C.sub.6 alkyl)carbonyl, (C.sub.1 -C.sub.6 alkoxy)carbonyl; (C.sub.1 -C.sub.6 alkyl)aminocarbonyl, C.sub.3 -C.sub.6 alkenyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.4 -C.sub.11 cycloalkylalkyl, aryl, heteroaryl(C.sub.1 -C.sub.6 alkyl)carbonyl, heteroarylcarbonyl, aryl C.sub.1 -C.sub.6 alkyl, (C.sub.1 -C.sub.6 alkyl)carbonyl, or arylcarbonyl, C.sub.1 -C.sub.6 alkylsulfonyl, arylsulfonyl, aryl(C.sub.1 -C.sub.6 alkyl)sulfonyl, heteroarylsulfonyl, heteroaryl(C.sub.1 -C.sub.6 alkyl)sulfonyl, aryloxycarbonyl, or aryl(C.sub.1 -C.sub.6 alkoxy)carbonyl, wherein said aryl groups are substituted with 0-2 substituents selected from the group consisting of C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, halo, CF.sub.3, and nitro;

R.sup.3 is selected from: H, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.4 -C.sub.11 cycloalkylalkyl, aryl, aryl(C.sub.1 -C.sub.6 alkyl)-, or heteroaryl(C.sub.1 -C.sub.6 alkyl)-;

R.sup.4 and R.sup.5 are independently selected from: H, C.sub.1 -C.sub.4 alkoxy, NR.sup.2 R.sup.3, halogen, NO.sub.2, CN, CF.sub.3, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 alkenyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.4 -C.sub.11 cycloalkylalkyl, aryl, aryl(C.sub.1 -C.sub.6 alkyl)-, (C.sub.1 -C.sub.6 alkyl)carbonyl, (C.sub.1 -C.sub.6 alkoxy)carbonyl, arylcarbonyl, or

alternatively, when substituents on adjacent atoms, R.sup.4 and R.sup.5 can be taken together with the carbon atoms to which they are attached to form a 5-7 membered carbocyclic or 5-7 membered heterocyclic aromatic or non-aromatic ring system, said carbocyclic or heterocyclic ring being optionally substituted with 0-2 groups selected from: C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, halo, cyano, amino, CF.sub.3, or NO.sub.2 ;

U is selected from:

--(CH.sub.2).sub.n --,

--(CH.sub.2).sub.n (CR.sup.7 .dbd.CR.sup.8)(CH.sub.2).sub.m --

--(CH.sub.2).sub.n (C.tbd.C)(CH.sub.2).sub.m --

--(CH.sub.2).sub.t Q(CH.sub.2).sub.m --

--(CH.sub.2).sub.n O(CH.sub.2).sub.m --,

--(CH.sub.2).sub.n N(R.sup.6)(CH.sub.2).sub.m --,

--(CH.sub.2).sub.n C(.dbd.O)(CH.sub.2).sub.m --,

--(CH.sub.2).sub.n (C.dbd.O)N(R.sup.6)(CH.sub.2).sub.m --

--(CH.sub.2).sub.n N(R.sup.6)(C.dbd.O)(CH.sub.2).sub.m --, or

--(CH.sub.2).sub.n S(O).sub.p (CH.sub.2).sub.m --;

wherein one of the methylene groups is optionally substituted with R.sup.7 ;

Q is selected from 1,2-cycloalkylene, 1,2-phenylene, 1,3-phenylene, 1,4-phenylene, 2,3-pyridinylene, 3,4-pyridinylene, 2,4-pyridinylene, or 3,4-pyridazinylene;

R.sup.6 is selected from: H, C.sub.1 -C.sub.4 alkyl, or benzyl;

R.sup.7 and R.sup.8 are independently selected from: H, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.4 -C.sub.11 cycloalkylalkyl, aryl, aryl(C.sub.1 -C.sub.6 alkyl)-, or heteroaryl(C.sub.0 -C.sub.6 alkyl)-;

R.sup.9 is selected from: H, CO.sub.2 R.sup.17, C(.dbd.O)R.sup.17, CONR.sup.17 R.sup.20, --SO.sub.2 R.sup.17, --SO.sub.2 NR.sup.17 R.sup.20, C.sub.1 -C.sub.6 alkyl substituted with 0-1 R.sup.15 or 0-1 R.sup.21, C.sub.3 -C.sub.6 alkenyl substituted with 0-1 R.sup.15 or 0-1 R.sup.21, C.sub.3 -C.sub.7 cycloalkyl substituted with 0-1 R.sup.15 or 0-1 R.sup.21, C.sub.4 -C.sub.11 cycloalkylalkyl substituted with 0-1 R.sup.15 or 0-1 R.sup.21, aryl substituted with 0-1 R.sup.15 or 0-2 R.sup.11 or 0-1 R.sup.21, or aryl(C.sub.1 -C.sub.6 alkyl)- substituted with 0-1 R.sup.15 or 0-2 R.sup.11 or 0-1 R.sup.21 ;

R.sup.11 is selected from H, halogen, CF.sub.3, CN, NO.sub.2 , hydroxy, NR.sup.2 R.sup.3, C.sub.1 -C.sub.4 alkyl substituted with 0-1 R.sup.21, C.sub.1 -C.sub.4 alkoxy substituted with 0-1 R.sup.21, aryl substituted with 0-1 R.sup.21, aryl(C.sub.1 -C.sub.6 alkyl)- substituted with 0-1 R.sup.21, (C.sub.1 -C.sub.4 alkoxy)carbonyl substituted with 0-1 R.sup.21, (C.sub.1 -C.sub.4 alkyl)carbonyl substituted with 0-1 R.sup.21, C.sub.1 -C.sub.4 alkylsulfonyl substituted with 0-1 R.sup.21, or C.sub.1 -C.sub.4 alkylaminosulfonyl substituted with 0-1 R.sup.21 ;

W is selected from:

--(C(R.sup.12).sub.2).sub.q C(.dbd.O)N(R.sup.13)--, or

--C(.dbd.O)--N(R.sup.13)--(C(R.sup.12).sub.2).sub.q --;

X is --C(R.sup.12)(R.sup.14)--C(R.sup.12)(R.sup.15)--; or

alternatively, W and X can be taken together to be ##STR93## R.sup.12 is selected from: H, halogen, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkynyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.4 -C.sub.10 cycloalkylalkyl, (C.sub.1 -C.sub.4 alkyl)carbonyl, aryl, or aryl(C.sub.1 -C.sub.6 alkyl)-;

R.sup.13 is selected from: H, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.7 cycloalkylmethyl, or aryl(C.sub.1 -C.sub.6 alkyl)-;

R.sup.14 is selected from:

H, C.sub.1 -C.sub.6 alkylthio(C.sub.1 -C.sub.6 alkyl)-, aryl(C.sub.1 -C.sub.10 alkylthioalkyl)-, aryl(C.sub.1 -C.sub.10 alkoxyalkyl)-, C.sub.1 -C.sub.10 alkyl, C.sub.1 -C.sub.10 alkoxyalkyl, C.sub.1 -C.sub.6 hydroxyalkyl, C.sub.2 -C.sub.10 alkenyl, C.sub.2 -C.sub.10 alkynyl, C.sub.3 -C.sub.10 cycloalkyl, C.sub.3 -C.sub.10 cycloalkylalkyl, aryl(C.sub.1 -C.sub.6 alkyl)-, heteroaryl(C.sub.1 -C.sub.6 alkyl)-, aryl, heteroaryl, CO.sub.2 R.sup.17, C(.dbd.O)R.sup.17, or CONR.sup.17 R.sup.20, provided that any of the above alkyl, cycloalkyl, aryl or heteroaryl groups may be unsubstituted or substituted independently with 0-1 R.sup.16 or 0-2 R.sup.11 ;

R.sup.15 is selected from:

H, R.sup.16, C.sub.1 -C.sub.10 alkyl, C.sub.1 -C.sub.10 alkoxyalkyl, C.sub.1 -C.sub.10 alkylaminoalkyl, C.sub.1 -C.sub.10 dialkylaminoalkyl, (C.sub.1 -C.sub.10 alkyl)carbonyl, aryl(C.sub.0 -C.sub.6 alkyl)carbonyl, C.sub.1 -C.sub.10 alkenyl, C.sub.1 -C.sub.10 alkynyl, C.sub.3 -C.sub.10 cycloalkyl, C.sub.3 -C.sub.10 cycloalkylalkyl, aryl(C.sub.1 -C.sub.6 alkyl)-, heteroaryl(C.sub.1 -C.sub.6 alkyl)-, aryl, heteroaryl, CO.sub.2 R.sup.17, C(.dbd.O)R.sup.17, CONR.sup.17 R.sup.20, SO.sub.2 R.sup.17, or SO.sub.2 NR.sup.17 R.sup.20, provided that any of the above alkyl, cycloalkyl, aryl or heteroaryl groups may be unsubstituted or substituted independently with 0-2 R.sup.11 ;

Y is selected from:

--COR.sup.19, --SO.sub.3 H, --PO.sub.3 H, tetrazolyl, --CONHNHSO.sub.2 CF.sub.3, --CONHSO.sub.2 R.sup.17, --CONHSO.sub.2 NHR.sup.17, --NHCOCF.sub.3, --NHCONHSO.sub.2 R.sup.17, --NHSO.sub.2 R.sup.17, --OPO.sub.3 H.sub.2, --OSO.sub.3 H, --PO.sub.3 H.sub.2, --SO.sub.3 H, --SO.sub.2 NHCOR.sup.17, --SO.sub.2 NHCO.sub.2 R.sup.17, ##STR94## R.sup.16 is selected from: --N(R.sup.20)--C(.dbd.O)--O--R.sup.17,

--N(R.sup.20)--C(.dbd.O)--R.sup.17,

--N(R.sup.20)--C(.dbd.O)--NH--R.sup.17,

--N(R.sup.20)SO.sub.2 --R.sup.17, or

--N(R.sup.20)SO.sub.2 --NR.sup.20 R.sup.17 ;

R.sup.17 is selected from:

C.sub.1 -C.sub.10 alkyl, C.sub.3 -C.sub.11 cycloalkyl, aryl(C.sub.1 -C.sub.6 alkyl)-, (C.sub.1 -C.sub.6 alkyl)aryl, heteroaryl(C.sub.1 -C.sub.6 alkyl)-, (C.sub.1 -C.sub.6 alkyl)heteroaryl, biaryl(C.sub.1 -C.sub.6 alkyl)-, heteroaryl, or aryl, wherein said aryl or heteroaryl groups are optionally substituted with 0-3 substituents selected from the group consisting of: C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, aryl, heteroaryl, halo, cyano, amino, CF.sub.3, and NO.sub.2 ;

R.sup.18 is selected from:

H,

--C(.dbd.O)--O--R.sup.17,

--C(.dbd.O)--R.sup.17,

--C(.dbd.O)--NH--R.sup.17,

--SO.sub.2 --R.sup.17, or

--SO.sub.2 --NR.sup.20 R.sup.17 ;

R.sup.19 is selected from hydroxy, C.sub.1 -C.sub.10 alkyloxy, C.sub.3 -C.sub.11 cycloalkyloxy, aryloxy, aryl(C.sub.1 -C.sub.6 alkoxy)-, C.sub.3 -C.sub.10 alkylcarbonyloxyalkyloxy, C.sub.3 -C.sub.10 alkoxycarbonyloxyalkyloxy, C.sub.2 -C.sub.10 alkoxycarbonylalkyloxy, C.sub.5 -C.sub.10 cycloalkylcarbonyloxyalkyloxy, C.sub.5 -C.sub.10 cycloalkoxycarbonyloxyalkyloxy, C.sub.5 -C.sub.10 cycloalkoxycarbonylalkyloxy, C.sub.7 -C.sub.11 aryloxycarbonylalkyloxy, C.sub.8 -C.sub.12 aryloxycarbonyloxyalkyloxy, C.sub.8 -C.sub.12 arylcarbonyloxyalkyloxy, C.sub.5 -C.sub.10 alkoxyalkylcarbonyloxyalkyloxy, C.sub.5 -C.sub.10 (5-alkyl-1,3-dioxa-cyclopenten-2-one-yl)methyloxy, C.sub.10 -C.sub.14 (5-aryl-1,3-dioxa-cyclopenten-2-one-yl)methyloxy, or (R.sup.11)(R.sup.12)N--(C.sub.1 -C.sub.10 alkoxy)-;

R.sup.20 is selected from: H, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.4 -C.sub.11 cycloalkylalkyl, aryl, aryl(C.sub.1 -C.sub.6 alkyl)-, or heteroaryl(C.sub.1 -C.sub.6 alkyl)-;

R.sup.21 is selected from COOH or NR.sup.6.sub.2 ;

m is 0-4;

n is 0-4;

p is 0-2;

q is 0-2; and

r is 0-2;

with the following provisos:

(1) t, n, m and q are chosen such that the number of atoms connecting R.sup.1 and Y is in the range of 10-14; and

(2) n and m are chosen such that the value of n plus m is greater than one unless U is --(CH.sub.2).sub.t Q(CH.sub.2).sub.m --.

12. A compound of claim 11 of the Formula Ic: ##STR95## and pharmaceutically acceptable salt forms thereof wherein: X.sup.1, X.sup.2, X.sup.3, and X.sup.4 are independently selected from nitrogen or carbon provided that at least two of X.sup.1, X.sup.2, X.sup.3 and X.sup.4 are carbon;

R.sup.1 is selected from: ##STR96## A and B are independently --CH.sub.2 --, --O--, --N(R.sup.2)--, or --C(.dbd.O)--;

A.sup.1 and B.sup.1 are independently --CH.sub.2 -- or --N(R.sup.3)--;

D is --N(R.sup.2)--, --O--, --S--, --C(.dbd.O)-- or --SO.sub.2 --;

E--F is --C(R.sup.4).dbd.C(R.sup.5)--, --N.dbd.C(R.sup.4)--, --C(R.sup.4).dbd.N--, or --C(R.sup.4).sub.2 C(R.sup.5).sub.2 --;

J, K, L and M are independently selected from: --C(R.sup.4)--, --C(R.sup.5)-- or --N--, provided that at least one of J, K, L and M is not --N--;

R.sup.2 is selected from: H, C.sub.1 -C.sub.6 alkyl, (C.sub.1 -C.sub.6 alkyl)carbonyl, (C.sub.1 -C.sub.6 alkoxy)carbonyl, C.sub.1 -C.sub.6 alkylaminocarbonyl, C.sub.3 -C.sub.6 alkenyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.4 -C.sub.11 cycloalkylalkyl, aryl, heteroaryl(C.sub.1 -C.sub.6 alkyl)carbonyl, heteroarylcarbonyl, aryl(C.sub.1 -C.sub.6 alkyl)-, (C.sub.1 -C.sub.6 alkyl)carbonyl, arylcarbonyl, alkylsulfonyl, arylsulfonyl, aryl(C.sub.1 -C.sub.6 alkyl)sulfonyl, heteroarylsulfonyl, heteroaryl(C.sub.1 -C.sub.6 alkyl)sulfonyl, aryloxycarbonyl, aryl(C.sub.1 -C.sub.6 alkoxy)carbonyl, wherein said aryl groups are substituted with 0-2 substituents selected from the group consisting of C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, halo, CF.sub.3, and nitro;

R.sup.3 is selected from: H, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.4 -C.sub.11 cycloalkylalkyl, aryl, aryl(C.sub.1 -C.sub.6 alkyl)-, or heteroaryl(C.sub.1 -C.sub.6 alkyl)-;

R.sup.4 and R.sup.5 are independently selected from: H, C.sub.1 -C.sub.4 alkoxy, NR.sup.2 R.sup.3, halogen, NO.sub.2, CN, CF.sub.3, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 alkenyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.4 -C.sub.11 cycloalkylalkyl, aryl, aryl(C.sub.1 -C.sub.6 alkyl)-, C.sub.2 -C.sub.7 alkylcarbonyl, arylcarbonyl or

alternatively, when substituents on adjacent atoms, R.sup.4 and R.sup.5 can be taken together with the carbon atoms to which they are attached to form a 5-7 membered carbocyclic or 5-7 membered heterocyclic aromatic or non-aromatic ring system, said carbocyclic or heterocyclic ring being optionally substituted with 0-2 groups selected from: C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, halo, cyano, amino, CF.sub.3, or NO.sub.2 ;

U is selected from:

--(CH.sub.2).sub.n --,

--(CH.sub.2).sub.n (CR.sup.7 .dbd.CR.sup.8)(CH.sub.2).sub.m --

--(CH.sub.2).sub.t Q(CH.sub.2).sub.m --,

--(CH.sub.2).sub.n O(CH.sub.2).sub.m --,

--(CH.sub.2).sub.n N(R.sup.6)(CH.sub.2).sub.m --,

--(CH.sub.2).sub.n C(.dbd.O)(CH.sub.2).sub.m --, or

--(CH.sub.2).sub.n S(O).sub.p (CH.sub.2).sub.m --;

wherein one of the methylene groups is optionally substituted with R.sup.7 ;

Q is selected from 1,2-phenylene, 1,3-phenylene, 2,3-pyridinylene, 3,4-pyridinylene, or 2,4-pyridinylene;

R.sup.6 is selected from: H, C.sub.1 -C.sub.4 alkyl, or benzyl;

R.sup.7 and R.sup.8 are independently selected from: H, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.4 -C.sub.11 cycloalkylalkyl, aryl, aryl(C.sub.1 -C.sub.6 alkyl)-, or heteroaryl(C.sub.0 -C.sub.6 alkyl)-;

R.sup.9 is selected from: H, CO.sub.2 R.sup.17, C(.dbd.O)R.sup.17, CONR.sup.17 R.sup.20, --SO.sub.2 R.sup.17, --SO.sub.2 NR.sup.17 R.sup.20, C.sub.1 -C.sub.6 alkyl substituted with 0-1 R.sup.15 or 0-1 R.sup.21, C.sub.3 -C.sub.6 alkenyl substituted with 0-1 R.sup.15 or 0-1 R.sup.21, C.sub.3 -C.sub.7 cycloalkyl substituted with 0-1 R.sup.15 or 0-1 R.sup.21, C.sub.4 -C.sub.11 cycloalkylalkyl substituted with 0-1 R.sup.15 or 0-1 R.sup.21, aryl substituted with 0-1 R.sup.15 or 0-2 R.sup.11 or 0-1 R.sup.21, or aryl(C.sub.1 -C.sub.6 alkyl)- substituted with 0-1 R.sup.15 or 0-2 R.sup.11 or 0-1 R.sup.21 ;

R.sup.11 is selected from: H, halogen, CF.sub.3, CN, NO.sub.2, hydroxy, NR.sup.2 R.sup.3, C.sub.1 -C.sub.4 alkyl substituted with 0-1 R.sup.21, C.sub.1 -C.sub.4 alkoxy substituted with 0-1 R.sup.21, aryl substituted with 0-1 R.sup.21, aryl(C.sub.1 -C.sub.6 alkyl)- substituted with 0-1 R.sup.21, (C.sub.1 -C.sub.4 alkoxy)carbonyl substituted with 0-1 R.sup.21, (C.sub.1 -C.sub.4 alkyl)carbonyl substituted with 0-1 R.sup.21, C.sub.1 -C.sub.4 alkylsulfonyl substituted with 0-1 R.sup.21, or C.sub.1 -C.sub.4 alkylaminosulfonyl substituted with 0-1 R.sup.21 ;

W is --C(.dbd.O)--N(R.sup.13)--(C(R.sup.12).sub.2).sub.q --;

X is --C(R.sup.12)(R.sup.14)--C(R.sup.12)(R.sup.15)--;

alternatively, W and X can be taken together to be ##STR97## R.sup.12 is H or C.sub.1 -C.sub.6 alkyl; R.sup.13 is selected from: H, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.7 cycloalkylmethyl, or aryl(C.sub.1 -C.sub.6 alkyl)-;

R.sup.14 is selected from:

H, C.sub.1 -C.sub.6 alkylthioalkyl, aryl(C.sub.1 -C.sub.10 alkylthioalkyl)-, aryl(C.sub.1 -C.sub.10 alkoxyalkyl)-, C.sub.1 -C.sub.10 alkyl, C.sub.1 -C.sub.10 alkoxyalkyl, C.sub.1 -C.sub.6 hydroxyalkyl, C.sub.2 -C.sub.10 alkenyl, C.sub.2 -C.sub.10 alkynyl, C.sub.3 -C.sub.10 cycloalkyl, C.sub.3 -C.sub.10 cycloalkylalkyl, aryl(C.sub.1 -C.sub.6 alkyl)-, heteroaryl(C.sub.1 -C.sub.6 alkyl)-, aryl, heteroaryl, CO.sub.2 R.sup.17, C(.dbd.O)R.sup.17, CONR.sup.17 R.sup.20, provided that any of the above alkyl, cycloalkyl, aryl or heteroaryl groups may be unsubstituted or substituted independently with 0-1 R.sup.16 or 0-2 R.sup.11 ;

R.sup.15 is selected from:

H, R.sup.16, C.sub.1 -C.sub.10 alkyl, C.sub.1 -C.sub.10 alkoxyalkyl, C.sub.1 -C.sub.10 alkylaminoalkyl, C.sub.1 -C.sub.10 dialkylaminoalkyl, C.sub.1 -C.sub.10 alkylcarbonyl, aryl(C.sub.0 -C.sub.6 alkyl)carbonyl, C.sub.2 -C.sub.10 alkenyl, C.sub.2 -C.sub.10 alkynyl, C.sub.3 -C.sub.10 cycloalkyl, C.sub.3 -C.sub.10 cycloalkylalkyl, aryl(C.sub.1 -C.sub.6 alkyl)-, heteroaryl(C.sub.1 -C.sub.6 alkyl)-, aryl, heteroaryl, CO.sub.2 R.sup.17, C(.dbd.O)R.sup.17, CONR.sup.17 R.sup.20, SO.sub.2 R.sup.17, or SO.sub.2 NR.sup.17 R.sup.20, provided that any of the above alkyl, cycloalkyl, aryl or heteroaryl groups may be unsubstituted or substituted independently with 0-2 R.sup.11 ;

Y is selected from: ##STR98## R.sup.16 is selected from: --N(R.sup.20)--C(.dbd.O)--O--R.sup.17,

--N(R.sup.20)--C(.dbd.O)--R.sup.17,

--N(R.sup.20)--C(.dbd.O)--NH--R.sup.17,

--N(R.sup.20)SO.sub.2 --R.sup.17, or

--N(R.sup.20)SO.sub.2 --NR.sup.20 R.sup.17 ;

R.sup.17 is selected from:

C.sub.1 -C.sub.10 alkyl, C.sub.3 -C.sub.11 cycloalkyl, aryl(C.sub.1 -C.sub.6 alkyl)-, (C.sub.1 -C.sub.6 alkyl)aryl, heteroaryl(C.sub.1 -C.sub.6 alkyl)-, (C.sub.1 -C.sub.6 alkyl)heteroaryl, biaryl(C.sub.1 -C.sub.6 alkyl)-, heteroaryl, or aryl, wherein said aryl or heteroaryl groups are optionally substituted with 0-3 substituents selected from the group consisting of: C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, aryl, heteroaryl, halo, cyano, amino, CF.sub.3, and NO.sub.2 ;

R.sup.18 is selected from:

H,

--C(.dbd.O)--O--R.sup.17,

--C(.dbd.O)--R.sup.17,

--C(.dbd.O)--NH--R.sup.17,

--SO.sub.2 --R.sup.17, or

--SO.sub.2 --NR.sup.20 R.sup.17 ;

R.sup.19 is selected from: hydroxy, C.sub.1 -C.sub.10 alkyloxy, C.sub.3 -C.sub.11 cycloalkyloxy, C.sub.6 -C.sub.10 aryloxy, C.sub.7 -C.sub.11 aralkyloxy, C.sub.3 -C.sub.10 alkylcarbonyloxyalkyloxy, C.sub.3 -C.sub.10 alkoxycarbonyloxyalkyloxy, C.sub.2 -C.sub.10 alkoxycarbonylalkyloxy, C.sub.5 -C.sub.10 cycloalkylcarbonyloxyalkyloxy, C.sub.5 -C.sub.10 cycloalkoxycarbonyloxyalkyloxy, C.sub.5 -C.sub.10 cycloalkoxycarbonylalkyloxy, C.sub.7 -C.sub.11 aryloxycarbonylalkyloxy, C.sub.8 -C.sub.12 aryloxycarbonyloxyalkyloxy, C.sub.8 -C.sub.12 arylcarbonyloxyalkyloxy, C.sub.5 -C.sub.10 alkoxyalkylcarbonyloxyalkyloxy, C.sub.5 -C.sub.10 (5-alkyl-1,3-dioxa-cyclopenten-2-one-yl)methyloxy, C.sub.10 -C.sub.14 (5-aryl-1,3-dioxa-cyclopenten-2-one-yl)methyloxy, or (R.sup.11)(R.sup.12)N--(C.sub.1 -C.sub.10 alkoxy)-;

R.sup.20 selected from: H, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.4 -C.sub.11 cycloalkylalkyl, aryl(C.sub.1 -C.sub.6 alkyl)-, or heteroaryl(C.sub.1 -C.sub.6 alkyl)-;

R.sup.21 is selected from COOH or NR.sup.6.sub.2 ;

m is 0-4;

n is 0-4;

t is 0-4;

p is 0-2;

q is 0-2; and

r is 0-2.

13. A compound of claim 11 of the Formula IIe or IIf: ##STR99## and pharmaceutically acceptable salt forms thereof, wherein: R.sup.1 is selected from: ##STR100## wherein the above heterocycles are optionally substituted with 0-2 substituents selected from the group consisting of: NH.sub.2, halogen, NO.sub.2, CN, CF.sub.3, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.6 alkyl, and C.sub.3 -C.sub.7 cycloalkyl;

U is --(CH.sub.2).sub.n --, --CH.sub.2).sub.t Q(CH.sub.2).sub.m -- or --(.dbd.O)(CH.sub.2).sub.n-1 --, wherein one of the methylene groups is optionally substituted with R.sup.7 ;

Q is selected from 1,2-phenylene 1,3-phenylene, 2,3-pyridinylene, 3,4-pyridinylene, or 2,4-pyridinylene;

R.sup.6 is selected from: H, C.sub.1 -C.sub.4 alkyl, or benzyl;

R.sup.7 is selected from: C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.4 -C.sub.11 cycloalkylalkyl, aryl, aryl(C.sub.1 -C.sub.6 alkyl), heteroaryl, or heteroaryl(C.sub.1 -C.sub.6 alkyl);

R.sup.9 is selected from: H, --SO.sub.2 R.sup.17, --SO.sub.2 NR.sup.17 R.sup.20, C.sub.1 -C.sub.6 alkyl substituted with 0-1 R.sup.15 or 0-1 R.sup.21, C.sub.3 -C.sub.7 cycloalkyl substituted with 0-1 R.sup.15 or 0-1 R.sup.21, C.sub.4 -C.sub.11 cycloalkylalkyl substituted with 0-1 R.sup.15 or 0-1 R.sup.21, aryl substituted with 0-1 R.sup.15 or 0-2 R.sup.11 or 0-1 R.sup.21, or aryl(C.sub.1 -C.sub.6 alkyl)- substituted with 0-1 R.sup.15 or 0-2 R.sup.11 or 0-1 R.sup.21 ;

R.sup.11 is selected from H, halogen, CF.sub.3, CN, NO.sub.2, hydroxy, NR.sup.2 R.sup.3, C.sub.1 -C.sub.4 alkyl substituted with 0-1 R.sup.21, C.sub.1 -C.sub.4 alkoxy substituted with 0-1 R.sup.21, aryl substituted with 0-1 R.sup.21, aryl(C.sub.1 -C.sub.6 alkyl)- substituted with 0-1 R.sup.21, (C.sub.1 -C.sub.4 alkoxy)carbonyl substituted with 0-1 R.sup.21, (C.sub.1 -C.sub.4 alkyl)carbonyl substituted with 0-1 R.sup.21, C.sub.1 -C.sub.4 alkylsulfonyl substituted with 0-1 R.sup.21, or C.sub.1 -C.sub.4 alkylaminosulfonyl substituted with 0-1 R.sup.21 ;

W is --C(.dbd.O)--N(R.sup.13)--;

X is --CH(R.sup.14)--CH(R.sup.15)--;

R.sup.13 is H or CH.sub.3 ;

R.sup.14 is selected from:

H, C.sub.1 -C.sub.10 alkyl, aryl, or heteroaryl, wherein said aryl or heteroaryl groups are optionally substituted with 0-3 substituents selected from the group consisting of: C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, aryl, halo, cyano, amino, CF.sub.3, and NO.sub.2 ;

R.sup.15 is H or R.sup.16 ;

is --COR.sup.19 ;

R.sup.16 is selected from:

--NH(R.sup.20)--C(.dbd.O)--O--R.sup.17,

--N(R.sup.20)--C(.dbd.O)--R.sup.17,

--N(R.sup.20)--C(.dbd.O)--NH--R.sup.17,

--N(R.sup.20)SO.sub.2 --R.sup.17, or

--N(R.sup.20)SO.sub.2 --N(R.sup.20)R.sup.17 ;

.sup.17 is selected from:

C.sub.1 -C.sub.10 alkyl, C.sub.3 -C.sub.11 cycloalkyl, aryl(C.sub.1 -C.sub.6 alkyl)-, (C.sub.1 -C.sub.6 alkyl)aryl, heteroaryl(C.sub.1 -C.sub.6 alkyl)-, (C.sub.1 -C.sub.6 alkyl)heteroaryl, biaryl(C.sub.1 -C.sub.6 alkyl)-, heteroaryl, or aryl, wherein said aryl or heteroaryl groups are optionally substituted with 0-3 substituents selected from the group consisting of: C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, aryl, heteroaryl, halo, cyano, amino, CF.sub.3, and NO.sub.2 ;

R.sup.19 is selected from:

hydroxy, C.sub.1 -C.sub.10 alkoxy,

methylcarbonyloxymethoxy-,

ethylcarbonyloxymethoxy-,

t-butylcarbonyloxymethoxy-,

cyclohexylcarbonyloxymethoxy-,

1-(methylcarbonyloxy)ethoxy-,

1-(ethylcarbonyloxy)ethoxy-,

1-(t-butylcarbonyloxy)ethoxy-,

1-(cyclohexylcarbonyloxy)ethoxy-,

i-propyloxycarbonyloxymethoxy-,

t-butyloxycarbonyloxymethoxy-,

1-(i-propyloxycarbonyloxy)ethoxy-,

1-(cyclohexyloxycarbonyloxy)ethoxy-,

1-(t-butyloxycarbonyloxy)ethoxy-,

dimethylaminoethoxy-,

diethylaminoethoxy-,

(5-methyl-1,3-dioxacyclopenten-2-on-4-yl)methoxy-,

(5-(t-butyl)-1,3-dioxacyclopenten-2-on-4-yl)methoxy-,

(1,3-dioxa-5-phenyl-cyclopenten-2-on-4-yl)methoxy-, or

1-(2-(2-methoxypropyl)carbonyloxy)ethoxy-;

R.sup.20 is H or CH.sub.3 ;

R.sup.21 is selected from COOH or NR.sup.6.sub.2 ; and

m is 0 or 1;

n is 1-4; and

t is 0 or 1.

14. A compound of claim 11 of the Formula IIe or IIf: ##STR101## and pharmaceutically acceptable salt forms thereof, wherein: R.sup.1 is selected from: ##STR102## wherein the above heterocycles are optionally substituted with 0-2 substituents selected from the group consisting of: NH.sub.2, halogen, NO.sub.2, CN, CF.sub.3, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.6 alkyl, and C.sub.3 -C.sub.7 cycloalkyl:

U is --(CH.sub.2).sub.n --, --(CH.sub.2).sub.t Q(CH.sub.2).sub.m -- or --C(.dbd.O)(CH.sub.2).sub.n-1 --, wherein one of the methylene groups is optionally substituted with R.sup.7 ;

Q is selected from 1,2-phenylene, 1,3-phenylene, 2,3-pyridinylene, 3,4-pyridinylene, or 2,4-pyridinylene;

R.sup.6 selected from: H, C.sub.1 -C.sub.4 alkyl, or benzyl;

R.sup.7 is selected from C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.4 -C.sub.11 cycloalkylalkyl, aryl, aryl(C.sub.1 -C.sub.6 alkyl), heteroaryl, or heteroaryl(C.sub.1 -C.sub.6 alkyl);

R.sup.9 is selected from: H, --SO.sub.2 R.sup.17, --SO.sub.2 NR.sup.17 R.sup.20, C.sub.1 -C.sub.6 alkyl substituted with 0-1 R.sup.15 or 0-1 R.sup.21, C.sub.3 -C.sub.7 cycloalkyl substituted with 0-1 R.sup.15 or 0-1 R.sup.21, C.sub.4 -C.sub.11 cycloalkylalkyl substituted with 0-1 R.sup.15 or 0-1 R.sup.21, aryl substituted with 0-1 R.sup.15 or 0-2 R.sup.11 or 0-1 R.sup.21, or aryl(C.sub.1 -C.sub.6 alkyl)- substituted with 0-1 R.sup.15 or 0-2 R.sup.11 or 0-1 R.sup.21 ;

R.sup.11 is selected from H, halogen, CF.sub.3, CN, NO.sub.2, hydroxy, NR.sup.2 R.sup.3, C.sub.1 -C.sub.4 alkyl substituted with 0-1 R.sup.21, C.sub.1 -C.sub.4 alkoxy substituted with 0-1 R.sup.21, aryl substituted with 0-1 R.sup.21, aryl(C.sub.1 -C.sub.6 alkyl)- substituted with 0-1 R.sup.21, (C.sub.1 -C.sub.4 alkoxy)carbonyl substituted with 0-1 R.sup.21, (C.sub.1 -C.sub.4 alkyl)carbonyl substituted with 0-1 R.sup.21, C.sub.1 -C.sub.4 alkylsulfonyl substituted with 0-1 R.sup.21, or C.sub.1 -C.sub.4 alkylaminosulfonyl substituted with 0-1 R.sup.21 ; W is --C(.dbd.O)--N(R.sup.13)--;

W is --C(.dbd.O)--N(R.sup.13)--;

X is --CH(R.sup.14)--CH(R.sup.15)--;

R.sup.13 is H or CH.sub.3 ;

R.sup.14 is selected from:

H, C.sub.1 -C.sub.10 alkyl, aryl, or heteroaryl, wherein said aryl or heteroaryl groups are optionally substituted with 0-3 substituents selected from the group consisting of: C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, aryl, halo, cyano, amino, CF.sub.3, and NO.sub.2 ;

R.sup.15 is H or R.sup.16 ;

Y is --COR.sup.19 ;

R.sup.16 is selected from:

--NH(R.sup.20)--C(.dbd.O--O--R.sup.17,

--N(R.sup.20)--C(.dbd.O)--R.sup.17,

--N(R.sup.20)--C(.dbd.O)--NH--R.sup.17,

--N(R.sup.20)SO.sub.2 --R.sup.17, or

--N(R.sup.20)SO.sub.2 --NR.sup.20 R.sup.17 ;

R.sup.17 is selected from:

C.sub.1 -C.sub.10 alkyl, C.sub.3 -C.sub.11 cycloalkyl, aryl(C.sub.1 -C.sub.6 alkyl)-, (C.sub.1 -C.sub.6 alkyl)aryl, heteroaryl(C.sub.1 -C.sub.6 alkyl)-, (C.sub.1 -C.sub.6 alkyl)heteroaryl, biaryl(C.sub.1 -C.sub.6 alkyl)-, heteroaryl, or aryl, wherein said aryl or heteroaryl groups are optionally substituted with 0-3 substituents selected from the group consisting of: C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, aryl, heteroaryl, halo, cyano, amino, CF.sub.3, and NO.sub.2 ;

R.sup.19 is selected from:

hydroxy, C.sub.1 -C.sub.10 alkoxy,

methylcarbonyloxymethoxy-,

ethylcarbonyloxymethoxy-,

t-butylcarbonyloxymethoxy-,

cyclohexylcarbonyloxymethoxy-,

1-(methylcarbonyloxy)ethoxy-,

1-(ethylcarbonyloxy)ethoxy-,

1-(t-butylcarbonyloxy)ethoxy-,

1-(cyclohexylcarbonyloxy)ethoxy-,

i-propyloxycarbonyloxymethoxy-,

t-butyloxycarbonyloxymethoxy-,

1-(i-propyloxycarbonyloxy)ethoxy-,

1-(cyclohexyloxycarbonyloxy)ethoxy-,

1-(t-butyloxycarbonyloxy)ethoxy-,

dimethylaminoethoxy-,

diethylaminoethoxy-,

(5-methyl-1,3-dioxacyclopenten-2-on-4-yl)methoxy-,

(5-(t-butyl)-1,3-dioxacyclopenten-2-on-4-yl)methoxy-,

(1,3-dioxa-5-phenyl-cyclopenten-2-on-4-yl)methoxy-, or

1-(2-(2-methoxypropyl)carbonyloxy)ethoxy-;

R.sup.20 is H or CH.sub.3 ;

R.sup.21 is selected from COOH or NR.sup.6.sub.2 ; and

m is 0 or 1;

n is 1-4; and

t is 0 or 1.

15. A method for the treatment of cancer metastasis, diabetic retinopathy, neovascular glaucoma, thrombosis, restenosis, osteoporosis, or macular degeneration which comprises administering to a host in need of such treatment a therapeutically effective amount of a compound of any one of claims 1-14.

16. A pharmaceutical composition comprising a pharmaceutically acceptable carrier and a compound of any one of claims 1-14.