Boronic acid and ester inhibitors of thrombin

Abstract

Novel boronic acid and ester and carboxyl-modified amino acid compounds of the Formula I, which are inhibitors of trypsin-like enzymes, are disclosed:R.sup.1 --Z--CHR.sup.2 --A,where R.sup.1, Z, R.sup.2 arid A are defined within.

Description

FIELD OF THE INVENTION

This invention relates to the discovery of new boronic acid derivatives which are inhibitors of thrombin and pharmaceutical compositions thereof.

BACKGROUND OF THE INVENTION

Hemostasis is the normal physiological process in which bleeding from an injured blood vessel is arrested. It is a dynamic and complex process in which proteolytic enzymes such as thrombin play a key role. Blood coagulation may occur through either of two cascades of zymogen activations, the extrinsic and intrinsic pathways of the coagulation cascade. Factor VIIa in the extrinsic pathway, and Factor IXa in the intrinsic pathway are important determinants of the activation of factor X to factor Xa, which itself catalyzes the activation of prothrombin to thrombin. The last protease in each pathway is thrombin, which acts to hydrolyze four small peptides (two FpA and two FpB) from each molecule of fibrinogen, thus deprotecting its polymerization sites. Once formed, the linear fibrin polymers may be cross-linked by factor XIIIa, which is itself activated by thrombin. In addition, thrombin is a potent activator of platelets, upon which it acts at specific receptors. Thrombin activation of platelets leads to aggregation of the cells and secretion of additional factors that further accelerate the creation of a hemostatic plug. Thrombin also potentiates its own production by the activation of factors V and VIII (see Hemker and Beguin in: Jolles, et. al., "Biology and Pathology of Platelet Vessel Wall Interactions," pp. 219-26 (1986), Crawford and Scrutton in: Bloom and Thomas, "Haemostasis and Thrombosis," pp. 47-77, (1987), Bevers, et. al., Eur. J. Biochem. 1982, 122, 429-36, Mann, Trends Biochemo Sci. 1987, 12, 229-33).

Thrombosis may be regarded as the pathological condition wherein improper activity of the hemostatic mechanism results in intravascular thrombus formation. Etiological factors such as the presence of atherosclerotic plaque, phlebitis and septicemia may cause thrombosis, leading to impaired blood flow to the effected tissues and possible serious pathological consequences. Thrombosis may be reduced by inhibition of the normal process of blood coagulation by anticoagulants. Anticoagulants act by reducing the amount of thrombin which is generated, or by inhibiting with the proteolytic actions of thrombin.

Currently, two of the most effective classes of drugs in clinical use as anticoagulants are the heparins and the vitamin K antagonists. The heparins are ill-defined mixtures of sulfated polysaccharides that bind to, and thus potentiate the action of antithrombin III. Antithrombin III is a naturally occurring inhibitor of the activated clotting factors IXa, Xa, XIa, thrombin and probably XIIa (see Jaques, Pharmacol. Rev. 1980, 31, pp. 99-166). The vitamin K antagonists, of which warfarin is the most well-known example, act indirectly by inhibiting the post-ribosomal carboxylations of the vitamin K dependent coagulation factors II, VII, IX and X (see Hirsch, Semin. Thromb. Hemostasis 1986, 12, 1-11). While effective therapies for the treatment of thrombosis, heparins and vitamin K antagonists have the unfortunate side effects of bleeding and marked interpatient variability, resulting in a small and unpredictable therapeutic safety margin. The use of direct acting thrombin inhibitors is expected to alleviate these problems.

Anticoagulants are also necessary in the processing of blood for therapeutic or diagnostic purposes or for the production of blood products or fragments, since contact of blood with the surfaces commonly used for blood collection and storage causes activation of coagulation leading to thrombin formation and clot formation.

The coagulation proteases thrombin, factor Xa, factor VIIa, and factor IXa are serine proteases having trypsin-like specificity for the cleavage of sequence-specific Arg-Xxx peptide bonds. As with other serine proteases, the cleavage event begins with an attack of the active site serine on the scissile bond of the substrate, resulting in the formation of a tetrahedral intermediate. This is followed by collapse of the tetrahedral intermediate to form an acyl enzyme and release of the amino terminus of the cleaved sequence. Hydrolysis of the acyl enzyme then releases the carboxy terminus.

A number of naturally occurring thrombin inhibitors have been reported. These include nazumamide A from Theonella sp. (see Fusetani, et. al., Tetrahedron Lett. 1991, 32, 707314 4), cyclotheonamide A from Theonella sp. (see Fusetani, et. al., J. Am. Chem. Soc. 1990, 112, 7053-4), amblyommin from Amblyomma hebraeum (see Bonin, et. al., EP 345614), hirudin from Hirudo medicinalis, recombinant versions of hirudin and hirudin fragments (see Rigbl and Jackson, EP 352903, Koerwer, WO 9109946, Meyer, et. al., WO 9108233, Dawson, et. al., WO 9109125, Maraganore, et. al., WO 9102750 and Maraganore, EP 333356).

Synthetic thrombin inhibitors have also been disclosed. Arylsulfonylarginine amides such as (2R,4R)-4-methyl-1-�N.sup.2 -{(3-methyl-1,2,3,4-tetrahydro-8-quinolinyl)sulfonyl}-L-arginyl!-2-piperidinecarboxylate have been shown to be effective inhibitors of thrombin (see Okamoto, et. al. Thromb Res. 1976, 8, 77-82, Ohshiro, et. al., Blood Vessel 1983, 14, 216-8), as have compounds containing constrained arginine mimics such as (2-naphthylsulfonylglycyl)-4-amidino-phenylalanyl piperidide (see Stuerzebecher, et. al., Thromb. Res. 1983, 29, 635-42), 1-�2-�5-(dimethylamino)naphth-1-ylsulfonamido!-3-(2-iminohexahydropyrimidin-5-yl)propanoyl!-4-methylpiperidine dihydrochloride (see Ishikawa, JP 88227572 and Ishikawa and Inamura, JP 88227573), N-(trans-4-amino-methylcyclohexylcarbonyl)-4-O-(2-picolyl)-L-tyrosine 4-acetanilide dihydrochloride (see Okamoto, et. al., EP 217286) and 4-�(aminoiminomethyl)amino!benzoic acid esters (see Fuji, et. al., DE 3005580, Matsuoka, et. al., Jpn. J. Pharmacol. 1989, 51, 455-63, and Takeshita, et. al., EP 435235).

Inhibitor design has benefitted from the knowledge of the mechanism of action and of the peptide sequences which are thought to bind in the catalytic site of thrombin, e.g., -Gly-Val-Arg-Gly- of fibrinogen (see Blomback, et. al., J. Biol. Chem., 1972, 247, 1496-512), Ile-Pro-Arg-Ser- of prothrombin (see Magnussen, et. al., in: Reich, et. al., "Proteases and Biological Control," pp. 123-149 (1975)) and -Val-Pro-Arg-Gly- of factor XIII (see Takagi and Doolittle, Biochemistry 1974, 13, 750-6 and Nakamura, et. al., Biochemo Biophys. Res. Commun. 1974, 58, 250-256). This class of mechanism-based inhibitors are exemplified by the tripepride aldehyde D-Phe-Pro-N-Me-Arg-H (see Bajusz, et. al., J. Med. Chem. 1990, 33, 1729-35), the chloromethyl ketone Ac-D-Phe-Pro-ArgCH.sub.2 Cl (see Kettner and Shaw, Thromb. Res. 1979, 14, 969-73) and the trifluoromethyl ketone D-Phe-Pro-ArgCF.sub.3 (see Kolb, et. al., U.S. Pat. No. 697,987).

Kettner and Shenvi (EP 293881, published Jun. 12, 1988), disclose peptide boronic acid inhibitors of trypsin-like proteases of formula (1)

R.sup.1 -�(A.sup.3).sub.q (A.sup.2).sub.p (A.sup.1).sub.o !.sub.n -NH-CHR.sup.2 -BY.sup.1 Y.sup.2 ( 1) wherein Y.sup.1 and Y.sup.2, independently, are hydroxyl or fluoro or, taken together, form a moiety derived from a dihydroxy compound having at least two hydroxy groups separated by at least two connecting atoms in a chain or ring, said chain or ring comprising 1 to about 20 carbon atoms and, optionally, a heteroatom which can be N, S, or O; R.sup.2 is a substituted alkyl selected from the group consisting of --(CH.sub.2).sub.z --X, --(CH(CH.sub.3)--(CH.sub.2).sub.2 --X, --CH.sub.2 --CH--(CH.sub.3)--CH.sub.2 --X, --(CH.sub.2).sub.2 --CH (CH.sub.3)--X and --(CH.sub.2).sub.2 --CH(CH.sub.3).sub.2 --X, where X is --NH.sub.2, --NH--C(NH)--NH.sub.2 or --S--C(NH)--NH.sub.2, and z is 3 to 5; n, o, p and q are, independently, either 0 or 1; A.sup.1, A.sup.2 and A.sup.3 are, independently, amino acids of L- or D-configuration selected from the group consisting of Ala, Arg, Asn, Asp, Cys, Gln, Glu, Gly, His, Ile, Leu, Lys, Met, Phe, Pro, Ser, Thr, Trp, Tyr and Val; and R.sup.1 is a peptide comprised of 1 to about 20 amino acids, an acyl or a sulfonyl group comprised of 1 to about 20 carbon atoms, H, or an N-terminal protecting group. In this disclosure, Kettner and Shenvi demonstrated that the pinanediol esters of boropeptides are pharmacogolically equivalent to the corresponding boronic acids. Metternich (EP 0471651 A2) discloses borolysine thrombin inhibitors of formula (2) W-Y-NR.sup.4 -CHR.sup.5 -BQ.sup.1 Q.sup.2 ( 2) wherein W is an N-protecting group; Y is a sequence of n amino acids such that the n+1 amino acid peptide Y-Lys or Y-Arg has an affinity for the active site of a trypsin-like protease; where n is an integer of from 1 to 10 and in which at least one amino acid is an unnatural amino acid having a hydrophobic side chain; Q.sup.1 and Q.sup.2 are the same or different and are selected from --OH, --COR.sub.1, --CONR.sub.1 R.sub.2, --NR.sub.1 R.sub.2 or --OR.sub.3 of Q.sup.1 and Q.sup.2 taken together form a diol residue; R.sub.1, R.sub.2 and R.sub.3 which may be the same or different, are C.sub.1-10 alkyl, C.sub.6-10 aryl, C.sub.6-10 aralkyl, or phenyl substituted by up to three groups selected from C.sub.1-4 alkyl, halogen and C.sub.1-4 alkoxy; R.sub.4 is hydrogen or C.sub.1-10 alkyl; R.sub.5 is a group --A--X; wherein A is --(CH.sub.2).sub.z -- in which z is 2, 3, 4 or 5; --CH(CH.sub.3)--(CH.sub.2).sub.2 --; --CH.sub.2 --CH(CH.sub.3)--CH.sub.2 --; --(CH.sub.2).sub.2 --CH(CH.sub.3)--; --(CH.sub.2).sub.2 --C(CH.sub.3).sub.2 --; CH(CH.sub.3)--(CH.sub.2).sub.3 --; --CH.sub.2 --CH(CH.sub.3)--(CH.sub.2).sub.2 --; --CH.sub.2 --CH.sub.2 --CH(CH.sub.3)--CH.sub.2 --; --(CH.sub.2).sub.3 --CH(CH.sub.3)--; --(CH.sub.2).sub.3 --C(CH.sub.3).sub.2 : C.sub.6-10 aryl C.sub.6-10 aralkyl and X is --NH.sub.2, --NH--C(NH)--NH.sub.2, --S--C(NH)--NH.sub.2, N.sub.3, -C.sub.1-4 alkoxy, C.sub.1-4 alkylthio or Si(CH.sub.3).sub.3 or R.sub.4 and R.sub.5 taken together form a trimethylene group and the asymmetric carbon atom may have the D- or L-configuration or represent any mixture of these.

Surprising for their lack of a basic residue at P.sub.1 are tripeptide thrombin inhibitors comprised of 1-aminoboronic and 1-aminophosphonic acid analogs of 3-methoxy-propylglycine (see Claeson, et. al., U.S. Ser. No. 07-245428) and pentylglycine (see Cheng, et. al., "Symposium on Thrombosis and Hemostasis," 1991, Amsterdam, Abstract 2150).

In addition to thrombin inhibition, boropeptides have been disclosed with utility as a treatment for tumors, viral infections and arthritis (U.S. Pat. No. 4,963,655 and EP 354522A), emphysema (U.S. Pat. No. 4,499,082), hypertension (EP 315574A) and as factor VII/VIIa inhibitors (WO 8909612A). Kleemann, et. al. (AU A-24693/88) disclose renin-inhibiting 1-amino boronic acid derivatives of formula (3)

A.sup.1 --A.sup.2 --HN--CHR.sup.2 --BXR.sup.3 (YR.sup.4) (3) in which A.sup.1 denotes a radical of formulae (4-8). R.sup.1 NR.sup.6 --CHR.sup.5 --C.dbd.O-- (4) R.sup.1 CHR.sup.12 --CHR.sup.5 --C.dbd.O-- (5) R.sup.1 NR.sup.6 --CHR.sup.5 --CHR.sup.7 --CHR.sup.8 --CHR.sup.9 --C.dbd.O--(6) R.sup.1 CHR.sup.12 --CHR.sup.5 --CHR.sup.7 --CHR.sup.8 --CHR.sup.9 --C.dbd.O-- (7) R.sup.10 --(CH.sub.2).sub.n --CH(CH.sub.2).sub.m R.sup.11 --C.dbd.O--(8)

Despite the foregoing, more efficacious and specific inhibitors of coagulation proteases are needed as potentially valuable therapeutic agents for the treatment of thrombosis. None of the cited references describe or suggest the new thrombin-inhibiting boronic acid derivatives of the present invention.

SUMMARY OF THE INVENTION

This invention pertains to novel compounds of formula (I):

R.sup.1 --Z--CHR.sup.2 --A (I) wherein A is a) --BY.sup.1 Y.sup.2, b) --C(.dbd.O)CF.sub.3, c) --C(.dbd.O)CHF.sub.2, d) --C(.dbd.O)CH.sub.2 F, e) --C(.dbd.O)CH.sub.2 Cl, f) --C(.dbd.O)OR.sup.3, g) --C(.dbd.O)NR.sup.15 R.sup.16, h) --C(.dbd.O)R.sup.3, i) --C(.dbd.O)COOR.sup.3, j) --C(.dbd.O)C(.dbd.O)NR.sup.15 R.sup.16, k) --C(.dbd.O)C(.dbd.O)R.sup.3, l) --C(.dbd.O)CY.sup.3 Y.sup.4 COOR.sup.3, m) --C(.dbd.O)CY.sup.3 Y.sup.4 C(.dbd.O)NR.sup.15 R.sup.16, n) --C(.dbd.O)CY.sup.3 Y.sup.4 C(.dbd.O)R.sup.3, o) --PO.sub.3 H.sub.2, or p) --CHO; Y.sup.1 and Y.sup.2 are independently a) --OH, b) --F, c) --NR.sup.3 R.sup.4, or d) C.sub.1 -C.sub.8 alkoxy; Y.sup.1 and Y.sup.2 can be taken together to form: e) a cyclic boron ester where said chain or ring contains from 2 to 20 carbon atoms and, from 0-3 heteroatoms which can be N, S, or O, f) a cyclic boron amide where said chain or ring contains from 2 to 20 carbon atoms and, from 0-3 heteroatoms which can be N, S, or O, g) a cyclic boron amide-ester where said chain or ring contains from 2 to 20 carbon atoms and, from 0-3 heteroatoms which can be N, S, or O; Y.sup.3 and Y.sup.4 are independently a) --OH or b) --F; Z is a) --(CH.sub.2).sub.m CONR.sup.8 --, b) --(CH.sub.2).sub.m CSNR.sup.8 --, c) --(CH.sub.2).sub.m SO.sub.2 NR.sup.8 --, d) --(CH.sub.2).sub.m CO.sub.2 --, e) --(CH.sub.2).sub.m C(S)O--, or f) --(CH.sub.2).sub.m SO.sub.2 O--; R.sup.1 is a) --(CH.sub.2).sub.p -aryl, wherein aryl is phenyl, naphthyl or biphenyl substituted with one, two or three substituents selected from the group consisting of: halo (F, Cl, Br, I), methylenedioxy, --R.sup.8, --NR.sup.8 COR.sup.9, C.sub.2 -C.sub.6 -alkenyl, C.sub.2 -C.sub.6 -alkynyl, --(CH.sub.2).sub.w --OR.sup.8, -(C.sub.1 -C.sub.6)-perfluoroalkyl, --(CH.sub.2).sub.w CN, --(CH.sub.2).sub.w NC, --(CH.sub.2).sub.w NO.sub.2, --(CH.sub.2).sub.w CF.sub.3, --(CH.sub.2).sub.w S(O).sub.r R.sup.7, --(CH.sub.2).sub.w NR.sup.8 R.sup.9, --(CH.sub.2).sub.w COR.sup.8, --(CH.sub.2).sub.w CHO; --(CH.sub.2).sub.w CO.sub.2 R.sup.8, --(CH.sub.2).sub.w CONR.sup.8 R.sup.9. --(CH.sub.2).sub.w SO.sub.2 NH--(C.sub.1 -C.sub.5)-alkyl, --(CH.sub.2).sub.w SO.sub.2 NH.sub.2, --(CH.sub.2).sub.w SO.sub.2 NH--CO--(C.sub.1 -C.sub.6)-alkyl, --(CH.sub.2).sub.w SO.sub.2 NH--CO.sub.2 --(C.sub.1 -C.sub.6)-alkyl, --(CH.sub.2).sub.w NHSO.sub.2 --(C.sub.1 -C.sub.6)-alkyl, --(CH.sub.2).sub.w NHSO.sub.2 --(C.sub.1 -C.sub.6)-perfluoroalkyl, --(CH.sub.2).sub.w NHSO.sub.2 -phenyl, --(CH.sub.2).sub.w NHSO.sub.2 -perfluorophenyl, --(CH.sub.2).sub.w CN.sup.4 H, --O(CH.sub.2).sub.w CN, --NH(CH.sub.2).sub.w CN, --S(CH.sub.2).sub.w CN, --(CH.sub.2).sub.w NH--CO--(C.sub.1 -C.sub.6 -alkyl ), --(CH.sub.2).sub.w NH--CO--(C.sub.1 -C.sub.6 -perfluoroalkyl), --(CH.sub.2).sub.w NH--CO--(phenyl), --(CH.sub.2).sub.w NH--CO.sub.2 --(C.sub.1 -C.sub.6 -alkyl), --(CH.sub.2).sub.w NH--CO.sub.2 --(C.sub.1 -C.sub.6 -perfluoroalkyl), --(CH.sub.2).sub.w NH--CO.sub.2 --(phenyl), --O(C.dbd.O)--(C.sub.1 -C.sub.5 -alkyl), ##STR1## b) heteroaryl, wherein heteroaryl is an unsubstituted, monosubstituted or disubstituted: quinolinyl, ii) isoquinolinyl, iii) benzopyranyl, iv) benzothiophenyl, v) benzofuranyl, vi) 5,6,7,8-tetrahydroquinolinyl, vii) 5,6,7,8-tetrahydroisoquinolinyl, and wherein the substituents are selected from the group consisting of halo (F, Cl, Br, I), --CN, C.sub.1 -C.sub.10 -alkyl, C.sub.3 -C.sub.8 -cycloalkyl, C.sub.2 -C.sub.10 -alkenyl, C.sub.2 -C.sub.10 -alkynyl, R.sup.8, --OR.sup.8, --NO.sub.2, --CF.sub.3, --S(O).sub.r R.sup.7, --NR.sup.8 R.sup.9, --COR.sup.8, --CO.sub.2 R.sup.8, --CONHR.sup.8, NR.sup.8 COR.sup.9, NR.sup.8 CO.sub.2 R.sup.9, ##STR2## wherein J is N or C and K, L, M and Q are independently selected at each occurrence from the group consisting of N, CR.sup.13, S or O, provided that: i) there may be only one S or O present in the ring at a time; ii) there may only be 1-2N present when there is an O or S present; iii) there may be only 1-4N present; g) ##STR3## wherein W, R, T, U and V are selected from the group consisting of: CR.sup.13 or N, provided that there be no less than 1 and no more than 3N present; ##STR4## is as defined above; ##STR5## is as defined above; ##STR6## wherein G is O, S, or NP, where P is an amine protecting group selected from the group consisting of: --R.sup.3, --C(.dbd.O)R.sup.3, --SO.sub.2 R.sup.3, --C(.dbd.O)OR.sup.3); ##STR7## wherein G is O, S, or NP, where P is an amine protecting group selected from the group consisting of: --R.sup.3, --C(.dbd.O)R.sup.3, --SO.sub.2 R.sup.3, --C(.dbd.O)OR.sup.3); R.sup.2 is a) --(C.sub.1 -C.sub.12 alkyl)--X, b) --(C.sub.2 -C.sub.12 alkenyl)--X, or ##STR8## X is a) halogen (F, Cl, Br, I), b) --CN, c) --NO.sub.2, d) --CF.sub.3, e) --S(O).sub.r R.sup.14, f) --NHR.sup.14 g) --NHS(O).sub.r R.sup.14, h) --NHC(NH)H, i) --NHC(NH)NHOH, j) --NHC(NH)NSCN, k) --NHC(NH)NHR.sup.14, l) --NHC(NH)NHCOR.sup.14, m) --C(NH)NHR.sup.14, n) --C(NH)NHCOR.sup.14, o) --C(O)NHR.sup.14, p) --C(O)NHC(O)R.sup.14, q) --C(O)OR.sup.14, r) --OR.sup.14, s) --OC(O)R.sup.14, t) --OC(O)OR.sup.14, u) --OC(O)NHR.sup.14, v) --OC(O)NHC(O)R.sup.14, w) --SC(.dbd.NH)NHR.sup.14, or x) --SC(.dbd.NH)NHC(.dbd.O)R.sup.14 ; R.sup.3 is a) hydrogen, b) C.sub.1 -C.sub.8 alkyl, c) --(C.sub.1 -C.sub.4 alkyl)-aryl, d) C.sub.5 -C.sub.7 cycloalkyl, e) phenyl; or R.sup.4 is a) hydrogen, b) C.sub.1 -C.sub.8 alkyl, c) -(C.sub.1 -C.sub.4 alkyl)-aryl, d) C.sub.5 -C.sub.7 cycloalkyl, e) phenyl, or f) phenylsulfonyl; R.sup.5 and R.sup.6 are hydrogen or when taken together form a six membered aromatic ring optionally substituted with one, two or three substituents selected from the group consisting of halo (F, Cl, Br, I), --CN, C.sub.1 -C.sub.10 -alkyl, C.sub.3 -C.sub.8 -cycloalkyl, C.sub.2 -C.sub.10 -alkenyl, C.sub.2 -C.sub.10 -alkynyl, --OR.sup.8, --NO.sub.2, --CF.sub.3, --S(O).sub.r R.sup.7, --NR.sup.8 R.sup.9, --COR.sup.8, --CO.sub.2 R.sup.8, --CONR.sup.8 R.sup.9, phenyl, benzyl, phenylethyl; R.sup.7 is a) phenyl, b) C.sub.1 -C.sub.8 -alkyl, c) C.sub.1 -C.sub.4 -alkoxy, d) --CF.sub.3, or e) benzyl; R.sup.8 and R.sup.9 are independently a) H, ##STR9## c) C.sub.3 -C.sub.7 cycloalkyl, or d) C.sub.1 -C.sub.8 -alkyl; R.sup.11 is a) halo (F, Cl, Br, I), b) --CN, c) C.sub.1 -C.sub.10 -alkyl, d) C.sub.3 -C.sub.8 -cycloalkyl, e) C.sub.2 -C.sub.10 -alkenyl, f) C.sub.2 -C.sub.10 -alkynyl, g) --OR.sup.8, h) --NO.sub.2, i) --CF.sub.3, j) --S(O).sub.r R.sup.7, k) --NR.sup.8 R.sup.9, l) --COR.sup.9, m) --CO.sub.2 R.sup.8, n) --CONR.sup.8 R.sup.9, or o) H R.sup.12 is H, C.sub.1 -C.sub.4 alkyl, phenyl, benzyl, --COR.sup.7, or --S(O).sub.r R.sup.7 ; R.sup.13 is H, halogen (F, Cl, Br, I), (C.sub.1 -C.sub.8)alkyl, (C.sub.1 -C.sub.6)-perfluoroalkyl, --(CH.sub.2).sub.r --D, C.sub.3 -C.sub.8 cycloalkyl, C.sub.2 -C.sub.6 -alkenyl, C.sub.2 -C.sub.6 -alkynyl, methylenedioxy, --(CH.sub.2).sub.w --OR.sup.8, --(CH.sub.2).sub.w NC, --(CH.sub.2).sub.w CN, --(CH.sub.2).sub.w NO.sub.2, --(CH.sub.2).sub.w CF.sub.3, --(CH.sub.2).sub.w S(O).sub.r R.sup.7, --(CH.sub.2).sub.w NR.sup.8 R.sup.9, --(CH.sub.2).sub.w COR.sup.8, --(CH.sub.2).sub.w CO.sub.2 R.sup.8, --(CH.sub.2).sub.w CONR.sup.8 R.sup.9, --(CH.sub.2).sub.w SO.sub.2 NH--(C.sub.1 -C.sub.6)-alkyl, --(CH.sub.2).sub.w SO.sub.2 NH.sub.2, --(CH.sub.2).sub.w SO.sub.2 NH--CO--(C.sub.1 -C.sub.6)-alkyl, --(CH.sub.2).sub.w SO.sub.2 NH--CO.sub.2 --(C.sub.1 -C.sub.6)-alkyl, --(CH.sub.2).sub.w SO.sub.2 NH, --(CH.sub.2).sub.w NHSO.sub.2 --(C.sub.1 -C.sub.6)-alkyl, --(CH.sub.2).sub.w NHSO.sub.2 --(C.sub.1 -C.sub.6)-perfluoroalkyl, --(CH.sub.2).sub.w NHSO.sub.2 -phenyl, --(CH.sub.2).sub.w NHSO.sub.2 -perfluorophenyl, --(CH.sub.2).sub.w CN.sup.4 H, --O(C.dbd.O)--(C.sub.1 -C.sub.5 -alkyl), --O(CH.sub.2).sub.w CN, --NH(CH.sub.2).sub.w CN, --S(CH.sub.2).sub.w CN, --(CH.sub.2).sub.w NH--CO--(C.sub.1 -C.sub.6 -alkyl), --(CH.sub.2).sub.w NH--CO--(C.sub.1 -C.sub.6 -perfluoroalkyl), --(CH.sub.2).sub.w NH--CO--(phenyl), --(CH.sub.2).sub.w NH--CO.sub.2 --(C.sub.1 -C.sub.6 -alkyl), --(CH.sub.2).sub.w NH--CO.sub.2 --(C.sub.1 -C.sub.6 -perfluoroalkyl), --(CH.sub.2).sub.w NH--CO.sub.2 --(phenyl), --(CH.sub.2).sub.u phenyl wherein the phenyl contains 0-3 substituents selected from R.sup.18, --S--(CH.sub.2).sub.u phenyl wherein the phenyl contains 0-3 substituents selected from R.sup.18, or --O--(CH.sub.2).sub.u phenyl wherein the phenyl contains 0-3 substituents selected from R.sup.18 ; R.sup.14 is a) --H, b) --CF.sub.3 c) -C.sub.1 -C.sub.4 alkyl, d) --(CH.sub.2).sub.q -aryl, wherein aryl is phenyl, biphenyl, naphthyl, or fluorenyl unsubstituted or substituted with one to three substituents selected from the group consisting of: halogen (F, Cl, Br, I), --CF.sub.3, -(C.sub.1 -C.sub.4 alkyl), --(CH.sub.2).sub.x R.sup.15, --(CH.sub.2).sub.x CO(CH.sub.2).sub.y R.sup.15, --(CH.sub.2).sub.x C(O)O(CH.sub.2).sub.y R.sup.15, --(CH.sub.2).sub.x C(O)N�(CH.sub.2).sub.y R.sup.15 !�(CH.sub.2).sub.y R.sup.16 !, -methylenedioxy, --(C.sub.1 -C.sub.4 alkoxy), --(CH.sub.2).sub.x O(CH.sub.2).sub.y R.sup.15, --(CH.sub.2).sub.x OCO(CH.sub.2).sub.y R.sup.15, --(CH.sub.2).sub.x OC(O)O(CH.sub.2).sub.y R.sup.15, --(CH.sub.2).sub.x OC(O)N�(CH.sub.2).sub.y R.sup.15 !�(CH.sub.2).sub.y R.sup.16 !, --(CH.sub.2).sub.x OC(O)N�(CH.sub.2).sub.y R.sup.15 !�CO(CH.sub.2).sub.y R.sup.16 !, --(CH.sub.2).sub.x S(O).sub.r (CH.sub.2).sub.y R.sup.15, --(CH.sub.2).sub.x S(O).sub.r (CH.sub.2).sub.y COR.sup.15, --(CH.sub.2).sub.x S(O).sub.r (CH.sub.2).sub.y C(O)OR.sup.15, --(CH.sub.2).sub.x S(O).sub.r N�(CH.sub.2).sub.y R.sup.15 !�(CH.sub.2).sub.y R.sup.16 ! --(CH.sub.2).sub.x N�(CH.sub.2).sub.y R.sup.15 !�(CH.sub.2).sub.y R.sup.16 !, --(CH.sub.2).sub.x N�(CH.sub.2).sub.y R.sup.15 !�CO(CH.sub.2).sub.y R.sup.16 !, --(CH.sub.2).sub.x N�(CH.sub.2).sub.y R.sup.15 !�C(O)O(CH.sub.2).sub.y R.sup.16 !, --(CH.sub.2).sub.x N�(CH.sub.2).sub.y R.sup.15 !CON�(CH.sub.2).sub.y R.sup.15 !�(CH.sub.2).sub.y R.sup.16 !, --(CH.sub.2).sub.x N�(CH.sub.2).sub.y R.sup.15 !CON�(CH.sub.2).sub.y R.sup.15 !--�CO(CH.sub.2).sub.y R.sup.16 !, --(CH.sub.2).sub.x N�(CH.sub.2).sub.y R.sup.15 !�S(O).sub.r (CH.sub.2).sub.y R.sup.16 !; R.sup.15 and R.sup.16 are independently a) hydrogen, b) C.sub.1 -C.sub.8 alkyl, c) -(C.sub.1 -C.sub.4 alkyl)-aryl, where aryl is defined above, d) C.sub.5 -C.sub.7 cycloalkyl, e) phenyl, substituted by 0-3 R.sup.18, f) benzyl, substituted by 0-3 R.sup.18, or g) -(C.sub.1 -C.sub.4 alkoxy); R.sup.15 and R.sup.16 can be taken together to form a ring: ##STR10## R.sup.18 and R.sup.19 are independently H, halo (F, Cl, Br, I), C.sub.1 -C.sub.8 -alkyl, C.sub.3 -C.sub.8 cycloalkyl, C.sub.2 -C.sub.6 -alkenyl, C.sub.2 -C.sub.6 -alkynyl, --(CH.sub.2).sub.w --OR.sup.8, --(CH.sub.2).sub.w CN, --(CH.sub.2).sub.w NC, --(CH.sub.2).sub.w NO.sub.2, --(CH.sub.2).sub.w CF.sub.3, --(CH.sub.2).sub.w S(O).sub.r R.sup.7, --(CH.sub.2).sub.w NR.sup.8 R.sup.9, --(CH.sub.2).sub.w COR.sup.8, --(CH.sub.2).sub.w CO.sub.2 R.sup.8, --(CH.sub.2).sub.w .sup.CONR.sup.8 R9, --(CH.sub.2).sub.w SO.sub.2 NH--(C.sub.1 -C.sub.6)-alkyl, --(CH.sub.2).sub.w SO.sub.2 NH.sub.2, --(CH.sub.2).sub.w SO.sub.2 NH--CO--(C.sub.1 -C.sub.6)-alkyl, --(CH.sub.2).sub.w SO.sub.2 NH--CO.sub.2 --(C.sub.1 -C.sub.6)-alkyl, --(CH.sub.2).sub.w SO.sub.2 NH--, --(CH.sub.2).sub.w NHSO.sub.2 --(C.sub.1 -C.sub.6)-alkyl, --(CH.sub.2).sub.w NHSO.sub.2 --(C.sub.1 -C.sub.6)-perfluoroalkyl, --(CH.sub.2).sub.w NHSO.sub.2 -phenyl, --(CH.sub.2).sub.w NHSO.sub.2 -perfluorophenyl, --(CH.sub.2).sub.w CN.sup.4 .sup.H, --O(C.dbd.O)--(C.sub.1 -C.sub.5 -alkyl), --O(CH.sub.2).sub.w CN, --NH(CH.sub.2).sub.w CN, --S(CH.sub.2).sub.w CN, --(CH.sub.2).sub.w NH--CO--(C.sub.1 -C.sub.6 -alkyl), --(CH.sub.2).sub.w NH--CO--(C.sub.1 -C.sub.6 -perfluoroalkyl), --(CH.sub.2).sub.w NH--CO--(C.sub.1 -C.sub.6 -phenyl), --(CH.sub.2).sub.w NH--CO.sub.2 --(C.sub.1 -C.sub.6 -alkyl), --(CH.sub.2).sub.w NH--CO.sub.2 --(C.sub.1 -C.sub.6 -phenyl), or --O(C.dbd.O)phenyl; R.sup.18 and R.sup.19 can be taken together to form a methylenedioxy group; R.sup.20 and R.sup.20a are independently (C.sub.1 -C.sub.8)alkyl, --(CH.sub.2).sub.u phenyl wherein the phenyl contains 0-3 substituents selected from R.sup.18, (C.sub.1 -C.sub.6)-perfluoroalkyl, or --(CH.sub.2).sub.r --D; m is 0 to 6; n is 1 to 2; p is 0 to 2; q is 0 to 4. r is 0 to 2; s is 0 to 3; t is 1 to 5; u is 0 to 5; v is 0 to 5; w is 0 to 5; x is 0 to 6; y is 0 to 6; D is fur-2-yl, fur-3-yl, thiophen-2-yl, thiophen-3-yl, oxazol-2-yl, oxazol-4-yl, thiazol-2-yl, thiazol-4-yl, isoxazol-3-yl, isoxazol-4-yl, isoxazol-5-yl, pyrid-2-yl, pyrid-4-yl, pyridazin-3-yl, pyridazin-4-yl, pyrimidin-2-yl, pyrimidin-4-yl, pyrazin-2-yl, or tetrazolyl; E is --CO--, --SO.sub.2 --, --CH.sub.2 -- or a single bond; F is --CO--; W is a) --O--, b) --S(O).sub.r --, c) --NR.sup.4 --, d) --NC(.dbd.O) R.sup.3 --, e) a bond, or f) --(CH.sub.2).sub.n --; or prodrugs or pharmaceutically acceptable salts thereof.

Preferred compounds of formula (I) are those compounds wherein:

Z is a) --(CH.sub.2).sub.m CONR.sup.8 --, b) --(CH.sub.2).sub.m CSNR.sup.8 --, c) --(CH.sub.2).sub.m SO.sub.2 NR.sup.8 --, R.sup.1 is a) --(CH.sub.2).sub.p -aryl, wherein aryl is phenyl, naphthyl or biphenyl substituted with one, two or three substituents selected from the group consisting of: halo (F, Cl, Br, I), methylenedioxy, --R.sup.8, --NR.sup.8 COR.sup.9, C.sub.2 -C.sub.6 -alkenyl, C.sub.2 -C.sub.6 -alkynyl, --(CH.sub.2).sub.w --OR.sup.8, -(C.sub.1 -C.sub.6)-perfluoroalkyl, --(CH.sub.2).sub.w CN, --(CH.sub.2).sub.w NC, --(CH.sub.2).sub.w NO.sub.2, --(CH.sub.2).sub.w CF.sub.3, --(CH.sub.2).sub.w S (O).sub.r R.sup.7, --(CH.sub.2).sub.w NR.sup.8 R.sup.9, --(CH.sub.2).sub.w COR.sup.8, --(CH.sub.2).sub.w CO.sub.2 R.sup.8, --(CH.sub.2).sub.w CONR.sup.8 R.sup.9. --(CH.sub.2).sub.w SO.sub.2 NH--(C.sub.1 -C.sub.6)-alkyl, --(CH.sub.2).sub.w SO.sub.2 NH.sub.2, --(CH.sub.2).sub.w SO.sub.2 NH--CO--(C.sub.1 -C.sub.6)-alkyl, --(CH.sub.2).sub.w SO.sub.2 NH--CO.sub.2 --(C.sub.1 -C.sub.6)-alkyl, --(CH.sub.2).sub.w NHSO.sub.2 --(C.sub.1 -C.sub.6)-alkyl, --(CH.sub.2).sub.w NHSO.sub.2 --(C.sub.1 -C.sub.6)-perfluoroalkyl, --(CH.sub.2).sub.w NHSO.sub.2 -phenyl, --(CH.sub.2).sub.w NHSO.sub.2 -perfluorophenyl, --(CH.sub.2).sub.w CN.sup.4 H, e--O(CH.sub.2).sub.w CN, --NH(CH.sub.2).sub.w CN, --S(CH.sub.2).sub.w CN, --(CH.sub.2).sub.w NH--CO--(C.sub.1 -C.sub.6 -alkyl), --(CH.sub.2).sub.w NH--CO--(C.sub.1 -C.sub.6 -perfluoroalkyl), --(CH.sub.2).sub.w NH--CO--(phenyl), --(CH.sub.2).sub.w NH--CO.sub.2 --(C.sub.1 -C.sub.6 -alkyl), --(CH.sub.2).sub.w NH--CO.sub.2 --(C.sub.1 -C.sub.6 -perfluoroalkyl), or --(CH.sub.2).sub.w NH--CO.sub.2 --(phenyl), --O(C.dbd.O--(C.sub.1 -C.sub.5 alkyl); b) heteroaryl, wherein heteroaryl is an unsubstituted, monosubstituted or disubstituted: i) quinolinyl, ii) isoquinolinyl, iii) benzopyranyl, iv) benzothiophenyl, v) benzofuranyl, vi) 5,6,7,8-tetrahydroquinolinyl, vii) 5,6,7,8-tetrahydroisoquinolinyl, and wherein the substituents are selected from the group consisting of halo (F, Cl, Br, I), --CN, C.sub.1 -C.sub.10 -alkyl, C.sub.3 -C.sub.8 -cycloalkyl, C.sub.2 -C.sub.10 -alkenyl, C.sub.2 -C.sub.10 -alkynyl, R.sup.8, --OR.sup.8, --NO.sub.2, --CF.sub.3, --S(O).sub.r R.sup.7, --NR.sup.8 R.sup.9, --COR.sup.8, --CO.sub.2 R.sup.8, --CONR.sup.8 H, NR.sup.8 COR.sup.9, NR.sup.8 CO.sub.2 R.sup.9 ; ##STR11## f) wherein the ring ##STR12## represented by --J--K--L--M--Q-- is a group selected from: 1) --N--C(R.sup.13).dbd.C(R.sup.13)--C(R.sup.13).dbd.C(R.sup.13)--, 2) --N--C(R.sup.13).dbd.C(R.sup.13)--C(R.sup.13).dbd.N--, 3) --N--C(R.sup.13).dbd.C(R.sup.13)--N.dbd.C(R.sup.13)--, 4) --N--C(R.sup.13).dbd.N--C(R.sup.13).dbd.N--, 5) --N--C(R.sup.13).dbd.C(R.sup.13)--N.dbd.N-- 6) --N--C(R.sup.13).dbd.N--N.dbd.N--, 7) --N--N.dbd.C(R.sup.13)--N.dbd.N--, 8) .dbd.C--0--C(R.sup.13).dbd.N--C(R.sup.13).dbd., 9) --C.dbd.C(R.sup.13)--O--C(R.sup.13).dbd.N--, 10) .dbd.C--O--C(R.sup.13).dbd.C(R.sup.13)--N.dbd., 11) --C.dbd.C(R.sup.13)--C(R.sup.13).dbd.N--O--, 12) .dbd.C--C(R.sup.13).dbd.C(R.sup.13)--O--N.dbd., 13) --C.dbd.C(R.sup.13)--O--N.dbd.C(R.sup.13)--, 14) .dbd.C--S--C(R.sup.13).dbd.N--C(R.sup.13).dbd., 15) --C.dbd.C(R.sup.13)--S--C(R.sup.13).dbd.N--, 16) .dbd.C--S--C(R.sup.13).dbd.C(R.sup.13)--N.dbd., 17) --C.dbd.N--S--N.dbd.C(R.sup.13)--, 18) --C.dbd.N--S--C(R.sup.13).dbd.N--, 19) .dbd.C--S--N.dbd.C(R.sup.13)--N.dbd., 20) .dbd.C--S--C(R.sup.13).dbd.C(R.sup.13)--C(R.sup.13).dbd., 21) --C.dbd.C(R.sup.13)--S--C(R.sup.13).dbd.C(R.sup.13)--, 22) .dbd.C--O--C(R.sup.13).dbd.C(R.sup.13)--C(R.sup.13).dbd., or 23) --C.dbd.C(R.sup.13)--O--C(R.sup.13).dbd.C(R.sup.13)--; g) wherein the ring ##STR13## represented by --C--W--R--T--U--V-- is a group selected from: 1) --C.dbd.N--C(R.sup.13).dbd.C(R.sup.13)--C(R.sup.13).dbd.C(R.sup.13)--, 2) --C.dbd.C(R.sup.13)--N.dbd.C(R.sup.13)--C(R.sup.13).dbd.C(R.sup.13)--, 3) --C.dbd.C(R.sup.13)--C(R.sup.13).dbd.N--C(R.sup.13).dbd.C(R.sup.13)--, 4) --C.dbd.N--N.dbd.C(R.sup.13)--C(R.sup.13).dbd.C(R.sup.13)--, 5) --C.dbd.C(R.sup.13)--N.dbd.N--C(R.sup.13).dbd.C(R.sup.13)--, 6) --C.dbd.N--C(R.sup.13).dbd.C(R.sup.13)--C(R.sup.13).dbd.N--, 7) --C.dbd.N--C(R.sup.13).dbd.C(R.sup.13)--N.dbd.C(R.sup.13)--, 8) --C.dbd.N--C(R.sup.13).dbd.N--C(R.sup.13)--N.dbd.C(R.sup.13)--, 9) --C.dbd.C(R.sup.13)--N.dbd.C(R.sup.13)--N.dbd.C(R.sup.13)--, 10) --C.dbd.N--C(R.sup.13).dbd.N--N.dbd.C(R.sup.13)--, 11) --C.dbd.N--C(R.sup.13).dbd.C(R.sup.13)--N.dbd.N--, or 12) --C.dbd.C(R.sup.13)--N.dbd.C(R.sup.13)--N.dbd.N--; ##STR14## is as defined above; ##STR15## is as defined above; ##STR16## wherein G is O, S, or NP (where P is an amine protecting group selected from the group consisting of: --R.sup.3, --C(.dbd.O)R.sup.3, --SO.sub.2 R.sup.3, --C(.dbd.O)OR.sup.3 ; ##STR17## wherein G is O, S, or NP (where P is an amine protecting group selected from the group consisting of: --R.sup.3, --C(.dbd.O)R.sup.3, --SO.sub.2 R.sup.3, --C(.dbd.O)OR.sup.3 ; R.sup.14 is a) --H, b) --CF.sub.3 c) -C.sub.1 -C.sub.4 alkyl, d) --(CH.sub.2).sub.q -aryl, wherein aryl is phenyl, biphenyl, naphthyl, or fluorenyl unsubstituted substituted with one to three substituents selected from the group consisting of: halogen (F, Cl, Br, I), --CF.sub.3, -(C.sub.1 -C.sub.4 alkyl), -methylenedioxy, -(C.sub.1 -C.sub.4 alkoxy), --(CH.sub.2).sub.x N�(CH.sub.2).sub.y R.sup.15 !�(CH.sub.2).sub.y R.sup.16 !; and all other required substituents of formula (I) are as defined in Claim 1.

More preferred compounds of the formula (I) are those compounds wherein:

A is a) --BY.sup.1 Y.sup.2, b) --C(.dbd.O)CF.sub.3, c) --C(.dbd.O)CHF.sub.2, d) --C(.dbd.O)CH.sub.2 F, e) --C(.dbd.O)CH.sub.2 Cl, f) --C(.dbd.O)R.sup.3, g) --C(.dbd.O)NR.sup.15 R.sup.16, h) --C(.dbd.O)R.sup.3, i) --C(.dbd.O)COOR.sup.3, j) --C(.dbd.O)C(.dbd.O)NR.sup.15 R.sup.16, k) --C(.dbd.O)C(.dbd.O)R.sup.3 , l) --CHO; Y.sup.1 and Y.sup.2 are independently a) --OH, or b) C.sub.1 -C.sub.8 alkoxy; Y.sup.1 and Y.sup.2 can be taken together to form a cyclic boron ester where said chain or ring contains from 2 to 20 carbon atoms and, from 0-3 heteroatoms which can be N, S, or O, Z is a) --(CH.sub.2).sub.m CONR.sup.8 --, b) --(CH.sub.2).sub.m CSNR.sup.8 --, or c) --(CH.sub.2).sub.m SO.sub.2 NR.sup.8 --; R.sup.1 is a)--(CH.sub.2).sub.p -aryl, wherein aryl is phenyl, naphthyl or biphenyl substituted with one, two or three substituents independently selected at each occurrence from the group consisting of: halo (F, Cl, Br, I), methylenedioxy, --R.sup.8, --NR.sup.8 COR.sup.9, C.sub.2 -C.sub.6 -alkenyl, C.sub.2 -C.sub.6 -alkynyl, --(CH.sub.2).sub.w --OR.sup.8, --(C.sub.1 -C.sub.6)-perfluoroalkyl, --(CH.sub.2).sub.w CN, --(CH.sub.2).sub.w NC, --(CH.sub.2).sub.w NO.sup.2, --(CH.sub.2).sub.w CF.sub.3, --(CH.sub.2).sub.w S (O).sub.r R.sup.7, --(CH.sub.2).sub.w NR.sup.8 R.sup.9, --(CH.sub.2).sub.w COR.sup.8, --(CH.sub.2).sub.w CO.sub.2 R.sup.8, --(CH.sub.2).sub.w CONR.sup.8 R.sup.9, --(CH.sub.2).sub.w SO.sub.2 NH--(C.sub.1 -C.sub.6)-alkyl, --(CH.sub.2).sub.w SO.sub.2 NH.sub.2, --(CH.sub.2).sub.w SO.sub.2 NH--CO--(C.sub.1 -C.sub.6)-alkyl, --(CH.sub.2).sub.w SO.sub.2 NH--CO.sub.2 --(C.sub.1 -C.sub.6)-alkyl, --(CH.sub.2).sub.w SO.sub.2 NH--, --(CH.sub.2).sub.w NHSO.sub.2 --(C.sub.1 -C.sub.6)-alkyl, --(CH.sub.2).sub.w NHSO.sub.2 --(C.sub.1 -C.sub.6)-perfluoroalkyl, --(CH.sub.2).sub.w NHSO.sub.2 -phenyl, --(CH.sub.2).sub.w NHSO.sub.2 -perfluorophenyl, --(CH.sub.2).sub.w CN.sup.4 H, --O(CH.sub.2).sub.w CN, --NH(CH.sub.2).sub.w CN, --S(CH.sub.2).sub.w CN, --(CH.sub.2).sub.w NH--CO--(C.sub.1 -C.sub.6 -alkyl), --(CH.sub.2).sub.w NH--CO--(C.sub.1 -C.sub.6 -perfluoroalkyl), --(CH.sub.2).sub.w NH--CO--(phenyl), --(CH.sub.2).sub.w NH--CO.sub.2 --(C.sub.1 -C.sub.6 -alkyl), --(CH.sub.2).sub.w NH--CO.sub.2 --(C.sub.1 -C.sub.6 -perfluoroalkyl), or --(CH.sub.2).sub.w NH--CO.sub.2 --(phenyl), --O(C.dbd.O)--C.sub.1 -C.sub.5 -alkyl); b) heteroaryl, wherein heteroaryl is an unsubstituted, monosubstituted or disubstituted: i) quinolinyl, ii) isoquinolinyl, iii) benzopyranyl, iv) benzothiophenyl, v) benzofuranyl, vi) 5,6,7,8-tetrahydroquinolinyl, vii) 5,6,7,8-tetrahydroisoquinolinyl, wherein the substituents are members selected from the group consisting of: halo (F, Cl, Br, I), --CN, C.sub.1 -C.sub.10 -alkyl, C.sub.3 -C.sub.8 -cycloalkyl, C.sub.2 -C.sub.10 -alkenyl, C.sub.2 -C.sub.10 -alkynyl, R.sup.8, --OR.sup.8, --NO.sub.2, --CF.sub.3, --S(O).sub.r R.sup.7, --NR.sup.8 R.sup.9, --COR.sup.8, --CO.sub.2 R.sup.8, --CONR.sup.8 H, NR.sup.8 COR.sup.9, NR.sup.8 CO.sub.2 R.sup.9 ; ##STR18## wherein the ring represented by --J--K--L--M--Q-- is a group selected from: 1) --N--C(R.sup.13).dbd.C(R.sup.13)--C(R.sup.13).dbd.C(R.sup.13)--, 2) --N--C(R.sup.13).dbd.C(R.sup.13)--C(R.sup.13).dbd.N--, 3) --N--C(R.sup.13).dbd.C(R.sup.13)--N.dbd.C(R.sup.13)--, 4) --N--C(R.sup.13).dbd.N--C(R.sup.13).dbd.N--, 5) --N--C(R.sup.13).dbd.C(R.sup.13)--N.dbd.N-- 6) --N--C(R.sup.13).dbd.N--N.dbd.N--, 7) --N--N.dbd.C(R.sup.13)--N.dbd.N--, 8) .dbd.C--O--C(R.sup.13).dbd.N--C(R.sup.13).dbd., 9) --C.dbd.C(R.sup.13)O--C(R.sup.13).dbd.N--, 10) .dbd.C--C(R.sup.13).dbd.C(R.sup.13)--N.dbd., 11) --C.dbd.C(R.sup.13)--C(R.sup.13).dbd.N--O--, 12) .dbd.C.dbd.C(R.sup.13).dbd.C(R.sup.13)--O--N.dbd., 13) --C.dbd.C(R.sup.13)--O--N.dbd.C(R.sup.13)--, 14) .dbd.C--S--C(R.sup.13).dbd.N--C(R.sup.13).dbd., 15) --C.dbd.C(R.sup.13)--S--C(R.sup.13).dbd.N--, 16) .dbd.C--S--C(R.sup.13).dbd.C(R.sup.13)--N.dbd., 17) .dbd.C--S--C(R.sup.13).dbd.C(R.sup.13)--C(R.sup.13).dbd., 18) --C.dbd.C(R.sup.13) --S--C(R.sup.13).dbd.C(R.sup.13)--, 19).dbd.C--O--C(R.sup.13).dbd.C(R.sup.13)--C(R.sup.13).dbd., or 20)--C.dbd.C(R.sup.13)--O--C(R.sup.13).dbd.C(R.sup.13)--; ##STR19## wherein the ring represented by --C--W--R--T--U--V-- is a group selected from: 1)--C.dbd.N--C(R.sup.13).dbd.C(R.sup.13)--C(R.sup.13).dbd.C(R.sup.13)--, 2)--C.dbd.C(R.sup.13)--N.dbd.C(R.sup.13)--C(R.sup.13).dbd.C(R.sup.13)--, 3)--C.dbd.C(R.sup.13)--C(R.sup.13).dbd.N--C(R.sup.13).dbd.C(R.sup.13)--, 4)--C.dbd.N--N.dbd.C(R.sup.13)--C(R.sup.13).dbd.C(R.sup.13)--, 5)--C.dbd.C(R.sup.13)--N.dbd.N--C(R.sup.13).dbd.C(R.sup.13)--, 6)--C.dbd.N--C(R.sup.13).dbd.C(R.sup.13)--C(R.sup.13).dbd.N-- 7)--C.dbd.N--C(R.sup.13).dbd.C(R.sup.13)--N.dbd.C(R13)--, 8)--C.dbd.N--C(R.sup.13).dbd.N--C(R.sup.13).dbd.C(R.sup.13)--, 9)--C.dbd.C(R.sup.13)--N.dbd.C(R.sup.13)--N.dbd.C(R13)--, 10)--C.dbd.N--C(R.sup.13).dbd.N--N.dbd.C(R.sup.13)--, 11)--C.dbd.N--C(R.sup.13).dbd.C(R.sup.13)--N.dbd.N--, or 12)--C.dbd.C(R.sup.13)--N.dbd.C(R.sup.13)--N.dbd.N--; ##STR20## is as defined above; ##STR21## is as defined above; or ##STR22## wherein G is O, S, or NP (where P is an amine protecting group selected from the group consisting of: --R.sup.3, --C(.dbd.O)R.sup.3, --SO.sub.2 R.sup.3, --C(.dbd.O)OR.sup.3); R.sup.2 is a) -(C.sub.1 -C.sub.12 alkyl)--X, b) -(C.sub.2 -C.sub.12 alkenyl)--X, or ##STR23## X is a) halogen (F, Cl, Br, I), b) --CN, c) --NO.sub.2, d) --CF.sub.3, e) --NHR.sup.14 f) --NHS(O).sub.r R.sup.14, g) --NHC(NH)H, h) --NHC(NH)NHOH, i) --NHC(NH)NHCN, j) --NHC(NH)NHR.sup.14, k) --NHC(NH)NHCOR.sup.14, l) --C(NH)NHR.sup.14, m) --C(NH)NHCOR.sup.14, n) --C(O)NHR.sup.14, o) --C(O)NHC(O)R.sup.14, p) --C(O)OR.sup.14, q) --OR.sup.14 r) --OC(O)R.sup.14, s) --OC(O)OR.sup.14, t) --OC(O)NHR.sup.14, u) --OC(O)NHC(O) R.sup.14, v) --SC(.dbd.NH)NHR.sup.14, or w) --SC(.dbd.NH)NHC(.dbd.O) R.sup.14 ; R.sup.13 is H, halogen (F, Cl, Br, I), (C.sub.1 -C.sub.6) alkyl, --(CH.sub.2).sub.r --D, methylenedioxy, --(CH.sub.2).sub.w --OR.sup.8, --(CH.sub.2).sub.w CONR.sup.8 R.sup.9, --(CH.sub.2).sub.w NC, --(CH.sub.2).sub.w CN, --(CH.sub.2).sub.w NO.sup.2, --(CH.sub.2).sub.w S(O).sub.r R.sup.7, --(CH.sub.2).sub.w COR.sup.8, --(CH.sub.2).sub.w CO.sub.2 R.sup.8, --(CH.sub.2).sub.w CONR.sup.8 R.sup.9, --(CH.sub.2).sub.w SO.sub.2 NH--(C.sub.1 -C.sub.5)-alkyl, --(CH.sub.2).sub.w SO.sub.2 NH.sub.2, --(CH.sub.2).sub.w SO.sub.2 NH--CO--(C.sub.1 -C.sub.6)-alkyl, --(CH.sub.2).sub.w SO.sub.2 NH--CO.sub.2 --(C.sub.1 -C.sub.6)-alkyl, --(CH.sub.2).sub.w NHSO.sub.2 --(C.sub.1 -C.sub.6)-alkyl, --(CH.sub.2).sub.w NHSO.sub.2 --(C.sub.1 -C.sub.6)-perfluoroalkyl, --(CH.sub.2).sub.w NHSO.sub.2 --phenyl, --(CH.sub.2).sub.w NHSO.sub.2 -perfluorophenyl, --(CH.sub.2).sub.w CN.sup.4 H, --O(C.dbd.O)--(C.sub.1 -C.sub.5 -alkyl), --O(CH.sub.2).sub.w CN, --NH (CH.sub.2).sub.w CN, --S (CH.sub.2).sub.w CN, --(CH.sub.2).sub.w NH--CO--(C.sub.1 -C.sub.6 -alkyl), --(CH.sub.2).sub.w NH--CO--(C.sub.1 -C.sub.6 -perfluoroalkyl), --(CH.sub.2).sub.w NH--CO--(C.sub.1 -C.sub.6 -phenyl), --(CH.sub.2).sub.w NH--CO.sub.2 --(C.sub.1 -C.sub.6 -alkyl), --(CH.sub.2).sub.w NH--CO.sub.2 --(C.sub.1 -C.sub.6 -phenyl), --(CH.sub.2).sub.u phenyl wherein the phenyl contains 0-3 substituents selected from R.sup.18, or --O(C.dbd.O)phenyl wherein the phenyl contains 0-3 substituents selected from R.sup.18 ; R.sup.14 is a) --H, b) --CF.sub.3 c) -C.sub.1 -C.sub.4 alkyl, d) --(CH.sub.2).sub.q -aryl, wherein aryl is phenyl, biphenyl, naphthyl, or fluorenyl are optionally substituted with one to three substituents selected from the group consisting of: halogen (F, Cl, Br, I), --CF.sub.3, -(C.sub.1 -C.sub.4 alkyl), -methylenedioxy, -(C.sub.1 -C.sub.4 alkoxy), or --CH.sub.2).sub.x N�(CH.sub.2).sub.y R.sup.15 !�CH.sub.2).sub.y R.sup.16 !; R.sup.18 and R.sup.19 are independently H, halo (F, Cl, Br, I, C.sub.1 -C.sub.6 -alkyl, --(CH.sub.2).sub.w --OR.sup.8, --(CH.sub.2).sub.w CN, --(CH.sub.2 WCN, --(CH.sub.2).sub.w NO.sub.2, --(CH.sub.2).sub.w S(O).sub.r R.sup.7, --(CH.sub.2).sub.w NR.sup.8 R.sup.9, --(CH.sub.2).sub.w COR.sup.8, --(CH.sub.2).sub.w CO.sub.2 R.sup.8, --(CH.sub.2).sub.w CONR.sup.8 R.sup.9, --(CH.sub.2).sub.w SO.sub.2 NH--(C.sub.1 -C.sub.5)-alkyl, --(CH.sub.2).sub.w SO.sub.2 NH.sub.2, --(CH.sub.2).sub.w SO.sub.2 NH--CO--(C.sub.1 -C.sub.6)-alkyl, --(CH.sub.2).sub.w SO.sub.2 NH--CO.sub.2 --(C.sub.1 -C.sub.6)-alkyl, --(CH.sub.2).sub.w NHSO.sub.2 --(C.sub.1 -C.sub.6)-alkyl, --(CH.sub.2).sub.w NHSO.sub.2 --(C.sub.1 -C.sub.6)-perfluoroalkyl, --(CH.sub.2).sub.w NHSO.sub.2 -phenyl, --(CH.sub.2).sub.w NHSO.sub.2 -perfluorophenyl, --(CH.sub.2).sub.w CN.sup.4 H, --O(C.dbd.O)--(C.sub.1 -C.sub.5 -alkyl), --O(CH.sub.2).sub.w CN, --NH(CH.sub.2).sub.w CN, --S(CH.sub.2).sub.w CN, --(CH.sub.2).sub.w NH--CO--(C.sub.1 -C.sub.6 -alkyl), --(CH.sub.2).sub.w NH--CO--(C.sub.1 -C.sub.6 -perfluoroalkyl), --(CH.sub.2).sub.w NH--CO--(C.sub.1 -C.sub.6 -phenyl), --(CH.sub.2).sub.w NH--CO.sub.2 (C.sub.1 -C.sub.6 -alkyl), --(CH.sub.2).sub.w NH--CO.sub.2 --(C.sub.1 -C.sub.6 -phenyl), or --O(C.dbd.O)phenyl; R.sup.18 and R.sup.19 can be taken together to form a methylenedioxy group; R.sup.20 and R.sup.20a are independently (C.sub.1 -C.sub.8)alkyl, --(CH.sub.2).sub.u phenyl wherein the phenyl contains 0-3 substituents selected from R.sup.18, (C.sub.1 -C.sub.6)-perfluoroalkyl, or --(CH.sub.2).sub.r --D; D is fur-2-yl, fur-3-yl, thiophen-2-yl, thiophen-3-yl, oxazol-2-yl, oxazol-4-yl, thiazol-2-yl, thiazol-4-yl, pyrid-2-yl, pyrid-4-yl, pyrimidin-2-yl, or pyrimidin-4-yl; W is a) --O--, b) --NR.sup.4 --, c) a bond, or d) --(CH.sub.2).sub.n --; and all other required substituents of formula (I) are as defined in Claim 2.

Most preferred compounds of the formula (I) are those compounds wherein:

A is --BY.sup.1 Y.sup.2 ; Y.sup.1 and Y.sup.2 are --OH; Y.sup.1 and Y.sup.2 can be taken together to form a cyclic boron ester where said chain or ring contains from 2 to 20 carbon atoms and, from 0-3 heteroatoms which can be N, S, or O, Z is --(CH.sub.2).sub.m CONR.sup.8 --; R.sup.1 is a) --(CH.sub.2).sub.p -aryl, wherein aryl is phenyl, naphthyl or biphenyl substituted with one, two or three substituents selected from the group consisting of: halo (F, Cl, Br, I), methylenedioxy, --R.sup.8,--NR.sup.8 COR.sup.9, C.sub.2 -C.sub.6 -alkenyl, C.sub.2 -C.sub.6 -alkynyl, --(CH.sub.2).sub.w --OR.sup.8, --(C.sub.1 -C.sub.6)-perfluoroalkyl, --(CH.sub.2).sub.w CN, --(CH.sub.2).sub.w NC, --(CH.sub.2).sub.w NO.sub.2, --(CH.sub.2).sub.w CF.sub.3, --(CH.sub.2).sub.w S (O).sub.r R.sup.7, --(CH.sub.2).sub.w NR.sup.8 R.sup.9, --(CH.sub.2).sub.w COR.sup.8, (CH.sub.2).sub.w CO.sub.2 R.sup.8, --(CH.sub.2).sub.w CONR.sup.8 R.sup.9. --(CH.sub.2).sub.w SO.sub.2 NH--(C.sub.1 -C.sub.6)-alkyl, --(CH.sub.2).sub.w SO.sub.2 NH.sub.2, --(CH.sub.2).sub.w SO.sub.2 NH--CO--(C.sub.1 -C.sub.6)-alkyl, --(CH.sub.2).sub.w SO.sub.2 NH--CO.sub.2 --(C.sub.1 -C.sub.6)-alkyl, --(CH.sub.2).sub.w NHSO.sub.2 --(C.sub.1 -C.sub.6)-alkyl, --(CH.sub.2).sub.w NHSO.sub.2 --(C.sub.1 -C.sub.6)-perfluoroalkyl, --(CH.sub.2).sub.w NHSO.sub.2 -phenyl, --(CH.sub.2).sub.w NHSO.sub.2 -perfluorophenyl, --(CH.sub.2).sub.w CN.sup.4 H, --O(CH.sub.2).sub.w CN, --NH(CH.sub.2).sub.w CN, --S(CH.sub.2).sub.w CN, --(CH.sub.2).sub.w NH--CO--(C.sub.1 -C.sub.6 -alkyl), --(CH.sub.2).sub.w NH--CO--(C.sub.1 -C.sub.6 -perfluoroalkyl), --(CH.sub.2).sub.w NH--CO--(C.sub.1 -C.sub.6 -phenyl), --(CH.sub.2).sub.w NH--CO.sub.2 --(C.sub.1 -C.sub.6 -alkyl), --(CH.sub.2).sub.w NH--CO.sub.2 --(C.sub.1 -C.sub.6 -perfluoroalkyl), or --(CH.sub.2).sub.w NH--CO.sub.2 --(C.sub.1 -C.sub.6 -phenyl); b) heteroaryl, wherein heteroaryl is an unsubstituted, monosubstituted or disubstituted isoquinolinyl wherein the substituents are members selected from the group consisting of: halo (F, Cl, Br, I), --CN, C.sub.1 -C.sub.10 -alkyl, C.sub.3 -C.sub.8 -cycloalkyl, C.sub.2 -C.sub.10 -alkenyl, C.sub.2 -C.sub.10 -alkynyl, R.sup.8, --OR.sup.8, --NO.sub.2, --CF.sub.3, --S(O).sub.r R.sup.7, --NR.sup.8 R.sup.9, --COR.sup.8, --CO.sub.2 R.sup.8, --CONR.sup.8 R.sup.9, NR.sup.8 COR.sup.9, NR.sup.8 CO.sub.2 R.sup.9, ##STR24## wherein the ring represented by --J--K--L--M--Q-- is a group selected from: 1) --N--C(R.sup.13).dbd.N--C(R.sup.13).dbd.N--, 2) --N--C(R.sup.13).dbd.C(R.sup.13)--N.dbd.N--, 3) --N--N.dbd.C(R.sup.13)--N.dbd.N--, 5) --N--C(R.sup.13).dbd.N--N.dbd.N--, 6) .dbd.C--S--C(R.sup.13).dbd.C(R.sup.13)--C(R.sup.13).dbd., or 7) .dbd.C--O--C(R.sup.13).dbd.C(R.sup.13)--C(R.sup.13).dbd.; ##STR25## wherein the ring represented by --C--W--R--T--U--V-- is a group selected from: 1) --C.dbd.N--C(R.sup.13).dbd.C(R.sup.13).dbd.C(R.sup.13)--C(R13).dbd.C(R.sup.13)--, 1) --C.dbd.C(R.sup.13)--N.dbd.C(R.sup.13)--C(R.sup.13).dbd.C(R.sup.13)--, 2) --C.dbd.C(R.sup.13)--C(R.sup.13).dbd.N--C(R.sup.13).dbd.C(R.sup.13)--, 3) --C.dbd.C(R.sup.13)--N.dbd.C(R.sup.13)--N.dbd.C(R.sup.13)--, 4) --C.dbd.N--C(R.sup.13).dbd.C(R.sup.13)--C(R.sup.13).dbd.N--, or 5) --C.dbd.N--C(R.sup.13).dbd.N--C(R.sup.13).dbd.C(R.sup.13)--; ##STR26## is as defined above; ##STR27## is as defined above; or ##STR28## wherein G is S; R.sup.2 is a) --(C.sub.1 -C.sub.12 alkyl)--X, or ##STR29## X is a) halogen (F, Cl, Br, I), b) --CN, c) --NHR.sup.14 d) --NHC(NH)H, e) --NHC(NH)NHR.sup.14, f) --C(NH)NHR.sup.14, g) --OR.sup.14, or h) --SC(.dbd.NH)NHR.sup.14 ; R.sup.11 is H; R.sup.13 is H, halogen (F, Cl, Br, I), --(CH.sub.2).sub.w NO.sub.2, C.sub.1 -C.sub.6)alkyl, --(CH.sub.2).sub.r --D, --(CH.sub.2).sub.w --OR.sup.8, --(CH.sub.2).sub.w CONR.sup.8 R.sup.9, --(CH.sub.2).sub.w CN, --(CH.sub.2).sub.w NC, --(CH.sub.2).sub.w NR.sup.8 R.sup.3, --(CH.sub.2).sub.w S (O).sub.2 R.sup.7, --(CH.sub.2).sub.w SO.sub.2 NHCO--(C.sub.1 -C.sub.6)-alkyl, --(CH.sub.2).sub.w NHSO.sub.2 -phenyl--(CH.sub.2).sub.w SO.sub.2 NH--(C.sub.1 -C.sub.5)-alkyl, --(CH.sub.2).sub.w SO.sub.2 NH.sub.2, --(CH.sub.2).sub.w SO.sub.2 NHCO.sub.2 (C.sub.1 -C.sub.6)-alkyl, --(CH.sub.2).sub.w NHSO.sub.2 --(C.sub.1 C.sub.6)-alkyl, --(CH.sub.2).sub.w NHSO.sub.2 --(C.sub.1 -C.sub.6)-perfluoroalkyl, --(CH.sub.2).sub.w CN.sup.4 H, --O(C.dbd.O)--(C.sub.1 -C.sub.5 -alkyl), --O(CH.sub.2).sub.t CN, --NH (CH.sub.2).sub.t CN, --S (CH.sub.2).sub.t CN, --(CH.sub.2).sub.w NH--CO--(C.sub.1 -C.sub.6 -alkyl), --(CH.sub.2).sub.w NH--CO--(C.sub.1 -C.sub.6 -perfluoroalkyl), or --(CH.sub.2).sub.u phenyl wherein the phenyl contains 0-3 substituents selected from R.sup.18 ; R.sup.14 is --H; R.sup.18 and R.sup.19 are independently H, halo (F, Cl, Br, I), C.sub.1 -C.sub.6 -alkyl, --(CH.sub.2).sub.w --OR.sup.8, --(CH.sub.2).sub.w CN, --(CH.sub.2).sub.w NC, --(CH.sub.2).sub.w NO.sub.2, (CH.sub.2).sub.w S (O).sub.r R.sup.7, --(CH.sub.2).sub.w NR.sup.8 R.sup.9, --(CH.sub.2).sub.w COR.sup.8, --(CH.sub.2).sub.w CO.sub.2 R.sup.8, --(CH.sub.2).sub.w CONR.sup.8 R.sup.9, --(CH.sub.2).sub.w SO.sub.2 NH--(C.sub.1 -C.sub.5)-alkyl, --(CH.sub.2).sub.w SO.sub.2 NH.sub.2, --(CH.sub.2).sub.w SO.sub.2 NH--CO--(C.sub.1 -C.sub.6)-alkyl, --(CH.sub.2).sub.w SO.sub.2 NH--CO.sub.2 --(C.sub.1 -C.sub.6)-alkyl, --(CH.sub.2).sub.w NHSO.sub.2 --(C.sub.1 -C.sub.6)-alkyl, --(CH.sub.2).sub.w NHSO.sub.2 --(C.sub.1 -C.sub.6)-perfluoroalkyl, --(CH.sub.2).sub.w NHSO.sub.2 -phenyl, --(CH.sub.2).sub.w NHSO.sub.2 -perfluorophenyl, --(CH.sub.2).sub.w CN.sub.4 H, --O(C.dbd.O)--(C.sub.1 -C.sub.5 -alkyl), --O(CH.sub.2).sub.t CN, --NH (CH.sub.2).sub.t CN, --S (CH.sub.2).sub.t CN, --(CH.sub.2).sub.w NH--CO--(C.sub.1 -C.sub.6 -alkyl), --(CH.sub.2).sub.w NH--CO--(C.sub.1 -C.sub.6 -perfluoroalkyl), --(CH.sub.2).sub.w NH--CO--(C.sub.1 -C.sub.6 -phenyl), --(CH.sub.2).sub.w NH--CO.sub.2 --(C.sub.1 -C.sub.6 -alkyl), --(CH.sub.2).sub.w NH--CO.sub.2 --(C.sub.1 -C.sub.6 -phenyl), or --O(C.dbd.O)phenyl; R.sup.18 and R.sup.19 can be taken together to form a methylenedioxy group; R.sup.20 is selected from the group consisting of: (CH.sub.2).sub.r --D, or --(CH.sub.2).sub.u phenyl wherein the phenyl contains 0-3 substituents selected from R.sup.18 ; and all other required substituents of formula (I) are defined as in Claim 3.

Specifically preferred are those most preferred compounds listed below:

N.sup.1 -(4-phenylbenzoyl)-(R)-boroarginine, hydrochloride N.sup.1 -(3-phenoxybenzoyl)-(R)-boroarginine, hydrochloride N.sup.1 -(1-fluorenonyl)-(R)-boroarginine, hydrochloride N.sup.1 -(4-�1-butyl!benzoyl)-(R)-boroarginine, hydrochloride N.sup.1 -(2-benzoylbenzoyl)-(R)-boroarginine, hydrochloride N.sup.1 -(5-phenyl-2-furoyl)-(R)-boroarginine, hydrochloride N.sup.1 -(3-�N-benzyloxycarbonyl-N-methylamino!-4-�1-butyl!-benzoyl)-(R)-boroarginine, hydrochloride N.sup.1 -(2-phenyl-4-isoquinoloyl)-(R)-boroarginine, hydrochloride N.sup.1 -(4-cyclohexylbenzoyl)-(R)-boroarginine, hydrochloride N.sup.1 -(2-methyl-4-phenylbenzoyl)-(R)-boroarginine, hydrochloride N.sup.1 -�4-phenyl-2-nitrobenzoyl!boroArg, (+)-pinanediol ester N.sup.1 -�4-phenyl-2-fluorobenzoyl!boroArg, (+)-pinanediol ester N.sup.1 -�4-phenyl-2-aminobenzoyl!boroArg, (+)-pinanediol ester N.sup.1 -�4-phenyl-2-(methylsulfonamido)benzoyl!boroArg, (+)-pinanediol ester N.sup.1 -�4-phenyl-2-(cyanomethylamino)benzoyl!boroArg, (+)-pinanediol ester N.sup.1 -�4-phenyl-2-(cyanomethyl)benzoyl!boroArg, (+)-pinanediol ester N.sup.1 -�4-phenyl-2-(diethylamino)benzoyl!boroArg, (+)-pinanediol ester N.sup.1 -�4-�2-(t-butylaminosulfonyl)phenyl!-2-methyl-benzoyl!boroArg, (+)pinanediol ester N.sup.1 -�4-�2-(aminosulfonyl)phenyl!-2-methyl-benzoyl!boroArg, (+)pinanediol ester N.sup.1 -�4-�2-(methoxycarbonylaminosulfonyl)phenyl!-2-methyl-benzoyl!boroArg, (+)-pinanediol ester N.sup.1 -�4-�2-(t-butylaminosulfonyl)phenyl!benzoyl!boroArg, (+)-pinanediol ester N.sup.1 -�4-�2-(t-butylaminosulfonyl)phenyl!benzoyl!boroArg-OH N.sup.1 -�4-�2-(n-butoxycarbonylaminosulfonyl)phenyl!-2-methyl-benzoyl!boroArg, (+)-pinanediol ester N.sup.1 -�4-�2-(diethylaminosulfonyl)phenyl!-2-methyl-benzoyl!boroArg, (+)pinanediol ester N.sup.1 -�4-�2-(t-butylaminosulfonyl)phenyl!-2-fluoro-benzoyl!boroArg, (+)pinanediol ester N.sup.1 -�4-�2-(aminosulfonyl)phenyl!-2-fluoro-benzoyl!boroArg, (+)pinanediol ester N.sup.1 -�4-�2-(methoxycarbonylaminosulfonyl)phenyl!-2-fluoro-benzoyl!boroArg, (+)-pinanediol ester N.sup.1 -�4-�2-(t-butylaminosulfonyl)phenyl!-2-nitro-benzoyl!boroArg, (+)pinanediol ester N.sup.1 -�4-�2-(aminosulfonyl)phenyl!-2-nitro-benzoyl!boroArg, (+)pinanediol ester N.sup.1 -�4-�2-(methoxycarbonylaminosulfonyl)phenyl!-2-nitro-benzoyl!boroArg, (+)-pinanediol ester N.sup.1 -(3-phenylbenzoyl)boroarg, (+)-pinanediol N.sup.1 -�4-(3-BOCNHphenyl).sub.2 -methylbenzoyl!boroarg, (+)-pinanediol N.sup.1 -(5-phenyl-2-furoyl)boroarg, (+)-pinanediol N.sup.1 -(5-phenyl-2-thienyl)boroarg, (+)-pinanediol N.sup.1 -�4-(3-nitrophenyl)benzoyl!boroarg, (+)-pinanediol N.sup.1 -�4-(3-aminophenyl)benzoyl!boroarg, (+)-pinanediol N.sup.1 -(3-phenylbenzoyl)borolys, (+)-pinanediol N.sup.1 -(5-phenyl-2-furoyl)boroarg-OH N.sup.1 -(3-phenylbenzoyl)boroIrg, (+)-pinanediol (R)-�5-amino-1-���5-(phenylmethyl)-1H-1,2,4-triazol-1-yl!acetyl!amino!-pentyl!boronic acid hydrochloride �3aS-�2(S*),3a.alpha.,4.beta.,6.beta.!!-(1,1-dimethylethyl) �3-�5-���4-�(amino-iminomethyl)amino!-1-(hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzo-dioxaborol-2-yl)butyl!amino!carbonyl!-2-thienyl!phenyl!carbamate hydrochloride �3aS-�2(S*),3a.alpha.,4.beta.,6.beta.,7a.alpha.!!-N-�5-amino-1-(hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl) pentyl!-5-(phenyl-methyl)-3-(2H-tetrazol-5-ylmethyl)-1H-1,2,4-triazole-1-acetamide hydrochloride �3aS-�2(S*),3a,4.beta.,6.beta.,7a.alpha.!!-1-�2-��5-amino-1-(hexahydro-3a, 5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2 -yl) pentyl!amino!-2-oxoethyl!-5-(phenylmethyl)-1H-1,2,4-triazole-3-acetic acid hydrochloride 1:1 with �3aS-�2(S*), 3a.alpha.,4.beta.,6.beta.,7a.alpha.!!-1-�2-��5-amino-1-(hexahydro-3a, 5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl)pentyl!amino!-2-oxoethyl!-3-(phenylmethyl)-1H-1,2,4-triazole-5-acetic acid hydrochloride �3aS-�2(S*),3a.alpha.,4.beta.,6.beta.,7a.alpha.!!-methyl 1-�2-��5-amino-1-(hexahydro-3a, 5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl) pentyl!-amino!-2-oxoethyl!-5-(phenylmethyl)-1H-1,2,4-triazole-3-acetate hydrochloride �3aS-�2(S*),3a.alpha.,4.beta.,6.beta.,7a.alpha.!!-methyl 1-�2-��5-amino-1-(hexahydro-3a, 5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl)pentyl!-amino!-2-oxoethyl!-3-(phenylmethyl)-1H-1,2,4-triazole-5-acetate hydrochloride �3aS-�2(S*), 3a.alpha.,4.beta.,6.beta.,7a.beta.!!-N-�5-amino-1-(hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl) pentyl!-3-phenyl-5-(phenyl -methyl)-1H-1,2,4-triazole-1-acetamide hydrochloride (R)-�5-amino-1-���3-phenyl-5-(phenylmethyl)-1H-1,2,4-triazol-1-yl!acetyl!-amino!pentyl!boronic acid hydrochloride �3aS-�2(S*), 3a.alpha.,4.beta.,6.beta.,7a.beta.!!-N-�5-amino-1-(hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl) pentyl!-3-(3-nitro-phenyl)-5-(phenylmethyl)-1H-1, 2,4-triazole-1-acetamide hydrochloride �3aS-�2(S*), 3a.alpha.,4.beta.,6.beta.,7a.beta.!!-N-�4-�(aminoiminomethyl)-amino!-1-(hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl) butyl!-3-(3-nitrophenyl)-5-(phenylmethyl)-1H-1,2,4-triazole-1-acetamide hydrochloride �3aS-�2(S*),3a.alpha.,4.beta.,6.beta.,7a.beta.!!-N-�5-amino-1-(hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl)pentyl!-3,5-bis(phenyl-methyl)-1H-1,2,4-triazole-1-acetamide hydrochloride �3aS-�2(S*),3a.alpha.,4.beta.,6.beta.,7a.beta.!!-N-�4-�(aminoiminomethyl)-amino!-1-(hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl)butyl!-3,5-bis(phenylmethyl)-1H-1,2,4-triazole-1-acetamide hydrochloride �3aS-�2(S*),3a.alpha.,4.beta.,6.beta.,7a.beta.!!-N-�5-amino-1-(hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl)pentyl!-3-(phenylmethyl)-1H-1,2,4-triazole-1-acetamide (R)-�5-amino-1-���3-(phenylmethyl)-1H-1,2,4-triazol-1-yl!acetyl!amino!-pentyl!boronic acid hydrochloride �3aS-�2(S*),3a.alpha.,4.beta.,6.beta.,7a.beta.!!-N-�5-amino-1-(hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl)pentyl!-5-methyl-3-(phenylmethyl)-1H-1,2,4-triazole-1-acetamide hydrochloride �3aS-�2(R*),3a.alpha.,4.beta.,6.beta.!!-N-�5-amino-1-(hexahydro-3a,5,5-tri-methyl-4,6-methano-1,3,2-benzodioxaborol-2-yl)pentyl!-5-�(phenyl-methoxy).sub.m ethyl!-3-(phenylmethyl)-1H-1,2,4-triazole-1-acetamide hydrochloride �3aS-�2(S*),3a.alpha.,4.beta.,6.beta.,7a.beta.!!-N-�5-amino-1-(hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl)pentyl!-5-(cyanomethyl)-3-(phenylmethyl)-1H-1,2,4-triazole-1-acetamide hydrochloride �3aS-�2(S*),3a.alpha.,4.beta.,6.beta.,7a.beta.!!-N-�5-amino-1-(hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl)pentyl!-3-(phenylmethyl)-5-propyl-1H-1,2,4-triazole-1-acetamide hydrochloride �3aS-�2(S*),3a.alpha.,4.beta.,6.beta.,7a.beta.!!-N-�5-amino-1-(hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl)pentyl!-5-phenyl-3-(phenylmethyl)-1H-1,2,4-triazole-1-acetamide hydrochloride (R)-�5-amino-1-���5-methyl-3-(phenylmethyl)-1H-1,2,4-triazol-1-yl!acetyl!-amino!pentyl!boronic acid hydrochloride �3aS-�2(S*), 3a.alpha.,4.beta.,6.beta.,7.beta.!!-N-�5-amino-1-(hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl) pentyl!-3-phenyl-1H-1,2,4-triazole-1-acetamide hydrochloride �3aS-�2(S*), 3a.alpha.,4.beta.,6.beta.,7a.beta.!!-N-�5-amino-1-(hexahydro-3a, 5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl) pentyl!-5-methyl -3-phenyl -1H-1,2,4-triazole-1-acetamide hydrochloride �3aS-�2(S*), 3a.alpha.,4.beta.,6.beta.,7a.beta.!!-N-�5-amino-1-(hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl) pentyl!-5-(2-phenyl-ethyl)-1H-1,2,4-triazole-1-acetamide (R)-�5-amino-1-���5-(2-phenylethyl)-1H-1,2,4-triazol-1-yl!acetyl!amino!-pentyl!boronic acid hydrochloride �3aS-�2(S*),3a.alpha.,4.beta.,6.beta.,7a.beta.!!-N-�5-amino-1-(hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl)pentyl!-3,5-bis(2-phenyl-ethyl)-1H-1,2,4-triazole-1-acetamide hydrochloride (R)-�5-amino-1-���3,5-bis(2-phenylethyl)-1H-1,2,4-triazol-1-yl!acetyl!amino!-pentyl!boronic acid hydrochloride �3aS-�2(S*), 3a.alpha.,4.beta.,6.beta.,7a.beta.!!-N-�5-amino-1-(hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl) pentyl!-3-(2-phenylethyl)-1H-1,2,4-triazole-1-acetamide (R)-�5-amino-1-���3-(2-phenylethyl)-1H-1,2,4-triazol-1-yl!acetyl!amino!-pentyl!boronic acid hydrochloride �3aS-�2(S*), 3a.alpha.,4.beta.,6.beta.,7a.beta.!!-N-�5-amino-1-(hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl) pentyl!-3-(3-phenyl-propyl)-1H-1,2,4-triazole-1-acetamide (R)-�5-amino-1-���5-(3-phenylpropyl)-1H-1,2,4-triazol-1-yl!acetyl!amino!-pentyl!boronic acid hydrochloride (R)-�5-amino-1-���3-(3-phenylpropyl)-1H-1,2,4-triazol-1-yl!acetyl!amino!-pentyl!boronic acid hydrochloride �3aS-�2(S*),3a.alpha.,4.beta.,6.beta.,7a.beta.!!-N-�5-amino-1-(hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl)pentyl!-1,5-bis(phenyl-methyl)-1H-1,2,4-triazole-3-acetamide hydrochloride 2:8 with (R)-�5-amino-1-���1,5-bis(phenylmethyl)-1H-1,2,4-triazol-3-yl!acetyl!amino!-pentyl!boronic acid hydrochloride �3aS-�2(S*),3a.alpha.,4.beta.,6.beta.,7a.beta.!!-N-�5-amino-1-(hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl)pentyl!-4-methyl-2-phenyl-5-pyrimidinecarboxamide hydrochloride �3aS-�2(S*),3a.alpha.,4.beta.,6.beta.,7a.beta.!!-N-�5-amino-1-(hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl)pentyl!-2,4-diphenyl-5-pyrimidinecarboxamide hydrochloride �3aS-�2(S*),3a.alpha.,4.beta.,6.beta.,7a.beta.!!-N-�4-�(amimoiminomethyl)amino!-1-(hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl)-butyl!-4-methyl-2-phenyl-5-pyrimidinecarboxamide hydrochloride �3aS-�2(S*),3.alpha.,4.beta.,6.beta.,7a.beta.!!-N-�5-amino-1-(hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl)pentyl!-6-phenyl-3-pyridinecarboxamide hydrochloride (R)-�5-amino-1-��(6-phenyl-3-pyridinyl)carbonyl!amino!pentyl!boronic acid dihydrochloride

Illustrative of the compounds of this invention are the following:

N.sup.1 -(4-phenylbenzoyl)-(R)-boroarginine (+)-pinanediol, bisulfite N.sup.1 -(3-phenylbenzoyl)-(R)-boroarginine (+)-pinanediol, bisulfite N.sup.1 -(3-phenoxybenzoyl)-(R)-boroarginine (+)-pinanediol, bisulfite N.sup.1 -(4-�4-pyridyl!benzoyl)-(R)-boroarginine (+)-pinanediol, bisulfite N.sup.1 -(2-benzoylbenzoyl)-(R)-boroarginine (+)-pinanediol, bisulfite N.sup.1 -(3-benzoylbenzoyl)-(R)-boroarginine (+)-pinanediol, bisulfite N.sup.1 -(4-benzoylbenzoyl)-(R)-boroarginine (+)-pinanediol, bisulfite N.sup.1 -(3-�N-benzyloxycarbonyl!aminobenzoyl)-(R)-boroarginine (+)-pinanediol, bisulfite N.sup.1 -(3-�N-benzyloxycarbonyl-N-methyl!aminobenzoyl)-(R)-boroarginine (+)-pinanediol, bisulfite N.sup.1 -(4-ethylbenzoyl)-(R)-boroarginine (+)-pinanediol, bisulfite N.sup.1 -(4-n-propylbenzoyl)-(R)-boroarginine (+)-pinanediol, bisulfite N.sup.1 -(4-isopropylbenzoyl)-(R)-boroarginine (+)-pinanediol, bisulfite N.sup.1 -(4-n-butylbenzoyl)-(R)-boroarginine (+)-pinanediol, bisulfite N.sup.1 -(4-tert-butylbenzoyl)-(R)-boroarginine (+)-pinanediol, bisulfite N.sup.1 -(4-n-hexylbenzoyl)-(R)-boroarginine (+)-pinanediol, bisulfite N.sup.1 -(4-cyclohexylbenzoyl)-(R)-boroarginine (+)-pinanediol, bisulfite N.sup.1 -(2-�N-(2-phenylethyl)carbonyl!aminobenzoyl)-(R)-boroarginine (+)-pinanediol, bisulfite N.sup.1 -(4-n-butyloxybenzoyl)-(R)-boroarginine (+)-pinanediol, bisulfite N.sup.1 -(4-�N-cyclopropylcarbonyl!aminobenzoyl)-(R)-boroarginine (+)-pinanediol, bisulfite N.sup.1 -(4-�N-cyclohexylcarbonyl!aminobenzoyl)-(R)-boroarginine (+)-pinanediol, bisulfite N.sup.1 -(4-�N-(4-methoxy)benzoyl!aminobenzoyl)-(R)-boroarginine (+)-pinanediol, bisulfite N.sup.1 -(4-�4-methoxy!phenylbenzoyl)-(R)-boroarginine (+)-pinanediol, bisulfite N.sup.1 -(2-�2-phenyl!benzyloxycarbonylbenzoyl)-(R)-boroarginine (+)-pinanediol, bisulfite N.sup.1 -(2-�1-naphthyl!benzoyl)-(R)-boroarginine (+)-pinanediol, bisulfite N.sup.1 -(4-�4-carboxy!phenylbenzoyl)-(R)-boroarginine (+)-pinanediol, bisulfite N.sup.1 -(4-phenylbenzoyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide N.sup.1 -(3-phenylbenzoyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide N.sup.1 -(3-phenoxybenzoyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide N.sup.1 -(2-benzoylbenzoyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide N.sup.1 -(3-benzoylbenzoyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide N.sup.1 -(4-benzoylbenzoyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide N.sup.1 -(3-�N-benzyloxycarbonyl!aminobenzoyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide N.sup.1 -(3-�N-benzyloxycarbonyl-N-methyl!aminobenzoyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide N.sup.1 -(4-ethylbenzoyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide N.sup.1 -(4-n-propylbenzoyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide N.sup.1 -(4-isopropylbenzoyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide N.sup.1 -(4-n-butylbenzoyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide N.sup.1 -(4-tert-butylbenzoyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide N.sup.1 -(4-n-hexylbenzoyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide N.sup.1 -(4-cyclohexylbenzoyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide N.sup.1 -(2-�N-(2-phenylethyl)carbonyl!aminobenzoyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide N.sup.1 -(4-n-butyloxybenzoyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide N.sup.1 -(4-�N-cyclopropylcarbonyl!aminobenzoyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide N.sup.1 -(4-�N-cyclohexylcarbonyl!aminobenzoyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide N.sup.1 -(4-�N-(4-methoxy)benzoyl!aminobenzoyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide N.sup.1 -(4-�4-methoxy!phenylbenzoyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide N.sup.1 -(2-�2-phenylbenzyloxycarbonyl!benzoyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide N.sup.1 -(2-�1-naphthyl!benzoyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide N.sup.1 -(4-�4-carboxy!phenylbenzoyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide N.sup.1 -(�2-anthraquinonyl!carbonyl)-(R)-boroarginine (+)-pinanediol, bisulfite N.sup.1 -(�2-dioxothioxanthinonyl!carbonyl)-(R)-boroarginine (+)-pinanediol, bisulfite N.sup.1 -(�2-anthraquinonyl!carbonyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide N.sup.1 -(�2-dioxothioxanthinonyl!carbonyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide N.sup.1 -(�2-fluoren-9-onyl!carbonyl)-(R)-borothiohomoarginine (+)-pinanediol, hydrobromide N.sup.1 -(�2-fluoren-9-onyl!carbonyl)-(R)-boroarginine (+)-pinanediol, bisulfite N.sup.1 -(�2-fluoren-9-onyl!carbonyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide N.sup.1 -(�3-fluoren-9-onyl!carbonyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide N.sup.1 -(�3-fluoren-9-onyl!carbonyl)-(R)-boroarginine (+)-pinanediol, bisulfite N.sup.1 -(�4-fluoren-9-onyl!carbonyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide N.sup.1 -(�4-fluoren-9-onyl!carbonyl)-(R)-boroarginine (+)-pinanediol, bisulfite N.sup.1 -(1-naphthoyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide N.sup.1 -(1-naphthoyl)-(R)-boroarginine (+)-pinanediol, bisulfite N.sup.1 -(2-methyl-4-phenyl-5-methoxybenzoyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide N.sup.1 -(2-methyl-4-phenyl-5-carboxamidobenzoyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide N.sup.1 -(2-methyl-4-phenyl-5-fluorobenzoyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide N.sup.1 -(2-methyl-4-phenyl-5-trifluoromethylbenzoyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide N.sup.1 -(2-methyl-4-phenyl-5-chlorobenzoyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide N.sup.1 -(2-methyl-4-phenyl-5-hydroxybenzoyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide N.sup.1 -(2-methyl-4-�4-carboxy!phenyl-5-methoxybenzoyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide N.sup.1 -(2-methyl-4-�4-carboxy!phenyl-5-carboxamidobenzoyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide N.sup.1 -(2-methyl-4-�4-carboxy!phenyl-5-fluorobenzoyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide N.sup.1 -(2-methyl-4-�4-carboxy!phenyl-5-trifluoromethylbenzoyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide N.sup.1 -(2-methyl-4-�4-carboxy!phenyl-5-chlorobenzoyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide N.sup.1 -(2-methyl-4-�4-carboxy!phenyl-5-hydroxybenzoyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide N.sup.1 -(2-methyl-4-phenyl-5-methoxybenzoyl)-(R)-boroarginine (+)-pinanediol, bisulfite N.sup.1 -(2-methyl-4-phenyl-5-carboxamidobenzoyl)-(R)-boroarginine (+)-pinanediol, bisulfite N.sup.1 -(2-methyl-4-phenyl-5-fluorobenzoyl)-(R)-boroarginine (+)-pinanediol, bisulfite N.sup.1 -(2-methyl-4-phenyl-5-trifluoromethylbenzoyl)-(R)-boroarginine (+)-pinanediol, bisulfite N.sup.1 -(2-methyl-4-phenyl-5-chlorobenzoyl)-(R)-boroarginine (+)-pinanediol, bisulfite N.sup.1 -(2-methyl-4-phenyl-5-hydroxybenzoyl)-(R)-boroarginine (+)-pinanediol, bisulfite N.sup.1 -(2-methyl-4-�4-carboxy!phenyl-5-methoxybenzoyl)-(R)-boroarginine (+)-pinanediol, bisulfite N.sup.1 -(2-methyl-4-�4-carboxy!phenyl-5-carboxamidobenzoyl)-(R)-boroarginine (+)-pinanediol, bisulfite N.sup.1 -(2-methyl-4-�4-carboxy!phenyl-5-fluorobenzoyl)-(R)-boroarginine (+)-pinanediol, bisulfite N.sup.1 -(2-methyl-4-�4-carboxy!phenyl-5-trifluoromethylbenzoyl)-(R)-boroarginine (+)-pinanediol, bisulfite N.sup.1 -(2-methyl-4-�4-carboxy!phenyl-5-chlorobenzoyl)-(R)-boroarginine (+)-pinanediol, bisulfite N.sup.1 -(2-methyl-4-�4-carboxy!phenyl-5-hydroxybenzoyl)-(R)-boroarginine (+)-pinanediol, bisulfite N.sup.1 -(2-�5-phenyl!furylcarbonyl)-(R)-boroarginine (+)-pinanediol, bisulfite N.sup.1 -(2-�5-phenyl!thiophen-ylcarbonyl)-(R)-boroarginine (+)-pinanediol, bisulfite N.sup.1 -(2-�5-phenyl!furylcarbonyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide N.sup.1 -(2-�5-phenyl!thiophen-ylcarbonyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide N.sup.1 -(3-�6-phenyl!pyridylcarbonyl)-(R)-boroarginine (+)-pinanediol, bisulfite N.sup.1 -(3-�5-benzyloxy!pyridylcarbonyl)-(R)-boroarginine (+)-pinanediol, bisulfite N.sup.1 -(3-�6-phenyl!pyridylcarbonyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide N.sup.1 -(3-�5-benzyloxy!pyridylcarbonyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide N.sup.1 -(2-benzopyronylcarbonyl)-(R)-boroarginine(+)-pinanediol, bisulfite N.sup.1 -(2-benzopyronylcarbonyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide N.sup.1 -(3-isoquinolinylcarbonyl)-(R)-boroarginine (+)-pinanediol, bisulfite N.sup.1 -(2-phenyl-4-isoquinolinylcarbonyl)-(R)-boroarginine (+)-pinanediol, bisulfite N.sup.1 -(3-isoquinolinylcarbonyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide N.sup.1 -(2-phenyl-4-isoquinolinylcarbonyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide N.sup.1 -(2-isoquinolinylcarbonyl)-(R)-boroarginine(+)-pinanediol, bisulfite N.sup.1 -(2-isoquinolinylcarbonyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide N.sup.1 -(4-phenylbenzoyl)-(R)-boroarginine, hydrochloride N.sup.1 -(3-phenylbenzoyl)-(R)-boroarginine, hydrochloride N.sup.1 -(3-phenoxybenzoyl)-(R)-boroarginine, hydrochloride N.sup.1 -(4-�4-pyridyl!benzoyl)-(R)-boroarginine, hydrochloride N.sup.1 -(2-benzoylbenzoyl)-(R)-boroarginine, hydrochloride N.sup.1 -(3-benzoylbenzoyl)-(R)-boroarginine, hydrochloride N.sup.1 -(4-benzoylbenzoyl)-(R)-boroarginine, hydrochloride N.sup.1 -(3-�N-benzyloxycarbonyl!aminobenzoyl)-(R)-boroarginine, hydrochloride N.sup.1 -(3-�N-benzyloxycarbonyl-N-methyl!aminobenzoyl)-(R)-boroarginine, hydrochloride N.sup.1 -(4-ethylbenzoyl)-(R)-boroarginine, hydrochloride N.sup.1 -(4-n-propylbenzoyl)-(R)-boroarginine, hydrochloride N.sup.1 -(4-isopropylbenzoyl)-(R)-boroarginine, hydrochloride N.sup.1 -(4-tert-butylbenzoyl)-(R)-boroarginine, hydrochloride N.sup.1 -(4-n-hexylbenzoyl)-(R)-boroarginine, hydrochloride N.sup.1 -(4-cyclohexylbenzoyl)-(R)-boroarginine, hydrochloride N.sup.1 -(2-�N-(2-phenylethyl)carbonyl!aminobenzoyl)-(R)-boroarginine, hydrochloride N.sup.1 -(4-n-butyloxybenzoyl)-(R)-boroarginine, hydrochloride N.sup.1 -(4-�N-cyclopropylcarbonyl!aminobenzoyl)-(R)-boroarginine, hydrochloride N.sup.1 -(4-�N-cyclohexylcarbonyl!aminobenzoyl)-(R)-boroarginine, hydrochloride N.sup.1 -(4-�N-(4-methoxy)benzoyl!aminobenzoyl)-(R)-boroarginine, hydrochloride N.sup.1 -(4-�4-methoxy!phenylbenzoyl)-(R)-boroarginine, hydrochloride N.sup.1 -(2-�2-phenyl!benzyloxycarbonylbenzoyl)-(R)-boroarginine, hydrochloride N.sup.1 -(2-�1-naphthyl!benzoyl)-(R)-boroarginine, hydrochloride N.sup.1 -(4-�4-carboxy!phenylbenzoyl)-(R)-boroarginine, hydrochloride N.sup.1 -(�2-anthraquinonyl!carbonyl)-(R)-boroarginine, hydrochloride N.sup.1 -(�2-dioxothioxanthinonyl!carbonyl)-(R)-boroarginine, hydrochloride N.sup.1 -(�2-fluoren-9-onyl!carbonyl)-(R)-boroarginine, hydrochloride N.sup.1 -(�3-fluoren-9-onyl!carbonyl)-(R)-boroarginine, hydrochloride N.sup.1 -(1-naphthoyl)-(R)-boroarginine, hydrochloride N.sup.1 -(�4-fluoren-9-onyl!carbonyl)-(R)-boroarginine, hydrochloride N.sup.1 -(2-methyl-4-phenyl-5-methoxybenzoyl)-(R)-boroarginine, hydrochloride N.sup.1 -(2-methyl-4-phenyl-5-carboxamidobenzoyl)-(R)-boroarginine, hydrochloride N.sup.1 -(2-methyl-4-phenyl-5-fluorobenzoyl)-(R)-boroarginine, hydrochloride N.sup.1 -(2-methyl-4-phenyl-5-trifluoromethylbenzoyl)-(R)-boroarginine, hydrochloride N.sup.1 -(2-methyl-4-phenyl-5-chlorobenzoyl)-(R)-boroarginine, hydrochloride N.sup.1 -(2-methyl-4-phenyl-5-hydroxybenzoyl)-(R)-boroarginine, hydrochloride N.sup.1 -(2-methyl-4-�4-carboxy!phenyl-5-methoxybenzoyl)-(R)-boroarginine, hydrochloride N.sup.1 -(2-methyl-4-�4-carboxy!phenyl-5-carboxamidobenzoyl)-(R)-boroarginine, hydrochloride N.sup.1 -(2-methyl-4-�4-carboxy!phenyl-5-fluorobenzoyl)-(R)-boroarginine, hydrochloride N.sup.1 -(2-methyl-4-�4-carboxy!phenyl-5-trifluoromethylbenzoyl)-(R)-boroarginine, hydrochloride N.sup.1 -(2-methyl-4-�4-carboxy!phenyl-5-chlorobenzoyl)-(R)-boroarginine, hydrochloride N.sup.1 -(2-methyl-4-�4-carboxy!phenyl-5-hydroxybenzoyl)-(R)-boroarginine, hydrochloride N.sup.1 -(2-�5-phenyl!furylcarbonyl)-(R)-boroarginine, hydrochloride N.sup.1 -(2-�5-phenyl!thiophen-ylcarbonyl)-(R)-boroarginine, hydrochloride N.sup.1 -(2-benzopyronylcarbonyl)-(R)-boroarginine, hydrochloride N.sup.1 -(2-isoquinolinylcarbonyl)-(R)-boroarginine, hydrochloride N.sup.1 -(3-isoquinolinylcarbonyl)-(R)-boroarginine, hydrochloride N.sup.1 -(2-phenyl-4-isoquinolinylcarbonyl)-(R)-boroarginine, hydrochloride N.sup.1 -(4-phenylbenzoyl)-(R)-borothioarginine, hydrochloride N.sup.1 -(3-phenylbenzoyl)-(R)-borothioarginine, hydrochloride N.sup.1 -(3-phenoxybenzoyl)-(R)-borothioarginine, hydrochloride N.sup.1 -(2-benzoylbenzoyl)-(R)-borothioarginine, hydrochloride N.sup.1 -(3-benzoylbenzoyl)-(R)-borothioarginine, hydrochloride N.sup.1 -(4-benzoylbenzoyl)-(R)-borothioarginine, hydrochloride N.sup.1 -(3-�N-benzyloxycarbonyl!aminobenzoyl)-(R)-borothioarginine, hydrochloride N.sup.1 -(3-�N-benzyloxycarbonyl-N-methyl!aminobenzoyl)-(R)-borothioarginine, hydrochloride N.sup.1 -(4-ethylbenzoyl)-(R)-borothioarginine, hydrochloride N.sup.1 -(4-n-propylbenzoyl)-(R)-borothioarginine, hydrochloride N.sup.1 -(4-isopropylbenzoyl)-(R)-borothioarginine, hydrochloride N.sup.1 -(4-n-butylbenzoyl)-(R)-borothioarginine, hydrochloride N.sup.1 -(4-tert-butylbenzoyl)-(R)-borothioarginine, hydrochloride N.sup.1 -(4-n-hexylbenzoyl)-(R)-borothioarginine, hydrochloride N.sup.1 -(4-cyclohexylbenzoyl)-(R)-borothioarginine, hydrochloride N.sup.1 -(2-�N-(2-phenylethyl)carbonyl!aminobenzoyl)-(R)-borothioarginine, hydrochloride N.sup.1 -(4-n-butyloxybenzoyl)-(R)-borothioarginine, hydrochloride N.sup.1 -(4-�N-cyclopropylcarbonyl!aminobenzoyl)-(R)-borothioarginine, hydrochloride N.sup.1 -(4-�N-cyclohexylcarbonyl!aminobenzoyl)-(R)-borothioarginine, hydrochloride N.sup.1 -(4-�N-(4-methoxy)benzoyl!aminobenzoyl)-(R)-borothioarginine, hydrochloride N.sup.1 -(4-�4-methoxy!phenylbenzoyl)-(R)-borothioarginine, hydrochloride N.sup.1 -(2-�2-phenylbenzyloxycarbonyl!benzoyl)-(R)-borothioarginine, hydrochloride N.sup.1 -(2-�1-naphthyl!benzoyl)-(R)-borothioarginine, hydrochloride N.sup.1 -(4-�4-carboxy!phenylbenzoyl)-(R)-borothioarginine, hydrochloride N.sup.1 -�(2-anthraquinonyl!carbonyl)-(R)-borothioarginine, hydrochloride N.sup.1 -�(2-dioxothioxanthinonyl!carbonyl)-(R)-borothioarginine, hydrochloride N.sup.1 -�(2-fluoren-9-onyl!carbonyl)-(R)-borothiohomoarginine, hydrochloride N.sup.1 -�(2-fluoren-9-onyl!carbonyl)-(R)-borothioarginine, hydrochloride N.sup.1 -�(3-fluoren-9-onyl!carbonyl)-(R)-borothioarginine, hydrochloride N.sup.1 -�(4-fluoren-9-onyl!carbonyl)-(R)-borothioarginine, hydrochloride N.sup.1 -(1-naphthoyl)-(R)-borothioarginine, hydrochloride N.sup.1 -(2-methyl-4-phenyl-5-methoxybenzoyl)-(R)-borothioarginine, hydrochloride N.sup.1 -(2-methyl-4-phenyl-5-carboxamidobenzoyl)-(R)-borothioarginine, hydrochloride N.sup.1 -(2-methyl-4-phenyl-5-fluorobenzoyl)-(R)-borothioarginine, hydrochloride N.sup.1 -(2-methyl-4-phenyl-5-trifluoromethylbenzoyl)-(R)-borothioarginine, hydrochloride N.sup.1 -(2-methyl-4-phenyl-5-chlorobenzoyl)-(R)-borothioarginine, hydrochloride N.sup.1 -(2-methyl-4-phenyl-5-hydroxybenzoyl)-(R)-borothioarginine, hydrochloride N.sup.1 -(2-methyl-4-�4-carboxy!phenyl-5-methoxybenzoyl)-(R)-borothioarginine, hydrochloride N.sup.1 -(2-methyl-4-�4-carboxy!phenyl-5-carboxamidobenzoyl)-(R)-borothioarginine, hydrochloride N.sup.1 -(2-methyl-4-�4-carboxy!phenyl-5-fluorobenzoyl)-(R)-borothioarginine, hydrochloride N.sup.1 -(2-methyl-4-�4-carboxy!phenyl-5-trifluoromethylbenzoyl)-(R)-borothioarginine, hydrochloride N.sup.1 -(2-methyl-4-�4-carboxy!phenyl-5-chlorobenzoyl)-(R)-borothioarginine, hydrochloride N.sup.1 -(2-methyl-4-�4-carboxy!phenyl-5-hydroxybenzoyl)-(R)-borothioarginine, hydrochloride N.sup.1 -(2-�5-phenyl!furylcarbonyl)-(R)-borothioarginine, hydrochloride N.sup.1 -(2-�5-phenyl!thiophenylcarbonyl)-(R)-borothioarginine, hydrochloride N.sup.1 -(3-�6-phenyl!pyridylcarbonyl)-(R)-boroarginine, hydrochloride N.sup.1 -(3-�5-benzyloxy!pyridylcarbonyl)-(R)-boroarginine, hydrochloride N.sup.1 -(3-�6-phenyl!pyridylcarbonyl)-(R)-borothioarginine, hydrochloride N.sup.1 -(3-�5-benzyloxy!pyridylcarbonyl)-(R)-borothioarginine, hydrochloride N.sup.1 -(2-benzopyronylcarbonyl)-(R)-borothioarginine, hydrochloride N.sup.1 -(3-isoquinolinylcarbonyl)-(R)-borothioarginine, hydrochloride N.sup.1 -(2-phenyl-4-isoquinolinylcarbonyl)-(R)-borothioarginine, hydrochloride N.sup.1 -(2-isoquinolinylcarbonyl)-(R)-borothioarginine, hydrochloride N.sup.1 -(4-phenylbenzoyl)-(R)-borolysine (+)-pinanediol, hydrochloride N.sup.1 -(3-phenylbenzoyl)-(R)-borolysine (+)-pinanediol, hydrochloride N.sup.1 -(3-phenoxybenzoyl)-(R)-borolysine (+)-pinanediol, hydrochloride N.sup.1 -(4-�4-pyridyl!benzoyl)-(R)-borolysine (+)-pinanediol, hydrochloride N.sup.1 -(2-benzoylbenzoyl)-(R)-borolysine (+)-pinanediol, hydrochloride N.sup.1 -(3-benzoylbenzoyl)-(R)-borolysine (+)-pinanediol, hydrochloride N.sup.1 -(4-benzoylbenzoyl)-(R)-borolysine (+)-pinanediol, hydrochloride N.sup.1 -(3-�N-benzyloxycarbonyl!aminobenzoyl)-(R)-borolysine (+)-pinanediol, hydrochloride N.sup.1 -(3-�N-benzyloxycarbonyl-N-methyl!aminobenzoyl)-(R)-borolysine (+)-pinanediol, hydrochloride N.sup.1 -(4-ethylbenzoyl)-(R)-borolysine (+)-pinanediol, hydrochloride N.sup.1 -(4-n-propylbenzoyl)-(R)-borolysine (+)-pinanediol, hydrochloride N.sup.1 -(4-isopropylbenzoyl)-(R)-borolysine (+)-pinanediol, hydrochloride N.sup.1 -(4-tert-butylbenzoyl)-(R)-borolysine (+)-pinanediol, hydrochloride N.sup.1 -(4-n-hexylbenzoyl)-(R)-borolysine (+)-pinanediol, hydrochloride N.sup.1 -(4-cyclohexylbenzoyl)-(R)-borolysine (+)-pinanediol, hydrochloride N.sup.1 -(2-�N-(2-phenylethyl)carbonyl!aminobenzoyl)-(R)-borolysine (+)-pinanediol, hydrochloride N.sup.1 -(4-n-butyloxybenzoyl)-(R)-borolysine (+)-pinanediol, hydrochloride N.sup.1 -(4-�N-cyclopropylcarbonyl!aminobenzoyl)-(R)-borolysine (+)-pinanediol, hydrochloride N.sup.1 -(4-�N-cyclohexylcarbonyl!aminobenzoyl)-(R)-borolysine (+)-pinanediol, hydrochloride N.sup.1 -(4-�N-(4-methoxy)benzoyl!aminobenzoyl)-(R)-borolysine (+)-pinanediol, hydrochloride N.sup.1 -(4-�4-methoxy!phenylbenzoyl)-(R)-borolysine (+)-pinanediol, hydrochloride N.sup.1 -(2-�2-phenyl!benzyloxycarbonylbenzoyl)-(R)-borolysine (+)-pinanediol, hydrochloride N.sup.1 -(2-�1-naphthyl!benzoyl)-(R)-borolysine (+)-pinanediol, hydrochloride N.sup.1 -(4-�4-carboxy!phenylbenzoyl)-(R)-borolysine (+)-pinanediol, hydrochloride N.sup.1 -(�2-anthraquinonyl!carbonyl)-(R)-borolysine (+)-pinanediol, hydrochloride N.sup.1 -(�2-dioxothioxanthinonyl!carbonyl)-(R)-borolysine (+)-pinanediol, hydrochloride N.sup.1 -(�2-fluoren-9-onyl!carbonyl)-(R)-borolysine (+)-pinanediol, hydrochloride N.sup.1 -(�3-fluoren-9-onyl!carbonyl)-(R)-borolysine (+)-pinanediol, hydrochloride N.sup.1 -(1-naphthoyl)-(R)-borolysine (+)-pinanediol, hydrochloride N.sup.1 -(�4-fluoren-9-onyl!carbonyl)-(R)-borolysine (+)-pinanediol, hydrochloride N.sup.1 -(2-methyl-4-phenyl-5-methoxybenzoyl)-(R)-borolysine (+)-pinanediol, hydrochloride N.sup.1 -(2-methyl-4-phenyl-5-carboxamidobenzoyl)-(R)-borolysine (+)-pinanediol, hydrochloride N.sup.1 -(2-methyl-4-phenyl-5-fluorobenzoyl)-(R)-borolysine (+)-pinanediol, hydrochloride N.sup.1 -(2-methyl-4-phenyl-5-trifluoromethylbenzoyl)-(R)-borolysine (+)-pinanediol, hydrochloride N.sup.1 -(2-methyl-4-phenyl-5-chlorobenzoyl)-(R)-borolysine (+)-pinanediol, hydrochloride N.sup.1 -(2-methyl-4-phenyl-5-hydroxybenzoyl)-(R)-borolysine (+)-pinanediol, hydrochloride N.sup.1 -(2-methyl-4-�4-carboxy!phenyl-5-methoxybenzoyl)-(R)-borolysine (+)-pinanediol, hydrochloride N.sup.1 -(2-methyl-4-�4-carboxy!phenyl-5-carboxamidobenzoyl)-(R)-borolysine (+)-pinanediol, hydrochloride N.sup.1 -(2-methyl-4-�4-carboxy!phenyl-5-fluorobenzoyl)-(R)-borolysine (+)-pinanediol, hydrochloride N.sup.1 -(2-methyl-4-�4-carboxy!phenyl-5-trifluoromethylbenzoyl)-(R)-borolysine (+)-pinanediol, hydrochloride N.sup.1 -(2-methyl-4-�4-carboxy!phenyl-5-chlorobenzoyl)-(R)-borolysine (+)-pinanediol, hydrochloride N.sup.1 -(2-methyl-4-�4-carboxy!phenyl-5-hydroxybenzoyl)-(R)-borolysine (+)-pinanediol, hydrochloride N.sup.1 -(2-�5-phenyl!furylcarbonyl)-(R)-borolysine (+)-pinanediol, hydrochloride N.sup.1 -(2-�5-phenyl!thiophen-ylcarbonyl)-(R)-borolysine (+)-pinanediol, hydrochloride N.sup.1 -(2-benzopyronylcarbonyl)-(R)-borolysine (+)-pinanediol, hydrochloride N.sup.1 -(2-isoquinolinylcarbonyl)-(R)-borolysine (+)-pinanediol, hydrochloride N.sup.1 -(3-isoquinolinylcarbonyl)-(R)-borolysine (+)-pinanediol, hydrochloride N.sup.1 -(2-phenyl-4-isoquinolinylcarbonyl)-(R)-borolysine (+)-pinanediol, hydrochloride N.sup.1 -(4-phenylbenzoyl)-(R)-borolysine, hydrochloride N.sup.1 -(3-phenylbenzoyl)-(R)-borolysine, hydrochloride N.sup.1 -(3-phenoxybenzoyl)-(R)-borolysine, hydrochloride N.sup.1 -(4-�4-pyridyl!benzoyl)-(R)-borolysine, hydrochloride N.sup.1 -(2-benzoylbenzoyl)-(R)-borolysine, hydrochloride N.sup.1 -(3-benzoylbenzoyl)-(R)-borolysine, hydrochloride N.sup.1 -(4-benzoylbenzoyl)-(R)-borolysine, hydrochloride N.sup.1 -(3-�N-benzyloxycarbonyl!aminobenzoyl)-(R)-borolysine, hydrochloride N.sup.1 -(3-�N-benzyloxycarbonyl-N-methyl!aminobenzoyl)-(R)-borolysine, hydrochloride N.sup.1 -(4-ethylbenzoyl)-(R)-borolysine, hydrochloride N.sup.1 -(4-n-propylbenzoyl)-(R)-borolysine, hydrochloride N.sup.1 -(4-isopropylbenzoyl)-(R)-borolysine, hydrochloride N.sup.1 -(4-tert-butylbenzoyl)-(R)-borolysine, hydrochloride N.sup.1 -(4-n-hexylbenzoyl)-(R)-borolysine, hydrochloride N.sup.1 -(4-cyclohexylbenzoyl)-(R)-borolysine, hydrochloride N.sup.1 -(2-�N-(2-phenylethyl)carbonyl!aminobenzoyl)-(R)-borolysine, hydrochloride N.sup.1 -(4-n-butyloxybenzoyl)-(R)-borolysine, hydrochloride N.sup.1 -(4-�N-cyclopropylcarbonyl!aminobenzoyl)-(R)-borolysine, hydrochloride N.sup.1 -(4-�N-cyclohexylcarbonyl!aminobenzoyl)-(R)-borolysine, hydrochloride N.sup.1 -(4-�N-(4-methoxy)benzoyl!aminobenzoyl)-(R)-borolysine, hydrochloride N.sup.1 -(4-�4-methoxy!phenylbenzoyl)-(R)-borolysine, hydrochloride N.sup.1 -(2-�2-phenyl!benzyloxycarbonylbenzoyl)-(R)-borolysine, hydrochloride N.sup.1 -(2-�1-naphthyl!benzoyl)-(R)-borolysine, hydrochloride N.sup.1 -(4-�4-carboxy!phenylbenzoyl)-(R)-borolysine, hydrochloride N.sup.1 -(�2-anthraquinonyl!carbonyl)-(R)-borolysine, hydrochloride N.sup.1 -(�2-dioxothioxanthinonyl!carbonyl)-(R)-borolysine, hydrochloride N.sup.1 -(�2-fluoren-9-onyl!carbonyl)-(R)-borolysine, hydrochloride N.sup.1 -(�3-fluoren-9-onyl!carbonyl)-(R)-borolysine, hydrochloride N.sup.1 -(1-naphthoyl)-(R)-borolysine, hydrochloride N.sup.1 -(�4-fluoren-9-onyl!carbonyl)-(R)-borolysine, hydrochloride N.sup.1 -(2-methyl-4-phenyl-5-methoxybenzoyl)-(R)-borolysine, hydrochloride N.sup.1 -(2-methyl-4-phenyl-5-carboxamidobenzoyl)-(R)-borolysine, hydrochloride N.sup.1 -(2-methyl-4-phenyl-5-fluorobenzoyl)-(R)-borolysine, hydrochloride N.sup.1 -(2-methyl-4-phenyl-5-trifluoromethylbenzoyl)-(R)-borolysine, hydrochloride N.sup.1 -(2-methyl-4-phenyl-5-chlorobenzoyl)-(R)-borolysine, hydrochloride N.sup.1 -(2-methyl-4-phenyl-5-hydroxybenzoyl)-(R)-borolysine, hydrochloride N.sup.1 -(2-methyl-4-�4-carboxy!phenyl-5-methoxybenzoyl)-(R)-borolysine, hydrochloride N.sup.1 -(2-methyl-4-�4-carboxy!phenyl-5-carboxamidobenzoyl)-(R)-borolysine, hydrochloride N.sup.1 -(2-methyl-4-�4-carboxy!phenyl-5-fluorobenzoyl)-(R)-borolysine, hydrochloride N.sup.1 -(2-methyl-4-�4-carboxy!phenyl-5-trifluoromethylbenzoyl)-(R)-borolysine, hydrochloride N.sup.1 -(2-methyl-4-�4-carboxy!phenyl-5-chlorobenzoyl)-(R)-borolysine, hydrochloride N.sup.1 -(2-methyl-4-�4-carboxy!phenyl-5-hydroxybenzoyl)-(R)-borolysine, hydrochloride N.sup.1 -(2-�5-phenyl!furylcarbonyl)-(R)-borolysine, hydrochloride N.sup.1 -(2-�5-phenyl!thiophenylcarbonyl)-(R)-borolysine, hydrochloride N.sup.1 -(2-benzopyronylcarbonyl)-(R)-borolysine, hydrochloride N.sup.1 -(2-isoquinolinylcarbonyl)-(R)-borolysine, hydrochloride N.sup.1 -(3-isoquinolinylcarbonyl)-(R)-borolysine, hydrochloride N.sup.1 -(2-phenyl-4-isoquinolinylcarbonyl)-(R)-borolysine, hydrochloride N.sup.1 -(2-methyl-4-phenylbenzoyl-R-borolysine, hydrochloride N.sup.1 -(2-methyl-4-phenylbenzoyl-R-borolysine, (+)-pinanediol, hydrochloride N.sup.1 -(2-methyl-4-phenylbenzoyl-R-borothioarginine, hydrobromide N.sup.1 -(2-methyl-4-phenylbenzoyl-R-borothioarginine, (+)-pinanediol, hydrochloride N.sup.1 -(2-methyl-4-phenylbenzoyl-R-boroarginine, hydrochloride N.sup.1 -(2-methyl-4-phenylbenzoyl-R-boroarginine, (+)-pinanediol, bisulfite N.sup.1 -�4-phenyl-2-nitrobenzoyl!boroArg(Me), (+)-pinanediol ester N.sup.1 -�4-phenyl-2-fluorobenzoyl!boroArg(Me), (+)-pinanediol ester N.sup.1 -�4-phenyl-2-aminobenzoyl!boroArg(Me), (+)-pinanediol ester N.sup.1 -�4-phenyl-2-(methylsulfonamido)benzoyl!boroArg(Me), (+)-pinanediol ester N.sup.1 -�4-phenyl-2-(cyanomethylamino)benzoyl!boroArg(Me), (+)-pinanediol ester N.sup.1 -�4-phenyl-2-(cyanomethyl)benzoyl!boroArg(Me), (+)-pinanediol ester N.sup.1 -�4-phenyl-2-(diethylamino)benzoyl!boroArg(Me), (+)-pinanediol ester N.sup.1 -�4-�2-(t-butylaminosulfonyl)phenyl!-2-methyl-benzoyl!boroArg (Me), (+) pinanediol ester N.sup.1 -�(4-�2-(aminosulfonyl)phenyl!-2-methyl-benzoyl!boroArg (Me), (+) pinanediol ester N.sup.1 -�4-�2-(methoxycarbonylaminosulfonyl)phenyl!-2-methyl-benzoyl!boroArg(Me), (+)-pinanediol ester N.sup.1 -�4-�2-(t-butylaminosulfonyl)phenyl!benzoyl!boroArg(Me), (+)-pinanediol ester N.sup.1 -�4-�2-(t-butylaminosulfonyl)phenyl!benzoyl!boroArg(Me)--OH N.sup.1 -�4-�2-(n-butoxycarbonylaminosulfonyl)phenyl!-2-methyl-benzoyl!boroArg(Me), (+)-pinanediol ester N.sup.1 -�4-�2-(diethylaminosulfonyl)phenyl!-2-methyl-benzoyl!boroArg(Me), (+)pinanediol ester N.sup.1 -�4-�2-(t-butylaminosulfonyl)phenyl!-2-fluoro-benzoyl!boroArg(Me), (+)pinanediol ester N.sup.1 -�4-�2-(aminosulfonyl)phenyl!-2-fluoro-benzoyl!boroArg(Me), (+)pinanediol ester N.sup.1 -�4-�2-(methoxycarbonylaminosulfonyl)phenyl!-2-fluoro-benzoyl!boroArg(Me), (+)-pinanediol ester N.sup.1 -�4-�2-(t-butylaminosulfonyl)phenyl!-2-nitro-benzoyl!boroArg(Me), (+)pinanediol ester N.sup.1 -�4-�2-(aminosulfonyl)phenyl!-2-nitro-benzoyl!boroArg(Me), (+)pinanediol ester N.sup.1 -�4-�2-(methoxycarbonylaminosulfonyl)phenyl!-2-nitro-benzoyl!boroArg(Me), (+)-pinanediol ester N.sup.1 -�4-phenyl-2-nitrobenzoyl!boroMPG, (+)-pinanediol ester N.sup.1 -�4-phenyl-2-fluorobenzoyl!boroMPG, (+)-pinanediol ester N.sup.1 -�4-phenyl-2-aminobenzoyl!boroMPG, (+)-pinanediol ester N.sup.1 -�4-phenyl-2-(methylsulfonamido)benzoyl!boroMPG, pinanediol ester N.sup.1 -�4-phenyl-2-(cyanomethylamino)benzoyl!boroMPG, (+)-pinanediol ester N.sup.1 -�4-phenyl-2-(cyanomethyl)benzoyl!boroMPG, (+)-pinanediol ester N.sup.1 -�4-phenyl-2-(diethylamino)benzoyl!boroMPG, (+)-pinanediol ester N.sup.1 -�4-�2-(t-butylaminosulfonyl)phenyl!-2-methyl-benzoyl!boroMPG, (+)pinanediol ester N.sup.1 -�4-�2-(aminosulfonyl)phenyl!-2-methyl-benzoyl!boroMPG, (+)pinanediol ester N.sup.1 -�4-�2-(methoxycarbonylaminosulfonyl)phenyl!-2-methyl-benzoyl!boroMPG, (+)-pinanediol ester N.sup.1 -�4-�2-(t-butylaminosulfonyl)phenyl!benzoyl!boroMPG, (+)-pinanediol ester N.sup.1 -�4-�2-(t-butylaminosulfonyl)phenyl!benzoyl!boroMPG--OH N.sup.1 -�4-�2-(n-butoxycarbonylaminosulfonyl)phenyl!-2-methyl-benzoyl!boroMPG, (+)-pinanediol ester N.sup.1 -�4-�2-(diethylaminosulfonyl)phenyl!-2-methyl-benzoyl!boroMPG, (+)pinanediol ester N.sup.1 -�4-�2-(t-butylaminosulfonyl)phenyl!-2-fluoro-benzoyl!boroMPG, (+)pinanediol ester N.sup.1 -�4-�2-(aminosulfonyl)phenyl!-2-fluoro-benzoyl!boroMPG, (+)pinanediol ester N.sup.1 -�4-�2-(methoxycarbonylaminosulfonyl)phenyl!-2-fluoro-benzoyl!boroMPG, (+)-pinanediol ester N.sup.1 -�4-�2-(t-butylaminosulfonyl)phenyl!-2-nitro-benzoyl!boroMPG, (+)pinanediol ester N.sup.1 -�4-�2-(aminosulfonyl)phenyl!-2-nitro-benzoyl!boroMPG, (+)pinanediol ester N.sup.1 -�4-�2-(methoxycarbonylaminosulfonyl)phenyl!-2-nitro-benzoyl!boroMPG, (+)-pinanediol ester N.sup.1 -�4-phenyl-2-nitrobenzoyl!boroACA, (+)-pinanediol ester N.sup.1 -�4-phenyl-2-fluorobenzoyl!boroACA, (+)-pinanediol ester N.sup.1 -�4-phenyl-2-aminobenzoyl!boroACA, (+)-pinanediol ester N.sup.1 -�4-phenyl-2-(methylsulfonamido)benzoyl!boroACA, (+)-pinanediol ester N.sup.1 -�4-phenyl-2-(cyanomethylamino)benzoyl!boroACA, (+)-pinanediol ester N.sup.1 -�4-phenyl-2-(cyanomethyl)benzoyl!boroACA, (+)-pinanediol ester N.sup.1 -�4-phenyl-2-(diethylamino)benzoyl!boroACA, (+)-pinanediol ester N.sup.1 -�4-�2-(t-butylaminosulfonyl)phenyl!-2-methyl-benzoyl!boroACA, (+)pinanediol ester N.sup.1 -�4-�2-(aminosulfonyl)phenyl!-2-methyl-benzoyl!boroACA, (+)pinanediol ester N.sup.1 -�4-�2-(methoxycarbonylaminosulfonyl)phenyl!-2-methyl-benzoyl!boroACA, (+)-pinanediol ester N.sup.1 -�4-�2-(t-butylaminosulfonyl)phenyl!benzoyl!boroACA, (+)-pinanediol ester N.sup.1 -�4-�2-(t-butylaminosulfonyl)phenyl!benzoyl!boroACA-OH N.sup.1 -�4-�2-(n-butoxycarbonylaminosulfonyl)phenyl!-2-methyl-benzoyl!boroACA, (+)-pinanediol ester N.sup.1 -�4-�2-(diethylaminosulfonyl)phenyl!-2-methyl-benzoyl!boroACA, (+)pinanediol ester N.sup.1 -�4-�2-(t-butylaminosulfonyl)phenyl!-2-fluoro-benzoyl!boroACA, (+)pinanediol ester N.sup.1 -�4-�2-(aminosulfonyl)phenyl!-2-fluoro-benzoyl!boroACA, (+)pinanediol ester N.sup.1 -�4-�2-(methoxycarbonylaminosulfonyl)Phenyl!.sup.- 2-fluoro-benzoyl!boroACA, (+)-pinanediol ester N.sup.1 -�4-�2-(t-butylaminosulfonyl)phenyl!-2-nitro-benzoyl!boroACA, (+)pinanediol ester N.sup.1 -�4-�2-(aminosulfonyl)phenyl!-2-nitro-benzoyl!boroACA, (+)pinanediol ester N.sup.1 -�4-�2-(methoxycarbonylaminosulfonyl)phenyl!-2-nitro-benzoyl!boroACA, (+)-pinanediol ester N.sup.1 -�4-phenyl-2-nitrobenzoyl!boroLys, (+)-pinanediol ester N.sup.1 -�4-phenyl-2-fluorobenzoyl!boroLys, (+)-pinanediol ester N.sup.1 -�4-phenyl-2-aminobenzoyl!boroLys, (+)-pinanediol ester N.sup.1 -�4-phenyl-2-(methylsulfonamido)benzoyl!boroLys, (+)-pinanediol ester N.sup.1 -�4-phenyl-2-(cyanomethylamino)benzoyl!boroLys, (+)-pinanediol ester N.sup.1 -�4-phenyl-2-(cyanomethyl)benzoyl!boroLys, (+)-pinanediol ester N.sup.1 -�4-phenyl-2-(diethylamino)benzoyl!boroLys, (+)-pinanediol ester N.sup.1 -�4-�2-(t-butylaminosulfonyl)phenyl!-2-methyl-benzoyl!boroLys, (+)pinanediol ester N.sup.1 -�4-�2-(aminosulfonyl)phenyl!-2-methyl-benzoyl!boroLys, (+)pinanediol ester N.sup.1 -�4-�2-(methoxycabonylaminosulfonyl)phenyl!-2-methyl-benzoyl!boroLys, (+)-pinanediol ester N.sup.1 -�4-�2-(t-butylaminosulfonyl)phenyl!benzoyl!boroLys, (+)-pinanediol ester N.sup.1 -�4-�2-(t-butylaminosulfonyl)phenyl!benzoyl!boroLys--OH N.sup.1 -�4-�2-(n-butoxycarbonylaminosulfonyl)phenyl!-2-methyl-benzoyl!boroLys, (+)-pinanediol ester N.sup.1 -�4-�2-(diethylaminosulfonyl)phenyl!-2-methyl-benzoyl!boroLys, (+)pinanediol ester N.sup.1 -�4-�2-(t-butylaminosulfonyl)phenyl!-2-fluoro-benzoyl!boroLys, (+)pinanediol ester N.sup.1 -�4-�2-(aminosulfonyl)phenyl!-2-fluoro-benzoyl!boroLys, (+)pinanediol ester N.sup.1 -�4-�2-(methoxycarbonylaminosulfonyl)phenyl!-2-fluoro-benzoyl!boroLys, (+)-pinanediol ester N.sup.1 -�4-�2-(t-butylaminosulfonyl)phenyl!-2-nitro-benzoyl!boroLys, (+)pinanediol ester N.sup.1 -�4-�2-(aminosulfonyl)phenyl!-2-nitro-benzoyl!boroLys, (+)pinanediol ester N.sup.1 -�4-�2-(methoxyaminosulfonyl)phenyl!-2-nitro-benzoyl!boroLys, (+)-pinanediol ester.

DETAILED DESCRIPTION OF THE INVENTION

Throughout the specification, the following conventional three-letter abbreviations for amino acid residues or amino acids apply:

Ala=alanine Arg=arginine Asn=asparagine Asp=aspartic acid Cys=cysteine Gln=glutamine Glu=glutamic acid Gly=glycine His=histidine Ile=isoleucine Leu=leucine Lys=lysine Met=methionine Phe=phenylalanine Pro=proline Ser=serine Thr=threonine Trp=tryptophan Tyr=tyrosine Val=valine Irg=arginine where the guanidine is replaced with an isothiouronium (--SC(.dbd.NH)NH.sub.2) Arg(Me)=arginine with the guanidino group methylated MPG=5-methoxy-propylglycine ACA=3-(4-amino)cyclohexylalanine

The prefix "boro" indicates amino acid residues where the carboxy group is replaced by a boronic acid (Formula I, Y.sup.1 and Y.sup.2 =--OH).

The pinanediol boronic acid ester and the pinacol boronic acid ester are abbreviated "-C.sub.10 H.sub.16 -" and -C.sub.6 H.sub.12 -" respectively. Other illustrations of diols useful for deriving a boronic acid orthoesters are 1,2-ethanediol, 1,3-propanediol, 1,2-propanediol, 2,3-butanediol, 1,2-diisopropylethanediol, 5,6-decanediol, 1,2-dicyclohexylethanediol.

The formamidino modified amino group is abbreviated (CH.dbd.NH). For example, the formamidino analog of -boroOrn--OH {--NH--CH�(CH.sub.2).sub.3 --NH--CH(NH)H!B(OH).sub.2 } is -boroOrn(CH.dbd.NH)--OH. Analogs containing sidechain substituents are described by indicating the substituent in parenthesis following the name of the parent residue. For example the analog of boroPhenylalanine containing a meta cyano group is -boroPhe(mCN)-. N-alkyl substituents on the guanidino group of boroArg- or on the isothiouronium analogs (boroIrg) are also put in parenthesis in a similar manner.

Other abbreviations are: Z, benzyloxycarbonyl; BSA, benzene sulfonic acid; THF, tetrahydrofuran; Boc-, g-butoxycarbonyl-; Ac-, acetyl; pNA, p-nitro-aniline; DMAP, 4-N,N-dimethylaminopyridine; Tris, Tris(hydroxymethyl)aminomethane; MS, mass spectrometry; FAB/MS, fast atom bombardment mass spectrometry. LRMS(NH.sub.3 --CI) and HRMS(NH.sub.3 --CI) are low and high resolution mass spectrometry, respectively, using NH.sub.3 as an ion source

As used herein, the structure ##STR30## wherein J is N or C and K, L, M and Q are independently selected at each occurrence from the group consisting of N, CR.sup.13, S or O, provided that:

i) there may be only one S or O present in the ring at a time; ii) there may only be 1-2N present when there is an O or S present; iii) there may be only 1-4N present; is used as a substituent definition for R.sup.1. This substituent may be exemplified by the following structures where --J--K--L--M--Q-- is: 1) --N--C(R.sup.13).dbd.C(R.sup.13)--C(R.sup.13).dbd.C(R.sup.13)--, 2) --N--C(R.sup.13).dbd.C(R.sup.13)--C(R.sup.13).dbd.N--, 3) --N--C(R.sup.13).dbd.C(R.sup.13)--N.dbd.C(R.sup.13)--, 4) --N--C(R.sup.13).dbd.N--C(R.sup.13).dbd.N--, 5) --N--C(R.sup.13).dbd.C(R.sup.13)--N.dbd.N-- 6) --N--C(R.sup.13).dbd.N--N.dbd.N--, 7) --N--N.dbd.C(R.sup.13)--N.dbd.N--, 8) .dbd.C--O--C(R.sup.13).dbd.N--C(R.sup.13).dbd., 9) --C.dbd.C(R.sup.13)--O--C(R.sup.13).dbd.N--, 10) .dbd.C--O--C(R.sup.13).dbd.C(R.sup.13)--N.dbd., 11) --C.dbd.C(R.sup.13)--C(R.sup.13).dbd.N--O--, 12) .dbd.C--C(R.sup.13).dbd.C(R.sup.13)--O--N.dbd., 13) --C.dbd.C(R.sup.13)--O--N.dbd.C(R.sup.13)--, 14) .dbd.C--S--C(R.sup.13).dbd.N--C(R.sup.13).dbd., 15) --C.dbd.C(R.sup.13)--S--C(R.sup.13).dbd.N--, 16) .dbd.C--S--C(R.sup.13).dbd.C(R.sup.13)--N.dbd., 17) --C.dbd.N--S--N.dbd.C(R.sup.13)--, 18) --C.dbd.N--S--C(R.sup.13).dbd.N--, 19) .dbd.C--S--N.dbd.C(R.sup.13)--N.dbd., 20) .dbd.C--S--C(R.sup.13).dbd.C(R.sup.13)--C(R.sup.13).dbd., 21) --C.dbd.C(R.sup.13)--S--C(R.sup.13).dbd.C(R.sup.13)--, 22) .dbd.C--O--C(R.sup.13).dbd.C(R.sup.13)--C(R.sup.13).dbd., or 23) --C.dbd.C(R.sup.13)--O--C(R.sup.13).dbd.C(R.sup.13)--.

As used herein, the structure ##STR31## wherein in W, R, T, U and V are independently selected at each occurrence from the group consiting of: CR.sup.13 or N, provided that there may be only 1-3N present, is used as a substituent definition for R.sup.1. This substituent may be exemplified by the following structures where --C--W--R--T--U--V-- is:

1) --C.dbd.N--C(R.sup.13).dbd.C(R.sup.13)--C(R.sup.13).dbd.C(R.sup.13)--, 2) --C.dbd.C(R.sup.13)--N.dbd.C(R.sup.13)--C(R.sup.13).dbd.C(R.sup.13)--, 3) --C.dbd.C(R.sup.13)--C(R.sup.13).dbd.N--C(R.sup.13).dbd.C(R.sup.13)--, 4) --C.dbd.N--N.dbd.C(R.sup.13)--C(R.sup.13).dbd.C(R.sup.13)--, 5) --C.dbd.C(R.sup.13)--N.dbd.N--C(R.sup.13).dbd.C(R.sup.13)--, 6) --C.dbd.N--C(R.sup.13).dbd.C(R.sup.13)--C(R.sup.13).dbd.N--, 7) --C.dbd.N--C(R.sup.13).dbd.C(R.sup.13)--N.dbd.C(R.sup.13)--, 8) --C.dbd.N--C(R.sup.13).dbd.N--C(R.sup.13).dbd.C(R.sup.13)--, 9) --C.dbd.C(R.sup.13)--N.dbd.C(R.sup.13)--N.dbd.C(R.sup.13)--, 10) --C.dbd.N--C(R.sup.13).dbd.N--N.dbd.C(R.sup.13)--, 11) --C.dbd.N--C(R.sup.13).dbd.C(R.sup.13)--N.dbd.N--, or 12) --C.dbd.C(R.sup.13)--N.dbd.C(R.sup.13)--N.dbd.N--.

"Amino acid residues" as used herein, refers to natural or unnatural amino acids of either D- or L-configuration. Natural amino acids residues are Ala, Arg, Asn, Asp, Aze, Cys, Gln, Glu, Gly, His, Ile, Irg Leu, Lys, Met, Orn, Phe, Phe(4-fluoro), Pro, Sar, Ser, Thr, Trp, Tyr, and Val. Roberts and Vellaccio, The Peptides, Vol 5; 341-449 (1983), Academic Press, New York, discloses numerous suitable unnatural amino acids and is incorporated herein by reference for that purpose.

"Amino acids residues" also refers to various amino acids where sidechain functional groups are coupled with appropriate protecting groups known to those skilled in the art. "The Peptides", Vol 3, 3-88 (1981) discloses numerous suitable protecting groups and is incorporated herein by reference for that purpose.

The reactions of the synthetic methods claimed herein are carried out in suitable solvents which may be readily selected by one of skill in the art of organic synthesis, said suitable solvents generally being any solvent which is substantially nonreactive with the starting materials (reactants), the intermediates, or products at the temperatures at which the reactions are carried out, i.e., temperatures which may range from the solvent's freezing temperature to the solvent's boiling temperature. A given reaction may be carried out in one solvent or a mixture of more than one solvent. Depending on the particular reaction step, suitable solvents for a particular reaction step may be selected.

The compounds herein described may have asymmetric centers. 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 certain compounds of the present invention contain an asymmetrically substituted carbon atom, and 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. Also, it is realized that cis and trans geometric isomers of the compounds of the present invention are described and may be isolated as a mixture of isomers or as separated isomeric forms. 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, R.sup.1 through R.sup.20, R.sup.20a, m, n, D, E, F, W, X, etc.) occurs more than one time in any constituent or in Formula (I), 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.11, then said group may optionally be substituted with up to three R.sup.11 and R.sup.11 at each occurrence is selected independently from the defined list of possible R.sup.11. Also, for example, in -N(R.sup.15).sub.2, each of the R.sup.15 substituents may be independently selected from the list of possible R.sup.20 groups defined. Also, combinations of substituents and/or variables are permissible only if such combinations result in stable compounds. Similarly, by way of example, for the group --C(R.sup.11).sub.2 --, each of the two R.sup.11 substituents on C is independently selected from the defined list of possible R.sup.11.

As used herein, "alkyl" is intended to include both branched and straight-chain saturated aliphatic hydrocarbon groups having the specified number of carbon atoms; "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, adamantyl and cyclooctyl; 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.

"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. By way of examples: the term "C.sub.7 -C.sub.10 arylalkyl" is intended to refer to an aryl group attached through a C.sub.1 -C.sub.4 alkyl bridge to the residue of the indicated compound; the term "(C.sub.1 -C.sub.3 alkyl)aryl" is intended to refer to a C.sub.1 -C.sub.3 alkyl group which is attached through an aryl ring to the residue of the indicated compound; the term "aryl(C.sub.1 -C.sub.3 alkyl)" is intended to refer to an aryl group attached through a C.sub.1 -C.sub.3 alkyl group to the residue of the indicated compound.

As used herein, "carbocycle" or "carbocyclic residue" is intended to mean any stable 3- to 8-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" is intended to mean a stable 5- to 7-membered monocyclic or bicyclic or 7- to 10-membered bicyclic heterocyclic ring which is saturated and 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 term "heteroaryl" is intended to mean an aromatic form of a heterocyclic ring. Unless otherwise specified, the heterocyclic and heteroaryl rings described herein may be substituted on carbon or on a nitrogen atom if the resulting compound is stable. Unless otherwise specified, examples of such heterocycles include, but are not limited to, pyridinyl, pyrimidinyl, furanyl, thienyl, pyrrolyl, pyrazolyl, imidazolyl, tetrazolyl, benzofuranyl, benzothiophenyl, indolyl, indolenyl, 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, thiophenyl, thianthrenyl, pyranyl, isobenzofuranyl, chromenyl, xanthenyl, phenoxathiinyl, 2H-pyrrolyl, isothiazolyl, isoxazolyl, pyrazinyl, pyridazinyl, indolizinyl, isoindolyl, 3H-indolyl, 1H-indazolyl, purinyl, 4H-quinolizinyl, phthalazinyl, naphthyridinyl, quinoxalinyl, quinazolinyl, cinnolinyl, pteridinyl, 4aH-carbazolyl, carbazolyl, .beta.-carbolinyl, phenanthridinyl, acridinyl, perimidinyl, phenanthrolinyl, phenazinyl, phenarsazinyl, phenothiazinyl, furazanyl, phenoxazinyl, isochromanyl, chromanyl, imidazolidinyl, imidazolinyl, pyrazolidinyl, pyrazolinyl, piperazinyl, indolinyl, isoindolinyl, quinuclidinyl, morpholinyl, oxazolidinyl, benzotriazolyl, benzisoxazolyl, oxindolyl, benzoxazolinyl, or isatinoyl. Also included are fused ring and spiro compounds containing, for example, the above heterocycles.

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 substituent is listed without indicating the atom via which such substituent is bonded to the rest of the compound of formula I, 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 (I) 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 an 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, the term "any group that, when administered to a mammalian subject, cleaves to form a free hydroxyl, amino or sulfhydryl" means any group bonded to an O, N, or S atom, respectively, which is cleaved from the O, N, or S atom when the compound is administered to a mammalian subject to provide a compound having a remaining free hydroxyl, amino, or sulfhydryl group, respectively. Examples of groups that, when administered to a mammalian subject, are cleaved to form a free hydroxyl, amino or sulfhydryl, include but are not limited to, phosphate esters, C.sub.1 -C.sub.6 alkyl substituted with 0-3 R.sup.11, C.sub.3 -C.sub.6 alkoxyalkyl substituted with 0-3 R.sup.11, C.sub.1 -C.sub.6 alkylcarbonyl substituted with 0-3 R.sup.11, C.sub.1 -C.sub.6 alkoxycarbonyl substituted with 0-3 R.sup.11, C.sub.1 -C.sub.6 alkylaminocarbonyl substituted with 0-3 R.sup.11, benzoyl substituted with 0-3 R.sup.12, phenoxycarbonyl substituted with 0-3 R.sup.12, phenylaminocarbonyl substituted with 0-3 R.sup.12, or heteroarylcarbonyl. Examples of groups that, when administered to a mammalian subject, are cleaved to form a free hydroxyl, amino or sulfhydryl, may include hydroxy, amine or sulfhydryl protecting groups, respectively.

As used herein, the term "amine protecting group" means any group known in the art of organic synthesis for the protection of amine groups. Such amine protecting groups include those listed in Greene and Wuts, "Protective Groups in Organic Synthesis" John Wiley & Sons, New York (1991) and "The Peptides: Analysis, Synthesis, Biology, Vol. 3, Academic Press, New York (1981), the disclosure of which is hereby incorporated by reference. Any amine protecting group known in the art can be used. Examples of amine protecting groups include, but are not limited to, the following: 1) acyl types such as formyl, trifluoroacetyl, phthalyl, and p-toluenesulfonyl; 2) aromatic carbamate types such as benzyloxycarbonyl (Cbz) and substituted benzyloxycarbonyls, 1-(p-biphenyl)-1-methylethoxycarbonyl, and 9-fluorenylmethoxycarbonyl (Fmoc); 3) aliphatic carbamate types such as tertbutyloxycarbonyl (Boc), ethoxycarbonyl, diisopropylmethoxycarbonyl, and allyloxycarbonyl; 4) cyclic alkyl carbamate types such as cyclopentyloxycarbonyl and adamantyloxycarbonyl; 5) alkyl types such as triphenylmethyl and benzyl; 6) trialkylsilane such as trimethylsilane; and 7) thiol containing types such as phenylthiocarbonyl and dithiasuccinoyl.

The term "amino acid" as used herein means an organic compound containing both a basic amino group and an acidic carboxyl group. Included within this term are natural amino acids, modified and unusual amino acids, as well as amino acids which are known to occur biologically in free or combined form but usually do not occur in proteins. Included within this term are modified and unusual amino acids,such as those disclosed in, for example, Roberts and Vellaccio (1983) The Peptides, 5: 342-429, the teaching of which is hereby incorporated by reference. Modified or unusual amino acids which can be used to practice the invention include, but are not limited to, D-amino acids, hydroxylysine, 4-hydroxyproline, an N--Cbz-protected amino acid, ornithine, 2,4-diaminobutyric acid, homoarginine, norleucine, N-methylaminobutyric acid, naphthylalanine, phenylglycine, .beta.-phenylproline, tert-leucine, 4-aminocyclohexylalanine, N-methyl-norleucine, 3,4-dehydroproline, N,N-dimethylaminoglycine, N-methylaminoglycine, 4-aminopiperidine-4-carboxylic acid, 6-aminocaproic acid, trans-4-(aminomethyl)-cyclohexanecarboxylic acid, 2-, 3-, and 4-(aminomethyl)-benzoic acid, 1-aminocyclopentanecarboxylic acid, 1-aminocyclopropanecarboxylic acid, and 2-benzyl-5-aminopentanoic acid.

The term "peptide" as used herein means a compound that consists of two or more amino acids (as defined herein) that are linked by means of a peptide bond. The term "peptide" also includes compounds containing both peptide and non-peptide components, such as pseudopeptide or peptide mimetic residues or other non-amino acid components. Such a compound containing both peptide and non-peptide components may also be referred to as a "peptide analog".

The term "peptide bond" means a covalent amide linkage formed by loss of a molecule of water between the carboxyl group of one amino acid and the amino group of a second amino acid.

As used herein, "pharmaceutically acceptable salts" refer to derivatives of the disclosed compounds wherein the parent compound of formula (I) is modified by making acid or base salts of the compound of formula (I). 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 (I) in vivo when such prodrug is administered to a mammalian subject. Prodrugs of the compounds of formula (I) 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 (I) wherein hydroxy, amine, or sulfhydryl groups are bonded to any group that, when administered to a mammalian subject, cleaves to form a free hydroxyl, amino, or sulfhydryl group, respectively. Examples of prodrugs include, but are not limited to, acetate, formate, or benzoate derivatives of alcohol and amine functional groups in the compounds of formula (I); phosphate esters, dimethylglycine esters, aminoalkylbenzyl esters, aminoalkyl esters and carboxyalkyl esters of alcohol and phenol functional groups in the compounds of formula (I); and the like.

The pharmaceutically acceptable salts of the compounds of formula (I) include the conventional non-toxic salts or the quaternary ammonium salts of the compounds of formula (I) 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, ethane disulfonic, oxalic, isethionic, and the like.

The pharmaceutically acceptable salts of the present invention can be synthesized from the compounds of formula (I) which contain a basic or acidic moiety by conventional chemical methods. Generally, such salts can be prepared by reacting the free acid or base form of these compounds with a stoichiometric amount of the appropriate base or acid in water or in an organic solvent, or in a mixture of the two; generally, nonaqueous media like ether, ethyl acetate, ethanol, isopropanol, or acetonitrile are preferred. Lists of suitable salts are found in water or in an organic nonaqueous media like ether, ethyl acetate, 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 formula (I) can be prepared using the reactions and techniques described below. The reactions are performed in a solvent appropriate to the reagents and materials employed and suitable for the transformations being affected. It will be understood by those skilled in the art of organic synthesis that the functionality present on the molecule should be consistent with the chemical transformations proposed and this will sometimes require judgment as to the order of synthetic steps or selection of particular process scheme used from that shown below in order to obtain a desired compound of the invention. ##STR32##

Amine hydrochloride 1 is readily available via the procedure of Kettner and Shenvi (EP 0293881 A2).

There are numerous synthetic methods by which to prepare amide 2, however, competing with amide formation is the cyclization of 1 to afford a complex mixture containing the desired amide and the corresponding N-acylboroproline. Since purification at this stage is unfeasible, choosing the correct method for amide formation is crucial to obtaining 2 in a purity suitable for subsequent synthetic transformations.

Three methods are preferred for the preparation of 2. In the first, a solution of 1 in tetrahydrofuran or dichloromethane at 0.degree. C. is treated sequentially with the desired acid chloride followed by two equivalents of triethylamine. The mixture is then allowed to warm to room temperature overnight. The second method is the mixed anhydride procedure of Anderson, et. al. (J. Am Chem. Soc. 1967, 89, 5012). In this method the isobutyl mixed anhydride is generated by dissolving the carboxylic acid component in tetrahydrofuran and adding one equivalent of N-methylmorpholine. The solution is cooled to 0.degree. C. and one equivalent of isobutyl chloroformate is added. After 5 minutes, a solution of 1 in chloroform is added, followed by the addition of one equivalent of triethylamine. The mixture is typically stirred at 0.degree. C. for one hour followed by one to several hours at room temperature. The third method for amide formation is the hydroxybenzotriazole/DCC method of Konig and Geiger (Chem. Ber. 1970, 103, 788-98). Thus, to a solution of 1 and the carboxylic acid component in dimethylformamide or tetrahydrofuran at 0.degree. C. is added N-methylmorpholine, 1-hydroxybenzotriazole hydrate (2 eq) and DCC (1.05 eq). The solution is allowed to warm to room temperature overnight.

The preferred method for the preparation of azide 3 is by reaction of 2 with sodium azide (1.1 eq) in dimethylformamide at 70.degree. C. for 2 hours.

The azide displacement may also be performed prior to amide formation. This is the preferred method in cases where the rate of amide formation is slow relative to the rate of cyclization. Azide 4 is prepared by a modification of the procedure of Kettner and Shenvi (EP 0293881 A2) as shown in Scheme 2. Thus, bromide 5 is reacted with sodium azide, followed by homologation to give 6, chloride displacement to afford 7 and acidic hydrolysis to give 4. Amide formation between 4 and the carboxylic acid component then affords 3 directly. ##STR33##

Reduction of azide 3 to amine 8 may be accomplished by hydrogenation over precious metal catalysts. The preferred catalyst for this transformation is Pearlman's catalyst (palladium hydroxide on carbon). The amine is typically isolated as the hydrochloride salt. Isolation of 8 as the free base typically results in lowered yields. Salts of 8 which may confer superior physical properties may be preferred over the hydrochloride salt.

Formamidination of amine 8 may be accomplished using cyanamide. Due to the low reactivity of amine 8, however, the preferred method for this transformation is reaction with 4-dimethylamin-opyridine (DMAP) and aminoiminomethanesulfonic acid (AMSA, prepared by the method of Kim, et. al., Tetrahedron Lett. 1988, 29, 3183-6). This affords guanidine 9, which is isolated as the bisulfite or hydrochloride salt.

Cleavage of pinanediol ester 9 may be accomplished using anhydrous boron trichloride according to the procedure of Matteson and Ray (J. Am. Chem. Soc. 1980, 102, 7588). This method, however, is strongly Lewis acidic and leads to partial destruction of the substrate. The preferred method for water soluble boronic acids is a transesterification reaction that is run in the presence of excess phenylboronic acid. The free boronic acid 10 may then be isolated using cation exchange chromatography.

The isothiouronium functionalized analogs 11/12 are prepared from bromide 2 according to the procedure of Kettner and Shenvi (EP 0293881 A2).

Inhibitors containing a sulfonamide in place of a carboxamide are prepared from either 1 or 4 by reaction with a sulfonyl chloride in the presence of a hindered amine (Scheme 3). The product sulfonamide 13 is then converted to the guanidinium 14 or isothiouronium 15 in the same manner as the corresponding carboxamides. ##STR34##

Inhibitors containing the borolysine moiety are prepared analogously to those containing boroarginine according to Kettner and Shenvi (EP 0293881 A2).

Novel biaryls synthesized in this invention are prepared through palladium catalyzed coupling of an appropriate arylmetal species to the aryl halide of choice using the methods described in Negishi, et. al., Org. Synth. 1987, 66, 67-74, and references cited within.

Synthetic approaches toward construction of pyrroles are numerous: R. J. Sundberg in "Comprehensive Heterocyclic Chemistry", A. R. Katritzky (Ed.), Pergamon Press, New York (1984), Vol. 4, p. 705; Synthesis, 1946, 281. The following discussion is restricted to the most common and reliable methods towards the synthesis of pyrroles within the general scope of the invention.

Compounds where R.sup.1 is a pyrrole can be synthesized as shown on Scheme 4. ##STR35##

Starting material diketone 16 may or may not have its substituents R.sup.13-16 in final form as defined in the scope. These substituents might be in protected forms or in the form of suitable precursors which make the heterocyclic portion, for example, amenable to synthesis. These precursor forms can then be converted to their final forms later on in the synthesis using procedures familiar to one skilled in the art.

The cyclization condensation of 1,4-dicarbonyl compounds with ammonia, primary amines or related compounds, the Paal-Knorr reaction, is one of the most general and widely applicable pyrrole syntheses, R. A. Jones and G. P. Bean, "The Chemistry of Pyrroles", Academic Press, London, 1977; p. 77-81. The generality of this approach is primarily determined by the availability of the dicarbonyl precursors, 16, as illustrated by Scheme 4. By heating such diketones with ammonia or amines in a solvent like benzene, toluene or methylene chloride with a catalyst such as sulfuric acid, acetic acid, p-toluenesulfonic acid, alumina or even titanium tetrachloride, pyrroles like 17 may be prepared.

Subsequent alkylation of pyrrole 17 with a bromoester, for example, leads to the alkylated heterocycle 18. Alkylation conditions include either first deprotonating with NaH or KH in DMF followed by addition of the alkylating agent or simply stirring the heterocycle with the alkylaning agent in an inert solvent such as DMF or DMSO at 0.degree. C. to 100.degree. C. in the presence of an acid scavenger such as K.sub.2 CO.sub.3.

Saponification of ester 18 followed by coupling aminoboronic ester 1 or 19 as discussed previously yields compound 20. This bromide may be either elaborated to the lysine side-chain 21 (X=1) or if X=0, into the corresponding ornithine side-chain or any other side-chain discussed previously. Subsequent hydrolysis of the boronic ester yields the boronic acid as discussed previously too.

The cyclization of diynes 23 with amines has been reported and an adaptation of this method is shown in Scheme 5 (K. E. Schulte et al., Chem. Ber (1965) 98; A. J. Chalk Tet. Lett. (1972).sub.3487). The diynes are made via transition metal catalyzed coupling of alkynes, i.e., the Cadio-Chodkiewicz reaction (W. Chodkiewicz Ann. Chim. (Paris) (1957)2 81g). ##STR36##

Furans (27) have been converted directly to pyrroles by treatment with amines but the harsh conditions required (400.degree. C./Al.sub.2 O.sub.3) precludes its generality. 2,5-Dialkoxytetrahydrofurans (29) have been more commonly employed as furan (or 1,4-dicarbonyl) equivalents and react readily with aliphatic or aromatic amines (and even weakly nucleophilic sulfonamides) to give pyrroles as shown in Scheme 6 , J. W. F. Wasley and K. Chan, Synth. Commun. 3, 303 (1973). Although commercially available 2,5-dialkoxytetrahydrofurans (29) (R.sup.1 =R.sup.2 =H))generally restrict one to preparing 1-substituted pyrroles, more highly substituted systems may be obtained by a three-step alcoholysis of the appropriate furans (27) to the more highly substituted 2,5-dialkoxytetrahydrofurans (29) as shown in Scheme 6, N. L. Weinberg and H. R. Weinberg, Chem. Rev., 68, 449 (1968); N. Elming, Adv. Org. chem., 2, 67 (1960).

The Hantzsch synthesis utilizes the condensation of .beta.-haloketones (30a) and .beta.-ketoesters (31) in the presence of ammonia or a primary amine to give pyrroles such as (32), as shown in Scheme 7, A. Hantzsch, Chem. Ber., 23, 1474 (1980); D. C. von Beelen, J. Walters, and S. von der Gen, Rec Trav. Chem. 98, 437 (1979). Among the numerous modifications reported over the years, the substitution of (30a) with the readily available .alpha.-hydroxyaldehydes or nitroalkenes has expanded the versatility and generality of this important method, D. M. McKinnon, Can. J. Chem. 43, 2628 (1965); H. George and H. J. Roth, Arch. Pharm. 307, 699 (1974); C. A. Grok and K. Camenisch, Helv. Chem. Acta, 36, 49 (1953). ##STR37##

The closely related Knorr condensation involves the reaction between amino carbonyl compounds (or their precursors) and carbonyl (or dicarbonyl) compounds, J. M. Patterson, Synthesis, 282 (1976). Representative methods for preparing substituted pyrroles (35 and 38) are shown by Scheme 8, equations a) and b), S. Umio et al., Jap. Pat. 7018653, Fujisawa Pharmaceutical Co., Ltd., 1970 (C.A. 73, 77039, 1970); K. Tanaka, K. Kariyone, S. Umio, Chem. Phram. Bull (Tokyo)), 17, 611 (1969).

The elaboration of an appropriately functionalized pyrrole is another method for preparing pyrroles of general formula I. Methyl (or ethyl) 5-formyl-1H-pyrrole-2-carboxylate (43) is a particularly useful intermediate with regards to pyrroles claimed in this invention and has been prepared by a number of methods as shown by Scheme 9, eq. a, W. A. Davies, A. R. Pinder and I. G. Morris, Tetrahedron 18, 405 (1962); Org Syn., vol 36, p. 74; Org. Syn., vol. 51.

More recently, Ullrich has extended the Vilsmeyer-Haack formylation of pyrroles to include vinylogous systems such as (46) by using the 3-(N,N-dimethylformamide derivative, as shown by Scheme 9, eq. b, F. W. Ullrich and E. Breitmaier, Synthesis, 641 (1983); W. Heinz, et al., Tetrahedron, 42, 3753 (1986).

An especially attractive approach to pyrroles claimed in this invention has recently been reported, whereby lithiation of the 6-dimethylamino-1-azafulvene dimer (49) followed by treatment with an appropriate electrophile and subsequent hydrolysis leads to 5-substituted pyrrole-2-carboxaldehydes (51), as illustrated in Scheme 10, J. M. Muchowski and P. Hess, Tetrahedron Lett, 29, 777 (1988). The carboxylic acid, ester and aldehyde side-chains depicted in Schemes 9-10 can be readily converted to R.sup.13-16 by methods familiar to one skilled in the art. ##STR38##

A general and versatile approach to pyrazoles (R.sup.1 =pyrazole) involves condensation of a 1,3-difunctional compound (usually dicarbonyl) with hydrazine or its derivatives, as shown in Scheme 11 for pyrazoles of the formula 53 and reviewed by G. Corspeau and J. Elguerv, Bull. Soc. Chim. Fr., 2717 (1970). Rarely have pyrazoles have been prepared in which the N--N bond is the last step of the ring closure, J. Elguerv in Comprehensive Heterocyclic Chemistry, S. R. Katritzky (Ed.) Pergamon Press, New York, Vol. 5 (1984), p. 274; J. Barluenga, J. Chem. Soc, Perkin Trans.1, 2275 (1983). ##STR39##

The condensation of 1,3-dicarbonyl compounds with hydrazine hydrate derivatives is generally carried out by admixture of the two components in a suitable solvent like a lower alcohol, ether, or THF at 0.degree. C. to the reflux temperature for 1-18 hours.

The synthesis of 1,3-dicarbonyl compounds has received considerable attention in the literature and most of the major approaches towards 1,3-diketones 52 of interest in this invention are illustrated by Scheme 12. ##STR40##

Esters 54a can be reacted with ketones 54 using bases like sodium ethoxide, sodium hydride or sodium amide in a suitable solvent like alcohol, DMF, DMSO or benzene at 0.degree. C. to reflux for 4-18 hours with 30-70% efficiency, J. M. Sprague, Lo J. Beckham and H. Adkins, J. Amer. Chem. Soc., 56, 2665 (1934). Metallation of hydrazines 55with n-BuLi followed by reaction with carboxylic acid chlorides and subsequent hydrolysis affords 52, D. Enders and P. Wenster, Tetrahedron Lett., 2853 (1978). Metallation of 54 with the non-nucleophilic mesityl lithium followed by acylation also affords 52, A. K. Beck, M. S. Hoelstein and D. Seebach, Tetrahedron Lett., 1187 (1977); D. Seebach, Tetrahedron Lett., 4839; (1976).

As shown in Scheme 12, equation b, the addition of Grignard reagents to .beta.-keto carboxylic acid chlorides may be limited to monoaddition at low temperatures to provide 52, C. D. Hurd and G. D. Kelso, J. Amer. Amer. Soc. 62, 1548 (1940); F .Sato, M. Trone, K. Oyuro, and M. Sato, Tetrahedron Lett. 4303 (1979). Lithium dialkyl copper reagents (R.sup.2 CuLi) have also been used, Luong-Thi and Riviero, J. Organomet. Chem. 77, C52 (1974). Analogously, addition of alkyllithium reagents (R.sup.15 Li) to the monoanions of .beta.-keto esters 57 also give rise to 1,3-diketones, S. N. Huckin and L. Weiler, Can. J. Chem. 52, 1379 (1974).

Eschenmoser has demonstrated a synthesis of .beta.-diketones through a sulfur extrusion reaction of keto thioesters 58 with tributylphosphine, triethylamine and lithium perchlorate, S. Eshenmoser, Helv. Chim. Acta., 54, 710 (1971).

The rearrangement of .alpha.,.beta.-epoxy ketones 59 to .beta.-diketones 52 catalyzed by Pd.degree. has been reported, R. Noyori, J. Amer. Chem. Soc. 102, 2095 (1980).

Mixed anhydrides such as 61, available from carboxylic acids 60 and trifluoroacetic anhydride, have been shown to acylate alkynes 62 to produce the enol trifluoroacetate of a .beta.-diketone 63. Transesterification by refluxing with methanol liberates the .beta.-diketone 52, A. L. Henne and J. M. Tedder, J. Chem. Soc. 3628 (1953). ##STR41##

Compounds where R.sup.1 50 imidazole, such as 65, are readily available by any of a number of standard methods. For example, acylaminoketone 64 can be cyclized with ammonia or equivalents thereof, D. Davidson, et al., J. Org. Chem., 2, 319 (1937) to the to corresponding imidazole as shown in Scheme 13. The corresponding oxazole 66 can also be converted to imidazole 65 by action of ammonia or amines in general, H. Bredereck, et. al., Ber., 88, 1351 (1955); J. W. Cornforth and R. H. Cornforth, J. Chem. Soc., 96, (1947).

Several alternative routes to imidazoles 65 are illustrated in Scheme 14. As shown in Scheme 14 equation a), reaction of the appropriate R.sup.13 substituted imidate esters 67 with an appropriately substituted .alpha.-hydroxy- or .alpha.-haloketone or aldehyde 68 in ammonia leads to imidazoles of formula 65, P. Dziuron, and W. Schunack, Archive, Pharmaz., 307 and 470 (1974).

The starting imidazole compounds 65 wherein R.sup.13 is hydrogen can be prepared as shown in equation b) by reaction of the appropriate R.sup.13 -substituted imidate ester 67 with .alpha.-aminoacetaldehyde dimethyl acetal, M. R. Grimmett, Adv. Heterocyclic Chem., 12, 103 (1970).

As shown in equation c), imidazole 72 (wherein R.sup.13 =hydrogen and CH.sub.2 OH) can be prepared by treatment of the imidate ester 67 with 1,3-dihydroxyacetone 71 in ammonia by the procedure described in Archive der Pharmazie, 307, 470 (1974). Halogenation of imidazole 72 or any imidazole wherein R.sup.13 is hydrogen is preferably accomplished by reaction with one to two equivalents of N-halosuccinimide in a polar solvent such as dioxane or 2-methoxyethanol at a temperature of 40.degree.-100.degree. C. for 1-10 hours.

Compounds of formula 73 can also be prepared from 70 by reaction with formaldehyde as described in E. F. Godefroi, et al., Recueil, 91, 1383 (1972) followed by halogenation as was described above.

As shown in equation d) the imidazoles 65 can also be prepared by reaction of R.sup.13 substituted amidines 74 with an .alpha.-hydroxy- or .alpha.-haloketone or aldehyde 68 as described by F. Kunckel, Ber., 34, 637, (1901).

As shown in equation e), preparation of the nitroimidazoles (65, R.sup.13 =NO.sub.2) is preferably accomplished by heating the appropriate starting imidazole in a 3:1 mixture of conc. sulfuric acid/conc. nitric acid at 60.degree.-100.degree. C. for 1-6 hours. Nitration of the imidazole can be achieved by first converting the hydroxmethylimidazole to the corresponding chloromethylimidazole 75 employing thionyl chloride or oxalyl chloride. Nitration, as described above, followed by hydrolysis provides the nitroimidazoles 77.

Imidazoles 80 where R.sup.13 =CN can be prepared as shown in equation f) by reaction of R.sup.13 substituted ortho esters, ortho acids or aldehydes (followed by oxidation of the aldehyde) with diaminomaleonitrile 79 by the procedure described by R. W. Begland et al., J. Org. Chem., 39, 2341 (1974). Likewise, R.sup.13 substituted imidate esters 67 also react with diaminomaleonitrile to give 4,5-dicyanoimidazoles 80. The nitrile groups can be further elaborated into other functional groups by methods familiar to one skilled in the art.

Compounds wherein R.sup.13 =alkyl of 1-6 (straight or branched), phenyl, phenalkyl where alkyl is 1-3 carbon atoms, etc. and another R.sup.13 =CH.sub.2 OH can be prepared as shown in equation g). The imidazoles 83 were prepared as described in L A. Reiter, J. Org. Chem., 52, 2714 (1987), Hydroxymethylation of 83 as described by U. Kempe, et al. in U.S. Pat. No. 4,278,801 provides the hydroxymethylimidazoles 84.

The CH.sub.2 OH group, as in imidazolemethanol 72, is a versatile synthon for other functional groups. Scheme 15 shows some of these transformations, all of which are familiar to one skilled in the art. ##STR42##

A suitably protected imidazole 85 may undergo selective halogen-metal exchange followed by quenching 5 with electrophiles to yield trisubstituted imidazoles (Scheme 16) (M. Groziak and L. Wei J. Org. Chem. (1992) 57, 3776). This strategy can be used to add several R.sup.13 groups onto the imidazole ring. By changing the order in which the electrophiles are added, one may change the position to which the electrophile gets attached onto the imidazole ring. ##STR43## where (R.sup.13)+ is a suitable electrophilic precursors to R.sup.13.

The pyrazoles and imidazoles disclosed previously and other heterocycles which will be mentioned later in this specification may undergo alkylation onto a nitrogen ##STR44## atom just as the pyrrole in Scheme 4 by simply stirring a mixture of the heterocycle 88 and alkylbromide, iodide, mesylate or tosylate 89 in the presence of an acid scavanger such as potassium carbonate in an inert solvent such as THF or DMF for several hours to several days at room temperature or up to the reflux temperature of the solvent (Scheme 17).

Another way to make 9Q involves first deprotonation of the N--H of heterocycle 88 with a base such as NaH, KH, n-BuLi, t-BuLi, etc., followed by displacement of the X-leaving group of 89 to yield 90.

This sequence can be performed in inert solvents such as ether or THF. NaH and KH can also be employed in DMF and DMSO at room temperature or at a higher temperature. Alkylation sometimes yields regioisomers when more than one nitrogen atom is present in the heterocycle. These isomers can be separated by standard methods such as crystallization or chromatography. Once alkylated, the Y group can be coupled to the boronic acid moiety and all protecting groups removed to yield compounds of Formula I by procedures described previously.

Compounds where R.sup.1 =1,2,4-triazole can be prepared by the route of H. Paul, G. Hilgetag and G. Jahnchen, Chem. Ber., 101, 2033 (1968) which is depicted in Scheme 18. Imidate ester 92 is formed from nitrile 91 by the method of P. Keynaud and R. D. Moreau Bull. Soc. Chim. France, 2997 (1964). Hydrazide 99 is easily ##STR45## prepared via the action of hydrazine on the corresponding methyl ester precursor. It is understood that R.sup.13 of 91 and 94 do not necessarily have to be in their final form, for example. In each case, they can exist as either a protected species or in the form of a precursor to R.sup.13.

Alkylation of triazole 96 yields two isomeric products 97 and 98 when the R.sup.13 groups are not identical. These intermediates can be converted into final products in the usual fashion as shown in Scheme 19. ##STR46##

The regioselective syntheses of both 97 and 98 are shown in Scheme 20. Imidate ester 93 is reacted with hydrazine to form amidrazone 103. Alkylation with methyl .mu.-bromoacetate yields 194. Ring closure with either an ortho-ester, acid chloride or anhydride yields triazole 98. For a similar triazole synthesis, see David B. Reitz, European Patent Application 508, 445, published 14.10.92., G. D. Searle & Co. For schemes 20, and 22, the different R.sup.13 groups are differentiated from one another by the placement of a prime symbol next to one of the R.sup.13 groups, i.e. R.sup.13'. ##STR47##

Yet another regioselective synthesis of 97 or 98 is depicted in Scheme 21 following a similar sequence as was shown in Scheme 20 (D. B. Reitz, ibid.). ##STR48##

1,2,4-Triazoles also undergo selective metalation at the 5-position when the nitrogen at the 1-position is suitably protected. The metallated triazole can then be quenched through the addition of an electrophile to result in a newly functionalized triazole at the 5-position. Suitable protecting groups are benzyl and trityl. (D. K. Anderson, et al., J. Heterocyclic Chem., 23, 1257 (1986) as well as diethoxymethyl (S. Ohta, et al., Chem. Pharm. Bull., 41, 1226 (1993). The 3-position can also be metallated if the 5-position is suitably protected (S. Ohta et al., ibid.). Thus here we have two other methods for introducing R.sup.13 substituents at the 5- or 3-positions of the 1,2,4-triazoles.

Compounds where R.sup.1 =1,2,3-triazole can be synthesized via the 1,3-dipolar cycloaddition of an azide to an alkyne as shown in Scheme 22 (for an example of this cycloaddition reaction, see W. Kirmse and L. Horner Justus Liebigs Ann. Chem. (1958) 614, 1). ##STR49##

Compounds where R.sup.1 =tetrazole can be synthesized by the methods outlined in Scheme 23. In line a, three methods are given for the conversion of a nitrile into a tetrazole (ammonium chloride/sodium azide: W. G. Finnegan et al., J. Am. Chem. Soc. 1958, 80, 3908; trialkyltin azides: J. G. Luitjen et al., Rec. Tray. Chim. Pays-Bas; dialkyltin oxide: S. Wittenberger and B. G. Donner, J. Org. Chem., 1993, 58, 4139).

In Scheme 23, line b, two procedures are given for the regioselective synthesis of 1,5-disubstituted tetrazoles (DEAD, Ph.sub.3 P, TMSN.sub.3 : J. V. Duncia, M. E. Pierce, J. B. Santella III, J. Org. Chem. 1991, 56 2395; Tf.sub.2 O/NaN.sub.3 : E. W. Thomas Synthesis, 1993, 767) which can be more difficult to synthesize due to the steric crowding of the substituents.

Compounds where R.sup.1 is an oxazole may be synthesized by a variety of methods including those outlined in Scheme 24. The oldest synthesis and one of the most versatile is shown on line a), namely the cyclodehydration of 2-acylaminoketones (The Robinson-Gabriel Synthesis) (see I. J. Turchi in Oxazoles, Turchi, I. J., ed. John Wiley and Sons, New York (1986) p. 1). The 2-acylaminoketone starting materials may be synthesized from the Dakin-West reaction and modifications thereof (G. H. Cleland and F. S. Bennett Synthesis (1985).sub.681 and references therein). Some cyclodehydration agents include PCl.sub.5, H.sub.2 SO.sub.4, P.sub.2 O.sub.5, SOCl.sub.2, etc). ##STR50##

R.sup.a, R.sup.b and R.sup.c are equal to R.sup.13 which is described in the scope of this application. R.sup.13 in Scheme 24 does not have to be in finalized form as it appears in the scope, but can be in protected form or in the form of suitable precursors. It is understood that only when the entire molecule of formula I is synthesized do all of the substituents have to appear in their final forms as stated in the scope. Protected forms and suitable precursors to R.sup.13 are readily recognized by one skilled in the art of organic synthesis.

In line b, the reaction of .alpha.-acylketones 131 with ammonium acetate/acetic acid also yields oxazole 130 (D. Davidson, M. Weiss, M. Jelling J. Org. Chem. (1937), 328). In line c, we find the regioselective formation of oxazole 130 from the reaction of an .alpha.-haloketone 134 with amide 133 (R. Lakham, B. Ternai, Adv, Heterocycl. Chem. (1974) 17, 99; I. J. Turchi, M. J. S. Dewar, Chem. Rev. (1975), 75, 389). Acid chlorides 135 react with oximes 136 to yield after a �3,3! sigmatropic rearrangement (138) oxazole 130 as shown in line d (G. S. Reddy and M. V. Bhatt Ind. J. Chem. (1981) 208, 322; M. V. Bhatt, G. S. Reddy Tet. Lett. (1980) 21, 2359). In line e, .mu.-azidoketones (140), after reaction with triphenylphosphine to yield 141, react with acid chloride 135 to yield oxazole 130 (E. Zbiral, E. Bauer, J. Stroh Monatsh. Chem. (1971) 102, 168). Finally, oxazoles undergo deprotonation with strong bases such as n-BuLi at the 2-position when the 4 and 5 positions are blocked and after quenching with an electrophile can yield oxazole 130 (R. Schroder, V. Schollkopf, E. Blume, I. Hoppe Liebigs Ann. Chem., (1975) 533). As stated earlier, R.sup.13 can be either in final form as defined in the scope of this application or in the form of precursor functionality which later on can be elaborated into final form by methods familiar to one skilled in the art. This holds true not only for the oxazoles discussed here, but for all of the other heterocyclic systems in this application where R.sup.13 appears as substituents.

Oxazoles are most readily brominated at the 5-position followed by the 4-position and finally the 2-position. A brominated oxazole (as well as other brominated heterocycles in this application) can undergo aryl cross-coupling reactions catalyzed by transition metals to yield aryl-or heteroaryl-substituted oxazoles (See for example E.-I. Negishi; A. O. King; N. Okukado J. Org. Chem. (1977) 42, 1821).

Compounds where R.sup.1 is an isoxazole may be synthesized by the methods outlined in Scheme 25. In line a, reaction of 1,3-diketone 143with hydroxylamine yields oxazoles 144 and 145. Nitrile oxide 146 can also add across the triple bond of alkyne 147 to yield isoxazoles 144 and 145. (See P. Grunanger and P. Vita-Finsi Isoxazoles, v. 49 pt. 1 of The Chemistry of Heterocyclic Compounds, E. C. Taylor and A. Weissberger, eds., John Wiley and Sons (New York: 1991) p. 126). ##STR51##

As discussed previously R.sup.a, R.sup.b and R.sup.c in Scheme 25 are again equal to R.sup.13 and are not necessarily in final form as they appear in the scope of this application.

Compounds wherein R.sup.1 is a thiazole may be synthesized by the method depicted in Scheme 26, which mimics the route of Scheme 24c) describing a route for oxazoles. Thus thioamide 148 reacts with .alpha.-halocarbonyl compound 134 to yield thiazole 149. Again as for the oxazole, R.sup.a, R.sup.b, and R.sup.c have the same definitions. For the synthesis of thiazoles, by the route depicted in Scheme 26, see G. Vernin "General Synthetic Methods for Thiazole and Thiazolium Salts" in Thiazole and Its Derivatives, J. V. Metzger, ed., volume 34, pt. 1 in The Chemistry of Heterocyclic Compounds, A. Weissberger and E. C. Taylor, eds. John Wiley and Sons (New York:1979) p. 180. ##STR52##

Compounds wherein R.sup.1 is a 1,2,5-thiadiazole may be synthesized by the methods shown in Scheme 27. Diamine 150 may be reacted with sulfur monochloride to yield 1,2,5-thiadiazole 151. Likewise, .alpha.-diketone 152 may be converted into bisoxime 153 which also reacts with S.sub.2 Cl.sub.2 to yield 151 (L. M. Weinstock, P. Davis, B. Handelsman, R. Tull J. Org. Chem. (1967) 32, 2823). Z is defined in Scheme 24. ##STR53##

Compounds wherein R.sup.1 is a 1,2,4-thiadiazole may be synthesized by the method depicted in Scheme 28. Oxidation of thioamide 154 with hydrogen peroxide yields S-oxide 155 which must be stored at 0.degree. C. Further reaction of the S-oxide intermediate with thioamide 156 yields thioacylamidine 157 which cyclizes to product 158 (V. Goerdeler, H. Porrmann Chem. Ber. (1962) 95, 627). R.sup.a and R.sup.b are as defined previously in Scheme 24.

Compounds where R.sup.1 is a furan may be synthesized by the methods shown in Scheme 29, but as understood by one skilled in the art, not limited thereto, as in the case as for all of the schemes in this patent application. In line a, cyclodehydration of 1,4-dicarbonyl compound 159 yields furan 160 (L. D. Krasnoslobodskaya, Ya. L Gol'dfarb Russ. Chem. Rev. (Engl. Trans.) 1969, 38, 389). In line b, .alpha.-bromoketone or aldehyde 161 protected as its dimethyl ketal or acetal reacts with trimethylsilylenol ether 162 to yield intermediate 163 which cyclizes to furan 160 (T. Mukaiyama, H. Ishihara, K. Inomata Chem. Lett., 1975, 527). R.sup.a, R.sup.b, R.sup.c, and R.sup.d are R.sup.13 which is described in the scope of this application and with similar limitations as were described under Scheme 24 for R.sup.13 with regards to being in final form or not.

Compounds where R.sup.1 is a thiophene may be synthesized by the methods shown in Scheme 30. In line a, 1,4-dicarbonyl compound 159 is reacted with a phosphorous sulfide (phosphorous pentasullfide, phosphorous trisulfide, phosphorous heptasulfide, etc.) to yield thiophene 164 (H. D. Hartough, Chem. Heterocycl. Compd., 1952, 3, 1). The dicarbonyl compound 159 also reacts with H.sub.2 S to favor thiophenes at lower temperatures (-50.degree. C.) (F. Duus Tetrahedron, 1976, 32, 2817). Reaction of alkenes 165 or 166 (line b) with sulfur and heat also yield thiophene 16 (A. S. Broun, M. G. Voronkov J. Gen. Chem. USSR, (Engl. Trans.) (1947) 17, 1162; M. g. Voronkov, A. S. Broun, ibid, (1948) 18, 700; J. Schmitt., M. Suquet, R. Fallard (C. R. Hebd, Seances Acad, Sci. (1956) 242, 1738. R.sup.a, R.sup.b, R.sup.c and R.sup.d are as defined in Scheme 29. ##STR54##

Compounds where R.sup.1 is a pyridine may be synthesized by the methods shown in Scheme 31. It is to be understood that each scheme and each reaction has its own scope and limitations and that no one synthesis is universally applicable. It is also to be understood that one skilled in the art will be able to determine which synthesis is best suited for his or her needs. In line a, reaction of enamine 167 with ethynyl ketone 168 will cyclize to pyridine 170 (F. Bohlmann, D. Rahtz Chem. Ber. (1957)90, 2265). Enamino ketones 171 (line b) condense with 1,3-diketones or beta-keto esters 172 to yield pyridine 174 where R is alkyl, aryl or alkoxy and aryloxy (N. K. Kachetkov, A. Gonsales, A. Nesmeyanov Dokl. Akad, Navk, SSSR (1951) 79, 609; S. Auricchio, R. Bernardi, A. Ricca Tet. Lett. (1976) 9831; H. Henecka Chem. Ber. (1949) 82, 41).

The Hantsch dihydropyridine synthesis can be used in the synthesis of pyridines as shown in line c. There are many modifications of this synthesis of which only one is shown. Reaction of 175 with beta-aminocrotonate 176 yields dihydropyridine 177 (F. Bassett, H. Meyer, E. Wehinger Angew. Chem. Int. Ed. Engl. (1981) 20, 762). Further oxidation with, for example, dilute nitric acid yields pyridine 178 where R and R.sup.1 can be different alkoxy groups (E. Knoevenagel, W. Rushhaupt Ber. (1898) 31 1025). Cycloaddition of oxazole 179 with alkene 180 can also yield a pyridine (182) (M. Ya Karpeiskii, V. L. Florent'ev Russ. Chem. Rev. (Engl. Trans.) (1969) 38, 540; R. Lakhan, B. Ternai Adv. Heterocyl. Chem. (1974) 17, 99). In all of these pyridine synthesis, R.sup.a, R.sup.b, R.sup.c, and R.sup.d are as described for Scheme 29. All of the substituents around the pyridine ring can be in final form or in the form of a precursor to a given functional group as would be recognized by one skilled in the art. Finally, in line e, hydroxypyridines, such as 183, may be triflated and coupled with an aryl-or heteroarylboronic acid or aryl-or heteroaryltrialkylstannane using a transition metal catalyst such as Pd to yield aryl or heteroarylpyridinecarboxylic acids, such as 186. This in turn may be coupled to aminoboronic acid esters as discussed previously to yield compounds of Formula I. Halogens, such as Br or I may be used instead of triflate in compound 184 to undergo what is known as the Suzuki coupling reaction. R and R.sup.1' in line e) are any of the allowed phenyl substituents in the scope of this application (Suzuki reactions: A. Suzuki Pure Appl. Chem. (1985) 57, 1749). ##STR55##

Compounds where R.sup.1 is a pyridazine may be synthesized by the routes shown in Scheme 32. Reaction of 1,4-carbonyl compound 187 with hydrazine yields pyridazine 188. If the 1,4-dicarbonyl compound is saturated as in line b (compound159), then the product from the reaction with hydrazine 189must be oxidized to yield pyridazine 188 (K. C. Nicolaou, W. E. Barnette, R. L. Magolda J. Am. Chem. Soc. (1979) 101, 766; ##STR56## M. Tisler, B. Stanovnik "Pyridazines and their Benzo Derivatives" in A. R. Katrizky, C W. Rees Comprehensive Heterocyclic Chemistry, v.3 (Pergamon Press: Oxford), 1984, p. 45). Halopyridazines or hydroxypyridazines may also undergo the same aromatic cross-coupling reactions as were described for pyridines. R.sup.a, R.sup.b, R.sup.c and R.sup.d, etc., are defined the same as in the pyridine case.

Compounds wherein R.sup.1 is a pyrimidine may be synthesized by the methods shown in Scheme 33. Reaction of 1,3-dicarbonyl compound 190 with amidine 191 yields pyrimidine 192 (D. J. Brown, S. F. Mason The Pyrimidines in A. Weissberger ed. The Chemistry of Heterocyclic Compounds, (John Wiley: New York) 1962, p. 31). ##STR57## Reaction of amidine 191 with 193 also yields pyrimidines (P. Schenone, L. Sansebastiano, L. Mosti J. Heterocyclic Chem. (1990) 27, 295). R.sup.a, R.sup.b, R.sup.c, and R.sup.d are as defined previously in Scheme 32. Halopyrimidines or hydroxypyrimidines may also undergo the same aromatic cross-coupling reactions as were described for pyridines. ##STR58##

Compounds in which R.sup.1 is a 1,2,4-triazine my be synthesized by the procedures outlined in Scheme 34. In line a, 1,3-dicarbonyl compound 194 is condensed with amidrazone 195 to yield triazine 196 (H. Neunhoeffer and P. F. Wiley Chemisrty of 1,2,3-Triazines and 1,2,4-Triazines and Pentazines, v. 33 in A. Weissberger, E. C. Taylor, eds., The Chemistry of Hetrocyclic Compounds John Wiley and Sons (New York: 1978) pp 194-200 and p. 524). In line b, cyclization of acylhydrazone 197 with ammonia or ammonium acetate leads to triazine 196 (H. Neunhoeffer, P. F. Wiley, ibid., p. 196, 197). In line c, reaction 1,2-dicarbonyl compound 194 with oxalamidrazonates 198 yields 1,2,4-triazine ester 199. Saponification of 199 yields 200 which can be decarboxylated to yield 1,2,4-triazine 201 (H. Neunhoeffer, P. F. Wiley, ibid., p. 526). R.sup.a, R.sup.b, and R.sup.c are as defined in the pyridine case. Halotriazines or hydroxytriazines may undergo the same aromatic cross-coupling reactions as were described earlier for pyridines.

Compounds in which R.sup.1 is as described in lines k and l in the scope of this application may be synthesized by the methods described in Scheme 35. If heterocycle --J--K--L--M--Q-- 202 contains a bromine, iodine or a hydroxyl group (which can be triflated) designated by X, then it can undergo a Suzuki coupling to yield 204 where u is 0 (A. Suzuki, ibid) (Scheme 35, line a). If instead of B(OH).sub.2 a trialkyltin group is present, then a Stille coupling can be performed when X=triflate (J. K. Stille Angew. Chem. Int. Ed. Engl. (1986) 25 508; J. K. Stille Pure Appl. Chem. (1985) 57, 1771). ##STR59## The X and B(OH).sub.2 (or trialkyltin) moieties may be reversed so that now X=B(OH).sub.2 (or R.sub.3 Sn) and the phenyl of 203 contains halogen or triflate group. The same coupling procedures may be used in synthesizing compounds where R.sup.1 is described by line 1 and u is 0 as were used in synthesizing compounds where R.sup.1 is described by line k and u is 0.

When u is not 0, heterocycle 205 and its six-membered ring counterpart --C--W--R--T--U--V-- (described in line 1) must be synthesized from scratch by the methods described heretofore, with the --(CH.sub.2).sub.u -Phenyl--(CH.sub.2).sub.m CO.sub.2 R group being one of the substituents in final or precursor form. If heterocycle 205 contains an N--H which is alkylatable, then alkylation with 206 where X is Cl, Br, I, mesylate tosylate or triflate yields 207 (Scheme 35, line b). The esters 204 and 297 can then be hydrolyzed to the free acid and coupled with aminoboronic acid ester derivative as described in Scheme 4, for example, to yield boronic acid esters which can also be hydrolyzed to the corresponding free boronic acid products.

A general method (Scheme 36) for the synthesis of 4-carboxydihydroheterocycles (oxazolines, thiazolines, imidazolines) utilizes the condensation of an .alpha.-amino acid ester (210) with an imidate (211) to provide 212, see: Meyers, A. I.; Hanagan, M. A.; Mazzu, A. L. Heterocycles 1981, 15, 361; Meyers, A. I.; Whitten, C. E. Heterocycles 1976, 1, 1687; North, M.; Pattenden, G. Tetrahedron 1990, 46, 8267; Jones, R. C. F.; Ward, G. J. Tetrahedron Lett. 1988, 29, 3853. In the case where R.sup.20 =H, the cyclization might be conducted with trimethyl orthoformate instead of 211, see: Martin, P. K. et al. J. Org. Chem. 1968, 33, 3758. For compounds that are substituted only at the 2-position of the heterocycle, serine or cysteine might be used as the amino acid ester partner. The dihydroimidazole-based materials would be prepared from an N.sup..alpha. -monoprotected diaminopropionic acid to prevent tautomerization of the double bond once the cyclic system of 212 has been formed, see: Martin, P. K. et al. J. Org. Chem. 1968, 33, 3758. Hydrolysis of the ester then affords carboxylic acid 213. ##STR60##

It may be desirable to prepare more highly substituted heterocycles as well (Scheme 37). An approach to the oxazoline class could utilize reaction between the anion of 215 and formaldehyde to provide adducts 216 as recorded by Kanemasa, S. et al. Tetrahedron Lett. 1993, 34, 677 and Ito, Y. et al. Tetrahedron 1988, 44, 5253. Hydrolysis of the imine should deliver 217, an example of an G-substituted .alpha.-amino acids, as a mixture of isomers. Condensation as before with imidate (211) should generate cyclic moieties of general structure 218 which are hydrolyzed to 219.

The corresponding thiazolines should be available by installing a sulfhydryl group prior to cyclocondensation. To that end, N--protection of 217, followed by reaction with a sulfur nucleophile, a thiol ester or an inorganic salt thereof, based on the work reported by Mitsunobu, O. Synthesis 1981, 1, and Yuan, W. et al. J. Med. Chem. 1993, 36, 211, should provide the substituted cysteine (220) upon premoval of the N-protecting group. Subsequent reaction with the imidate should deliver 221 and ultimately 222, after hydrolysis of the ester. ##STR61##

The imidazolines should be obtained via the condensation described by Jones, R. C. F.; Ward, G. J. Tetrahedron Lett. 1988, 29, 3853, of a suitable diamino acid with imidate 211. The preparation parallels the sequences discussed above where the anion of 215 would be expected to generate adduct 223 as described by Gilbert, I. et al. Tetrahedron Lett. 1991, 32, 2277. Manipulation of the protecting groups and implementation of the aforementioned cyclization should give imidazoline 225 which may be converted to the corresponding carboxylic acid 226.

Using an analogous synthetic sequence (Scheme 38), the polysubstituted versions of these heterocycles should also be accessible. For the oxazo--or imidazo--type compounds, reaction of the anion of 215 with an electrophile 227 should deliver 228, as reported by Kanemasa, S. et al. Tetrahedron Lett. 1993, 34, 677 �cf. Meyer, R. et al. Liebigs Ann. Chem. 1977, 1183!, and liberation of the a -amino group should then provide 229, as a mixture of isomers. Application of the now standard cyclocondensation should complete the synthesis of 231 upon hydrolysis of 230.

A similar sequence should provide an entry into the thiazolines series (235). However, in the case where R.sup.3b =H, this material would be prepared by converting 232 to the corresponding mercaptan 233 using the conditions described earlier; the ester in 234 could then be hydrolyzed to afford 235. This reaction sequence would be preferred to avoid use of a presumably unstable thioaldehyde (227 where U=S and R.sup.3b =H), see: Takahashi, T. et al. Heterocycles 1993, 36, 1601 and references therein. ##STR62##

Alternative methods for the preparation of these polysubstitutued heterocycles employ (Scheme 39) the addition of the anion of isocyanide 236 to an electrophile 227 to provide the heterocycle 237, see: Ito, Y. et al. Tetrahedron Lett. 1989, 30, 4681; Ito, Y. et al. Tetrahedron Lett. 1988, 29, 6321, 235; Ito, Y. et al. Tetrahedron Lett. 1987, 28, 6215; Ito, Y. et al. Tetrahedron 1988, 44, 5253; Meyer, R. et al. Liebigs Ann. Chem. 1977, 1183. The carboxylic ester may be manipulated at this time, however the preferred sequence would implement either an exchange reaction mediated by a transition metal catalyst as reported by Ito, Y. et al. Tetrahedron 1988, 44, 5253 to provide derivatives 238; standard hydrolysis followed by reaction with imidate 211 would also yield 238. Subsequent conversion to the carboxylic acid 239 should proceed smoothly. For cyclic compounds (243) where R.sup.20 =H, the preferred sequence would involve the sequential hydrolysis of adduct 240, transformation of the hydroxyl group into a sulfhydryl function, cyclocondensation to thiazoline 242 and finally hydrolysis to afford the desired carboxylic acid 243. ##STR63##

Another noteworthy method (Scheme 40) for the assembly of oxazolines and thiazolines utilizes an appropriate N-acyl-.beta.-hydroxy-.alpha.-amino acid (244) which reacts intramolecularly by cyclization of the amide carbonyl onto the hydroxyl group of the amino acid. This transformation may occur upon treatment with triphenylphosphine and an azodicarboxylate, as reported by Wipf, P.; Miller, C. P. Tetrahedron Lett. 1992, 33, 6267, 907 and Galeotti, N. et al. Ibid., 2807, or through the use of diphenyl sulfoxide and triflic anhydride, as demonstrated by Yokokawa, F. et al. Synlett 1992, 153, to generate the requisite ring system; in 245. Hydrolysis of the ester then provides 246. Alternatively, this cyclization may be effected by intramolecular displacement of the corresponding halo derivative (--OH.fwdarw.halogen in 244), which is generated in situ, to provide the oxazoline (245), see: Evans, D. A. et al. J. Org. Chem. 1992, 57, 1961. ##STR64##

The regioisomeric 5-carboxyheterocycles may be synthesized (Scheme 41) by condensation of an appropriate .alpha.-functionalized .beta.-amino acid with imidate 211; for an example of this type of cyclization, see: Wolfe, S. et al. Tetrahedron Lett. 1979, 3913. In the event, nucleophilic opening of an a, b-epoxy acid (247) with an inorganic azide such as lithium azide according to Chong, J. M.; Sharpless, K. B. J. Org. Chem. 1985, 50, 1563 should provide 248; the corresponding esters also participate in this reaction, see: Commer.cedilla.on, A. et al. Tetrahedron Lett. 1992, 33, 5185. Reduction should give the requisite (.alpha.-hydroxy-.beta.-amino acid 249. Alternatively, it may be desirable to prepare 249 from an a--amino acid directly as described by Poss, M. A.; Reid J. A. Tetrahedron Lett. 1992, 33, 1411, by reaction of the appropriate N-BOC compound (250) with 2-furyllithium to provide vicinal amino alcohol (251); manipulation of the furan moiety and deprotection then generates 249. A similar approach using 2-ithiothiazoles may also be useful, see: Dondoni, A.; Perrone, D. Tetrahedron Lett. 1992, 33, 7259. ##STR65##

Completion of the syntheses of the heterocycles should follow precedent. Reaction with of 249 with 211 should provide oxazoline 254 directly. This alcohol may also be used in a sequence described previously to allow for incorporartion of sulfur and ultimately provide 250; this mercaptan should lead to thiazoline 251. Additionally, 249 could be employed as a substrate for reaction with a nitrogen based nucleophile, see: Mitsunobu, O. Synthesis 1981, 1 �cf. Cardani, S. et al. Tetrahedron 1988, 44, 5563!, to deliver 252 as a precursor for imidazoline 253.

The regioisomeric imiodazolines should be available from other routes as well (Scheme 42). One method would call for hydrolysis of imine 223, discussed earlier in Scheme 37, followed by protection of the newly liberated .alpha.-amino group to give 254. Cleavage of the phthaloyl residue and reaction with imidate 211 should provide 255 which is hydrolyzed to 256. An alternative approach calls for reaction of an .alpha.-bromo-.alpha.,.beta.-unsaturated ester (257) with an amidine (258) �sterically hindered (P is large ) materials do not react!to generate 259 in a single step as reported by Marsura, A. et al. Synthesis 1985, 537; hydrolysis of the ester should yield the acid 260. ##STR66##

The several types of inhibitors disclosed in this invention can be broadly classified by their electrophilic functional group A, as defined in Formula (I). The compounds described below, unlike the boron containing peptides, utilize a highly electrophilic carbon atom at A to interact with the active site serine of thrombin. The precursor for the electrophilic carbon inhibitors is the appropriately protected amino acid (261) of Scheme 43. ##STR67## The preparation of (261) can be found in the general chemical literature, one such reference being the review by Morrison and Mosher (1976). According to Scheme 43 various terminal functional groups are available from (261): the formamidino-(262), cyanoguanidino-(263), hydroxyguanidino-(264) and guanidino-analogs (265).

The preparation of amidine derivative (267) and phenylguanidines of formula (269) from amino acids (266) and (268), respectively, is shown in Scheme 44. The conditions used Lo prepare amidines of formula (267) is discussed for (303) of Scheme 53 while the method for formamidinylation of (268) to give (269) is the same as that described to prepare (295) of Scheme 52. ##STR68##

As shown in Scheme 45, appropriately protected derivatives of formulae (261-269), wherein M is an alkyl or benzyl group can be coupled with N,N-disubstituted acid (270) or (271) (wherein M is hydrogen). The X group in compounds of formulae (261) through (269) and (272) in Scheme 45, as well as in compounds illustrated in the Schemes to follow, is a protected version of the terminal functional group X, as defined by Formula (I), unless deprotection is indicated to obtain the final compound of the sequence. ##STR69## It is understood that the protecting group(s) used should compatible with the conditions of the process discussed; a good source for information on protecting group chemistry is Greene and Wuts (1991).

The preparation of the thrombin inhibitors trihalomethyl ketone (274) and .alpha.-ketoester (275) are shown in Scheme 46. The coupled ester (272), wherein M is alkyl or benzyl can be converted to the acid (M is hydrogen) by the methodology appropriate for the particular ester functionality as described in Greene and Wuts (1984). The aldehyde (273) can be prepared by selective reduction of the acid (272, M is hydrogen) to the primary alcohol followed by oxidation. ##STR70## To obtain the primary alcohol, the acid can be transformed to the mixed anhydride by condensation of the trialkylammonium salt of the acid with an alkyl- or arylchloroformate in an inert non-polar solvent such as tetrahydrofuran, 1,2-dimethoxyethane or toluene at -78.degree. C. to room temperature. The solution of the resulting mixed anhydride is filtered and reduced to the peptidyl alcohol with an excess of a borohydride reducing agent in a compatible solvent like water or an alcohol at -78.degree. C. to room temperature according to the method of Rodriguez et. al., Tetrahedron Lett. 32, 923 (1991). The peptidyl alcohol can be oxidized to aldehyde (273) without over oxidation by a variety of procedures, as detailed by Hudlicky in Oxidations in Organic Chemistry, American Chemical Society, p. 114 (1991); the preferred methods include Swern oxidation described by Omura and Swern, Tetrahedron 34, 1651 (1978); and the Pfitzner-Moffat oxidation described by Fearon et al. in J. Med. Chem. 30, 1617 (1987). A two step protocol reported by Edwards, Tetrahedron Lett. 33, 4279 (1992) can be used to prepare the trifluoromethyl ketones (274) (J is fluorine) from aldehyde (273). In this procedure a metallated trifluoromethyl anion is generated from an excess of trifluoromethyliodide or -bromide and an active metal such as zinc, magnesium, lithium or cadmium in inert, anhydrous solvents like tetrahydrofuran or N,N-dimethylformamide at temperatures of -100.degree. C. up to the reflux point of the solvent. Alternatively, the metallated trifluoromethyl anion may be generated by the transmetallation of trifluoromethyliodide or -bromide with an organometallic compound such as a Grignard reagent or alkyllithium compound in an inert solvent like tetrahydrofuran, hexane or ether at temperatures ranging from -78.degree. C. up to the reflux point of the selected solvent. Aldehyde (273) can be added to the solution of the metallated trifluoromethyl anion to form the trifluoroethanol derivative at temperatures of -100.degree. C. or higher. To obtain the trifluoromethyl ketone (274) where J is fluoro, the alcohol is oxidized by the Pfitzner-Moffat or Swern procedure. Removal of the protecting group(s) on terminal group X by the appropriate method will provide the thrombin inhibitors of formulae (274).

Trihalomethyl analogs of (274), where J is fluoro can also be prepared from aldehyde (273) by a different method. The trihalomethyl ketones are prepared by treating aldehyde (273) with either the trimethylsilyl trihaloacetate or the potassium or sodium trihaloacetate in a polar solvent such as an alcohol, N,N-dimethylformamide or methylsulfoxide with or without a base such as a trialkyl amine, potassium carbonate or sodium hydroxide at temperatures of -78.degree. C. or higher according to the method of Beaulieu, Tetrahedron Lett. 32, 1031 (1991); Shell Int. Res., European Patent Application EP 16504). The resulting .alpha.,.alpha.,.alpha.-trihaloethanol is oxidized and group X can be deprotected as above to give the thrombin inhibitors or formulae (274).

The .alpha.-ketoester thrombin inhibitors, exemplified by (276), are prepared according to a route disclosed by Iwanowicz et. al. in Bioorgan. Med. Chem. Lett. 12, 1607 (1992). The tris(ethylthio)methyl anion is added to the peptidyl aldehyde (273) in a solvent such as tetrahydrofuran, 1,2-dimethoxyethane or toluene at -100.degree. C. or higher to give the alcohol (275). The .alpha.-hydroxyl ester is generated from (275) by treatment with a mixture of mercuric salts, such as mercuric chloride and mercuric oxide, in an alcohol or water. Swern or Pfitzner-Moffat oxidation of the s-hydroxyl ester followed by the deprotection of substituent X protecting group provides thrombin inhibitors of formula (276).

Another method for the preparation of compound (276) substitutes a 1-lithio-1-alkoxyethene or 1-magnesio-1-alkoxyethene for the tris(ethylthio)methyl anion of Scheme 15 in an addition reaction with peptidyl aldehyde (273). There can be obtained an adduct analogus to the tris(ethylthio)hydroxyethyl compound (275) when excess 1-magnesio- or 1-lithio-1-alkoxyethene anion is stirred at temperatures ranging from -100.degree. C. to ambient temperature with (273) in anhydrous solvents such as diethyl ether or tetrahydrofuran. This alkoxyolefin product may then be transformed to (276) by oxidative cleavage with reagents such as ozone or periodate in an inert solvent such as a halohydrocarbon, lower alkyl ketone, an alcohol or water at temperatures ranging from -100.degree. C. to ambient temperature, followed by oxidation of the intervening .alpha.-hydroxyester and deprotection as described above.

The preparation of the .alpha.,.alpha.-dihalomethylketone thrombin inhibitors of this invention is outlined in Scheme 47. ##STR71## The .alpha.,.alpha.-dihalomethylketone (279), where J is fluoro can be prepared from the aldehyde (273) by selective reaction of the aldehyde with the anion of the corresponding dihalomethane. The metallated dihalomethane anion is generated from one equivalent each of a strong hindered base, such as lithium tetramethylpiperidide or tertbutyllithium, and the selected dihalomethane in an anhydrous, inert solvent like tetrahydrofuran or 1,2-dimethoxyethane at -100.degree. C. or higher according to the method of Taguchi et. al. Bull. Chem. Soc. Jpn., 50, 1588 (1977). The metallated dihalomethane anion can be added to the aldehyde (273) at -100.degree. C. or higher. Alternatively, the dihalomethane anion is generated from a dihalomethyl(trimethyl)silane and an anhydrous fluoride ion source such as tris(diethylamino)sulfonium difluoromethyl silicate in an inert solvent like benzene, acetonitrile or tetrahydrofuran at -78.degree. C. or higher, then (273) can be added to give dihaloethanol (278) according to the method of Fujita and Hiyama, J. Am. Chem. Soc. 107, 4085 (1985). The resulting dihaloethanol can be oxidized to ketone (279) by the Swern or Pfitzner-Moffat procedure. Removal of the protecting group(s) on substituent X of (279) gives the .alpha.,.alpha.-dihalomethylketone thrombin inhibitors.

.alpha.-Halomethylketone thrombin inhibitors can be prepared by the process illustrated in Scheme 48. The acid chloride (281) can be prepared from acid (272), wherein M is hydrogen or its trialkylammonium, sodium or potassium salt with a chlorinating agent such as thionyl chloride, oxalyl chloride or dichloromethylmethyl ether in a solvent like tetrahydrofuran or dichloromethane with or without a catalytic amount of N,N-dimethylformamide at -78.degree. C. or higher. Alternatively, the mixed anhydride of (272).sub.m ay be prepared as described for (272) in Scheme 46. Compound (281) or the mixed anhydride of (272) can be treated with an ether solution of diazomethane and either anhydrous hydrogen fluoride or hydrogen chloride gas according to that described by McPhee and Klingsbury, Org. Synth. Coll. III, 119 (1955); or hydrogen bromide according to the method Miescher and Kaji, Helv. Chim. Acta. 24, 1471 (1941). ##STR72## Selection of the hydrogen fluoride gas will give the .alpha.-fluoromethylketone analog, (282) wherein J is fluoro; and hydrogen chloride gas gives the .alpha.-chloromethylketone analog (282) wherein J is chloro. Deprotection of X gives the corresponding thrombin inhibitors of (282).

The general preparative route for the .alpha.,.beta.-diketoester, -amide and -ketone thrombin inhibitors of this invention is exemplified in Scheme 49. Compound (281) or the mixed anhydride of (272) can be reacted with a Wittig reagent such as methyl (triphenyl-phosphoranylidene)acetate in a solvent like tetrahydrofuran or acetonitrile at temperatures ranging from 0.degree. C. to the reflux point of the solvent to give (284). Oxidative cleavage of the phosphoranylidene (284) with an oxidizing agent like ozone or OXONE.TM. in an inert solvent such as tetrahydrofuran, dichloromethane or water at temperatures of -78.degree. C. or higher gives the vicinal tricarbonyl compound (285), analogous to that described by Wasserman and Vu, Tetrahedron Lett. 31, 5205 (1990). Cleavage of the protecting group can provide thrombin inhibitors of formula (285). ##STR73##

The preparative routes for the synthesis of the .alpha.-mono- and .alpha.,.alpha.-dihalo-.beta.-ketoester -amide and ketone thrombin inhibitors of this invention are summarized in Scheme 50. The exemplified .beta.-ketoester (287) is available from the acid derivative (272). The acid (272) can be treated with carbonyl diimidazole in an inert solvent such as tetrahydrofuran or dichloromethane at 0.degree. C. or higher to form the acyl imidazole. This acyl imidazole, or the mixed anhydride of (272), can be further reacted with lithioethylacetate in solvents such as 1,2-dimethoxyethane or tetrahydrofuran/hexane at temperatures ranging from -100.degree. C. to ambient temperature, according to the method of Dow, J. Org. Chem. 55, 386 (1990) to give .beta.-ketoester (287). ##STR74## Compound (287) serves as a substrate for both mono- and dihalogenation. The .alpha.-monochloro analog of (288), where J is each chlorine and hydrogen, can be prepared by controlled halogenation reactions with reagents like N-chlorosuccinimide or thionyl chloride in an inert halogenated solvent and at temperatures ranging from -20.degree. C. to the reflux point of the selected solvent according to the methods of Uhle, J. Am. Chem. Soc. 83, 1460 (1961); and DeKimpe et. al., Synthesis 2, 188 (1987). The .alpha.,.alpha.-dihalo analog (289) where J is chloro is available from halogenation with molecular chlorine in a halogenated solvent at temperatures of -20.degree. C. or higher according to the method of Bigelow and Hanslick, Org. Syn. Coll. II, 244 (1943). Reagents such as N-fluorobis�(trifluoromethyl sulfonyl!imide are useful for the preparation of mono- and difluoro analogs (288) and (289) by reacting the appropriate stoichiometry of this reagent with (287) in a halogenated solvent at temperatures of -78.degree. C. or higher according to the method of Resnati and DesMarteau, J. Org. Chem. 56, 4925 (1991). Deprotection of substituent X of the halogenation products (288) and (289) can provide the corresponding thrombin inhibitors.

Compounds of formula (287) also serves as a substrate for the preparation of tricarbonyl derivatives such as (285) (Scheme 49). Condensation of (287) with an aldehyde, such as benzaldehyde, gives an .beta.-ene-.alpha.,.gamma.dione. This ene-dione can be oxidatively cleaved with reagents like ozone or periodate to give tricarbonyl analog (285).

The preparation of the mono- and dihalomethylketone thrombin inhibitors is outlined in Scheme 51. The intermediates formed in the preparation of the .alpha.-mono- and .alpha.,.alpha.-dihalo-.beta.-ketoester thrombin inhibitors of Scheme 49 can be used in these preparations. ##STR75## The decarboxylation of these halogenation products, (288) and (289), can be effected by saponification of the ester with mild aqueous base such as potassium carbonate or sodium hydroxide in water miscible solvents like an alcohol, tetrahydrofuran or N,N-dimethylformamide, followed by adjusting the pH to a range of 4 to 6. This mixture can be either stirred at ambient temperatures or heated at various temperatures up to the reflux point of the solvent chosen until the formation of (279) or (282) is complete and is similar to that reported in Matsuda et. al., Tetrahedron Lett. 30, 4259 (1989). Removal of protecting group(s) can provide thrombin inhibitors corresponding to (279) or (282).

A process for the preparation of the boropeptide thrombin inhibitors of this invention from intermediates (291) and (292) is disclosed in Scheme 52. Compound (291) serves as a starting point for isothiouronium thrombin inhibitors (296) and (297). The boronic ester (296) is prepared by stirring a solution of (291) and thiourea in an inert polar solvent, such as an alcohol or N,N-dimethylformamide, at temperatures ranging from ambient to the reflux temperature of the selected solvent. It is understood that a boronic acid ester like compound (296) is an effective thrombin inhibitor, however, it may be transformed to the corresponding free boronic acid (297) without a loss of biological activity. Compound (297) is derived from the boron ester (296 by transesterification under equilibrium conditions. ##STR76## Thus stirring ester (296) with an excess of an alkyl- or aryl boric acid in a biphasic mixture of neutral or acidic water and an immiscible solvent, such as ethyl ether or toluene, gives (297) after several hours at ambient temperature. The conditions generally preferred use 5 to 10 equivalents of phenylboric acid in ethyl ether/water at neutral pH. Thrombin inhibitors (293) to (299) are obtained by reduction of an azide intermediate prepared from (291) or (292). The azide intermediate is prepared by heating either (291) or (292) with an inorganic azide, such as sodium or potassium azide, in an anhydrous polar aprotic solvent, such as acetone, dimethylformamide or methyl sulfoxide at temperatures ranging from ambient to 130.degree. C. Alternatively, phase transfer conditions may be employed to prepare the azide intermediate from (291) or (292). For example, a tetraalkylammonium azide in a non-polar aprotic solvent, such as tetrahydrofuran or toluene, or a crown ether and inorganic azide in biphasic mixtures of water and an immiscible solvent, such as benzene, toluene or xylene, can be stirred at room temperature or heated up to the reflux point of the selected solvent. The primary amines (293) and (294) are most conveniently obtained from the catalytic hydrogenation of the azide in an inert solvent, such as an alcohol, ethyl acetate or tetrahydrofuran with a transition metal catalyst such as platinum or palladium on carbon under an atmosphere of hydrogen gas. A variety of alternative methods are also useful and can be found in the monograph by Hudlicky (1984, pp. 76). The acid salt of the resulting amines (293) and (294) may be formed by the addition of one equivalent of the desired acid to the hydrogenation mixture. Phenylboric acid mediated hydrolysis of esters (293) and (294) gives the free boronic acid thrombin inhibitors (298) and (299), compounds of formula (I) of the invention.

Compounds containing a primary guanidine or N-alkyl guanidine functionality may be prepared by the alternative process outlined in Scheme 52. As illustrated with primary amine (293), the transformation to (295) is effected with a guanidinylation agent, such as an S-alkyl thiourea, aminoiminomethane sulfonic acid reported by Miller and Bischoff Synthesis 9, 777 (1986), cyanamide reported by Kettner et al. (1990) or their N-alkyl derivatives. This mixture is stirred at room temperature or higher with a base, such as potassium carbonate, triethylamine or N,N-dimethylaminopyridine in an inert solvent like water, alcohol, N,N-dimethylformamide or acetone. The guanidine boronic acid esters (295) can be deesterified to give the corresponding boronic acid (300) by the phenylboric acid procedure described above.

According to Scheme 53, the bromide (292) is converted to the corresponding alkylnitrile (302) upon exposure to the cyanide anion under a variety of conditions. ##STR77## Effective methods include the use of potassium or sodium cyanides in polar aprotic solvents, such as N,N-dimethylformamide, methylsulfoxide, acetone or ethylmethyl ketone, at temperatures ranging from ambient up to the reflux point of the selected solvent. More useful, however, are conditions employing phase transfer agents such as tetrabutylammonium cyanide in a nonpolar aprotic solvent such as tetrahydrofuran or toluene, or a biphasic mixture of a crown ether and an inorganic cyanide in water with an immiscible solvent like benzene, toluene or xylene. These mixtures can be stirred at ambient temperature or heated up to the reflux temperature of the selected solvent. An amidine like (303) is prepared by first treating nitrile (302) with a saturated solution of a mineral acid such as hydrogen chloride in an alcohol solvent at room temperature or lower. The intermediate O-alkylimidate can be exposed to ammonia, or a primary or secondary amine under anhydrous conditions with or without an inert solvent. As illustrated in Scheme 5, compound (303) is produced by treating the O-alkylimidate formed from (302) with neat anhydrous ammonia at reflux. The free boronic acid (304) is obtained by transesterification of (303) with phenylboric acid in a mixture of water and diethyl ether.

EXAMPLE 1

N.sup.1 -(4-Phenylbenzoyl)boroarginine (+)-Pinanediol, Bisulfite

Part A: (+)-Pinanediol 4-bromo-1(R)-(4-phenylbenzo-yl)-aminobutane-1-boronate.

To a solution of (+)-pinanediol 4-bromo-1(R)-aminobutane-1-boronate hydrochloride (5.00 g, 13.6 mmol) in dichloromethane (50 mL) at 0.degree. C. was added 4-phenylbenzoyl chloride (4.97 g, 22.9 mmol) followed by N-methylmorpholine (4 mL, 36 mmol). After 1 hour, the cooling bath was removed and the mixture stirred at room temperature for 2 hours. The mixture was then diluted with ethyl acetate and washed with 0.1M hydrochloric acid, saturated sodium bicarbonate and saturated sodium chloride. The organic phase was dried over anhydrous magnesium sulfate, filtered and the filtrate concentrated in vacuo to afford 3.37 g (48%) of the desired amide, mass spectrum: (M+H).sup.+ =510/512; .sup.1 H NMR (300 MHz, CDCl.sub.3) d7.9 (2H, d, J=8.3), 7.84 (1H, bs), 7.6 (2H, d, J=8.3), 7.44 (5H, m), 4.37 (1H, m), 3.41 (1H, t, J=6.9), 2.0 (10H, m) 1.49 (3H, s), 1.38 (1H, m), 1.29 (3H, s), 0.91 (3H, s).

Part B: (+)-Pinanediol 4-azido-1(R)-(4-phenylbenzo-yl)-aminobutane-1-boronate.

To a solution of (+)-pinanediol 4-bromo-1(R)-(4-phenylbenzoyl)aminobutane-1-boronate (3.37 g, 6.60 mmol) in dimethylformamide (6 mL) was added sodium azide (547 mg, 8.41 mmol). The resulting mixture was heated at 70.degree. C. for 2 hours, cooled to room temperature, and diluted with ethyl acetate. The mixture was then washed with water, saturated sodium chloride and dried over anhydrous magnesium sulfate. Filtration, followed by concentration of the filtrate in vacuo gave 3.04 g (97%) of the desired azide, mass spectrum: (M+H).sup.+ =473; .sup.1 H NMR (300 MHz, CDCl.sub.3) d7.89 (2H, d, J=8.3), 7.75 (1H, bs), 7.3 (7H, m), 4.32 (1H, m), 3.32 (1H, m), 2.0 (10H, m) 1.48 (3H, s), 1.3 (4H, m), 0.9 (3H, s).

Part C: N.sup.1 -(4-Phenylbenzoyl)boroarginine (+)-pinanediol, hydrochloride

To a solution of (+)-pinanediol 4-azido-1(R )--(4-phenylbenzoyl) aminobutane-1-boronate (3.04 g, 6.44 mmol) in methanol (30 mL) was added Pearlman's catalyst (Pd(OH).sub.2 /C, 200 mg) and 1M hydrochloric acid (6.5 mL, 6.5 mmol). The mixture was placed on a Parr apparatus and hydrogenated at 50 psi for 3 hours. The mixture was filtered using Celite.TM., washed with methanol and the filtrate concentrated in vacuo. The resulting amorphous solid was dissolved in water and washed with ether. The aqueous phase was then concentrated in vacuo and crystallized from ethyl acetate-hexanes, giving 1.52 g (49%) of the desired amine hydrochloride, mass spectrum: (M+H).sup.+ =447; mp: 157.degree.-170.degree. C.; .sup.1 H NMR (400 MHz, CDCl.sub.3 /DMSO-d.sub.6) d9.88 (1H, bs), 8.18, (2H, d, J=8.3), 8.13 (3H, bs), 7.68 (2H, d, J=8.3), 7.61 (2H, d J=7.0), 7.45 (2H, d, J=7.0), 7.37 (1H, d, J=7.30), 4.20 (1H, d, J=6.3), 2.99 (1H, m), 2.87 (2H, m), 2.31 (1H, m), 2.13 (1H, m), 1.84 (7H, m), 1.56 (1H, d, J=10.0), 1.42 (3H, s), 1.29 (3H, s), 0.89 (3H, s).

Part D: N.sup.1 -(4-Phenylbenzoyl)boroarginine (+)-pinanediol, bisulfite.

To a solution of

N.sup.1 -(4-phenylbenzoyl)boroarginine (+)-pinanediol, hydrochloride (80 mg, 0.17 mmol) in ethanol (2 mL) was added 4-dimethylaminopyridine (40 mg, 0.33 mmol). After 15 minutes, aminoiminomethanesulfonic acid (40 mg, 0.32 mmol) was added and the resulting mixture heated at reflux for 3 hours. After cooling to room temperature, the mixture was filtered and the filtrate concentrated in vacuo. The residue was dissolved in chloroform and washed with 0.1M hydrochloric acid, water and dried over anhydrous magnesium sulfate. Filtration, followed by concentration of the filtrate in vacuo afforded 73 mg (84%) of the desired guanidine, mass spectrum: (M+H).sup.+ =489; .sup.1 H NMR (400 MHz, CDCl.sub.3, 60.degree. C.) d9.48 (1H, bs), 8.10 (2H, d, J=8.1), 8.07 (1H, bs), 7.75 (1H, bs), 7.54 (2H, d, J=8.3), 7.48 (2H, d, J=7.0), 7.35 (3H, m), 7.06 (4H, bs), 4.19 (1H, bd, J=8.3), 3.1 (2H, m), 2.84 (1H, m), 2.29 (1H, m), 2.12 (1H, m), 1.96 (1H, m), 1.75 (6H, m), 1.47 (1H, d, J=10.2), 1.40 (3H, s), 1.24 (3H, s), 0.83 (3H, s).

EXAMPLE 34

(+)-Pinanediol 4-(Formamidino)Thio-1(R)-(4-Phenylbenzoyl)Aminobutane-1-Boronate, Hydrobromide

(+)-Pinanediol 4-(formamidino)thio-1(R)-(4-phenylbenzoyl)aminobutane-1-boronate, hydrobromide.

To a solution of (+)-pinanediol 4-bromo-1(R)-(4-phenyl-benzoyl)aminobutane-1-boronate (200 mg, 0.392 mmol) in methanol (3 mL) was added thiourea (120 mg, 1.58 mmol). The reaction was stirred at room temperature for 3 days. The mixture was concentrated in vacuo, the residue dissolved in water and washed with ether. Concentration of the aqueous portion afforded 80 mg (35%) of the desired isothiourea, mass spectrum: (M+H).sup.+ =506; .sup.1 H NMR (300 MHz, CDCl.sub.3) d8.15 (2H, d, J=8.4), 7.61 (2H, d, J=8.4), 7.52 (2H, m), 7.38 (3H, m), 6.47 (1H, bs), 4.23 (1H, dd, J=6.6, 1.9), 3.24 (1H, m), 3.14, (1H, m), 2.96, (1H, m), 2.32 (1H, m), 2.15 (1H, m), 1.99 (1H, m), 1.78 (6H, m), 1.48 (1H, d, J=10.1), 1.42 (3H, s), 1.27 (3H, s), 0.86 (3H, s). ##STR78##

EXAMPLE 898

R-N.sup.1 -(3-Cyanomethyl-5-phenylmethyl-1,2,4-triazol-1-yl)acetyl-borolysine, (+)-pinanediol ester, hydrochloride; X=--CH.sub.2 NH.sub.2, R.sup.13 =--CH.sub.2 Ph, R.sup.14 =--CH.sub.2 CN, Y.sup.1, Y.sub.2 =(+)-pin ##STR79## Part A. Ethyl benzylimidate, hydrochloride.

HCl gas (17.1 g, 469 mmol, 1.1 eq) was slowly bubbled into a solution of phenylacetonitrile (50.00 g, 427 mmol, 1 eq) in ethanol (27.6 mL, 469 mmol, 1.1 eq) at 0.degree. C. The reaction was put into the refrigerator over the weekend. After warming to room temperature, ether (300 mL) was added to the reaction mixture which had solidified and the contents were vigorously stirred at 0.degree. C. to pulverize the mixture. The solid material was filtered while cold under an inert atmosphere and the filter cake rinsed with some more ether. The product was dried under high vacuum to yield 60.0 g (mp 94.0.degree.-95.0.degree. C.) of a white solid. A second crop yielded 20.98 g (96.0.degree.-97.5.degree. C.). ##STR80## Part B. 3-Cyanomethyl-5-phenylmethyl-1,2,4-triazole.

The imidate from part A (14.92 g, 91 mmol, 1 eq) was dissolved in ethanol (250 mL) and cooled to 0.degree. C. under an inert atmosphere. Cyanoacetohydrazide (9.06 g, 91 mmol, 1 eq) dissolved as best possible in warm ethanol was added, and the resultant mixture stirred at room temperature overnight. The mixture was filtered, and the filtrate concentrated to yield a gummy orange solid. Trituration from hexanes yielded 19.72 g of solid product acylamidrazone (MS detects (M+H).sup.+ =216). This intermediate was heated neat (oil bath) at 170.degree. C. under an inert atmosphere for 0.5 h to crack out water. The product was cooled to room temperature and dissolved in ethyl acetate. The solvent was dried (MgSO4) and stripped to yield 11.89 g of an orange solid. Flash chromatography over silica gel in solvent systems consisting of 3:1 pentane/ethyl acetate to 100% ethyl acetate to 4:1 chloroform/methanol yielded 6.76 g (38%) of a light pink solid product; m.p.=140.0.degree.-142.5.degree. C. NMR (DMSO-d.sub.6) .delta. 14.00-13.60 (bs, 1H); 7.40-7.10 (m, 5H); 4.08 (s, 2H); 4.05 (s, 2H). MS: (M+H).sup.+ =199. ##STR81## Part C. Ethyl (3-cyanomethyl-5-phenylmethyl-1,2,4-triazol-1-yl)acetate.

The compound from part B (3.36 g, 17 mmol, 1 eq) was added portionwise to a mixture of DMF and 50% NaH (0.81 g, 17 mmol, 1 eq) at 25.degree. C. After H.sub.2 evolution had ceased, the mixture was heated a little with a heat gun to ensure complete deprotonation. The mixture was cooled to 0.degree. C. and ethyl bromoacetate (1.88 mL, 17 mmol, 1 eq ) was added. The reaction was allowed to warm to room temperature and was stirred overnight. Ethyl acetate was added and the mixture washed with water (5.times.) to remove the DMF. The organic layer was dried (MgSO.sub.4) and stripped to yield 6.10 g of a reddish oil. Flash chromatography in 3:1 hexanes/ethyl acetate to 1:1 hexanes/ethyl acetate yielded 2.93 g of an amber oil which consisted of a 4:1 mixture of regioisomers as determined by NMR with the major isomer being depicted above. NMR (major isomer) (CDCl.sub.3) .delta. 7.40-7.20 (m, 5H); 4.68 (s, 2H); 4.25-4.05 (m, 4H); 3.84 (s, 2H); 1.23 (t, 3H, J=7 Hz). ##STR82## Part D. (3-Cyanomethyl-5-phenylmethyl-1,2,4-triazol-1-yl)acetate acid.

The product of part C (1.00g, 3.52 mmol, 1 eq), 1.000N NaOH (7.03 mL, 7.03 mmol, 2 eq) and methanol (10 mL) were mixed and stirred at room temperature. After 24 h, the methanol was stripped and the aqueous mixture washed with ether (2x). The aqueous layer was then acidified with conc. HCl and extracted with ethyl acetate (3.times.). The organic layers were combined, dried (MgSO.sub.4) and stripped to yield 0.66 g of an off-white glass. MS (M+H).sup.+ =257. ##STR83## Part E. (+)-Pinanediol 5bromo-1(R)-((3-Cyanomethyl-5-phenylmethyl-1,2,4-triazol-1-yl)acetamido)pentane-1-boronate.

N-methylmorpholine (0.42 mL, 3.86 mmol, 1.5 eq) was added to a solution of the product in part D (0.66 g, 2.58 mmol, 1 eq) in THF at 25.degree. C. The mixture was cooled to -20.degree. C. and isobutylchloroformate (0.50 mL, 3.86 mmol, 1.5 eq) in THF was added dropwise. In a seperate flask, pinanediol 5-bromo-1-R-aminopentane-1-boronate hydrochloride (0.98 g, 2.58 mmol, 1 eq) was dissolved in CHCl.sub.13 and cooled to -78.degree. C. Triethylamine (0.36 mL, 2.58 mmol, 1 eq) was then added and the mixture syringed immediately into the reaction flask with the mixed anhydride. The reaction was allowed then to warm to room temperature overnight. The next day, the precipitate was filtered off and the solids were rinsed with THF. The filtrate was stripped to yield 410 mg of a white oil. Flash chromatography over silica gel in solvent systems consisting of 3:1 pentane/ethyl acetate to 100% ethyl acetate to 4:1 chloroform/methanol yielded 300 mg of a clear, colorless viscous oil and only one regioisomer by NMR. MS (M+H).sup.+ =633 and 635. NMR (CDCl.sub.3) .delta. 7.40-7.10 (m, 5H); 6.13 (d, 1H, J=6 Hz); 4.62 (s, 2H); 4.40-4.20 (m, 1H); 4.17 (s, 2H); 3.86 (s, 1H); 3.50-3.20 (m, 3H); 2.40-2.10 (m, 2H); 2.10-1.75 (m, 4H); 1.75-1.10 (m, 13 H); 0.83 (s, 3H). ##STR84## Part F. (+)-Pinanediol 5bromo-1(R)-((3-Cyanomethyl-5-phenylmethyl-1,2,4-triazol-1-yl)acetamido)pentane-1-boronate.

The product from Part E (300 mg, 0.52 mmol, 1 eq), sodium azide (1.03 mmol, 2 eq), and DMSO (5 mL) were mixed and stirred at room temperature under an inert atmosphere for 24 h. Ethyl acetate was added and the mixture rinsed with water (5.times.). The ethyl acetate layer was dried (MgSO.sub.4) and stripped to yield 256 mg of a light amber oil. IR (neat).sub.2096 cm-1. NMR (CDCl3) .delta. 7.40-7.10 (m, 5H); 6.15 (d, 1H, J=6 Hz); 4.62 (s, 2H); 4.40-4.20 (d of d, 1H, J=7, 2 Hz); 4.20-4.10 (m, 2H); 3.85 (s, 2H); 3.40-3.10 (m, 3H); 2.50-1.40 (m, 9H); 1.40-1.00 (m, 9 H); 0.84 (s, 3H). ##STR85## Part G. (+)-Pinanediol 5bromo-1(R)-((3-Cyanomethyl-5-phenylmethyl-1,2,4-triazol-1-yl)acetamido)pentane-1-boronate, hydrochloride salt.

The product from Part F (250 mg, 0.46mmol, 1 eq) and triphenylphosphine (157 mg, 0.6 mmol, 1.3 eq) and THF (5 mL) were mixed and stirred at room temperature. After 1 h, water (11 .mu.M, 0.6 mmol, 1.3 eq) was added and the mixture stirred overnight. After 24 h, the reaction was not finished, and thus 1.3 eq more equivalents of water were added and the reaction stirred for another 24 h. The reaction was now complete and 1 equivalent of 1.000N HCl was added. The reaction was then stripped and water was added and the reaction again stripped. Ethyl ether was added and the mixture stripped once more. The residue was dried under high vacuum to yield 138 mg of a white glass. MS detects (M+H).sup.+ =519 and 385 (minus pinanediol). Mass calculated for C.sub.28 H.sub.40 BN.sub.6 O.sub.3 : 519.3255. Found: 519.3274. NMR shows a 1:1 mixture of pinanediol ester and free boronic acid. ##STR86##

EXAMPLE 908

R-N.sup.1 -(3-(1H-tetrazol-5-yl)methyl-5-phenylmethyl-1,2,4-triazol-1-yl)acetyl-borolysine, (+)-pinanediol ester, hydrochloride; X=--CH.sub.2 NH.sub.2, R.sup.13 =--CH.sub.2 Ph, R.sup.14 =--CH.sub.2 --(CN.sup.4 H), Y.sup.1, Y.sup.2 =(+)-pin ##STR87## Part A. Ethyl (3)-N-triphenylmethyl)-1H-tetrazol-5-methyl-5-phenylmethyl-1,2,4-triazol-1-yl)acetate

The product from Example 360, part C (1.83 g, 6.44 mmol, 1 eq), tributyltin chloride (1.75 mL, 6.44 mmol, 1 eq), sodium azide (0.42 g, 6.44 mmol, 1 eq), and xylenes (15 mL) were mixed and refluxed for 24 h under an inert atmosphere. The mixture was cooled to room temperature and pyridine was then added (0.57 mL, 7.08 mmol, 1.1 eq) followed after 0.5 h by trityl chloride (1.97 g, 7.08 mmol, 1.1 eq). The following day, the reaction was worked up by adding ethyl ether and rinsing the mixture with water (3.times.). The ether layer was dried (MgSO4), and stripped to yield 5.66 g of an amber oil. Flash chromatography in 3:1 pentane/ethyl acetate to 100% ethyl acetate over silica gel yielded 1.33 g of an amber oil which eventually crystallized. MS detects (M+H).sup.+ =570 and 328 (M+H--CPh.sub.3).sup.+. ##STR88## Part B. (3)-N-Triphenylmethyl)-1H-tetrazol-5-yl)methyl-5-phenylmethyl-1,2,4-triazol-1-yl)acetic acid.

The product from part A (200 mg, 0.35 mmol, 1 eq), 1,000N NaOH (0.39 mL, 0.39 mmol, 1.1 eq) and THF (5 mL) were mixed and stirred at room temperature under an inert atmosphere for 24 h. The reaction was not finished and thus 0.5 eq more of 1,000N NaOH were added and stirred overnight. Water was then added and the pH adjusted to 5 with 1N HCl . The mixture was stripped to dryness. THe residue was stirred in ethyl acetate. Some solids were filtered and the filtrate was stripped to yield 190 mg of a white glass. NMR (CDCl.sub.3) .delta. 7.40-7.15 (m, 12 H); 7.15-7.00 (m, 8 H); 4.55 (s, 2); 4.40 (s, 2H); 4.10 (s, 2H). ##STR89## Part C. (+)-Pinanediol 5-azido-1(R)-((3-N-triphenylmethyl)-1H-tetrazol-5-ylmethyl-)5-phenylmethyl1,2,4-triazol-1-yl)acetamido)pentane-1-boronate.

The compound in part B was converted to the corresponding azidoboronic acid pinanediol ester by the methods disclosed in example 360, parts E and F. IR (neat) 2095 cm.sup.-1. NMR (CDCl.sub.3) .delta. 7.45-7.20 (m, 12H); 7.17 (d, 2H, J=7 Hz); 7.12 (d, 6H, J=7 Hz); 6.34 (d, 1H, J=6 Hz); 4.60 (s, 2H); 4.42 (s, 2H); 4.27 (d, 1H, J=7 Hz); 3.13 (t, 2H, J=2 Hz); 3.06 (q, 1H, J=7 Hz); 2.40-2.10 (m, 2H); 2.01 (t, 1H, J=6 Hz); 1.95-1.70 (m, 2H); 1.60-1.40 (m, 4H); 1.37 (s, 3H); 1.35-1.20 (m, 5H); 1.16 (d, 1H, J=11 Hz); 0.82 (s, 3H). MS detects (M+H).sup.+ =830 and (M+H--CPh.sub.3).sup.+ =588. ##STR90## Part D. R-N.sup.1 -(3-(1H-tetrazol-5-yl)methyl-5-phenylmethyl-1,2,4-triazol-1-yl)acetyl-borolysine, (+)-pinanediol ester, hydrochloride.

The product from part C (135 mg, 0.16 mmol, 1 eq), 10% Pd on carbon (25 mg), chloroform (39 .mu.L, 0.49 mmol, 3 eq) and methanol (5 mL) were mixed and stirred under hydrogen under balloon pressure for 24 h at room temperature. The mixture was filtered through a Celite.RTM. cake rinsing the cake well with methanol afterwards. The filtrate was stripped to yield an off-white glass. This glass was triturated with ethyl ether to yield after drying 50 mg of an off-white solid. Mass calcd. for C.sub.28 H.sub.41 BN.sup.9 O.sub.3 : 562.3425. Found: 562.3413. NMR (DMSO-d.sub.6) .delta. 8.75-8.50 (m, 1H); 7.40-7.10 (m, 5H); 4.87 (bs, 2H); 4.30-4.00 (m, 5H); 2.96-2.60 (m, 3H); 2.40-2.00 (m, 2H); 1.91 (t, 1H, J=6 Hz); 1.90-1.75 (m, 1H); 1.75-1.10 (m, 14 H); 0.80 (s, 3H). ##STR91##

EXAMPLE 3458

R-N.sup.1 -((2-phenyl-4-methylpyrimidin-5-yl)carbonyl)borolysine, (+)-pinanediol ester, hydrochloride; X=--CH.sub.2 NH.sub.2, R.sup.13 =--Ph, R.sup.14 =--CH.sub.3, R.sup.15 =H, Y.sup.1, Y.sup.2 =(+)-pin ##STR92## Part A. 2-Phenyl-4-methylpyrimidin-5-carboxylic acid.

The above compound was synthesized by the procedure of P. Schenone, L. Sansebastiano, L. Mosti J. Heterocyclic Chem. 1990, 27, 302 which is generally applicable to a wide variety of pyrimidine-5-carboxylic acids.

Part B. R-N.sup.1 -((2-phenyl-4-methylpyrimidine-5-yl)carbonyl)borolysine, (+)-pinanediol ester, hydrochloride.

The product was obtained using the procedures described in example 360, parts E and F and example 361, part D followed by prepatory TLC in 4:1 chloroform/methanol. (M+H).sup.+ =477. NMR (DMSO-d.sub.6) .delta. 8.86 (s, 1H); 8.50-8.30 (m, 2H); 7.70-7.40 (m, 3H); 4.25 (d, 1H, J=7 Hz); 2.90-2.70 (m, 3H); 2.64 (s, 3H); 2.40-1.00 (m, 15H); 0.84 (s, 3H). ##STR93##

EXAMPLE 3538

R-N.sup.1 -((2-phenyl-4-methylpyrimidin-5-yl)carbonyl)boroarginine, (+)-pinanediol ester, hydrochloride; X=--NH (C.dbd.NH) NH.sub.2, R.sup.13 =--Ph, R.sup.14 =--CH.sub.3, R.sup.15 =H, Y.sup.1, Y.sup.2 =(+)-pin ##STR94## Part A. R-N.sup.1 -((2-phenyl-4-methylpyrimidin-5-yl)carbonyl)boroarginine, (+)-pinanediol ester, hydrochloride.

The above intermediate was synthesized by the procedures described for example 361 using the appropriate starting materials.

Part B. R-N.sup.1 -((2-phenyl-4-methylpyrimidin-5-yl)carbonyl)boroarginine, (+)-pinanediol ester, hydrochloride.

The product from part A (500 mg, 1 mmol, 1 eq), formamidinesulfonic acid (224 mg, 1.8 mmol, 2 eq), 4-(N,N-dimethylamino)pyridine (220 mg, 1.8 mmol, 2 eq, and ethanol (20 mL) were mixed and refluxed under an inert atmosphere for 5 hours. Some solid material was filtered and the filtrate was stripped to yield a yellow glass. The glass was taken up in chloroform/0.1N HCl. Solids precipitated. These were filtered and dried to yield 144 mg of product as a white powder: mp 132.degree. C. (dec.). (M+H).sup.+= 505.

Mass calcd. for C.sub.27 H.sub.38 BN.sub.6 O.sub.3 : 505.3086. Found: 505.3098. NMR (DMSO-d.sub.6) .delta. 8.89 (s, 1H); 8.60-8.40 (m, 2H); 8.05-7.80 (m, 1H); 7.65-7.40 (m, 3H); 7.40-6.80 (m, 3H); 4.19 (d, 1H, J=7 HZ); 3.60-3.20 (m, 3H); 2.85-2.40 (m, 4H); 2.40-1.95 (m, 1H); 1.95-1.00 (m, 16 H); 0.80 (t, 3H). ##STR95##

EXAMPLE 5926

N.sup.1 -�(4R)-2-(2-Phenyl)ethyl-Thiazoline-4-Carboxy!-R-borothioarginine-(+)-pinanediol ester

Part A. (4R )-2-(2-phenyl)-thiazoline-4-carboxylic acid ethyl ester.

Cysteine ethyl ester hydrochloride (950 mg, 5.10 mmol) was added to a solution of ethyl (2-phenyl)ethylimidate (900 mg, 5.10 mmol) �prepared by the method of North, M.; Pattenden, G. Tetrahedron 1990, 46, 8267! in EtOH (20 mL) at room temperature. The reaction mixture was stirred for 16 h and concentrated under reduced pressure. The residue was partitioned between H.sub.2 O (ca. 50 mL) and EtOAc (ca. 100 mL) and the layers were separated; the aqueous phase was extracted with EtOAc (1.times.20 mL). The combined organic layers were washed with saturated aqueous NaCl.sub.1 (1.times.50 mL), dried (Na.sub.2 SO.sub.4), and concentrated under reduced pressure to give an oil which was purified by flash chromatography, elution with 3:1 hexanes--EtOAc, to afford 885 mg (66%) of the title compound as a colorless oil. .sup.1 H NMR (300 MHz, CDCl.sub.3) .delta. 7.23 (comp, 5H), 5.05 (dd, 1H, J=9.5, 9.1 Hz), 4.27 (dq, 2H, J=7.0, 1.8 Hz), 3.55 (m, 2H), 2.97 (m, 2H), 2.86 (m, 2H), 1.32 (t, 3H, J=7.0 Hz); LRMS 264 (M+1, base).

Part B. (4R)-2-(2-phenyl)ethyl-thiazoline-4carboxylic acid.

A solution of lithium hydroxide monohydrate (96 mg, 2.28 mmol) in H.sub.2 O (2 mL) was added to a solution of (4R)-2-(2-phenyl)ethyl-thiazoline-4-carboxylic acid ethyl ester (400 mg, 1.52 mmol) in THF (8 mL) and MeOH (5 mL). The reaction mixture was stirred at room temperature for 1 h at which time 2M aqueous HCl was added until pH=2 and the aqueous phase was extracted with EtOAc (2-30 mL). The combined organic layers were washed with saturated aqueous NaCl (1-20 mL), dried (MgSO.sub.4), and concentrated under reduced pressure to give 340 mg (95%) of the title compound as an oil. .sup.1 H NMR (300 MHz, CDCl.sub.3) .delta. 7.22 (comp, 5H), 6.86 (br s, 1H), 5.14 (dd, 1H, J=9.5, 9.1 Hz), 3.64 (m, 2H), 2.96 (comp, 4H); LRMS 236 (M+1, base).

Part C. (1R)-4-Bromo-1-�(4R)-2-(2-Phenyl)ethyl-thiazoline-4carbox!amido-1-boronic acid-(+)-pinanediol ester.

A solution of (4R)-2-(2-phenyl)ethyl-thiazoline-4-carboxylic acid (335 mg, 1.43 mmol) and 4-methylmorpholine (0.47 mL, 4.28 mmol) in 10 mL of anhydrous THF at -20.degree. C. was treated with i--butyl chloroformate (0.20 mL, 1.57 mmol) and stirred for 2 min after which a solution of (1R)-4-bromoaminobutane-1-boronic acid (+)-pinanediol ester (522 mg, 1.43 mmol) in 4 mL of anhydrous DMF was added. The reaction mixture was stirred at -20.degree. C. for 15 min, warmed to room temperature over 18 h then poured into EtOAc (ca. 100 mL) and washed with H.sub.2 O (3-25 mL), and saturated aqueous NaCl (1-25 mL), dried (Na.sub.2 SO.sub.4) and concentrated under reduced pressure. The residue was purified by flash chromatography, elution with 3:2 hexanes--EtOAc, to give 306 mg (39%) of the title compound as an oil. LRMS 549, 547 (M+1, base).

Part D. N.sup.1 -�(4R -2-2-Phenyl)ethyl-Thiazoline-4-Carboxy!-R-borothioarginine-(+)-pinanediol ester.

A mixture of (1R)-4-bromo-1-�(4R)-2-(2 -phenyl)ethyl-thiazoline-4-carbox!amido-1-boronic acid (+)-pinanediol ester (295 mg, 0.54 mmol) and thiourea (82 mg, 1.08 mmol) in 10 mL of EtOH was heated at reflux for 14 h then cooled to room temperature and concentrated under reduced pressure. The residue was purified by size exclusion chromatography on Sephadex LH-20, elution with MeOH, to give a glass which was dissolved in 3 mL of THF and treated with Et.sub.2 O (ca. 10 mL) to give a solid that was washed with Et.sub.2 O (ca. 5 mL) and dried to afford 230 mg (68%) of the title compound. LRMS 543 (M+1, base); HRMS Calcd for C.sub.27 H.sub.40 BN.sub.4 O.sub.3 S.sub.2 : 543.2635. Found: 543.2643.

The compounds in the following tables were or can be synthesized by the methods discussed previously or by methods familiar to one skilled in the art.

The compounds listed in Tables 1-61 may be prepared using the above examples. It is understood that R.sup.14-16 and R.sup.A-C in the tables correspond to independent R13 groups as described within the scope of this application.

TABLE 1__________________________________________________________________________ ##STR96##Ex X R.sup.A R.sup.B R.sup.C Y.sup.1, Y.sup.2 Phys Data__________________________________________________________________________1 NHC(NH)NH.sub.2 H H Ph (+)-pin A2 NHC(NH)NH.sub.2 H Ph H (+)-pin BZ3 NHC(NH)NH.sub.2 H OPh Ph (+)-pin B4 NHC(NH)NH.sub.2 H H 4-pyridyl (+)-pin C5 NHC(NH)NH.sub.2 COPh H H (+)-pin6 NHC(NH)NH.sub.2 H COPh H (+)-pin7 NHC(NH)NH.sub.2 H H COPh (+)-pin8 NHC(NH)NH.sub.2 H NHCbz H (+)-pin9 NHC(NH)NH.sub.2 H NMeCbz H (+)-pin10 NHC(NH)NH.sub.2 H H Et (+)-pin11 NHC(NH)NH.sub.2 H H n-Pr (+)-pin12 NHC(NH)NH.sub.2 H H i-Pr (+)-pin13 NHC(NH)NH.sub.2 H H n-Bu (+)-pin14 NHC(NH)NH.sub.2 H H t-Bu (+)-pin15 NHC(NH)NH.sub.2 H H n-hexyl (+)-pin16 NHC(NH)NH.sub.2 H H cyclohexyl (+)-pin17 NHC(NH)NH.sub.2 NHCO(CH.sub.2).sub.2 Ph H H (+)-pin18 NHC(NH)NH.sub.2 H H O-n-Bu (+)-Pin19 NHC(NH)NH.sub.2 H H NHCOcyclopropyl (+)-pin20 NHC(NH)NH.sub.2 H H NHCO-cyclohexyl (+)-pin21 NHC(NH)NH.sub.2 H H NHCO(4-C.sub.6 H.sub.4 OMe) (+)-pin22 NHC(NH)NH.sub.2 H H 4-C.sub.6 H.sub.4 OMe (+)-pin23 NHC(NH)NH.sub.2 CO.sub.2 CH.sub.2 (2-C.sub.6 H.sub.4 Ph) H H (+)-pin24 NHC(NH)NH.sub.2 H H 1-naphthyl (+)-pin25 NHC(NH)NH.sub.2 H H 4-C.sub.6 H.sub.4 CO.sub.2 H (+)-pin26 NHC(NH)NH.sub.2 COPh H Me (+)-pin27 NHC(NH)NH.sub.2 H NHCbz n-Bu (+)-pin28 NHC(NH)NH.sub.2 H NMeCbz n-Bu (+)-pin29 NHC(NH)NH.sub.2 Me H Ph (+)-pin CB30 NHC(NH)NH.sub.2 Me H 4-C.sub.6 H.sub.4 CO.sub.2 H (+)-pin31 NHC(NH)NH.sub.2 H H 4-C.sub.6 H.sub.4 CO.sub.2 Me (+)-pin32 NHC(NH)NH.sub.2 Me H 4-C.sub.6 H.sub.4 CO.sub.2 Me (+)-pin33 NHC(NH)NH.sub.2 H OMe Ph (+)-pin34 SC(NH)NH.sub.2 H H Ph (+)-pin D35 SC(NH)NH.sub.2 H Ph H (+)-pin E36 SC(NH)NH.sub.2 H OPh H (+)-pin F37 SC(NH)NH.sub.2 COPh H H (+)-pin G38 SC(NH)NH.sub.2 H COPh H (+)-pin H39 SC(NH)NH.sub.2 H H COPh (+)-pin I40 SC(NH)NH.sub.2 H NHCbz H (+)-pin J41 SC(NH)NH.sub.2 H NMeCbz H (+)-pin K42 SC(NH)NH.sub.2 H H Et (+)-pin L43 SC(NH)NH.sub.2 H H n-Pr (+)-pin M44 SC(NH)NH.sub.2 H H i-Pr (+)-pin N45 SC(NH)NH.sub.2 H H n-Bu (+)-pin O46 SC(NH)NH.sub.2 H H t-Bu (+)-pin P47 SC(NH)NH.sub.2 H H n-hexyl (+)-pin Q48 SC(NH)NH.sub.2 H H cyclohexyl (+)-pin R49 SC(NH)NH.sub.2 NHCOCH.sub.2 CH.sub.2 Ph H H (+)-pin S50 SC(NH)NH.sub.2 H H O-n-Bu (+)-pin P51 SC(NH)NH.sub.2 H H NHCOcyclopropyl (+)-pin U52 SC(NH)NH.sub.2 H H NHCOcyclohexyl (+)-pin V53 SC(NH)NH.sub.2 H H NHCO(4-C.sub.6 H.sub.4 OMe) (+)-pin W54 SC(NH)NH.sub.2 H H 4-C.sub.6 H.sub.4 OMe (+)-pin X55 SC(NH)NH.sub.2 CO.sub.2 CH.sub.2 (2-C.sub.6 H.sub.4 Ph) H H (+)-pin Y56 SC(NH)NH.sub.2 H H 1-naphthyl (+)-pin57 SC(NH)NH.sub.2 H H 4-C.sub.6 H.sub.4 CO.sub.2 H (+)-pin58 SC(NH)NH.sub.2 H NHCbz n-Bu (+)-pin Z59 SC(NH)NH.sub.2 H NMeCbz n-Bu (+)-pin AA60 SC(NH)NH.sub.2 COPh H Me (+)-pin BB61 SC(NH)NH.sub.2 H H 4-pyridyl (+)-pin62 SC(NH)NH.sub.2 Me H 4-C.sub.6 H.sub.4 CO.sub.2 H (+)-pin63 SC(NH)NH.sub.2 H H 4-C.sub.6 H.sub.4 CO.sub.2 Me (+)-pin64 SC(NH)NH.sub.2 Me H 4-C.sub.6 H.sub.4 CO.sub.2 Me (+)-pin65 SC(NH)NH.sub.2 Me H Ph (+)-pin66 SC(NH)NH.sub.2 H OMe Ph (+)-pin67 CH.sub.2 NH.sub.2 H H Ph (+)-pin68 CH.sub.2 NH.sub.2 H Ph H (+)-pin YY69 CH.sub.2 NH.sub.2 H OPh H (+)-pin70 CH.sub.2 NH.sub.2 COPh H H (+)-pin71 CH.sub.2 NH.sub.2 H COPh H (+)-pin72 CH.sub.2 NH.sub.2 H H COPh (+)-pin73 CH.sub.2 NH.sub.2 H NHCbz H (+)-pin74 CH.sub.2 NH.sub.2 H NMeCbz H (+)-pin75 CH.sub.2 NH.sub.2 H H Et (+)-pin76 CH.sub.2 NH.sub.2 H H n-Pr (+)-pin77 CH.sub.2 NH.sub.2 H H i-Pr (+)-pin78 CH.sub.2 NH.sub.2 H H n-Bu (+)-pin79 CH.sub.2 NH.sub.2 H H t-Bu (+)-pin80 CH.sub.2 NH.sub.2 H H n-hexyl (+)-pin81 CH.sub.2 NH.sub.2 H H cyclohexyl (+)-pin82 CH.sub.2 NH.sub.2 NHCOCH.sub.2 CH.sub.2 Ph H H (+)-pin83 CH.sub.2 NH.sub.2 H H O-n-Bu (+)-pin84 CH.sub.2 NH.sub.2 H H NHCOcyclopropyl (+)-pin85 CH.sub.2 NH.sub.2 H H NHCOcyclohexyl (+)-pin86 CH.sub.2 NH.sub.2 H H NHCO(4-C.sub.6 H.sub.4 OMe) (+)-pin87 CH.sub.2 NH.sub.2 H H 4-C.sub.6 H.sub.4 OMe (+)-pin88 CH.sub.2 NH.sub.2 CO.sub.2 CH.sub.2 (2-C.sub.6 H.sub.4 Ph) H H (+)-pin89 CH.sub.2 NH.sub.2 H H 1-naphthyl (+)-pin90 CH.sub.2 NH.sub.2 H H 4-C.sub.6 H.sub.4 CO.sub.2 H (+)-pin91 CH.sub.2 NH.sub.2 H NHCbz n-Bu (+)-pin92 CH.sub.2 NH.sub.2 H NMeCbz n-Bu (+)-pin93 CH.sub.2 NH.sub.2 COPh H Me (+)-pin94 CH.sub.2 NH.sub.2 H H 4-pyridyl (+)-pin95 CH.sub.2 NH.sub.2 Me H 4-C.sub.6 H.sub.4 CO.sub.2 H (+)-pin96 CH.sub.2 NH.sub.2 H H 4-C.sub.6 H.sub.4 CO.sub.2 Me (+)-pin97 CH.sub.2 NH.sub.2 Me H 4-C.sub.6 H.sub.4 CO.sub.2 Me (+)-pin98 CH.sub.2 NH.sub.2 Me H Ph (+)-pin99 CH.sub.2 NH.sub.2 H OMe Ph (+)-pin100 CH.sub.2 NH.sub.2 H OMe Ph OH, OH101 NHC(NH)NH.sub.2 H H Ph OH, OH102 NHC(NH)NH.sub.2 H Ph H OH, OH103 NHC(NH)NH.sub.2 H OPh Ph OH, OH104 NHC(NH)NH.sub.2 H H 4-pyridyl OH, OH105 NHC(NH)NH.sub.2 COPh H H OH, OH106 NHC(NH)NH.sub.2 H COPh H OH, OH107 NHC(NH)NH.sub.2 H H COPh OH, OH108 NHC(NH)NH.sub.2 H NHCbz H OH, OH109 NHC(NH)NH.sub.2 H NMeCbz H OH, OH110 NHC(NH)NH.sub.2 H H Et OH, OH111 NHC(NH)NH.sub.2 H H n-Pr OH, OH112 NHC(NH)NH.sub.2 H H i-Pr OH, OH113 NHC(NH)NH.sub.2 H H n-Bu OH, OH114 NHC(NH)NH.sub.2 H H t-Bu OH, OH115 NHC(NH)NH.sub.2 H H n-hexyl OH, OH116 NHC(NH)NH.sub.2 H H cyclohexyl OH, OH117 NHC(NH)NH.sub.2 NHCO(CH.sub.2).sub.2 Ph H H OH, OH118 NHC(NH)NH.sub.2 H H O-n-Bu OH, OH119 NHC(NH)NH.sub.2 H H NHCOcyclopropyl OH, OH120 NHC(NH)NH.sub.2 H H NHCO-cyclohexyl OH, OH121 NHC(NH)NH.sub.2 H H NHCO(4-C.sub.6 H.sub.4 OMe) OH, OH122 NHC(NH)NH.sub.2 H H 4-C.sub.6 H.sub.4 OMe OH, OH123 NHC(NH)NH.sub.2 CO.sub.2 CH.sub.2 (2-C.sub.6 H.sub.4 Ph) H H OH, OH124 NHC(NH)NH.sub.2 H H 1-naphthyl OH, OH125 NHC(NH)NH.sub.2 H H 4-C.sub.6 H.sub.4 CO.sub.2 H OH, OH126 NHC(NH)NH.sub.2 COPh H Me OH, OH127 NHC(NH)NH.sub.2 H NHCbz n-Bu OH, OH128 NHC(NH)NH.sub.2 H NMeCbz n-Bu OH, OH129 NHC(NH)NH.sub.2 Me H Ph OH, OH CD130 NHC(NH)NH.sub.2 Me H 4-C.sub.6 H.sub.4 CO.sub.2 H OH, OH131 NHC(NH)NH.sub.2 H H 4-C.sub.6 H.sub.4 CO.sub.2 Me OH, OH132 NHC(NH)NH.sub.2 Me H 4-C.sub.6 H.sub.4 CO.sub.2 Me OH, OH133 NHC(NH)NH.sub.2 H OMe Ph OH, OH134 SC(NH)NH.sub.2 H H Ph OH, OH135 SC(NH)NH.sub.2 H Ph H OH, OH136 SC(NH)NH.sub.2 H OPh H OH, OH137 SC(NH)NH.sub.2 COPh H H OH, OH138 SC(NH)NH.sub.2 H COPh H OH, OH139 SC(NH)NH.sub.2 H H COPh OH, OH140 SC(NH)NH.sub.2 H NHCbz H OH, OH141 SC(NH)NH.sub.2 H NMeCbz H OH, OH142 SC(NH)NH.sub.2 H H Et OH, OH143 SC(NH)NH.sub.2 H H n-Pr OH, OH144 SC(NH)NH.sub.2 H H i-Pr OH, OH145 SC(NH)NH.sub.2 H H n-Bu OH, OH146 SC(NH)NH.sub.2 H H t-Bu OH, OH147 SC(NH)NH.sub.2 H H n-hexyl OH, OH148 SC(NH)NH.sub.2 H H cyclohexyl OH, OH149 SC(NH)NH.sub.2 NHCOCH.sub.2 CH.sub.2 Ph H H OH, OH150 SC(NH)NH.sub.2 H H O-n-Bu OH, OH151 SC(NH)NH.sub.2 H H NHCOcyclopropyl OH, OH152 SC(NH)NH.sub.2 H H NHCOcyclohexyl OH, OH153 SC(NH)NH.sub.2 H H NHCO(4-C.sub.6 H.sub.4 OMe) OH, OH154 SC(NH)NH.sub.2 H H 4-C.sub.6 H.sub.4 OMe OH, OH155 SC(NH)NH.sub.2 CO.sub.2 CH.sub.2 (2-C.sub.6 H.sub.4 Ph) H H OH, OH156 SC(NH)NH.sub.2 H H 1-naphthyl OH, OH157 SC(NH)NH.sub.2 H H 4-C.sub.6 H.sub.4 CO.sub.2 H OH, OH158 SC(NH)NH.sub.2 H NHCbz n-Bu OH, OH159 SC(NH)NH.sub.2 H NMeCbz n-Bu OH, OH160 SC(NH)NH.sub.2 COPh H Me OH, OH161 SC(NH)NH.sub.2 H H 4-pyridyl OH, OH162 SC(NH)NH.sub.2 Me H 4-C.sub.6 H.sub.4 CO.sub.2 H OH, OH163 SC(NH)NH.sub.2 H H 4-C.sub.6 H.sub.4 CO.sub.2 Me OH, OH164 SC(NH)NH.sub.2 Me H 4-C.sub.6 H.sub.4 CO.sub.2 Me OH, OH165 SC(NH)NH.sub.2 Me H Ph OH, OH166 SC(NH)NH.sub.2 H OMe Ph OH, OH167 CH.sub.2 NH.sub.2 H H Ph OH, OH168 CH.sub.2 NH.sub.2 H Ph H OH, OH169 CH.sub.2 NH.sub.2 H OPh H OH, OH170 CH.sub.2 NH.sub.2 COPh H H OH, OH171 CH.sub.2 NH.sub.2 H COPh H OH, OH172 CH.sub.2 NH.sub.2 H H COPh OH, OH173 CH.sub.2 NH.sub.2 H NHCbz H OH, OH174 CH.sub.2 NH.sub.2 H NMeCbz H OH, OH175 CH.sub.2 NH.sub.2 H H Et OH, OH176 CH.sub.2 NH.sub.2 H H n-Pr OH, OH177 CH.sub.2 NH.sub.2 H H i-Pr OH, OH178 CH.sub.2 NH.sub.2 H H n-Bu OH, OH179 CH.sub.2 NH.sub.2 H H t-Bu OH, OH180 CH.sub.2 NH.sub.2 H H n-hexyl OH, OH181 CH.sub.2 NH.sub.2 H H cyclohexyl OH, OH182 CH.sub.2 NH.sub.2 NHCOCH.sub.2 CH.sub.2 Ph H H OH, OH183 CH.sub.2 NH.sub.2 H H O-n-Bu OH, OH184 CH.sub.2 NH.sub.2 H H NHCOcyclopropyl OH, OH185 CH.sub.2 NH.sub.2 H H NHCOcyclohexyl OH, OH186 CH.sub.2 NH.sub.2 H H NHCO(4-C.sub.6 H.sub.4 OMe) OH, OH187 CH.sub.2 NH.sub.2 H H 4-C.sub.6 H.sub.4 OMe OH, OH188 CH.sub.2 NH.sub.2 CO.sub.2 CH.sub.2 (2-C.sub.6 H.sub.4 Ph) H H OH, OH189 CH.sub.2 NH.sub.2 H H 1-naphthyl OH, OH190 CH.sub.2 NH.sub.2 H H 4-C.sub.6 H.sub.4 CO.sub.2 H OH, OH191 CH.sub.2 NH.sub.2 H NHCbz n-Bu OH, OH192 CH.sub.2 NH.sub.2 H NMeCbz n-Bu OH, OH193 CH.sub.2 NH.sub.2 COPh H Me OH, OH194 CH.sub.2 NH.sub.2 H H 4-pyridyl OH, OH195 CH.sub.2 NH.sub.2 Me H 4-C.sub.6 H.sub.4 CO.sub.2 H OH, OH196 CH.sub.2 NH.sub.2 H H 4-C.sub.6 H.sub.4 CO.sub.2 Me OH, OH197 CH.sub.2 NH.sub.2 Me H 4-C.sub.6 H.sub.4 CO.sub.2 Me OH, OH198 CH.sub.2 NH.sub.2 Me H Ph OH, OH199 NH(CNH)NH.sub.2 F H Ph (+)-pin SS200 NH(CNH)NH.sub.2 F H Ph OH, OH201 NH(CNH)NH.sub.2 NH.sub.2 H Ph (+)-pin202 NH(CNH)NH.sub.2 NH.sub.2 H Ph OH, OH203 NH(CNH)NH.sub.2 NO.sub.2 H Ph (+)-pin TT204 NH(CNH)NH.sub.2 NO.sub.2 H Ph OH, OH205 NH(CNH)NH.sub.2 OH H Ph (+)-pin206 NH(CNH)NH.sub.2 OH H Ph OH, OH207 NH(CNH)NH.sub.2 NHSO.sub.2 CF.sub.3 H Ph (+)-pin208 NH(CNH)NH.sub.2 NHSO.sub.2 CF.sub.3 H Ph (+)-pin209 NH(CNH)NH.sub.2 NHSO.sub.2 CH.sub.3 H Ph (+)-pin210 NH(CNH)NH.sub.2 NHSO.sub.2 CH.sub.3 H Ph (+)-pin211 NH(CNH)NH.sub.2 CH.sub.2 CN H Ph (+)-pin212 NH(CNH)NH.sub.2 CH.sub.2 CN H Ph OH, OH213 NH(CNH)NH.sub.2 CH.sub.2 CH.sub.2 CN H Ph (+)-pin214 NH(CNH)NH.sub.2 CH.sub.2 CH.sub.2 CN H Ph OH, OH215 NH(CNH)NH.sub.2 OCH.sub.2 CN H Ph (+)-pin216 NH(CNH)NH.sub.2 OCH.sub.2 CN H Ph OH, OH217 NH(CNH)NH.sub.2 SCH.sub.2 CN H Ph (+)-pin218 NH(CNH)NH.sub.2 SCH.sub.2 CN H Ph OH, OH219 NH(CNH)NH.sub.2 NHCH.sub.2 CN H Ph (+)-pin220 NH(CNH)NH.sub.2 NHCH.sub.2 CN H Ph OH, OH221 NH(CNH)NH.sub.2 CH.sub.2 OH H Ph (+)-pin222 NH(CNH)NH.sub.2 CH.sub.2 OH H Ph OH, OH223 NH(CNH)NH.sub.2 CH.sub.3 H 2-(t-butyl-NHSO.sub.2)Ph (+)-pin UU224 NH(CNH)NH.sub.2 CH.sub.3 H 2-(t-butyl-NHSO.sub.2)Ph OH, OH225 NH(CNH)NH.sub.2 CH.sub.3 H 2-(ethyl-NHSO.sub.2)Ph (+)-pin226 NH(CNH)NH.sub.2 CH.sub.3 H 2-(ethyl-NHSO.sub.2)Ph OH, OH227 NH(CNH)NH.sub.2 CH.sub.3 H 2-(H.sub.2 NSO.sub.2)Ph (+)-pin ZZ228 NH(CNH)NH.sub.2 CH.sub.3 H 2-(H.sub.2 NSO.sub.2)Ph OH, OH229 NH(CNH)NH.sub.2 CH.sub.3 H 2-(MeCONHSO.sub.2)Ph (+)-pin230 NH(CNH)NH.sub.2 CH.sub.3 H 2-(MeCONHSO.sub.2)Ph OH, OH231 NH(CNH)NH.sub.2 CH.sub.3 H 2-(MeOCONHSO.sub.2)Ph (+)-pin AB232 NH(CNH)NH.sub.2 CH.sub.3 H 2-(MeOCONHSO.sub.2)Ph OH, OH233 NH(CNH)NH.sub.2 CH.sub.3 H 2-(NH.sub.2)Ph (+)-pin234 NH(CNH)NH.sub.2 CH.sub.3 H 2-(NH.sub.2)Ph OH, OH235 NH(CNH)NH.sub.2 CH.sub.3 H 2-(CH.sub.3 SO.sub.2 NH)Ph (+)-pin236 NH(CNH)NH.sub.2 CH.sub.3 H 2-(CH.sub.3 SO.sub.2 NH)Ph OH, OH237 NH(CNH)NH.sub.2 CH.sub.3 H 2-(CF.sub.3 SO.sub.2 NH)Ph (+)-pin238 NH(CNH)NH.sub.2 CH.sub.3 H 2-(CF.sub.3 SO.sub.2 NH)Ph OH, OH239 NH(CNH)NH.sub.2 CH.sub.3 H 2-(CN.sub.4 H)Ph (+)-pin240 NH(CNH)NH.sub.2 CH.sub.3 H 2-(CN.sub.4 H)Ph OH, OH241 NH(CNH)NH.sub.2 CH.sub.3 H 2-(COOH)Ph (+)-pin242 NH(CNH)NH.sub.2 CH.sub.3 H 2-(COOH)Ph OH, OH243 NH(CNH)NH.sub.2 CH.sub.3 H 3-(NH.sub.2)Ph (+)-pin244 NH(CNH)NH.sub.2 CH.sub.3 H 3-(NH.sub.2)Ph OH, OH245 NH(CNH)NH.sub.2 CH.sub.3 H 3-(CH.sub.3 SO.sub.2 NH)Ph (+)-pin246 NH(CNH)NH.sub.2 CH.sub.3 H 3-(CH.sub.3 SO.sub.2 NH)Ph OH, OH247 NH(CNH)NH.sub.2 CH.sub.3 OH Ph (+)-pin248 NH(CNH)NH.sub.2 CH.sub.3 OH Ph OH, OH249 NH(CNH)NH.sub.2 CH.sub.3 NH.sub.2 Ph (+)-pin250 NH(CNH)NH.sub.2 CH.sub.3 NH.sub.2 Ph OH, OH251 NH(CNH)NH.sub.2 F H 2-(t-butyl-NHSO.sub.2)Ph (+)-pin252 NH(CNH)NH.sub.2 F H 2-(t-butyl-NHSO.sub.2)Ph OH, OH253 NH(CNH)NH.sub.2 F H 2-(ethyl-NHSO.sub.2)Ph (+)-pin254 NH(CNH)NH.sub.2 F H 2-(ethyl-NHSO.sub.2)Ph OH, OH255 NH(CNH)NH.sub.2 F H 2-(H.sub.2 NSO.sub.2)Ph (+)-pin256 NH(CNH)NH.sub.2 F H 2-(H.sub.2 NSO.sub.2)Ph OH, OH257 NH(CNH)NH.sub.2 F H 2-(MeCONHSO.sub.2)Ph (+)-pin258 NH(CNH)NH.sub.2 F H 2-(MeCONHSO.sub.2)Ph OH, OH259 NH(CNH)NH.sub.2 F H 2-(MeOCONHSO.sub.2)Ph (+)-pin260 NH(CNH)NH.sub.2 F H 2-(MeOCONHSO.sub.2)Ph OH, OH261 NH(CNH)NH.sub.2 H H 2-(t-butyl-NHSO.sub.2)Ph (+)-pin AC262 NH(CNH)NH.sub.2 Cl H 2-(t-butyl-NHSO.sub.2)Ph (+)-pin CE263 NH(CNH)NH.sub.2 H H 2-(t-butyl-NHSO.sub.2)Ph OH, OH AD264 NH(CNH)NH.sub.2 Cl H 2-(t-butyl-NHSO.sub.2)Ph OH, OH265 NH(CNH)NH.sub.2 Cl H 2-(ethyl-NHSO.sub.2)Ph (+)-pin266 NH(CNH)NH.sub.2 Cl H 2-(ethyl-NHSO.sub.2)Ph OH, OH267 NH(CNH)NH.sub.2 Cl H 2-(H.sub.2 NSO.sub.2)Ph (+)-pin268 NH(CNH)NH.sub.2 Cl H 2-(H.sub.2 NSO.sub.2)Ph OH, OH269 NH(CNH)NH.sub.2 Cl H 2-(MeCONHSO.sub.2)Ph (+)-pin270 NH(CNH)NH.sub.2 Cl H 2-(MeCONHSO.sub.2)Ph OH, OH271 NH(CNH)NH.sub.2 Cl H 2-(MeOCONHSO.sub.2)Ph (+)-pin272 NH(CNH)NH.sub.2 Cl H 2-(MeOCONHSO.sub.2)Ph OH, OH273 NH(CNH)NH.sub.2 NHSO.sub.2 CH.sub.3 H 2-(t-butyl-NHSO.sub.2)Ph (+)-pin274 NH(CNH)NH.sub.2 NHSO.sub.2 CH.sub.3 H 2-(t-butyl-NHSO.sub.2)Ph OH, OH275 NH(CNH)NH.sub.2 NHSO.sub.2 CH.sub.3 H 2-(ethyl-NHSO.sub.2)Ph (+)-pin276 NH(CNH)NH.sub.2 NHSO.sub.2 CH.sub.3 H 2-(ethyl-NHSO.sub.2)Ph OH, OH277 NH(CNH)NH.sub.2 NHSO.sub.2 CH.sub.3 H 2-(H.sub.2 NSO.sub.2)Ph (+)-pin278 NH(CNH)NH.sub.2 NHSO.sub.2 CH.sub.3 H 2-(H.sub.2 NSO.sub.2)Ph OH, OH279 NH(CNH)NH.sub.2 NHSO.sub.2 CH.sub.3 H 2-(MeCONHSO.sub.2)Ph (+)-pin280 NH(CNH)NH.sub.2 NHSO.sub.2 CH.sub.3 H 2-(MeCONHSO.sub.2)Ph OH, OH281 NH(CNH)NH.sub.2 NHSO.sub.2 CH.sub.3 H 2-(MeOCONHSO.sub.2)Ph (+)-pin282 NH(CNH)NH.sub.2 NHSO.sub.2 CH.sub.3 H 2-(MeOCONHSO.sub.2)Ph OH, OH283 NH(CNH)NH.sub.2 CH.sub.3 H 3-(t-butylOCONH)Ph (+)-pin VV284 NH(CNH)NH.sub.2 CH.sub.3 H 3-(t-butylOCONH)Ph OH, OH285 NH(CNH)NH.sub.2 N(Et).sub.2 H Ph (+)-pin286 NH(CNH)NH.sub.2 CH.sub.3 H 2-((ethyl).sub.2 -NSO.sub.2)Ph (+)-pin CF287 NH(CNH)NH.sub.2 CH.sub.3 H 2-(n-BuOCONHSO.sub.2)Ph (+)-pin288 NH(CNH)NH.sub.2 NO.sub.2 H 2-(t-butyl-NHSO.sub.2)Ph (+)-pin CG289 NH(CNH)NH.sub.2 NO.sub.2 H 2-(t-butyl-NHSO.sub.2)Ph OH, OH290 NH(CNH)NH.sub.2 NO.sub.2 H 2-(ethyl-NHSO.sub.2)Ph (+)-pin291 NH(CNH)NH.sub.2 NO.sub.2 H 2-(ethyl-NHSO.sub.2)Ph OH, OH292 NH(CNH)NH.sub.2 NO.sub.2 H 2-(H.sub.2 NSO.sub.2)Ph (+)-pin293 NH(CNH)NH.sub.2 NO.sub.2 H 2-(H.sub.2 NSO.sub.2)Ph OH, OH294 NH(CNH)NH.sub.2 NO.sub.2 H 2-(MeCONHSO.sub.2)Ph (+)-pin295 NH(CNH)NH.sub.2 NO.sub.2 H 2-(MeCONHSO.sub.2)Ph OH, OH296 NH(CNH)NH.sub.2 NO.sub.2 H 2-(MeOCONHSO.sub.2)Ph (+)-pin297 NH(CNH)NH.sub.2 NO.sub.2 H 2-(MeOCONHSO.sub.2)Ph OH, OH298 NH(CNH)NH.sub.2 H NO.sub.2 Ph (+)-pin AE299 NH(CNH)NH.sub.2 H NH.sub.2 Ph (+)-pin AF300 NH(CNH)NH.sub.2 H NO.sub.2 Ph OH, OH301 NH(CNH)NH.sub.2 H NH.sub.2 Ph OH, OH302 NH(CNH)H H H 2-(t-butyl-NHSO.sub.2)Ph (+)-pin CH303 NH(CNH)NH.sub.2 2-NHBOC H Ph (+)-pin CI304 NH(CNH)NH.sub.2 2-NO.sub.2 H Ph (+)-pin CJ305 OCH.sub.3 2-Me H 2-(H.sub.2 NSO.sub.2)Ph (+)-pin CK306 CH.sub.2 NH.sub.2 CH.sub.3 H 4-thiophen-2-yl (+)-pin307 CH.sub.2 NH.sub.2 CH.sub.3 H 4-thiophen-3-yl (+)-pin308 CH.sub.2 NH.sub.2 CH.sub.3 3-thiophen-2-yl H (+)-pin309 CH.sub.2 NH.sub.2 CH.sub.3 3-thiophen-3-yl H (+)-pin310 CH.sub.2 NH.sub.2 CH.sub.3 H 4-furan-2-yl (+)-pin311 CH.sub.2 NH.sub.2 CH.sub.3 H 4-furan-3-yl (+)-pin312 CH.sub.2 NH.sub.2 CH.sub.3 3-furan-2-yl H (+)-pin313 CH.sub.2 NH.sub.2 CH.sub.3 3-furan-3-yl H (+)-pin314 CH.sub.2 NH.sub.2 CH.sub.3 H 4-imidazol-2-yl (+)-pin315 CH.sub.2 NH.sub.2 CH.sub.3 H 4-imidazol-4-yl (+)-pin316 CH.sub.2 NH.sub.2 CH.sub.3 3-imidazol-2-yl H (+)-pin317 CH.sub.2 NH.sub.2 CH.sub.3 3-imidazol-4-yl H (+)-pin318 CH.sub.2 NH.sub.2 CH.sub.3 H 4-pyrazol-1-yl (+)-pin319 CH.sub.2 NH.sub.2 CH.sub.3 H 4-pyrazol-2-yl (+)-pin320 CH.sub.2 NH.sub.2 CH.sub.3 3-pyrazol-1-yl H (+)-pin321 CH.sub.2 NH.sub.2 CH.sub.3 3-pyrazol-2-yl H (+)-pin322 CH.sub.2 NH.sub.2 CH.sub.3 H 4-pyrrol-1-yl (+)-pin323 CH.sub.2 NH.sub.2 CH.sub.3 H 4-pyrrol-2-yl (+)-pin324 CH.sub.2 NH.sub.2 CH.sub.3 3-pyrrol-1-yl H (+)-pin325 CH.sub.2 NH.sub.2 CH.sub.3 3-pyrrol-2-yl H (+)-pin326 CH.sub.2 NH.sub.2 CH.sub.3 H 4-(1,2,4-triazol-1-yl) (+)-pin327 CH.sub.2 NH.sub.2 CH.sub.3 H 4-(1,2,4-triazol-2-yl) (+)-pin328 CH.sub.2 NH.sub.2 CH.sub.3 3-(1,2,4-triazol-1-yl) H (+)-pin329 CH.sub.2 NH.sub.2 CH.sub.3 3-(1,2,4-triazol-1-yl) H (+)-pin330 CH.sub.2 NH.sub.2 CH.sub.3 H 4-(1,2,3-triazol-1-yl) (+)-pin331 CH.sub.2 NH.sub.2 CH.sub.3 H 4-(1,2,3-triazol-4-yl) (+)-pin332 CH.sub.2 NH.sub.2 CH.sub.3 3-(1,2,3-triazol-1-yl) H (+)-pin333 CH.sub.2 NH.sub.2 CH.sub.3 3-(1,2,3-triazol-4-yl) H (+)-pin334 CH.sub.2 NH.sub.2 CH.sub.3 H 4-tetrazol-1-yl (+)-pin335 CH.sub.2 NH.sub.2 CH.sub.3 H 4-tetrazol-5-yl (+)-pin336 CH.sub.2 NH.sub.2 CH.sub.3 3-tetrazol-1-yl H (+)-pin337 CH.sub.2 NH.sub.2 CH.sub.3 3-tetrazol-5-yl H (+)-pin338 CH.sub.2 NH.sub.2 CH.sub.3 H 4-oxazol-2-yl (+)-pin339 CH.sub.2 NH.sub.2 CH.sub.3 H 4-oxazol-4-yl (+)-pin340 CH.sub.2 NH.sub.2 CH.sub.3 H 4-oxazol-5-yl (+)-pin341 CH.sub.2 NH.sub.2 CH.sub.3 3-oxazol-2-yl H (+)-pin342 CH.sub.2 NH.sub.2 CH.sub.3 3-oxazol-4-yl H (+)-pin343 CH.sub.2 NH.sub.2 CH.sub.3 3-oxazol-5-yl H (+)-pin344 CH.sub.2 NH.sub.2 CH.sub.3 H 4-thiazol-2-yl (+)-pin345 CH.sub.2 NH.sub.2 CH.sub.3 H 4-thiazol-4-yl (+)-pin346 CH.sub.2 NH.sub.2 CH.sub.3 H 4-thiazol-5-yl (+)-pin347 CH.sub.2 NH.sub.2 CH.sub.3 3-thiazol-2-yl H (+)-pin348 CH.sub.2 NH.sub.2 CH.sub.3 3-thiazol-4-yl H (+)-pin349 CH.sub.2 NH.sub.2 CH.sub.3 3-thiazol-5-yl H (+)-pin350 CH.sub.2 NH.sub.2 CH.sub.3 H 4-pyridin-2-yl (+)-pin351 CH.sub.2 NH.sub.2 CH.sub.3 H 4-pyridin-3-yl (+)-pin352 CH.sub.2 NH.sub.2 CH.sub.3 3-pyridin-2-yl H (+)-pin353 CH.sub.2 NH.sub.2 CH.sub.3 3-pyridin-3-yl H (+)-pin354 CH.sub.2 NH.sub.2 CH.sub.3 H 4-pyrimidin-2-yl (+)-pin355 CH.sub.2 NH.sub.2 CH.sub.3 H 4-pyrimidin-4-yl (+)-pin356 CH.sub.2 NH.sub.2 CH.sub.3 H 4-pyrimidin-5-yl (+)-pin357 CH.sub.2 NH.sub.2 CH.sub.3 3-pyrimidin-2-yl H (+)-pin358 CH.sub.2 NH.sub.2 CH.sub.3 3-pyrimidin-4-yl H (+)-pin359 CH.sub.2 NH.sub.2 CH.sub.3 3-pyrimidin-5-yl H (+)-pin__________________________________________________________________________ (+)-pin indicates (+)pinanediol A: MS (M + H).sup.+ = 489; B: MS (DCINH.sub.3), 505 (M + H).sup.+. C: MS (M + H).sup.+ = 490. D: MS (M + H).sup.+ = 506; E: mp 145-150.degree. C.; MS (DCINH.sub.3), Calc: 506, Found: 506. F: MS (DCINH.sub.3), 522 (M + H).sup.+. G: HRMS (DCINH.sub.3), Calc: 534.2597, Found: 534.2609. H: HRMS (DCINH.sub.3), Calc: 534.2597, Found: 534.2605. I: HRMS (DCINH.sub.3), Calc: 534.2597, Found: 534.2609. J: �a!.sub.D = -14,85.degree. (c = 0.606, MeOH); MS (CINH.sub.3), m/e (%) 537.2 (10.2, M + HH.sub.2 NCN).sup.+), 429.0 (42.8), 277.0 (100); Anal. Calcd for C.sub.30 H.sub.40 BBrN.sub.4 O.sub.5 S: C, 54.64; H, 6.11; N, 8.50; B, 1.64. Found: C, 54.52; H, 6.16; N, 8.45; B, 1.60. K: �a!.sub.D = -15.07.degree. (c = 0.604, MeOH); MS (CINH.sub.3), m/e (%) 593.2 (1.2, (M + H).sup.+), 568.3 (22, (M + NH.sub.4 H.sub.2 NCN).sup.+), 551.3 (100, (M + HH.sub.2 NCN).sup.+); Anal. Calcd for C.sub.31 H.sub.42 BBrN.sub.4 O.sub.5 S: C, 55.29; H, 6.29; N, 8.32; B, 1.61. Found: C, 55.15; H, 6.21; N, 8.22; B, 1.47. L: �a!.sub.D = -14.12.degree. (c = 0.602, MeOH); MS (DCINH.sub.3), m/e (% 458 (100, (M + H).sup.+); Anal. Calcd for C.sub.24 H.sub.37 BBrN.sub.3 O.sub.3 S: C, 53.54; H, 6.93; N, 7.81; B, 2.01. Found: C, 53.75; H, 6.98; N, 7.74; B, 1.97. M: �a!.sub.D = -14.21.degree. (c = 0.556, MeOH); MS (CINH.sub.3), m/e (%) 472.2 (13.5, (M + H).sup.+), 430.2 (100, (M + HH.sub.2 NCN).sup.+), 278.0 (61.9); Anal. Calcd for C.sub.25 H.sub.39 BBrN.sub.3 O.sub.3 S: C, 54.36; H, 7.12; N, 7,61; B, 1.96. Found: C, 54.50; H, 7.18; N, 7.83; B, 1.73. N: �a!.sub.D = -13.79.degree. (c = 0.602, MeOH); MS (DCINH.sub.3), m/e (% 472 (100, (M + H).sup.+), 430 (37, (M + HH.sub.2 NCN).sup.+); Anal. Calcd for C.sub.25 H.sub.39 BBrN.sub.3 O.sub.3 S: C, 54.36; H, 7.12; N, 7.61; B 1.96. Found: C, 54.64; H, 7.17; N, 7.50; B, 1.74. O: �a .sub.D = -13.19.degree. (c = 0.364, MeOH); MS (CINH.sub.3), m/e (%) 486.2 (3.3, (M + H).sup.+), 444.2 (87.1, (M + HH.sub.2 NCN).sup.+), 292.0 (100); Anal. Calcd for C.sub.26 H.sub.41 BBrN.sub.3 O.sub.3 S: C, 55.13; H, 7.30; N, 7.42; B, 1.91. Found: C, 54.99; H, 7,22; N, 7.29; B, 2.07. P: �a!.sub.D = -12.71.degree. (c = 0.598, MeOH); MS (DCINH.sub.3), m/e (% 486 (100, (M + H).sup.+), 444 (16, (M + HH.sub.2 NCN).sup.+); Anal. Calcd for C.sub.26 H.sub.41 BBrN.sub.3 O.sub.3 S: C, 55.13; H, 7.30; N, 7.42; B 1.91. Found: C, 55.09; H, 7.45; N, 7.40; B, 1.67. Q: MS (DCIAB,4 NH.sub.3), m/e (%) 514 (100, (M + H).sup.+), 472 (16, (M + HH.sub.2 NCN).sup.+); Anal. Calcd for C.sub.28 H.sub.45 BBrN.sub.3 O.sub. S: C, 56.57; H, 7.63; N, 7.07; B, 1.82. Found: C, 56.19; H, 7.53; N, 6.97 B, 1.99. R: �a!.sub.D = -12.70.degree. (c = 0.530, MeOH); MS (DCINH.sub.3), m/e (% 512 (100, (M + H).sup.+), 470 (40, (M + HH.sub.2 NCN).sup.+); Anal. Calcd for C.sub.28 H.sub.43 BBrN.sub.3 O.sub.3 S: C, 56.77; H, 7.32; N, 7.09; B 1.82. Found: C, 56.49; H, 7.38; N, 6.96; B, 1.75. S: HRMS (DCINH.sub.3), Calc: 577.3019, Found: 577.3025. T: �a!.sub.D = -8.31.degree. (c = 0.614, MeOH); MS (DCINH.sub.3), m/e (%) 502 (100, (M + H).sup.+), 460 (28, (M + HH.sub.2 NCN).sup.+); Anal. Calcd for C.sub.26 H.sub.41 BBrN.sub.3 O.sub.4 S: C, 53.62; H, 7.10; N, 7.21; B 1.86. Found: C, 53.61; H, 7.09; N, 7.20; B, 1.78. U: HRMS (DCINH.sub.3), Calc: 513.2707, Found: 513.2702. V: HRMS (DCINH.sub.3), Calc: 555.3165, Found: 555.3176. W: HRMS (DCINH.sub.3), Calc: 579.2812, Found: 579.2801. X: HRMS (DCINH.sub.3), Calc: 450.2962, Found: 450.2958. Y: HRMS (DCINH.sub.3), Calc: 640.3019, Found: 640.3022. Z: �a!.sub.D = -8.80.degree. (c = 0.602, MeOH); MS (CINH.sub.3), m/e (%) 593.2 (1.3, (M + H).sup.+), 485.2 (42.7), 333.0 (100); Anal. Calcd for C.sub.34 H.sub.48 BBrN.sub.4 O.sub.5 S: C, 57.07; H, 6.76; N, 7.83; B, 1.51. Found: C, 57.17; H, 6.84; N, 7.76; B, 1.41. AA: MS (CINH.sub.3), m/e (%) 649.4 (1.9, (M + H).sup.+), 624.4 (31, (M + NH.sub.4 H.sub.2 NCN).sup.+), 607.2 (100, (M + HH.sub.2 NCN).sup.+), 455. (39), 444.0 (29.8); Anal. Calcd for C.sub.35 H.sub.50 BBrN.sub.4 O.sub.5 S: C, 57.62; H, 6.91; N, 7.68; B, 1.48. Found: C, 57.37; H, 6.86; N, 7.64 B, 1.40. BB: HRMS (DCINH.sub.3), Calc: 520.2805, Found: 520.2796. SS. MS (DCINH.sub.3), Calc: 507, Found: 507. TT. MS (DCINH.sub.3), Calc: 534, Found: 534. UU. MS (DCINH.sub.3), Calc: 638, Found: 638. VV. MS (DCINH.sub.3), Calc: 618, Found: 618. XX. MS (DCINH.sub.3), Calc: 489, Found: 489. YY. MS (DCINH.sub.3), Calc: 461, Found: 461. ZZ. MS (DCINH.sub.3), Calc: 582, Found: 582. AB. MS (DCINH.sub.3), Calc: 641, Found: 641. AC. MS (DCINH.sub.3), Calc: 625, Found: 625. AD. MS (DCINH.sub.3), Calc: 490, Found: 490. AE. MS (DCINH.sub.3), Calc: 534, Found: 534. AF. MS (DCINH.sub.3), Calc: 504, Found: 504. CB. MS (M + H).sup.+, Calc: 503.32, Found: 503.32. CD. MS (M + H).sup.+, Calc: , Found: .(WITYAK) CE. MS (M + H).sup.+, Calc: 658, Found: 658. CF. MS (M + H).sup.+, Calc: 638, Found: 638. CG. MS (M + H).sup.+, Calc: 669, Found: 669. CH. MS (M + H).sup.+, Calc: 609, Found: 609. CI. MS (M + H).sup.+, Calc: 604, Found: 604. CJ. MS (M + H).sup.+, Calc: 641, Found: 641. CK. MS (M + H).sup.+, Calc: 555, Found: 555. TABLE 2______________________________________ ##STR97##Ex X Y Y.sup.1, Y.sup.2 Phys Data______________________________________365 CH.sub.2 NH.sub.2 CO (+)-pin366 CH.sub.2 NH.sub.2 SO.sub.2 (+)-pin367 NHC(NH)NH.sub.2 CO (+)-pin368 NHC(NH)NH.sub.2 SO.sub.2 (+)-pin369 SC(NH)NH.sub.2 CO (+)-pin CC370 SC(NH)NH.sub.2 SO.sub.2 (+)-pin DD371 CH.sub.2 NH.sub.2 CO OH, OH372 CH.sub.2 NH.sub.2 SO.sub.2 OH, OH373 NHC(NH)NH.sub.2 CO OH, OH374 NHC(NH)NH.sub.2 SO.sub.2 OH, OH375 SC(NH)NH.sub.2 CO OH, OH376 SC(NH)NH.sub.2 SO.sub.2 OH, OH______________________________________ CC: HRMS (DCINH.sub.3), Calc: 560.2390, Found: 560.2407. DD: HRMS (DCINH.sub.3), Calc: 596.2060, Found: 596.2055. TABLE 3______________________________________ ##STR98##Ex X t Y.sup.1, Y.sup.2 Phys Data______________________________________382 NH.sub.2 2 (+)-pin383 SC(NH)NH.sub.2 2 (+)-pin EE384 SC(NH)NH.sub.2 1 (+)-pin FF385 NHC(NH)NH.sub.2 2 (+)-pin386 NHC(NH)NH.sub.2 1 (+)-pin387 NH.sub.2 2 OH, OH388 SC(NH)NH.sub.2 2 OH, OH389 SC(NH)NH.sub.2 1 OH, OH390 NHC(NH)NH.sub.2 2 OH, OH391 NHC(NH)NH.sub.2 1 OH, OH______________________________________ EE: HRMS (DCINH.sub.3), Calc: 546.2597, Found: 546.2604. FF: HRMS (DCINH.sub.3), Calc: 534.2597, Found: 534.2609. TABLE 4______________________________________ ##STR99##Ex X Y.sup.1, Y.sup.2 Phys Data______________________________________397 CH.sub.2 NH.sub.2 (+)-pin398 NHC(NH)NH.sub.2 (+)-pin399 SC(NH)NH.sub.2 (+)-pin CG400 CH.sub.2 NH.sub.2 OH, OH401 NHC(NH)NH.sub.2 OH, OH402 SC(NH)NH.sub.2 OH, OH______________________________________ GG: HRMS (DCINH.sub.3), Calc: 532.2441, Found: 532.2445. TABLE 5______________________________________ ##STR100##Ex X Y.sup.1, Y.sup.2 Phys Data______________________________________403 CH.sub.2 NH.sub.2 (+)-pin404 NHC(NH)NH.sub.2 (+)-pin405 SC(NH)NH.sub.2 (+)-pin HH406 CH.sub.2 NH.sub.2 OH, OH407 NHC(NH)NH.sub.2 OH, OH408 SC(NH)NH.sub.2 OH, OH______________________________________ HH: HRMS (DCINH.sub.3), Calc: 532.2441, Found: 532.2452. TABLE 6______________________________________ ##STR101##Ex X Y.sup.1, Y.sup.2 Phys Data______________________________________436 NHC(NH)NH.sub.2 (+)-pin437 SC(NH)NH.sub.2 (+)-pin II438 CH.sub.2 NH.sub.2 (+)-pin439 NHC(NH)NH.sub.2 OH, OH440 SC(NH)NH.sub.2 OH, OH441 CH.sub.2 NH.sub.2 OH, OH______________________________________ II: HRMS (DCINH.sub.3), Calc: 480.2493, Found: 480.2492. TABLE 7______________________________________ ##STR102##Ex X Y Y.sup.1, Y.sup.2 Phys Data______________________________________447 NHC(NH)NH.sub.2 O (+)-pin WW448 SC(NH)NH.sub.2 O (+)-pin JJ449 CH.sub.2 NH.sub.2 O (+)-pin450 NHC(NH)NH.sub.2 S (+)-pin451 SC(NH)NH.sub.2 S (+)-pin452 CH.sub.2 NH.sub.2 S (+)-pin453 NHC(NH)NH.sub.2 O OH, OH454 SC(NH)NH.sub.2 O OH, OH455 CH.sub.2 NH.sub.2 O OH, OH456 NHC(NH)NH.sub.2 S OH, OH457 SC(NH)NH.sub.2 S OH, OH458 CH.sub.2 NH.sub.2 S OH, OH______________________________________ JJ: HRMS (DCINH.sub.3), Calc: 496.2441, Found: 496.2449. WW. MS (DCINH.sub.3), Calc: 345, Found: 345. TABLE 8______________________________________ ##STR103##Ex X R.sup.B R.sup.C Y.sup.1, Y.sup.2 Phys Data______________________________________464 NHC(NH)NH.sub.2 H Ph (+)-pin465 NHC(NH)NH.sub.2 OBn H (+)-pin466 SC(NH)NH.sub.2 H Ph (+)-pin KK467 SC(NH)NH.sub.2 OBn H (+)-pin LL468 CH.sub.2 NH.sub.2 H Ph (+)-pin CL469 CH.sub.2 NH.sub.2 OBn H (+)-pin470 NHC(NH)NH.sub.2 H Ph OH, OH471 NHC(NH)NH.sub.2 OBn H OH, OH472 SC(NH)NH.sub.2 H Ph OH, OH473 SC(NH)NH.sub.2 OBn H OH, OH474 CH.sub.2 NH.sub.2 H Ph OH, OH CM475 CH.sub.2 NH.sub.2 OBn H OH, OH______________________________________ KK: HRMS (DCINH.sub.3), Calc: 507.2601, Found: 507.2592. LL: HRMS (DCINH.sub.3), Calc: 537.2667, Found: 537.2685. CL: Anal. Calc'd. for C.sub.27 H.sub.36 BN.sub.3 O.sub.3.(HCl).sub.1.7.(H.sub.2 O).sub.2.2 : C, 57.60; H, 7.54; Cl, 10.70; N, 7.46. Found: C, 57.40; H, 7.23; Cl, 10.78; N, 7.53. MS (M + H).sup.+ : calc. 462, Found 462. CM: MS (M + H).sup.+ : Calc: 328, Found: 328. TABLE 9______________________________________ ##STR104##Ex X Y.sup.1, Y.sup.2 Phys Data______________________________________476 NHC(NH)NH.sub.2 (+)-pin477 SC(NH)NH.sub.2 (+)-pin MM478 CH.sub.2 NH.sub.2 (+)-pin479 NHC(NH)NH.sub.2 OH, OH480 SC(NH)NH.sub.2 OH, OH481 CH.sub.2 NH.sub.2 OH, OH______________________________________ MM: HRMS (DCINH.sub.3), Calc: 498.2233, Found: 498.2231. TABLE 10______________________________________ ##STR105##Ex X W.sup.1 W.sup.2 R.sup.3 Y.sup.1, Y.sup.2 Phys Data______________________________________482 NHC(NH)NH.sub.2 N CH H (+)-pin483 SC(NH)NH.sub.2 N CH H (+)-pin NN484 CH.sub.2 NH.sub.2 N CH H (+)-pin485 NHC(NH)NH.sub.2 CH N Ph (+)-pin486 SC(NH)NH.sub.2 CH N Ph (+)-pin OO487 CH.sub.2 NH.sub.2 CH N Ph (+)-pin488 NHC(NH)NH.sub.2 N CH H OH, OH489 SC(NH)NH.sub.2 N CH H OH, OH490 CH.sub.2 NH.sub.2 N CH H OH, OH491 NHC(NH)NH.sub.2 CH N Ph OH, OH492 SC(NH)NH.sub.2 CH N Ph OH, OH493 CH.sub.2 NH.sub.2 CH N Ph OH, OH______________________________________ NN: HRMS (DCINH.sub.3), Calc: 481.2445, Found: 481.2442. OO: HRMS (DCINH.sub.3), Calc: 557.2758, Found: 557.2754. TABLE 11______________________________________ ##STR106##Ex X Y.sup.1, Y.sup.2 Phys Data______________________________________499 NHC(NH)NH.sub.2 (+)-pin500 SC(NH)NH.sub.2 (+)-pin PP501 CH.sub.2 NH.sub.2 (+)-pin502 NHC(NH)NH.sub.2 OH, OH503 SC(NH)NH.sub.2 OH, OH504 CH.sub.2 NH.sub.2 OH, OH______________________________________ PP: HRMS (DCINH.sub.3), Calc: 5481.2445, Found: 481.2440. TABLE 12______________________________________ ##STR107##Ex X R.sup.3 Y.sup.1, Y.sup.2 Phys Data______________________________________510 SC(NH)NH.sub.2 H (+)-pin QQ______________________________________ QQ: HRNS (NH.sub.3 CI/DEP), Calc: 503.3193, Found: 503.3199. TABLE 13______________________________________ ##STR108## PhysEx m, X R.sup.A R.sup.B R.sup.C Y.sup.1, Y.sup.2 Data______________________________________516 2, H NHCO H (+)-pin RR SC(NH)NH.sub.2 (CH.sub.2).sub.2 Ph517 2, H Ph H (+)-pin SC (NH) NH.sub.2518 2, H OPh Ph (+)-pin SC(NH)NH.sub.2519 1, H H 4- (+)-pin SC(NH)NH.sub.2 pyridyl520 1, COPh H H (+)-pin NHC(NH)NH.sub.2521 3, H COPh H (+)-pin NHC(NH)NH.sub.2522 3, H H COPh (+)-pin NHC(NH)NH.sub.2______________________________________ RR: HRMS (DCINH.sub.3), Calc: 605.333, Found: 605.3325. TABLE 14__________________________________________________________________________ ##STR109## Phys.Ex X m R.sup.13 R.sup.14 Y.sup.1 Y.sup.2 Data__________________________________________________________________________ 528 CH.sub.2 NH.sub.2 1 Ph H (+)-pin 529 CH.sub.2 NH.sub.2 1 Ph Methyl (+)-pin 530 CH.sub.2 NH.sub.2 1 Ph Ethyl (+)-pin 531 CH.sub.2 NH.sub.2 1 Ph n-Propyl (+)-pin 532 CH.sub.2 NH.sub.2 1 Ph n-Butyl (+)-pin 533 CH.sub.2 NH.sub.2 1 Ph CH.sub.2 SCH.sub.3 (+)-pin 534 CH.sub.2 NH.sub.2 1 Ph CH.sub.2 (SO)CH.sub.3 (+)-pin 535 CH.sub.2 NH.sub.2 1 Ph CH.sub.2 (SO.sub.2)CH.sub.3 (+)-pin 536 CH.sub.2 NH.sub.2 1 Ph CH.sub.2 CH.sub.2 SCH.sub.3 (+)-pin 537 CH.sub.2 NH.sub.2 1 Ph CH.sub.2 CH.sub.2 (SO)CH.sub.3 (+)-pin 538 CH.sub.2 NH.sub.2 1 Ph CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3 (+)-pin 539 CH.sub.2 NH.sub.2 1 Ph CH.sub.2 CN (+)-pin 540 CH.sub.2 NH.sub.2 1 Ph CH.sub.2 CH.sub.2 CN (+)-pin 541 CH.sub.2 NH.sub.2 1 Ph CH.sub.2 CH.sub.2 CH.sub.2 CN (+)-pin 542 CH.sub.2 NH.sub.2 1 Ph CF.sub.3 (+)-pin 543 CH.sub.2 NH.sub.2 1 Ph CF.sub.2 CF.sub.3 (+)-pin 544 CH.sub.2 NH.sub.2 1 Ph CF.sub.2 CF.sub.2 CF.sub.3 (+)-pin 545 CH.sub.2 NH.sub.2 1 Ph CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3 (+)-pin 546 CH.sub.2 NH.sub.2 1 Ph F.sub.5 -Ph (+)-pin 547 CH.sub.2 NH.sub.2 1 Ph CH.sub.2 CO.sub.2 H (+)-pin 548 CH.sub.2 NH.sub.2 1 Ph (CH.sub.2).sub.2 CO.sub.2 H (+)-pin 549 CH.sub.2 NH.sub.2 1 Ph (CH.sub.2).sub.3 CO.sub.2 H (+)-pin 550 CH.sub.2 NH.sub.2 1 Ph CH.sub.2 CN.sub.4 H (+)-pin 551 CH.sub.2 NH.sub.2 1 Ph (CH.sub.2).sub.2 CN.sub.4 H (+)-pin 552 CH.sub.2 NH.sub.2 1 Ph (CH.sub.2).sub.3 CN.sub.4 H (+)-pin 553 CH.sub.2 NH.sub.2 1 Ph CH.sub.2 NO.sub.2 (+)-pin 554 CH.sub.2 NH.sub.2 1 Ph (CH.sub.2).sub.2 NO.sub.2 (+)-pin 555 CH.sub.2 NH.sub.2 1 Ph (CH.sub.2).sub.3 NO.sub.2 (+)-pin 556 CH.sub.2 NH.sub.2 1 Ph CH.sub.2 OH (+)-pin 557 CH.sub.2 NH.sub.2 1 Ph (CH.sub.2).sub.2 OH (+)-pin 558 CH.sub.2 NH.sub.2 1 Ph (CH.sub.2).sub.3 OH (+)-pin 559 CH.sub.2 NH.sub.2 1 Ph CH.sub.2 CO.sub.2 Me (+)-pin 560 CH.sub.2 NH.sub.2 1 Ph (CH.sub.2).sub.2 CO.sub.2 Me (+)-pin 561 CH.sub.2 NH.sub.2 1 Ph (CH.sub.2).sub.3 CO.sub.2 Me (+)-pin 562 CH.sub.2 NH.sub.2 1 Ph Ph (+)-pin 563 CH.sub.2 NH.sub.2 1 Ph PhCH.sub.2 (+)-pin AG 564 CH.sub.2 NH.sub.2 1 Ph Ph(CH.sub.2).sub.2 (+)-pin 565 CH.sub.2 NH.sub.2 1 Ph 3-NO.sub.2 -Ph (+)-pin 566 CH.sub.2 NH.sub.2 1 Ph 4-NO.sub.2 -Ph (+)-pin 567 CH.sub.2 NH.sub.2 1 Ph 3-CO.sub.2 H-Ph (+)-pin 568 CH.sub.2 NH.sub.2 1 Ph 4-CO.sub.2 H-Ph (+)-pin 569 CH.sub.2 NH.sub.2 1 Ph 3-CN.sub.4 H-Ph (+)-pin 570 CH.sub.2 NH.sub.2 1 Ph 4-CN.sub.4 H-Ph (+)-pin 571 CH.sub.2 NH.sub.2 1 Ph 3-(HOCH.sub.2)-Ph (+)-pin 572 CH.sub.2 NH.sub.2 1 Ph 4-(HOCH.sub.2)-Ph (+)-pin 573 NH(CNH)NH.sub.2 1 Ph H (+)-pin 574 NH(CNH)NH.sub.2 1 Ph Methyl (+)-pin 575 NH(CNH)NH.sub.2 1 Ph Ethyl (+)-pin 576 NH(CNH)NH.sub.2 1 Ph n-Propyl (+)-pin 577 NH(CNH)NH.sub.2 1 Ph n-Butyl (+)-pin 578 NH(CNH)NH.sub.2 1 Ph CH.sub.2 SCH.sub.3 (+)-pin 579 NH(CNH)NH.sub.2 1 Ph CH.sub.2 (SO)CH.sub.3 (+)-pin 580 NH(CNH)NH.sub.2 1 Ph CH.sub.2 (SO.sub.2)CH.sub.3 (+)-pin 581 NH(CNH)NH.sub.2 1 Ph CH.sub.2 CH.sub.2 SCH.sub.3 (+)-pin 582 NH(CNH)NH.sub.2 1 Ph CH.sub.2 CH.sub.2 (SO)CH.sub.3 (+)-pin 583 NH(CNH)NH.sub.2 1 Ph CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3 (+)-pin 584 NH(CNH)NH.sub.2 1 Ph CH.sub.2 CN (+)-pin 585 NH(CNH)NH.sub.2 1 Ph CH.sub.2 CH.sub.2 CN (+)-pin 586 NH(CNH)NH.sub.2 1 Ph CH.sub.2 CH.sub.2 CH.sub.2 CN (+)-pin 587 NH(CNH)NH.sub.2 1 Ph CF.sub.3 (+)-pin 588 NH(CNH)NH.sub.2 1 Ph CF.sub.2 CF.sub.3 (+)-pin 589 NH(CNH)NH.sub.2 1 Ph CF.sub.2 CF.sub.2 CF.sub.3 (+)-pin 590 NH(CNH)NH.sub.2 1 Ph CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3 (+)-pin 591 NH(CNH)NH.sub.2 1 Ph F.sub.5 -Ph (+)-pin 592 NH(CNH)NH.sub.2 1 Ph CH.sub.2 CO.sub.2 H (+)-pin 593 NH(CNH)NH.sub.2 1 Ph (CH.sub.2).sub.2 CO.sub.2 H (+)-pin 594 NH(CNH)NH.sub.2 1 Ph (CH.sub.2).sub.3 CO.sub.2 H (+)-pin 595 NH(CNH)NH.sub.2 1 Ph CH.sub.2 CN.sub.4 H (+)-pin 596 NH(CNH)NH.sub.2 1 Ph (CH.sub.2).sub.2 CN.sub.4 H (+)-pin 597 NH(CNH)NH.sub.2 1 Ph (CH.sub.2).sub.3 CN.sub.4 H (+)-pin 598 NH(CNH)NH.sub.2 1 Ph CH.sub.2 NO.sub.2 (+)-pin 599 NH(CNH)NH.sub.2 1 Ph (CH.sub.2).sub.2 NO.sub.2 (+)-pin 600 NH(CNH)NH.sub.2 1 Ph (CH.sub.2).sub.3 NO.sub.2 (+)-pin 601 NH(CNH)NH.sub.2 1 Ph CH.sub.2 OH (+)-pin 602 NH(CNH)NH.sub.2 1 Ph (CH.sub.2).sub.2 OH (+)-pin 603 NH(CNH)NH.sub.2 1 Ph (CH.sub.2).sub.3 OH (+)-pin 604 NH(CNH)NH.sub.2 1 Ph CH.sub.2 CO.sub.2 Me (+)-pin 605 NH(CNH)NH.sub.2 1 Ph (CH.sub.2).sub.2 CO.sub.2 Me (+)-pin 606 NH(CNH)NH.sub.2 1 Ph (CH.sub.2).sub.3 CO.sub.2 Me (+)-pin 607 NH(CNH)NH.sub.2 1 Ph Ph (+)-pin 609 NH(CNH)NH.sub.2 1 Ph 3-NO.sub.2 -Ph (+)-pin 610 NH(CNH)NH.sub.2 1 Ph 4-NO.sub.2 -Ph (+)-pin 611 NH(CNH)NH.sub.2 1 Ph 3-CO.sub.2 H-Ph (+)-pin 612 NH(CNH)NH.sub.2 1 Ph 4-CO.sub.2 H-Ph (+)-pin 613 NH(CNH)NH.sub.2 1 Ph 3-CN.sub.4 H-Ph (+)-pin 614 NH(CNH)NH.sub.2 1 Ph 4-CN.sub.4 H-Ph (+)-pin 615 NH(CNH)NH.sub.2 1 Ph 3-(HOCH.sub.2)-Ph (+)-pin 616 NH(CNH)NH.sub.2 1 Ph 4-(HOCH.sub.2)-Ph (+)-pin 617 CH.sub.2 NH.sub.2 1 Ph H OH, OH 618 CH.sub.2 NH.sub.2 1 Ph Methyl OH, OH 619 CH.sub.2 NH.sub.2 1 Ph Ethyl OH, OH 620 CH.sub.2 NH.sub.2 1 Ph n-Propyl OH, OH 621 CH.sub.2 NH.sub.2 1 Ph n-Butyl OH, OH 622 CH.sub.2 NH.sub.2 1 Ph CH.sub.2 SCH.sub.3 OH, OH 623 CH.sub.2 NH.sub.2 1 Ph CH.sub.2 (SO)CH.sub.3 OH, OH 624 CH.sub.2 NH.sub.2 1 Ph CH.sub.2 (SO.sub.2)CH.sub.3 OH, OH 625 CH.sub.2 NH.sub.2 1 Ph CH.sub.2 CH.sub.2 SCH.sub.3 OH, OH 626 CH.sub.2 NH.sub.2 1 Ph CH.sub.2 CH.sub.2 (SO)CH.sub.3 OH, OH 627 CH.sub.2 NH.sub.2 1 Ph CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3 OH, OH 628 CH.sub.2 NH.sub.2 1 Ph CH.sub.2 CN OH, OH 629 CH.sub.2 NH.sub.2 1 Ph CH.sub.2 CH.sub.2 CN OH, OH 630 CH.sub.2 NH.sub.2 1 Ph CH.sub.2 CH.sub.2 CH.sub.2 CN OH, OH 631 CH.sub.2 NH.sub.2 1 Ph CF.sub.3 OH, OH 632 CH.sub.2 NH.sub.2 1 Ph CF.sub.2 CF.sub.3 OH, OH 633 CH.sub.2 NH.sub.2 1 Ph CF.sub.2 CF.sub.2 CF.sub.3 OH, OH 634 CH.sub.2 NH.sub.2 1 Ph CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3 OH, OH 635 CH.sub.2 NH.sub.2 1 Ph F.sub.5 -Ph OH, OH 636 CH.sub.2 NH.sub.2 1 Ph CH.sub.2 CO.sub.2 H OH, OH 637 CH.sub.2 NH.sub.2 1 Ph (CH.sub.2).sub.2 CO.sub.2 H OH, OH 638 CH.sub.2 NH.sub.2 1 Ph (CH.sub.2).sub.3 CO.sub.2 H OH, OH 639 CH.sub.2 NH.sub.2 1 Ph CH.sub.2 CN.sub.4 H OH, OH 640 CH.sub.2 NH.sub.2 1 Ph (CH.sub.2).sub.2 CN.sub.4 H OH, OH 641 CH.sub.2 NH.sub.2 1 Ph (CH.sub.2).sub.3 CN.sub.4 H OH, OH 642 CH.sub.2 NH.sub.2 1 Ph CH.sub.2 NO.sub.2 OH, OH 643 CH.sub.2 NH.sub.2 1 Ph (CH.sub.2).sub.2 NO.sub.2 OH, OH 644 CH.sub.2 NH.sub.2 1 Ph (CH.sub.2).sub.3 NO.sub.2 OH, OH 645 CH.sub.2 NH.sub.2 1 Ph CH.sub.2 OH OH, OH 646 CH.sub.2 NH.sub.2 1 Ph (CH.sub.2).sub.2 OH OH, OH 647 CH.sub.2 NH.sub.2 1 Ph (CH.sub.2).sub.3 OH OH, OH 648 CH.sub.2 NH.sub.2 1 Ph CH.sub.2 CO.sub.2 Me OH, OH 649 CH.sub.2 NH.sub.2 1 Ph (CH.sub.2).sub.2 CO.sub.2 Me OH, OH 650 CH.sub.2 NH.sub.2 1 Ph (CH.sub.2).sub.3 CO.sub.2 Me OH, OH 651 CH.sub.2 NH.sub.2 1 Ph Ph OH, OH 652 CH.sub.2 NH.sub.2 1 Ph PhCH.sub.2 OH, OH AH 653 CH.sub.2 NH.sub.2 1 Ph Ph(CH.sub.2).sub.2 OH, OH 654 CH.sub.2 NH.sub.2 1 Ph 3-NO.sub.2 -Ph OH, OH 655 CH.sub.2 NH.sub.2 1 Ph 4-NO.sub.2 -Ph OH, OH 656 CH.sub.2 NH.sub.2 1 Ph 3-CO.sub.2 H-Ph OH, OH 657 CH.sub.2 NH.sub.2 1 Ph 4-CO.sub.2 H-Ph OH, OH 658 CH.sub.2 NH.sub.2 1 Ph 3-CN.sub.4 H-Ph OH, OH 659 CH.sub.2 NH.sub.2 1 Ph 4-CN.sub.4 H-Ph OH, OH 660 CH.sub.2 NH.sub.2 1 Ph 3-(HOCH.sub.2)-Ph OH, OH 661 CH.sub.2 NH.sub.2 1 Ph 4-(HOCH.sub.2)-Ph OH, OH 662 NH(CNH)NH.sub.2 1 Ph H OH, OH 663 NH(CNH)NH.sub.2 1 Ph Methyl OH, OH 664 NH(CNH)NH.sub.2 1 Ph Ethyl OH, OH 665 NH(CNH)NH.sub.2 1 Ph n-Propyl OH, OH 666 NH(CNH)NH.sub.2 1 Ph n-Butyl OH, OH 667 NH(CNH)NH.sub.2 1 Ph CH.sub.2 SCH.sub.3 OH, OH 668 NH(CNH)NH.sub.2 1 Ph CH.sub.2 (SO)CH.sub.3 OH, OH 669 NH(CNH)NH.sub.2 1 Ph CH.sub.2 (SO.sub.2)CH.sub.3 OH, OH 670 NH(CNH)NH.sub.2 1 Ph CH.sub.2 CH.sub.2 SCH.sub.3 OH, OH 671 NH(CNH)NH.sub.2 1 Ph CH.sub.2 CH.sub.2 (SO)CH.sub.3 OH, OH 672 NH(CNH)NH.sub.2 1 Ph CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3 OH, OH 673 NH(CNH)NH.sub.2 1 Ph CH.sub.2 CN OH, OH 674 NH(CNH)NH.sub.2 1 Ph CH.sub.2 CH.sub.2 CN OH, OH 675 NH(CNH)NH.sub.2 1 Ph CH.sub.2 CH.sub.2 CH.sub.2 CN OH, OH 676 NH(CNH)NH.sub.2 1 Ph CF.sub.3 OH, OH 677 NH(CNH)NH.sub.2 1 Ph CF.sub.2 CF.sub.3 OH, OH 678 NH(CNH)NH.sub.2 1 Ph CF.sub.2 CF.sub.2 CF.sub.3 OH, OH 679 NH(CNH)NH.sub.2 1 Ph CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3 OH, OH 680 NH(CNH)NH.sub.2 1 Ph F.sub.5 -Ph OH, OH 681 NH(CNH)NH.sub.2 1 Ph CH.sub.2 CO.sub.2 H OH, OH 682 NH(CNH)NH.sub.2 1 Ph (CH.sub.2).sub.2 CO.sub.2 H OH, OH 683 NH(CNH)NH.sub.2 1 Ph (CH.sub.2).sub.3 CO.sub.2 H OH, OH 684 NH(CNH)NH.sub.2 1 Ph CH.sub.2 CN.sub.4 H OH, OH 685 NH(CNH)NH.sub.2 1 Ph (CH.sub.2).sub.2 CN.sub.4 H OH, OH 686 NH(CNH)NH.sub.2 1 Ph (CH.sub.2).sub.3 CN.sub.4 H OH, OH 687 NH(CNH)NH.sub.2 1 Ph CH.sub.2 NO.sub.2 OH, OH 688 NH(CNH)NH.sub.2 1 Ph (CH.sub.2).sub.2 NO.sub.2 OH, OH 689 NH(CNH)NH.sub.2 1 Ph (CH.sub.2).sub.3 NO.sub.2 OH, OH 690 NH(CNH)NH.sub.2 1 Ph CH.sub.2 OH OH, OH 691 NH(CNH)NH.sub.2 1 Ph (CH.sub.2).sub.2 OH OH, OH 692 NH(CNH)NH.sub.2 1 Ph (CH.sub.2).sub.3 OH OH, OH 693 NH(CNH)NH.sub.2 1 Ph CH.sub.2 CO.sub.2 Me OH, OH 694 NH(CNH)NH.sub.2 1 Ph (CH.sub.2).sub.2 CO.sub.2 Me OH, OH 695 NH(CNH)NH.sub.2 1 Ph (CH.sub.2).sub.3 CO.sub.2 Me OH, OH 696 NH(CNH)NH.sub.2 1 Ph Ph OH, OH 697 NH(CNH)NH.sub.2 1 Ph PhCH.sub.2 OH, OH 698 NH(CNH)NH.sub.2 1 Ph Ph(CH.sub.2).sub.2 OH, OH 699 NH(CNH)NH.sub.2 1 Ph 3-NO.sub.2 -Ph OH, OH 700 NH(CNH)NH.sub.2 1 Ph 4-NO.sub.2 -Ph OH, OH 701 NH(CNH)NH.sub.2 1 Ph 3-CO.sub.2 H-Ph OH, OH 702 NH(CNH)NH.sub.2 1 Ph 4-CO.sub.2 H-Ph OH, OH 703 NH(CNH)NH.sub.2 1 Ph 3-CN.sub.4 H-Ph OH, OH 704 NH(CNH)NH.sub.2 1 Ph 4-CN.sub.4 H-Ph OH, OH 705 NH(CNH)NH.sub.2 1 Ph 3-(HOCH.sub.2)-Ph OH, OH 706 NH(CNH)NH.sub.2 1 Ph 4-(HOCH.sub.2)-Ph OH, OH 707 S(CNH)NH.sub.2 1 Ph H (+)-pin 708 S(CNH)NH.sub.2 1 Ph Methyl (+)-pin 709 S(CNH)NH.sub.2 1 Ph Ethyl (+)-pin 710 S(CNH)NH.sub.2 1 Ph n-Propyl (+)-pin 711 S(CNH)NH.sub.2 1 Ph n-Butyl (+)-pin 712 S(CNH)NH.sub.2 1 Ph CH.sub.2 SCH.sub.3 (+)-pin 713 S(CNH)NH.sub.2 1 Ph CH.sub.2 (SO)CH.sub.3 (+)-pin 714 S(CNH)NH.sub.2 1 Ph CH.sub.2 (SO.sub.2)CH.sub.3 (+)-pin 715 S(CNH)NH.sub.2 1 Ph CH.sub.2 CH.sub.2 SCH.sub.3 (+)-pin 716 S(CNH)NH.sub.2 1 Ph CH.sub.2 CH.sub.2 (SO)CH.sub.3 (+)-pin 717 S(CNH)NH.sub.2 1 Ph CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3 (+)-pin 718 S(CNH)NH.sub.2 1 Ph CH.sub.2 CN (+)-pin 719 S(CNH)NH.sub.2 1 Ph CH.sub.2 CH.sub.2 CN (+)-pin 720 S(CNH)NH.sub.2 1 Ph CH.sub.2 CH.sub.2 CH.sub.2 CN (+)-pin 721 S(CNH)NH.sub.2 1 Ph CF.sub.3 (+)-pin 722 S(CNH)NH.sub.2 1 Ph CF.sub.2 CF.sub.3 (+)-pin 723 S(CNH)NH.sub.2 1 Ph CF.sub.2 CF.sub.2 CF.sub.3 (+)-pin 724 S(CNH)NH.sub.2 1 Ph CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3 (+)-pin 725 S(CNH)NH.sub.2 1 Ph F.sub.5 -Ph (+)-pin 726 S(CNH)NH.sub.2 1 Ph CH.sub.2 CO.sub.2 H (+)-pin 727 S(CNH)NH.sub.2 1 Ph (CH.sub.2).sub.2 CO.sub.2 H (+)-pin 728 S(CNH)NH.sub.2 1 Ph (CH.sub.2).sub.3 CO.sub.2 H (+)-pin 729 S(CNH)NH.sub.2 1 Ph CH.sub.2 CN.sub.4 H (+)-pin 730 S(CNH)NH.sub.2 1 Ph (CH.sub.2).sub.2 CN.sub.4 H (+)-pin 731 S(CNH)NH.sub.2 1 Ph (CH.sub.2).sub.3 CN.sub.4 H (+)-pin 732 S(CNH)NH.sub.2 1 Ph CH.sub.2 NO.sub.2 (+)-pin 733 S(CNH)NH.sub.2 1 Ph (CH.sub.2).sub.2 NO.sub.2 (+)-pin 734 S(CNH)NH.sub.2 1 Ph (CH.sub.2).sub.3 NO.sub.2 (+)-pin 735 S(CNH)NH.sub.2 1 Ph CH.sub.2 OH (+)-pin 736 S(CNH)NH.sub.2 1 Ph (CH.sub.2).sub.2 OH (+)-pin 737 S(CNH)NH.sub.2 1 Ph (CH.sub.2).sub.3 OH (+)-pin 738 S(CNH)NH.sub.2 1 Ph CH.sub.2 CO.sub.2 Me (+)-pin 739 S(CNH)NH.sub.2 1 Ph (CH.sub.2).sub.2 CO.sub.2 Me (+)-pin 740 S(CNH)NH.sub.2 1 Ph (CH.sub.2).sub.3 CO.sub.2 Me (+)-pin 741 S(CNH)NH.sub.2 1 Ph Ph (+)-pin 742 S(CNH)NH.sub.2 1 Ph 3-NO.sub.2 -Ph (+)-pin 743 S(CNH)NH.sub.2 1 Ph 4-NO.sub.2 -Ph (+)-pin 744 S(CNH)NH.sub.2 1 Ph 3-CO.sub.2 H-Ph (+)-pin 745 S(CNH)NH.sub.2 1 Ph 4-CO.sub.2 H-Ph (+)-pin 746 S(CNH)NH.sub.2 1 Ph 3-CN.sub.4 H-Ph (+)-pin 747 S(CNH)NH.sub.2 1 Ph 4-CN.sub.4 H-Ph (+)-pin 748 S(CNH)NH.sub.2 1 Ph 3-(HOCH.sub.2)-Ph (+)-pin 749 S(CNH)NH.sub.2 1 Ph 4-(HOCH.sub.2)-Ph (+)-pin 750 S(CNH)NH.sub.2 1 Ph H OH, OH 751 S(CNH)NH.sub.2 1 Ph Methyl OH, OH 752 S(CNH)NH.sub.2 1 Ph Ethyl OH, OH 753 S(CNH)NH.sub.2 1 Ph n-Propyl OH, OH 754 S(CNH)NH.sub.2 1 Ph n-Butyl OH, OH 755 S(CNH)NH.sub.2 1 Ph CH.sub.2 SCH.sub.3 OH, OH 756 S(CNH)NH.sub.2 1 Ph CH.sub.2 (SO)CH.sub.3 OH, OH 757 S(CNH)NH.sub.2 1 Ph CH.sub.2 (SO.sub.2)CH.sub.3 OH, OH 758 S(CNH)NH.sub.2 1 Ph CH.sub.2 CH.sub.2 SCH.sub.3 OH, OH 759 S(CNH)NH.sub.2 1 Ph CH.sub.2 CH.sub.2 (SO)CH.sub.3 OH, OH 760 S(CNH)NH.sub.2 1 Ph CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3 OH, OH 761 S(CNH)NH.sub.2 1 Ph CH.sub.2 CN OH, OH 762 S(CNH)NH.sub.2 1 Ph CH.sub.2 CH.sub.2 CN OH, OH 763 S(CNH)NH.sub.2 1 Ph CH.sub.2 CH.sub.2 CH.sub.2 CN OH, OH 764 S(CNH)NH.sub.2 1 Ph CF.sub.3 OH, OH 765 S(CNH)NH.sub.2 1 Ph CF.sub.2 CF.sub.3 OH, OH 766 S(CNH)NH.sub.2 1 Ph CF.sub.2 CF.sub.2 CF.sub.3 OH, OH 767 S(CNH)NH.sub.2 1 Ph CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3 OH, OH 768 S(CNH)NH.sub.2 1 Ph F.sub.5 -Ph OH, OH 769 S(CNH)NH.sub.2 1 Ph CH.sub.2 CO.sub.2 H OH, OH 770 S(CNH)NH.sub.2 1 Ph (CH.sub.2).sub.2 CO.sub.2 H OH, OH 771 S(CNH)NH.sub.2 1 Ph (CH.sub.2).sub.3 CO.sub.2 H OH, OH 772 S(CNH)NH.sub.2 1 Ph CH.sub.2 CN.sub.4 H OH, OH 773 S(CNH)NH.sub.2 1 Ph (CH.sub.2).sub.2 CN.sub.4 H OH, OH 774 S(CNH)NH.sub.2 1 Ph (CH.sub.2).sub.3 CN.sub.4 H OH, OH 775 S(CNH)NH.sub.2 1 Ph CH.sub.2 NO.sub.2 OH, OH 776 S(CNH)NH.sub.2 1 Ph (CH.sub.2).sub.2 NO.sub.2 OH, OH 777 S(CNH)NH.sub.2 1 Ph (CH.sub.2).sub.3 NO.sub.2 OH, OH 778 S(CNH)NH.sub.2 1 Ph CH.sub.2 OH OH, OH 779 S(CNH)NH.sub.2 1 Ph (CH.sub.2).sub.2 OH OH, OH 780 S(CNH)NH.sub.2 1 Ph (CH.sub.2).sub.3 OH OH, OH 781 S(CNH)NH.sub.2 1 Ph CH.sub.2 CO.sub.2 Me OH, OH 782 S(CNH)NH.sub.2 1 Ph (CH.sub.2).sub.2 CO.sub.2 Me OH, OH 783 S(CNH)NH.sub.2 1 Ph (CH.sub.2).sub.3 CO.sub.2 Me OH, OH 784 S(CNH)NH.sub.2 1 Ph Ph OH, OH 785 S(CNH)NH.sub.2 1 Ph PhCH.sub.2 OH, OH 786 S(CNH)NH.sub.2 1 Ph Ph(CH.sub.2).sub.2 OH, OH 787 S(CNH)NH.sub.2 1 Ph 3-NO.sub.2 -Ph OH, OH 788 S(CNH)NH.sub.2 1 Ph 4-NO.sub.2 -Ph OH, OH 789 S(CNH)NH.sub.2 1 Ph 3-CO.sub.2 H-Ph OH, OH 790 S(CNH)NH.sub.2 1 Ph 4-CO.sub.2 H-Ph OH, OH 791 S(CNH)NH.sub.2 1 Ph 3-CN.sub.4 H-Ph OH, OH 792 S(CNH)NH.sub.2 1 Ph 4-CN.sub.4 H-Ph OH, OH 793 S(CNH)NH.sub.2 1 Ph 3-(HOCH.sub.2)-Ph OH, OH 794 S(CNH)NH.sub.2 1 Ph 4-(HOCH.sub.2)-Ph OH, OH 795 CH.sub.2 NH.sub.2 2 Ph H (+)-pin 796 CH.sub.2 NH.sub.2 2 Ph H OH, OH 797 OMe 1 Ph H (+)-pin 798 OMe 1 Ph Methyl (+)-pin 799 OMe 1 Ph Ethyl (+)-pin 800 OMe 1 Ph n-Propyl (+)-pin 801 OMe 1 Ph n-Butyl (+)-pin 802 OMe 1 Ph CH.sub.2 SCH.sub.3 (+)-pin 803 OMe 1 Ph CH.sub.2 (SO)CH.sub.3 (+)-pin 804 OMe 1 Ph CH.sub.2 (SO.sub.2)CH.sub.3 (+)-pin 805 OMe 1 Ph CH.sub.2 CH.sub.2 SCH.sub.3 (+)-pin 806 OMe 1 Ph CH.sub.2 CH.sub.2 (SO)CH.sub.3 (+)-pin 807 OMe 1 Ph CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3 (+)-pin 808 OMe 1 Ph CH.sub.2 CN (+)-pin 809 OMe 1 Ph CH.sub.2 CH.sub.2 CN (+)-pin 810 OMe 1 Ph CH.sub.2 CH.sub.2 CH.sub.2 CN (+)-pin 811 OMe 1 Ph CF.sub.3 (+)-pin 812 OMe 1 Ph CF.sub.2 CF.sub.3 (+)-pin 813 OMe 1 Ph CF.sub.2 CF.sub.2 CF.sub.3 (+)-pin 814 OMe 1 Ph CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3 (+)-pin 815 OMe 1 Ph F.sub.5 -Ph (+)-pin 816 OMe 1 Ph CH.sub.2 CO.sub.2 H (+)-pin 817 OMe 1 Ph (CH.sub.2).sub.2 CO.sub.2 H (+)-pin 818 OMe 1 Ph (CH.sub.2).sub.3 CO.sub.2 H (+)-pin 819 OMe 1 Ph CH.sub.2 CN.sub.4 H (+)-pin 820 OMe 1 Ph (CH.sub.2).sub.2 CN.sub.4 H (+)-pin 821 OMe 1 Ph (CH.sub.2).sub.3 CN.sub.4 H (+)-pin 822 OMe 1 Ph CH.sub.2 NO.sub.2 (+)-pin 823 OMe 1 Ph (CH.sub.2).sub.2 NO.sub.2 (+)-pin 824 OMe 1 Ph (CH.sub.2).sub.3 NO.sub.2 (+)-pin 825 OMe 1 Ph CH.sub.2 OH (+)-pin 826 OMe 1 Ph (CH.sub.2).sub.2 OH (+)-pin 827 OMe 1 Ph (CH.sub.2).sub.3 OH (+)-pin 828 OMe 1 Ph CH.sub.2 CO.sub.2 Me (+)-pin 829 OMe 1 Ph (CH.sub.2).sub.2 CO.sub.2 Me (+)-pin 830 OMe 1 Ph (CH.sub.2).sub.3 CO.sub.2 Me (+)-pin 831 OMe 1 Ph Ph (+)-pin 832 OMe 1 Ph PhCH.sub.2 (+)-pin 833 OMe 1 Ph Ph(CH.sub.2).sub.2 (+)-pin 834 OMe 1 Ph 3-NO.sub.2 -Ph (+)-pin 835 OMe 1 Ph 4-NO.sub.2 -Ph (+)-pin 836 OMe 1 Ph 3-CO.sub.2 H-Ph (+)-pin 837 OMe 1 Ph 4-CO.sub.2 H-Ph (+)-pin 838 OMe 1 Ph 3-CN.sub.4 H-Ph (+)-pin 839 OMe 1 Ph 4-CN.sub.4 H-Ph (+)-pin 840 OMe 1 Ph 3-(HOCH.sub.2)-Ph (+)-pin 841 OMe 1 Ph 4-(HOCH.sub.2)-Ph (+)-pin 842 OMe 1 Ph H OH, OH 843 OMe 1 Ph Methyl OH, OH 844 OMe 1 Ph Ethyl OH, OH 845 OMe 1 Ph n-Propyl OH, OH 846 OMe 1 Ph n-Butyl OH, OH 847 OMe 1 Ph CH.sub.2 SCH.sub.3 OH, OH 848 OMe 1 Ph CH.sub.2 (SO)CH.sub.3 OH, OH 849 OMe 1 Ph CH.sub.2 (SO.sub.2)CH.sub.3 OH, OH 850 OMe 1 Ph CH.sub.2 CH.sub.2 SCH.sub.3 OH, OH 851 OMe 1 Ph CH.sub.2 CH.sub.2 (SO)CH.sub.3 OH, OH 852 OMe 1 Ph CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3 OH, OH 853 OMe 1 Ph CH.sub.2 CN OH, OH 854 OMe 1 Ph CH.sub.2 CH.sub.2 CN OH, OH 855 OMe 1 Ph CH.sub.2 CH.sub.2 CH.sub.2 CN OH, OH 856 OMe 1 Ph CF.sub.3 OH, OH 857 OMe 1 Ph CF.sub.2 CF.sub.3 OH, OH 858 OMe 1 Ph CF.sub.2 CF.sub.2 CF.sub.3 OH, OH 859 OMe 1 Ph CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3 OH, OH 860 OMe 1 Ph F.sub.5 -Ph OH, OH 861 OMe 1 Ph CH.sub.2 CO.sub.2 H OH, OH 862 OMe 1 Ph (CH.sub.2).sub.2 CO.sub.2 H OH, OH 863 OMe 1 Ph (CH.sub.2).sub.3 CO.sub.2 H OH, OH 864 OMe 1 Ph CH.sub.2 CN.sub.4 H OH, OH 865 OMe 1 Ph (CH.sub.2).sub.2 CN.sub.4 H OH, OH 866 OMe 1 Ph (CH.sub.2).sub.3 CN.sub.4 H OH, OH 867 OMe 1 Ph CH.sub.2 NO.sub.2 OH, OH 868 OMe 1 Ph (CH.sub.2).sub.2 NO.sub.2 OH, OH 869 OMe 1 Ph (CH.sub.2).sub.3 NO.sub.2 OH, OH 870 OMe 1 Ph CH.sub.2 OH OH, OH 871 OMe 1 Ph (CH.sub.2).sub.2 OH OH, OH 872 OMe 1 Ph (CH.sub.2).sub.3 OH OH, OH 873 OMe 1 Ph CH.sub.2 CO.sub.2 Me OH, OH 874 OMe 1 Ph (CH.sub.2).sub.2 CO.sub.2 Me OH, OH 875 OMe 1 Ph (CH.sub.2).sub.3 CO.sub.2 Me OH, OH 876 OMe 1 Ph Ph OH, OH 877 OMe 1 Ph PhCH.sub.2 OH, OH 878 OMe 1 Ph Ph(CH.sub.2).sub.2 OH, OH 879 OMe 1 Ph 3-NO.sub.2 -Ph OH, OH 880 OMe 1 Ph 4-NO.sub.2 -Ph OH, OH 881 OMe 1 Ph 3-CO.sub.2 H-Ph OH, OH 882 OMe 1 Ph 4-CO.sub.2 H-Ph OH, OH 883 OMe 1 Ph 3-CN.sub.4 H-Ph OH, OH 884 OMe 1 Ph 4-CN.sub.4 H-Ph OH, OH 885 OMe 1 Ph 3-(HOCH.sub.2)-Ph OH, OH 886 OMe 1 Ph 4-(HOCH.sub.2)-Ph OH, OH 887 CH.sub.2 NH.sub.2 1 PhCH.sub.2 H (+)-pin AK 888 CH.sub.2 NH.sub.2 1 PhCH.sub.2 Methyl (+)-pin AL 889 CH.sub.2 NH.sub.2 1 PhCH.sub.2 Ethyl (+)-pin 890 CH.sub.2 NH.sub.2 1 PhCH.sub.2 n-Propyl (+)-pin AM 891 CH.sub.2 NH.sub.2 1 PhCH.sub.2 n-Butyl (+)-pin 892 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 SCH.sub.3 (+)-pin AN 893 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 (SO)CH.sub.3 (+)-pin 894 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 (SO.sub.2)CH.sub.3 (+)-pin 895 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 SCH.sub.3 (+)-pin 896 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 (SO)CH.sub.3 (+)-pin 897 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3 (+)-pin 898 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 CN (+)-pin CN 899 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 CN (+)-pin 900 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CF.sub.3 (+)-pin 901 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CF.sub.2 CF.sub.3 (+)-pin 902 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CF.sub.2 CF.sub.2 CF.sub.3 (+)-pin 903 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3 (+)-pin 904 CH.sub.2 NH.sub.2 1 PhCH.sub.2 F.sub.5 -Ph (+)-pin 905 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 CO.sub.2 H (+)-pin AW 906 CH.sub.2 NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.2 CO.sub.2 H (+)-pin 907 CH.sub.2 NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.3 CO.sub.2 H (+)-pin 908 CH.sub.2 NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.2 CN.sub.4 H (+)-pin 909 CH.sub.2 NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.3 CN.sub.4 H (+)-pin 910 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 NO.sub.2 (+)-pin 911 CH.sub.2 NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.2 NO.sub.2 (+)-pin 912 CH.sub.2 NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.3 NO.sub.2 (+)-pin 913 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 OH (+)-pin AO 914 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 OCH.sub.2 Ph (+)-pin AP 915 CH.sub.2 NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.2 OH (+)-pin 916 CH.sub.2 NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.3 OH (+)-pin 917 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 CO.sub.2 Me (+)-pin CP 918 CH.sub.2 NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.2 CO.sub.2 Me (+)-pin 919 CH.sub.2 NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.3 CO.sub.2 Me (+)-pin 920 CH.sub.2 NH.sub.2 1 PhCH.sub.2 Ph (+)-pin AQ 921 CH.sub.2 NH.sub.2 1 PhCH.sub.2 PhCH.sub.2 (+)-pin AR 922 CH.sub.2 NH.sub.2 1 PhCH.sub.2 Ph(CH.sub.2).sub.2 (+)-pin 923 CH.sub.2 NH.sub.2 1 PhCH.sub.2 3-NO.sub.2 -Ph (+)-pin AS 924 CH.sub.2 NH.sub.2 1 PhCH.sub.2 4-NO.sub.2 -Ph (+)-pin 925 CH.sub.2 NH.sub.2 1 PhCH.sub.2 3-CO.sub.2 H-Ph (+)-pin 926 CH.sub.2 NH.sub.2 1 PhCH.sub.2 4-CO.sub.2 H-Ph (+)-pin 927 CH.sub.2 NH.sub.2 1 PhCH.sub.2 3-CN.sub.4 H-Ph (+)-pin 928 CH.sub.2 NH.sub.2 1 PhCH.sub.2 4-CN.sub.4 H-Ph (+)-pin 929 CH.sub.2 NH.sub.2 1 PhCH.sub.2 3-(HOCH.sub.2)-Ph (+)-pin 930 CH.sub.2 NH.sub.2 1 PhCH.sub.2 4-(HOCH.sub.2)-Ph (+)-pin 931 CH.sub.2 NH.sub.2 1 PhCH.sub.2 3-NH.sub.2 -Ph (+)-pin CQ 932 NH(CNH)NH.sub.2 1 PhCH.sub.2 H (+)-pin 933 NH(CNH)NH.sub.2 1 PhCH.sub.2 Methyl (+)-pin 934 NH(CNH)NH.sub.2 1 PhCH.sub.2 Ethyl (+)-pin 935 NH(CNH)NH.sub.2 1 PhCH.sub.2 n-Propyl (+)-pin 936 NH(CNH)NH.sub.2 1 PhCH.sub.2 n-Butyl (+)-pin 937 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 SCH.sub.3 (+)-pin 938 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 (SO)CH.sub.3 (+)-pin 939 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 (SO.sub.2)CH.sub.3 (+)-pin 940 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 SCH.sub.3 (+)-pin 941 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 (SO)CH.sub.3 (+)-pin 942 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3 (+)-pin 943 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CN (+)-pin 944 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CN (+)-pin 945 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 CN (+)-pin 946 NH(CNH)NH.sub.2 1 PhCH.sub.2 CF.sub.3 (+)-pin 947 NH(CNH)NH.sub.2 1 PhCH.sub.2 CF.sub.2 CF.sub.3 (+)-pin 948 NH(CNH)NH.sub.2 1 PhCH.sub.2 CF.sub.2 CF.sub.2 CF.sub.3 (+)-pin 949 NH(CNH)NH.sub.2 1 PhCH.sub.2 CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3 (+)-pin 950 NH(CNH)NH.sub.2 1 PhCH.sub.2 F.sub.5 -Ph (+)-pin 951 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CO.sub.2 H (+)-pin 952 NH(CNH)NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.2 CO.sub.2 H (+)-pin 953 NH(CNH)NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.3 CO.sub.2 H (+)-pin 954 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CN.sub.4 H (+)-pin 955 NH(CNH)NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.2 CN.sub.4 H (+)-pin 956 NH(CNH)NH.sub.2 1 PhCH.sub.2 (CH.sub.2)CH.sub.3 CN.sub.4 H (+)-pin 957 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 NO.sub.2 (+)-pin 958 NH(CNH)NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.2 NO.sub.2 (+)-pin 959 NH(CNH)NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.3 NO.sub.2 (+)-pin 960 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 OH (+)-pin 961 NH(CNH)NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.2 OH (+)-pin 962 NH(CNH)NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.3 OH (+)-pin 963 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CO.sub.2 Me (+)-pin 964 NH(CNH)NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.2 CO.sub.2 Me (+)-pin 965 NH(CNH)NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.3 CO.sub.2 Me (+)-pin 966 NH(CNH)NH.sub.2 1 PhCH.sub.2 Ph (+)-pin 967 NH(CNH)NH.sub.2 1 PhCH.sub.2 PhCH.sub.2 (+)-pin AT 968 NH(CNH)NH.sub.2 1 PhCH.sub.2 Ph(CH.sub.2).sub.2 (+)-pin 969 NH(CNH)NH.sub.2 1 PhCH.sub.2 3-NO.sub.2 -Ph (+)-pin AU 970 NH(CNH)NH.sub.2 1 PhCH.sub.2 4-NO.sub.2 Ph (+)-pin 971 NH(CNH)NH.sub.2 1 PhCH.sub.2 3-CO.sub.2 H-Ph (+)-pin 972 NH(CNH)NH.sub.2 1 PhCH.sub.2 4-CO.sub.2 H-Ph (+)-pin 973 NH(CNH)NH.sub.2 1 PhCH.sub.2 3-CN.sub.4 H-Ph (+)-pin 974 NH(CNH)NH.sub.2 1 PhCH.sub.2 4-CN.sub.4 H-Ph (+)-pin 975 NH(CNH)NH.sub.2 1 PhCH.sub.2 3-(HOCH.sub.2)-Ph (+)-pin 976 NH(CNH)NH.sub.2 1 PhCH.sub.2 4-(HOCH.sub.2)-Ph (+)-pin 977 CH.sub.2 NH.sub.2 1 PhCH.sub.2 H OH, OH AI 978 CH.sub.2 NH.sub.2 1 PhCH.sub.2 Methyl OH, OH 979 CH.sub.2 NH.sub.2 1 PhCH.sub.2 Ethyl OH, OH 980 CH.sub.2 NH.sub.2 1 PhCH.sub.2 n-Propyl OH, OH 981 CH.sub.2 NH.sub.2 1 PhCH.sub.2 n-Butyl OH, OH 982 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 SCH.sub.3 OH, OH 983 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 (SO)CH.sub.3 OH, OH 984 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 (SO.sub.2)CH.sub.3 OH, OH 985 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 SCH.sub.3 OH, OH 986 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 (SO)CH.sub.3 OH, OH 987 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3 OH, OH 988 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 CN OH, OH 989 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CN OH, OH 990 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 CN OH, OH 991 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CF.sub.3 OH, OH 992 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CF.sub.2 CF.sub.3 OH, OH 993 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CF.sub.2 CF.sub.2 CF.sub.3 OH, OH 994 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3 OH, OH 995 CH.sub.2 NH.sub.2 1 PhCH.sub.2 F.sub.5 -Ph OH, OH 996 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 CO.sub.2 H OH, OH 997 CH.sub.2 NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.2 CO.sub.2 H OH, OH 998 CH.sub.2 NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.3 CO.sub.2 H OH, OH 999 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 CN.sub.4 H OH, OH1000 CH.sub.2 NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.2 CN.sub.4 H OH, OH1001 CH.sub.2 NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.3 CN.sub.4 H OH, OH1002 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 NO.sub.2 OH, OH1003 CH.sub.2 NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.2 NO.sub.2 OH, OH1004 CH.sub.2 NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.3 NO.sub.2 OH, OH1005 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 OH OH, OH1006 CH.sub.2 NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.2 OH OH, OH1007 CH.sub.2 NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.3 OH OH, OH1008 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 CO.sub.2 Me OH, OH1009 CH.sub.2 NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.2 CO.sub.2 Me OH, OH1010 CH.sub.2 NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.3 CO.sub.2 Me OH, OH1011 CH.sub.2 NH.sub.2 1 PhCH.sub.2 Ph OH, OH AV1012 CH.sub.2 NH.sub.2 1 PhCH.sub.2 PhCH.sub.2 OH, OH1013 CH.sub.2 NH.sub.2 1 PhCH.sub.2 Ph(CH.sub.2).sub.2 OH, OH1014 CH.sub.2 NH.sub.2 1 PhCH.sub.2 3-NO.sub.2 -Ph OH, OH1015 CH.sub.2 NH.sub.2 1 PhCH.sub.2 4-NO.sub.2 -Ph OH, OH1016 CH.sub.2 NH.sub.2 1 PhCH.sub.2 3-CO.sub.2 H-Ph OH, OH1017 CH.sub.2 NH.sub.2 1 PhCH.sub.2 4-CO.sub.2 H-Ph OH, OH1018 CH.sub.2 NH.sub.2 1 PhCH.sub.2 3-CN.sub.4 H-Ph OH, OH1019 CH.sub.2 NH.sub.2 1 PhCH.sub.2 4-CN.sub.4 H-Ph OH, OH1020 CH.sub.2 NH.sub.2 1 PhCH.sub.2 3-(HOCH.sub.2)-Ph OH, OH1021 CH.sub.2 NH.sub.2 1 PhCH.sub.2 4-(HOCH.sub.2)-Ph OH, OH1022 CH.sub.2 NH.sub.2 1 PhCH.sub.2 F (+)-pin1023 CH.sub.2 NH.sub.2 1 PhCH.sub.2 Cl (+)-pin1024 CH.sub.2 NH.sub.2 1 PhCH.sub.2 Br (+)-pin1025 CH.sub.2 NH.sub.2 1 PhCH.sub.2 I (+)-pin1026 CH.sub.2 NH.sub.2 1 PhCH.sub.2 COOH (+)-pin1027 CH.sub.2 NH.sub.2 1 PhCH.sub.2 COOMe (+)-pin1028 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CHO (+)-pin1029 CH.sub.2 NH.sub.2 1 PhCH.sub.2 COMe (+)-pin1030 CH.sub.2 NH.sub.2 1 PhCH.sub.2 NO.sub.2 (+)-pin1031 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CN (+)-pin1032 CH.sub.2 NH.sub.2 1 PhCH.sub.2 isopropyl (+)-pin1033 CH.sub.2 NH.sub.2 1 PhCH.sub.2 3-F-phenyl (+)-pin1034 CH.sub.2 NH.sub.2 1 PhCH.sub.2 3-Cl-phenyl (+)-pin1035 CH.sub.2 NH.sub.2 1 PhCH.sub.2 4-Br-phenyl (+)-pin1036 CH.sub.2 NH.sub.2 1 PhCH.sub.2 4-I-phenyl (+)-pin1037 CH.sub.2 NH.sub.2 1 PhCH.sub.2 3-CH.sub.3 -phenyl (+)-pin1038 CH.sub.2 NH.sub.2 1 PhCH.sub.2 3-MeO-phenyl (+)-pin1039 CH.sub.2 NH.sub.2 1 PhCH.sub.2 3-CN-phenyl (+)-pin1040 CH.sub.2 NH.sub.2 1 PhCH.sub.2 4-CN-phenyl (+)-pin1041 CH.sub.2 NH.sub.2 1 PhCH.sub.2 3-NC-phenyl (+)-pin1042 CH.sub.2 NH.sub.2 1 PhCH.sub.2 4-NC-phenyl (+)-pin1043 CH.sub.2 NH.sub.2 1 PhCH.sub.2 3-CF.sub.3 -phenyl (+)-pin1044 CH.sub.2 NH.sub.2 1 PhCH.sub.2 3-CH.sub.2 S-phenyl (+)-pin1045 CH.sub.2 NH.sub.2 1 PhCH.sub.2 3-CH.sub.3 SO-phenyl (+)-pin1046 CH.sub.2 NH.sub.2 1 PhCH.sub.2 3-CH.sub.3 SO.sub.2 -phenyl (+)-pin1047 CH.sub.2 NH.sub.2 1 PhCH.sub.2 3-N(Me).sub.2 -phenyl (+)-pin1048 CH.sub.2 NH.sub.2 1 PhCH.sub.2 3-MeCO-phenyl (+)-pin1049 CH.sub.2 NH.sub.2 1 PhCH.sub.2 3-CHO-phenyl (+)-pin1050 CH.sub.2 NH.sub.2 1 PhCH.sub.2 3-CO.sub.2 Me-phenyl (+)-pin1051 CH.sub.2 NH.sub.2 1 PhCH.sub.2 3-CONH.sub.2 -phenyl (+)-pin1052 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 NHSO.sub.2 CF.sub.3 (+)-pin1053 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 NHSO.sub.2 CH.sub.3 (+)-pin1054 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 CO.sub.2 -i-propyl (+)-pin1055 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 CHO (+)-pin1056 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 OMe (+)-pin1057 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 O-i-propyl (+)-pin1058 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 OCOMe (+)-pin1059 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 OCO-i-propyl (+)-pin1060 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 OCO-Phenyl (+)-pin1061 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 NHCOMe (+)-pin1062 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 NHCO-i-propyl (+)-pin1063 CH.sub.2 NH.sub.2 1 PhCH.sub.2 F OH, OH1064 CH.sub.2 NH.sub.2 1 PhCH.sub.2 Cl OH, OH1065 CH.sub.2 NH.sub.2 1 PhCH.sub.2 Br OH, OH1066 CH.sub.2 NH.sub.2 1 PhCH.sub.2 I OH, OH1067 CH.sub.2 NH.sub.2 1 PhCH.sub.2 COOH OH, OH1068 CH.sub.2 NH.sub.2 1 PhCH.sub.2 COOMe OH, OH1069 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CHO OH, OH1070 CH.sub.2 NH.sub.2 1 PhCH.sub.2 COMe OH, OH1071 CH.sub.2 NH.sub.2 1 PhCH.sub.2 NO.sub.2 OH, OH1072 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CN OH, OH1073 CH.sub.2 NH.sub.2 1 PhCH.sub.2 isopropyl OH, OH1074 CH.sub.2 NH.sub.2 1 PhCH.sub.2 3-F-phenyl OH, OH1075 CH.sub.2 NH.sub.2 1 PhCH.sub.2 3-Cl-phenyl OH, OH1076 CH.sub.2 NH.sub.2 1 PhCH.sub.2 4-Br-phenyl OH, OH1077 CH.sub.2 NH.sub.2 1 PhCH.sub.2 4-I-phenyl OH, OH1078 CH.sub.2 NH.sub.2 1 PhCH.sub.2 3-CH.sub.3 -phenyl OH, OH1079 CH.sub.2 NH.sub.2 1 PhCH.sub.2 3-MeO-phenyl OH, OH1080 CH.sub.2 NH.sub.2 1 PhCH.sub.2 3-CN-phenyl OH, OH1081 CH.sub.2 NH.sub.2 1 PhCH.sub.2 4-CN-phenyl OH, OH1082 CH.sub.2 NH.sub.2 1 PhCH.sub.2 3-NC-phenyl OH, OH1083 CH.sub.2 NH.sub.2 1 PhCH.sub.2 4-NC-phenyl OH, OH1084 CH.sub.2 NH.sub.2 1 PhCH.sub.2 3-CF.sub.3 -phenyl OH, OH1085 CH.sub.2 NH.sub.2 1 PhCH.sub.2 3-CH.sub.2 S-phenyl OH, OH1086 CH.sub.2 NH.sub.2 1 PhCH.sub.2 3-CH.sub.3 SO-phenyl OH, OH1087 CH.sub.2 NH.sub.2 1 PhCH.sub.2 3-CH.sub.3 SO.sub.2 -phenyl OH, OH1088 CH.sub.2 NH.sub.2 1 PhCH.sub.2 3-N(Me).sub.2 -phenyl OH, OH1089 CH.sub.2 NH.sub.2 1 PhCH.sub.2 3-MeCO-phenyl OH, OH1090 CH.sub.2 NH.sub.2 1 PhCH.sub.2 3-CHO-phenyl OH, OH1091 CH.sub.2 NH.sub.2 1 PhCH.sub.2 3-CO.sub.2 Me-phenyl OH, OH1092 CH.sub.2 NH.sub.2 1 PhCH.sub.2 3-CONH.sub.2 -phenyl OH, OH1093 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 NHSO.sub.2 CF.sub.3 OH, OH1094 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 NHSO.sub.2 CH.sub.3 OH, OH1095 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 CO.sub.2 -i-propyl OH, OH1096 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 CHO OH, OH1097 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 OMe OH, OH1098 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 O-i-propyl OH, OH1099 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 OCOMe OH, OH1100 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 OCO-i-propyl OH, OH1101 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 OCO-Phenyl OH, OH1102 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 NHCOMe OH, OH1103 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 NHCO-i-propyl OH, OH1104 CH.sub.2 NH.sub.2 1 3,4-Di-F-PhCH.sub.2 CH.sub.2 CN (+)-pin1105 CH.sub.2 NH.sub.2 1 3,4-Di-Cl-PhCH.sub.2 CH.sub.2 CN (+)-pin1106 CH.sub.2 NH.sub.2 1 4-Br-PhCH.sub.2 CH.sub.2 CN (+)-pin1107 CH.sub.2 NH.sub.2 1 4-I-PhCH.sub.2 CH.sub.2 CN (+)-pin1108 CH.sub.2 NH.sub.2 1 4-Me-PhCH.sub.2 CH.sub.2 CN (+)-pin1109 CH.sub.2 NH.sub.2 1 2-MeO-PhCH.sub.2 CH.sub.2 CN (+)-pin1110 CH.sub.2 NH.sub.2 1 2-CN-PhCH.sub.2 CH.sub.2 CN (+)-pin1111 CH.sub.2 NH.sub.2 1 2-NC-PhCH.sub.2 CH.sub.2 CN (+)-pin1112 CH.sub.2 NH.sub.2 1 2-NO.sub.2 -PhCH.sub.2 CH.sub.2 CN (+)-pin1113 CH.sub.2 NH.sub.2 1 2-CF.sub.3 -PhCH.sub.2 CH.sub.2 CN (+)-pin1114 CH.sub.2 NH.sub.2 1 2-MeS-PhCH.sub.2 CH.sub.2 CN (+)-pin1115 CH.sub.2 NH.sub.2 1 3-MeSO-PhCH.sub.2 CH.sub.2 CN (+)-pin1116 CH.sub.2 NH.sub.2 1 3-MeSO.sub.2 -PhCH.sub.2 CH.sub.2 CN (+)-pin1117 CH.sub.2 NH.sub.2 1 2-NH.sub.2 -PhCH.sub.2 CH.sub.2 CN (+)-pin1118 CH.sub.2 NH.sub.2 1 3-NHMe-PhCH.sub.2 CH.sub.2 CN (+)-pin1119 CH.sub.2 NH.sub.2 1 2-CHO-PhCH.sub.2 CH.sub.2 CN (+)-pin1120 CH.sub.2 NH.sub.2 1 3-MeCO-PhCH.sub.2 CH.sub.2 CN (+)-pin1121 CH.sub.2 NH.sub.2 1 2-MeO.sub.2 C-PhCH.sub.2 CH.sub.2 CN (+)-pin1122 CH.sub.2 NH.sub.2 1 2-NH.sub.2 OC-PhCH.sub.2 CH.sub.2 CN (+)-pin1123 CH.sub.2 NH.sub.2 1 2-HOCH.sub.2 -PhCH.sub.2 CH.sub.2 CN (+)-pin1124 CH.sub.2 NH.sub.2 1 3,4-Di-F-PhCH.sub.2 CH.sub.2 CN OH, OH1125 CH.sub.2 NH.sub.2 1 3,4-Di-Cl-PhCH.sub.2 CH.sub.2 CN OH, OH1126 CH.sub.2 NH.sub.2 1 4-Br-PhCH.sub.2 CH.sub.2 CN OH, OH1127 CH.sub.2 NH.sub.2 1 4-I-PhCH.sub.2 CH.sub.2 CN OH, OH1128 CH.sub.2 NH.sub.2 1 4-Me-PhCH.sub.2 CH.sub.2 CN OH, OH1129 CH.sub.2 NH.sub.2 1 2-MeO-PhCH.sub.2 CH.sub.2 CN OH, OH1130 CH.sub.2 NH.sub.2 1 2-CN-PhCH.sub.2 CH.sub.2 CN OH, OH1131 CH.sub.2 NH.sub.2 1 2-NC-PhCH.sub.2 CH.sub.2 CN OH, OH1132 CH.sub.2 NH.sub.2 1 2-NO.sub.2 -PhCH.sub.2 CH.sub.2 CN OH, OH1133 CH.sub.2 NH.sub.2 1 2-CF.sub.3 -PhCH.sub.2 CH.sub.2 CN OH, OH1134 CH.sub.2 NH.sub.2 1 2-MeS-PhCH.sub.2 CH.sub.2 CN OH, OH1135 CH.sub.2 NH.sub.2 1 3-MeSO-PhCH.sub.2 CH.sub.2 CN OH, OH1136 CH.sub.2 NH.sub.2 1 3-MeSO.sub.2 -PhCH.sub.2 CH.sub.2 CN OH, OH1137 CH.sub.2 NH.sub.2 1 2-NH.sub.2 -PhCH.sub.2 CH.sub.2 CN OH, OH1138 CH.sub.2 NH.sub.2 1 3-NHMe-PhCH.sub.2 CH.sub.2 CN OH, OH1139 CH.sub.2 NH.sub.2 1 2-CHO-PhCH.sub.2 CH.sub.2 CN OH, OH1140 CH.sub.2 NH.sub.2 1 3-MeCO-PhCH.sub.2 CH.sub.2 CN OH, OH1141 CH.sub.2 NH.sub.2 1 2-MeO.sub.2 C-PhCH.sub.2 CH.sub.2 CN OH, OH1142 CH.sub.2 NH.sub.2 1 2-NH.sub.2 OC-PhCH.sub.2 CH.sub.2 CN OH, OH1143 CH.sub.2 NH.sub.2 1 2-HOCH.sub.2 -PhCH.sub.2 CH.sub.2 CN OH, OH1144 NH(CNH)NH.sub.2 1 PhCH.sub.2 H OH, OH1145 NH(CNH)NH.sub.2 1 PhCH.sub.2 Methyl OH, OH1146 NH(CNH)NH.sub.2 1 PhCH.sub.2 Ethyl OH, OH1147 NH(CNH)NH.sub.2 1 PhCH.sub.2 n-Propyl OH, OH1148 NH(CNH)NH.sub.2 1 PhCH.sub.2 n-Butyl OH, OH1149 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 SCH.sub.3 OH, OH1150 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 (SO)CH.sub.3 OH, OH1151 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 (SO.sub.2)CH.sub.3 OH, OH1152 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 SCH.sub.3 OH, OH1153 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 (SO)CH.sub.3 OH, OH1154 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3 OH, OH1155 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CN OH, OH1156 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CN OH, OH1157 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 CN OH, OH1158 NH(CNH)NH.sub.2 1 PhCH.sub.2 CF.sub.3 OH, OH1159 NH(CNH)NH.sub.2 1 PhCH.sub.2 CF.sub.2 CF.sub.3 OH, OH1160 NH(CNH)NH.sub.2 1 PhCH.sub.2 CF.sub.2 CF.sub.2 CF.sub.3 OH, OH1161 NH(CNH)NH.sub.2 1 PhCH.sub.2 CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3 OH, OH1162 NH(CNH)NH.sub.2 1 PhCH.sub.2 F.sub.5 -Ph OH, OH1163 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CO.sub.2 H OH, OH1164 NH(CNH)NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.2 CO.sub.2 H OH, OH1165 NH(CNH)NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.3 CO.sub.2 H OH, OH1166 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CN.sub.4 H OH, OH1167 NH(CNH)NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.2 CN.sub.4 H OH, OH1168 NH(CNH)NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.3 CN.sub.4 H OH, OH1169 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 NO.sub.2 OH, OH1170 NH(CNH)NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.2 NO.sub.2 OH, OH1171 NH(CNH)NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.3 NO.sub.2 OH, OH1172 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 OH OH, OH1173 NH(CNH)NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.2 OH OH, OH1174 NH(CNH)NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.3 OH OH, OH1175 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CO.sub.2 Me OH, OH1176 NH(CNH)NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.2 CO.sub.2 Me OH, OH1177 NH(CNH)NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.3 CO.sub.2 Me OH, OH1178 NH(CNH)NH.sub.2 1 PhCH.sub.2 Ph OH, OH1179 NH(CNH)NH.sub.2 1 PhCH.sub.2 PhCH.sub.2 OH, OH1180 NH(CNH)NH.sub.2 1 PhCH.sub.2 Ph(CH.sub.2).sub.2 OH, OH1181 NH(CNH)NH.sub.2 1 PhCH.sub.2 3-NO.sub.2 -Ph OH, OH1182 NH(CNH)NH.sub.2 1 PhCH.sub.2 4-NO.sub.2 -Ph OH, OH1183 NH(CNH)NH.sub.2 1 PhCH.sub.2 3-CO.sub.2 H-Ph OH, OH1184 NH(CNH)NH.sub.2 1 PhCH.sub.2 4-CO.sub.2 H-Ph OH, OH1185 NH(CNH)NH.sub.2 1 PhCH.sub.2 3-CN.sub.4 H-Ph OH, OH1186 NH(CNH)NH.sub.2 1 PhCH.sub.2 4-CN.sub.4 H-Ph OH, OH1187 NH(CNH)NH.sub.2 1 PhCH.sub.2 3-(HOCH.sub.2)-Ph OH, OH1188 NH(CNH)NH.sub.2 1 PhCH.sub.2 4-(HOCH.sub.2)-Ph OH, OH1189 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CHO (+)-pin1190 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CHO OH, OH1191 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 CHO (+)-pin1192 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 CHO OH, OH1193 S(CNH)NH.sub.2 1 PhCH.sub.2 H (+)-pin1194 S(CNH)NH.sub.2 1 PhCH.sub.2 Methyl (+)-pin1195 S(CNH)NH.sub.2 1 PhCH.sub.2 Ethyl (+)-pin1196 S(CNH)NH.sub.2 1 PhCH.sub.2 n-Propyl (+)-pin1197 S(CNH)NH.sub.2 1 PhCH.sub.2 n-Butyl (+)-pin1198 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 SCH.sub.3 (+)-pin1199 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 (SO)CH.sub.3 (+)-pin1200 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 (SO.sub.2)CH.sub.3 (+)-pin1201 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 SCH.sub.3 (+)-pin1202 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 (SO)CH.sub.3 (+)-pin1203 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3 (+)-pin1204 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CN (+)-pin1205 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CN (+)-pin1206 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 CN (+)-pin1207 S(CNH)NH.sub.2 1 PhCH.sub.2 CF.sub.3 (+)-pin1208 S(CNH)NH.sub.2 1 PhCH.sub.2 CF.sub.2 CF.sub.3 (+)-pin1209 S(CNH)NH.sub.2 1 PhCH.sub.2 CF.sub.2 CF.sub.2 CF.sub.3 (+)-pin1210 S(CNH)NH.sub.2 1 PhCH.sub.2 CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3 (+)-pin1211 S(CNH)NH.sub.2 1 PhCH.sub.2 F.sub.5 -Ph (+)-pin1212 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CO.sub.2 H (+)-pin1213 S(CNH)NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.2 CO.sub.2 H (+)-pin1214 S(CNH)NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.3 CO.sub.2 H (+)-pin1215 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CN.sub.4 H (+)-pin1216 S(CNH)NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.2 CN.sub.4 H (+)-pin1217 S(CNH)NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.3 CN.sub.4 H (+)-pin1218 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 NO.sub.2 (+)-pin1219 S(CNH)NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.2 NO.sub.2 (+)-pin1220 S(CNH)NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.3 NO.sub.2 (+)-pin1221 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 OH (+)-pin1222 S(CNH)NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.2 OH (+)-pin1223 S(CNH)NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.3 OH (+)-pin1224 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CO.sub.2 Me (+)-pin1225 S(CNH)NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.2 CO.sub.2 Me (+)-pin1226 S(CNH)NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.3 CO.sub.2 Me (+)-pin1227 S(CNH)NH.sub.2 1 PhCH.sub.2 Ph (+)-pin1228 S(CNH)NH.sub.2 1 PhCH.sub.2 PhCH.sub.2 (+)-pin1229 S(CNH)NH.sub.2 1 PhCH.sub.2 Ph(CH.sub.2).sub.2 (+)-pin1230 S(CNH)NH.sub.2 1 PhCH.sub.2 3-NO.sub.2 -Ph (+)-pin1231 S(CNH)NH.sub.2 1 PhCH.sub.2 4-NO.sub.2 -Ph (+)-pin1232 S(CNH)NH.sub.2 1 PhCH.sub.2 3-CO.sub.2 H-Ph (+)-pin1233 S(CNH)NH.sub.2 1 PhCH.sub.2 4-CO.sub.2 H-Ph (+)-pin1234 S(CNH)NH.sub.2 1 PhCH.sub.2 3-CN.sub.4 H-Ph (+)-pin1235 S(CNH)NH.sub.2 1 PhCH.sub.2 4-CN.sub.4 H-Ph (+)-pin1236 S(CNH)NH.sub.2 1 PhCH.sub.2 3-(HOCH.sub.2)-Ph (+)-pin1237 S(CNH)NH.sub.2 1 PhCH.sub.2 4-(HOCH.sub.2)-Ph (+)-pin1238 CN 1 PhCH.sub.2 CH.sub.2 CN (+)-pin1239 NO.sub.2 1 PhCH.sub.2 CH.sub.2 CN (+)-pin1240 CH.sub.2 NO.sub.2 1 PhCH.sub.2 CH.sub.2 CN (+)-pin1241 CF.sub.3 1 PhCH.sub.2 CH.sub.2 CN (+)-pin1242 NH.sub.2 1 PhCH.sub.2 CH.sub.2 CN (+)-pin1243 NHOH 1 PhCH.sub.2 CH.sub.2 CN (+)-pin1244 NHOME 1 PhCH.sub.2 CH.sub.2 CN (+)-pin1245 CH.sub.2 NHOH 1 PhCH.sub.2 CH.sub.2 CN (+)-pin1246 CH.sub.2 NHOMe 1 PhCH.sub.2 CH.sub.2 CN (+)-pin1247 NH(CNH)CH.sub.3 1 PhCH.sub.2 CH.sub.2 CN (+)-pin1248 NH(CNH)NHOH 1 PhCH.sub.2 CH.sub.2 CN (+)-pin1249 NH(CNH)NHNH.sub.2 1 PhCH.sub.2 CH.sub.2 CN (+)-pin1250 NH(CNH)NHCN 1 PhCH.sub.2 CH.sub.2 CN (+)-pin1251 NH(CNH)NHCH.sub.3 1 PhCH.sub.2 CH.sub.2 CN (+)-pin1252 NH(CNH)NHCOCH.sub.3 1 PhCH.sub.2 CH.sub.2 CN (+)-pin1253 C(NH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CN (+)-pin1254 C(NH)NHMe 1 PhCH.sub.2 CH.sub.2 CN (+)-pin1255 C(NH)NHCOMe 1 PhCH.sub.2 CH.sub.2 CN (+)-pin1256 CONH.sub.2 1 PhCH.sub.2 CH.sub.2 CN (+)-pin1257 CONHCH.sub.3 1 PhCH.sub.2 CH.sub.2 CN (+)-pin1258 CO.sub.2 CH.sub.3 1 PhCH.sub.2 CH.sub.2 CN (+)-pin1259 OH 1 PhCH.sub.2 CH.sub.2 CN (+)-pin1260 CH.sub.2 OH 1 PhCH.sub.2 CH.sub.2 CN (+)-pin1261 SCH.sub.3 1 PhCH.sub.2 CH.sub.2 CN (+)-pin1262 SOCH.sub.3 1 PhCH.sub.2 CH.sub.2 CN (+)-pin1263 SO.sub.2 CH.sub.3 1 PhCH.sub.2 CH.sub.2 CN (+)-pin1264 S(CNH)NHCH.sub.3 1 PhCH.sub.2 CH.sub.2 CN (+)-pin1265 S(CNH)NHCOCH.sub.3 1 PhCH.sub.2 CH.sub.2 CN (+)-pin1266 S(CNH)NH.sub.2 1 PhCH.sub.2 H OH, OH1267 S(CNH)NH.sub.2 1 PhCH.sub.2 Methyl OH, OH1268 S(CNH)NH.sub.2 1 PhCH.sub.2 Ethyl OH, OH1269 S(CNH)NH.sub.2 1 PhCH.sub.2 n-Propyl OH, OH1270 S(CNH)NH.sub.2 1 PhCH.sub.2 n-Butyl OH, OH1271 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 SCH.sub.3 OH, OH1272 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 (SO)CH.sub.3 OH, OH1273 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 (SO.sub.2)CH.sub.3 OH, OH1274 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 SCH.sub.3 OH, OH1275 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 (SO)CH.sub.3 OH, OH1276 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3 OH, OH1277 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CN OH, OH1278 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CN OH, OH1279 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 CN OH, OH1280 S(CNH)NH.sub.2 1 PhCH.sub.2 CF.sub.3 OH, OH1281 S(CNH)NH.sub.2 1 PhCH.sub.2 CF.sub.2 CF.sub.3 OH, OH1282 S(CNH)NH.sub.2 1 PhCH.sub.2 CF.sub.2 CF.sub.2 CF.sub.3 OH, OH1283 S(CNH)NH.sub.2 1 PhCH.sub.2 CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3 OH, OH1284 S(CNH)NH.sub.2 1 PhCH.sub.2 F.sub.5 -Ph OH, OH1285 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CO.sub.2 H OH, OH1286 S(CNH)NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.2 CO.sub.2 H OH, OH1287 S(CNH)NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.3 CO.sub.2 H OH, OH1288 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CN.sub.4 H OH, OH1289 S(CNH)NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.2 CN.sub.4 H OH, OH1290 S(CNH)NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.3 CN.sub.4 H OH, OH1291 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 NO.sub.2 OH, OH1292 S(CNH)NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.2 NO.sub.2 OH, OH1293 S(CNH)NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.3 NO.sub.2 OH, OH1294 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 OH OH, OH1295 S(CNH)NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.2 OH OH, OH1296 S(CNH)NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.3 OH OH, OH1297 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CO.sub.2 Me OH, OH1298 S(CNH)NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.2 CO.sub.2 Me OH, OH1299 S(CNH)NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.3 CO.sub.2 Me OH, OH1300 S(CNH)NH.sub.2 1 PhCH.sub.2 Ph OH, OH1301 S(CNH)NH.sub.2 1 PhCH.sub.2 PhCH.sub.2 OH, OH1302 S(CNH)NH.sub.2 1 PhCH.sub.2 Ph(CH.sub.2).sub.2 OH, OH1303 S(CNH)NH.sub.2 1 PhCH.sub.2 3-NO.sub.2 -Ph OH, OH1304 S(CNH)NH.sub.2 1 PhCH.sub.2 4-NO.sub.2 -Ph OH, OH1305 S(CNH)NH.sub.2 1 PhCH.sub.2 3-CO.sub.2 H-Ph OH, OH1306 S(CNH)NH.sub.2 1 PhCH.sub.2 4-CO.sub.2 H-Ph OH, OH1307 S(CNH)NH.sub.2 1 PhCH.sub.2 3-CN.sub.4 H-Ph OH, OH1308 S(CNH)NH.sub.2 1 PhCH.sub.2 4-CN.sub.4 H-Ph OH, OH1309 S(CNH)NH.sub.2 1 PhCH.sub.2 3-(HOCH.sub.2)-Ph OH, OH1310 S(CNH)NH.sub.2 1 PhCH.sub.2 4-(HOCH.sub.2)-Ph OH, OH1311 CN 1 PhCH.sub.2 CH.sub.2 CN OH, OH1312 NO.sub.2 1 PhCH.sub.2 CH.sub.2 CN OH, OH1313 CH.sub.2 NO.sub.2 1 PhCH.sub.2 CH.sub.2 CN OH, OH1314 CF.sub.3 1 PhCH.sub.2 CH.sub.2 CN OH, OH1315 NH.sub.2 1 PhCH.sub.2 CH.sub.2 CN OH, OH1316 NHOH 1 PhCH.sub.2 CH.sub.2 CN OH, OH1317 NHOME 1 PhCH.sub.2 CH.sub.2 CN OH, OH1318 CH.sub.2 NHOH 1 PhCH.sub.2 CH.sub.2 CN OH, OH1319 CH.sub.2 NHOMe 1 PhCH.sub.2 CH.sub.2 CN OH, OH1320 NH(CNH)CH.sub.3 1 PhCH.sub.2 CH.sub.2 CN OH, OH1321 NH(CNH)NHOH 1 PhCH.sub.2 CH.sub.2 CN OH, OH1322 NH(CNH)NHNH.sub.2 1 PhCH.sub.2 CH.sub.2 CN OH, OH1323 NH(CNH)NHCN 1 PhCH.sub.2 CH.sub.2 CN OH, OH1324 NH(CNH)NHCH.sub.3 1 PhCH.sub.2 CH.sub.2 CN OH, OH1325 NH(CNH)NHCOCH.sub.3 1 PhCH.sub.2 CH.sub.2 CN OH, OH1326 C(NH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CN OH, OH1327 C(NH)NHMe 1 PhCH.sub.2 CH.sub.2 CN OH, OH1328 C(NH)NHCOMe 1 PhCH.sub.2 CH.sub.2 CN OH, OH1329 CONH.sub.2 1 PhCH.sub.2 CH.sub.2 CN OH, OH1330 CONHCH.sub.3 1 PhCH.sub.2 CH.sub.2 CN OH, OH1331 CO.sub.2 CH.sub.3 1 PhCH.sub.2 CH.sub.2 CN OH, OH1332 OH 1 PhCH.sub.2 CH.sub.2 CN OH, OH1333 CH.sub.2 OH 1 PhCH.sub.2 CH.sub.2 CN OH, OH1334 SCH.sub.3 1 PhCH.sub.2 CH.sub.2 CN OH, OH1335 SOCH.sub.3 1 PhCH.sub.2 CH.sub.2 CN OH, OH1336 SO.sub.2 CH.sub.3 1 PhCH.sub.2 CH.sub.2 CN OH, OH1337 S(CNH)NHCH.sub.3 1 PhCH.sub.2 CH.sub.2 CN OH, OH1338 S(CNH)NHCOCH.sub.3 1 PhCH.sub.2 CH.sub.2 CN OH, OH1339 CH.sub.2 NH.sub.2 2 PhCH.sub.2 H (+)-pin1340 CH.sub.2 NH.sub.2 2 PhCH.sub.2 H OH, OH1341 OMe 1 PhCH.sub.2 H (+)-pin1342 OMe 1 PhCH.sub.2 Methyl (+)-pin1343 OMe 1 PhCH.sub.2 Ethyl (+)-pin1344 OMe 1 PhCH.sub.2 n-Propyl (+)-pin1345 OMe 1 PhCH.sub.2 n-Butyl (+)-pin1346 OMe 1 PhCH.sub.2 CH.sub.2 SCH.sub.3 (+)-pin1347 OMe 1 PhCH.sub.2 CH.sub.2 (SO)CH.sub.3 (+)-pin1348 OMe 1 PhCH.sub.2 CH.sub.2 (SO.sub.2)CH.sub.3 (+)-pin1349 OMe 1 PhCH.sub.2 CH.sub.2 CH.sub.2 SCH.sub.3 (+)-pin1350 OMe 1 PhCH.sub.2 CH.sub.2 CH.sub.2 (SO)CH.sub.3 (+)-pin1351 OMe 1 PhCH.sub.2 CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3 (+)-pin1352 OMe 1 PhCH.sub.2 CH.sub.2 CN (+)-pin CR1353 OMe 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CN (+)-pin1354 OMe 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 CN (+)-pin1355 OMe 1 PhCH.sub.2 CF.sub.3 (+)-pin1356 OMe 1 PhCH.sub.2 CF.sub.2 CF.sub.3 (+)-pin1357 OMe 1 PhCH.sub.2 CF.sub.2 CF.sub.2 CF.sub.3 (+)-pin1358 OMe 1 PhCH.sub.2 CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3 (+)-pin1359 OMe 1 PhCH.sub.2 F.sub.5 -Ph (+)-pin1360 OMe 1 PhCH.sub.2 CH.sub.2 CO.sub.2 H (+)-pin1361 OMe 1 PhCH.sub.2 (CH.sub.2).sub.2 CO.sub.2 H (+)-pin1362 OMe 1 PhCH.sub.2 (CH.sub.2).sub.3 CO.sub.2 H (+)-pin1363 OMe 1 PhCH.sub.2 CH.sub.2 CN.sub.4 H (+)-pin1364 OMe 1 PhCH.sub.2 (CH.sub.2).sub.2 CN.sub.4 H (+)-pin1365 OMe 1 PhCH.sub.2 (CH.sub.2).sub.3 CN.sub.4 H (+)-pin1366 OMe 1 PhCH.sub.2 CH.sub.2 NO.sub.2 (+)-pin1367 OMe 1 PhCH.sub.2 (CH.sub.2).sub.2 NO.sub.2 (+)-pin1368 OMe 1 PhCH.sub.2 (CH.sub.2).sub.3 NO.sub.2 (+)-pin1369 OMe 1 PhCH.sub.2 CH.sub.2 OH (+)-pin1370 OMe 1 PhCH.sub.2 (CH.sub.2).sub.2 OH (+)-pin1371 OMe 1 PhCH.sub.2 (CH.sub.2).sub.3 OH (+)-pin1372 OMe 1 PhCH.sub.2 CH.sub.2 CO.sub.2 Me (+)-pin1373 OMe 1 PhCH.sub.2 (CH.sub.2).sub.2 CO.sub.2 Me (+)-pin1374 OMe 1 PhCH.sub.2 (CH.sub.2).sub.3 CO.sub.2 Me (+)-pin1375 OMe 1 PhCH.sub.2 Ph (+)-pin1376 OMe 1 PhCH.sub.2 PhCH.sub.2 (+)-pin1377 OMe 1 PhCH.sub.2 Ph(CH.sub.2).sub.2 (+)-pin1378 OMe 1 PhCH.sub.2 3-NO.sub.2 -Ph (+)-pin1379 OMe 1 PhCH.sub.2 4-NO.sub.2 -Ph (+)-pin1380 OMe 1 PhCH.sub.2 3-CO.sub.2 H-Ph (+)-pin1381 OMe 1 PhCH.sub.2 4-CO.sub.2 H-Ph (+)-pin1382 OMe 1 PhCH.sub.2 3-CN.sub.4 H-Ph (+)-pin1383 OMe 1 PhCH.sub.2 4-CN.sub.4 H-Ph (+)-pin1384 OMe 1 PhCH.sub.2 3-(HOCH.sub.2)-Ph (+)-pin1385 OMe 1 PhCH.sub.2 4-(HOCH.sub.2)-Ph (+)-pin1386 OMe 1 PhCH.sub.2 H OH, OH1387 OMe 1 PhCH.sub.2 Methyl OH, OH1388 OMe 1 PhCH.sub.2 Ethyl OH, OH1389 OMe 1 PhCH.sub.2 n-Propyl OH, OH1390 OMe 1 PhCH.sub.2 n-Butyl OH, OH1391 OMe 1 PhCH.sub.2 CH.sub.2 SCH.sub.3 OH, OH1392 OMe 1 PhCH.sub.2 CH.sub.2 (SO)CH.sub.3 OH, OH1393 OMe 1 PhCH.sub.2 CH.sub.2 (SO.sub.2)CH.sub.3 OH, OH1394 OMe 1 PhCH.sub.2 CH.sub.2 CH.sub.2 SCH.sub.3 OH, OH1395 OMe 1 PhCH.sub.2 CH.sub.2 CH.sub.2 (SO)CH.sub.3 OH, OH1396 OMe 1 PhCH.sub.2 CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3 OH, OH1397 OMe 1 PhCH.sub.2 CH.sub.2 CN OH, OH1398 OMe 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CN OH, OH1399 OMe 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 CN OH, OH1400 OMe 1 PhCH.sub.2 CF.sub.3 OH, OH1401 OMe 1 PhCH.sub.2 CF.sub.2 CF.sub.3 OH, OH1402 OMe 1 PhCH.sub.2 CF.sub.2 CF.sub.2 CF.sub.3 OH, OH1403 OMe 1 PhCH.sub.2 CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3 OH, OH1404 OMe 1 PhCH.sub.2 F.sub.5 -Ph OH, OH1405 OMe 1 PhCH.sub.2 CH.sub.2 CO.sub.2 H OH, OH1406 OMe 1 PhCH.sub.2 (CH.sub.2).sub.2 CO.sub.2 H OH, OH1407 OMe 1 PhCH.sub.2 (CH.sub.2).sub.3 CO.sub.2 H OH, OH1408 OMe 1 PhCH.sub.2 CH.sub.2 CN.sub.4 H OH, OH1409 OMe 1 PhCH.sub.2 (CH.sub.2).sub.2 CN.sub.4 H OH, OH1410 OMe 1 PhCH.sub.2 (CH.sub.2).sub.3 CN.sub.4 H OH, OH1411 OMe 1 PhCH.sub.2 CH.sub.2 NO.sub.2 OH, OH1412 OMe 1 PhCH.sub.2 (CH.sub.2).sub.2 NO.sub.2 OH, OH1413 OMe 1 PhCH.sub.2 (CH.sub.2).sub.3 NO.sub.2 OH, OH1414 OMe 1 PhCH.sub.2 CH.sub.2 OH OH, OH1415 OMe 1 PhCH.sub.2 (CH.sub.2).sub.2 OH OH, OH1416 OMe 1 PhCH.sub.2 (CH.sub.2).sub.3 OH OH, OH1417 OMe 1 PhCH.sub.2 CH.sub.2 CO.sub.2 Me OH, OH1418 OMe 1 PhCH.sub.2 (CH.sub.2).sub.2 CO.sub.2 Me OH, OH1419 OMe 1 PhCH.sub.2 (CH.sub.2).sub.3 CO.sub.2 Me OH, OH1420 OMe 1 PhCH.sub.2 PhCH.sub.2 OH, OH1421 OMe 1 PhCH.sub.2 PhCH.sub.2 OH, OH1422 OMe 1 PhCH.sub.2 Ph(CH.sub.2).sub.2 OH, OH1423 OMe 1 PhCH.sub.2 3-NO.sub.2 -Ph OH, OH1424 OMe 1 PhCH.sub.2 4-NO.sub.2 -Ph OH, OH1425 OMe 1 PhCH.sub.2 3-CO.sub.2 H-Ph OH, OH1426 OMe 1 PhCH.sub.2 4-CO.sub.2 H-Ph OH, OH1427 OMe 1 PhCH.sub.2 3-CN.sub.4 H-Ph OH, OH1428 OMe 1 PhCH.sub.2 4-CN.sub.4 H-Ph OH, OH1429 OMe 1 PhCH.sub.2 3-(HOCH.sub.2)-Ph OH, OH1430 OMe 1 PhCH.sub.2 4-(HOCH.sub.2)-Ph OH, OH1431 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 H (+)-pin AX1432 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 Methyl (+)-pin1433 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 Ethyl (+)-pin1434 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 n-Propyl (+)-pin1435 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 n-Butyl (+)-pin1436 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 SCH.sub.3 (+)-pin1437 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 (SO)CH.sub.3 (+)-pin1438 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 (SO.sub.2)CH.sub.3 (+)-pin1439 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 SCH.sub.3 (+)-pin1440 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 (SO)CH.sub.3 (+)-pin1441 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3 (+)-pin1442 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CN (+)-pin1443 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 CN (+)-pin1444 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 CN (+)-pin1445 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 CF.sub.3 (+)-pin1446 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 CF.sub.2 CF.sub.3 (+)-pin1447 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 CF.sub.2 CF.sub.2 CF.sub.3 (+)-pin1448 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3 (+)-pin1449 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 F.sub.5 -Ph (+)-pin1450 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CO.sub.2 H (+)-pin1451 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.2 CO.sub.2 H (+)-pin1452 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.3 CO.sub.2 H (+)-pin1453 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CN.sub.4 H (+)-pin1454 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.2 CN.sub.4 H (+)-pin1455 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.3 CN.sub.4 H (+)-pin1456 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 NO.sub.2 (+)-pin1457 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.2 NO.sub.2 (+)-pin1458 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.3 NO.sub.2 (+)-pin1459 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 OH (+)-pin CS1460 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.2 OH (+)-pin1461 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.3 OH (+)-pin1462 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CO.sub.2 Me (+)-pin1463 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.2 CO.sub.2 Me (+)-pin1464 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.3 CO.sub.2 Me (+)-pin1465 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 Ph (+)-pin1466 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 PhCH.sub.2 (+)-pin1467 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 Ph(CH.sub.2).sub.2 (+)-pin AY1468 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 3-NO.sub.2 -Ph (+)-pin1469 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 4-NO.sub.2 -Ph (+)-pin1470 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 3-CO.sub.2 H-Ph (+)-pin1471 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 4-CO.sub.2 H-Ph (+)-pin1472 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 3-CN.sub.4 H-Ph (+)-pin1473 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 4-CN.sub.4 H-Ph (+)-pin1474 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 3-(HOCH.sub.2)-Ph (+)-pin1475 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 4-(HOCH.sub.2)-Ph (+)-pin1476 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 H (+)-pin1477 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 Methyl (+)-pin1478 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 Ethyl (+)-pin1479 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 n-Propyl (+)-pin1480 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 n-Butyl (+)-pin1481 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 SCH.sub.3 (+)-pin1482 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 (SO)CH.sub.3 (+)-pin1483 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 (SO.sub.2)CH.sub.3 (+)-pin1484 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 SCH.sub.3 (+)-pin1485 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 (SO)CH.sub.3 (+)-pin1486 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3 (+)-pin1487 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CN (+)-pin1488 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 CN (+)-pin1489 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 CN (+)-pin1490 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CF.sub.3 (+)-pin1491 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CF.sub.2 CF.sub.3 (+)-pin1492 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CF.sub.2 CF.sub.2 CF.sub.3 (+)-pin1493 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3 (+)-pin1494 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 F.sub.5 -Ph (+)-pin1495 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CO.sub.2 H (+)-pin1496 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.2 CO.sub.2 H (+)-pin1497 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.3 CO.sub.2 H (+)-pin1498 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CN.sub.4 H (+)-pin1499 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.2 CN.sub.4 H (+)-pin1500 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.3 CN.sub.4 H (+)-pin1501 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 NO.sub.2 (+)-pin1502 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.2 NO.sub.2 (+)-pin1503 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.3 NO.sub.2 (+)-pin1504 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 OH (+)-pin1505 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.2 OH (+)-pin1506 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.3 OH (+)-pin1507 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CO.sub.2 Me (+)-pin1508 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.2 CO.sub.2 Me (+)-pin1509 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.3 CO.sub.2 Me (+)-pin1510 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 Ph (+)-pin1511 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 PhCH.sub.2 (+)-pin1512 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 Ph(CH.sub.2).sub.2 (+)-pin1513 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 3-NO.sub.2 -Ph (+)-pin1514 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 4-NO.sub.2 -Ph (+)-pin1515 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 3-CO.sub.2 H-Ph (+)-pin1516 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 4-CO.sub.2 H-Ph (+)-pin1517 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 3-CN.sub.4 H-Ph (+)-pin1518 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 4-CN.sub.4 H-Ph (+)-pin1519 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 3-(HOCH.sub.2)-Ph (+)-pin1520 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 4-(HOCH.sub.2)-Ph (+)-pin1521 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 H OH, OH AZ1522 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 Methyl OH, OH1523 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 Ethyl OH, OH1524 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 n-Propyl OH, OH1525 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 n-Butyl OH, OH1526 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 SCH.sub.3 OH, OH1527 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 (SO)CH.sub.3 OH, OH1528 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 (SO.sub.2)CH.sub.3 OH, OH1529 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 SCH.sub.3 OH, OH1530 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 (SO)CH.sub.3 OH, OH1531 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3 OH, OH1532 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CN OH, OH1533 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 CN OH, OH1534 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 CN OH, OH1535 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 CF.sub.3 OH, OH1536 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 CF.sub.2 CF.sub.3 OH, OH1537 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 CF.sub.2 CF.sub.2 CF.sub.3 OH, OH1538 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3 OH, OH1539 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 F.sub.5 -Ph OH, OH1540 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CO.sub.2 H OH, OH1541 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.2 CO.sub.2 H OH, OH1542 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.3 CO.sub.2 H OH, OH1543 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CN.sub.4 H OH, OH1544 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.2 CN.sub.4 H OH, OH1545 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.3 CN.sub.4 H OH, OH1546 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 NO.sub.2 OH, OH1547 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.2 NO.sub.2 OH, OH1548 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.3 NO.sub.2 OH, OH1549 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 OH OH, OH1550 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.2 OH OH, OH1551 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.3 OH OH, OH1552 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CO.sub.2 Me OH, OH1553 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.2 CO.sub.2 Me OH, OH1554 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.3 CO.sub.2 Me OH, OH1555 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 Ph OH, OH1556 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 PhCH.sub.2 OH, OH1557 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 Ph(CH.sub.2).sub.2 OH, OH AJ1558 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 3-NO.sub.2 -Ph OH, OH1559 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 4-NO.sub.2 -Ph OH, OH1560 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 3-CO.sub.2 H-Ph OH, OH1561 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 4-CO.sub.2 H-Ph OH, OH1562 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 3-CN.sub.4 H-Ph OH, OH1563 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 4-CN.sub.4 H-Ph OH, OH1564 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 3-(HOCH.sub.2)-Ph OH, OH1565 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 4-(HOCH.sub.2)-Ph OH, OH1566 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 H OH, OH1567 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 Methyl OH, OH1568 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 Ethyl OH, OH1569 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 n-Propyl OH, OH1570 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 n-Butyl OH, OH1571 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 SCH.sub.3 OH, OH1572 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 (SO)CH.sub.3 OH, OH1573 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 (SO.sub.2)CH.sub.3 OH, OH1574 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 SCH.sub.3 OH, OH1575 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 (SO)CH.sub.3 OH, OH1576 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3 OH, OH1577 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CN OH, OH1578 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 CN OH, OH1579 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 CN OH, OH1580 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CF.sub.3 OH, OH1581 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CF.sub.2 CF.sub.3 OH, OH1582 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CF.sub.2 CF.sub.2 CF.sub.3 OH, OH1583 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3 OH, OH1584 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 F.sub.5 -Ph OH, OH1585 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CO.sub.2 H OH, OH1586 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.2 CO.sub.2 H OH, OH1587 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.3 CO.sub.2 H OH, OH1588 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CN.sub.4 H OH, OH1589 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.2 CN.sub.4 H OH, OH1590 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.3 CN.sub.4 H OH, OH1591 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 NO.sub.2 OH, OH1592 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.2 NO.sub.2 OH, OH1593 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.3 NO.sub.2 OH, OH1594 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 OH OH, OH1595 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.2 OH OH, OH1596 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.3 OH OH, OH1597 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CO.sub.2 Me OH, OH1598 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.2 CO.sub.2 Me OH, OH1599 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.3 CO.sub.2 Me OH, OH1600 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 PhCH.sub.2 CH.sub.2 OH, OH1601 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 PhCH.sub.2 CH.sub.2 OH, OH1602 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 Ph(CH.sub.2).sub.2 OH, OH1603 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 3-NO.sub.2 -Ph OH, OH1604 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 4-NO.sub.2 -Ph OH, OH1605 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 3-CO.sub.2 H-Ph OH, OH1606 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 4-CO.sub.2 H-Ph OH, OH1607 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 3-CN.sub.4 H-Ph OH, OH1608 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 4-CN.sub.4 H-Ph OH, OH1609 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 3-(HOCH.sub.2)-Ph OH, OH1610 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 4-(HOCH.sub.2)-Ph OH, OH1611 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 H (+)-pin1612 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 Methyl (+)-pin1613 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 Ethyl (+)-pin1614 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 n-Propyl (+)-pin1615 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 n-Butyl (+)-pin1616 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 SCH.sub.3 (+)-pin1617 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 (SO)CH.sub.3 (+)-pin1618 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 (SO.sub.2)CH.sub.3 (+)-pin1619 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 SCH.sub.3 (+)-pin1620 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 (SO)CH.sub.3 (+)-pin1621 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3 (+)-pin1622 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CN (+)-pin1623 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 CN (+)-pin1624 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 CN (+)-pin1625 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CF.sub.3 (+)-pin1626 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CF.sub.2 CF.sub.3 (+)-pin1627 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CF.sub.2 CF.sub.2 CF.sub.3 (+)-pin1628 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3 (+)-pin1629 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 F.sub.5 -Ph (+)-pin1630 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CO.sub.2 H (+)-pin1631 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.2 CO.sub.2 H (+)-pin1632 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.3 CO.sub.2 H (+)-pin1633 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CN.sub.4 H (+)-pin1634 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.2 CN.sub.4 H (+)-pin1635 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.3 CN.sub.4 H (+)-pin1636 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 NO.sub.2 (+)-pin1637 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.2 NO.sub.2 (+)-pin1638 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.3 NO.sub.2 (+)-pin1639 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 OH (+)-pin1640 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.2 OH (+)-pin1641 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.3 OH (+)-pin1642 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CO.sub.2 Me (+)-pin1643 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.2 CO.sub.2 Me (+)-pin1644 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.3 CO.sub.2 Me (+)-pin1645 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 Ph (+)-pin1646 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 PhCH.sub.2 (+)-pin1647 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 Ph(CH.sub.2).sub.2 (+)-pin1648 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 3-NO.sub.2 -Ph (+)-pin1649 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 4-NO.sub.2 -Ph (+)-pin1650 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 3-CO.sub.2 H-Ph (+)-pin1651 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 4-CO.sub.2 H-Ph (+)-pin1652 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 3-CN.sub.4 H-Ph (+)-pin1653 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 4-CN.sub.4 H-Ph (+)-pin1654 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 3-(HOCH.sub.2)-Ph (+)-pin1655 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 4-(HOCH.sub.2)-Ph (+)-pin1656 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 H OH, OH1657 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 Methyl OH, OH1658 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 Ethyl OH, OH1659 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 n-Propyl OH, OH1660 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 n-Butyl OH, OH1661 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 SCH.sub.3 OH, OH1662 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 (SO)CH.sub.3 OH, OH1663 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 (SO.sub.2)CH.sub.3 OH, OH1664 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 SCH.sub.3 OH, OH1665 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 (SO)CH.sub.3 OH, OH1666 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3 OH, OH1667 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CN OH, OH1668 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 CN OH, OH1669 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 CN OH, OH1670 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CF.sub.3 OH, OH1671 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CF.sub.2 CF.sub.3 OH, OH1672 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CF.sub.2 CF.sub.2 CF.sub.3 OH, OH1673 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3 OH, OH1674 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 F.sub.5 -Ph OH, OH1675 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CO.sub.2 H OH, OH1676 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.2 CO.sub.2 H OH, OH1677 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.3 CO.sub.2 H OH, OH1678 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CN.sub.4 H OH, OH1679 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.2 CN.sub.4 H OH, OH1680 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.3 CN.sub.4 H OH, OH1681 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 NO.sub.2 OH, OH1682 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.2 NO.sub.2 OH, OH1683 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.3 NO.sub.2 OH, OH1684 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 OH OH, OH1685 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.2 OH OH, OH1686 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.3 OH OH, OH1687 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CO.sub.2 Me OH, OH1688 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.2 CO.sub.2 Me OH, OH1689 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.3 CO.sub.2 Me OH, OH1690 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 Ph OH, OH1691 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 PhCH.sub.2 OH, OH1692 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 Ph(CH.sub.2).sub.2 OH, OH1693 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 3-NO.sub.2 -Ph OH, OH1694 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 4-NO.sub.2 -Ph OH, OH1695 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 3-CO.sub.2 H-Ph OH, OH1696 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 4-CO.sub.2 H-Ph OH, OH1697 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 3-CN.sub.4 H-Ph OH, OH1698 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 4-CN.sub.4 H-Ph OH, OH1699 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 3-(HOCH.sub.2)-Ph OH, OH1700 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 4-(HOCH.sub.2)-Ph OH, OH1701 OMe 1 PhCH.sub.2 CH.sub.2 H (+)-pin1702 OMe 1 PhCH.sub.2 CH.sub.2 Methyl (+)-pin1703 OMe 1 PhCH.sub.2 CH.sub.2 Ethyl (+)-pin1704 OMe 1 PhCH.sub.2 CH.sub.2 n-Propyl (+)-pin1705 OMe 1 PhCH.sub.2 CH.sub.2 n-Butyl (+)-pin1706 OMe 1 PhCH.sub.2 CH.sub.2 CH.sub.2 SCH.sub.3 (+)-pin1707 OMe 1 PhCH.sub.2 CH.sub.2 CH.sub.2 (SO)CH.sub.3 (+)-pin1708 OMe 1 PhCH.sub.2 CH.sub.2 CH.sub.2 (SO.sub.2)CH.sub.3 (+)-pin1709 OMe 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 SCH.sub.3 (+)-pin1710 OMe 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 (SO)CH.sub.3 (+)-pin1711 OMe 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3 (+)-pin1712 OMe 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CN (+)-pin CR1713 OMe 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 CN (+)-pin1714 OMe 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 CN (+)-pin1715 OMe 1 PhCH.sub.2 CH.sub.2 CF.sub.3 (+)-pin1716 OMe 1 PhCH.sub.2 CH.sub.2 CF.sub.2 CF.sub.3 (+)-pin1717 OMe 1 PhCH.sub.2 CH.sub.2 CF.sub.2 CF.sub.2 CF.sub.3 (+)-pin1718 OMe 1 PhCH.sub.2 CH.sub.2 CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3 (+)-pin1719 OMe 1 PhCH.sub.2 CH.sub.2 F.sub.5 -Ph (+)-pin1720 OMe 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CO.sub.2 H (+)-pin1721 OMe 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.2 CO.sub.2 H (+)-pin1722 OMe 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.3 CO.sub.2 H (+)-pin1723 OMe 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CN.sub.4 H (+)-pin1724 OMe 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.2 CN.sub.4 H (+)-pin1725 OMe 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.3 CN.sub.4 H (+)-pin1726 OMe 1 PhCH.sub.2 CH.sub.2 CH.sub.2 NO.sub.2 (+)-pin1727 OMe 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.2 NO.sub.2 (+)-pin1728 OMe 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.3 NO.sub.2 (+)-pin1729 OMe 1 PhCH.sub.2 CH.sub.2 CH.sub.2 OH (+)-pin1730 OMe 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.2 OH (+)-pin1731 OMe 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.3 OH (+)-pin1732 OMe 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CO.sub.2 Me (+)-pin1733 OMe 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.2 CO.sub.2 Me (+)-pin1734 OMe 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.3 CO.sub.2 Me (+)-pin1735 OMe 1 PhCH.sub.2 CH.sub.2 Ph (+)-pin1736 OMe 1 PhCH.sub.2 CH.sub.2 PhCH.sub.2 (+)-pin1737 OMe 1 PhCH.sub.2 CH.sub.2 Ph(CH.sub.2).sub.2 (+)-pin1738 OMe 1 PhCH.sub.2 CH.sub.2 3-NO.sub.2 -Ph (+)-pin1739 OMe 1 PhCH.sub.2 CH.sub.2 4-NO.sub.2 -Ph (+)-pin1740 OMe 1 PhCH.sub.2 CH.sub.2 3-CO.sub.2 H-Ph (+)-pin1741 OMe 1 PhCH.sub.2 CH.sub.2 4-CO.sub.2 H-Ph (+)-pin1742 OMe 1 PhCH.sub.2 CH.sub.2 3-CN.sub.4 H-Ph (+)-pin1743 OMe 1 PhCH.sub.2 CH.sub.2 4-CN.sub.4 H-Ph (+)-pin1744 OMe 1 PhCH.sub.2 CH.sub.2 3-(HOCH.sub.2)-Ph (+)-pin1745 OMe 1 PhCH.sub.2 CH.sub.2 4-(HOCH.sub.2)-Ph (+)-pin1746 OMe 1 PhCH.sub.2 CH.sub.2 H OH, OH1747 OMe 1 PhCH.sub.2 CH.sub.2 Methyl OH, OH1748 OMe 1 PhCH.sub.2 CH.sub.2 Ethyl OH, OH1749 OMe 1 PhCH.sub.2 CH.sub.2 n-Propyl OH, OH1750 OMe 1 PhCH.sub.2 CH.sub.2 n-Butyl OH, OH1751 OMe 1 PhCH.sub.2 CH.sub.2 CH.sub.2 SCH.sub.3 OH, OH1752 OMe 1 PhCH.sub.2 CH.sub.2 CH.sub.2 (SO)CH.sub.3 OH, OH1753 OMe 1 PhCH.sub.2 CH.sub.2 CH.sub.2 (SO.sub.2)CH.sub.3 OH, OH1754 OMe 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 SCH.sub.3 OH, OH1755 OMe 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 (SO)CH.sub.3 OH, OH1756 OMe 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3 OH, OH1757 OMe 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CN OH, OH1758 OMe 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 CN OH, OH1759 OMe 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 CN OH, OH1760 OMe 1 PhCH.sub.2 CH.sub.2 CF.sub.3 OH, OH1761 OMe 1 PhCH.sub.2 CH.sub.2 CF.sub.2 CF.sub.3 OH, OH1762 OMe 1 PhCH.sub.2 CH.sub.2 CF.sub.2 CF.sub.2 CF.sub.3 OH, OH1763 OMe 1 PhCH.sub.2 CH.sub.2 CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3 OH, OH1764 OMe 1 PhCH.sub.2 CH.sub.2 F.sub.5 -Ph OH, OH1765 OMe 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CO.sub.2 H OH, OH1766 OMe 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.2 CO.sub.2 H OH, OH1767 OMe 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.3 CO.sub.2 H OH, OH1768 OMe 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CN.sub.4 H OH, OH1769 OMe 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.2 CN.sub.4 H OH, OH1770 OMe 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.3 CN.sub.4 H OH, OH1771 OMe 1 PhCH.sub.2 CH.sub.2 CH.sub.2 NO.sub.2 OH, OH1772 OMe 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.2 NO.sub.2 OH, OH1773 OMe 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.3 NO.sub.2 OH, OH1774 OMe 1 PhCH.sub.2 CH.sub.2 CH.sub.2 OH OH, OH1775 OMe 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.2 OH OH, OH1776 OMe 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.3 OH OH, OH1777 OMe 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CO.sub.2 Me OH, OH1778 OMe 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.2 CO.sub.2 Me OH, OH1779 OMe 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.3 CO.sub.2 Me OH, OH1780 OMe 1 PhCH.sub.2 CH.sub.2 Ph OH, OH1781 OMe 1 PhCH.sub.2 CH.sub.2 PhCH.sub.2 OH, OH1782 OMe 1 PhCH.sub.2 CH.sub.2 Ph(CH.sub.2).sub.2 OH, OH1783 OMe 1 PhCH.sub.2 CH.sub.2 3-NO.sub.2 -Ph OH, OH1784 OMe 1 PhCH.sub.2 CH.sub.2 4-NO.sub.2 -Ph OH, OH1785 OMe 1 PhCH.sub.2 CH.sub.2 3-CO.sub.2 H-Ph OH, OH1786 OMe 1 PhCH.sub.2 CH.sub.2 4-CO.sub.2 H-Ph OH, OH1787 OMe 1 PhCH.sub.2 CH.sub.2 3-CN.sub.4 H-Ph OH, OH1788 OMe 1 PhCH.sub.2 CH.sub.2 4-CN.sub.4 H-Ph OH, OH1789 OMe 1 PhCH.sub.2 CH.sub.2 3-(HOCH.sub.2)-Ph OH, OH1790 OMe 1 PhCH.sub.2 CH.sub.2 4-(HOCH.sub.2)-Ph OH, OH1791 NH(CNH)H 1 Ph H (+)-pin1792 NH(CNH)H 1 Ph Methyl (+)-pin1793 NH(CNH)H 1 Ph Ethyl (+)-pin1794 NH(CNH)H 1 Ph n-Propyl (+)-pin1795 NH(CNH)H 1 Ph n-Butyl (+)-pin1796 NH(CNH)H 1 Ph CH.sub.2 SCH.sub.3 (+)-pin1797 NH(CNH)H 1 Ph CH.sub.2 (SO)CH.sub.3 (+)-pin1798 NH(CNH)H 1 Ph CH.sub.2 (SO.sub.2)CH.sub.3 (+)-pin1799 NH(CNH)H 1 Ph CH.sub.2 CH.sub.2 SCH.sub.3 (+)-pin1800 NH(CNH)H 1 Ph CH.sub.2 CH.sub.2 (SO)CH.sub.3 (+)-pin1801 NH(CNH)H 1 Ph CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3 (+)-pin1802 NH(CNH)H 1 Ph CH.sub.2 CN (+)-pin1803 NH(CNH)H 1 Ph CH.sub.2 CH.sub.2 CN (+)-pin1804 NH(CNH)H 1 Ph CH.sub.2 CH.sub.2 CH.sub.2 CN (+)-pin1805 NH(CNH)H 1 Ph CF.sub.3 (+)-pin1806 NH(CNH)H 1 Ph CF.sub.2 CF.sub.3 (+)-pin1807 NH(CNH)H 1 Ph CF.sub.2 CF.sub.2 CF.sub.3 (+)-pin1808 NH(CNH)H 1 Ph CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3 (+)-pin1809 NH(CNH)H 1 Ph F.sub.5 -Ph (+)-pin1810 NH(CNH)H 1 Ph CH.sub.2 CO.sub.2 H (+)-pin1811 NH(CNH)H 1 Ph (CH.sub.2).sub.2 CO.sub.2 H (+)-pin1812 NH(CNH)H 1 Ph (CH.sub.2).sub.3 CO.sub.2 H (+)-pin1813 NH(CNH)H 1 Ph CH.sub.2 CN.sub.4 H (+)-pin1814 NH(CNH)H 1 Ph (CH.sub.2).sub.2 CN.sub.4 H (+)-pin1815 NH(CNH)H 1 Ph (CH.sub.2).sub.3 CN.sub.4 H (+)-pin1816 NH(CNH)H 1 Ph CH.sub.2 NO.sub.2 (+)-pin1817 NH(CNH)H 1 Ph (CH.sub.2).sub.2 NO.sub.2 (+)-pin1818 NH(CNH)H 1 Ph (CH.sub.2).sub.3 NO.sub.2 (+)-pin1819 NH(CNH)H 1 Ph CH.sub.2 OH (+)-pin1820 NH(CNH)H 1 Ph (CH.sub.2).sub.2 OH (+)-pin1821 NH(CNH)H 1 Ph (CH.sub.2).sub.3 OH (+)-pin1822 NH(CNH)H 1 Ph CH.sub.2 CO.sub.2 Me (+)-pin1823 NH(CNH)H 1 Ph (CH.sub.2).sub.2 CO.sub.2 Me (+)-pin1824 NH(CNH)H 1 Ph (CH.sub.2).sub.3 CO.sub.2 Me (+)-pin1825 NH(CNH)H 1 Ph Ph (+)-pin1826 NH(CNH)H 1 Ph PhCH.sub.2 (+)-pin1827 NH(CNH)H 1 Ph Ph(CH.sub.2).sub.2 (+)-pin1828 NH(CNH)H 1 Ph 3-NO.sub.2 -Ph (+)-pin1829 NH(CNH)H 1 Ph 4-NO.sub.2 -Ph (+)-pin1830 NH(CNH)H 1 Ph 3-CO.sub.2 H-Ph (+)-pin1831 NH(CNH)H 1 Ph 4-CO.sub.2 H-Ph (+)-pin1832 NH(CNH)H 1 Ph 3-CN.sub.4 H-Ph (+)-pin1833 NH(CNH)H 1 Ph 4-CN.sub.4 H-Ph (+)-pin1834 NH(CNH)H 1 Ph 3-(HOCH.sub.2)-Ph (+)-pin1835 NH(CNH)H 1 Ph 4-(HOCH.sub.2)-Ph (+)-pin1836 NH(CNH)H 1 Ph H OH, OH1837 NH(CNH)H 1 Ph Methyl OH, OH1838 NH(CNH)H 1 Ph Ethyl OH, OH1839 NH(CNH)H 1 Ph n-Propyl OH, OH1840 NH(CNH)H 1 Ph n-Butyl OH, OH1841 NH(CNH)H 1 Ph CH.sub.2 SCH.sub.3 OH, OH1842 NH(CNH)H 1 Ph CH.sub.2 (SO)CH.sub.3 OH, OH1843 NH(CNH)H 1 Ph CH.sub.2 (SO.sub.2)CH.sub.3 OH, OH1844 NH(CNH)H 1 Ph CH.sub.2 CH.sub.2 SCH.sub.3 OH, OH1845 NH(CNH)H 1 Ph CH.sub.2 CH.sub.2 (SO)CH.sub.3 OH, OH1846 NH(CNH)H 1 Ph CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3 OH, OH1847 NH(CNH)H 1 Ph CH.sub.2 CN OH, OH1848 NH(CNH)H 1 Ph CH.sub.2 CH.sub.2 CN OH, OH1849 NH(CNH)H 1 Ph CH.sub.2 CH.sub.2 CH.sub.2 CN OH, OH1850 NH(CNH)H 1 Ph CF.sub.3 OH, OH1851 NH(CNH)H 1 Ph CF.sub.2 CF.sub.3 OH, OH1852 NH(CNH)H 1 Ph CF.sub.2 CF.sub.2 CF.sub.3 OH, OH1853 NH(CNH)H 1 Ph CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3 OH, OH1854 NH(CNH)H 1 Ph F.sub.5 -Ph OH, OH1855 NH(CNH)H 1 Ph CH.sub.2 CO.sub.2 H OH, OH1856 NH(CNH)H 1 Ph (CH.sub.2).sub.2 CO.sub.2 H OH, OH1857 NH(CNH)H 1 Ph (CH.sub.2).sub.3 CO.sub.2 H OH, OH1858 NH(CNH)H 1 Ph CH.sub.2 CN.sub.4 H OH, OH1859 NH(CNH)H 1 Ph (CH.sub.2).sub.2 CN.sub.4 H OH, OH1860 NH(CNH)H 1 Ph (CH.sub.2).sub.3 CN.sub.4 H OH, OH1861 NH(CNH)H 1 Ph CH.sub.2 NO.sub.2 OH, OH1862 NH(CNH)H 1 Ph (CH.sub.2).sub.2 NO.sub.2 OH, OH1863 NH(CNH)H 1 Ph (CH.sub.2).sub.3 NO.sub.2 OH, OH1864 NH(CNH)H 1 Ph CH.sub.2 OH OH, OH1865 NH(CNH)H 1 Ph (CH.sub.2).sub.2 OH OH, OH1866 NH(CNH)H 1 Ph (CH.sub.2).sub.3 OH OH, OH1867 NH(CNH)H 1 Ph CH.sub.2 CO.sub.2 Me OH, OH1868 NH(CNH)H 1 Ph (CH.sub.2).sub.2 CO.sub.2 Me OH, OH1869 NH(CNH)H 1 Ph (CH.sub.2).sub.3 CO.sub.2 Me OH, OH1870 NH(CNH)H 1 Ph Ph OH, OH1871 NH(CNH)H 1 Ph PhCH.sub.2 OH, OH1872 NH(CNH)H 1 Ph Ph(CH.sub.2).sub.2 OH, OH1873 NH(CNH)H 1 Ph 3-NO.sub.2 -Ph OH, OH1874 NH(CNH)H 1 Ph 4-NO.sub.2 -Ph OH, OH1875 NH(CNH)H 1 Ph 3-CO.sub.2 H-Ph OH, OH1876 NH(CNH)H 1 Ph 4-CO.sub.2 H-Ph OH, OH1877 NH(CNH)H 1 Ph 3-CN.sub.4 H-Ph OH, OH1878 NH(CNH)H 1 Ph 4-CN.sub.4 H-Ph OH, OH1879 NH(CNH)H 1 Ph 3-(HOCH.sub.2)-Ph OH, OH1880 NH(CNH)H 1 Ph 4-(HOCH.sub.2)-Ph OH, OH1881 NH(CNH)H 1 PhCH.sub.2 H (+)-pin1882 NH(CNH)H 1 PhCH.sub.2 Methyl (+)-pin1883 NH(CNH)H 1 PhCH.sub.2 Ethyl (+)-pin1884 NH(CNH)H 1 PhCH.sub.2 n-Propyl (+)-pin1885 NH(CNH)H 1 PhCH.sub.2 n-Butyl (+)-pin1886 NH(CNH)H 1 PhCH.sub.2 CH.sub.2 SCH.sub.3 (+)-pin1887 NH(CNH)H 1 PhCH.sub.2 CH.sub.2 (SO)CH.sub.3 (+)-pin1888 NH(CNH)H 1 PhCH.sub.2 CH.sub.2 (SO.sub.2)CH.sub.3 (+)-pin1889 NH(CNH)H 1 PhCH.sub.2 CH.sub.2 CH.sub.2 SCH.sub.3 (+)-pin1890 NH(CNH)H 1 PhCH.sub.2 CH.sub.2 CH.sub.2 (SO)CH.sub.3 (+)-pin1891 NH(CNH)H 1 PhCH.sub.2 CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3 (+)-pin1892 NH(CNH)H 1 PhCH.sub.2 CH.sub.2 CN (+)-pin1893 NH(CNH)H 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CN (+)-pin1894 NH(CNH)H 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 CN (+)-pin1895 NH(CNH)H 1 PhCH.sub.2 CF.sub.3 (+)-pin1896 NH(CNH)H 1 PhCH.sub.2 CF.sub.2 CF.sub.3 (+)-pin1897 NH(CNH)H 1 PhCH.sub.2 CF.sub.2 CF.sub.2 CF.sub.3 (+)-pin1898 NH(CNH)H 1 PhCH.sub.2 CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3 (+)-pin1899 NH(CNH)H 1 PhCH.sub.2 F.sub.5 -Ph (+)-pin1900 NH(CNH)H 1 PhCH.sub.2 CH.sub.2 CO.sub.2 H (+)-pin1901 NH(CNH)H 1 PhCH.sub.2 (CH.sub.2).sub.2 CO.sub.2 H (+)-pin1902 NH(CNH)H 1 PhCH.sub.2 (CH.sub.2).sub.3 CO.sub.2 H (+)-pin1903 NH(CNH)H 1 PhCH.sub.2 CH.sub.2 CN.sub.4 H (+)-pin1904 NH(CNH)H 1 PhCH.sub.2 (CH.sub.2).sub.2 CN.sub.4 H (+)-pin1905 NH(CNH)H 1 PhCH.sub.2 (CH.sub.2).sub.3 CN.sub.4 H (+)-pin1906 NH(CNH)H 1 PhCH.sub.2 CH.sub.2 NO.sub.2 (+)-pin1907 NH(CNH)H 1 PhCH.sub.2 (CH.sub.2).sub.2 NO.sub.2 (+)-pin1908 NH(CNH)H 1 PhCH.sub.2 (CH.sub.2).sub.3 NO.sub.2 (+)-pin1909 NH(CNH)H 1 PhCH.sub.2 CH.sub.2 OH (+)-pin1910 NH(CNH)H 1 PhCH.sub.2 (CH.sub.2).sub.2 OH (+)-pin1911 NH(CNH)H 1 PhCH.sub.2 (CH.sub.2).sub.3 OH (+)-pin1912 NH(CNH)H 1 PhCH.sub.2 CH.sub.2 CO.sub.2 Me (+)-pin1913 NH(CNH)H 1 PhCH.sub.2 (CH.sub.2).sub.2 CO.sub.2 Me (+)-pin1914 NH(CNH)H 1 PhCH.sub.2 (CH.sub.2).sub.3 CO.sub.2 Me (+)-pin1915 NH(CNH)H 1 PhCH.sub.2 Ph (+)-pin1916 NH(CNH)H 1 PhCH.sub.2 PhCH.sub.2 (+)-pin1917 NH(CNH)H 1 PhCH.sub.2 Ph(CH.sub.2).sub.2 (+)-pin1918 NH(CNH)H 1 PhCH.sub.2 3-NO.sub.2 -Ph (+)-pin1919 NH(CNH)H 1 PhCH.sub.2 4-NO.sub.2 -Ph (+)-pin1920 NH(CNH)H 1 PhCH.sub.2 3-CO.sub.2 H-Ph (+)-pin1921 NH(CNH)H 1 PhCH.sub.2 4-CO.sub.2 H-Ph (+)-pin1922 NH(CNH)H 1 PhCH.sub.2 3-CN.sub.4 H-Ph (+)-pin1923 NH(CNH)H 1 PhCH.sub.2 4-CN.sub.4 H-Ph (+)-pin1924 NH(CNH)H 1 PhCH.sub.2 3-(HOCH.sub.2)-Ph (+)-pin1925 NH(CNH)H 1 PhCH.sub.2 4-(HOCH.sub.2)-Ph (+)-pin1926 NH(CNH)H 1 PhCH.sub.2 H OH, OH1927 NH(CNH)H 1 PhCH.sub.2 Methyl OH, OH1928 NH(CNH)H 1 PhCH.sub.2 Ethyl OH, OH1929 NH(CNH)H 1 PhCH.sub.2 n-Propyl OH, OH1930 NH(CNH)H 1 PhCH.sub.2 n-Butyl OH, OH1931 NH(CNH)H 1 PhCH.sub.2 CH.sub.2 SCH.sub.3 OH, OH1932 NH(CNH)H 1 PhCH.sub.2 CH.sub.2 (SO)CH.sub.3 OH, OH1933 NH(CNH)H 1 PhCH.sub.2 CH.sub.2 (SO.sub.2)CH.sub.3 OH, OH1934 NH(CNH)H 1 PhCH.sub.2 CH.sub.2 CH.sub.2 SCH.sub.3 OH, OH1935 NH(CNH)H 1 PhCH.sub.2 CH.sub.2 CH.sub.2 (SO)CH.sub.3 OH, OH1936 NH(CNH)H 1 PhCH.sub.2 CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3 OH, OH1937 NH(CNH)H 1 PhCH.sub.2 CH.sub.2 CN OH, OH1938 NH(CNH)H 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CN OH, OH1939 NH(CNH)H 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 CN OH, OH1940 NH(CNH)H 1 PhCH.sub.2 CF.sub.3 OH, OH1941 NH(CNH)H 1 PhCH.sub.2 CF.sub.2 CF.sub.3 OH, OH1942 NH(CNH)H 1 PhCH.sub.2 CF.sub.2 CF.sub.2 CF.sub.3 OH, OH1943 NH(CNH)H 1 PhCH.sub.2 CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3 OH, OH1944 NH(CNH)H 1 PhCH.sub.2 F.sub.5 -Ph OH, OH1945 NH(CNH)H 1 PhCH.sub.2 CH.sub.2 CO.sub.2 H OH, OH1946 NH(CNH)H 1 PhCH.sub.2 (CH.sub.2).sub.2 CO.sub.2 H OH, OH1947 NH(CNH)H 1 PhCH.sub.2 (CH.sub.2).sub.3 CO.sub.2 H OH, OH1948 NH(CNH)H 1 PhCH.sub.2 CH.sub.2 CN.sub.4 H OH, OH1949 NH(CNH)H 1 PhCH.sub.2 (CH.sub.2).sub.2 CN.sub.4 H OH, OH1950 NH(CNH)H 1 PhCH.sub.2 (CH.sub.2).sub.3 CN.sub.4 H OH, OH1951 NH(CNH)H 1 PhCH.sub.2 CH.sub.2 NO.sub.2 OH, OH1952 NH(CNH)H 1 PhCH.sub.2 (CH.sub.2).sub.2 NO.sub.2 OH, OH1953 NH(CNH)H 1 PhCH.sub.2 (CH.sub.2).sub.3 NO.sub.2 OH, OH1954 NH(CNH)H 1 PhCH.sub.2 CH.sub.2 OH OH, OH1955 NH(CNH)H 1 PhCH.sub.2 (CH.sub.2).sub.2 OH OH, OH1956 NH(CNH)H 1 PhCH.sub.2 (CH.sub.2).sub.3 OH OH, OH1957 NH(CNH)H 1 PhCH.sub.2 CH.sub.2 CO.sub.2 Me OH, OH1958 NH(CNH)H 1 PhCH.sub.2 (CH.sub.2).sub.2 CO.sub.2 Me OH, OH1959 NH(CNH)H 1 PhCH.sub.2 (CH.sub.2).sub.3 CO.sub.2 Me OH, OH1960 NH(CNH)H 1 PhCH.sub.2 Ph OH, OH1961 NH(CNH)H 1 PhCH.sub.2 PhCH.sub.2 OH, OH1962 NH(CNH)H 1 PhCH.sub.2 Ph(CH.sub.2).sub.2 OH, OH1963 NH(CNH)H 1 PhCH.sub.2 3-NO.sub.2 -Ph OH, OH1964 NH(CNH)H 1 PhCH.sub.2 4-NO.sub.2 -Ph OH, OH1965 NH(CNH)H 1 PhCH.sub.2 3-CO.sub.2 H-Ph OH, OH1966 NH(CNH)H 1 PhCH.sub.2 4-CO.sub.2 H-Ph OH, OH1967 NH(CNH)H 1 PhCH.sub.2 3-CN.sub.4 H-Ph OH, OH1968 NH(CNH)H 1 PhCH.sub.2 4-CN.sub.4 H-Ph OH, OH1969 NH(CNH)H 1 PhCH.sub.2 3-(HOCH.sub.2)-Ph OH, OH1970 NH(CNH)H 1 PhCH.sub.2 4-(HOCH.sub.2)-Ph OH, OH1971 NH(CNH)H 1 PhCH.sub.2 CH.sub.2 H (+)-pin1972 NH(CNH)H 1 PhCH.sub.2 CH.sub.2 Methyl (+)-pin1973 NH(CNH)H 1 PhCH.sub.2 CH.sub.2 Ethyl (+)-pin1974 NH(CNH)H 1 PhCH.sub.2 CH.sub.2 n-Propyl (+)-pin1975 NH(CNH)H 1 PhCH.sub.2 CH.sub.2 n-Butyl (+)-pin1976 NH(CNH)H 1 PhCH.sub.2 CH.sub.2 CH.sub.2 SCH.sub.3 (+)-pin1977 NH(CNH)H 1 PhCH.sub.2 CH.sub.2 CH.sub.2 (SO)CH.sub.3 (+)-pin1978 NH(CNH)H 1 PhCH.sub.2 CH.sub.2 CH.sub.2 (SO.sub.2)CH.sub.3 (+)-pin1979 NH(CNH)H 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 SCH.sub.3 (+)-pin1980 NH(CNH)H 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 (SO)CH.sub.3 (+)-pin1981 NH(CNH)H 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3 (+)-pin1982 NH(CNH)H 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CN (+)-pin1983 NH(CNH)H 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 CN (+)-pin1984 NH(CNH)H 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 CN (+)-pin1985 NH(CNH)H 1 PhCH.sub.2 CH.sub.2 CF.sub.3 (+)-pin1986 NH(CNH)H 1 PhCH.sub.2 CH.sub.2 CF.sub.2 CF.sub.3 (+)-pin1987 NH(CNH)H 1 PhCH.sub.2 CH.sub.2 CF.sub.2 CF.sub.2 CF.sub.3 (+)-pin1988 NH(CNH)H 1 PhCH.sub.2 CH.sub.2 CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3 (+)-pin1989 NH(CNH)H 1 PhCH.sub.2 CH.sub.2 F.sub.5 -Ph (+)-pin1990 NH(CNH)H 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CO.sub.2 H (+)-pin1991 NH(CNH)H 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.2 CO.sub.2 H (+)-pin1992 NH(CNH)H 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.3 CO.sub.2 H (+)-pin1993 NH(CNH)H 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CN.sub.4 H (+)-pin1994 NH(CNH)H 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.2 CN.sub.4 H (+)-pin1995 NH(CNH)H 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.3 CN.sub.4 H (+)-pin1996 NH(CNH)H 1 PhCH.sub.2 CH.sub.2 CH.sub.2 NO.sub.2 (+)-pin1997 NH(CNH)H 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.2 NO.sub.2 (+)-pin1998 NH(CNH)H 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.3 NO.sub.2 (+)-pin1999 NH(CNH)H 1 PhCH.sub.2 CH.sub.2 CH.sub.2 OH (+)-pin2000 NH(CNH)H 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.2 OH (+)-pin2001 NH(CNH)H 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.3 OH (+)-pin2002 NH(CNH)H 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CO.sub.2 Me (+)-pin2003 NH(CNH)H 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.2 CO.sub.2 Me (+)-pin2004 NH(CNH)H 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.3 CO.sub.2 Me (+)-pin2005 NH(CNH)H 1 PhCH.sub.2 CH.sub.2 Ph (+)-pin2006 NH(CNH)H 1 PhCH.sub.2 CH.sub.2 PhCH.sub.2 (+)-pin2007 NH(CNH)H 1 PhCH.sub.2 CH.sub.2 Ph(CH.sub.2).sub.2 (+)-pin2008 NH(CNH)H 1 PhCH.sub.2 CH.sub.2 3-NO.sub.2 -Ph (+)-pin2009 NH(CNH)H 1 PhCH.sub.2 CH.sub.2 4-NO.sub.2 -Ph (+)-pin2010 NH(CNH)H 1 PhCH.sub.2 CH.sub.2 3-CO.sub.2 H-Ph (+)-pin2011 NH(CNH)H 1 PhCH.sub.2 CH.sub.2 4-CO.sub.2 H-Ph (+)-pin2012 NH(CNH)H 1 PhCH.sub.2 CH.sub.2 3-CN.sub.4 H-Ph (+)-pin2013 NH(CNH)H 1 PhCH.sub.2 CH.sub.2 4-CN.sub.4 H-Ph (+)-pin2014 NH(CNH)H 1 PhCH.sub.2 CH.sub.2 3-(HOCH.sub.2)-Ph (+)-pin2015 NH(CNH)H 1 PhCH.sub.2 CH.sub.2 4-(HOCH.sub.2)-Ph (+)-pin2016 NH(CNH)H 1 PhCH.sub.2 CH.sub.2 H OH, OH2017 NH(CNH)H 1 PhCH.sub.2 CH.sub.2 Methyl OH, OH2018 NH(CNH)H 1 PhCH.sub.2 CH.sub.2 Ethyl OH, OH2019 NH(CNH)H 1 PhCH.sub.2 CH.sub.2 n-Propyl OH, OH2020 NH(CNH)H 1 PhCH.sub.2 CH.sub.2 n-Butyl OH, OH2021 NH(CNH)H 1 PhCH.sub.2 CH.sub.2 CH.sub.2 SCH.sub.3 OH, OH2022 NH(CNH)H 1 PhCH.sub.2 CH.sub.2 CH.sub.2 (SO)CH.sub.3 OH, OH2023 NH(CNH)H 1 PhCH.sub.2 CH.sub.2 CH.sub.2 (SO.sub.2)CH.sub.3 OH, OH2024 NH(CNH)H 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 SCH.sub.3 OH, OH2025 NH(CNH)H 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 (SO)CH.sub.3 OH, OH2026 NH(CNH)H 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3 OH, OH2027 NH(CNH)H 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CN OH, OH2028 NH(CNH)H 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 CN OH, OH2029 NH(CNH)H 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 CN OH, OH2030 NH(CNH)H 1 PhCH.sub.2 CH.sub.2 CF.sub.3 OH, OH2031 NH(CNH)H 1 PhCH.sub.2 CH.sub.2 CF.sub.2 CF.sub.3 OH, OH2032 NH(CNH)H 1 PhCH.sub.2 CH.sub.2 CF.sub.2 CF.sub.2 CF.sub.3 OH, OH2033 NH(CNH)H 1 PhCH.sub.2 CH.sub.2 CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3 OH, OH2034 NH(CNH)H 1 PhCH.sub.2 CH.sub.2 F.sub.5 -Ph OH, OH2035 NH(CNH)H 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CO.sub.2 H OH, OH2036 NH(CNH)H 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.2 CO.sub.2 H OH, OH2037 NH(CNH)H 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.3 CO.sub.2 H OH, OH2038 NH(CNH)H 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CN.sub.4 H OH, OH2039 NH(CNH)H 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.2 CN.sub.4 H OH, OH2040 NH(CNH)H 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.3 CN.sub.4 H OH, OH2041 NH(CNH)H 1 PhCH.sub.2 CH.sub.2 CH.sub.2 NO.sub.2 OH, OH2042 NH(CNH)H 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.2 NO.sub.2 OH, OH2043 NH(CNH)H 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.3 NO.sub.2 OH, OH2044 NH(CNH)H 1 PhCH.sub.2 CH.sub.2 CH.sub.2 OH OH, OH2045 NH(CNH)H 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.2 OH OH, OH2046 NH(CNH)H 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.3 OH OH, OH2047 NH(CNH)H 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CO.sub.2 Me OH, OH2048 NH(CNH)H 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.2 CO.sub.2 Me OH, OH2049 NH(CNH)H 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.3 CO.sub.2 Me OH, OH2050 NH(CNH)H 1 PhCH.sub.2 CH.sub.2 Ph OH, OH2051 NH(CNH)H 1 PhCH.sub.2 CH.sub.2 PhCH.sub.2 OH, OH2052 NH(CNH)H 1 PhCH.sub.2 CH.sub.2 Ph(CH.sub.2).sub.2 OH, OH2053 NH(CNH)H 1 PhCH.sub.2 CH.sub.2 3-NO.sub.2 -Ph OH, OH2054 NH(CNH)H 1 PhCH.sub.2 CH.sub.2 4-NO.sub.2 -Ph OH, OH2055 NH(CNH)H 1 PhCH.sub.2 CH.sub.2 3-CO.sub.2 H-Ph OH, OH2056 NH(CNH)H 1 PhCH.sub.2 CH.sub.2 4-CO.sub.2 H-Ph OH, OH2057 NH(CNH)H 1 PhCH.sub.2 CH.sub.2 3-CN.sub.4 H-Ph OH, OH2058 NH(CNH)H 1 PhCH.sub.2 CH.sub.2 4-CN.sub.4 H-Ph OH, OH2059 NH(CNH)H 1 PhCH.sub.2 CH.sub.2 3-(HOCH.sub.2)-Ph OH, OH2060 NH(CNH)H 1 PhCH.sub.2 CH.sub.2 4-(HOCH.sub.2)-Ph OH, OH2061 CH.sub.2 NH.sub.2 1 PhCH.sub.2 3-NO.sub.2 Ph (+)-pin CU2062 NH(CNH)NH.sub.2 1 Ph PhCH.sub.2 (+)-pin2063 NH(CNH)NH.sub.2 1 Ph PhCH.sub.2 CH.sub.2 (+)-pin2064 S(CNH)NH.sub.2 1 Ph PhCH.sub.2 (+)-pin2065 S(CNH)NH.sub.2 1 Ph PhCH.sub.2 CH.sub.2 (+)-pin2066 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 CN (+)-pin CN2067 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 CN.sub.4 H (+)-pin CO2068 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 OCH.sub.2 Ph (+)-pin CT__________________________________________________________________________ AG. Anal. calcd. for C.sub.32 H.sub.42 BN.sub.5 O.sub.3.0.7H.sub.2 O.17HCl: 6, 61.00; H, 7.21; Cl, 9.56 N, 11.11. Found: C, 60.93; H, 7.20; Cl, 9.57 N, 11.55. AH. Anal. calcd. for C.sub.22 H.sub.28 BN.sub.5 O.sub.3.12H.sub.2 O.2.6HCl: C, 36.09; Cl., 12.59; N, 9.56. Found: C, 36.25; Cl, 12.52; N, 9.32. AI. Anal. calcd. for C.sub.16 H.sub.24 BN.sub.5 O.sub.3.1.5H.sub.2 O.1.8HCl: C, 43.89; H, 6.63; Cl, 14.57; N, 16.06. Found: C, 44.01; H, 6.28; Cl, 14.21; N, 15.59. AJ. Anal. calcd. for C.sub.25 H.sub.34 BN.sub.5 O.sub.3.2H.sub.2 O.1.6HCl C, 53.84; H, 7.16; Cl, 10.17; N, 12.56. Found: C, 53.71; H, 7.13; Cl, 10.25; N, 12.60. AK. MS (M+H).sup.+ : Calc. 480, Found 480. AL. MS (M+H).sup.+ : Calc. 494, Found 494. AM. MS (M+H).sup.+ : Calc. 522, Found 522. AN MS (M+H).sup.+ : Calc. 540, Found 540. AO. MS (M+H).sup.+ : Calc. 510, Found 510. AP. MS (M+H).sup.+ : Calc. 600, Found 600. AQ. MS (M+H).sup.+ : Calc. 556, Found 556. AR. MS (M+H).sup.+ : Calc. 570, Found 570. AS. MS (M+H).sup.+ : Calc. 601, Found 601. AT. MS (M+H).sup.+ : Calc. 598, FOund 598. AU. MS (M+H).sup.+ : Calc. 629, Found 629. AV. MS (M+H).sup.+ : Calc. 422, Found 422. AW. MS (M+H).sup.+ : Calc. 538, Found 538. AX. MS (M+H).sup.+ : Calc. 494, Found 494. AY. MS (M+H).sup.+ : Calc. 598, Found 598. AZ. MS (M+H).sup.+ : Calc. 360, Found 360. CN. MS (M+H).sup.+ : Calc. 519, Found 519. CO. MS (M+H).sup.+ : Calc. 562, Found 562. CP. MS (M+H).sup.+ : Calc. 552, Found 552. CQ. MS (M+H).sup.+ : Calc. 571, Found 571. CR. MS (M+H).sup.+ : Calc. 520, Found 520. CS. MS (M+H).sup.+ : Calc. 524, Found 524. CT. MS (M+H).sup.+ : Calc. 614, Found 614. CU. MS (M+H).sup.+ : Calc. 571, Found 571. TABLE 15__________________________________________________________________________ ##STR110## Phys.Ex X m R.sup.13 R.sup.14 Y.sup.1 Y.sup.2 Data__________________________________________________________________________2073 CH.sub.2 NH.sub.2 1 Ph H (+)-pin BW2074 CH.sub.2 NH.sub.2 1 Ph Methyl (+)-pin BX2075 CH.sub.2 NH.sub.2 1 Ph Ethyl (+)-pin2076 CH.sub.2 NH.sub.2 1 Ph n-Propyl (+)-pin2077 CH.sub.2 NH.sub.2 1 Ph n-Butyl (+)-pin2078 CH.sub.2 NH.sub.2 1 Ph CH.sub.2 SCH.sub.3 (+)-pin2079 CH.sub.2 NH.sub.2 1 Ph CH.sub.2 (SO)CH.sub.3 (+)-pin2080 CH.sub.2 NH.sub.2 1 Ph CH.sub.2 (SO.sub.2)CH.sub.3 (+)-pin2081 CH.sub.2 NH.sub.2 1 Ph CH.sub.2 CH.sub.2 SCH.sub.3 (+)-pin2082 CH.sub.2 NH.sub.2 1 Ph CH.sub.2 CH.sub.2 (SO)CH.sub.3 (+)-pin2083 CH.sub.2 NH.sub.2 1 Ph CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3 (+)-pin2084 CH.sub.2 NH.sub.2 1 Ph CH.sub.2 CN (+)-pin2085 CH.sub.2 NH.sub.2 1 Ph CH.sub.2 CH.sub.2 CN (+)-pin2086 CH.sub.2 NH.sub.2 1 Ph CH.sub.2 CH.sub.2 CH.sub.2 CN (+)-pin2087 CH.sub.2 NH.sub.2 1 Ph CF.sub.3 (+)-pin2088 CH.sub.2 NH.sub.2 1 Ph CF.sub.2 CF.sub.3 (+)-pin2089 CH.sub.2 NH.sub.2 1 Ph CF.sub.2 CF.sub.2 CF.sub.3 (+)-pin2090 CH.sub.2 NH.sub.2 1 Ph CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3 (+)-pin2091 CH.sub.2 NH.sub.2 1 Ph F.sub.5 -Ph (+)-pin2092 CH.sub.2 NH.sub.2 1 Ph CH.sub.2 CO.sub.2 H (+)-pin2093 CH.sub.2 NH.sub.2 1 Ph (CH.sub.2).sub.2 CO.sub.2 H (+)-pin2094 CH.sub.2 NH.sub.2 1 Ph (CH.sub.2).sub.3 CO.sub.2 H (+)-pin2095 CH.sub.2 NH.sub.2 1 Ph CH.sub.2 CN.sub.4 H (+)-pin2096 CH.sub.2 NH.sub.2 1 Ph (CH.sub.2).sub.2 CN.sub.4 H (+)-pin2097 CH.sub.2 NH.sub.2 1 Ph (CH.sub.2).sub.3 CN.sub.4 H (+)-pin2098 CH.sub.2 NH.sub.2 1 Ph CH.sub.2 NO.sub.2 (+)-pin2099 CH.sub.2 NH.sub.2 1 Ph (CH.sub.2).sub.2 NO.sub.2 (+)-pin2100 CH.sub.2 NH.sub.2 1 Ph (CH.sub.2).sub.3 NO.sub.2 (+)-pin2101 CH.sub.2 NH.sub.2 1 Ph CH.sub.2 OH (+)-pin2102 CH.sub.2 NH.sub.2 1 Ph (CH.sub.2).sub.2 OH (+)-pin2103 CH.sub.2 NH.sub.2 1 Ph (CH.sub.2).sub.3 OH (+)-pin2104 CH.sub.2 NH.sub.2 1 Ph CH.sub.2 CO.sub.2 Me (+)-pin2105 CH.sub.2 NH.sub.2 1 Ph (CH.sub.2).sub.2 CO.sub.2 Me (+)-pin2106 CH.sub.2 NH.sub.2 1 Ph (CH.sub.2).sub.3 CO.sub.2 Me (+)-pin2107 CH.sub.2 NH.sub.2 1 Ph 3-NO.sub.2 -Ph (+)-pin2108 CH.sub.2 NH.sub.2 1 Ph 4-NO.sub.2 -Ph (+)-pin2109 CH.sub.2 NH.sub.2 1 Ph 3-CO.sub.2 H-Ph (+)-pin2110 CH.sub.2 NH.sub.2 1 Ph 4-CO.sub.2 H-Ph (+)-pin2111 CH.sub.2 NH.sub.2 1 Ph 3-CN.sub.4 H-Ph (+)-pin2112 CH.sub.2 NH.sub.2 1 Ph 4-CN.sub.4 H-Ph (+)-pin2113 CH.sub.2 NH.sub.2 1 Ph 3-(HOCH.sub.2)-Ph (+)-pin2114 CH.sub.2 NH.sub.2 1 Ph 4-(HOCH.sub.2)-Ph (+)-pin2115 NH(CNH)NH.sub.2 1 Ph H (+)-pin2116 NH(CNH)NH.sub.2 1 Ph Methyl (+)-pin2117 NH(CNH)NH.sub.2 1 Ph Ethyl (+)-pin2118 NH(CNH)NH.sub.2 1 Ph n-Propyl (+)-pin2119 NH(CNH)NH.sub.2 1 Ph n-Butyl (+)-pin2120 NH(CNH)NH.sub.2 1 Ph CH.sub.2 SCH.sub.3 (+)-pin2121 NH(CNH)NH.sub.2 1 Ph CH.sub.2 (SO)CH.sub.3 (+)-pin2122 NH(CNH)NH.sub.2 1 Ph CH.sub.2 (SO.sub.2)CH.sub.3 (+)-pin2123 NH(CNH)NH.sub.2 1 Ph CH.sub.2 CH.sub.2 SCH.sub.3 (+)-pin2124 NH(CNH)NH.sub.2 1 Ph CH.sub.2 CH.sub.2 (SO)CH.sub.3 (+)-pin2125 NH(CNH)NH.sub.2 1 Ph CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3 (+)-pin2126 NH(CNH)NH.sub.2 1 Ph CH.sub.2 CN (+)-pin2127 NH(CNH)NH.sub.2 1 Ph CH.sub.2 CH.sub.2 CN (+)-pin2128 NH(CNH)NH.sub.2 1 Ph CH.sub.2 CH.sub.2 CH.sub.2 CN (+)-pin2129 NH(CNH)NH.sub.2 1 Ph CF.sub.3 (+)-pin2130 NH(CNH)NH.sub.2 1 Ph CF.sub.2 CF.sub.3 (+)-pin2131 NH(CNH)NH.sub.2 1 Ph CF.sub.2 CF.sub.2 CF.sub.3 (+)-pin2132 NH(CNH)NH.sub.2 1 Ph CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3 (+)-pin2133 NH(CNH)NH.sub.2 1 Ph F.sub.5 -Ph (+)-pin2134 NH(CNH)NH.sub.2 1 Ph CH.sub.2 CO.sub.2 H (+)-pin2135 NH(CNH)NH.sub.2 1 Ph (CH.sub.2).sub.2 CO.sub.2 H (+)-pin2136 NH(CNH)NH.sub.2 1 Ph (CH.sub.2).sub.3 CO.sub.2 H (+)-pin2137 NH(CNH)NH.sub.2 1 Ph CH.sub.2 CN.sub.4 H (+)-pin2138 NH(CNH)NH.sub.2 1 Ph (CH.sub.2).sub.2 CN.sub.4 H (+)-pin2139 NH(CNH)NH.sub.2 1 Ph (CH.sub.2).sub.3 CN.sub.4 H (+)-pin2140 NH(CNH)NH.sub.2 1 Ph CH.sub.2 NO.sub.2 (+)-pin2141 NH(CNH)NH.sub.2 1 Ph (CH.sub.2).sub.2 NO.sub.2 (+)-pin2142 NH(CNH)NH.sub.2 1 Ph (CH.sub.2).sub.3 NO.sub.2 (+)-pin2143 NH(CNH)NH.sub.2 1 Ph CH.sub.2 OH (+)-pin2144 NH(CNH)NH.sub.2 1 Ph (CH.sub.2).sub.2 OH (+)-pin2145 NH(CNH)NH.sub.2 1 Ph (CH.sub.2).sub.3 OH (+)-pin2146 NH(CNH)NH.sub.2 1 Ph CH.sub.2 CO.sub.2 Me (+)-pin2147 NH(CNH)NH.sub.2 1 Ph (CH.sub.2).sub.2 CO.sub.2 Me (+)-pin2148 NH(CNH)NH.sub.2 1 Ph (CH.sub.2).sub.3 CO.sub.2 Me (+)-pin2149 NH(CNH)NH.sub.2 1 Ph 3-NO.sub.2 -Ph (+)-pin2150 NH(CNH)NH.sub.2 1 Ph 4-NO.sub.2 -Ph (+)-pin2151 NH(CNH)NH.sub.2 1 Ph 3-CO.sub.2 H-Ph (+)-pin2152 NH(CNH)NH.sub.2 1 Ph 4-CO.sub.2 H-Ph (+)-pin2153 NH(CNH)NH.sub.2 1 Ph 3-CN.sub.4 H-Ph (+)-pin2154 NH(CNH)NH.sub.2 1 Ph 4-CN.sub.4 H-Ph (+)-pin2155 NH(CNH)NH.sub.2 1 Ph 3-(HOCH.sub.2)-Ph (+)-pin2156 NH(CNH)NH.sub.2 1 Ph 4-(HOCH.sub.2)-Ph (+)-pin2157 CH.sub.2 NH.sub.2 1 Ph H OH, OH2158 CH.sub.2 NH.sub.2 1 Ph Methyl OH, OH2159 CH.sub.2 NH.sub.2 1 Ph Ethyl OH, OH2160 CH.sub.2 NH.sub.2 1 Ph n-Propyl OH, OH2161 CH.sub.2 NH.sub.2 1 Ph n-Butyl OH, OH2162 CH.sub.2 NH.sub.2 1 Ph CH.sub.2 SCH.sub.3 OH, OH2163 CH.sub.2 NH.sub.2 1 Ph CH.sub.2 (SO)CH.sub.3 OH, OH2164 CH.sub.2 NH.sub.2 1 Ph CH.sub.2 (SO.sub.2)CH.sub.3 OH, OH2165 CH.sub.2 NH.sub.2 1 Ph CH.sub.2 CH.sub.2 SCH.sub.3 OH, OH2166 CH.sub.2 NH.sub.2 1 Ph CH.sub.2 CH.sub.2 (SO)CH.sub.3 OH, OH2167 CH.sub.2 NH.sub.2 1 Ph CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3 OH, OH2168 CH.sub.2 NH.sub.2 1 Ph CH.sub.2 CN OH, OH2169 CH.sub.2 NH.sub.2 1 Ph CH.sub.2 CH.sub.2 CN OH, OH2170 CH.sub.2 NH.sub.2 1 Ph CH.sub.2 CH.sub.2 CH.sub.2 CN OH, OH2171 CH.sub.2 NH.sub.2 1 Ph CF.sub.3 OH, OH2172 CH.sub.2 NH.sub.2 1 Ph CF.sub.2 CF.sub.3 OH, OH2173 CH.sub.2 NH.sub.2 1 Ph CF.sub.2 CF.sub.2 CF.sub.3 OH, OH2174 CH.sub.2 NH.sub.2 1 Ph CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3 OH, OH2175 CH.sub.2 NH.sub.2 1 Ph F.sub.5 -Ph OH, OH2176 CH.sub.2 NH.sub.2 1 Ph CH.sub.2 CO.sub.2 H OH, OH2177 CH.sub.2 NH.sub.2 1 Ph (CH.sub.2).sub.2 CO.sub.2 H OH, OH2178 CH.sub.2 NH.sub.2 1 Ph (CH.sub.2).sub.3 CO.sub.2 H OH, OH2179 CH.sub.2 NH.sub.2 1 Ph CH.sub.2 CN.sub.4 H OH, OH2180 CH.sub.2 NH.sub.2 1 Ph (CH.sub.2).sub.2 CN.sub.4 H OH, OH2181 CH.sub.2 NH.sub.2 1 Ph (CH.sub.2).sub.3 CN.sub.4 H OH, OH2182 CH.sub.2 NH.sub.2 1 Ph CH.sub.2 NO.sub.2 OH, OH2183 CH.sub.2 NH.sub.2 1 Ph (CH.sub.2).sub.2 NO.sub.2 OH, OH2184 CH.sub.2 NH.sub.2 1 Ph (CH.sub.2).sub.3 NO.sub.2 OH, OH2185 CH.sub.2 NH.sub.2 1 Ph CH.sub.2 OH OH, OH2186 CH.sub.2 NH.sub.2 1 Ph (CH.sub.2).sub.2 OH OH, OH2187 CH.sub.2 NH.sub.2 1 Ph (CH.sub.2).sub.3 OH OH, OH2188 CH.sub.2 NH.sub.2 1 Ph CH.sub.2 CO.sub.2 Me OH, OH2189 CH.sub.2 NH.sub.2 1 Ph (CH.sub.2).sub.2 CO.sub.2 Me OH, OH2190 CH.sub.2 NH.sub.2 1 Ph (CH.sub.2).sub.3 CO.sub.2 Me OH, OH2191 CH.sub.2 NH.sub.2 1 Ph 3-NO.sub.2 -Ph OH, OH2192 CH.sub.2 NH.sub.2 1 Ph 4-NO.sub.2 -Ph OH, OH2193 CH.sub.2 NH.sub.2 1 Ph 3-CO.sub.2 H-Ph OH, OH2194 CH.sub.2 NH.sub.2 1 Ph 4-CO.sub.2 H-Ph OH, OH2195 CH.sub.2 NH.sub.2 1 Ph 3-CN.sub.4 H-Ph OH, OH2196 CH.sub.2 NH.sub.2 1 Ph 4-CN.sub.4 H-Ph OH, OH2197 CH.sub.2 NH.sub.2 1 Ph 3-(HOCH.sub.2)-Ph OH, OH2198 CH.sub.2 NH.sub.2 1 Ph 4-(HOCH.sub.2)-Ph OH, OH2199 NH(CNH)NH.sub.2 1 Ph H OH, OH2200 NH(CNH)NH.sub.2 1 Ph Methyl OH, OH2201 NH(CNH)NH.sub.2 1 Ph Ethyl OH, OH2202 NH(CNH)NH.sub.2 1 Ph n-Propyl OH, OH2203 NH(CNH)NH.sub.2 1 Ph n-Butyl OH, OH2204 NH(CNH)NH.sub.2 1 Ph CH.sub.2 SCH.sub.3 OH, OH2205 NH(CNH)NH.sub.2 1 Ph CH.sub.2 (SO)CH.sub.3 OH, OH2206 NH(CNH)NH.sub.2 1 Ph CH.sub.2 (SO.sub.2)CH.sub.3 OH, OH2207 NH(CNH)NH.sub.2 1 Ph CH.sub.2 CH.sub.2 SCH.sub.3 OH, OH2208 NH(CNH)NH.sub.2 1 Ph CH.sub.2 CH.sub.2 (SO)CH.sub.3 OH, OH2209 NH(CNH)NH.sub.2 1 Ph CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3 OH, OH2210 NH(CNH)NH.sub.2 1 Ph CH.sub.2 CN OH, OH2211 NH(CNH)NH.sub.2 1 Ph CH.sub.2 CH.sub.2 CN OH, OH2212 NH(CNH)NH.sub.2 1 Ph CH.sub.2 CH.sub.2 CH.sub.2 CN OH, OH2213 NH(CNH)NH.sub.2 1 Ph CF.sub.3 OH, OH2214 NH(CNH)NH.sub.2 1 Ph CF.sub.2 CF.sub.3 OH, OH2215 NH(CNH)NH.sub.2 1 Ph CF.sub.2 CF.sub.2 CF.sub.3 OH, OH2216 NH(CNH)NH.sub.2 1 Ph CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3 OH, OH2217 NH(CNH)NH.sub.2 1 Ph F.sub.5 -Ph OH, OH2218 NH(CNH)NH.sub.2 1 Ph CH.sub.2 CO.sub.2 H OH, OH2219 NH(CNH)NH.sub.2 1 Ph (CH.sub.2).sub.2 CO.sub.2 H OH, OH2220 NH(CNH)NH.sub.2 1 Ph (CH.sub.2).sub.3 CO.sub.2 H OH, OH2221 NH(CNH)NH.sub.2 1 Ph CH.sub.2 CN.sub.4 H OH, OH2222 NH(CNH)NH.sub.2 1 Ph (CH.sub.2).sub.2 CN.sub.4 H OH, OH2223 NH(CNH)NH.sub.2 1 Ph (CH.sub.2).sub.3 CN.sub.4 H OH, OH2224 NH(CNH)NH.sub.2 1 Ph CH.sub.2 NO.sub.2 OH, OH2225 NH(CNH)NH.sub.2 1 Ph (CH.sub.2).sub.2 NO.sub.2 OH, OH2226 NH(CNH)NH.sub.2 1 Ph (CH.sub.2).sub.3 NO.sub.2 OH, OH2227 NH(CNH)NH.sub.2 1 Ph CH.sub.2 OH OH, OH2228 NH(CNH)NH.sub.2 1 Ph (CH.sub.2).sub.2 OH OH, OH2229 NH(CNH)NH.sub.2 1 Ph (CH.sub.2).sub.3 OH OH, OH2230 NH(CNH)NH.sub.2 1 Ph CH.sub.2 CO.sub.2 Me OH, OH2231 NH(CNH)NH.sub.2 1 Ph (CH.sub.2).sub.2 CO.sub.2 Me OH, OH2232 NH(CNH)NH.sub.2 1 Ph (CH.sub.2).sub.3 CO.sub.2 Me OH, OH2233 NH(CNH)NH.sub.2 1 Ph 3-NO.sub.2 -Ph OH, OH2234 NH(CNH)NH.sub.2 1 Ph 4-NO.sub.2 -Ph OH, OH2235 NH(CNH)NH.sub.2 1 Ph 3-CO.sub.2 H-Ph OH, OH2236 NH(CNH)NH.sub.2 1 Ph 4-CO.sub.2 H-Ph OH, OH2237 NH(CNH)NH.sub.2 1 Ph 3-CN.sub.4 H-Ph OH, OH2238 NH(CNH)NH.sub.2 1 Ph 4-CN.sub.4 H-Ph OH, OH2239 NH(CNH)NH.sub.2 1 Ph 3-(HOCH.sub.2)-Ph OH, OH2240 NH(CNH)NH.sub.2 1 Ph 4-(HOCH.sub.2)-Ph OH, OH2241 S(CNH)NH.sub.2 1 Ph H (+)-pin2242 S(CNH)NH.sub.2 1 Ph Methyl (+)-pin2243 S(CNH)NH.sub.2 1 Ph Ethyl (+)-pin2244 S(CNH)NH.sub.2 1 Ph n-Propyl (+)-pin2245 S(CNH)NH.sub.2 1 Ph n-Butyl (+)-pin2246 S(CNH)NH.sub.2 1 Ph CH.sub.2 SCH.sub.3 (+)-pin2247 S(CNH)NH.sub.2 1 Ph CH.sub.2 (SO)CH.sub.3 (+)-pin2248 S(CNH)NH.sub.2 1 Ph CH.sub.2 (SO.sub.2)CH.sub.3 (+)-pin2249 S(CNH)NH.sub.2 1 Ph CH.sub.2 CH.sub.2 SCH.sub.3 (+)-pin2250 S(CNH)NH.sub.2 1 Ph CH.sub.2 CH.sub.2 (SO)CH.sub.3 (+)-pin2251 S(CNH)NH.sub.2 1 Ph CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3 (+)-pin2252 S(CNH)NH.sub.2 1 Ph CH.sub.2 CN (+)-pin2253 S(CNH)NH.sub.2 1 Ph CH.sub.2 CH.sub.2 CN (+)-pin2254 S(CNH)NH.sub.2 1 Ph CH.sub.2 CH.sub.2 CH.sub.2 CN (+)-pin2255 S(CNH)NH.sub.2 1 Ph CF.sub.3 (+)-pin2256 S(CNH)NH.sub.2 1 Ph CF.sub.2 CF.sub.3 (+)-pin2257 S(CNH)NH.sub.2 1 Ph CF.sub.2 CF.sub.2 CF.sub.3 (+)-pin2258 S(CNH)NH.sub.2 1 Ph CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3 (+)-pin2259 S(CNH)NH.sub.2 1 Ph F.sub.5 -Ph (+)-pin2260 S(CNH)NH.sub.2 1 Ph CH.sub.2 CO.sub.2 H (+)-pin2261 S(CNH)NH.sub.2 1 Ph (CH.sub.2).sub.2 CO.sub.2 H (+)-pin2262 S(CNH)NH.sub.2 1 Ph (CH.sub.2).sub.3 CO.sub.2 H (+)-pin2263 S(CNH)NH.sub.2 1 Ph CH.sub.2 CN.sub.4 H (+)-pin2264 S(CNH)NH.sub.2 1 Ph (CH.sub.2).sub.2 CN.sub.4 H (+)-pin2265 S(CNH)NH.sub.2 1 Ph (CH.sub.2).sub.3 CN.sub.4 H (+)-pin2266 S(CNH)NH.sub.2 1 Ph CH.sub.2 NO.sub.2 (+)-pin2267 S(CNH)NH.sub.2 1 Ph (CH.sub.2).sub.2 NO.sub.2 (+)-pin2268 S(CNH)NH.sub.2 1 Ph (CH.sub.2).sub.3 NO.sub.2 (+)-pin2269 S(CNH)NH.sub.2 1 Ph CH.sub.2 OH (+)-pin2270 S(CNH)NH.sub.2 1 Ph (CH.sub.2).sub.2 OH (+)-pin2271 S(CNH)NH.sub.2 1 Ph (CH.sub.2).sub.3 OH (+)-pin2272 S(CNH)NH.sub.2 1 Ph CH.sub.2 CO.sub.2 Me (+)-pin2273 S(CNH)NH.sub.2 1 Ph (CH.sub.2).sub.2 CO.sub.2 Me (+)-pin2274 S(CNH)NH.sub.2 1 Ph (CH.sub.2).sub.3 CO.sub.2 Me (+)-pin2275 S(CNH)NH.sub.2 1 Ph 3-NO.sub.2 -Ph (+)-pin2276 S(CNH)NH.sub.2 1 Ph 4-NO.sub.2 -Ph (+)-pin2277 S(CNH)NH.sub.2 1 Ph 3-CO.sub.2 H-Ph (+)-pin2278 S(CNH)NH.sub.2 1 Ph 4-CO.sub.2 H-Ph (+)-pin2279 S(CNH)NH.sub.2 1 Ph 3-CN.sub.4 H-Ph (+)-pin2280 S(CNH)NH.sub.2 1 Ph 4-CN.sub.4 H-Ph (+)-pin2281 S(CNH)NH.sub.2 1 Ph 3-(HOCH.sub.2)-Ph (+)-pin2282 S(CNH)NH.sub.2 1 Ph 4-(HOCH.sub.2)-Ph (+)-pin2283 S(CNH)NH.sub.2 1 Ph H OH, OH2284 S(CNH)NH.sub.2 1 Ph Methyl OH, OH2285 S(CNH)NH.sub.2 1 Ph Ethyl OH, OH2286 S(CNH)NH.sub.2 1 Ph n-Propyl OH, OH2287 S(CNH)NH.sub.2 1 Ph n-Butyl OH, OH2288 S(CNH)NH.sub.2 1 Ph CH.sub.2 SCH.sub.3 OH, OH2289 S(CNH)NH.sub.2 1 Ph CH.sub.2 (SO)CH.sub.3 OH, OH2290 S(CNH)NH.sub.2 1 Ph CH.sub.2 (SO.sub.2)CH.sub.3 OH, OH2291 S(CNH)NH.sub.2 1 Ph CH.sub.2 CH.sub.2 SCH.sub.3 OH, OH2292 S(CNH)NH.sub.2 1 Ph CH.sub.2 CH.sub.2 (SO)CH.sub.3 OH, OH2293 S(CNH)NH.sub.2 1 Ph CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3 OH, OH2294 S(CNH)NH.sub.2 1 Ph CH.sub.2 CN OH, OH2295 S(CNH)NH.sub.2 1 Ph CH.sub.2 CH.sub.2 CN OH, OH2296 S(CNH)NH.sub.2 1 Ph CH.sub.2 CH.sub.2 CH.sub.2 CN OH, OH2297 S(CNH)NH.sub.2 1 Ph CF.sub.3 OH, OH2298 S(CNH)NH.sub.2 1 Ph CF.sub.2 CF.sub.3 OH, OH2299 S(CNH)NH.sub.2 1 Ph CF.sub.2 CF.sub.2 CF.sub.3 OH, OH2300 S(CNH)NH.sub.2 1 Ph CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3 OH, OH2301 S(CNH)NH.sub.2 1 Ph F.sub.5 -Ph OH, OH2302 S(CNH)NH.sub.2 1 Ph CH.sub.2 CO.sub.2 H OH, OH2303 S(CNH)NH.sub.2 1 Ph (CH.sub.2).sub.2 CO.sub.2 H OH, OH2304 S(CNH)NH.sub.2 1 Ph (CH.sub.2).sub.3 CO.sub.2 H OH, OH2305 S(CNH)NH.sub.2 1 Ph CH.sub.2 CN.sub.4 H OH, OH2306 S(CNH)NH.sub.2 1 Ph (CH.sub.2).sub.2 CN.sub.4 H OH, OH2307 S(CNH)NH.sub.2 1 Ph (CH.sub.2).sub.3 CN.sub.4 H OH, OH2308 S(CNH)NH.sub.2 1 Ph CH.sub.2 NO.sub.2 OH, OH2309 S(CNH)NH.sub.2 1 Ph (CH.sub.2).sub.2 NO.sub.2 OH, OH2310 S(CNH)NH.sub.2 1 Ph (CH.sub.2).sub.3 NO.sub.2 OH, OH2311 S(CNH)NH.sub.2 1 Ph CH.sub.2 OH OH, OH2312 S(CNH)NH.sub.2 1 Ph (CH.sub.2).sub.2 OH OH, OH2313 S(CNH)NH.sub.2 1 Ph (CH.sub.2).sub.3 OH OH, OH2314 S(CNH)NH.sub.2 1 Ph CH.sub.2 CO.sub.2 Me OH, OH2315 S(CNH)NH.sub.2 1 Ph (CH.sub.2).sub.2 CO.sub.2 Me OH, OH2316 S(CNH)NH.sub.2 1 Ph (CH.sub.2).sub.3 CO.sub.2 Me OH, OH2317 S(CNH)NH.sub.2 1 Ph 3-NO.sub.2 -Ph OH, OH2318 S(CNH)NH.sub.2 1 Ph 4-NO.sub.2 -Ph OH, OH2319 S(CNH)NH.sub.2 1 Ph 3-CO.sub.2 H-Ph OH, OH2320 S(CNH)NH.sub.2 1 Ph 4-CO.sub.2 H-Ph OH, OH2321 S(CNH)NH.sub.2 1 Ph 3-CN.sub.4 H-Ph OH, OH2322 S(CNH)NH.sub.2 1 Ph 4-CN.sub.4 H-Ph OH, OH2323 S(CNH)NH.sub.2 1 Ph 3-(HOCH.sub.2)-Ph OH, OH2324 S(CNH)NH.sub.2 1 Ph 4-(HOCH.sub.2)-Ph OH, OH2325 CH.sub.2 NH.sub.2 2 Ph H (+)-pin2326 CH.sub.2 NH.sub.2 2 Ph H OH, OH2327 OMe 1 Ph H (+)-pin2328 OMe 1 Ph Methyl (+)-pin2329 OMe 1 Ph Ethyl (+)-pin2330 OMe 1 Ph n-Propyl (+)-pin2331 OMe 1 Ph n-Butyl (+)-pin2332 OMe 1 Ph CH.sub.2 SCH.sub.3 (+)-pin2333 OMe 1 Ph CH.sub.2 (SO)CH.sub.3 (+)-pin2334 OMe 1 Ph CH.sub.2 (SO.sub.2)CH.sub.3 (+)-pin2335 OMe 1 Ph CH.sub.2 CH.sub.2 SCH.sub.3 (+)-pin2336 OMe 1 Ph CH.sub.2 CH.sub.2 (SO)CH.sub.3 (+)-pin2337 OMe 1 Ph CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3 (+)-pin2338 OMe 1 Ph CH.sub.2 CN (+)-pin2339 OMe 1 Ph CH.sub.2 CH.sub.2 CN (+)-pin2340 OMe 1 Ph CH.sub.2 CH.sub.2 CH.sub.2 CN (+)-pin2341 OMe 1 Ph CF.sub.3 (+)-pin2342 OMe 1 Ph CF.sub.2 CF.sub.3 (+)-pin2343 OMe 1 Ph CF.sub.2 CF.sub.2 CF.sub.3 (+)-pin2344 OMe 1 Ph CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3 (+)-pin2345 OMe 1 Ph F.sub.5 -Ph (+)-pin2346 OMe 1 Ph CH.sub.2 CO.sub.2 H (+)-pin2347 OMe 1 Ph (CH.sub.2).sub.2 CO.sub.2 H (+)-pin2348 OMe 1 Ph (CH.sub.2).sub.3 CO.sub.2 H (+)-pin2349 OMe 1 Ph CH.sub.2 CN.sub.4 H (+)-pin2350 OMe 1 Ph (CH.sub.2).sub.2 CN.sub.4 H (+)-pin2351 OMe 1 Ph (CH.sub.2).sub.3 CN.sub.4 H (+)-pin2352 OMe 1 Ph CH.sub.2 NO.sub.2 (+)-pin2353 OMe 1 Ph (CH.sub.2).sub.2 NO.sub.2 (+)-pin2354 OMe 1 Ph (CH.sub.2).sub.3 NO.sub.2 (+)-pin2355 OMe 1 Ph CH.sub.2 OH (+)-pin2356 OMe 1 Ph (CH.sub.2).sub.2 OH (+)-pin2357 OMe 1 Ph (CH.sub.2).sub.3 OH (+)-pin2358 OMe 1 Ph CH.sub.2 CO.sub.2 Me (+)-pin2359 OMe 1 Ph (CH.sub.2).sub.2 CO.sub.2 Me (+)-pin2360 OMe 1 Ph (CH.sub.2).sub.3 CO.sub.2 Me (+)-pin2361 OMe 1 Ph 3-NO.sub.2 -Ph (+)-pin2362 OMe 1 Ph 4-NO.sub.2 -Ph (+)-pin2363 OMe 1 Ph 3-CO.sub.2 H-Ph (+)-pin2364 OMe 1 Ph 4-CO.sub.2 H-Ph (+)-pin2365 OMe 1 Ph 3-CN.sub.4 H-Ph (+)-pin2366 OMe 1 Ph 4-CN.sub.4 H-Ph (+)-pin2367 OMe 1 Ph 3-(HOCH.sub.2)-Ph (+)-pin2368 OMe 1 Ph 4-(HOCH.sub.2)-Ph (+)-pin2369 OMe 1 Ph H OH, OH2370 OMe 1 Ph Methyl OH, OH2371 OMe 1 Ph Ethyl OH, OH2372 OMe 1 Ph n-Propyl OH, OH2373 OMe 1 Ph n-Butyl OH, OH2374 OMe 1 Ph CH.sub.2 SCH.sub.3 OH, OH2375 OMe 1 Ph CH.sub.2 (SO)CH.sub.3 OH, OH2376 OMe 1 Ph CH.sub.2 (SO.sub.2)CH.sub.3 OH, OH2377 OMe 1 Ph CH.sub.2 CH.sub.2 SCH.sub.3 OH, OH2378 OMe 1 Ph CH.sub.2 CH.sub.2 (SO)CH.sub.3 OH, OH2379 OMe 1 Ph CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3 OH, OH2380 OMe 1 Ph CH.sub.2 CN OH, OH2381 OMe 1 Ph CH.sub.2 CH.sub.2 CN OH, OH2382 OMe 1 Ph CH.sub.2 CH.sub.2 CH.sub.2 CN OH, OH2383 OMe 1 Ph CF.sub.3 OH, OH2384 OMe 1 Ph CF.sub.2 CF.sub.3 OH, OH2385 OMe 1 Ph CF.sub.2 CF.sub.2 CF.sub.3 OH, OH2386 OMe 1 Ph CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3 OH, OH2387 OMe 1 Ph F.sub.5 -Ph OH, OH2388 OMe 1 Ph CH.sub.2 CO.sub.2 H OH, OH2389 OMe 1 Ph (CH.sub.2).sub.2 CO.sub.2 H OH, OH2390 OMe 1 Ph (CH.sub.2).sub.3 CO.sub.2 H OH, OH2391 OMe 1 Ph CH.sub.2 CN.sub.4 H OH, OH2392 OMe 1 Ph (CH.sub.2).sub.2 CN.sub.4 H OH, OH2393 OMe 1 Ph (CH.sub.2).sub.3 CN.sub.4 H OH, OH2394 OMe 1 Ph CH.sub.2 NO.sub.2 OH, OH2395 OMe 1 Ph (CH.sub.2).sub.2 NO.sub.2 OH, OH2396 OMe 1 Ph (CH.sub.2).sub.3 NO.sub.2 OH, OH2397 OMe 1 Ph CH.sub.2 OH OH, OH2398 OMe 1 Ph (CH.sub.2).sub.2 OH OH, OH2399 OMe 1 Ph (CH.sub.2).sub.3 OH OH, OH2400 OMe 1 Ph CH.sub.2 CO.sub.2 Me OH, OH2401 OMe 1 Ph (CH.sub.2).sub.2 CO.sub.2 Me OH, OH2402 OMe 1 Ph (CH.sub.2).sub.3 CO.sub.2 Me OH, OH2403 OMe 1 Ph 3-NO.sub.2 -Ph OH, OH2404 OMe 1 Ph 4-NO.sub.2 -Ph OH, OH2405 OMe 1 Ph 3-CO.sub.2 H-Ph OH, OH2406 OMe 1 Ph 4-CO.sub.2 H-Ph OH, OH2407 OMe 1 Ph 3-CN.sub.4 H-Ph OH, OH2408 OMe 1 Ph 4-CN.sub.4 H-Ph OH, OH2409 OMe 1 Ph 3-(HOCH.sub.2)-Ph OH, OH2410 OMe 1 Ph 4-(HOCH.sub.2)-Ph OH, OH2411 CH.sub.2 NH.sub.2 1 PhCH.sub.2 H (+)-pin BA2412 CH.sub.2 NH.sub.2 1 PhCH.sub.2 Methyl (+)-pin BC2413 CH.sub.2 NH.sub.2 1 PhCH.sub.2 Ethyl (+)-pin2414 CH.sub.2 NH.sub.2 1 PhCH.sub.2 n-Propyl (+)-pin BD2415 CH.sub.2 NH.sub.2 1 PhCH.sub.2 n-Butyl (+)-pin2416 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 SCH.sub.3 (+)-pin BE2417 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 (SO)CH.sub.3 (+)-pin2418 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 (SO.sub.2)CH.sub.3 (+)-pin2419 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 SCH.sub.3 (+)-pin2420 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 (SO)CH.sub.3 (+)-pin2421 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3 (+)-pin2422 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 CN (+)-pin BF2423 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CN (+)-pin2424 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 CN (+)-pin2425 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CF.sub.3 (+)-pin2426 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CF.sub.2 CF.sub.3 (+)-pin2427 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CF.sub.2 CF.sub.2 CF.sub.3 (+)-pin2428 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3 (+)-pin2429 CH.sub.2 NH.sub.2 1 PhCH.sub.2 F.sub.5 -Ph (+)-pin2430 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 CO.sub.2 H (+)-pin BG2431 CH.sub.2 NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.2 CO.sub.2 H (+)-pin2432 CH.sub.2 NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.3 CO.sub.2 H (+)-pin2433 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 CN.sub.4 H (+)-pin2434 CH.sub.2 NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.2 CN.sub.4 H (+)-pin2435 CH.sub.2 NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.3 CN.sub.4 H (+)-pin2436 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 NO.sub.2 (+)-pin2437 CH.sub.2 NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.2 NO.sub.2 (+)-pin2438 CH.sub.2 NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.3 NO.sub.2 (+)-pin2439 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 OH (+)-pin CV2440 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 OCH.sub.2 Ph (+)-pin CW2441 CH.sub.2 NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.2 OH (+)-pin2442 CH.sub.2 NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.3 OH (+)-pin2443 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 CO.sub.2 Me (+)-pin2444 CH.sub.2 NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.2 CO.sub.2 Me (+)-pin CX2445 CH.sub.2 NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.3 CO.sub.2 Me (+)-pin2446 CH.sub.2 NH.sub.2 1 PhCH.sub.2 Ph (+)-pin2447 CH.sub.2 NH.sub.2 1 PhCH.sub.2 PhCH.sub.2 (+)-pin2448 CH.sub.2 NH.sub.2 1 PhCH.sub.2 3-NO.sub.2 -Ph (+)-pin2449 CH.sub.2 NH.sub.2 1 PhCH.sub.2 4-NO.sub.2 -Ph (+)-pin2450 CH.sub.2 NH.sub.2 1 PhCH.sub.2 3-CO.sub.2 H-Ph (+)-pin2451 CH.sub.2 NH.sub.2 1 PhCH.sub.2 4-CO.sub.2 H-Ph (+)-pin2452 CH.sub.2 NH.sub.2 1 PhCH.sub.2 3-CN.sub.4 H-Ph (+)-pin2453 CH.sub.2 NH.sub.2 1 PhCH.sub.2 4-CN.sub.4 H-Ph (+)-pin2454 CH.sub.2 NH.sub.2 1 PhCH.sub.2 3-(HOCH.sub.2)-Ph (+)-pin2455 CH.sub.2 NH.sub.2 1 PhCH.sub.2 4-(HOCH.sub.2)-Ph (+)-pin2456 NH(CNH)NH.sub.2 1 PhCH.sub.2 H (+)-pin2457 NH(CNH)NH.sub.2 1 PhCH.sub.2 Methyl (+)-pin2458 NH(CNH)NH.sub.2 1 PhCH.sub.2 Ethyl (+)-pin2459 NH(CNH)NH.sub.2 1 PhCH.sub.2 n-Propyl (+)-pin2460 NH(CNH)NH.sub.2 1 PhCH.sub.2 n-Butyl (+)-pin2461 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 SCH.sub.3 (+)-pin2462 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 (SO)CH.sub.3 (+)-pin2463 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 (SO.sub.2)CH.sub.3 (+)-pin2464 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 SCH.sub.3 (+)-pin2465 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 (SO)CH.sub.3 (+)-pin2466 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3 (+)-pin2467 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CN (+)-pin2468 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CN (+)-pin2469 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 CN (+)-pin2470 NH(CNH)NH.sub.2 1 PhCH.sub.2 CF.sub.3 (+)-pin2471 NH(CNH)NH.sub.2 1 PhCH.sub.2 CF.sub.2 CF.sub.3 (+)-pin2472 NH(CNH)NH.sub.2 1 PhCH.sub.2 CF.sub.2 CF.sub.2 CF.sub.3 (+)-pin2473 NH(CNH)NH.sub.2 1 PhCH.sub.2 CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3 (+)-pin2474 NH(CNH)NH.sub.2 1 PhCH.sub.2 F.sub.5 -Ph (+)-pin2475 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CO.sub.2 H (+)-pin2476 NH(CNH)NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.2 CO.sub.2 H (+)-pin2477 NH(CNH)NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.3 CO.sub.2 H (+)-pin2478 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CN.sub.4 H (+)-pin2479 NH(CNH)NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.2 CN.sub.4 H (+)-pin2480 NH(CNH)NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.3 CN.sub.4 H (+)-pin2481 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 NO.sub.2 (+)-pin2482 NH(CNH)NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.2 NO.sub.2 (+)-pin2483 NH(CNH)NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.3 NO.sub.2 (+)-pin2484 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 OH (+)-pin2485 NH(CNH)NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.2 OH (+)-pin2486 NH(CNH)NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.3 OH (+)-pin2487 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CO.sub.2 Me (+)-pin2488 NH(CNH)NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.2 CO.sub.2 Me (+)-pin2489 NH(CNH)NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.3 CO.sub.2 Me (+)-pin2490 NH(CNH)NH.sub.2 1 PhCH.sub.2 Ph (+)-pin2491 NH(CNH)NH.sub.2 1 PhCH.sub.2 3-NO.sub.2 -Ph (+)-pin CY2492 NH(CNH)NH.sub.2 1 PhCH.sub.2 4-NO.sub.2 -Ph (+)-pin2493 NH(CNH)NH.sub.2 1 PhCH.sub.2 3-CO.sub.2 H-Ph (+)-pin2494 NH(CNH)NH.sub.2 1 PhCH.sub.2 4-CO.sub.2 H-Ph (+)-pin2495 NH(CNH)NH.sub.2 1 PhCH.sub.2 3-CN.sub.4 H-Ph (+)-pin2496 NH(CNH)NH.sub.2 1 PhCH.sub.2 4-CN.sub.4 H-Ph (+)-pin2497 NH(CNH)NH.sub.2 1 PhCH.sub.2 3-(HOCH.sub.2)-Ph (+)-pin2498 NH(CNH)NH.sub.2 1 PhCH.sub.2 4-(HOCH.sub.2)-Ph (+)-pin2499 CH.sub.2 NH.sub.2 1 PhCH.sub.2 H OH, OH BH2500 CH.sub.2 NH.sub.2 1 PhCH.sub.2 Methyl OH, OH2501 CH.sub.2 NH.sub.2 1 PhCH.sub.2 Ethyl OH, OH2502 CH.sub.2 NH.sub.2 1 PhCH.sub.2 n-Propyl OH, OH2503 CH.sub.2 NH.sub.2 1 PhCH.sub.2 n-Butyl OH, OH2504 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 SCH.sub.3 OH, OH2505 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 (SO)CH.sub.3 OH, OH2506 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 (SO.sub.2)CH.sub.3 OH, OH2507 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 SCH.sub.3 OH, OH2508 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 (SO)CH.sub.3 OH, OH2509 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3 OH, OH2510 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 CN OH, OH2511 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CN OH, OH2512 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 CN OH, OH2513 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CF.sub.3 OH, OH2514 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CF.sub.2 CF.sub.3 OH, OH2515 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CF.sub.2 CF.sub.2 CF.sub.3 OH, OH2516 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3 OH, OH2517 CH.sub.2 NH.sub.2 1 PhCH.sub.2 F.sub.5 -Ph OH, OH2518 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 CO.sub.2 H OH, OH2519 CH.sub.2 NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.2 CO.sub.2 H OH, OH2520 CH.sub.2 NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.3 CO.sub.2 H OH, OH2521 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 CN.sub.4 H OH, OH2522 CH.sub.2 NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.2 CN.sub.4 H OH, OH2523 CH.sub.2 NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.3 CN.sub.4 H OH, OH2524 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 NO.sub.2 OH, OH2525 CH.sub.2 NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.2 NO.sub.2 OH, OH2526 CH.sub.2 NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.3 NO.sub.2 OH, OH2527 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 OH OH, OH2528 CH.sub.2 NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.2 OH OH, OH2529 CH.sub.2 NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.3 OH OH, OH2530 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 CO.sub.2 Me OH, OH2531 CH.sub.2 NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.2 CO.sub.2 Me OH, OH2532 CH.sub.2 NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.3 CO.sub.2 Me OH, OH2533 CH.sub.2 NH.sub.2 1 PhCH.sub.2 Ph OH, OH2534 CH.sub.2 NH.sub.2 1 PhCH.sub.2 3-NO.sub.2 -Ph OH, OH2535 CH.sub.2 NH.sub.2 1 PhCH.sub.2 4-NO.sub.2 -Ph OH, OH2536 CH.sub.2 NH.sub.2 1 PhCH.sub.2 3-CO.sub.2 H-Ph OH, OH2537 CH.sub.2 NH.sub.2 1 PhCH.sub.2 4-CO.sub.2 H-Ph OH, OH2538 CH.sub.2 NH.sub.2 1 PhCH.sub.2 3-CN.sub.4 H-Ph OH, OH2539 CH.sub.2 NH.sub.2 1 PhCH.sub.2 4-CN.sub.4 H-Ph OH, OH2540 CH.sub.2 NH.sub.2 1 PhCH.sub.2 3-(HOCH.sub.2)-Ph OH, OH2541 CH.sub.2 NH.sub.2 1 PhCH.sub.2 4-(HOCH.sub.2)-Ph OH, OH2542 NH(CNH)NH.sub.2 1 PhCH.sub.2 H OH, OH2543 NH(CNH)NH.sub.2 1 PhCH.sub.2 Methyl OH, OH2544 NH(CNH)NH.sub.2 1 PhCH.sub.2 Ethyl OH, OH2545 NH(CNH)NH.sub.2 1 PhCH.sub.2 n-Propyl OH, OH2546 NH(CNH)NH.sub.2 1 PhCH.sub.2 n-Butyl OH, OH2547 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 SCH.sub.3 OH, OH2548 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 (SO)CH.sub.3 OH, OH2549 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 (SO.sub.2)CH.sub.3 OH, OH2550 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 SCH.sub.3 OH, OH2551 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 (SO)CH.sub.3 OH, OH2552 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3 OH, OH2553 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CN OH, OH2554 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CN OH, OH2555 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 CN OH, OH2556 NH(CNH)NH.sub.2 1 PhCH.sub.2 CF.sub.3 OH, OH2557 NH(CNH)NH.sub.2 1 PhCH.sub.2 CF.sub.2 CF.sub.3 OH, OH2558 NH(CNH)NH.sub.2 1 PhCH.sub.2 CF.sub.2 CF.sub.2 CF.sub.3 OH, OH2559 NH(CNH)NH.sub.2 1 PhCH.sub.2 CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3 OH, OH2560 NH(CNH)NH.sub.2 1 PhCH.sub.2 F.sub.5 -Ph OH, OH2561 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CO.sub.2 H OH, OH2562 NH(CNH)NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.2 CO.sub.2 H OH, OH2563 NH(CNH)NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.3 CO.sub.2 H OH, OH2564 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CN.sub.4 H OH, OH2565 NH(CNH)NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.2 CN.sub.4 H OH, OH2566 NH(CNH)NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.3 CN.sub.4 H OH, OH2567 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 NO.sub.2 OH, OH2568 NH(CNH)NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.2 NO.sub.2 OH, OH2569 NH(CNH)NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.3 NO.sub.2 OH, OH2570 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 OH OH, OH2571 NH(CNH)NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.2 OH OH, OH2572 NH(CNH)NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.3 OH OH, OH2573 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CO.sub.2 Me OH, OH2574 NH(CNH)NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.2 CO.sub.2 Me OH, OH2575 NH(CNH)NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.3 CO.sub.2 Me OH, OH2576 NH(CNH)NH.sub.2 1 PhCH.sub.2 3-NO.sub.2 -Ph OH, OH2577 NH(CNH)NH.sub.2 1 PhCH.sub.2 4-NO.sub.2 -Ph OH, OH2578 NH(CNH)NH.sub.2 1 PhCH.sub.2 3-CO.sub.2 H-Ph OH, OH2579 NH(CNH)NH.sub.2 1 PhCH.sub.2 4-CO.sub.2 H-Ph OH, OH2580 NH(CNH)NH.sub.2 1 PhCH.sub.2 3-CN.sub.4 H-Ph OH, OH2581 NH(CNH)NH.sub.2 1 PhCH.sub.2 4-CN.sub.4 H-Ph OH, OH2582 NH(CNH)NH.sub.2 1 PhCH.sub.2 3-(HOCH.sub.2)-Ph OH, OH2583 NH(CNH)NH.sub.2 1 PhCH.sub.2 4-(HOCH.sub.2)-Ph OH, OH2584 S(CNH)NH.sub.2 1 PhCH.sub.2 H (+)-pin2585 S(CNH)NH.sub.2 1 PhCH.sub.2 Methyl (+)-pin2586 S(CNH)NH.sub.2 1 PhCH.sub.2 Ethyl (+)-pin2587 S(CNH)NH.sub.2 1 PhCH.sub.2 n-Propyl (+)-pin2588 S(CNH)NH.sub.2 1 PhCH.sub.2 n-Butyl (+)-pin2589 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 SCH.sub.3 (+)-pin2590 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 (SO)CH.sub.3 (+)-pin2591 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 (SO.sub.2)CH.sub.3 (+)-pin2592 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 SCH.sub.3 (+)-pin2593 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 (SO)CH.sub.3 (+)-pin2594 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3 (+)-pin2595 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CN (+)-pin2596 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CN (+)-pin2597 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 CN (+)-pin2598 S(CNH)NH.sub.2 1 PhCH.sub.2 CF.sub.3 (+)-pin2599 S(CNH)NH.sub.2 1 PhCH.sub.2 CF.sub.2 CF.sub.3 (+)-pin2600 S(CNH)NH.sub.2 1 PhCH.sub.2 CF.sub.2 CF.sub.2 CF.sub.3 (+)-pin2601 S(CNH)NH.sub.2 1 PhCH.sub.2 CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3 (+)-pin2602 S(CNH)NH.sub.2 1 PhCH.sub.2 F.sub.5 -Ph (+)-pin2603 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CO.sub.2 H (+)-pin2604 S(CNH)NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.2 CO.sub.2 H (+)-pin2605 S(CNH)NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.3 CO.sub.2 H (+)-pin2606 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CN.sub.4 H (+)-pin2607 S(CNH)NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.2 CN.sub.4 H (+)-pin2608 S(CNH)NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.3 CN.sub.4 H (+)-pin2609 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 NO.sub.2 (+)-pin2610 S(CNH)NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.2 NO.sub.2 (+)-pin2611 S(CNH)NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.3 NO.sub.2 (+)-pin2612 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 OH (+)-pin2613 S(CNH)NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.2 OH (+)-pin2614 S(CNH)NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.3 OH (+)-pin2615 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CO.sub.2 Me (+)-pin2616 S(CNH)NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.2 CO.sub.2 Me (+)-pin2617 S(CNH)NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.3 CO.sub.2 Me (+)-pin2618 S(CNH)NH.sub.2 1 PhCH.sub.2 3-NO.sub.2 -Ph (+)-pin2619 S(CNH)NH.sub.2 1 PhCH.sub.2 4-NO.sub.2 -Ph (+)-pin2620 S(CNH)NH.sub.2 1 PhCH.sub.2 3-CO.sub.2 H-Ph (+)-pin2621 S(CNH)NH.sub.2 1 PhCH.sub.2 4-CO.sub.2 H-Ph (+)-pin2622 S(CNH)NH.sub.2 1 PhCH.sub.2 3-CN.sub.4 H-Ph (+)-pin2623 S(CNH)NH.sub.2 1 PhCH.sub.2 4-CN.sub.4 H-Ph (+)-pin2624 S(CNH)NH.sub.2 1 PhCH.sub.2 3-(HOCH.sub.2)-Ph (+)-pin2625 S(CNH)NH.sub.2 1 PhCH.sub.2 4-(HOCH.sub.2)-Ph (+)-pin2626 S(CNH)NH.sub.2 1 PhCH.sub.2 H OH, OH2627 S(CNH)NH.sub.2 1 PhCH.sub.2 Methyl OH, OH2628 S(CNH)NH.sub.2 1 PhCH.sub.2 Ethyl OH, OH2629 S(CNH)NH.sub.2 1 PhCH.sub.2 n-Propyl OH, OH2630 S(CNH)NH.sub.2 1 PhCH.sub.2 n-Butyl OH, OH2631 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 SCH.sub.3 OH, OH2632 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 (SO)CH.sub.3 OH, OH2633 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 (SO.sub.2)CH.sub.3 OH, OH2634 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 SCH.sub.3 OH, OH2635 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 (SO)CH.sub.3 OH, OH2636 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3 OH, OH2637 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CN OH, OH2638 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CN OH, OH2639 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 CN OH, OH2640 S(CNH)NH.sub.2 1 PhCH.sub.2 CF.sub.3 OH, OH2641 S(CNH)NH.sub.2 1 PhCH.sub.2 CF.sub.2 CF.sub.3 OH, OH2642 S(CNH)NH.sub.2 1 PhCH.sub.2 CF.sub.2 CF.sub.2 CF.sub.3 OH, OH2643 S(CNH)NH.sub.2 1 PhCH.sub.2 CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3 OH, OH2644 S(CNH)NH.sub.2 1 PhCH.sub.2 F.sub.5 -Ph OH, OH2645 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CO.sub.2 H OH, OH2646 S(CNH)NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.2 CO.sub.2 H OH, OH2647 S(CNH)NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.3 CO.sub.2 H OH, OH2648 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CN.sub.4 H OH, OH2649 S(CNH)NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.2 CN.sub.4 H OH, OH2650 S(CNH)NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.3 CN.sub.4 H OH, OH2651 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 NO.sub.2 OH, OH2652 S(CNH)NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.2 NO.sub.2 OH, OH2653 S(CNH)NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.3 NO.sub.2 OH, OH2654 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 OH OH, OH2655 S(CNH)NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.2 OH OH, OH2656 S(CNH)NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.3 OH OH, OH2657 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CO.sub.2 Me OH, OH2658 S(CNH)NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.2 CO.sub.2 Me OH, OH2659 S(CNH)NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.3 CO.sub.2 Me OH, OH2660 S(CNH)NH.sub.2 1 PhCH.sub.2 3-NO.sub.2 -Ph OH, OH2661 S(CNH)NH.sub.2 1 PhCH.sub.2 4-NO.sub.2 -Ph OH, OH2662 S(CNH)NH.sub.2 1 PhCH.sub.2 3-CO.sub.2 H-Ph OH, OH2663 S(CNH)NH.sub.2 1 PhCH.sub.2 4-CO.sub.2 H-Ph OH, OH2664 S(CNH)NH.sub.2 1 PhCH.sub.2 3-CN.sub.4 H-Ph OH, OH2665 S(CNH)NH.sub.2 1 PhCH.sub.2 4-CN.sub.4 H-Ph OH, OH2666 S(CNH)NH.sub.2 1 PhCH.sub.2 3-(HOCH.sub.2)-Ph OH, OH2667 S(CNH)NH.sub.2 1 PhCH.sub.2 4-(HOCH.sub.2)-Ph OH, OH2668 OMe 1 PhCH.sub.2 H (+)-pin2669 OMe 1 PhCH.sub.2 Methyl (+)-pin2670 OMe 1 PhCH.sub.2 Ethyl (+)-pin2671 OMe 1 PhCH.sub.2 n-Propyl (+)-pin2672 OMe 1 PhCH.sub.2 n-Butyl (+)-pin2673 OMe 1 PhCH.sub.2 CH.sub.2 SCH.sub.3 (+)-pin2674 OMe 1 PhCH.sub.2 CH.sub.2 (SO)CH.sub.3 (+)-pin2675 OMe 1 PhCH.sub.2 CH.sub.2 (SO.sub.2)CH.sub.3 (+)-pin2676 OMe 1 PhCH.sub.2 CH.sub.2 CH.sub.2 SCH.sub.3 (+)-pin2677 OMe 1 PhCH.sub.2 CH.sub.2 CH.sub.2 (SO)CH.sub.3 (+)-pin2678 OMe 1 PhCH.sub.2 CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3 (+)-pin2679 OMe 1 PhCH.sub.2 CH.sub.2 CN (+)-pin2680 OMe 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CN (+)-pin2681 OMe 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 CN (+)-pin2682 OMe 1 PhCH.sub.2 CF.sub.3 (+)-pin2683 OMe 1 PhCH.sub.2 CF.sub.2 CF.sub.3 (+)-pin2684 OMe 1 PhCH.sub.2 CF.sub.2 CF.sub.2 CF.sub.3 (+)-pin2685 OMe 1 PhCH.sub.2 CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3 (+)-pin2686 OMe 1 PhCH.sub.2 F.sub.5 -Ph (+)-pin2687 OMe 1 PhCH.sub.2 CH.sub.2 CO.sub.2 H (+)-pin2688 OMe 1 PhCH.sub.2 (CH.sub.2).sub.2 CO.sub.2 H (+)-pin2689 OMe 1 PhCH.sub.2 (CH.sub.2).sub.3 CO.sub.2 H (+)-pin2690 OMe 1 PhCH.sub.2 CH.sub.2 CN.sub.4 H (+)-pin2691 OMe 1 PhCH.sub.2 (CH.sub.2).sub.2 CN.sub.4 H (+)-pin2692 OMe 1 PhCH.sub.2 (CH.sub.2).sub.3 CN.sub.4 H (+)-pin2693 OMe 1 PhCH.sub.2 CH.sub.2 NO.sub.2 (+)-pin2694 OMe 1 PhCH.sub.2 (CH.sub.2).sub.2 NO.sub.2 (+)-pin2695 OMe 1 PhCH.sub.2 (CH.sub.2).sub.3 NO.sub.2 (+)-pin2696 OMe 1 PhCH.sub.2 CH.sub.2 OH (+)-pin2697 OMe 1 PhCH.sub.2 (CH.sub.2).sub.2 OH (+)-pin2698 OMe 1 PhCH.sub.2 (CH.sub.2).sub.3 OH (+)-pin2699 OMe 1 PhCH.sub.2 CH.sub.2 CO.sub.2 Me (+)-pin2700 OMe 1 PhCH.sub.2 (CH.sub.2).sub.2 CO.sub.2 Me (+)-pin2701 OMe 1 PhCH.sub.2 (CH.sub.2).sub.3 CO.sub.2 Me (+)-pin2702 OMe 1 PhCH.sub.2 3-NO.sub.2 -Ph (+)-pin2703 OMe 1 PhCH.sub.2 4-NO.sub.2 -Ph (+)-pin2704 OMe 1 PhCH.sub.2 3-CO.sub.2 H-Ph (+)-pin2705 OMe 1 PhCH.sub.2 4-CO.sub.2 H-Ph (+)-pin2706 OMe 1 PhCH.sub.2 3-CN.sub.4 H-Ph (+)-pin2707 OMe 1 PhCH.sub.2 4-CN.sub.4 H-Ph (+)-pin2708 OMe 1 PhCH.sub.2 3-(HOCH.sub.2)-Ph (+)-pin2709 OMe 1 PhCH.sub.2 4-(HOCH.sub.2)-Ph (+)-pin2710 OMe 1 PhCH.sub.2 H OH, OH2711 OMe 1 PhCH.sub.2 Methyl OH, OH2712 OMe 1 PhCH.sub.2 Ethyl OH, OH2713 OMe 1 PhCH.sub.2 n-Propyl OH, OH2714 OMe 1 PhCH.sub.2 n-Butyl OH, OH2715 OMe 1 PhCH.sub.2 CH.sub.2 SCH.sub.3 OH, OH2716 OMe 1 PhCH.sub.2 CH.sub.2 (SO)CH.sub.3 OH, OH2717 OMe 1 PhCH.sub.2 CH.sub.2 (SO.sub.2)CH.sub.3 OH, OH2718 OMe 1 PhCH.sub.2 CH.sub.2 CH.sub.2 SCH.sub.3 OH, OH2719 OMe 1 PhCH.sub.2 CH.sub.2 CH.sub.2 (SO)CH.sub.3 OH, OH2720 OMe 1 PhCH.sub.2 CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3 OH, OH2721 OMe 1 PhCH.sub.2 CH.sub.2 CN OH, OH2722 OMe 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CN OH, OH2723 OMe 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 CN OH, OH2724 OMe 1 PhCH.sub.2 CF.sub.3 OH, OH2725 OMe 1 PhCH.sub.2 CF.sub.2 CF.sub.3 OH, OH2726 OMe 1 PhCH.sub.2 CF.sub.2 CF.sub.2 CF.sub.3 OH, OH2727 OMe 1 PhCH.sub.2 CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3 OH, OH2728 OMe 1 PhCH.sub.2 F.sub.5 -Ph OH, OH2729 OMe 1 PhCH.sub.2 CH.sub.2 CO.sub.2 H OH, OH2730 OMe 1 PhCH.sub.2 (CH.sub.2).sub.2 CO.sub.2 H OH, OH2731 OMe 1 PhCH.sub.2 (CH.sub.2).sub.3 CO.sub.2 H OH, OH2732 OMe 1 PhCH.sub.2 CH.sub.2 CN.sub.4 H OH, OH2733 OMe 1 PhCH.sub.2 (CH.sub.2).sub.2 CN.sub.4 H OH, OH2734 OMe 1 PhCH.sub.2 (CH.sub.2).sub.3 CN.sub.4 H OH, OH2735 OMe 1 PhCH.sub.2 CH.sub.2 NO.sub.2 OH, OH2736 OMe 1 PhCH.sub.2 (CH.sub.2).sub.2 NO.sub.2 OH, OH2737 OMe 1 PhCH.sub.2 (CH.sub.2).sub.3 NO.sub.2 OH, OH2738 OMe 1 PhCH.sub.2 CH.sub.2 OH OH, OH2739 OMe 1 PhCH.sub.2 (CH.sub.2).sub.2 OH OH, OH2740 OMe 1 PhCH.sub.2 (CH.sub.2).sub.3 OH OH, OH2741 OMe 1 PhCH.sub.2 CH.sub.2 CO.sub.2 Me OH, OH2742 OMe 1 PhCH.sub.2 (CH.sub.2).sub.2 CO.sub.2 Me OH, OH2743 OMe 1 PhCH.sub.2 (CH.sub.2).sub.3 CO.sub.2 Me OH, OH2744 OMe 1 PhCH.sub.2 3-NO.sub.2 -Ph OH, OH2745 OMe 1 PhCH.sub.2 4-NO.sub.2 -Ph OH, OH2746 OMe 1 PhCH.sub.2 3-CO.sub.2 H-Ph OH, OH2747 OMe 1 PhCH.sub.2 4-CO.sub.2 H-Ph OH, OH2748 OMe 1 PhCH.sub.2 3-CN.sub.4 H-Ph OH, OH2749 OMe 1 PhCH.sub.2 4-CN.sub.4 H-Ph OH, OH2750 OMe 1 PhCH.sub.2 3-(HOCH.sub.2)-Ph OH, OH2751 OMe 1 PhCH.sub.2 4-(HOCH.sub.2)-Ph OH, OH2752 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 H (+)-pin BI2753 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 Methyl (+)-pin2754 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 Ethyl (+)-pin2755 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 n-Propyl (+)-pin2756 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 n-Butyl (+)-pin2757 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 SCH.sub.3 (+)-pin2758 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 (SO)CH.sub.3 (+)-pin2759 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 (SO.sub.2)CH.sub.3 (+)-pin2760 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 SCH.sub.3 (+)-pin2761 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 (SO)CH.sub.3 (+)-pin2762 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3 (+)-pin2763 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CN (+)-pin2764 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 CN (+)-pin2765 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 CN (+)-pin2766 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 CF.sub.3 (+)-pin2767 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 CF.sub.2 CF.sub.3 (+)-pin2768 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 CF.sub.2 CF.sub.2 CF.sub.3 (+)-pin2769 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3 (+)-pin2770 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 F.sub.5 -Ph (+)-pin2771 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CO.sub.2 H (+)-pin2772 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.2 CO.sub.2 H (+)-pin2773 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.3 CO.sub.2 H (+)-pin2774 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CN.sub.4 H (+)-pin2775 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.2 CN.sub.4 H (+)-pin2776 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.3 CN.sub.4 H (+)-pin2777 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 NO.sub.2 (+)-pin2778 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.2 NO.sub.2 (+)-pin2779 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.3 NO.sub.2 (+)-pin2780 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 OH (+)-pin CZ2781 CH.sub.2 NH.sub.2 1 CH.sub.2 CH.sub.2 OCH.sub.2 Ph (+)-pin DA2782 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.2 OH (+)-pin2783 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.3 OH (+)-pin2784 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CO.sub.2 Me (+)-pin2785 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.2 CO.sub.2 Me (+)-pin2786 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.3 CO.sub.2 Me (+)-pin2787 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 3-NO.sub.2 -Ph (+)-pin2788 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 4-NO.sub.2 -Ph (+)-pin2789 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 3-CO.sub.2 H-Ph (+)-pin2790 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 4-CO.sub.2 H-Ph (+)-pin2791 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 3-CN.sub.4 H-Ph (+)-pin2792 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 4-CN.sub.4 H-Ph (+)-pin2793 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 3-(HOCH.sub.2)-Ph (+)-pin2794 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 4-(HOCH.sub.2)-Ph (+)-pin2795 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 H (+)-pin2796 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 Methyl (+)-pin2797 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 Ethyl (+)-pin2798 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 n-Propyl (+)-pin2799 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 n-Butyl (+)-pin2800 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 SCH.sub.3 (+)-pin2801 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 (SO)CH.sub.3 (+)-pin2802 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 (SO.sub.2)CH.sub.3 (+)-pin2803 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 SCH.sub.3 (+)-pin2804 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 (SO)CH.sub.3 (+)-pin2805 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3 (+)-pin2806 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CN (+)-pin2807 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 CN (+)-pin2808 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 CN (+)-pin2809 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CF.sub.3 (+)-pin2810 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CF.sub.2 CF.sub.3 (+)-pin2811 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CF.sub.2 CF.sub.2 CF.sub.3 (+)-pin2812 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3 (+)-pin2813 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 F.sub.5 -Ph (+)-pin2814 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CO.sub.2 H (+)-pin2815 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.2 CO.sub.2 H (+)-pin2816 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.3 CO.sub.2 H (+)-pin2817 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CN.sub.4 H (+)-pin2818 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.2 CN.sub.4 H (+)-pin2819 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.3 CN.sub.4 H (+)-pin2820 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 NO.sub.2 (+)-pin2821 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.2 NO.sub.2 (+)-pin2822 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.3 NO.sub.2 (+)-pin2823 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 OH (+)-pin2824 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.2 OH (+)-pin2825 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.3 OH (+)-pin2826 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CO.sub.2 Me (+)-pin2827 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.2 CO.sub.2 Me (+)-pin2828 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.3 CO.sub.2 Me (+)-pin2829 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 3-NO.sub.2 -Ph (+)-pin2830 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 4-NO.sub.2 -Ph (+)-pin2831 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 3-CO.sub.2 H-Ph (+)-pin2832 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 4-CO.sub.2 H-Ph (+)-pin2833 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 3-CN.sub.4 H-Ph (+)-pin2834 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 4-CN.sub.4 H-Ph (+)-pin2835 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 3-(HOCH.sub.2)-Ph (+)-pin2836 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 4-(HOCH.sub.2)-Ph (+)-pin2837 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 H OH, OH BJ2838 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 Methyl OH, OH2839 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 Ethyl OH, OH2840 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 n-Propyl OH, OH2841 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 n-Butyl OH, OH2842 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 SCH.sub.3 OH, OH2843 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 (SO)CH.sub.3 OH, OH2844 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 (SO.sub.2)CH.sub.3 OH, OH2845 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 SCH.sub.3 OH, OH2846 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 (SO)CH.sub.3 OH, OH2847 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3 OH, OH2848 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CN OH, OH2849 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 CN OH, OH2850 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 CN OH, OH2851 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 CF.sub.3 OH, OH2852 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 CF.sub.2 CF.sub.3 OH, OH2853 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 CF.sub.2 CF.sub.2 CF.sub.3 OH, OH2854 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3 OH, OH2855 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 F.sub.5 -Ph OH, OH2856 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CO.sub.2 H OH, OH2857 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.2 CO.sub.2 H OH, OH2858 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.3 CO.sub.2 H OH, OH2859 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CN.sub.4 H OH, OH2860 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.2 CN.sub.4 H OH, OH2861 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.3 CN.sub.4 H OH, OH2862 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 NO.sub.2 OH, OH2863 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.2 NO.sub.2 OH, OH2864 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.3 NO.sub.2 OH, OH2865 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 OH OH, OH2866 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.2 OH OH, OH2867 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.3 OH OH, OH2868 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CO.sub.2 Me OH, OH2869 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.2 CO.sub.2 Me OH, OH2870 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.3 CO.sub.2 Me OH, OH2871 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 3-NO.sub.2 -Ph OH, OH2872 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 4-NO.sub.2 -Ph OH, OH2873 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 3-CO.sub.2 H-Ph OH, OH2874 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 4-CO.sub.2 H-Ph OH, OH2875 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 3-CN.sub.4 H-Ph OH, OH2876 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 4-CN.sub.4 H-Ph OH, OH2877 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 3-(HOCH.sub.2)-Ph OH, OH2878 CH.sub.2 NH.sub.2 1 PhCH.sub.2 CH.sub.2 4-(HOCH.sub.2)-Ph OH, OH2879 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 H OH, OH2880 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 Methyl OH, OH2881 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 Ethyl OH, OH2882 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 n-Propyl OH, OH2883 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 n-Butyl OH, OH2884 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 SCH.sub.3 OH, OH2885 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 (SO)CH.sub.3 OH, OH2886 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 (SO.sub.2)CH.sub.3 OH, OH2887 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 SCH.sub.3 OH, OH2888 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 (SO)CH.sub.3 OH, OH2889 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3 OH, OH2890 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CN OH, OH2891 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 CN OH, OH2892 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 CN OH, OH2893 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CF.sub.3 OH, OH2894 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CF.sub.2 CF.sub.3 OH, OH2895 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CF.sub.2 CF.sub.2 CF.sub.3 OH, OH2896 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3 OH, OH2897 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 F.sub.5 -Ph OH, OH2898 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CO.sub.2 H OH, OH2899 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.2 CO.sub.2 H OH, OH2900 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.3 CO.sub.2 H OH, OH2901 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CN.sub.4 H OH, OH2902 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.2 CN.sub.4 H OH, OH2903 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.3 CN.sub.4 H OH, OH2904 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 NO.sub.2 OH, OH2905 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.2 NO.sub.2 OH, OH2906 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.3 NO.sub.2 OH, OH2907 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 OH OH, OH2908 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.2 OH OH, OH2909 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.3 OH OH, OH2910 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CO.sub.2 Me OH, OH2911 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.2 CO.sub.2 Me OH, OH2912 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.3 CO.sub.2 Me OH, OH2913 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 3-NO.sub.2 -Ph OH, OH2914 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 4-NO.sub.2 -Ph OH, OH2915 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 3-CO.sub.2 H-Ph OH, OH2916 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 4-CO.sub.2 H-Ph OH, OH2917 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 3-CN.sub.4 H-Ph OH, OH2918 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 4-CN.sub.4 H-Ph OH, OH2919 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 3-(HOCH.sub.2)-Ph OH, OH2920 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 4-(HOCH.sub.2)-Ph OH, OH2921 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 H (+)-pin2922 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 Methyl (+)-pin2923 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 Ethyl (+)-pin2924 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 n-Propyl (+)-pin2925 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 n-Butyl (+)-pin2926 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 SCH.sub.3 (+)-pin2927 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 (SO)CH.sub.3 (+)-pin2928 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 (SO.sub.2)CH.sub.3 (+)-pin2929 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 SCH.sub.3 (+)-pin2930 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 (SO)CH.sub.3 (+)-pin2931 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3 (+)-pin2932 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CN (+)-pin2933 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 CN (+)-pin2934 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 CN (+)-pin2935 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CF.sub.3 (+)-pin2936 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CF.sub.2 CF.sub.3 (+)-pin2937 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CF.sub.2 CF.sub.2 CF.sub.3 (+)-pin2938 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3 (+)-pin2939 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 F.sub.5 -Ph (+)-pin2940 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CO.sub.2 H (+)-pin2941 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.2 CO.sub.2 H (+)-pin2942 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.3 CO.sub.2 H (+)-pin2943 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CN.sub.4 H (+)-pin2944 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.2 CN.sub.4 H (+)-pin2945 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.3 CN.sub.4 H (+)-pin2946 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 NO.sub.2 (+)-pin2947 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.2 NO.sub.2 (+)-pin2948 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.3 NO.sub.2 (+)-pin2949 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 OH (+)-pin2950 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.2 OH (+)-pin2951 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.3 OH (+)-pin2952 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CO.sub.2 Me (+)-pin2953 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.2 CO.sub.2 Me (+)-pin2954 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.3 CO.sub.2 Me (+)-pin2955 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 3-NO.sub.2 -Ph (+)-pin2956 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 4-NO.sub.2 -Ph (+)-pin2957 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 3-CO.sub.2 H-Ph (+)-pin2958 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 4-CO.sub.2 H-Ph (+)-pin2959 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 3-CN.sub.4 H-Ph (+)-pin2960 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 4-CN.sub.4 H-Ph (+)-pin2961 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 3-(HOCH.sub.2)-Ph (+)-pin2962 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 4-(HOCH.sub.2)-Ph (+)-pin2963 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 H OH, OH2964 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 Methyl OH, OH2965 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 Ethyl OH, OH2966 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 n-Propyl OH, OH2967 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 n-Butyl OH, OH2968 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 SCH.sub.3 OH, OH2969 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 (SO)CH.sub.3 OH, OH2970 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 (SO.sub.2)CH.sub.3 OH, OH2971 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 SCH.sub.3 OH, OH2972 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 (SO)CH.sub.3 OH, OH2973 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3 OH, OH2974 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CN OH, OH2975 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 CN OH, OH2976 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 CN OH, OH2977 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CF.sub.3 OH, OH2978 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CF.sub.2 CF.sub.3 OH, OH2979 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CF.sub.2 CF.sub.2 CF.sub.3 OH, OH2980 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3 OH, OH2981 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 F.sub.5 -Ph OH, OH2982 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CO.sub.2 H OH, OH2983 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.2 CO.sub.2 H OH, OH2984 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.3 CO.sub.2 H OH, OH2985 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CN.sub.4 H OH, OH2986 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.2 CN.sub.4 H OH, OH2987 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.3 CN.sub.4 H OH, OH2988 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 NO.sub.2 OH, OH2989 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.2 NO.sub.2 OH, OH2990 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.3 NO.sub.2 OH, OH2991 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 OH OH, OH2992 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.2 OH OH, OH2993 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.3 OH OH, OH2994 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CO.sub.2 Me OH, OH2995 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.2 CO.sub.2 Me OH, OH2996 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.3 CO.sub.2 Me OH, OH2997 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 3-NO.sub.2 -Ph OH, OH2998 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 4-NO.sub.2 -Ph OH, OH2999 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 3-CO.sub.2 H-Ph OH, OH3000 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 4-CO.sub.2 H-Ph OH, OH3001 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 3-CN.sub.4 H-Ph OH, OH3002 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 4-CN.sub.4 H-Ph OH, OH3003 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 3-(HOCH.sub.2)-Ph OH, OH3004 S(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 4-(HOCH.sub.2)-Ph OH, OH3005 OMe 1 PhCH.sub.2 CH.sub.2 H (+)-pin3006 OMe 1 PhCH.sub.2 CH.sub.2 Methyl (+)-pin3007 OMe 1 PhCH.sub.2 CH.sub.2 Ethyl (+)-pin3008 OMe 1 PhCH.sub.2 CH.sub.2 n-Propyl (+)-pin3009 OMe 1 PhCH.sub.2 CH.sub.2 n-Butyl (+)-pin3010 OMe 1 PhCH.sub.2 CH.sub.2 CH.sub.2 SCH.sub.3 (+)-pin3011 OMe 1 PhCH.sub.2 CH.sub.2 CH.sub.2 (SO)CH.sub.3 (+)-pin3012 OMe 1 PhCH.sub.2 CH.sub.2 CH.sub.2 (SO.sub.2)CH.sub.3 (+)-pin3013 OMe 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 SCH.sub.3 (+)-pin3014 OMe 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 (SO)CH.sub.3 (+)-pin3015 OMe 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3 (+)-pin3016 OMe 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CN (+)-pin3017 OMe 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 CN (+)-pin3018 OMe 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 CN (+)-pin3019 OMe 1 PhCH.sub.2 CH.sub.2 CF.sub.3 (+)-pin3020 OMe 1 PhCH.sub.2 CH.sub.2 CF.sub.2 CF.sub.3 (+)-pin3021 OMe 1 PhCH.sub.2 CH.sub.2 CF.sub.2 CF.sub.2 CF.sub.3 (+)-pin3022 OMe 1 PhCH.sub.2 CH.sub.2 CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3 (+)-pin3023 OMe 1 PhCH.sub.2 CH.sub.2 F.sub.5 -Ph (+)-pin3024 OMe 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CO.sub.2 H (+)-pin3025 OMe 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.2 CO.sub.2 H (+)-pin3026 OMe 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.3 CO.sub.2 H (+)-pin3027 OMe 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CN.sub.4 H (+)-pin3028 OMe 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.2 CN.sub.4 H (+)-pin3029 OMe 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.3 CN.sub.4 H (+)-pin3030 OMe 1 PhCH.sub.2 CH.sub.2 CH.sub.2 NO.sub.2 (+)-pin3031 OMe 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.2 NO.sub.2 (+)-pin3032 OMe 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.3 NO.sub.2 (+)-pin3033 OMe 1 PhCH.sub.2 CH.sub.2 CH.sub.2 OH (+)-pin3034 OMe 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.2 OH (+)-pin3035 OMe 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.3 OH (+)-pin3036 OMe 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CO.sub.2 Me (+)-pin3037 OMe 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.2 CO.sub.2 Me (+)-pin3038 OMe 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.3 CO.sub.2 Me (+)-pin3039 OMe 1 PhCH.sub.2 CH.sub.2 3-NO.sub.2 -Ph (+)-pin3040 OMe 1 PhCH.sub.2 CH.sub.2 4-NO.sub.2 -Ph (+)-pin3041 OMe 1 PhCH.sub.2 CH.sub.2 3-CO.sub.2 H-Ph (+)-pin3042 OMe 1 PhCH.sub.2 CH.sub.2 4-CO.sub.2 H-Ph (+)-pin3043 OMe 1 PhCH.sub.2 CH.sub.2 3-CN.sub.4 H-Ph (+)-pin3044 OMe 1 PhCH.sub.2 CH.sub.2 4-CN.sub.4 H-Ph (+)-pin3045 OMe 1 PhCH.sub.2 CH.sub.2 3-(HOCH.sub.2)-Ph (+)-pin3046 OMe 1 PhCH.sub.2 CH.sub.2 4-(HOCH.sub.2)-Ph (+)-pin3047 OMe 1 PhCH.sub.2 CH.sub.2 H OH, OH3048 OMe 1 PhCH.sub.2 CH.sub.2 Methyl OH, OH3049 OMe 1 PhCH.sub.2 CH.sub.2 Ethyl OH, OH3050 OMe 1 PhCH.sub.2 CH.sub.2 n-Propyl OH, OH3051 OMe 1 PhCH.sub.2 CH.sub.2 n-Butyl OH, OH3052 OMe 1 PhCH.sub.2 CH.sub.2 CH.sub.2 SCH.sub.3 OH, OH3053 OMe 1 PhCH.sub.2 CH.sub.2 CH.sub.2 (SO)CH.sub.3 OH, OH3054 OMe 1 PhCH.sub.2 CH.sub.2 CH.sub.2 (SO.sub.2)CH.sub.3 OH, OH3055 OMe 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 SCH.sub.3 OH, OH3056 OMe 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 (SO)CH.sub.3 OH, OH3057 OMe 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3 OH, OH3058 OMe 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CN OH, OH3059 OMe 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 CN OH, OH3060 OMe 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 CN OH, OH3061 OMe 1 PhCH.sub.2 CH.sub.2 CF.sub.3 OH, OH3062 OMe 1 PhCH.sub.2 CH.sub.2 CF.sub.2 CF.sub.3 OH, OH3063 OMe 1 PhCH.sub.2 CH.sub.2 CF.sub.2 CF.sub.2 CF.sub.3 OH, OH3064 OMe 1 PhCH.sub.2 CH.sub.2 CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3 OH, OH3065 OMe 1 PhCH.sub.2 CH.sub.2 F.sub.5 -Ph OH, OH3066 OMe 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CO.sub.2 H OH, OH3067 OMe 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.2 CO.sub.2 H OH, OH3068 OMe 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.3 CO.sub.2 H OH, OH3069 OMe 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CN.sub.4 H OH, OH3070 OMe 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.2 CN.sub.4 H OH, OH3071 OMe 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.3 CN.sub.4 H OH, OH3072 OMe 1 PhCH.sub.2 CH.sub.2 CH.sub.2 NO.sub.2 OH, OH3073 OMe 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.2 NO.sub.2 OH, OH3074 OMe 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.3 NO.sub.2 OH, OH3075 OMe 1 PhCH.sub.2 CH.sub.2 CH.sub.2 OH OH, OH3076 OMe 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.2 OH OH, OH3077 OMe 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.3 OH OH, OH3078 OMe 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CO.sub.2 Me OH, OH3079 OMe 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.2 CO.sub.2 Me OH, OH3080 OMe 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.3 CO.sub.2 Me OH, OH3081 OMe 1 PhCH.sub.2 CH.sub.2 3-NO.sub.2 -Ph OH, OH3082 OMe 1 PhCH.sub.2 CH.sub.2 4-NO.sub.2 -Ph OH, OH3083 OMe 1 PhCH.sub.2 CH.sub.2 3-CO.sub.2 H-Ph OH, OH3084 OMe 1 PhCH.sub.2 CH.sub.2 4-CO.sub.2 H-Ph OH, OH3085 OMe 1 PhCH.sub.2 CH.sub.2 3-CN.sub.4 H-Ph OH, OH3086 OMe 1 PhCH.sub.2 CH.sub.2 4-CN.sub.4 H-Ph OH, OH3087 OMe 1 PhCH.sub.2 CH.sub.2 3-(HOCH.sub.2)-Ph OH, OH3088 OMe 1 PhCH.sub.2 CH.sub.2 4-(HOCH.sub.2)-Ph OH, OH3089 NH(CNH)NH.sub.2 1 Ph H (+)-pin3090 NH(CNH)NH.sub.2 1 Ph Methyl (+)-pin3091 NH(CNH)NH.sub.2 1 Ph Ethyl (+)-pin3092 NH(CNH)NH.sub.2 1 Ph n-Propyl (+)-pin3093 NH(CNH)NH.sub.2 1 Ph n-Butyl (+)-pin3094 NH(CNH)NH.sub.2 1 Ph CH.sub.2 SCH.sub.3 (+)-pin3095 NH(CNH)NH.sub.2 1 Ph CH.sub.2 (SO)CH.sub.3 (+)-pin3096 NH(CNH)NH.sub.2 1 Ph CH.sub.2 (SO.sub.2)CH.sub.3 (+)-pin3097 NH(CNH)NH.sub.2 1 Ph CH.sub.2 CH.sub.2 SCH.sub.3 (+)-pin3098 NH(CNH)NH.sub.2 1 Ph CH.sub.2 CH.sub.2 (SO)CH.sub.3 (+)-pin3099 NH(CNH)NH.sub.2 1 Ph CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3 (+)-pin3100 NH(CNH)NH.sub.2 1 Ph CH.sub.2 CN (+)-pin3101 NH(CNH)NH.sub.2 1 Ph CH.sub.2 CH.sub.2 CN (+)-pin3102 NH(CNH)NH.sub.2 1 Ph CH.sub.2 CH.sub.2 CH.sub.2 CN (+)-pin3103 NH(CNH)NH.sub.2 1 Ph CF.sub.3 (+)-pin3104 NH(CNH)NH.sub.2 1 Ph CF.sub.2 CF.sub.3 (+)-pin3105 NH(CNH)NH.sub.2 1 Ph CF.sub.2 CF.sub.2 CF.sub.3 (+)-pin3106 NH(CNH)NH.sub.2 1 Ph CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3 (+)-pin3107 NH(CNH)NH.sub.2 1 Ph F.sub.5 -Ph (+)-pin3108 NH(CNH)NH.sub.2 1 Ph CH.sub.2 CO.sub.2 H (+)-pin3109 NH(CNH)NH.sub.2 1 Ph (CH.sub.2).sub.2 CO.sub.2 H (+)-pin3110 NH(CNH)NH.sub.2 1 Ph (CH.sub.2).sub.3 CO.sub.2 H (+)-pin3111 NH(CNH)NH.sub.2 1 Ph CH.sub.2 CN.sub.4 H (+)-pin3112 NH(CNH)NH.sub.2 1 Ph (CH.sub.2).sub.2 CN.sub.4 H (+)-pin3113 NH(CNH)NH.sub.2 1 Ph (CH.sub.2).sub.3 CN.sub.4 H (+)-pin3114 NH(CNH)NH.sub.2 1 Ph CH.sub.2 NO.sub.2 (+)-pin3115 NH(CNH)NH.sub.2 1 Ph (CH.sub.2).sub.2 NO.sub.2 (+)-pin3116 NH(CNH)NH.sub.2 1 Ph (CH.sub.2).sub.3 NO.sub.2 (+)-pin3117 NH(CNH)NH.sub.2 1 Ph CH.sub.2 OH (+)-pin3118 NH(CNH)NH.sub.2 1 Ph (CH.sub.2).sub.2 OH (+)-pin3119 NH(CNH)NH.sub.2 1 Ph (CH.sub.2).sub.3 OH (+)-pin3120 NH(CNH)NH.sub.2 1 Ph CH.sub.2 CO.sub.2 Me (+)-pin3121 NH(CNH)NH.sub.2 1 Ph (CH.sub.2).sub.2 CO.sub.2 Me (+)-pin3122 NH(CNH)NH.sub.2 1 Ph (CH.sub.2).sub.3 CO.sub.2 Me (+)-pin3123 NH(CNH)NH.sub.2 1 Ph 3-NO.sub.2 -Ph (+)-pin3124 NH(CNH)NH.sub.2 1 Ph 4-NO.sub.2 -Ph (+)-pin3125 NH(CNH)NH.sub.2 1 Ph 3-CO.sub.2 H-Ph (+)-pin3126 NH(CNH)NH.sub.2 1 Ph 4-CO.sub.2 H-Ph (+)-pin3127 NH(CNH)NH.sub.2 1 Ph 3-CN.sub.4 H-Ph (+)-pin3128 NH(CNH)NH.sub.2 1 Ph 4-CN.sub.4 H-Ph (+)-pin3129 NH(CNH)NH.sub.2 1 Ph 3-(HOCH.sub.2)-Ph (+)-pin3130 NH(CNH)NH.sub.2 1 Ph 4-(HOCH.sub.2)-Ph (+)-pin3131 NH(CNH)NH.sub.2 1 Ph H OH, OH3132 NH(CNH)NH.sub.2 1 Ph Methyl OH, OH3133 NH(CNH)NH.sub.2 1 Ph Ethyl OH, OH3134 NH(CNH)NH.sub.2 1 Ph n-Propyl OH, OH3135 NH(CNH)NH.sub.2 1 Ph n-Butyl OH, OH3136 NH(CNH)NH.sub.2 1 Ph CH.sub.2 SCH.sub.3 OH, OH3137 NH(CNH)NH.sub.2 1 Ph CH.sub.2 (SO)CH.sub.3 OH, OH3138 NH(CNH)NH.sub.2 1 Ph CH.sub.2 (SO.sub.2)CH.sub.3 OH, OH3139 NH(CNH)NH.sub.2 1 Ph CH.sub.2 CH.sub.2 SCH.sub.3 OH, OH3140 NH(CNH)NH.sub.2 1 Ph CH.sub.2 CH.sub.2 (SO)CH.sub.3 OH, OH3141 NH(CNH)NH.sub.2 1 Ph CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3 OH, OH3142 NH(CNH)NH.sub.2 1 Ph CH.sub.2 CN OH, OH3143 NH(CNH)NH.sub.2 1 Ph CH.sub.2 CH.sub.2 CN OH, OH3144 NH(CNH)NH.sub.2 1 Ph CH.sub.2 CH.sub.2 CH.sub.2 CN OH, OH3145 NH(CNH)NH.sub.2 1 Ph CF.sub.3 OH, OH3146 NH(CNH)NH.sub.2 1 Ph CF.sub.2 CF.sub.3 OH, OH3147 NH(CNH)NH.sub.2 1 Ph CF.sub.2 CF.sub.2 CF.sub.3 OH, OH3148 NH(CNH)NH.sub.2 1 Ph CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3 OH, OH3149 NH(CNH)NH.sub.2 1 Ph F.sub.5 -Ph OH, OH3150 NH(CNH)NH.sub.2 1 Ph CH.sub.2 CO.sub.2 H OH, OH3151 NH(CNH)NH.sub.2 1 Ph (CH.sub.2).sub.2 CO.sub.2 H OH, OH3152 NH(CNH)NH.sub.2 1 Ph (CH.sub.2).sub.3 CO.sub.2 H OH, OH3153 NH(CNH)NH.sub.2 1 Ph CH.sub.2 CN.sub.4 H OH, OH3154 NH(CNH)NH.sub.2 1 Ph (CH.sub.2).sub.2 CN.sub.4 H OH, OH3155 NH(CNH)NH.sub.2 1 Ph (CH.sub.2).sub.3 CN.sub.4 H OH, OH3156 NH(CNH)NH.sub.2 1 Ph CH.sub.2 NO.sub.2 OH, OH3157 NH(CNH)NH.sub.2 1 Ph (CH.sub.2).sub.2 NO.sub.2 OH, OH3158 NH(CNH)NH.sub.2 1 Ph (CH.sub.2).sub.3 NO.sub.2 OH, OH3159 NH(CNH)NH.sub.2 1 Ph CH.sub.2 OH OH, OH3160 NH(CNH)NH.sub.2 1 Ph (CH.sub.2).sub.2 OH OH, OH3161 NH(CNH)NH.sub.2 1 Ph (CH.sub.2).sub.3 OH OH, OH3162 NH(CNH)NH.sub.2 1 Ph CH.sub.2 CO.sub.2 Me OH, OH3163 NH(CNH)NH.sub.2 1 Ph (CH.sub.2).sub.2 CO.sub.2 Me OH, OH3164 NH(CNH)NH.sub.2 1 Ph (CH.sub.2).sub.3 CO.sub.2 Me OH, OH3165 NH(CNH)NH.sub.2 1 Ph 3-NO.sub.2 -Ph OH, OH3166 NH(CNH)NH.sub.2 1 Ph 4-NO.sub.2 -Ph OH, OH3167 NH(CNH)NH.sub.2 1 Ph 3-CO.sub.2 H-Ph OH, OH3168 NH(CNH)NH.sub.2 1 Ph 4-CO.sub.2 H-Ph OH, OH3169 NH(CNH)NH.sub.2 1 Ph 3-CN.sub.4 H-Ph OH, OH3170 NH(CNH)NH.sub.2 1 Ph 4-CN.sub.4 H-Ph OH, OH3171 NH(CNH)NH.sub.2 1 Ph 3-(HOCH.sub.2)-Ph OH, OH3172 NH(CNH)NH.sub.2 1 Ph 4-(HOCH.sub.2)-Ph OH, OH3173 NH(CNH)NH.sub.2 1 PhCH.sub.2 H (+)-pin3174 NH(CNH)NH.sub.2 1 PhCH.sub.2 Methyl (+)-pin3175 NH(CNH)NH.sub.2 1 PhCH.sub.2 Ethyl (+)-pin3176 NH(CNH)NH.sub.2 1 PhCH.sub.2 n-Propyl (+)-pin3177 NH(CNH)NH.sub.2 1 PhCH.sub.2 n-Butyl (+)-pin3178 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 SCH.sub.3 (+)-pin3179 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 (SO)CH.sub.3 (+)-pin3180 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 (SO.sub.2)CH.sub.3 (+)-pin3181 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 SCH.sub.3 (+)-pin3182 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 (SO)CH.sub.3 (+)-pin3183 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3 (+)-pin3184 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CN (+)-pin3185 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CN (+)-pin3186 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 CN (+)-pin3187 NH(CNH)NH.sub.2 1 PhCH.sub.2 CF.sub.3 (+)-pin3188 NH(CNH)NH.sub.2 1 PhCH.sub.2 CF.sub.2 CF.sub.3 (+)-pin3189 NH(CNH)NH.sub.2 1 PhCH.sub.2 CF.sub.2 CF.sub.2 CF.sub.3 (+)-pin3190 NH(CNH)NH.sub.2 1 PhCH.sub.2 CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3 (+)-pin3191 NH(CNH)NH.sub.2 1 PhCH.sub.2 F.sub.5 -Ph (+)-pin3192 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CO.sub.2 H (+)-pin3193 NH(CNH)NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.2 CO.sub.2 H (+)-pin3194 NH(CNH)NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.3 CO.sub.2 H (+)-pin3195 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CN.sub.4 H (+)-pin3196 NH(CNH)NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.2 CN.sub.4 H (+)-pin3197 NH(CNH)NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.3 CN.sub.4 H (+)-pin3198 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 NO.sub.2 (+)-pin3199 NH(CNH)NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.2 NO.sub.2 (+)-pin3200 NH(CNH)NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.3 NO.sub.2 (+)-pin3201 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 OH (+)-pin3202 NH(CNH)NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.2 OH (+)-pin3203 NH(CNH)NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.3 OH (+)-pin3204 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CO.sub.2 Me (+)-pin3205 NH(CNH)NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.2 CO.sub.2 Me (+)-pin3206 NH(CNH)NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.3 CO.sub.2 Me (+)-pin3207 NH(CNH)NH.sub.2 1 PhCH.sub.2 3-NO.sub.2 -Ph (+)-pin3208 NH(CNH)NH.sub.2 1 PhCH.sub.2 4-NO.sub.2 -Ph (+)-pin3209 NH(CNH)NH.sub.2 1 PhCH.sub.2 3-CO.sub.2 H-Ph (+)-pin3210 NH(CNH)NH.sub.2 1 PhCH.sub.2 4-CO.sub.2 H-Ph (+)-pin3211 NH(CNH)NH.sub.2 1 PhCH.sub.2 3-CN.sub.4 H-Ph (+)-pin3212 NH(CNH)NH.sub.2 1 PhCH.sub.2 4-CN.sub.4 H-Ph (+)-pin3213 NH(CNH)NH.sub.2 1 PhCH.sub.2 3-(HOCH.sub.2)-Ph (+)-pin3214 NH(CNH)NH.sub.2 1 PhCH.sub.2 4-(HOCH.sub.2)-Ph (+)-pin3215 NH(CNH)NH.sub.2 1 PhCH.sub.2 H OH, OH3216 NH(CNH)NH.sub.2 1 PhCH.sub.2 Methyl OH, OH3217 NH(CNH)NH.sub.2 1 PhCH.sub.2 Ethyl OH, OH3218 NH(CNH)NH.sub.2 1 PhCH.sub.2 n-Propyl OH, OH3219 NH(CNH)NH.sub.2 1 PhCH.sub.2 n-Butyl OH, OH3220 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 SCH.sub.3 OH, OH3221 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 (SO)CH.sub.3 OH, OH3222 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 (SO.sub.2)CH.sub.3 OH, OH3223 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 SCH.sub.3 OH, OH3224 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 (SO)CH.sub.3 OH, OH3225 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3 OH, OH3226 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CN OH, OH3227 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CN OH, OH3228 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 CN OH, OH3229 NH(CNH)NH.sub.2 1 PhCH.sub.2 CF.sub.3 OH, OH3230 NH(CNH)NH.sub.2 1 PhCH.sub.2 CF.sub.2 CF.sub.3 OH, OH3231 NH(CNH)NH.sub.2 1 PhCH.sub.2 CF.sub.2 CF.sub.2 CF.sub.3 OH, OH3232 NH(CNH)NH.sub.2 1 PhCH.sub.2 CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3 OH, OH3233 NH(CNH)NH.sub.2 1 PhCH.sub.2 F.sub.5 -Ph OH, OH3234 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CO.sub.2 H OH, OH3235 NH(CNH)NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.2 CO.sub.2 H OH, OH3236 NH(CNH)NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.3 CO.sub.2 H OH, OH3237 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CN.sub.4 H OH, OH3238 NH(CNH)NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.2 CN.sub.4 H OH, OH3239 NH(CNH)NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.3 CN.sub.4 H OH, OH3240 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 NO.sub.2 OH, OH3241 NH(CNH)NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.2 NO.sub.2 OH, OH3242 NH(CNH)NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.3 NO.sub.2 OH, OH3243 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 OH OH, OH3244 NH(CNH)NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.2 OH OH, OH3245 NH(CNH)NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.3 OH OH, OH3246 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CO.sub.2 Me OH, OH3247 NH(CNH)NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.2 CO.sub.2 Me OH, OH3248 NH(CNH)NH.sub.2 1 PhCH.sub.2 (CH.sub.2).sub.3 CO.sub.2 Me OH, OH3249 NH(CNH)NH.sub.2 1 PhCH.sub.2 3-NO.sub.2 -Ph OH, OH3250 NH(CNH)NH.sub.2 1 PhCH.sub.2 4-NO.sub.2 -Ph OH, OH3251 NH(CNH)NH.sub.2 1 PhCH.sub.2 3-CO.sub.2 H-Ph OH, OH3252 NH(CNH)NH.sub.2 1 PhCH.sub.2 4-CO.sub.2 H-Ph OH, OH3253 NH(CNH)NH.sub.2 1 PhCH.sub.2 3-CN.sub.4 H-Ph OH, OH3254 NH(CNH)NH.sub.2 1 PhCH.sub.2 4-CN.sub.4 H-Ph OH, OH3255 NH(CNH)NH.sub.2 1 PhCH.sub.2 3-(HOCH.sub.2)-Ph OH, OH3256 NH(CNH)NH.sub.2 1 PhCH.sub.2 4-(HOCH.sub.2)-Ph OH, OH3257 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 H (+)-pin3258 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 Methyl (+)-pin3259 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 Ethyl (+)-pin3260 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 n-Propyl (+)-pin3261 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 n-Butyl (+)-pin3262 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 SCH.sub.3 (+)-pin3263 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 (SO)CH.sub.3 (+)-pin3264 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 (SO.sub.2)CH.sub.3 (+)-pin3265 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 SCH.sub.3 (+)-pin3266 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 (SO)CH.sub.3 (+)-pin3267 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3 (+)-pin3268 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CN (+)-pin3269 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 CN (+)-pin3270 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 CN (+)-pin3271 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CF.sub.3 (+)-pin3272 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CF.sub.2 CF.sub.3 (+)-pin3273 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CF.sub.2 CF.sub.2 CF.sub.3 (+)-pin3274 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3 (+)-pin3275 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 F.sub.5 -Ph (+)-pin3276 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CO.sub.2 H (+)-pin3277 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.2 CO.sub.2 H (+)-pin3278 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.3 CO.sub.2 H (+)-pin3279 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CN.sub.4 H (+)-pin3280 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.2 CN.sub.4 H (+)-pin3281 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.3 CN.sub.4 H (+)-pin3282 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 NO.sub.2 (+)-pin3283 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.2 NO.sub.2 (+)-pin3284 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.3 NO.sub.2 (+)-pin3285 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 OH (+)-pin3286 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.2 OH (+)-pin3287 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.3 OH (+)-pin3288 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CO.sub.2 Me (+)-pin3289 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.2 CO.sub.2 Me (+)-pin3290 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.3 CO.sub.2 Me (+)-pin3291 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 3-NO.sub.2 -Ph (+)-pin3292 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 4-NO.sub.2 -Ph (+)-pin3293 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 3-CO.sub.2 H-Ph (+)-pin3294 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 4-CO.sub.2 H-Ph (+)-pin3295 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 3-CN.sub.4 H-Ph (+)-pin3296 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 4-CN.sub.4 H-Ph (+)-pin3297 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 3-(HOCH.sub.2)-Ph (+)-pin3298 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 4-(HOCH.sub.2)-Ph (+)-pin3299 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 H OH, OH3300 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 Methyl OH, OH3301 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 Ethyl OH, OH3302 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 n-Propyl OH, OH3303 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 n-Butyl OH, OH3304 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 SCH.sub.3 OH, OH3305 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 (SO)CH.sub.3 OH, OH3306 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 (SO.sub.2)CH.sub.3 OH, OH3307 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 SCH.sub.3 OH, OH3308 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 (SO)CH.sub.3 OH, OH3309 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3 OH, OH3310 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CN OH, OH3311 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 CN OH, OH3312 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 CN OH, OH3313 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CF.sub.3 OH, OH3314 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CF.sub.2 CF.sub.3 OH, OH3315 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CF.sub.2 CF.sub.2 CF.sub.3 OH, OH3316 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3 OH, OH3317 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 F.sub.5 -Ph OH, OH3318 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CO.sub.2 H OH, OH3319 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.2 CO.sub.2 H OH, OH3320 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.3 CO.sub.2 H OH, OH3321 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CN.sub.4 H OH, OH3322 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.2 CN.sub.4 H OH, OH3323 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.3 CN.sub.4 H OH, OH3324 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 NO.sub.2 OH, OH3325 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.2 NO.sub.2 OH, OH3326 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.3 NO.sub.2 OH, OH3327 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 OH OH, OH3328 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.2 OH OH, OH3329 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.3 OH OH, OH3330 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 CH.sub.2 CO.sub.2 Me OH, OH3331 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.2 CO.sub.2 Me OH, OH3332 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 (CH.sub.2).sub.3 CO.sub.2 Me OH, OH3333 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 3-NO.sub.2 -Ph OH, OH3334 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 4-NO.sub.2 -Ph OH, OH3335 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 3-CO.sub.2 H-Ph OH, OH3336 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 4-CO.sub.2 H-Ph OH, OH3337 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 3-CN.sub.4 H-Ph OH, OH3338 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 4-CN.sub.4 H-Ph OH, OH3339 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 3-(HOCH.sub.2)-Ph OH, OH3340 NH(CNH)NH.sub.2 1 PhCH.sub.2 CH.sub.2 4-(HOCH.sub.2)-Ph OH, OH__________________________________________________________________________ BA. MS (M+H).sup.+ : Calc. 480, Found 480. BC. MS (M+H).sup.+ : Calc. 494, Found 494. BD. MS (M+H).sup.+ : Calc. 522, Found 522. BE. MS (M+H).sup.+ : Calc. 540, Found 540. BF. MS (M+H).sup.+ : Calc. 519, Found 519. BG. MS (M+H).sup.+ : Calc. 538, Found 538. BH. MS (M+H).sup.+ : Calc. 346, Found 346. BI. MS (M+H).sup.+ : Calc. 494, Found 494. BJ. Anal. calcd. for C.sub.17 H.sub.26 BN.sub.5 O.sub.3.2H.sub.2 O.1.8HCl C, 44.30; H, 6.95; Cl, 13.84; N, 15.20. Found: C, 44.22; H, 6.66; Cl, 14.03; N, 14.03. BW. MS (M+H).sup.+ : Calc. 466, Found 466. BX. MS (M+H).sup.+ : Calc. 480, Found 480. CV. MS (M+H).sup.+ : Calc. 510, Found 510. CW. MS (M+H).sup.+ : Calc. 600, Found 600. CX. MS (M+H).sup.+ : Calc. 552, Found 552. CY. MS (M+H).sup.+ : Calc. 629, Found 629. CZ. MS (M+H).sup.+ : Calc. 524, Found 524. DA. MS (M+H).sup.+ : Calc. 614, Found 614. TABLE 16______________________________________ ##STR111## Phys.Ex X m R.sup.13 R.sup.14 Y.sup.1 Y.sup.2 Data______________________________________3345 CH.sub.2 NH.sub.2 1 Ph Ph (+)-pin3346 CH.sub.2 NH.sub.2 1 Ph PhCH.sub.2 (+)-pin3347 CH.sub.2 NH.sub.2 1 Ph Ph(CH.sub.2).sub.2 (+)-pin3348 CH.sub.2 NH.sub.2 1 PhCH.sub.2 Ph (+)-pin3349 CH.sub.2 NH.sub.2 1 PhCH.sub.2 PhCH.sub.2 (+)-pin BY3350 CH.sub.2 NH.sub.2 1 PhCH.sub.2 Ph(CH.sub.2).sub.2 (+)-pin3351 CH.sub.2 NH.sub.2 1 Ph(CH.sub.2).sub.2 Ph (+)-pin3352 CH.sub.2 NH.sub.2 1 Ph(CH.sub.2).sub.2 PhCH.sub.2 (+)-pin3353 CH.sub.2 NH.sub.2 1 Ph(CH.sub.2).sub.2 Ph(CH.sub.2).sub.2 (+)-pin3354 CH.sub.2 NH.sub.2 1 Ph Ph OH, OH3355 CH.sub.2 NH.sub.2 1 Ph PhCH.sub.2 OH, OH3356 CH.sub.2 NH.sub.2 1 Ph Ph(CH.sub.2).sub.2 OH, OH3357 CH.sub.2 NH.sub.2 1 PhCH.sub.2 Ph OH, OH3358 CH.sub.2 NH.sub.2 1 PhCH.sub.2 PhCH.sub.2 OH, OH3359 CH.sub.2 NH.sub.2 1 PhCH.sub.2 Ph(CH.sub.2).sub.2 OH, OH3360 CH.sub.2 NH.sub.2 1 Ph(CH.sub.2).sub.2 Ph OH, OH3361 CH.sub.2 NH.sub.2 1 Ph(CH.sub.2).sub.2 PhCH.sub.2 OH, OH3362 CH.sub.2 NH.sub.2 1 Ph(CH.sub.2).sub.2 Ph(CH.sub.2).sub.2 OH, OH3363 NH(CNH)NH.sub.2 1 Ph Ph (+)-pin3364 NH(CNH)NH.sub.2 1 Ph PhCH.sub.2 (+)-pin3365 NH(CNH)NH.sub.2 1 Ph Ph(CH.sub.2).sub.2 (+)-pin3366 NH(CNH)NH.sub.2 1 PhCH.sub.2 Ph (+)-pin3367 NH(CNH)NH.sub.2 1 PhCH.sub.2 PhCH.sub.2 (+)-pin3368 NH(CNH)NH.sub.2 1 PhCH.sub.2 Ph(CH.sub.2).sub.2 (+)-pin3369 NH(CNH)NH.sub.2 1 Ph(CH.sub.2).sub.2 Ph (+)-pin3370 NH(CNH)NH.sub.2 1 Ph(CH.sub.2).sub.2 PhCH.sub.2 (+)-pin3371 NH(CNH)NH.sub.2 1 Ph(CH.sub.2).sub.2 Ph(CH.sub.2).sub.2 (+)-pin3372 NH(CNH)NH.sub.2 1 Ph Ph OH, OH3373 NH(CNH)NH.sub.2 1 Ph PhCH.sub.2 OH, OH3374 NH(CNH)NH.sub.2 1 Ph Ph(CH.sub.2).sub.2 OH, OH3375 NH(CNH)NH.sub.2 1 PhCH.sub.2 Ph OH, OH3376 NH(CNH)NH.sub.2 1 PhCH.sub.2 PhCH.sub.2 OH, OH3377 NH(CNH)NH.sub.2 1 PhCH.sub.2 Ph(CH.sub.2).sub.2 OH, OH3378 NH(CNH)NH.sub.2 1 Ph(CH.sub.2).sub.2 Ph OH, OH3379 NH(CNH)NH.sub.2 1 Ph(CH.sub.2).sub.2 PhCH.sub.2 OH, OH3380 NH(CNH)NH.sub.2 1 Ph(CH.sub.2).sub.2 Ph(CH.sub.2).sub.2 OH, OH3381 OMe 1 Ph Ph (+)-pin3382 OMe 1 Ph PhCH.sub.2 (+)-pin3383 OMe 1 Ph Ph(CH.sub.2).sub.2 (+)-pin3384 OMe 1 PhCH.sub.2 Ph (+)-pin3385 OMe 1 PhCH.sub.2 PhCH.sub.2 (+)-pin3386 OMe 1 PhCH.sub.2 Ph(CH.sub.2).sub.2 (+)-pin3387 OMe 1 Ph(CH.sub.2).sub.2 Ph (+)-pin3388 OMe 1 Ph(CH.sub.2).sub.2 PhCH.sub.2 (+)-pin3389 OMe 1 Ph(CH.sub.2).sub.2 Ph(CH.sub.2).sub.2 (+)-pin3390 OMe 1 Ph Ph OH, OH3391 OMe 1 Ph PhCH.sub.2 OH, OH3392 OMe 1 Ph Ph(CH.sub.2).sub.2 OH, OH3393 OMe 1 PhCH.sub.2 Ph OH, OH3394 OMe 1 PhCH.sub.2 PhCH.sub.2 OH, OH3395 OMe 1 PhCH.sub.2 Ph(CH.sub.2).sub.2 OH, OH3396 OMe 1 Ph(CH.sub.2).sub.2 Ph OH, OH3397 OMe 1 Ph(CH.sub.2).sub.2 PhCH.sub.2 OH, OH3398 OMe 1 Ph(CH.sub.2).sub.2 Ph(CH.sub.2).sub.2 OH, OH3399 NH(CNH)H 1 Ph Ph (+)-pin3400 NH(CNH)H 1 Ph PhCH.sub.2 (+)-pin3401 NH(CNH)H 1 Ph Ph(CH.sub.2).sub.2 (+)-pin3402 NH(CNH)H 1 PhCH.sub.2 Ph (+)-pin3403 NH(CNH)H 1 PhCH.sub.2 PhCH.sub.2 (+)-pin3404 NH(CNH)H 1 PhCH.sub.2 Ph(CH.sub.2).sub.2 (+)-pin3405 NH(CNH)H 1 Ph(CH.sub.2).sub.2 Ph (+)-pin3406 NH(CNH)H 1 Ph(CH.sub.2).sub.2 PhCH.sub.2 (+)-pin3407 NH(CNH)H 1 Ph(CH.sub.2).sub.2 Ph(CH.sub.2).sub.2 (+)-pin3408 NH(CNH)H 1 Ph Ph OH, OH3409 NH(CNH)H 1 Ph PhCH.sub.2 OH, OH3410 NH(CNH)H 1 Ph Ph(CH.sub.2).sub.2 OH, OH3411 NH(CNH)H 1 PhCH.sub.2 Ph OH, OH3412 NH(CNH)H 1 PhCH.sub.2 PhCH.sub.2 OH, OH3413 NH(CNH)H 1 PhCH.sub.2 Ph(CH.sub.2).sub.2 OH, OH3414 NH(CNH)H 1 Ph(CH.sub.2).sub.2 Ph OH, OH3415 NH(CNH)H 1 Ph(CH.sub.2).sub.2 PhCH.sub.2 OH, OH3416 NH(CNH)H 1 Ph(CH.sub.2).sub.2 Ph(CH.sub.2).sub.2 OH, OH3417 CH.sub.2 NH.sub.2 2 Ph Ph (+)-pin3418 CH.sub.2 NH.sub.2 2 Ph PhCH.sub.2 (+)-pin3419 CH.sub.2 NH.sub.2 2 Ph Ph(CH.sub.2).sub.2 (+)-pin3420 CH.sub.2 NH.sub.2 2 PhCH.sub.2 Ph (+)-pin3421 CH.sub.2 NH.sub.2 2 PhCH.sub.2 PhCH.sub.2 (+)-pin3422 CH.sub.2 NH.sub.2 2 PhCH.sub.2 Ph(CH.sub.2).sub.2 (+)-pin3423 CH.sub.2 NH.sub.2 2 Ph(CH.sub.2).sub.2 Ph (+)-pin3424 CH.sub.2 NH.sub.2 2 Ph(CH.sub.2).sub.2 PhCH.sub.2 (+)-pin3425 CH.sub.2 NH.sub.2 2 Ph(CH.sub.2).sub.2 Ph(CH.sub.2).sub.2 (+)-pin3426 CH.sub.2 NH.sub.2 2 Ph Ph OH, OH3427 CH.sub.2 NH.sub.2 2 Ph PhCH.sub.2 OH, OH3428 CH.sub.2 NH.sub.2 2 Ph Ph(CH.sub.2).sub.2 OH, OH3429 CH.sub.2 NH.sub.2 2 PhCH.sub.2 Ph OH, OH3430 CH.sub.2 NH.sub.2 2 PhCH.sub.2 PhCH.sub.2 OH, OH3431 CH.sub.2 NH.sub.2 2 PhCH.sub.2 Ph(CH.sub.2).sub.2 OH, OH3432 CH.sub.2 NH.sub.2 2 Ph(CH.sub.2).sub.2 Ph OH, OH3433 CH.sub.2 NH.sub.2 2 Ph(CH.sub.2).sub.2 PhCH.sub.2 OH, OH3434 CH.sub.2 NH.sub.2 2 Ph(CH.sub.2).sub.2 Ph(CH.sub.2).sub.2 OH, OH3435 NH(CNH)NH.sub.2 2 Ph Ph (+)-pin3436 NH(CNH)NH.sub.2 2 Ph PhCH.sub.2 (+)-pin3437 NH(CNH)NH.sub.2 2 Ph Ph(CH.sub.2).sub.2 (+)-pin3438 NH(CNH)NH.sub.2 2 PhCH.sub.2 Ph (+)-pin3439 NH(CNH)NH.sub.2 2 PhCH.sub.2 PhCH.sub.2 (+)-pin3440 NH(CNH)NH.sub.2 2 PhCH.sub.2 Ph(CH.sub.2).sub.2 (+)-pin3441 NH(CNH)NH.sub.2 2 Ph(CH.sub.2).sub.2 Ph (+)-pin3442 NH(CNH)NH.sub.2 2 Ph(CH.sub.2).sub.2 PhCH.sub.2 (+)-pin3443 NH(CNH)NH.sub.2 2 Ph(CH.sub.2).sub.2 Ph(CH.sub.2).sub.2 (+)-pin3444 NH(CNH)NH.sub.2 2 Ph Ph OH, OH3445 NH(CNH)NH.sub.2 2 Ph PhCH.sub.2 OH, OH3446 NH(CNH)NH.sub.2 2 Ph Ph(CH.sub.2).sub.2 OH, OH3447 NH(CNH)NH.sub.2 2 PhCH.sub.2 Ph OH, OH3448 NH(CNH)NH.sub.2 2 PhCH.sub.2 PhCH.sub.2 OH, OH3449 NH(CNH)NH.sub.2 2 PhCH.sub.2 Ph(CH.sub.2).sub.2 OH, OH3450 NH(CNH)NH.sub.2 2 Ph(CH.sub.2).sub.2 Ph OH, OH3451 NH(CNH)NH.sub.2 2 Ph(CH.sub.2).sub.2 PhCH.sub.2 OH, OH3452 NH(CNH)NH.sub.2 2 Ph(CH.sub.2).sub.2 Ph(CH.sub.2).sub.2 OH, OH______________________________________ BY. MS (M+H).sup.+ : Calc. 570, Found 570. TABLE 17__________________________________________________________________________ ##STR112## Phys.Ex X R.sup.13 R.sup.14 R.sup.15 Y.sup.1 Y.sup.2 Data__________________________________________________________________________3457 CH.sub.2 NH.sub.2 Ph H H (+)-pin3458 CH.sub.2 NH.sub.2 Ph methyl H (+)-pin BK3459 CH.sub.2 NH.sub.2 Ph methyl H (+)-pin3460 CH.sub.2 NH.sub.2 Ph methyl methyl (+)-pin3461 CH.sub.2 NH.sub.2 Ph ethyl H (+)-pin3462 CH.sub.2 NH.sub.2 Ph ethyl methyl (+)-pin3463 CH.sub.2 NH.sub.2 Ph ethyl ethyl (+)-pin3464 CH.sub.2 NH.sub.2 Ph isopropyl H (+)-pin3465 CH.sub.2 NH.sub.2 Ph phenyl H (+)-pin BL3466 CH.sub.2 NH.sub.2 Ph CH.sub.2 CN H (+)-pin3467 CH.sub.2 NH.sub.2 Ph CH.sub.2 NC H (+)-pin3468 CH.sub.2 NH.sub.2 Ph CH.sub.2 NO.sub.2 H (+)-pin3469 CH.sub.2 NH.sub.2 Ph CH.sub.2 SCH.sub.3 H (+)-pin3470 CH.sub.2 NH.sub.2 Ph CH.sub.2 SOCH.sub.3 H (+)-pin3471 CH.sub.2 NH.sub.2 Ph CH.sub.2 SO.sub.2 CH.sub.3 H (+)-pin3472 CH.sub.2 NH.sub.2 Ph CH.sub.2 OH H (+)-pin3473 CH.sub.2 NH.sub.2 Ph CH.sub.2 COOH H (+)-pin3474 CH.sub.2 NH.sub.2 Ph (CH.sub.2).sub.2 COOH H (+)-pin3475 CH.sub.2 NH.sub.2 Ph (CH.sub.2).sub.2 CN H (+)-pin3476 CH.sub.2 NH.sub.2 Ph CHCHCOOMe H (+)-pin3477 CH.sub.2 NH.sub.2 Ph CHCHCOOH H (+)-pin3478 CH.sub.2 NH.sub.2 Ph CHCHCN H (+)-pin3479 CH.sub.2 NH.sub.2 Ph CH.sub.2 CN.sub.4 H H (+)-pin3480 CH.sub.2 NH.sub.2 Ph CH.sub.2 NHSO.sub.2 CF.sub.3 H (+)-pin3481 CH.sub.2 NH.sub.2 Ph CH.sub.2 CH.sub.2 CN H (+)-pin3482 CH.sub.2 NH.sub.2 Ph CH.sub.2 CH.sub.2 NC H (+)-pin3483 CH.sub.2 NH.sub.2 Ph CH.sub.2 CH.sub.2 NO.sub.2 H (+)-pin3484 CH.sub.2 NH.sub.2 Ph CH.sub.2 CH.sub.2 SCH.sub.3 H (+)-pin3485 CH.sub.2 NH.sub.2 Ph CH.sub.2 CH.sub.2 SOCH.sub.3 H (+)-pin3486 CH.sub.2 NH.sub.2 Ph CH.sub.2 CH.sub.2 SO.sub.2 CH.sub.3 H (+)-pin3487 CH.sub.2 NH.sub.2 Ph CH.sub.2 CH.sub.2 CH.sub.2 OH H (+)-pin3488 CH.sub.2 NH.sub.2 Ph NO.sub.2 H (+)-pin3489 CH.sub.2 NH.sub.2 Ph F H (+)-pin3490 CH.sub.2 NH.sub.2 Ph OH H (+)-pin3491 CH.sub.2 NH.sub.2 Ph H H OH, OH3492 CH.sub.2 NH.sub.2 Ph methyl H OH, OH3493 CH.sub.2 NH.sub.2 Ph methyl methyl OH, OH3494 CH.sub.2 NH.sub.2 Ph ethyl H OH, OH3495 CH.sub.2 NH.sub.2 Ph ethyl methyl OH, OH3496 CH.sub.2 NH.sub.2 Ph ethyl ethyl OH, OH3497 CH.sub.2 NH.sub.2 Ph isopropyl H OH, OH3498 CH.sub.2 NH.sub.2 Ph phenyl H OH, OH3499 CH.sub.2 NH.sub.2 Ph CH.sub.2 CN H OH, OH3500 CH.sub.2 NH.sub.2 Ph CH.sub.2 NC H OH, OH3501 CH.sub.2 NH.sub.2 Ph CH.sub.2 NO.sub.2 H OH, OH3502 CH.sub.2 NH.sub.2 Ph CH.sub.2 SCH.sub.3 H OH, OH3503 CH.sub.2 NH.sub.2 Ph CH.sub.2 SOCH.sub.3 H OH, OH3504 CH.sub.2 NH.sub.2 Ph CH.sub.2 SO.sub.2 CH.sub.3 H OH, OH3505 CH.sub.2 NH.sub.2 Ph CH.sub.2 OH H OH, OH3506 CH.sub.2 NH.sub.2 Ph CH.sub.2 COOH H OH, OH3507 CH.sub.2 NH.sub.2 Ph (CH.sub.2).sub.2 COOH H OH, OH3508 CH.sub.2 NH.sub.2 Ph (CH.sub.2).sub.2 CN H OH, OH3509 CH.sub.2 NH.sub.2 Ph CHCHCOOMe H OH, OH3510 CH.sub.2 NH.sub.2 Ph CHCHCOOH H OH, OH3511 CH.sub.2 NH.sub.2 Ph CH.sub.2 CN.sub.4 H H OH, OH3512 CH.sub.2 NH.sub.2 Ph CH.sub.2 NHSO.sub.2 CF.sub.3 H OH, OH3513 CH.sub.2 NH.sub.2 Ph CH.sub.2 CH.sub.2 CN H OH, OH3514 CH.sub.2 NH.sub.2 Ph CH.sub.2 CH.sub.2 NC H OH, OH3515 CH.sub.2 NH.sub.2 Ph CH.sub.2 CH.sub.2 NO.sub.2 H OH, OH3516 CH.sub.2 NH.sub.2 Ph CH.sub.2 CH.sub.2 SCH.sub.3 H OH, OH3517 CH.sub.2 NH.sub.2 Ph CH.sub.2 CH.sub.2 SOCH.sub.3 H OH, OH3518 CH.sub.2 NH.sub.2 Ph CH.sub.2 CH.sub.2 SO.sub.2 CH.sub.3 H OH, OH3519 CH.sub.2 NH.sub.2 Ph CH.sub.2 CH.sub.2 OH H OH, OH3520 CH.sub.2 NH.sub.2 Ph CH.sub.2 CH.sub.2 COOH H OH, OH3521 CH.sub.2 NH.sub.2 Ph CH.sub.2 CH.sub.2 CN.sub.4 H H OH, OH3522 CH.sub.2 NH.sub.2 Ph CH.sub.2 CH.sub.2 NHSO.sub.2 CF.sub.3 H OH, OH3523 CH.sub.2 NH.sub.2 PhCH.sub.2 H H (+)-pin3524 CH.sub.2 NH.sub.2 PhO methyl H (+)-pin3525 CH.sub.2 NH.sub.2 PhS methyl methyl (+)-pin3526 CH.sub.2 NH.sub.2 PhNH ethyl H (+)-pin3527 CH.sub.2 NH.sub.2 PhCONH ethyl methyl (+)-pin3528 CH.sub.2 NH.sub.2 PhNHCO ethyl ethyl (+)-pin3529 CH.sub.2 NH.sub.2 Ph isopropyl H (+)-pin3530 CH.sub.2 NH.sub.2 PhCH.sub.2 phenyl H (+)-pin3531 CH.sub.2 NH.sub.2 PhO CH.sub.2 CN H (+)-pin3532 CH.sub.2 NH.sub.2 PhS CH.sub.2 NC H (+)-pin3533 CH.sub.2 NH.sub.2 PhNH CH.sub.2 NO.sub.2 H (+)-pin3534 CH.sub.2 NH.sub.2 PhCONH CH.sub.2 SCH.sub.3 H (+)-pin3535 CH.sub.2 NH.sub.2 PhNHCO CH.sub.2 SOCH.sub.3 H (+)-pin3536 CH.sub.2 NH.sub.2 Ph(CH.sub.2).sub.2 CH.sub.2 SO.sub.2 CH.sub.3 H (+)-pin3537 NH(CNH)NH.sub.2 Ph H H (+)-pin3538 NH(CNH)NH.sub.2 Ph methyl H (+)-pin BM3539 NH(CNH)NH.sub.2 Ph methyl H (+)-pin3540 NH(CNH)NH.sub.2 Ph methyl methyl (+)-pin3541 NH(CNH)NH.sub.2 Ph ethyl H (+)-pin3542 NH(CNH)NH.sub.2 Ph ethyl methyl (+)-pin3543 NH(CNH)NH.sub.2 Ph ethyl ethyl (+)-pin3544 NH(CNH)NH.sub.2 Ph isopropyl H (+)-pin3545 NH(CNH)NH.sub.2 Ph phenyl H (+)-pin3546 NH(CNH)NH.sub.2 Ph CH.sub.2 CN H (+)-pin3547 NH(CNH)NH.sub.2 Ph CH.sub.2 NC H (+)-pin3548 NH(CNH)NH.sub.2 Ph CH.sub.2 NO.sub.2 H (+)-pin3549 NH(CNH)NH.sub.2 Ph CH.sub.2 SCH.sub.3 H (+)-pin3550 NH(CNH)NH.sub.2 Ph CH.sub.2 SOCH.sub.3 H (+)-pin3551 NH(CNH)NH.sub.2 Ph CH.sub.2 SO.sub.2 CH.sub.3 H (+)-pin3552 NH(CNH)NH.sub.2 Ph CH.sub.2 OH H (+)-pin3553 NH(CNH)NH.sub.2 Ph CH.sub.2 COOH H (+)-pin3554 NH(CNH)NH.sub.2 Ph (CH.sub.2).sub.2 COOH H (+)-pin3555 NH(CNH)NH.sub.2 Ph (CH.sub.2).sub.2 CN H (+)-pin3556 NH(CNH)NH.sub.2 Ph CHCHCOOMe H (+)-pin3557 NH(CNH)NH.sub.2 Ph CHCHCOOH H (+)-pin3558 NH(CNH)NH.sub.2 Ph CH.sub.2 CN.sub.4 H H (+)-pin3559 NH(CNH)NH.sub.2 Ph CH.sub.2 NHSO.sub.2 CF.sub.3 H (+)-pin3560 NH(CNH)NH.sub.2 Ph CH.sub.2 CH.sub.2 CN H (+)-pin3561 NH(CNH)NH.sub.2 Ph CH.sub.2 CH.sub.2 NC H (+)-pin3562 NH(CNH)NH.sub.2 Ph CH.sub.2 CH.sub.2 NO.sub.2 H (+)-pin3563 NH(CNH)NH.sub.2 Ph CH.sub.2 CH.sub.2 SCH.sub.3 H (+)-pin3564 NH(CNH)NH.sub.2 Ph CH.sub.2 CH.sub.2 SOCH.sub.3 H (+)-pin3565 NH(CNH)NH.sub.2 Ph CH.sub.2 CH.sub.2 SO.sub.2 CH.sub.3 H (+)-pin3566 NH(CNH)NH.sub.2 Ph CH.sub.2 CH.sub.2 OH H (+)-pin3567 NH(CNH)NH.sub.2 Ph NO.sub.2 H (+)-pin3568 NH(CNH)NH.sub.2 Ph F H (+)-pin3569 NH(CNH)NH.sub.2 Ph OH H (+)-pin3570 NH(CNH)NH.sub.2 Ph H H OH, OH3571 NH(CNH)NH.sub.2 Ph methyl H OH, OH3572 NH(CNH)NH.sub.2 Ph methyl methyl OH, OH3573 NH(CNH)NH.sub.2 Ph ethyl H OH, OH3574 NH(CNH)NH.sub.2 Ph ethyl methyl OH, OH3575 NH(CNH)NH.sub.2 Ph ethyl ethyl OH, OH3576 NH(CNH)NH.sub.2 Ph isopropyl H OH, OH3577 NH(CNH)NH.sub.2 Ph phenyl H OH, OH3578 NH(CNH)NH.sub.2 Ph CH.sub.2 CN H OH, OH3579 NH(CNH)NH.sub.2 Ph CH.sub.2 NC H OH, OH3580 NH(CNH)NH.sub.2 Ph CH.sub.2 NO.sub.2 H OH, OH3581 NH(CNH)NH.sub.2 Ph CH.sub.2 SCH.sub.3 H OH, OH3582 NH(CNH)NH.sub.2 Ph CH.sub.2 SOCH.sub.3 H OH, OH3583 NH(CNH)NH.sub.2 Ph CH.sub.2 SO.sub.2 CH.sub.3 H OH, OH3584 NH(CNH)NH.sub.2 Ph CH.sub.2 OH H OH, OH3585 NH(CNH)NH.sub.2 Ph CH.sub.2 COOH H OH, OH3586 NH(CNH)NH.sub.2 Ph (CH.sub.2).sub.2 COOH H OH, OH3587 NH(CNH)NH.sub.2 Ph (CH.sub.2).sub.2 CN H OH, OH3588 NH(CNH)NH.sub.2 Ph CHCHCOOMe H OH, OH3589 NH(CNH)NH.sub.2 Ph CHCHCOOH H OH, OH3590 NH(CNH)NH.sub.2 Ph CH.sub.2 CN.sub.4 H H OH, OH3591 NH(CNH)NH.sub.2 Ph CH.sub.2 NHSO.sub.2 CF.sub.3 H OH, OH3592 NH(CNH)NH.sub.2 Ph CH.sub.2 CH.sub.2 CN H OH, OH3593 NH(CNH)NH.sub.2 Ph CH.sub.2 CH.sub.2 NC H OH, OH3594 NH(CNH)NH.sub.2 Ph CH.sub.2 CH.sub.2 NO.sub.2 H OH, OH3595 NH(CNH)NH.sub.2 Ph CH.sub.2 CH.sub.2 SCH.sub.3 H OH, OH3596 NH(CNH)NH.sub.2 Ph CH.sub.2 CH.sub.2 SOCH.sub.3 H OH, OH3597 NH(CNH)NH.sub.2 Ph CH.sub.2 CH.sub.2 SO.sub.2 CH.sub.3 H OH, OH3598 NH(CNH)NH.sub.2 Ph CH.sub.2 CH.sub.2 OH H OH, OH3599 NH(CNH)NH.sub.2 Ph CH.sub.2 CH.sub.2 COOH H OH, OH3600 NH(CNH)NH.sub.2 Ph CH.sub.2 CH.sub.2 CN.sub.4 H H OH, OH3601 NH(CNH)NH.sub.2 Ph CH.sub.2 CH.sub.2 NHSO.sub.2 CF.sub.3 H OH, OH3602 NH(CNH)NH.sub.2 PhCH.sub.2 H H (+)-pin3603 NH(CNH)NH.sub.2 PhO methyl H (+)-pin3604 NH(CNH)NH.sub.2 PhS methyl methyl (+)-pin3605 NH(CNH)NH.sub.2 PhNH ethyl H (+)-pin3606 NH(CNH)NH.sub.2 PhCONH ethyl methyl (+)-pin3607 NH(CNH)NH.sub.2 PhNHCO ethyl ethyl (+)-pin3608 NH(CNH)NH.sub.2 Ph isopropyl H (+)-pin3609 NH(CNH)NH.sub.2 PhCH.sub.2 phenyl H (+)-pin3610 NH(CNH)NH.sub.2 PhO CH.sub.2 CN H (+)-pin3611 NH(CNH)NH.sub.2 PhS CH.sub.2 NC H (+)-pin3612 NH(CNH)NH.sub.2 PhNH CH.sub.2 NO.sub.2 H (+)-pin3613 NH(CNH)NH.sub.2 PhCONH CH.sub.2 SCH.sub.3 H (+)-pin3614 NH(CNH)NH.sub.2 PhNHCO CH.sub.2 SOCH.sub.3 H (+)-pin3615 NH(CNH)NH.sub.2 Ph(CH.sub.2).sub.2 CH.sub.2 SO.sub.2 CH.sub.3 H (+)-pin3616 OMe Ph CH.sub.3 H (+)-pin3617 NH(CNH)H Ph CH.sub.3 H (+)-pin3618 OMe Ph CH.sub.3 H OH, OH3619 NH(CNH)H Ph CH.sub.3 H OH, OH__________________________________________________________________________ BK. MS (M=H).sup.+ : Calc. 477, Found 477. BL. MS (M=H).sup.+ : Calc. 539, Found 539. BM. MS (M=H).sup.+ : Calc. 505, Found 505. TABLE 18__________________________________________________________________________ ##STR113## Phys.Ex X R.sup.13 R.sup.14 R.sup.15 Y.sup.1 Y.sup.2 Data__________________________________________________________________________3624 CH.sub.2 NH.sub.2 Ph H H (+)-pin3625 CH.sub.2 NH.sub.2 Ph methyl H (+)-pin3626 CH.sub.2 NH.sub.2 Ph ethyl H (+)-pin3627 CH.sub.2 NH.sub.2 Ph ethyl methyl (+)-pin3628 CH.sub.2 NH.sub.2 Ph ethyl ethyl (+)-pin3629 CH.sub.2 NH.sub.2 Ph isopropyl H (+)-pin3630 CH.sub.2 NH.sub.2 Ph phenyl H (+)-pin3631 CH.sub.2 NH.sub.2 Ph CH.sub.2 CN H (+)-pin3632 CH.sub.2 NH.sub.2 Ph CH.sub.2 NC H (+)-pin3633 CH.sub.2 NH.sub.2 Ph CH.sub.2 NO.sub.2 H (+)-pin3634 CH.sub.2 NH.sub.2 Ph CH.sub.2 SCH.sub.3 H (+)-pin3635 CH.sub.2 NH.sub.2 Ph CH.sub.2 SOCH.sub.3 H (+)-pin3636 CH.sub.2 NH.sub.2 Ph CH.sub.2 SO.sub.2 CH.sub.3 H (+)-pin3637 CH.sub.2 NH.sub.2 Ph CH.sub.2 OH H (+)-pin3638 CH.sub.2 NH.sub.2 Ph CH.sub.2 COOH H (+)-pin3639 CH.sub.2 NH.sub.2 Ph CH.sub.2 CN.sub.4 H H (+)-pin3640 CH.sub.2 NH.sub.2 Ph CH.sub.2 NHSO.sub.2 CF.sub.3 H (+)-pin3641 CH.sub.2 NH.sub.2 Ph CH.sub.2 CH.sub.2 CN H (+)-pin3642 CH.sub.2 NH.sub.2 Ph CH.sub.2 CH.sub.2 NC H (+)-pin3643 CH.sub.2 NH.sub.2 Ph CH.sub.2 CH.sub.2 NO.sub.2 H (+)-pin3644 CH.sub.2 NH.sub.2 Ph CH.sub.2 CH.sub.2 SCH.sub.3 H (+)-pin3645 CH.sub.2 NH.sub.2 Ph CH.sub.2 CH.sub.2 SOCH.sub.3 H (+)-pin3646 CH.sub.2 NH.sub.2 Ph CH.sub.2 CH.sub.2 SO.sub.2 CH.sub.3 H (+)-pin3647 CH.sub.2 NH.sub.2 Ph CH.sub.2 CH.sub.2 CH.sub.2 OH H (+)-pin3648 CH.sub.2 NH.sub.2 Ph NO.sub.2 H (+)-pin3649 CH.sub.2 NH.sub.2 Ph F H (+)-pin3650 CH.sub.2 NH.sub.2 Ph OH H (+)-pin3651 CH.sub.2 NH.sub.2 Ph H H OH, OH3652 CH.sub.2 NH.sub.2 Ph methyl H OH, OH3653 CH.sub.2 NH.sub.2 Ph methyl methyl OH, OH3654 CH.sub.2 NH.sub.2 Ph ethyl H OH, OH3655 CH.sub.2 NH.sub.2 Ph ethyl methyl OH, OH3656 CH.sub.2 NH.sub.2 Ph ethyl ethyl OH, OH3657 CH.sub.2 NH.sub.2 Ph isopropyl H OH, OH3658 CH.sub.2 NH.sub.2 Ph phenyl H OH, OH3659 CH.sub.2 NH.sub.2 Ph CH.sub.2 CN H OH, OH3660 CH.sub.2 NH.sub.2 Ph CH.sub.2 NC H OH, OH3661 CH.sub.2 NH.sub.2 Ph CH.sub.2 NO.sub.2 H OH, OH3662 CH.sub.2 NH.sub.2 Ph CH.sub.2 SCH.sub.3 H OH, OH3663 CH.sub.2 NH.sub.2 Ph CH.sub.2 SOCH.sub.3 H OH, OH3664 CH.sub.2 NH.sub.2 Ph CH.sub.2 SO.sub.2 CH.sub.3 H OH, OH3665 CH.sub.2 NH.sub.2 Ph CH.sub.2 OH H OH, OH3666 CH.sub.2 NH.sub.2 Ph CH.sub.2 COOH H OH, OH3667 CH.sub.2 NH.sub.2 Ph CH.sub.2 CN.sub.4 H H OH, OH3668 CH.sub.2 NH.sub.2 Ph CH.sub.2 NHSO.sub.2 CF.sub.3 H OH, OH3669 CH.sub.2 NH.sub.2 Ph CH.sub.2 CH.sub.2 CN H OH, OH3670 CH.sub.2 NH.sub.2 Ph CH.sub.2 CH.sub.2 NC H OH, OH3671 CH.sub.2 NH.sub.2 Ph CH.sub.2 CH.sub.2 NO.sub.2 H OH, OH3672 CH.sub.2 NH.sub.2 Ph CH.sub.2 CH.sub.2 SCH.sub.3 H OH, OH3673 CH.sub.2 NH.sub.2 Ph CH.sub.2 CH.sub.2 SOCH.sub.3 H OH, OH3674 CH.sub.2 NH.sub.2 Ph CH.sub.2 CH.sub.2 SO.sub.2 CH.sub.3 H OH, OH3675 CH.sub.2 NH.sub.2 Ph CH.sub.2 CH.sub.2 OH H OH, OH3676 CH.sub.2 NH.sub.2 Ph CH.sub.2 CH.sub.2 COOH H OH, OH3677 CH.sub.2 NH.sub.2 Ph CH.sub.2 CH.sub.2 CN.sub.4 H H OH, OH3678 CH.sub.2 NH.sub.2 Ph CH.sub.2 CH.sub.2 NHSO.sub.2 CF.sub.3 H OH, OH3679 CH.sub.2 NH.sub.2 PhCH.sub.2 H H (+)-pin3680 CH.sub.2 NH.sub.2 PhO methyl H (+)-pin3681 CH.sub.2 NH.sub.2 PhS methyl methyl (+)-pin3682 CH.sub.2 NH.sub.2 PhNH ethyl H (+)-pin3683 CH.sub.2 NH.sub.2 PhCONH ethyl methyl (+)-pin3684 CH.sub.2 NH.sub.2 PhNHCO ethyl ethyl (+)-pin3685 CH.sub.2 NH.sub.2 Ph isopropyl H (+)-pin3686 CH.sub.2 NH.sub.2 PhCH.sub.2 phenyl H (+)-pin3687 CH.sub.2 NH.sub.2 PhO CH.sub.2 CN H (+)-pin3688 CH.sub.2 NH.sub.2 PhS CH.sub.2 NC H (+)-pin3689 CH.sub.2 NH.sub.2 PhNH CH.sub.2 NO.sub.2 H (+)-pin3690 CH.sub.2 NH.sub.2 PhCONH CH.sub.2 SCH.sub.3 H (+)-pin3691 CH.sub.2 NH.sub.2 PhNHCO CH.sub.2 SOCH.sub.3 H (+)-pin3692 CH.sub.2 NH.sub.2 Ph(CH.sub.2).sub.2 CH.sub.2 SO.sub.2 CH.sub.3 H (+)-pin3693 NH(CNH)NH.sub.2 Ph H H (+)-pin3694 NH(CNH)NH.sub.2 Ph methyl methyl (+)-pin3695 NH(CNH)NH.sub.2 Ph ethyl H (+)-pin3696 NH(CNH)NH.sub.2 Ph ethyl methyl (+)-pin3697 NH(CNH)NH.sub.2 Ph ethyl ethyl (+)-pin3698 NH(CNH)NH.sub.2 Ph isopropyl H (+)-pin3699 NH(CNH)NH.sub.2 Ph phenyl H (+)-pin3700 NH(CNH)NH.sub.2 Ph CH.sub.2 CN H (+)-pin3701 NH(CNH)NH.sub.2 Ph CH.sub.2 NC H (+)-pin3702 NH(CNH)NH.sub.2 Ph CH.sub.2 NO.sub.2 H (+)-pin3703 NH(CNH)NH.sub.2 Ph CH.sub.2 SCH.sub.3 H (+)-pin3704 NH(CNH)NH.sub.2 Ph CH.sub.2 SOCH.sub.3 H (+)-pin3705 NH(CNH)NH.sub.2 Ph CH.sub.2 SO.sub.2 CH.sub.3 H (+)-pin3706 NH(CNH)NH.sub.2 Ph CH.sub.2 OH H (+)-pin3707 NH(CNH)NH.sub.2 Ph CH.sub.2 COOH H (+)-pin3708 NH(CNH)NH.sub.2 Ph CH.sub.2 CN.sub.4 H H (+)-pin3709 NH(CNH)NH.sub.2 Ph CH.sub.2 NHSO.sub.2 CF.sub.3 H (+)-pin3710 NH(CNH)NH.sub.2 Ph CH.sub.2 CH.sub.2 CN H (+)-pin3711 NH(CNH)NH.sub.2 Ph CH.sub.2 CH.sub.2 NC H (+)-pin3712 NH(CNH)NH.sub.2 Ph CH.sub.2 CH.sub.2 NO.sub.2 H (+)-pin3713 NH(CNH)NH.sub.2 Ph CH.sub.2 CH.sub.2 SCH.sub.3 H (+)-pin3714 NH(CNH)NH.sub.2 Ph CH.sub.2 CH.sub.2 SOCH.sub.3 H (+)-pin3715 NH(CNH)NH.sub.2 Ph CH.sub.2 CH.sub.2 SO.sub.2 CH.sub.3 H (+)-pin3716 NH(CNH)NH.sub.2 Ph CH.sub.2 CH.sub.2 OH H (+)-pin3717 NH(CNH)NH.sub.2 Ph NO.sub.2 H (+)-pin3718 NH(CNH)NH.sub.2 Ph F H (+)-pin3719 NH(CNH)NH.sub.2 Ph OH H (+)-pin3720 NH(CNH)NH.sub.2 Ph H H OH, OH3721 NH(CNH)NH.sub.2 Ph methyl H OH, OH3722 NH(CNH)NH.sub.2 Ph methyl methyl OH, OH3723 NH(CNH)NH.sub.2 Ph ethyl H OH, OH3724 NH(CNH)NH.sub.2 Ph ethyl methyl OH, OH3725 NH(CNH)NH.sub.2 Ph ethyl ethyl OH, OH3726 NH(CNH)NH.sub.2 Ph isopropyl H OH, OH3727 NH(CNH)NH.sub.2 Ph phenyl H OH, OH3728 NH(CNH)NH.sub.2 Ph CH.sub.2 CN H OH, OH3729 NH(CNH)NH.sub.2 Ph CH.sub.2 NC H OH, OH3730 NH(CNH)NH.sub.2 Ph CH.sub.2 NO.sub.2 H OH, OH3731 NH(CNH)NH.sub.2 Ph CH.sub.2 SCH.sub.3 H OH, OH3732 NH(CNH)NH.sub.2 Ph CH.sub.2 SOCH.sub.3 H OH, OH3733 NH(CNH)NH.sub.2 Ph CH.sub.2 SO.sub.2 CH.sub.3 H OH, OH3734 NH(CNH)NH.sub.2 Ph CH.sub.2 OH H OH, OH3735 NH(CNH)NH.sub.2 Ph CH.sub.2 COOH H OH, OH3736 NH(CNH)NH.sub.2 Ph CH.sub.2 CN.sub.4 H H OH, OH3737 NH(CNH)NH.sub.2 Ph CH.sub.2 NHSO.sub.2 CF.sub.3 H OH, OH3738 NH(CNH)NH.sub.2 Ph CH.sub.2 CH.sub.2 CN H OH, OH3739 NH(CNH)NH.sub.2 Ph CH.sub.2 CH.sub.2 NC H OH, OH3740 NH(CNH)NH.sub.2 Ph CH.sub.2 CH.sub.2 NO.sub.2 H OH, OH3741 NH(CNH)NH.sub.2 Ph CH.sub.2 CH.sub.2 SCH.sub.3 H OH, OH3742 NH(CNH)NH.sub.2 Ph CH.sub.2 CH.sub.2 SOCH.sub.3 H OH, OH3743 NH(CNH)NH.sub.2 Ph CH.sub.2 CH.sub.2 SO.sub.2 CH.sub.3 H OH, OH3744 NH(CNH)NH.sub.2 Ph CH.sub.2 CH.sub.2 OH H OH, OH3745 NH(CNH)NH.sub.2 Ph CH.sub.2 CH.sub.2 COOH H OH, OH3746 NH(CNH)NH.sub.2 Ph CH.sub.2 CH.sub.2 CN.sub.4 H H OH, OH3747 NH(CNH)NH.sub.2 Ph CH.sub.2 CH.sub.2 NHSO.sub.2 CF.sub.3 H OH, OH3748 NH(CNH)NH.sub.2 PhCH.sub.2 H H (+)-pin3749 NH(CNH)NH.sub.2 PhO methyl H (+)-pin3750 NH(CNH)NH.sub.2 PhS methyl methyl (+)-pin3751 NH(CNH)NH.sub.2 PhNH ethyl H (+)-pin3752 NH(CNH)NH.sub.2 PhCONH ethyl methyl (+)-pin3753 NH(CNH)NH.sub.2 PhNHCO ethyl ethyl (+)-pin3754 NH(CNH)NH.sub.2 Ph isopropyl H (+)-pin3755 NH(CNH)NH.sub.2 PhCH.sub.2 phenyl H (+)-pin3756 NH(CNH)NH.sub.2 PhO CH.sub.2 CN H (+)-pin3757 NH(CNH)NH.sub.2 PhS CH.sub.2 NC H (+)-pin3758 NH(CNH)NH.sub.2 PhNH CH.sub.2 NO.sub.2 H (+)-pin3759 NH(CNH)NH.sub.2 PhCONH CH.sub.2 SCH.sub.3 H (+)-pin3760 NH(CNH)NH.sub.2 PhNHCO CH.sub.2 SOCH.sub.3 H (+)-pin3761 NH(CNH)NH.sub.2 Ph(CH.sub.2).sub.2 CH.sub.2 SO.sub.2 CH.sub.3 H (+)-pin3762 OMe Ph CH.sub.3 H (+)-pin3763 NH(CNH)H Ph CH.sub.3 H (+)-pin3764 OMe Ph CH.sub.3 H OH, OH3765 NH(CNH)H Ph CH.sub.3 H OH, OH__________________________________________________________________________ TABLE 19______________________________________ ##STR114## Phys.Ex X R.sup.13 R.sup.14 R.sup.15 Y.sup.1 Y.sup.2 Data______________________________________3770 CH.sub.2 NH.sub.2 Ph H H (+)-pin3771 CH.sub.2 NH.sub.2 Ph methyl H (+)-pin3772 CH.sub.2 NH.sub.2 Ph H H OH, OH3773 CH.sub.2 NH.sub.2 Ph methyl H OH, OH3774 NH(CNH)NH.sub.2 Ph H H (+)-pin3775 NH(CNH)NH.sub.2 Ph methyl H (+)-pin3776 NH(CNH)NH.sub.2 Ph H H OH, OH3777 NH(CNH)NH.sub.2 Ph methyl H OH, OH3778 OMe Ph CH.sub.3 H (+)-pin3779 NH(CNH)H Ph CH.sub.3 H (+)-pin3780 OMe Ph CH.sub.3 H OH, OH3781 NH(CNH)H Ph CH.sub.3 H OH, OH______________________________________ TABLE 20__________________________________________________________________________ ##STR115## Phys.Ex X R.sup.13 R.sup.14 R.sup.15 Y.sup.1 Y.sup.2 Data__________________________________________________________________________3786 CH.sub.2 NH.sub.2 Ph H H (+)-pin3787 CH.sub.2 NH.sub.2 Ph methyl methyl (+)-pin3788 CH.sub.2 NH.sub.2 Ph ethyl H (+)-pin3789 CH.sub.2 NH.sub.2 Ph ethyl methyl (+)-pin3790 CH.sub.2 NH.sub.2 Ph ethyl ethyl (+)-pin3791 CH.sub.2 NH.sub.2 Ph isopropyl H (+)-pin3792 CH.sub.2 NH.sub.2 Ph phenyl H (+)-pin3793 CH.sub.2 NH.sub.2 Ph CH.sub.2 CN H (+)-pin3794 CH.sub.2 NH.sub.2 Ph CH.sub.2 NC H (+)-pin3795 CH.sub.2 NH.sub.2 Ph CH.sub.2 NO.sub.2 H (+)-pin3796 CH.sub.2 NH.sub.2 Ph CH.sub.2 SCH.sub.3 H (+)-pin3797 CH.sub.2 NH.sub.2 Ph CH.sub.2 SOCH.sub.3 H (+)-pin3798 CH.sub.2 NH.sub.2 Ph CH.sub.2 SO.sub.2 CH.sub.3 H (+)-pin3799 CH.sub.2 NH.sub.2 Ph CH.sub.2 OH H (+)-pin3800 CH.sub.2 NH.sub.2 Ph CH.sub.2 COOH H (+)-pin3801 CH.sub.2 NH.sub.2 Ph CH.sub.2 CN.sub.4 H H (+)-pin3802 CH.sub.2 NH.sub.2 Ph CH.sub.2 NHSO.sub.2 CF.sub.3 H (+)-pin3803 CH.sub.2 NH.sub.2 Ph CH.sub.2 CH.sub.2 CN H (+)-pin3804 CH.sub.2 NH.sub.2 Ph CH.sub.2 CH.sub.2 NC H (+)-pin3805 CH.sub.2 NH.sub.2 Ph CH.sub.2 CH.sub.2 NO.sub.2 H (+)-pin3806 CH.sub.2 NH.sub.2 Ph CH.sub.2 CH.sub.2 SCH.sub.3 H (+)-pin3807 CH.sub.2 NH.sub.2 Ph CH.sub.2 CH.sub.2 SOCH.sub.3 H (+)-pin3808 CH.sub.2 NH.sub.2 Ph CH.sub.2 CH.sub.2 SO.sub.2 CH.sub.3 H (+)-pin3809 CH.sub.2 NH.sub.2 Ph CH.sub.2 CH.sub.2 OH H (+)-pin3810 CH.sub.2 NH.sub.2 Ph NO.sub.2 H (+)-pin3811 CH.sub.2 NH.sub.2 Ph F H (+)-pin3812 CH.sub.2 NH.sub.2 Ph OH H (+)-pin3813 CH.sub.2 NH.sub.2 Ph H H OH, OH3814 CH.sub.2 NH.sub.2 Ph methyl H OH, OH3815 CH.sub.2 NH.sub.2 Ph methyl methyl OH, OH3816 CH.sub.2 NH.sub.2 Ph ethyl H OH, OH3817 CH.sub.2 NH.sub.2 Ph ethyl methyl OH, OH3818 CH.sub.2 NH.sub.2 Ph ethyl ethyl OH, OH3819 CH.sub.2 NH.sub.2 Ph isopropyl H OH, OH3820 CH.sub.2 NH.sub.2 Ph phenyl H OH, OH3821 CH.sub.2 NH.sub.2 Ph CH.sub.2 CN H OH, OH3822 CH.sub.2 NH.sub.2 Ph CH.sub.2 NC H OH, OH3823 CH.sub.2 NH.sub.2 Ph CH.sub.2 NO.sub.2 H OH, OH3824 CH.sub.2 NH.sub.2 Ph CH.sub.2 SCH.sub.3 H OH, OH3825 CH.sub.2 NH.sub.2 Ph CH.sub.2 SOCH.sub.3 H OH, OH3826 CH.sub.2 NH.sub.2 Ph CH.sub.2 SO.sub.2 CH.sub.3 H OH, OH3827 CH.sub.2 NH.sub.2 Ph CH.sub.2 OH H OH, OH3828 CH.sub.2 NH.sub.2 Ph CH.sub.2 COOH H OH, OH3829 CH.sub.2 NH.sub.2 Ph CH.sub.2 CN.sub.4 H H OH, OH3830 CH.sub.2 NH.sub.2 Ph CH.sub.2 NHSO.sub.2 CF.sub.3 H OH, OH3831 CH.sub.2 NH.sub.2 Ph CH.sub.2 CH.sub.2 CN H OH, OH3832 CH.sub.2 NH.sub.2 Ph CH.sub.2 CH.sub.2 NC H OH, OH3833 CH.sub.2 NH.sub.2 Ph CH.sub.2 CH.sub.2 NO.sub.2 H OH, OH3834 CH.sub.2 NH.sub.2 Ph CH.sub.2 CH.sub.2 SCH.sub.3 H OH, OH3835 CH.sub.2 NH.sub.2 Ph CH.sub.2 CH.sub.2 SOCH.sub.3 H OH, OH3836 CH.sub.2 NH.sub.2 Ph CH.sub.2 CH.sub.2 SO.sub.2 CH.sub.3 H OH, OH3837 CH.sub.2 NH.sub.2 Ph CH.sub.2 CH.sub.2 OH H OH, OH3838 CH.sub.2 NH.sub.2 Ph CH.sub.2 CH.sub.2 COOH H OH, OH3839 CH.sub.2 NH.sub.2 Ph CH.sub.2 CH.sub.2 CN.sub.4 H H OH, OH3840 CH.sub.2 NH.sub.2 Ph CH.sub.2 CH.sub.2 NHSO.sub.2 CF.sub.3 H OH, OH3841 CH.sub.2 NH.sub.2 PhCH.sub.2 H H (+)-pin3842 CH.sub.2 NH.sub.2 PhO methyl H (+)-pin3843 CH.sub.2 NH.sub.2 PhS methyl methyl (+)-pin3844 CH.sub.2 NH.sub.2 PhNH ethyl H (+)-pin3845 CH.sub.2 NH.sub.2 PhCONH ethyl methyl (+)-pin3846 CH.sub.2 NH.sub.2 PhNHCO ethyl ethyl (+)-pin3847 CH.sub.2 NH.sub.2 Ph isopropyl H (+)-pin3848 CH.sub.2 NH.sub.2 PhCH.sub.2 phenyl H (+)-pin3849 CH.sub.2 NH.sub.2 PhO CH.sub.2 CN H (+)-pin3850 CH.sub.2 NH.sub.2 PhS CH.sub.2 NC H (+)-pin3851 CH.sub.2 NH.sub.2 PhNH CH.sub.2 NO.sub.2 H (+)-pin3852 CH.sub.2 NH.sub.2 PhCONH CH.sub.2 SCH.sub.3 H (+)-pin3853 CH.sub.2 NH.sub.2 PhNHCO CH.sub.2 SOCH.sub.3 H (+)-pin3854 CH.sub.2 NH.sub.2 Ph(CH.sub.2).sub.2 CH.sub.2 SO.sub.2 CH.sub.3 H (+)-pin3855 NH(CNH)NH.sub.2 Ph H H (+)-pin3856 NH(CNH)NH.sub.2 Ph methyl methyl (+)-pin3857 NH(CNH)NH.sub.2 Ph ethyl H (+)-pin3858 NH(CNH)NH.sub.2 Ph ethyl methyl (+)-pin3859 NH(CNH)NH.sub.2 Ph ethyl ethyl (+)-pin3860 NH(CNH)NH.sub.2 Ph isopropyl H (+)-pin3861 NH(CNH)NH.sub.2 Ph phenyl H (+)-pin3862 NH(CNH)NH.sub.2 Ph CH.sub.2 CN H (+)-pin3863 NH(CNH)NH.sub.2 Ph CH.sub.2 NC H (+)-pin3864 NH(CNH)NH.sub.2 Ph CH.sub.2 NO.sub.2 H (+)-pin3865 NH(CNH)NH.sub.2 Ph CH.sub.2 SCH.sub.3 H (+)-pin3866 NH(CNH)NH.sub.2 Ph CH.sub.2 SOCH.sub.3 H (+)-pin3867 NH(CNH)NH.sub.2 Ph CH.sub.2 SO.sub.2 CH.sub.3 H (+)-pin3868 NH(CNH)NH.sub.2 Ph CH.sub.2 OH H (+)-pin3869 NH(CNH)NH.sub.2 Ph CH.sub.2 COOH H (+)-pin3870 NH(CNH)NH.sub.2 Ph CH.sub.2 CN.sub.4 H H (+)-pin3871 NH(CNH)NH.sub.2 Ph CH.sub.2 NHSO.sub.2 CF.sub.3 H (+)-pin3872 NH(CNH)NH.sub.2 Ph CH.sub.2 CH.sub.2 CN H (+)-pin3873 NH(CNH)NH.sub.2 Ph CH.sub.2 CH.sub.2 NC H (+)-pin3874 NH(CNH)NH.sub.2 Ph CH.sub.2 CH.sub.2 NO.sub.2 H (+)-pin3875 NH(CNH)NH.sub.2 Ph CH.sub.2 CH.sub.2 SCH.sub.3 H (+)-pin3876 NH(CNH)NH.sub.2 Ph CH.sub.2 CH.sub.2 SOCH.sub.3 H (+)-pin3877 NH(CNH)NH.sub.2 Ph CH.sub.2 CH.sub.2 SO.sub.2 CH.sub.3 H (+)-pin3878 NH(CNH)NH.sub.2 Ph CH.sub.2 CH.sub.2 OH H (+)-pin3879 NH(CNH)NH.sub.2 Ph NO.sub.2 H (+)-pin3880 NH(CNH)NH.sub.2 Ph F H (+)-pin3881 NH(CNH)NH.sub.2 Ph OH H (+)-pin3882 NH(CNH)NH.sub.2 Ph H H OH, OH3883 NH(CNH)NH.sub.2 Ph methyl H OH, OH3884 NH(CNH)NH.sub.2 Ph methyl methyl OH, OH3885 NH(CNH)NH.sub.2 Ph ethyl H OH, OH3886 NH(CNH)NH.sub.2 Ph ethyl methyl OH, OH3887 NH(CNH)NH.sub.2 Ph ethyl ethyl OH, OH3888 NH(CNH)NH.sub.2 Ph isopropyl H OH, OH3889 NH(CNH)NH.sub.2 Ph phenyl H OH, OH3890 NH(CNH)NH.sub.2 Ph CH.sub.2 CN H OH, OH3891 NH(CNH)NH.sub.2 Ph CH.sub.2 NC H OH, OH3892 NH(CNH)NH.sub.2 Ph CH.sub.2 NO.sub.2 H OH, OH3893 NH(CNH)NH.sub.2 Ph CH.sub.2 SCH.sub.3 H OH, OH3894 NH(CNH)NH.sub.2 Ph CH.sub.2 SOCH.sub.3 H OH, OH3895 NH(CNH)NH.sub.2 Ph CH.sub.2 SO.sub.2 CH.sub.3 H OH, OH3896 NH(CNH)NH.sub.2 Ph CH.sub.2 OH H OH, OH3897 NH(CNH)NH.sub.2 Ph CH.sub.2 COOH H OH, OH3898 NH(CNH)NH.sub.2 Ph CH.sub.2 CN.sub.4 H H OH, OH3899 NH(CNH)NH.sub.2 Ph CH.sub.2 NHSO.sub.2 CF.sub.3 H OH, OH3900 NH(CNH)NH.sub.2 Ph CH.sub.2 CH.sub.2 CN H OH, OH3901 NH(CNH)NH.sub.2 Ph CH.sub.2 CH.sub.2 NC H OH, OH3902 NH(CNH)NH.sub.2 Ph CH.sub.2 CH.sub.2 NO.sub.2 H OH, OH3903 NH(CNH)NH.sub.2 Ph CH.sub.2 CH.sub.2 SCH.sub.3 H OH, OH3904 NH(CNH)NH.sub.2 Ph CH.sub.2 CH.sub.2 SOCH.sub.3 H OH, OH3905 NH(CNH)NH.sub.2 Ph CH.sub.2 CH.sub.2 SO.sub.2 CH.sub.3 H OH, OH3906 NH(CNH)NH.sub.2 Ph CH.sub.2 CH.sub.2 OH H OH, OH3907 NH(CNH)NH.sub.2 Ph CH.sub.2 CH.sub.2 COOH H OH, OH3908 NH(CNH)NH.sub.2 Ph CH.sub.2 CH.sub.2 CN.sub.4 H H OH, OH3909 NH(CNH)NH.sub.2 Ph CH.sub.2 CH.sub.2 NHSO.sub.2 CF.sub.3 H OH, OH3910 NH(CNH)NH.sub.2 PhCH.sub.2 H H (+)-pin3911 NH(CNH)NH.sub.2 PhO methyl H (+)-pin3912 NH(CNH)NH.sub.2 PhS methyl methyl (+)-pin3913 NH(CNH)NH.sub.2 PhNH ethyl H (+)-pin3914 NH(CNH)NH.sub.2 PhCONH ethyl methyl (+)-pin3915 NH(CNH)NH.sub.2 PhNHCO ethyl ethyl (+)-pin3916 NH(CNH)NH.sub.2 Ph isopropyl H (+)-pin3917 NH(CNH)NH.sub.2 PhCH.sub.2 phenyl H (+)-pin3918 NH(CNH)NH.sub.2 PhO CH.sub.2 CN H (+)-pin3919 NH(CNH)NH.sub.2 PhS CH.sub.2 NC H (+)-pin3920 NH(CNH)NH.sub.2 PhNH CH.sub.2 NO.sub.2 H (+)-pin3921 NH(CNH)NH.sub.2 PhCONH CH.sub.2 SCH.sub.3 H (+)-pin3922 NH(CNH)NH.sub.2 PhNHCO CH.sub.2 SOCH.sub.3 H (+)-pin3923 NH(CNH)NH.sub.2 Ph(CH.sub.2).sub.2 CH.sub.2 SO.sub.2 CH.sub.3 H (+)-pin3924 OMe Ph CH.sub.3 H (+)-pin3925 NH(CNH)H Ph CH.sub.3 H (+)-pin3926 OMe Ph CH.sub.3 H OH, OH3927 NH(CNH)H Ph CH.sub.3 H OH, OH__________________________________________________________________________ TABLE 21______________________________________ ##STR116## Phys.Ex X R.sup.13 R.sup.14 R.sup.15 Y.sup.1 Y.sup.2 Data______________________________________3932 CH.sub.2 NH.sub.2 Ph H H (+)-pin3933 CH.sub.2 NH.sub.2 Ph methyl H (+)-pin3934 CH.sub.2 NH.sub.2 Ph H H OH, OH3935 CH.sub.2 NH.sub.2 Ph methyl H OH, OH3936 NH(CNH)NH.sub.2 Ph H H (+)-pin3937 NH(CNH)NH.sub.2 Ph methyl H (+)-pin3938 NH(CNH)NH.sub.2 Ph H H OH, OH3939 NH(CNH)NH.sub.2 Ph methyl H OH, OH3940 OMe Ph CH.sub.3 H (+)-pin3941 NH(CNH)H Ph CH.sub.3 H (+)-pin3942 OMe Ph CH.sub.3 H OH, OH3943 NH(CNH)H Ph CH.sub.3 H OH, OH______________________________________ TABLE 22______________________________________ ##STR117## Phys.Ex X R.sup.13 R.sup.14 R.sup.15 Y.sup.1 Y.sup.2 Data______________________________________3948 CH.sub.2 NH.sub.2 Ph H H (+)-pin3949 CH.sub.2 NH.sub.2 Ph methyl H (+)-pin3950 CH.sub.2 NH.sub.2 Ph H H OH, OH3951 CH.sub.2 NH.sub.2 Ph methyl H OH, OH3952 NH(CNH)NH.sub.2 Ph H H (+)-pin3953 NH(CNH)NH.sub.2 Ph methyl H (+)-pin3954 NH(CNH)NH.sub.2 Ph H H OH, OH3955 NH(CNH)NH.sub.2 Ph methyl H OH, OH3956 OMe Ph CH.sub.3 H (+)-pin3957 NH(CNH)H Ph CH.sub.3 H (+)-pin3958 OMe Ph CH.sub.3 H OH, OH3959 NH(CNH)H Ph CH.sub.3 H OH, OH______________________________________ TABLE 23______________________________________ ##STR118## Phys.Ex X R.sup.13 R.sup.14 R.sup.15 Y.sup.1 Y.sup.2 Data______________________________________3964 CH.sub.2 NH.sub.2 Ph H H (+)-pin3965 CH.sub.2 NH.sub.2 Ph methyl H (+)-pin3966 CH.sub.2 NH.sub.2 Ph H H OH, OH3967 CH.sub.2 NH.sub.2 Ph methyl H OH, OH3968 NH(CNH)NH.sub.2 Ph H H (+)-pin3969 NH(CNH)NH.sub.2 Ph methyl H (+)-pin3970 NH(CNH)NH.sub.2 Ph H H OH, OH3971 NH(CNH)NH.sub.2 Ph methyl H OH, OH3972 OMe Ph CH.sub.3 H (+)-pin3973 NH(CNH)H Ph CH.sub.3 H (+)-pin3974 OMe Ph CH.sub.3 H OH, OH3975 NH(CNH)H Ph CH.sub.3 H OH, OH______________________________________ TABLE 24______________________________________ ##STR119## Phys.Ex X R.sup.13 R.sup.14 R.sup.15 Y.sup.1 Y.sup.2 Data______________________________________3980 CH.sub.2 NH.sub.2 Ph H H (+)-pin3981 CH.sub.2 NH.sub.2 Ph methyl H (+)-pin3982 CH.sub.2 NH.sub.2 Ph H H OH, OH3983 CH.sub.2 NH.sub.2 Ph methyl H OH, OH3984 NH(CNH)NH.sub.2 Ph H H (+)-pin3985 NH(CNH)NH.sub.2 Ph methyl H (+)-pin3986 NH(CNH)NH.sub.2 Ph H H OH, OH3987 NH(CNH)NH.sub.2 Ph methyl H OH, OH3988 OMe Ph CH.sub.3 H (+)-pin3989 NH(CNH)H Ph CH.sub.3 H (+)-pin3990 OMe Ph CH.sub.3 H OH, OH3991 NH(CNH)H Ph CH.sub.3 H OH, OH______________________________________ TABLE 25______________________________________ ##STR120## Phys.Ex X R.sup.13 R.sup.14 R.sup.15 Y.sup.1 Y.sup.2 Data______________________________________3996 CH.sub.2 NH.sub.2 Ph H H (+)-pin3997 CH.sub.2 NH.sub.2 Ph methyl H (+)-pin3998 CH.sub.2 NH.sub.2 Ph H H OH, OH3999 CH.sub.2 NH.sub.2 Ph methyl H OH, OH4000 NH(CNH)NH.sub.2 Ph H H (+)-pin4001 NH(CNH)NH.sub.2 Ph methyl H (+)-pin4002 NH(CNH)NH.sub.2 Ph H H OH, OH4003 NH(CNH)NH.sub.2 Ph methyl H OH, OH4004 OMe Ph CH.sub.3 H (+)-pin4005 NH(CNH)H Ph CH.sub.3 H (+)-pin4006 OMe Ph CH.sub.3 H OH, OH4007 NH(CNH)H Ph CH.sub.3 H OH, OH______________________________________ TABLE 26______________________________________ ##STR121## Phys.Ex X R.sup.13 R.sup.14 R.sup.15 Y.sup.1 Y.sup.2 Data______________________________________4012 CH.sub.2 NH.sub.2 Ph H H (+)-pin4013 CH.sub.2 NH.sub.2 Ph methyl H (+)-pin4014 CH.sub.2 NH.sub.2 Ph H H OH, OH4015 CH.sub.2 NH.sub.2 Ph methyl H OH, OH4016 CH.sub.2 NH.sub.2 Ph H Ph (+)-pin4017 CH.sub.2 NH.sub.2 Ph H Ph OH, OH4018 NH(CNH)NH.sub.2 Ph H H (+)-pin4019 NH(CNH)NH.sub.2 Ph methyl H (+)-pin4020 NH(CNH)NH.sub.2 Ph H H OH, OH4021 NH(CNH)NH.sub.2 Ph methyl H OH, OH4022 NH(CNH)NH.sub.2 Ph H Ph (+)-pin4023 NH(CNH)NH.sub.2 Ph H Ph OH, OH4024 OMe Ph CH.sub.3 H (+)-pin4025 NH(CNH)H Ph CH.sub.3 H (+)-pin4026 OMe Ph CH.sub.3 H OH, OH4027 NH(CNH)H Ph CH.sub.3 H OH, OH______________________________________ TABLE 27__________________________________________________________________________ ##STR122##Ex X R.sup.13 R.sup.14 R.sup.15 R.sup.16 Y.sup.1 Y.sup.2 Phys. Data__________________________________________________________________________4032 CH.sub.2 NH.sub.2 Ph H H H (+)-pin4033 CH.sub.2 NH.sub.2 Ph methyl H H (+)-pin4034 CH.sub.2 NH.sub.2 Ph H H H OH, OH4035 CH.sub.2 NH.sub.2 Ph methyl H H OH, OH4036 NH(CNH)NH.sub.2 Ph H H H (+)-pin4037 NH(CNH)NH.sub.2 Ph methyl H H (+)-pin4038 NH(CNH)NH.sub.2 Ph H H H OH, OH4039 NH(CNH)NH.sub.2 Ph methyl H H OH, OH4040 NH(CNH)NH.sub.2 Ph H CH.sub.3 CH.sub.3 (+)-pin4041 NH(CNH)NH.sub.2 Ph H CH.sub.3 CH.sub.3 OH, OH4042 OMe Ph CH.sub.3 H H (+)-pin4043 NH(CNH)H Ph CH.sub.3 H H (+)-pin4044 OMe Ph CH.sub.3 H H OH, OH4045 NH(CNH)H Ph CH.sub.3 H H OH, OH__________________________________________________________________________ TABLE 28__________________________________________________________________________ ##STR123##Ex X R.sup.13 R.sup.14 R.sup.15 R.sup.16 Y.sup.1 Y.sup.2 Phys. Data__________________________________________________________________________4050 CH.sub.2 NH.sub.2 Ph CH.sub.2 CO.sub.2 H H H (+)-pin4051 CH.sub.2 NH.sub.2 Ph methyl H H (+)-pin4052 CH.sub.2 NH.sub.2 Ph CH.sub.2 CO.sub.2 H H H OH, OH4053 CH.sub.2 NH.sub.2 Ph methyl H H OH, OH4054 NH(CNH)NH.sub.2 Ph CH.sub.2 CN H H (+)-pin4055 NH(CNH)NH.sub.2 Ph methyl H H (+)-pin4056 NH(CNH)NH.sub.2 Ph CH.sub.2 CN H H OH, OH4057 NH(CNH)NH.sub.2 Ph methyl H H OH, OH4058 NH(CNH)NH.sub.2 Ph CH.sub.3 CH.sub.3 H (+)-pin4059 NH(CNH)NH.sub.2 Ph CH.sub.3 CH.sub.3 H OH, OH4060 OMe Ph CH.sub.3 H H (+)-pin4061 NH(CNH)H Ph CH.sub.3 H H (+)-pin4062 OMe Ph CH.sub.3 H H OH, OH4063 N(CNH)H Ph CH.sub.3 H H OH, OH4064 CH.sub.2 NH.sub.2 Ph H H H (+)-pin4065 CH.sub.2 NH.sub.2 Ph H H H OH, OH__________________________________________________________________________ TABLE 29__________________________________________________________________________ ##STR124##Ex X R.sup.13 R.sup.14 R.sup.15 R.sup.16 Y.sup.1 Y.sup.2 Phys. Data__________________________________________________________________________4070 CH.sub.2 NH.sub.2 Ph H H H (+)-pin4071 CH.sub.2 NH.sub.2 Ph methyl H H (+)-pin4072 CH.sub.2 NH.sub.2 Ph H H H OH, OH4073 CH.sub.2 NH.sub.2 Ph methyl H H OH, OH4074 NH(CNH)NH.sub.2 Ph H H H (+)-pin4075 NH(CNH)NH.sub.2 Ph methyl H H (+)-pin4076 NH(CNH)NH.sub.2 Ph H H H OH, OH4077 NH(CNH)NH.sub.2 Ph methyl H H OH, OH4078 NH(CNH)NH.sub.2 Ph CH.sub.3 CH.sub.3 H (+)-pin4079 NH(CNH)NH.sub.2 Ph CH.sub.3 CH.sub.3 H OH, OH4080 OMe Ph H H OH (+)-pin4081 NH(CNH)H Ph H H F (+)-pin4082 OMe Ph H H Me OH, OH4083 NH(CNH)H Ph H H Et OH, OH__________________________________________________________________________ TABLE 30__________________________________________________________________________ ##STR125## Phys.Ex X R.sup.13 R.sup.14 R.sup.15 R.sup.16 Y.sup.1 Y.sup.2 Data__________________________________________________________________________4088 CH.sub.2 NH.sub.2 PhCH.sub.2 H H Cl (+)-pin4089 CH.sub.2 NH.sub.2 PhCH.sub.2 H methyl H (+)-pin4090 CH.sub.2 NH.sub.2 PhCH.sub.2 H CH.sub.2 CN H (+)-pin4091 CH.sub.2 NH.sub.2 PhCH.sub.2 H CH.sub.2 COOH H (+)-pin4092 CH.sub.2 NH.sub.2 PhCH.sub.2 H CH.sub.2 NC H (+)-pin4093 CH.sub.2 NH.sub.2 PhCH.sub.2 H CH.sub.2 NO.sub.2 H (+)-pin4094 CH.sub.2 NH.sub.2 PhCH.sub.2 H (CH.sub.2).sub.2 OH H (+)-pin4095 CH.sub.2 NH.sub.2 PhCH.sub.2 H CH.sub.2 SOCH.sub.3 H (+)-pin4096 CH.sub.2 NH.sub.2 PhCH.sub.2 H H NO.sub.2 OH, OH4097 CH.sub.2 NH.sub.2 PhCH.sub.2 H methyl H OH, OH4098 CH.sub.2 NH.sub.2 PhCH.sub.2 H CH.sub.2 CN H OH, OH4099 CH.sub.2 NH.sub.2 PhCH.sub.2 H CH.sub.2 COOH H OH, OH4100 CH.sub.2 NH.sub.2 PhCH.sub.2 H CH.sub.2 NC H OH, OH4101 CH.sub.2 NH.sub.2 PhCH.sub.2 H CH.sub.2 NO.sub.2 H OH, OH4102 CH.sub.2 NH.sub.2 PhCH.sub.2 H (CH.sub.2).sub.2 OH H OH, OH4103 CH.sub.2 NH.sub.2 PhCH.sub.2 H CH.sub.2 SOCH.sub.3 H OH, OH4104 NH(CNH)NH.sub.2 PhCH.sub.2 H H H (+)-pin4105 NH(CNH)NH.sub.2 PhCH.sub.2 H methyl H (+)-pin4106 NH(CNH)NH.sub.2 PhCH.sub.2 H CH.sub.2 CN H (+)-pin4107 NH(CNH)NH.sub.2 PhCH.sub.2 H CH.sub.2 COOH H (+)-pin4108 NH(CNH)NH.sub.2 PhCH.sub.2 H CH.sub.2 NC H (+)-pin4109 NH(CNH)NH.sub.2 PhCH.sub.2 H CH.sub.2 NO.sub.2 H (+)-pin4110 NH(CNH)NH.sub.2 PhCH.sub.2 H (CH.sub.2).sub.2 OH H (+)-pin4111 NH(CNH)NH.sub.2 PhCH.sub.2 H CH.sub.2 SOCH.sub.3 H (+)-pin4112 NH(CNH)NH.sub.2 PhCH.sub.2 H H H OH, OH4113 NH(CNH)NH.sub.2 PhCH.sub.2 H methyl H OH, OH4114 NH(CNH)NH.sub.2 PhCH.sub.2 H CH.sub.2 CN H OH, OH4115 NH(CNH)NH.sub.2 PhCH.sub.2 H CH.sub.2 COOH H OH, OH4116 NH(CNH)NH.sub.2 PhCH.sub.2 H CH.sub.2 NC H OH, OH4117 NH(CNH)NH.sub.2 PhCH.sub.2 H CH.sub.2 NO.sub.2 H OH, OH4118 NH(CNH)NH.sub.2 PhCH.sub.2 H (CH.sub.2).sub.2 OH H OH, OH4119 NH(CNH)NH.sub.2 PhCH.sub.2 H CH.sub.2 SOCH.sub.3 H OH, OH__________________________________________________________________________ TABLE 31__________________________________________________________________________ ##STR126##Ex X R.sup.13 R.sup.14 R.sup.15 Y.sup.1 Y.sup.2 Phys. Data__________________________________________________________________________4124 CH.sub.2 NH.sub.2 PhCH.sub.2 H H (+)-pin4125 CH.sub.2 NH.sub.2 PhCH.sub.2 H methyl (+)-pin4126 CH.sub.2 NH.sub.2 PhCH.sub.2 H CH.sub.2 CN (+)-pin4127 CH.sub.2 NH.sub.2 PhCH.sub.2 H CH.sub.2 COOH (+)-pin4128 CH.sub.2 NH.sub.2 PhCH.sub.2 H CH.sub.2 NC (+)-pin4129 CH.sub.2 NH.sub.2 PhCH.sub.2 H CH.sub.2 NO.sub.2 (+)-pin4130 CH.sub.2 NH.sub.2 PhCH.sub.2 H (CH.sub.2).sub.2 OH (+)-pin4131 CH.sub.2 NH.sub.2 PhCH.sub.2 H CH.sub.2 SOCH.sub.3 (+)-pin4132 CH.sub.2 NH.sub.2 PhCH.sub.2 H H OH, OH4133 CH.sub.2 NH.sub.2 PhCH.sub.2 H methyl OH, OH4134 CH.sub.2 NH.sub.2 PhCH.sub.2 H CH.sub.2 CN OH, OH4135 CH.sub.2 NH.sub.2 PhCH.sub.2 H CH.sub.2 COOH OH, OH4136 CH.sub.2 NH.sub.2 PhCH.sub.2 H CH.sub.2 NC OH, OH4137 CH.sub.2 NH.sub.2 PhCH.sub.2 H CH.sub.2 NO.sub.2 OH, OH4138 CH.sub.2 NH.sub.2 PhCH.sub.2 H (CH.sub.2).sub.2 OH OH, OH4139 CH.sub.2 NH.sub.2 PhCH.sub.2 H CH.sub.2 SOCH.sub.3 OH, OH4140 NH(CNH)NH.sub.2 PhCH.sub.2 H H (+)-pin4141 NH(CNH)NH.sub.2 PhCH.sub.2 H methyl (+)-pin4142 NH(CNH)NH.sub.2 PhCH.sub.2 H CH.sub.2 CN (+)-pin4143 NH(CNH)NH.sub.2 PhCH.sub.2 H CH.sub.2 COOH (+)-pin4144 NH(CNH)NH.sub.2 PhCH.sub.2 H CH.sub.2 NC (+)-pin4145 NH(CNH)NH.sub.2 PhCH.sub.2 H CH.sub.2 NO.sub.2 (+)-pin4146 NH(CNH)NH.sub.2 PhCH.sub.2 H (CH.sub.2).sub.2 OH (+)-pin4147 NH(CNH)NH.sub.2 PhCH.sub.2 H CH.sub.2 SOCH.sub.3 (+)-pin4148 NH(CNH)NH.sub.2 PhCH.sub.2 H H OH, OH4149 NH(CNH)NH.sub.2 PhCH.sub.2 H methyl OH, OH4150 NH(CNH)NH.sub.2 PhCH.sub.2 H CH.sub.2 CN OH, OH4151 NH(CNH)NH.sub.2 PhCH.sub.2 H CH.sub.2 COOH OH, OH4152 NH(CNH)NH.sub.2 PhCH.sub.2 H CH.sub.2 NC OH, OH4153 NH(CNH)NH.sub.2 PhCH.sub.2 H CH.sub.2 NO.sub.2 OH, OH4154 NH(CNH)NH.sub.2 PhCH.sub.2 H (CH.sub.2).sub.2 OH OH, OH4155 NH(CNH)NH.sub.2 PhCH.sub.2 H CH.sub.2 SOCH.sub.3 OH, OH__________________________________________________________________________ TABLE 32__________________________________________________________________________ ##STR127##Ex X R.sup.13 R.sup.14 R.sup.15 Y.sup.1 Y.sup.2 Phys. Data__________________________________________________________________________4160 CH.sub.2 NH.sub.2 PhCH.sub.2 H H (+)-pin4161 CH.sub.2 NH.sub.2 PhCH.sub.2 Cl H (+)-pin4162 CH.sub.2 NH.sub.2 PhCH.sub.2 H methyl (+)-pin4163 CH.sub.2 NH.sub.2 PhCH.sub.2 H CH.sub.2 CN (+)-pin4164 CH.sub.2 NH.sub.2 PhCH.sub.2 Cl CH.sub.2 CN (+)-pin4165 CH.sub.2 NH.sub.2 PhCH.sub.2 H CH.sub.2 COOH (+)-pin4166 CH.sub.2 NH.sub.2 PhCH.sub.2 H CH.sub.2 NC (+)-pin4167 CH.sub.2 NH.sub.2 PhCH.sub.2 H CH.sub.2 NO.sub.2 (+)-pin4168 CH.sub.2 NH.sub.2 PhCH.sub.2 H (CH.sub.2).sub.2 OH (+)-pin4169 CH.sub.2 NH.sub.2 PhCH.sub.2 H CH.sub.2 SOCH.sub.3 (+)-pin4170 CH.sub.2 NH.sub.2 PhCH.sub.2 H H OH, OH4171 CH.sub.2 NH.sub.2 PhCH.sub.2 Cl H OH, OH4172 CH.sub.2 NH.sub.2 PhCH.sub.2 H methyl OH, OH4173 CH.sub.2 NH.sub.2 PhCH.sub.2 H CH.sub.2 CN OH, OH4174 CH.sub.2 NH.sub.2 PhCH.sub.2 Cl CH.sub.2 CN OH, OH4175 CH.sub.2 NH.sub.2 PhCH.sub.2 H CH.sub.2 COOH OH, OH4176 CH.sub.2 NH.sub.2 PhCH.sub.2 H CH.sub.2 NC OH, OH4177 CH.sub.2 NH.sub.2 PhCH.sub.2 H CH.sub.2 NO.sub.2 OH, OH4178 CH.sub.2 NH.sub.2 PhCH.sub.2 H (CH.sub.2).sub.2 OH OH, OH4179 CH.sub.2 NH.sub.2 PhCH.sub.2 H CH.sub.2 SOCH.sub.3 OH, OH4180 NH(CNH)NH.sub.2 PhCH.sub.2 H H (+)-pin4181 NH(CNH)NH.sub.2 PhCH.sub.2 H methyl (+)-pin4182 NH(CNH)NH.sub.2 PhCH.sub.2 H CH.sub.2 CN (+)-pin4183 NH(CNH)NH.sub.2 PhCH.sub.2 H CH.sub.2 COOH (+)-pin4184 NH(CNH)NH.sub.2 PhCH.sub.2 H CH.sub.2 NC (+)-pin4185 NH(CNH)NH.sub.2 PhCH.sub.2 H CH.sub.2 NO.sub.2 (+)-pin4186 NH(CNH)NH.sub.2 PhCH.sub.2 H (CH.sub.2).sub.2 OH (+)-pin4187 NH(CNH)NH.sub.2 PhCH.sub.2 H CH.sub.2 SOCH.sub.3 (+)-pin4188 NH(CNH)NH.sub.2 PhCH.sub.2 H H OH, OH4189 NH(CNH)NH.sub.2 PhCH.sub.2 H methyl OH, OH4190 NH(CNH)NH.sub.2 PhCH.sub.2 H CH.sub.2 CN OH, OH4191 NH(CNH)NH.sub.2 PhCH.sub.2 H CH.sub.2 COOH OH, OH4192 NH(CNH)NH.sub.2 PhCH.sub.2 H CH.sub.2 NC OH, OH4193 NH(CNH)NH.sub.2 PhCH.sub.2 H CH.sub.2 NO.sub.2 OH, OH4194 NH(CNH)NH.sub.2 PhCH.sub.2 H (CH.sub.2).sub.2 OH OH, OH4195 NH(CNH)NH.sub.2 PhCH.sub.2 H CH.sub.2 SOCH.sub.3 OH, OH__________________________________________________________________________ TABLE 33______________________________________ ##STR128## Phys.Ex X R.sup.13 R.sup.14 Y.sup.1 Y.sup.2 Data______________________________________4200 CH.sub.2 NH.sub.2 PhCH.sub.2 H (+)-pin4201 CH.sub.2 NH.sub.2 PhCH.sub.2 methyl (+)-pin4202 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 CN (+)-pin4203 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 CN (+)-pin4204 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 COOH (+)-pin4205 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 NC (+)-pin4206 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 NO.sub.2 (+)-pin4207 CH.sub.2 NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 OH (+)-pin4208 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 SOCH.sub.3 (+)-pin4209 CH.sub.2 NH.sub.2 PhCH.sub.2 H OH, OH4210 CH.sub.2 NH.sub.2 PhCH.sub.2 methyl OH, OH4211 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 CN OH, OH4212 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 CN OH, OH4213 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 COOH OH, OH4214 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 NC OH, OH4215 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 NO.sub.2 OH, OH4216 CH.sub.2 NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 OH OH, OH4217 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 SOCH.sub.3 OH, OH4218 NH(CNH)NH.sub.2 PhCH.sub.2 H (+)-pin4219 NH(CNH)NH.sub.2 PhCH.sub.2 methyl (+)-pin4220 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 CN (+)-pin4221 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 CN (+)-pin4222 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 COOH (+)-pin4223 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 COOH4224 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 NC (+)-pin4225 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 NO.sub.2 (+)-pin4226 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 OH (+)-pin4227 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 SOCH.sub.3 (+)-pin4228 NH(CNH)NH.sub.2 PhCH.sub.2 H OH, OH4229 NH(CNH)NH.sub.2 PhCH.sub.2 methyl OH, OH4230 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 CN OH, OH4231 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 CN OH, OH4232 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 COOH OH, OH4233 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 COOH OH, OH4234 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 NC OH, OH4235 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 NO.sub.2 OH, OH4236 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 OH OH, OH4237 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 SOCH.sub.3 OH, OH______________________________________ TABLE 34______________________________________ ##STR129##Ex X R.sup.13 Y.sup.1 Y.sup.2 Phys. Data______________________________________m = 14242 CH.sub.2 NH.sub.2 PhCH.sub.2 (+)-pin4243 CH.sub.2 NH.sub.2 PhCH.sub.2 OH, OH4244 NH(CNH)NH.sub.2 PhCH.sub.2 (+)-pin4245 NH(CNH)NH.sub.2 PhCH.sub.2 OH, OH4246 OMe PhCH.sub.2 (+)-pin4247 OMe PhCH.sub.2 OH, OH4248 NH(CNH)H PhCH.sub.2 (+)-pin4249 NH(CNH)H PhCH.sub.2 OH, OH4250 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 (+)-pin DB4251 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 OH, OH4252 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 (+)-pin4253 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 OH, OH4254 OMe PhCH.sub.2 CH.sub.2 (+)-pin4255 OMe PhCH.sub.2 CH.sub.2 OH, OH4256 NH(CNH)H PhCH.sub.2 CH.sub.2 (+)-pin4257 NH(CNH)H PhCH.sub.2 CH.sub.2 OH, OH DC4258 CH.sub.2 NH.sub.2 Ph (+)-pin4259 CH.sub.2 NH.sub.2 Ph OH, OH4260 NH(CNH)NH.sub.2 Ph (+)-pin4261 NH(CNH)NH.sub.2 Ph OH, OH4262 OMe Ph (+)-pin4263 OMe Ph OH, OH4264 NH(CNH)H Ph (+)-pin4265 NH(CNH)H Ph OH, OH4266 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 S (+)-pin4267 CH.sub.2 NH.sub.2 PhCH.sub.2 S (+)-pin4268 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 S OH, OH4269 CH.sub.2 NH.sub.2 PhCH.sub.2 S OH, OH4270 m = 24271 CH.sub.2 NH.sub.2 PhCH.sub.2 (+)-pin4272 CH.sub.2 NH.sub.2 PhCH.sub.2 OH, OH4273 NH(CNH)NH.sub.2 PhCH.sub.2 (+)-pin4274 NH(CNH)NH.sub.2 PhCH.sub.2 OH, OH4275 OMe PhCH.sub.2 (+)-pin4276 OMe PhCH.sub.2 OH, OH4277 NH(CNH)H PhCH.sub.2 (+)-pin4278 NH(CNH)H PhCH.sub.2 OH, OH4279 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 (+)-pin4280 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 OH, OH4281 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 (+)-pin4282 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 OH, OH4283 OMe PhCH.sub.2 CH.sub.2 (+)-pin4284 OMe PhCH.sub.2 CH.sub.2 OH, OH4285 NH(CNH)H PhCH.sub.2 CH.sub.2 (+)-pin4286 NH(CNH)H PhCH.sub.2 CH.sub.2 OH, OH4287 CH.sub.2 NH.sub.2 Ph (+)-pin4288 CH.sub.2 NH.sub.2 Ph OH, OH4289 NH(CNH)NH.sub.2 Ph (+)-pin4290 NH(CNH)NH.sub.2 Ph OH, OH4291 OMe Ph (+)-pin4292 OMe Ph OH, OH4293 NH(CNH)H Ph (+)-pin4294 NH(CNH)H Ph OH, OH______________________________________ DB. HRMS Calc'd. 495.3255, Found 495.3257 DC. HRMS Calc'd. 467.2442, Found 467.2950 TABLE 35______________________________________ ##STR130##Ex X R.sup.13 Y.sup.1 Y.sup.2 Phys. Data______________________________________m = 14299 CH.sub.2 NH.sub.2 PhCH.sub.2 (+)-pin4300 CH.sub.2 NH.sub.2 PhCH.sub.2 OH, OH4301 NH(CNH)NH.sub.2 PhCH.sub.2 (+)-pin4302 NH(CNH)NH.sub.2 PhCH.sub.2 OH, OH4303 OMe PhCH.sub.2 (+)-pin4304 OMe PhCH.sub.2 OH, OH4305 NH(CNH)H PhCH.sub.2 (+)-pin4306 NH(CNH)H PhCH.sub.2 OH, OH4307 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 (+)-pin DE4308 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 OH, OH4309 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 (+)-pin4310 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 OH, OH4311 OMe PhCH.sub.2 CH.sub.2 (+)-pin4312 OMe PhCH.sub.2 CH.sub.2 OH, OH4313 NH(CNH)H PhCH.sub.2 CH.sub.2 (+)-pin4314 NH(CNH)H PhCH.sub.2 CH.sub.2 OH, OH4315 CH.sub.2 NH.sub.2 Ph (+)-pin4316 CH.sub.2 NH.sub.2 Ph OH, OH4317 NH(CNH)NH.sub.2 Ph (+)-pin4318 NH(CNH)NH.sub.2 Ph OH, OH4319 OMe Ph (+)-pin4320 OMe Ph OH, OH4321 NH(CNH)H Ph (+)-pin4322 NH(CNH)H Ph OH, OH4323 m = 24324 CH.sub.2 NH.sub.2 PhCH.sub.2 (+)-pin4325 CH.sub.2 NH.sub.2 PhCH.sub.2 OH, OH4326 NH(CNH)NH.sub.2 PhCH.sub.2 (+)-pin4327 NH(CNH)NH.sub.2 PhCH.sub.2 OH, OH4328 OMe PhCH.sub.2 (+)-pin4329 OMe PhCH.sub.2 OH, OH4330 NH(CNH)H PhCH.sub.2 (+)-pin4331 NH(CNH)H PhCH.sub.2 OH, OH4332 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 (+)-pin4333 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 OH, OH4334 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 (+)-pin4335 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 OH, OH4336 OMe PhCH.sub.2 CH.sub.2 (+)-pin4337 OMe PhCH.sub.2 CH.sub.2 OH, OH4338 NH(CNH)H PhCH.sub.2 CH.sub.2 (+)-pin4339 NH(CNH)H PhCH.sub.2 CH.sub.2 OH, OH4340 CH.sub.2 NH.sub.2 Ph (+)-pin4341 CH.sub.2 NH.sub.2 Ph OH, OH4342 NH(CNH)NH.sub.2 Ph (+)-pin4343 NH(CNH)NH.sub.2 Ph OH, OH4344 OMe Ph (+)-pin4345 OMe Ph OH, OH4346 NH(CNH)H Ph (+)-pin4347 NH(CNH)H Ph OH, OH______________________________________ DE. HRMS Calc'd. 495.3255, Found 495.3249 TABLE 36______________________________________ ##STR131## Phys.Ex X R.sup.13 R.sup.14 Y.sup.1 Y.sup.2 Data______________________________________m = 14348 CH.sub.2 NH.sub.2 PhCH.sub.2 H (+)-pin4349 CH.sub.2 NH.sub.2 PhCH.sub.2 methyl (+)-pin4350 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 CN (+)-pin4351 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 COOH (+)-pin4352 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 NC (+)-pin4353 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 NO.sub.2 (+)-pin4354 CH.sub.2 NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 OH (+)-pin4355 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 SOCH.sub.3 (+)-pin4356 CH.sub.2 NH.sub.2 PhCH.sub.2 H OH, OH4357 CH.sub.2 NH.sub.2 PhCH.sub.2 methyl OH, OH4358 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 CN OH, OH4359 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 COOH OH, OH4360 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 NC OH, OH4361 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 NO.sub.2 OH, OH4362 CH.sub.2 NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 OH OH, OH4363 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 SOCH.sub.3 OH, OH4364 NH(CNH)NH.sub.2 PhCH.sub.2 H (+)-pin4365 NH(CNH)NH.sub.2 PhCH.sub.2 methyl (+)-pin4366 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 CN (+)-pin4367 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 CN (+)-pin4368 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 COOH (+)-pin4369 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 COOH (+)-pin4370 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 NC (+)-pin4371 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 NO.sub.2 (+)-pin4372 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 OH (+)-pin4373 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 SOCH.sub.3 (+)-pin4374 NH(CNH)NH.sub.2 PhCH.sub.2 H H, OH4375 NH(CNH)NH.sub.2 PhCH.sub.2 methyl OH, OH4376 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 CN OH, OH4377 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 CN OH, OH4378 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 COOH OH, OH4379 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 COOH OH, OH4380 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 NC OH, OH4381 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 NO.sub.2 OH, OH4382 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 OH OH, OH4383 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 SOCH.sub.3 OH, OH4384 m = 24385 CH.sub.2 NH.sub.2 PhCH.sub.2 H (+)-pin4386 CH.sub.2 NH.sub.2 PhCH.sub.2 methyl (+)-pin4387 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 CN (+)-pin4388 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 COOH (+)-pin4389 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 NC (+)-pin4390 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 NO.sub.2 (+)-pin4391 CH.sub.2 NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 OH (+)-pin4392 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 SOCH.sub.3 (+)-pin4393 CH.sub.2 NH.sub.2 PhCH.sub.2 H OH, OH4394 CH.sub.2 NH.sub.2 PhCH.sub.2 methyl OH, OH4395 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 CN OH, OH4396 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 COOH OH, OH4397 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 NC OH, OH4398 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 NO.sub.2 OH, OH4399 CH.sub.2 NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 OH OH, OH4400 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 SOCH.sub.3 OH, OH4401 NH(CNH)NH.sub.2 PhCH.sub.2 (+)-pin4402 NH(CNH)NH.sub.2 PhCH.sub.2 ethyl (+)-pin4403 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 CN (+)-pin4404 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 CN (+)-pin4405 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 COOH (+)-pin4406 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 COOH (+)-pin4407 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 NC (+)-pin4408 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 NO.sub.2 (+)-pin4409 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 OH (+)-pin4410 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 SOCH.sub.3 (+)-pin4411 NH(CNH)NH.sub.2 PhCH.sub.2 H OH, OH4412 NH(CNH)NH.sub.2 PhCH.sub.2 methyl OH, OH4413 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 CN OH, OH4414 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 CN OH, OH4415 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 COOH OH, OH4416 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 COOH OH, OH4417 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 NC OH, OH4418 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 NO.sub.2 OH, OH4419 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 OH OH, OH4420 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 SOCH.sub.3 OH, OH4421 m = 04422 CH.sub.2 NH.sub.2 PhCH.sub.2 H (+)-pin4423 CH.sub.2 NH.sub.2 PhCH.sub.2 methyl (+)-pin4424 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 CN (+)-pin4425 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 COOH (+)-pin4426 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 NC (+)-pin4427 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 NO.sub.2 (+)-pin4428 CH.sub.2 NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 OH (+)-pin4429 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 SOCH.sub.3 (+)-pin4430 CH.sub.2 NH.sub.2 PhCH.sub.2 H OH, OH4431 CH.sub.2 NH.sub.2 PhCH.sub.2 methyl OH, OH4432 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 CN OH, OH4433 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 COOH OH, OH4434 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 NC OH, OH4435 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 NO.sub.2 OH, OH4436 CH.sub.2 NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 OH OH, OH4437 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 SOCH.sub.3 OH, OH4438 NH(CNH)NH.sub.2 PhCH.sub.2 H (+)-pin4439 NH(CNH)NH.sub.2 PhCH.sub.2 methyl (+)-pin4440 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 CN (+)-pin4441 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 CN (+)-pin4442 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 COOH (+)-pin4443 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 COOH (+)-pin4444 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 NC (+)-pin4445 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 NO.sub.2 (+)-pin4446 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 OH (+)-pin4447 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 SOCH.sub.3 (+)-pin4448 NH(CNH)NH.sub.2 PhCH.sub.2 H H, OH4449 NH(CNH)NH.sub.2 PhCH.sub.2 methyl OH, OH4450 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 CN OH, OH4451 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 CN OH, OH4452 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 COOH OH, OH4453 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 COOH OH, OH4454 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 NC OH, OH4455 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 NO.sub.2 OH, OH4456 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 OH OH, OH4457 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 SOCH.sub.3 OH, OH______________________________________ TABLE 37______________________________________ ##STR132## Phys.Ex X R.sup.13 R.sup.14 Y.sup.1 Y.sup.2 Data______________________________________m = 14462 CH.sub.2 NH.sub.2 PhCH.sub.2 H (+)-pin4463 CH.sub.2 NH.sub.2 PhCH.sub.2 methyl (+)-pin4464 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 CN (+)-pin4465 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 COOH (+)-pin4466 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 NC (+)-pin4467 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 NO.sub.2 (+)-pin4468 CH.sub.2 NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 OH (+)-pin4469 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 SOCH.sub.3 (+)-pin4470 CH.sub.2 NH.sub.2 PhCH.sub.2 H OH, OH4471 CH.sub.2 NH.sub.2 PhCH.sub.2 methyl OH, OH4472 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 CN OH, OH4473 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 COOH OH, OH4474 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 NC OH, OH4475 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 NO.sub.2 OH, OH4476 CH.sub.2 NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 OH OH, OH4477 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 SOCH.sub.3 OH, OH4478 NH(CNH)NH.sub.2 PhCH.sub.2 H (+)-pin4479 NH(CNH)NH.sub.2 PhCH.sub.2 methyl (+)-pin4480 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 CN (+)-pin4481 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 CN (+)-pin4482 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 COOH (+)-pin4483 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 COOH (+)-pin4484 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 NC (+)-pin4485 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 NO.sub.2 (+)-pin4486 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 OH (+)-pin4487 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 SOCH.sub.3 (+)-pin4488 NH(CNH)NH.sub.2 PhCH.sub.2 H OH, OH4489 NH(CNH)NH.sub.2 PhCH.sub.2 methyl OH, OH4490 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 CN OH, OH4491 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 CN OH, OH4492 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 COOH OH, OH4493 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 COOH OH, OH4494 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 NC OH, OH4495 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 NO.sub.2 OH, OH4496 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 OH OH, OH4497 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 SOCH.sub.3 OH, OH4498 m = 24499 CH.sub.2 NH.sub.2 PhCH.sub.2 H (+)-pin4500 CH.sub.2 NH.sub.2 PhCH.sub.2 methyl (+)-pin4501 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 CN (+)-pin4502 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 COOH (+)-pin4503 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 NC (+)-pin4504 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 NO.sub.2 (+)-pin4505 CH.sub.2 NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 OH (+)-pin4506 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 SOCH.sub.3 (+)-pin4507 CH.sub.2 NH.sub.2 PhCH.sub.2 H OH, OH4508 CH.sub.2 NH.sub.2 PhCH.sub.2 methyl OH, OH4509 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 CN OH, OH4510 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 COOH OH, OH4511 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 NC OH, OH4512 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 NO.sub.2 OH, OH4513 CH.sub.2 NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 OH OH, OH4514 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 SOCH.sub.3 OH, OH4515 NH(CNH)NH.sub.2 PhCH.sub.2 H (+)-pin4516 NH(CNH)NH.sub.2 PhCH.sub.2 methyl (+)-pin4517 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 CN (+)-pin4518 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 CN (+)-pin4519 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 COOH (+)-pin4520 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 COOH (+)-pin4521 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 NC (+)-pin4522 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 NO.sub.2 (+)-pin4523 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 OH (+)-pin4524 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 SOCH.sub.3 (+)-pin4525 NH(CNH)NH.sub.2 PhCH.sub.2 H OH, OH4526 NH(CNH)NH.sub.2 PhCH.sub.2 methyl OH, OH4527 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 CN OH, OH4528 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 CN OH, OH4529 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 COOH OH, OH4530 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 COOH OH, OH4531 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 NC OH, OH4532 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 NO.sub.2 OH, OH4533 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 OH OH, OH4534 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 SOCH.sub.3 OH, OH m = 04535 CH.sub.2 NH.sub.2 PhCH.sub.2 H (+)-pin4536 CH.sub.2 NH.sub.2 PhCH.sub.2 methyl (+)-pin4537 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 CN (+)-pin4538 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 COOH (+)-pin4539 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 NC (+)-pin4540 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 NO.sub.2 (+)-pin4541 CH.sub.2 NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 OH (+)-pin4542 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 SOCH.sub.3 (+)-pin4543 CH.sub.2 NH.sub.2 PhCH.sub.2 H OH, OH4544 CH.sub.2 NH.sub.2 PhCH.sub.2 methyl OH, OH4545 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 CN OH, OH4546 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 COOH OH, OH4547 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 NC OH, OH4548 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 NO.sub.2 OH, OH4549 CH.sub.2 NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 OH OH, OH4550 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 SOCH.sub.3 OH, OH4551 NH(CNH)NH.sub.2 PhCH.sub.2 H (+)-pin4552 NH(CNH)NH.sub.2 PhCH.sub.2 methyl (+)-pin4553 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 CN (+)-pin4554 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 CN (+)-pin4555 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 COOH (+)-pin4556 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 COOH (+)-pin4557 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 NC (+)-pin4558 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 NO.sub.2 (+)-pin4559 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 OH (+)-pin4560 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 SOCH.sub.3 (+)-pin4561 NH(CNH)NH.sub.2 PhCH.sub.2 H OH, OH4562 NH(CNH)NH.sub.2 PhCH.sub.2 methyl OH, OH4563 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 CN OH, OH4564 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 CN OH, OH4565 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 COOH OH, OH4566 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 COOH OH, OH4567 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 NC OH, OH4568 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 NO.sub.2 OH, OH4569 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 OH OH, OH4570 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 SOCH.sub.3 OH, OH______________________________________ TABLE 38______________________________________ ##STR133## Phys.Ex X R.sup.13 R.sup.14 Y.sup.1 Y.sup.2 Data______________________________________m = 14575 CH.sub.2 NH.sub.2 PhCH.sub.2 H (+)-pin4576 CH.sub.2 NH.sub.2 PhCH.sub.2 methyl (+)-pin4577 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 CN (+)-pin4578 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 COOH (+)-pin4579 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 NC (+)-pin4580 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 NO.sub.2 (+)-pin4581 CH.sub.2 NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 OH (+)-pin4582 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 SOCH.sub.3 (+)-pin4583 CH.sub.2 NH.sub.2 PhCH.sub.2 H OH, OH4584 CH.sub.2 NH.sub.2 PhCH.sub.2 methyl OH, OH4585 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 CN OH, OH4586 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 COOH OH, OH4587 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 NC OH, OH4588 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 NO.sub.2 OH, OH4589 CH.sub.2 NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 OH OH, OH4590 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 SOCH.sub.3 OH, OH4591 NH(CNH)NH.sub.2 PhCH.sub.2 H (+)-pin4592 NH(CNH)NH.sub.2 PhCH.sub.2 methyl (+)-pin4593 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 CN (+)-pin4594 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 CN (+)-pin4595 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 COOH (+)-pin4596 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 COOH (+)-pin4597 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 NC (+)-pin4598 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 NO.sub.2 (+)-pin4599 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 OH (+)-pin4600 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 SOCH.sub.3 (+)-pin4601 NH(CNH)NH.sub.2 PhCH.sub.2 H OH, OH4602 NH(CNH)NH.sub.2 PhCH.sub.2 methyl OH, OH4603 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 CN OH, OH4604 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 CN OH, OH4605 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 COOH OH, OH4606 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 COOH OH, OH4607 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 NC OH, OH4608 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 NO.sub.2 OH, OH4609 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 OH OH, OH4610 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 SOCH.sub.3 OH, OH m = 04611 CH.sub.2 NH.sub.2 PhCH.sub.2 H (+)-pin4612 CH.sub.2 NH.sub.2 PhCH.sub.2 methyl (+)-pin4613 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 CN (+)-pin4614 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 COOH (+)-pin4615 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 NC (+)-pin4616 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 NO.sub.2 (+)-pin4617 CH.sub.2 NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 OH (+)-pin4618 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 SOCH.sub.3 (+)-pin4619 CH.sub.2 NH.sub.2 PhCH.sub.2 H OH, OH4620 CH.sub.2 NH.sub.2 PhCH.sub.2 methyl OH, OH4621 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 CN OH, OH4622 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 COOH OH, OH4623 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 NC OH, OH4624 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 NO.sub.2 OH, OH4625 CH.sub.2 NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 OH OH, OH4626 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 SOCH.sub.3 OH, OH4627 NH(CNH)NH.sub.2 PhCH.sub.2 H (+)-pin4628 NH(CNH)NH.sub.2 PhCH.sub.2 methyl (+)-pin4629 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 CN (+)-pin4630 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 CN (+)-pin4631 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 COOH (+)-pin4632 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 COOH (+)-pin4633 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 NC (+)-pin4634 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 NO.sub.2 (+)-pin4635 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 OH (+)-pin4636 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 SOCH.sub.3 (+)-pin4637 NH(CNH)NH.sub.2 PhCH.sub.2 H OH, OH4638 NH(CNH)NH.sub.2 PhCH.sub.2 methyl OH, OH4639 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 CN OH, OH4640 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 CN OH, OH4641 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 COOH OH, OH4642 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 COOH OH, OH4643 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 NC OH, OH4644 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 NO.sub.2 OH, OH4645 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 OH OH, OH4646 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 SOCH.sub.3 OH, OH______________________________________ TABLE 39______________________________________ ##STR134## Phys.Ex X R.sup.13 R.sup.14 Y.sup.1 Y.sup.2 Data______________________________________m = 14651 CH.sub.2 NH.sub.2 PhCH.sub.2 H (+)-pin4652 CH.sub.2 NH.sub.2 PhCH.sub.2 methyl (+)-pin4653 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 CN (+)-pin4654 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 COOH (+)-pin4655 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 NC (+)-pin4656 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 NO.sub.2 (+)-pin4657 CH.sub.2 NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 OH (+)-pin4658 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 SOCH.sub.3 (+)-pin4659 CH.sub.2 NH.sub.2 PhCH.sub.2 H OH, OH4660 CH.sub.2 NH.sub.2 PhCH.sub.2 methyl OH, OH4661 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 CN OH, OH4662 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 COOH OH, OH4663 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 NC OH, OH4664 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 NO.sub.2 OH, OH4665 CH.sub.2 NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 OH OH, OH4666 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 SOCH.sub.3 OH, OH4667 NH(CNH)NH.sub.2 PhCH.sub.2 H (+)-pin4668 NH(CNH)NH.sub.2 PhCH.sub.2 methyl (+)-pin4669 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 CN (+)-pin4670 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 CN (+)-pin4671 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 COOH (+)-pin4672 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 COOH (+)-pin4673 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 NC (+)-pin4674 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 NO.sub.2 (+)-pin4675 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 OH (+)-pin4676 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 SOCH.sub.3 (+)-pin4677 NH(CNH)NH.sub.2 PhCH.sub.2 H OH, OH4678 NH(CNH)NH.sub.2 PhCH.sub.2 methyl OH, OH4679 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 CN OH, OH4680 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 CN OH, OH4681 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 COOH OH, OH4682 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 COOH OH, OH4683 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 NC OH, OH4684 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 NO.sub.2 OH, OH4685 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 OH OH, OH4686 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 SOCH.sub.3 OH, OH m = 04687 CH.sub.2 NH.sub.2 PhCH.sub.2 H (+)-pin4688 CH.sub.2 NH.sub.2 PhCH.sub.2 methyl (+)-pin4689 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 CN (+)-pin4690 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 COOH (+)-pin4691 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 NC (+)-pin4692 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 NO.sub.2 (+)-pin4693 CH.sub.2 NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 OH (+)-pin4694 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 SOCH.sub.3 (+)-pin4695 CH.sub.2 NH.sub.2 PhCH.sub.2 H OH, OH4696 CH.sub.2 NH.sub.2 PhCH.sub.2 methyl OH, OH4697 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 CN OH, OH4698 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 COOH OH, OH4699 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 NC OH, OH4700 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 NO.sub.2 OH, OH4701 CH.sub.2 NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 OH OH, OH4702 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 SOCH.sub.3 OH, OH4703 NH(CNH)NH.sub.2 PhCH.sub.2 H (+)-pin4704 NH(CNH)NH.sub.2 PhCH.sub.2 methyl (+)-pin4705 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 CN (+)-pin4706 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 CN (+)-pin4707 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 COOH (+)-pin4708 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 COOH (+)-pin4709 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 NC (+)-pin4710 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 NO.sub.2 (+)-pin4711 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 OH (+)-pin4712 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 SOCH.sub.3 (+)-pin4713 NH(CNH)NH.sub.2 PhCH.sub.2 H OH, OH4714 NH(CNH)NH.sub.2 PhCH.sub.2 methyl OH, OH4715 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 CN OH, OH4716 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 CN OH, OH4717 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 COOH OH, OH4718 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 COOH OH, OH4719 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 NC OH, OH4720 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 NO.sub.2 OH, OH4721 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 OH OH, OH4722 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 SOCH.sub.3 OH, OH______________________________________ TABLE 40______________________________________ ##STR135## Phys.Ex X R.sup.13 R.sup.14 Y.sup.1 Y.sup.2 Data______________________________________m = 14727 CH.sub.2 NH.sub.2 PhCH.sub.2 H (+)-pin4728 CH.sub.2 NH.sub.2 PhCH.sub.2 methyl (+)-pin4729 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 CN (+)-pin4730 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 COOH (+)-pin4731 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 NC (+)-pin4732 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 NO.sub.2 (+)-pin4733 CH.sub.2 NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 OH (+)-pin4734 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 SOCH.sub.3 (+)-pin4735 CH.sub.2 NH.sub.2 PhCH.sub.2 H OH, OH4736 CH.sub.2 NH.sub.2 PhCH.sub.2 methyl OH, OH4737 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 CN OH, OH4738 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 COOH OH, OH4739 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 NC OH, OH4740 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 NO.sub.2 OH, OH4741 CH.sub.2 NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 OH OH, OH4742 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 SOCH.sub.3 OH, OH4743 NH(CNH)NH.sub.2 PhCH.sub.2 H (+)-pin4744 NH(CNH)NH.sub.2 PhCH.sub.2 methyl (+)-pin4745 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 CN (+)-pin4746 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 CN (+)-pin4747 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 COOH (+)-pin4748 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 COOH (+)-pin4749 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 NC (+)-pin4750 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 NO.sub.2 (+)-pin4751 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 OH (+)-pin4752 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 SOCH.sub.3 (+)-pin4753 NH(CNH)NH.sub.2 PhCH.sub.2 H OH, OH4754 NH(CNH)NH.sub.2 PhCH.sub.2 methyl OH, OH4755 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 CN OH, OH4756 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 CN OH, OH4757 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 COOH OH, OH4758 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 COOH OH, OH4759 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 NC OH, OH4760 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 NO.sub.2 OH, OH4761 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 OH OH, OH4762 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 SOCH.sub.3 OH, OH m = 04763 CH.sub.2 NH.sub.2 PhCH.sub.2 H (+)-pin4764 CH.sub.2 NH.sub.2 PhCH.sub.2 methyl (+)-pin4765 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 CN (+)-pin4766 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 COOH (+)-pin4767 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 NC (+)-pin4768 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 NO.sub.2 (+)-pin4769 CH.sub.2 NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 OH (+)-pin4770 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 SOCH.sub.3 (+)-pin4771 CH.sub.2 NH.sub.2 PhCH.sub.2 H OH, OH4772 CH.sub.2 NH.sub.2 PhCH.sub.2 methyl OH, OH4773 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 CN OH, OH4774 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 COOH OH, OH4775 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 NC OH, OH4776 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 NO.sub.2 OH, OH4777 CH.sub.2 NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 OH OH, OH4778 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 SOCH.sub.3 OH, OH4779 NH(CNH)NH.sub.2 PhCH.sub.2 H (+)-pin4780 NH(CNH)NH.sub.2 PhCH.sub.2 methyl (+)-pin4781 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 CN (+)-pin4782 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 CN (+)-pin4783 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 COOH (+)-pin4784 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 COOH (+)-pin4785 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 NC (+)-pin4786 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 NO.sub.2 (+)-pin4787 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 OH (+)-pin4788 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 SOCH.sub.3 (+)-pin4789 NH(CNH)NH.sub.2 PhCH.sub.2 H OH, OH4790 NH(CNH)NH.sub.2 PhCH.sub.2 methyl OH, OH4791 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 CN OH, OH4792 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 CN OH, OH4793 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 COOH OH, OH4794 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 COOH OH, OH4795 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 NC OH, OH4796 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 NO.sub.2 OH, OH4797 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 OH OH, OH4798 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 SOCH.sub.3 OH, OH______________________________________ TABLE 41______________________________________ ##STR136## Phys.Ex X R.sup.13 R.sup.14 Y.sup.1 Y.sup.2 Data______________________________________m = 14803 CH.sub.2 NH.sub.2 PhCH.sub.2 H (+)-pin4804 CH.sub.2 NH.sub.2 PhCH.sub.2 methyl (+)-pin4805 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 CN (+)-pin4806 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 COOH (+)-pin4807 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 NC (+)-pin4808 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 NO.sub.2 (+)-pin4809 CH.sub.2 NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 OH (+)-pin4810 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 SOCH.sub.3 (+)-pin4811 CH.sub.2 NH.sub.2 PhCH.sub.2 H OH, OH4812 CH.sub.2 NH.sub.2 PhCH.sub.2 methyl OH, OH4813 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 CN OH, OH4814 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 COOH OH, OH4815 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 NC OH, OH4816 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 NO.sub.2 OH, OH4817 CH.sub.2 NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 OH OH, OH4818 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 SOCH.sub.3 OH, OH4819 NH(CNH)NH.sub.2 PhCH.sub.2 H (+)-pin4820 NH(CNH)NH.sub.2 PhCH.sub.2 methyl (+)-pin4821 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 CN (+)-pin4822 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 CN (+)-pin4823 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 COOH (+)-pin4824 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 COOH (+)-pin4825 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 NC (+)-pin4826 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 NO.sub.2 (+)-pin4827 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 OH (+)-pin4828 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 SOCH.sub.3 (+)-pin4829 NH(CNH)NH.sub.2 PhCH.sub.2 H OH, OH4830 NH(CNH)NH.sub.2 PhCH.sub.2 methyl OH, OH4831 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 CN OH, OH4832 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 CN OH, OH4833 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 COOH OH, OH4834 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 COOH OH, OH4835 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 NC OH, OH4836 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 NO.sub.2 OH, OH4837 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 OH OH, OH4838 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 SOCH.sub.3 OH, OH m = 04839 CH.sub.2 NH.sub.2 PhCH.sub.2 H (+)-pin4840 CH.sub.2 NH.sub.2 PhCH.sub.2 methyl (+)-pin4841 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 CN (+)-pin4842 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 COOH (+)-pin4843 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 NC (+)-pin4844 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 NO.sub.2 (+)-pin4845 CH.sub.2 NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 OH (+)-pin4846 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 SOCH.sub.3 (+)-pin4847 CH.sub.2 NH.sub.2 PhCH.sub.2 H OH, OH4848 CH.sub.2 NH.sub.2 PhCH.sub.2 methyl OH, OH4849 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 CN OH, OH4850 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 COOH OH, OH4851 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 NC OH, OH4852 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 NO.sub.2 OH, OH4853 CH.sub.2 NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 OH OH, OH4854 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 SOCH.sub.3 OH, OH4855 NH(CNH)NH.sub.2 PhCH.sub.2 H (+)-pin4856 NH(CNH)NH.sub.2 PhCH.sub.2 methyl (+)-pin4857 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 CN (+)-pin4858 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 CN (+)-pin4859 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 COOH (+)-pin4860 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 COOH (+)-pin4861 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 NC (+)-pin4862 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 NO.sub.2 (+)-pin4863 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 OH (+)-pin4864 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 SOCH.sub.3 (+)-pin4865 NH(CNH)NH.sub.2 PhCH.sub.2 H OH, OH4866 NH(CNH)NH.sub.2 PhCH.sub.2 methyl OH, OH4867 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 CN OH, OH4868 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 CN OH, OH4869 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 COOH OH, OH4870 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 COOH OH, OH4871 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 NC OH, OH4872 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 NO.sub.2 OH, OH4873 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 OH OH, OH4874 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 SOCH.sub.3 OH, OH______________________________________ TABLE 42______________________________________ ##STR137## Phys.Ex X R.sup.13 R.sup.14 Y.sup.1 Y.sup.2 Data______________________________________m = 14879 CH.sub.2 NH.sub.2 PhCH.sub.2 H (+)-pin4880 CH.sub.2 NH.sub.2 PhCH.sub.2 methyl (+)-pin4881 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 CN (+)-pin4882 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 COOH (+)-pin4883 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 NC (+)-pin4884 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 NO.sub.2 (+)-pin4885 CH.sub.2 NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 OH (+)-pin4886 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 SOCH.sub.3 (+)-pin4887 CH.sub.2 NH.sub.2 PhCH.sub.2 H OH, OH4888 CH.sub.2 NH.sub.2 PhCH.sub.2 methyl OH, OH4889 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 CN OH, OH4890 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 COOH OH, OH4891 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 NC OH, OH4892 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 NO.sub.2 OH, OH4893 CH.sub.2 NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 OH OH, OH4894 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 SOCH.sub.3 OH, OH4895 NH(CNH)NH.sub.2 PhCH.sub.2 H (+)-pin4896 NH(CNH)NH.sub.2 PhCH.sub.2 methyl (+)-pin4897 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 CN (+)-pin4898 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 CN (+)-pin4899 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 COOH (+)-pin4900 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 COOH (+)-pin4901 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 NC (+)-pin4902 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 NO.sub.2 (+)-pin4903 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 OH (+)-pin4904 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 SOCH.sub.3 (+)-pin4905 NH(CNH)NH.sub.2 PhCH.sub.2 H OH, OH4906 NH(CNH)NH.sub.2 PhCH.sub.2 methyl OH, OH4907 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 CN OH, OH4908 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 CN OH, OH4909 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 COOH OH, OH4910 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 COOH OH, OH4911 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 NC OH, OH4912 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 NO.sub.2 OH, OH4913 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 OH OH, OH4914 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 SOCH.sub.3 OH, OH m = 24915 CH.sub.2 NH.sub.2 PhCH.sub.2 H (+)-pin4916 CH.sub.2 NH.sub.2 PhCH.sub.2 methyl (+)-pin4917 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 CN (+)-pin4918 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 COOH (+)-pin4919 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 NC (+)-pin4920 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 NO.sub.2 (+)-pin4921 CH.sub.2 NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 OH (+)-pin4922 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 SOCH.sub.3 (+)-pin4923 CH.sub.2 NH.sub.2 PhCH.sub.2 H OH, OH4924 CH.sub.2 NH.sub.2 PhCH.sub.2 methyl OH, OH4925 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 CN OH, OH4926 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 COOH OH, OH4927 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 NC OH, OH4928 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 NO.sub.2 OH, OH4929 CH.sub.2 NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 OH OH, OH4930 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 SOCH.sub.3 OH, OH4931 NH(CNH)NH.sub.2 PhCH.sub.2 H (+)-pin4932 NH(CNH)NH.sub.2 PhCH.sub.2 methyl (+)-pin4933 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 CN (+)-pin4934 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 CN (+)-pin4935 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 COOH (+)-pin4936 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 COOH (+)-pin4937 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 NC (+)-pin4938 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 NO.sub.2 (+)-pin4939 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 OH (+)-pin4940 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 SOCH.sub.3 (+)-pin4941 NH(CNH)NH.sub.2 PhCH.sub.2 H OH, OH4942 NH(CNH)NH.sub.2 PhCH.sub.2 methyl OH, OH4943 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 CN OH, OH4944 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 CN OH, OH4945 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 COOH OH, OH4946 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 COOH OH, OH4947 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 NC OH, OH4948 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 NO.sub.2 OH, OH4949 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 OH OH, OH4950 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 SOCH.sub.3 OH, OH m = 04951 CH.sub.2 NH.sub.2 PhCH.sub.2 H (+)-pin4952 CH.sub.2 NH.sub.2 PhCH.sub.2 methyl (+)-pin4953 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 CN (+)-pin4954 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 COOH (+)-pin4955 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 NC (+)-pin4956 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 NO.sub.2 (+)-pin4957 CH.sub.2 NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 OH (+)-pin4958 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 SOCH.sub.3 (+)-pin4959 CH.sub.2 NH.sub.2 PhCH.sub.2 H OH, OH4960 CH.sub.2 NH.sub.2 PhCH.sub.2 methyl OH, OH4961 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 CN OH, OH4962 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 COOH OH, OH4963 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 NC OH, OH4964 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 NO.sub.2 OH, OH4965 CH.sub.2 NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 OH OH, OH4966 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 SOCH.sub.3 OH, OH4967 NH(CNH)NH.sub.2 PhCH.sub.2 H (+)-pin4968 NH(CNH)NH.sub.2 PhCH.sub.2 methyl (+)-pin4969 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 CN (+)-pin4970 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 CN (+)-pin4971 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 COOH (+)-pin4972 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 COOH (+)-pin4973 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 NC (+)-pin4974 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 NO.sub.2 (+)-pin4975 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 OH (+)-pin4976 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 SOCH.sub.3 (+)-pin4977 NH(CNH)NH.sub.2 PhCH.sub.2 H OH, OH4978 NH(CNH)NH.sub.2 PhCH.sub.2 methyl OH, OH4979 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 CN OH, OH4980 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 CN OH, OH4981 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 COOH OH, OH4982 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 COOH OH, OH4983 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 NC OH, OH4984 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 NO.sub.2 OH, OH4985 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 OH OH, OH4986 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 SOCH.sub.3 OH, OH______________________________________ TABLE 43______________________________________ ##STR138## Phys.Ex X R.sup.13 R.sup.14 Y.sup.1 Y.sup.2 Data______________________________________m = 14991 CH.sub.2 NH.sub.2 PhCH.sub.2 H (+)-pin4992 CH.sub.2 NH.sub.2 PhCH.sub.2 methyl (+)-pin4993 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 CN (+)-pin4994 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 COOH (+)-pin4995 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 NC (+)-pin4996 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 NO.sub.2 (+)-pin4997 CH.sub.2 NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 OH (+)-pin4998 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 SOCH.sub.3 (+)-pin4999 CH.sub.2 NH.sub.2 PhCH.sub.2 H OH, OH5000 CH.sub.2 NH.sub.2 PhCH.sub.2 methyl OH, OH5001 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 CN OH, OH5002 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 COOH OH, OH5003 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 NC OH, OH5004 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 NO.sub.2 OH, OH5005 CH.sub.2 NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 OH OH, OH5006 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 SOCH.sub.3 OH, OH5007 NH(CNH)NH.sub.2 PhCH.sub.2 H (+)-pin5008 NH(CNH)NH.sub.2 PhCH.sub.2 methyl (+)-pin5009 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 CN (+)-pin5010 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 CN (+)-pin5011 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 COOH (+)-pin5012 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 COOH (+)-pin5013 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 NC (+)-pin5014 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 NO.sub.2 (+)-pin5015 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 OH (+)-pin5016 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 SOCH.sub.3 (+)-pin5017 NH(CNH)NH.sub.2 PhCH.sub.2 H OH, OH5018 NH(CNH)NH.sub.2 PhCH.sub.2 methyl OH, OH5019 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 CN OH, OH5020 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 CN OH, OH5021 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 COOH OH, OH5022 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 COOH OH, OH5023 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 NC OH, OH5024 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 NO.sub.2 OH, OH5025 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 OH OH, OH5026 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 SOCH.sub.3 OH, OH m = 25027 CH.sub.2 NH.sub.2 PhCH.sub.2 H (+)-pin5028 CH.sub.2 NH.sub.2 PhCH.sub.2 methyl (+)-pin5029 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 CN (+)-pin5030 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 COOH (+)-pin5031 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 NC (+)-pin5032 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 NO.sub.2 (+)-pin5033 CH.sub.2 NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 OH (+)-pin5034 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 SOCH.sub.3 (+)-pin5035 CH.sub.2 NH.sub.2 PhCH.sub.2 H OH, OH5036 CH.sub.2 NH.sub.2 PhCH.sub.2 methyl OH, OH5037 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 CN OH, OH5038 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 COOH OH, OH5039 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 NC OH, OH5040 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 NO.sub.2 OH, OH5041 CH.sub.2 NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 OH OH, OH5042 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 SOCH.sub.3 OH, OH5043 NH(CNH)NH.sub.2 PhCH.sub.2 H (+)-pin5044 NH(CNH)NH.sub.2 PhCH.sub.2 methyl (+)-pin5045 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 CN (+)-pin5046 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 CN (+)-pin5047 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 COOH (+)-pin5048 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 COOH (+)-pin5049 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 NC (+)-pin5050 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 NO.sub.2 (+)-pin5051 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 OH (+)-pin5052 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 SOCH.sub.3 (+)-pin5053 NH(CNH)NH.sub.2 PhCH.sub.2 H OH, OH5054 NH(CNH)NH.sub.2 PhCH.sub.2 methyl OH, OH5055 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 CN OH, OH5056 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 CN OH, OH5057 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 COOH OH, OH5058 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 COOH OH, OH5059 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 NC OH, OH5060 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 NO.sub.2 OH, OH5061 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 OH OH, OH5062 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 SOCH.sub.3 OH, OH m = 05063 CH.sub.2 NH.sub.2 PhCH.sub.2 H (+)-pin5064 CH.sub.2 NH.sub.2 PhCH.sub.2 methyl (+)-pin5065 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 CN (+)-pin5066 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 COOH (+)-pin5067 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 NC (+)-pin5068 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 NO.sub.2 (+)-pin5069 CH.sub.2 NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 OH (+)-pin5070 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 SOCH.sub.3 (+)-pin5071 CH.sub.2 NH.sub.2 PhCH.sub.2 H OH, OH5072 CH.sub.2 NH.sub.2 PhCH.sub.2 methyl OH, OH5073 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 CN OH, OH5074 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 COOH OH, OH5075 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 NC OH, OH5076 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 NO.sub.2 OH, OH5077 CH.sub.2 NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 OH OH, OH5078 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 SOCH.sub.3 OH, OH5079 NH(CNH)NH.sub.2 PhCH.sub.2 H (+)-pin5080 NH(CNH)NH.sub.2 PhCH.sub.2 methyl (+)-pin5081 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 CN (+)-pin5082 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 CN (+)-pin5083 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 COOH (+)-pin5084 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 COOH (+)-pin5085 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 NC (+)-pin5086 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 NO.sub.2 (+)-pin5087 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 OH (+)-pin5088 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 SOCH.sub.3 (+)-pin5089 NH(CNH)NH.sub.2 PhCH.sub.2 H OH, OH5090 NH(CNH)NH.sub.2 PhCH.sub.2 methyl OH, OH5091 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 CN OH, OH5092 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 CN OH, OH5093 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 COOH OH, OH5094 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 COOH OH, OH5095 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 NC OH, OH5096 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 NO.sub.2 OH, OH5097 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 OH OH, OH5098 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 SOCH.sub.3 OH, OH______________________________________ TABLE 44______________________________________ ##STR139## Phys.Ex X R.sup.13 R.sup.14 Y.sup.1 Y.sup.2 Data______________________________________m = 15103 CH.sub.2 NH.sub.2 PhCH.sub.2 H (+)-pin5104 CH.sub.2 NH.sub.2 PhCH.sub.2 methyl (+)-pin5105 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 CN (+)-pin5106 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 COOH (+)-pin5107 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 NC (+)-pin5108 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 NO.sub.2 (+)-pin5109 CH.sub.2 NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 OH (+)-pin5110 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 SOCH.sub.3 (+)-pin5111 CH.sub.2 NH.sub.2 PhCH.sub.2 H OH, OH5112 CH.sub.2 NH.sub.2 PhCH.sub.2 methyl OH, OH5113 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 CN OH, OH5114 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 COOH OH, OH5115 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 NC OH, OH5116 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 NO.sub.2 OH, OH5117 CH.sub.2 NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 OH OH, OH5118 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 SOCH.sub.3 OH, OH5119 NH(CNH)NH.sub.2 PhCH.sub.2 H (+)-pin5120 NH(CNH)NH.sub.2 PhCH.sub.2 methyl (+)-pin5121 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 CN (+)-pin5122 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 CN (+)-pin5123 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 COOH (+)-pin5124 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 COOH (+)-pin5125 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 NC (+)-pin5126 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 NO.sub.2 (+)-pin5127 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 OH (+)-pin5128 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 SOCH.sub.3 (+)-pin5129 NH(CNH)NH.sub.2 PhCH.sub.2 H OH, OH5130 NH(CNH)NH.sub.2 PhCH.sub.2 methyl OH, OH5131 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 CN OH, OH5132 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 CN OH, OH5133 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 COOH OH, OH5134 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 COOH OH, OH5135 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 NC OH, OH5136 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 NO.sub.2 OH, OH5137 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 OH OH, OH5138 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 SOCH.sub.3 OH, OH m = 25139 CH.sub.2 NH.sub.2 PhCH.sub.2 H (+)-pin5140 CH.sub.2 NH.sub.2 PhCH.sub.2 methyl (+)-pin5141 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 CN (+)-pin5142 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 COOH (+)-pin5143 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 NC (+)-pin5144 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 NO.sub.2 (+)-pin5145 CH.sub.2 NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 OH (+)-pin5146 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 SOCH.sub.3 (+)-pin5147 CH.sub.2 NH.sub.2 PhCH.sub.2 H OH, OH5148 CH.sub.2 NH.sub.2 PhCH.sub.2 methyl OH, OH5149 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 CN OH, OH5150 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 COOH OH, OH5151 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 NC OH, OH5152 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 NO.sub.2 OH, OH5153 CH.sub.2 NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 OH OH, OH5154 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 SOCH.sub.3 OH, OH5155 NH(CNH)NH.sub.2 PhCH.sub.2 H (+)-pin5156 NH(CNH)NH.sub.2 PhCH.sub.2 methyl (+)-pin5157 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 CN (+)-pin5158 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 CN (+)-pin5159 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 COOH (+)-pin5160 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 COOH (+)-pin5161 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 NC (+)-pin5162 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 NO.sub.2 (+)-pin5163 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 OH (+)-pin5164 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 SOCH.sub.3 (+)-pin5165 NH(CNH)NH.sub.2 PhCH.sub.2 H OH, OH5166 NH(CNH)NH.sub.2 PhCH.sub.2 methyl OH, OH5167 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 CN OH, OH5168 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 CN OH, OH5169 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 COOH OH, OH5170 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 COOH OH, OH5171 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 NC OH, OH5172 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 NO.sub.2 OH, OH5173 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 OH OH, OH5174 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 SOCH.sub.3 OH, OH m = 05175 CH.sub.2 NH.sub.2 PhCH.sub.2 H (+)-pin5176 CH.sub.2 NH.sub.2 PhCH.sub.2 methyl (+)-pin5177 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 CN (+)-pin5178 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 COOH (+)-pin5179 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 NC (+)-pin5180 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 NO.sub.2 (+)-pin5181 CH.sub.2 NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 OH (+)-pin5182 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 SOCH.sub.3 (+)-pin5183 CH.sub.2 NH.sub.2 PhCH.sub.2 H OH, OH5184 CH.sub.2 NH.sub.2 PhCH.sub.2 methyl OH, OH5185 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 CN OH, OH5186 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 COOH OH, OH5187 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 NC OH, OH5188 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 NO.sub.2 OH, OH5189 CH.sub.2 NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 OH OH, OH5190 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 SOCH.sub.3 OH, OH5191 NH(CNH)NH.sub.2 PhCH.sub.2 H (+)-pin5192 NH(CNH)NH.sub.2 PhCH.sub.2 methyl (+)-pin5193 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 CN (+)-pin5194 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 CN (+)-pin5195 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 COOH (+)-pin5196 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 COOH (+)-pin5197 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 NC (+)-pin5198 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 NO.sub.2 (+)-pin5199 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 OH (+)-pin5200 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 SOCH.sub.3 (+)-pin5201 NH(CNH)NH.sub.2 PhCH.sub.2 H OH, OH5202 NH(CNH)NH.sub.2 PhCH.sub.2 methyl OH, OH5203 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 CN OH, OH5204 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 CN OH, OH5205 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 COOH OH, OH5206 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 COOH OH, OH5207 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 NC OH, OH5208 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 NO.sub.2 OH, OH5209 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 OH OH, OH5210 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 SOCH.sub.3 OH, OH______________________________________ TABLE 45______________________________________ ##STR140##Ex X R.sup.13 Y.sup.1 Y.sup.2 Phys. Data______________________________________m = 15215 CH.sub.2 NH.sub.2 PhCH.sub.2 (+)-pin5216 CH.sub.2 NH.sub.2 PhCH.sub.2 OH, OH5217 NH(CNH)NH.sub.2 PhCH.sub.2 (+)-pin5218 NH(CNH)NH.sub.2 PhCH.sub.2 OH, OH5219 OMe PhCH.sub.2 (+)-pin5220 OMe PhCH.sub.2 OH, OH5221 NH(CNH)H PhCH.sub.2 (+)-pin5222 NH(CNH)H PhCH.sub.2 OH, OH5223 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 (+)-pin5224 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 OH, OH5225 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 (+)-pin5226 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 OH, OH5227 OMe PhCH.sub.2 CH.sub.2 (+)-pin5228 OMe PhCH.sub.2 CH.sub.2 OH, OH5229 NH(CNH)H PhCH.sub.2 CH.sub.2 (+)-pin5230 NH(CNH)H PhCH.sub.2 CH.sub.2 OH, OH5231 CH.sub.2 NH.sub.2 Ph (+)-pin5232 CH.sub.2 NH.sub.2 Ph OH, OH5233 NH(CNH)NH.sub.2 Ph (+)-pin5234 NH(CNH)NH.sub.2 Ph OH, OH5235 OMe Ph (+)-pin5236 OMe Ph OH, OH5237 NH(CNH)H Ph (+)-pin5238 NH(CNH)H Ph OH, OH m = 05239 CH.sub.2 NH.sub.2 PhCH.sub.2 (+)-pin5240 CH.sub.2 NH.sub.2 PhCH.sub.2 OH, OH5241 NH(CNH)NH.sub.2 PhCH.sub.2 (+)-pin5242 NH(CNH)NH.sub.2 PhCH.sub.2 OH, OH5243 OMe PhCH.sub.2 (+)-pin5244 OMe PhCH.sub.2 OH, OH5245 NH(CNH)H PhCH.sub.2 (+)-pin5246 NH(CNH)H PhCH.sub.2 OH, OH5247 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 (+)-pin5248 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 OH, OH5249 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 (+)-pin5250 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 OH, OH5251 OMe PhCH.sub.2 CH.sub.2 (+)-pin5252 OMe PhCH.sub.2 CH.sub.2 OH, OH5253 NH(CNH)H PhCH.sub.2 CH.sub.2 (+)-pin5254 NH(CNH)H PhCH.sub.2 CH.sub.2 OH, OH5255 CH.sub.2 NH.sub.2 Ph (+)-pin5256 CH.sub.2 NH.sub.2 Ph OH, OH5257 NH(CNH)NH.sub.2 Ph (+)-pin5258 NH(CNH)NH.sub.2 Ph OH, OH5259 OMe Ph (+)-pin5260 OMe Ph OH, OH5261 NH(CNH)H Ph (+)-pin5262 NH(CNH)H Ph OH, OH______________________________________ TABLE 46______________________________________ ##STR141##Ex X R.sup.13 Y.sup.1 Y.sup.2 Phys. Data______________________________________m = 15267 CH.sub.2 NH.sub.2 PhCH.sub.2 (+)-pin5268 CH.sub.2 NH.sub.2 PhCH.sub.2 OH, OH5269 NH(CNH)NH.sub.2 PhCH.sub.2 (+)-pin5270 NH(CNH)NH.sub.2 PhCH.sub.2 OH, OH5271 OMe PhCH.sub.2 (+)-pin5272 OMe PhCH.sub.2 OH, OH5273 NH(CNH)H PhCH.sub.2 (+)-pin5274 NH(CNH)H PhCH.sub.2 OH, OH5275 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 (+)-pin5276 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 OH, OH5277 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 (+)-pin5278 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 OH, OH5279 OMe PhCH.sub.2 CH.sub.2 (+)-pin5280 OMe PhCH.sub.2 CH.sub.2 OH, OH5281 NH(CNH)H PhCH.sub.2 CH.sub.2 (+)-pin5282 NH(CNH)H PhCH.sub.2 CH.sub.2 OH, OH5283 CH.sub.2 NH.sub.2 Ph (+)-pin5284 CH.sub.2 NH.sub.2 Ph OH, OH5285 NH(CNH)NH.sub.2 Ph (+)-pin5286 NH(CNH)NH.sub.2 Ph OH, OH5287 OMe Ph (+)-pin5288 OMe Ph OH, OH5289 NH(CNH)H Ph (+)-pin5290 NH(CNH)H Ph OH, OH m = 05291 CH.sub.2 NH.sub.2 PhCH.sub.2 (+)-pin5292 CH.sub.2 NH.sub.2 PhCH.sub.2 OH, OH5293 NH(CNH)NH.sub.2 PhCH.sub.2 (+)-pin5294 NH(CNH)NH.sub.2 PhCH.sub.2 OH, OH5295 OMe PhCH.sub.2 (+)-pin5296 OMe PhCH.sub.2 OH, OH5297 NH(CNH)H PhCH.sub.2 (+)-pin5298 NH(CNH)H PhCH.sub.2 OH, OH5299 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 (+)-pin5300 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 OH, OH5301 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 (+)-pin5302 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 OH, OH5303 OMe PhCH.sub.2 CH.sub.2 (+)-pin5304 OMe PhCH.sub.2 CH.sub.2 OH, OH5305 NH(CNH)H PhCH.sub.2 CH.sub.2 (+)-pin5306 NH(CNH)H PhCH.sub.2 CH.sub.2 OH, OH5307 CH.sub.2 NH.sub.2 Ph (+)-pin5308 CH.sub.2 NH.sub.2 Ph OH, OH5309 NH(CNH)NH.sub.2 Ph (+)-pin5310 NH(CNH)NH.sub.2 Ph OH, OH5311 OMe Ph (+)-pin5312 OMe Ph OH, OH5313 NH(CNH)H Ph (+)-pin5314 NH(CNH)H Ph OH, OH______________________________________ TABLE 47______________________________________ ##STR142##Ex X R.sup.13 Y.sup.1 Y.sup.2 Phys. Data______________________________________m = 15319 CH.sub.2 NH.sub.2 PhCH.sub.2 (+)-pin5320 CH.sub.2 NH.sub.2 PhCH.sub.2 OH, OH5321 NH(CNH)NH.sub.2 PhCH.sub.2 (+)-pin5322 NH(CNH)NH.sub.2 PhCH.sub.2 OH, OH5323 OMe PhCH.sub.2 (+)-pin5324 OMe PhCH.sub.2 OH, OH5325 NH(CNH)H PhCH.sub.2 (+)-pin5326 NH(CNH)H PhCH.sub.2 OH, OH5327 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 (+)-pin5328 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 OH, OH5329 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 (+)-pin5330 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 OH, OH5331 OMe PhCH.sub.2 CH.sub.2 (+)-pin5332 OMe PhCH.sub.2 CH.sub.2 OH, OH5333 NH(CNH)H PhCH.sub.2 CH.sub.2 (+)-pin5334 NH(CNH)H PhCH.sub.2 CH.sub.2 OH, OH5335 CH.sub.2 NH.sub.2 Ph (+)-pin5336 CH.sub.2 NH.sub.2 Ph OH, OH5337 NH(CNH)NH.sub.2 Ph (+)-pin5338 NH(CNH)NH.sub.2 Ph OH, OH5339 OMe Ph (+)-pin5340 OMe Ph OH, OH5341 NH(CNH)H Ph (+)-pin5342 NH(CNH)H Ph OH, OH m = 05343 CH.sub.2 NH.sub.2 PhCH.sub.2 (+)-pin5344 CH.sub.2 NH.sub.2 PhCH.sub.2 OH, OH5345 NH(CNH)NH.sub.2 PhCH.sub.2 (+)-pin5346 NH(CNH)NH.sub.2 PhCH.sub.2 OH, OH5347 OMe PhCH.sub.2 (+)-pin5348 OMe PhCH.sub.2 OH, OH5349 NH(CNH)H PhCH.sub.2 (+)-pin5350 NH(CNH)H PhCH.sub.2 OH, OH5351 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 (+)-pin5352 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 OH, OH5353 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 (+)-pin5354 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 OH, OH5355 OMe PhCH.sub.2 CH.sub.2 (+)-pin5356 OMe PhCH.sub.2 CH.sub.2 OH, OH5357 NH(CNH)H PhCH.sub.2 CH.sub.2 (+)-pin5358 NH(CNH)H PhCH.sub.2 CH.sub.2 OH, OH5359 CH.sub.2 NH.sub.2 Ph (+)-pin5360 CH.sub.2 NH.sub.2 Ph OH, OH5361 NH(CNH)NH.sub.2 Ph (+)-pin5362 NH(CNH)NH.sub.2 Ph OH, OH5363 OMe Ph (+)-pin5364 OMe Ph OH, OH5365 NH(CNH)H Ph (+)-pin5366 NH(CNH)H Ph OH, OH______________________________________ TABLE 48__________________________________________________________________________ ##STR143## Phys.Ex X R.sup.13 R.sup.14 R.sup.15 Y.sup.1 Y.sup.2 Data__________________________________________________________________________5371 CH.sub.2 NH.sub.2 PhCH.sub.2 H H (+)-pin5372 CH.sub.2 NH.sub.2 PhCH.sub.2 H methyl (+)-pin5373 CH.sub.2 NH.sub.2 PhCH.sub.2 H CH.sub.2 CN (+)-pin5374 CH.sub.2 NH.sub.2 PhCH.sub.2 H CH.sub.2 COOH (+)-pin5375 CH.sub.2 NH.sub.2 PhCH.sub.2 H CH.sub.2 NC (+)-pin5376 CH.sub.2 NH.sub.2 PhCH.sub.2 H CH.sub.2 NO.sub.2 (+)-pin5377 CH.sub.2 NH.sub.2 PhCH.sub.2 H (CH.sub.2).sub.2 OH (+)-pin5378 CH.sub.2 NH.sub.2 PhCH.sub.2 H CH.sub.2 SOCH.sub.3 (+)-pin5379 CH.sub.2 NH.sub.2 PhCH.sub.2 H H OH, OH5380 CH.sub.2 NH.sub.2 PhCH.sub.2 H methyl OH, OH5381 CH.sub.2 NH.sub.2 PhCH.sub.2 H CH.sub.2 CN OH, OH5382 CH.sub.2 NH.sub.2 PhCH.sub.2 H CH.sub.2 COOH OH, OH5383 CH.sub.2 NH.sub.2 PhCH.sub.2 H CH.sub.2 NC OH, OH5384 CH.sub.2 NH.sub.2 PhCH.sub.2 H CH.sub.2 NO.sub.2 OH, OH5385 CH.sub.2 NH.sub.2 PhCH.sub.2 H (CH.sub.2).sub.2 OH OH, OH5386 CH.sub.2 NH.sub.2 PhCH.sub.2 H CH.sub.2 SOCH.sub.3 OH, OH5387 NH(CNH)NH.sub.2 PhCH.sub.2 H H (+)-pin5388 NH(CNH)NH.sub.2 PhCH.sub.2 H methyl (+)-pin5389 NH(CNH)NH.sub.2 PhCH.sub.2 H CH.sub.2 CN (+)-pin5390 NH(CNH)NH.sub.2 PhCH.sub.2 H CH.sub.2 COOH (+)-pin5391 NH(CNH)NH.sub.2 PhCH.sub.2 H CH.sub.2 NC (+)-pin5392 NH(CNH)NH.sub.2 PhCH.sub.2 H CH.sub.2 NO.sub.2 (+)-pin5393 NH(CNH)NH.sub.2 PhCH.sub.2 H (CH.sub.2).sub.2 OH (+)-pin5394 NH(CNH)NH.sub.2 PhCH.sub.2 H CH.sub.2 SOCH.sub.3 (+)-pin5395 NH(CNH)NH.sub.2 PhCH.sub.2 H H OH, OH5396 NH(CNH)NH.sub.2 PhCH.sub.2 H methyl OH, OH5397 NH(CNH)NH.sub.2 PhCH.sub.2 H CH.sub.2 CN OH, OH5398 NH(CNH)NH.sub.2 PhCH.sub.2 H CH.sub.2 COOH OH, OH5399 NH(CNH)NH.sub.2 PhCH.sub.2 H CH.sub.2 NC OH, OH5400 NH(CNH)NH.sub.2 PhCH.sub.2 H CH.sub.2 NO.sub.2 OH, OH5401 NH(CNH)NH.sub.2 PhCH.sub.2 H (CH.sub.2).sub.2 OH OH, OH5402 NH(CNH)NH.sub.2 PhCH.sub.2 H CH.sub.2 SOCH.sub.3 OH, OH5403 m = 05404 NH(CNH)NH.sub.2 H H 3-(t-butyl-O.sub.2 CNH)-Ph (+)-pin BS5405 NH(CNH)NH.sub.2 H H 3-(t-butyl-O.sub.2 CNH)-Ph OH, OH5406 NH(CNH)NH.sub.2 H H 3-(NH.sub.2)-Ph (+)-pin5407 NH(CNH)NH.sub.2 H H 3-(NH.sub.2)-Ph OH, OH5408 NH(CNH)NH.sub.2 H H 3-(CH.sub.3 SO.sub.2 NH)-Ph (+)-pin5409 NH(CNH)NH.sub.2 H H 3-(CH.sub.3 SO.sub.2 NH)-Ph OH, OH5410 NH(CNH)NH.sub.2 H methyl Ph (+)-pin5411 NH(CNH)NH.sub.2 H methyl Ph OH, OH5412 NH(CNH)NH.sub.2 H CH.sub.2 CN Ph (+)-pin5413 NH(CNH)NH.sub.2 H CH.sub.2 CN Ph OH, OH5414 NH(CNH)NH.sub.2 H methyl 3-(CH.sub.3 SO.sub.2 NH)-Ph (+)-pin5415 NH(CNH)NH.sub.2 H methyl 3-(CH.sub.3 SO.sub.2 NH)-Ph OH, OH5416 NH(CNH)NH.sub.2 H CH.sub.3 2-(CH.sub.3 SO.sub.2 NH)-Ph (+)-pin5417 NH(CNH)NH.sub.2 H CH.sub.3 2-(CH.sub.3 SO.sub.2 NH)-Ph OH, OH5418 NH(CNH)NH.sub.2 H CH.sub.2 CN 3-(CH.sub.3 SO.sub.2 NH)-Ph (+)-pin5419 NH(CNH)NH.sub.2 H CH.sub.2 CN 3-(CH.sub.3 SO.sub.2 NH)-Ph OH, OH5420 NH(CNH)NH.sub.2 H CH.sub.2 CN 2-(CH.sub.3 SO.sub.2 NH)-Ph (+)-pin5421 NH(CNH)NH.sub.2 H CH.sub.2 CN 2-(CH.sub.3 SO.sub.2 NH)-Ph OH, OH5422 NH(CNH)NH.sub.2 H CH.sub.2 COOH 3-(CH.sub.3 SO.sub.2 NH)-Ph (+)-pin5423 NH(CNH)NH.sub.2 H CH.sub.2 COOH 3-(CH.sub.3 SO.sub.2 NH)-Ph OH, OH5424 NH(CNH)NH.sub.2 H CH.sub.2 COOH 2-(CH.sub.3 SO.sub.2 NH)-Ph (+)-pin5425 NH(CNH)NH.sub.2 H CH.sub.2 COOH 2-(CH.sub.3 SO.sub.2 NH)-Ph OH, OH5426 NH(CNH)NH.sub.2 H H 3-(t-butylOCONH)-Ph (+)-pin BP__________________________________________________________________________ BP. MS (M+H)+: Calc 610, Found 610. BS. MS (M+H)+: Calc 610, Found 610. TABLE 49______________________________________ ##STR144## Phys.Ex X R.sup.13 R.sup.14 Y.sup.1 Y.sup.2 Data______________________________________m = 15431 CH.sub.2 NH.sub.2 PhCH.sub.2 H (+)-pin5432 CH.sub.2 NH.sub.2 PhCH.sub.2 methyl (+)-pin5433 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 CN (+)-pin5434 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 COOH (+)-pin5435 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 NC (+)-pin5436 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 NO.sub.2 (+)-pin5437 CH.sub.2 NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 OH (+)-pin5438 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 SOCH.sub.3 (+)-pin5439 CH.sub.2 NH.sub.2 PhCH.sub.2 H OH, OH5440 CH.sub.2 NH.sub.2 PhCH.sub.2 methyl OH, OH5441 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 CN OH, OH5442 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 COOH OH, OH5443 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 NC OH, OH5444 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 NO.sub.2 OH, OH5445 CH.sub.2 NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 OH OH, OH5446 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 SOCH.sub.3 OH, OH5447 NH(CNH)NH.sub.2 PhCH.sub.2 H (+)-pin5448 NH(CNH)NH.sub.2 PhCH.sub.2 methyl (+)-pin5449 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 CN (+)-pin5450 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 COOH (+)-pin5451 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 NC (+)-pin5452 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 NO.sub.2 (+)-pin5453 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 OH (+)-pin5454 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 SOCH.sub.3 (+)-pin5455 NH(CNH)NH.sub.2 PhCH.sub.2 H OH, OH5456 NH(CNH)NH.sub.2 PhCH.sub.2 methyl OH, OH5457 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 CN OH, OH5458 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 COOH OH, OH5459 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 NC OH, OH5460 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 NO.sub.2 OH, OH5461 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 OH OH, OH5462 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 SOCH.sub.3 OH, OH m = 05463 CH.sub.2 NH.sub.2 PhCH.sub.2 H (+)-pin5464 CH.sub.2 NH.sub.2 PhCH.sub.2 methyl (+)-pin5465 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 CN (+)-pin5466 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 COOH (+)-pin5465 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 NC (+)-pin5466 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 NO.sub.2 (+)-pin5467 CH.sub.2 NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 OH (+)-pin5468 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 SOCH.sub.3 (+)-pin5469 CH.sub.2 NH.sub.2 PhCH.sub.2 H OH, OH5470 CH.sub.2 NH.sub.2 PhCH.sub.2 methyl OH, OH5471 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 CN OH, OH5472 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 COOH OH, OH5473 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 NC OH, OH5474 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 NO.sub.2 OH, OH5475 CH.sub.2 NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 OH OH, OH5476 CH.sub.2 NH.sub.2 PhCH.sub.2 CH.sub.2 SOCH.sub.3 OH, OH5477 NH(CNH)NH.sub.2 PhCH.sub.2 H (+)-pin5478 NH(CNH)NH.sub.2 PhCH.sub.2 methyl (+)-pin5479 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 CN (+)-pin5480 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 COOH (+)-pin5481 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 NC (+)-pin5482 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 NO.sub.2 (+)-pin5483 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 OH (+)-pin5484 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 SOCH.sub.3 (+)-pin5485 NH(CNH)NH.sub.2 PhCH.sub.2 H OH, OH5486 NH(CNH)NH.sub.2 PhCH.sub.2 methyl OH, OH5487 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 CN OH, OH5488 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 COOH OH, OH5489 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 NC OH, OH5490 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 NO.sub.2 OH, OH5491 NH(CNH)NH.sub.2 PhCH.sub.2 (CH.sub.2).sub.2 OH OH, OH5492 NH(CNH)NH.sub.2 PhCH.sub.2 CH.sub.2 SOCH.sub.3 OH, OH______________________________________ TABLE 50__________________________________________________________________________ ##STR145## Phys.Ex X R.sup.13 R.sup.14 R.sup.15 Y.sup.1 Y.sup.2 Data__________________________________________________________________________5497 CH.sub.2 NH.sub.2 PhCH.sub.2 H H (+)-pin5498 CH.sub.2 NH.sub.2 PhCH.sub.2 H methyl (+)-pin5499 CH.sub.2 NH.sub.2 PhCH.sub.2 H CH.sub.2 CN (+)-pin5500 CH.sub.2 NH.sub.2 PhCH.sub.2 H CH.sub.2 COOH (+)-pin5501 CH.sub.2 NH.sub.2 PhCH.sub.2 H CH.sub.2 NC (+)-pin5502 CH.sub.2 NH.sub.2 PhCH.sub.2 H CH.sub.2 NO.sub.2 (+)-pin5503 CH.sub.2 NH.sub.2 PhCH.sub.2 H (CH.sub.2).sub.2 OH (+)-pin5504 CH.sub.2 NH.sub.2 PhCH.sub.2 H CH.sub.2 SOCH.sub.3 (+)-pin5505 CH.sub.2 NH.sub.2 PhCH.sub.2 H H OH, OH5506 CH.sub.2 NH.sub.2 PhCH.sub.2 H methyl OH, OH5507 CH.sub.2 NH.sub.2 PhCH.sub.2 H CH.sub.2 CN OH, OH5508 CH.sub.2 NH.sub.2 PhCH.sub.2 H CH.sub.2 COOH OH, OH5509 CH.sub.2 NH.sub.2 PhCH.sub.2 H CH.sub.2 NC OH, OH5510 CH.sub.2 NH.sub.2 PhCH.sub.2 H CH.sub.2 NO.sub.2 OH, OH5511 CH.sub.2 NH.sub.2 PhCH.sub.2 H (CH.sub.2).sub.2 OH OH, OH5512 CH.sub.2 NH.sub.2 PhCH.sub.2 H CH.sub.2 SOCH.sub.3 OH, OH5513 NH(CNH)NH.sub.2 PhCH.sub.2 H H (+)-pin5514 NH(CNH)NH.sub.2 PhCH.sub.2 H methyl (+)-pin5515 NH(CNH)NH.sub.2 PhCH.sub.2 H CH.sub.2 CN (+)-pin5516 NH(CNH)NH.sub.2 PhCH.sub.2 H CH.sub.2 COOH (+)-pin5517 NH(CNH)NH.sub.2 PhCH.sub.2 H CH.sub.2 NC (+)-pin5518 NH(CNH)NH.sub.2 PhCH.sub.2 H CH.sub.2 NO.sub.2 (+)-pin5519 NH(CNH)NH.sub.2 PhCH.sub.2 H (CH.sub.2).sub.2 OH (+)-pin5520 NH(CNH)NH.sub.2 PhCH.sub.2 H CH.sub.2 SOCH.sub.3 (+)-pin5521 NH(CNH)NH.sub.2 PhCH.sub.2 H H OH, OH5522 NH(CNH)NH.sub.2 PhCH.sub.2 H methyl OH, OH5523 NH(CNH)NH.sub.2 PhCH.sub.2 H CH.sub.2 CN OH, OH5524 NH(CNH)NH.sub.2 PhCH.sub.2 H CH.sub.2 COOH OH, OH5525 NH(CNH)NH.sub.2 PhCH.sub.2 H CH.sub.2 NC OH, OH5526 NH(CNH)NH.sub.2 PhCH.sub.2 H CH.sub.2 NO.sub.2 OH, OH5527 NH(CNH)NH.sub.2 PhCH.sub.2 H (CH.sub.2).sub.2 OH OH, OH5528 NH(CNH)NH.sub.2 PhCH.sub.2 H CH.sub.2 SOCH.sub.3 OH, OH m = 05529 NH(CNH)NH.sub.2 H H 3-(t-butyl-O.sub.2 CNH)-Ph (+)-pin BT5530 NH(CNH)NH.sub.2 H H 3-(t-butyl-O.sub.2 CNH)-Ph OH, OH5531 NH(CNH)NH.sub.2 H H 3-(NH.sub.2)-Ph (+)-pin5532 NH(CNH)NH.sub.2 H H 3-(NH.sub.2)-Ph OH, OH5533 NH(CNH)NH.sub.2 H H 3-(CH.sub.3 SO.sub.2 NH)-Ph (+)-pin5534 NH(CNH)NH.sub.2 H H 3-(CH.sub.3 SO.sub.2 NH)-Ph OH, OH5535 NH(CNH)NH.sub.2 H H Ph (+)-pin BU5536 NH(CNH)NH.sub.2 H H Ph OH, OH BV5537 NH(CNH)NH.sub.2 H CH.sub.3 Ph (+)-pin5538 NH(CNH)NH.sub.2 H CH.sub.3 Ph OH, OH5539 NH(CNH)NH.sub.2 H CH.sub.2 CN Ph (+)-pin5540 NH(CNH)NH.sub.2 H CH.sub.2 CN Ph OH, OH5541 NH(CNH)NH.sub.2 H CH.sub.2 COOH Ph (+)-pin5542 NH(CNH)NH.sub.2 H CH.sub.2 COOH Ph OH, OH5543 NH(CNH)NH.sub.2 H CH.sub.2 SO.sub.2 NH.sub.2 Ph (+)-pin5544 NH(CNH)NH.sub.2 H CH.sub.2 SO.sub.2 NH.sub.2 Ph OH, OH5545 NH(CNH)NH H CH.sub.2 CN 3-(CH.sub.3 SO.sub.2 NH)-Ph (+)-pin5546 NH(CNH)NH H CH.sub.2 CN 3-(CH.sub.3 SO.sub.2 NH)-Ph OH, OH5547 NH(CNH)NH H CH.sub.2 COOH 3-(CH.sub.3 SO.sub.2 NH)-Ph (+)-pin5548 NH(CNH)NH H CH.sub.2 COOH 3-(CH.sub.3 SO.sub.2 NH)-Ph OH, OH5549 NH(CNH)NH H CH.sub.2 COOH 2-(CH.sub.3 SO.sub.2 NH)-Ph (+)-pin5550 NH(CNH)NH H CH.sub.2 COOH 2-(CH.sub.3 SO.sub.2 NH)-Ph OH, OH5551 NH(CNH)NH.sub.2 H H 3-(t-butylOCONH)-Ph (+)-pin BO5552 NH(CNH)NH.sub.2 H H Ph (+)-pin BQ5553 NH(CNH)NH.sub.2 H H Ph OH BR__________________________________________________________________________ BO. MS (M+H).sup.+ : Calc. 594, Found 594. BQ. MS (M+H).sup.+ : Calc. 479, Found 479. BS. MS (M+H).sup.+ : Calc. 345, Found 345. BT. MS (M+H).sup.+ : Calc. 594, Found 594. BU. MS (M+H).sup.+ : Calc. 479, Found 479. BV. MS (M+H).sup.+ : Calc. 345, Found 345. TABLE 51__________________________________________________________________________ ##STR146## Phys.Ex X R.sup.13 R.sup.14 R.sup.15 Y.sup.1 Y.sup.2 Data__________________________________________________________________________m = 15558 CH.sub.2 NH.sub.2 PhCH.sub.2 H H (+)-pin5559 CH.sub.2 NH.sub.2 PhCH.sub.2 H methyl (+)-pin5560 CH.sub.2 NH.sub.2 PhCH.sub.2 H CH.sub.2 CN (+)-pin5561 CH.sub.2 NH.sub.2 PhCH.sub.2 H CH.sub.2 COOH (+)-pin5562 CH.sub.2 NH.sub.2 PhCH.sub.2 H CH.sub.2 NC (+)-pin5563 CH.sub.2 NH.sub.2 PhCH.sub.2 H CH.sub.2 NO.sub.2 (+)-pin5564 CH.sub.2 NH.sub.2 PhCH.sub.2 H (CH.sub.2).sub.2 OH (+)-pin5565 CH.sub.2 NH.sub.2 PhCH.sub.2 H CH.sub.2 SOCH.sub.3 (+)-pin5566 CH.sub.2 NH.sub.2 PhCH.sub.2 H H OH, OH5567 CH.sub.2 NH.sub.2 PhCH.sub.2 H methyl OH, OH5568 CH.sub.2 NH.sub.2 PhCH.sub.2 H CH.sub.2 CN OH, OH5569 CH.sub.2 NH.sub.2 PhCH.sub.2 H CH.sub.2 COOH OH, OH5570 CH.sub.2 NH.sub.2 PhCH.sub.2 H CH.sub.2 NC OH, OH5571 CH.sub.2 NH.sub.2 PhCH.sub.2 H CH.sub.2 NO.sub.2 OH, OH5572 CH.sub.2 NH.sub.2 PhCH.sub.2 H (CH.sub.2).sub.2 OH OH, OH5573 CH.sub.2 NH.sub.2 PhCH.sub.2 H CH.sub.2 SOCH.sub.3 OH, OH5574 NH(CNH)NH.sub.2 PhCH.sub.2 H H (+)-pin5575 NH(CNH)NH.sub.2 PhCH.sub.2 H methyl (+)-pin5576 NH(CNH)NH.sub.2 PhCH.sub.2 H CH.sub.2 CN (+)-pin5577 NH(CNH)NH.sub.2 PhCH.sub.2 H CH.sub.2 COOH (+)-pin5578 NH(CNH)NH.sub.2 PhCH.sub.2 H CH.sub.2 NC (+)-pin5579 NH(CNH)NH.sub.2 PhCH.sub.2 H CH.sub.2 NO.sub.2 (+)-pin5580 NH(CNH)NH.sub.2 PhCH.sub.2 H (CH.sub.2).sub.2 OH (+)-pin5581 NH(CNH)NH.sub.2 PhCH.sub.2 H CH.sub.2 SOCH.sub.3 (+)-pin5582 NH(CNH)NH.sub.2 PhCH.sub.2 H H OH, OH5583 NH(CNH)NH.sub.2 PhCH.sub.2 H methyl OH, OH5584 NH(CNH)NH.sub.2 PhCH.sub.2 H CH.sub.2 CN OH, OH5585 NH(CNH)NH.sub.2 PhCH.sub.2 H CH.sub.2 COOH OH, OH5586 NH(CNH)NH.sub.2 PhCH.sub.2 H CH.sub.2 NC OH, OH5587 NH(CNH)NH.sub.2 PhCH.sub.2 H CH.sub.2 NO.sub.2 OH, OH5588 NH(CNH)NH.sub.2 PhCH.sub.2 H (CH.sub.2).sub.2 OH OH, OH5589 NH(CNH)NH.sub.2 PhCH.sub.2 H CH.sub.2 SOCH.sub.3 OH, OHm = 05590 CH.sub.2 NH.sub.2 PhCH.sub.2 H H (+)-pin5591 CH.sub.2 NH.sub.2 PhCH.sub.2 H methyl (+)-pin5592 CH.sub.2 NH.sub.2 PhCH.sub.2 H CH.sub.2 CN (+)-pin5593 CH.sub.2 NH.sub.2 PhCH.sub.2 H CH.sub.2 COOH (+)-pin5594 CH.sub.2 NH.sub.2 PhCH.sub.2 H CH.sub.2 NC (+)-pin5595 CH.sub.2 NH.sub.2 PhCH.sub.2 H CH.sub.2 NO.sub.2 (+)-pin5596 CH.sub.2 NH.sub.2 PhCH.sub.2 H (CH.sub.2).sub.2 OH (+)-pin5597 CH.sub.2 NH.sub.2 PhCH.sub.2 H CH.sub.2 SOCH.sub.3 (+)-pin5598 CH.sub.2 NH.sub.2 PhCH.sub.2 H H OH, OH5599 CH.sub.2 NH.sub.2 PhCH.sub.2 H methyl OH, OH5600 CH.sub.2 NH.sub.2 PhCH.sub.2 H CH.sub.2 CN OH, OH5601 CH.sub.2 NH.sub.2 PhCH.sub.2 H CH.sub.2 COOH OH, OH5602 CH.sub.2 NH.sub.2 PhCH.sub.2 H CH.sub.2 NC OH, OH5603 CH.sub.2 NH.sub.2 PhCH.sub.2 H CH.sub.2 NO.sub.2 OH, OH5604 CH.sub.2 NH.sub.2 PhCH.sub.2 H (CH.sub.2).sub.2 OH OH, OH5605 CH.sub.2 NH.sub.2 PhCH.sub.2 H CH.sub.2 SOCH.sub.3 OH, OH5606 NH(CNH)NH.sub.2 PhCH.sub.2 H H (+)-pin5607 NH(CNH)NH.sub.2 PhCH.sub.2 H methyl (+)-pin5608 NH(CNH)NH.sub.2 PhCH.sub.2 H CH.sub.2 CN (+)-pin5609 NH(CNH)NH.sub.2 PhCH.sub.2 H CH.sub.2 COOH (+)-pin5610 NH(CNH)NH.sub.2 PhCH.sub.2 H CH.sub.2 NC (+)-pin5611 NH(CNH)NH.sub.2 PhCH.sub.2 H CH.sub.2 NO.sub.2 (+)-pin5612 NH(CNH)NH.sub.2 PhCH.sub.2 H (CH.sub.2).sub.2 OH (+)-pin5613 NH(CNH)NH.sub.2 PhCH.sub.2 H CH.sub.2 SOCH.sub.3 (+)-pin5614 NH(CNH)NH.sub.2 PhCH.sub.2 H H OH, OH5615 NH(CNH)NH.sub.2 PhCH.sub.2 H methyl OH, OH5616 NH(CNH)NH.sub.2 PhCH.sub.2 H CH.sub.2 CN OH, OH5617 NH(CNH)NH.sub.2 PhCH.sub.2 H CH.sub.2 COOH OH, OH5618 NH(CNH)NH.sub.2 PhCH.sub.2 H CH.sub.2 NC OH, OH5619 NH(CNH)NH.sub.2 PhCH.sub.2 H CH.sub.2 NO.sub.2 OH, OH5620 NH(CNH)NH.sub.2 PhCH.sub.2 H (CH.sub.2).sub.2 OH OH, OH5621 NH(CNH)NH.sub.2 PhCH.sub.2 H CH.sub.2 SOCH.sub.3 OH, OH__________________________________________________________________________ TABLE 52__________________________________________________________________________ ##STR147##Ex X R.sup.13 R.sup.14 Y.sup.1 Y.sup.2 Phys. Data__________________________________________________________________________m = 15626 CH.sub.2 NH.sub.2 H H (+)-pin5627 CH.sub.2 NH.sub.2 H methyl (+)-pin5628 CH.sub.2 NH.sub.2 H H OH, OH5629 CH.sub.2 NH.sub.2 H methyl OH, OH5630 CH.sub.2 NH.sub.2 H CH.sub.2 CN (+)-pin5631 CH.sub.2 NH.sub.2 H (CH.sub.2).sub.2 COOH (+)-pin5632 CH.sub.2 NH.sub.2 H CH.sub.2 CN OH, OH5633 CH.sub.2 NH.sub.2 H (CH.sub.2 ).sub.2 COOH OH, OH5634 CH.sub.2 NH.sub.2 H CH.sub.2 COOMe (+)-pin5635 CH.sub.2 NH.sub.2 H (CH.sub.2)COOH (+)-pin5636 CH.sub.2 NH.sub.2 H CH.sub.2 COOMe OH, OH5637 CH.sub.2 NH.sub.2 H (CH.sub.2)COOH OH, OH5638 CH.sub.2 NH.sub.2 H (CH.sub.2).sub.2 CN.sub.4 H (+)-pin5639 CH.sub.2 NH.sub.2 H (CH.sub.2)CN.sub.4 H (+)-pin5640 CH.sub.2 NH.sub.2 H (CH.sub.2).sub.2 CN.sub.4 H OH, OH5641 CH.sub.2 NH.sub.2 H (CH.sub.2)CN.sub.4 H OH, OH5642 NH(CNH)NH.sub.2 H H (+)-pin5643 NH(CNH)NH.sub.2 H methyl (+)-pin5644 NH(CNH)NH.sub.2 H H OH, OH5645 NH(CNH)NH.sub.2 H methyl OH, OH5646 NH(CNH)NH.sub.2 H CH.sub.2 CN (+)-pin5647 NH(CNH)NH.sub.2 H (CH.sub.2).sub.2 COOH (+)-pin5648 NH(CNH)NH.sub.2 H CH.sub.2 CN OH, OH5649 NH(CNH)NH.sub.2 H (CH.sub.2 ).sub.2 COOH OH, OH5650 NH(CNH)NH.sub.2 H CH.sub.2 COOMe (+)-pin5651 NH(CNH)NH.sub.2 H (CH.sub.2)COOH (+)-pin5652 NH(CNH)NH.sub.2 H CH.sub.2 COOMe OH, OH5653 NH(CNH)NH.sub.2 H (CH.sub.2)COOH OH, OH5654 NH(CNH)NH.sub.2 H (CH.sub.2).sub.2 CN.sub.4 H (+)-pin5655 NH(CNH)NH.sub.2 H (CH.sub.2)CN.sub.4 H (+)-pin5656 NH(CNH)NH.sub.2 H (CH.sub.2).sub.2 CN.sub.4 H OH, OH5657 NH(CNH)NH.sub.2 H (CH.sub.2)CN.sub.4 H OH, OH5658 OMe H H (+)-pin5659 OMe H H OH, OH5660 NH(CNH)H H H (+)-pin5661 NH(CNH)H H H OH, OH5662 CH.sub.2 NH.sub.2 CH.sub.2 CN H (+)-pin5663 CH.sub.2 NH.sub.2 CH.sub.2 CN H OH, OH5664 NH(CNH)NH.sub.2 (CH.sub.2).sub.2 COOH H (+)-pin5665 NH(CNH)NH.sub.2 (CH.sub.2).sub.2 COOH H OH, OH5666 OMe CH.sub.2 COOMe H (+)-pin5667 OMe CH.sub.2 COOMe H OH, OH5668 NH(CNH)H (CH.sub.2).sub.2 CN.sub.4 H H OH, OH5669 NH(CNH)H (CH.sub.2).sub.2 CN.sub.4 H H (+)-pinm = 15670 CH.sub.2 NH.sub.2 H H (+)-pin5671 CH.sub.2 NH.sub.2 H methyl (+)-pin5672 CH.sub.2 NH.sub.2 H H OH, OH5673 CH.sub.2 NH.sub.2 H methyl OH, OH5674 CH.sub.2 NH.sub.2 H CH.sub.2 CN (+)-pin5675 CH.sub.2 NH.sub.2 H (CH.sub.2).sub.2 COOH (+)-pin5676 CH.sub.2 NH.sub.2 H CH.sub.2 CN OH, OH5677 CH.sub.2 NH.sub.2 H (CH.sub.2 ).sub.2 COOH OH, OH5678 CH.sub.2 NH.sub.2 H CH.sub.2 COOMe (+)-pin5679 CH.sub.2 NH.sub.2 H (CH.sub.2)COOH (+)-pin5680 CH.sub.2 NH.sub.2 H CH.sub.2 COOMe OH, OH5681 CH.sub.2 NH.sub.2 H (CH.sub.2)COOH OH, OH5682 CH.sub.2 NH.sub.2 H (CH.sub.2).sub.2 CN.sub.4 H (+)-pin5683 CH.sub.2 NH.sub.2 H (CH.sub.2)CN.sub.4 H (+)-pin5684 CH.sub.2 NH.sub.2 H (CH.sub.2).sub.2 CN.sub.4 H OH, OH5685 CH.sub.2 NH.sub.2 H (CH.sub.2)CN.sub.4 H OH, OH5686 NH(CNH)NH.sub.2 H H (+)-pin5687 NH(CNH)NH.sub.2 H methyl (+)-pin5688 NH(CNH)NH.sub.2 H H OH, OH5689 NH(CNH)NH.sub.2 H methyl OH, OH5690 NH(CNH)NH.sub.2 H CH.sub.2 CN (+)-pin5691 NH(CNH)NH.sub.2 H (CH.sub.2).sub.2 COOH (+)-pin5692 NH(CNH)NH.sub.2 H CH.sub.2 CN OH, OH5693 NH(CNH)NH.sub.2 H (CH.sub.2 ).sub.2 COOH OH, OH5694 NH(CNH)NH.sub.2 H CH.sub.2 COOMe (+)-pin5695 NH(CNH)NH.sub.2 H (CH.sub.2)COOH (+)-pin5696 NH(CNH)NH.sub.2 H CH.sub.2 COOMe OH, OH5697 NH(CNH)NH.sub.2 H (CH.sub.2)COOH OH, OH5698 NH(CNH)NH.sub.2 H (CH.sub.2).sub.2 CN.sub.4 H (+)-pin5699 NH(CNH)NH.sub.2 H (CH.sub.2)CN.sub.4 H (+)-pin5700 NH(CNH)NH.sub.2 H (CH.sub.2).sub.2 CN.sub.4 H OH, OH5701 NH(CNH)NH.sub.2 H (CH.sub.2)CN.sub.4 H OH, OH5702 OMe H H (+)-pin5703 OMe H H OH, OH5704 NH(CNH)H H H (+)-pin5705 NH(CNH)H H H OH, OH5706 CH.sub.2 NH.sub.2 CH.sub.2 CN H (+)-pin5707 CH.sub.2 NH.sub.2 CH.sub.2 CN H OH, OH5708 NH(CNH)NH.sub.2 (CH.sub.2).sub.2 COOH H (+)-pin5709 NH(CNH)NH.sub.2 (CH.sub.2).sub.2 COOH H OH, OH5710 OMe CH.sub.2 COOMe H (+)-pin5711 OMe CH.sub.2 COOMe H OH, OH5712 NH(CNH)H (CH.sub.2).sub.2 CN.sub.4 H H OH, OH5713 NH(CNH)H (CH.sub.2).sub.2 CN.sub.4 H H (+)-pinm = 05714 CH.sub.2 NH.sub.2 H H (+)-pin5715 CH.sub.2 NH.sub.2 H methyl (+)-pin5716 CH.sub.2 NH.sub.2 H H OH, OH5717 CH.sub.2 NH.sub.2 H methyl OH, OH5718 CH.sub.2 NH.sub.2 H CH.sub.2 CN (+)-pin5719 CH.sub.2 NH.sub.2 H (CH.sub.2).sub.2 COOH (+)-pin5720 CH.sub.2 NH.sub.2 H CH.sub.2 CN OH, OH5721 CH.sub.2 NH.sub.2 H (CH.sub.2 ).sub.2 COOH OH, OH5722 CH.sub.2 NH.sub.2 H CH.sub.2 COOMe (+)-pin5723 CH.sub.2 NH.sub.2 H (CH.sub.2)COOH (+)-pin5724 CH.sub.2 NH.sub.2 H CH.sub.2 COOMe OH, OH5725 CH.sub.2 NH.sub.2 H (CH.sub.2)COOH OH, OH5726 CH.sub.2 NH.sub.2 H (CH.sub.2).sub.2 CN.sub.4 H (+)-pin5727 CH.sub.2 NH.sub.2 H (CH.sub.2)CN.sub.4 H (+)-pin5728 CH.sub.2 NH.sub.2 H (CH.sub.2).sub.2 CN.sub.4 H OH, OH5729 CH.sub.2 NH.sub.2 H (CH.sub.2)CN.sub.4 H OH, OH5730 NH(CNH)NH.sub.2 H H (+)-pin5731 NH(CNH)NH.sub.2 H methyl (+)-pin5732 NH(CNH)NH.sub.2 H H OH, OH5733 NH(CNH)NH.sub.2 H methyl OH, OH5734 NH(CNH)NH.sub.2 H CH.sub.2 CN (+)-pin5735 NH(CNH)NH.sub.2 H (CH.sub.2).sub.2 COOH (+)-pin5736 NH(CNH)NH.sub.2 H CH.sub.2 CN OH, OH5737 NH(CNH)NH.sub.2 H (CH.sub.2 ).sub.2 COOH OH, OH5738 NH(CNH)NH.sub.2 H CH.sub.2 COOMe (+)-pin5739 NH(CNH)NH.sub.2 H (CH.sub.2)COOH (+)-pin5740 NH(CNH)NH.sub.2 H CH.sub.2 COOMe OH, OH5741 NH(CNH)NH.sub.2 H (CH.sub.2)COOH OH, OH5742 NH(CNH)NH.sub.2 H (CH.sub.2).sub.2 CN.sub.4 H (+)-pin5743 NH(CNH)NH.sub.2 H (CH.sub.2)CN.sub.4 H (+)-pin5744 NH(CNH)NH.sub.2 H (CH.sub.2).sub.2 CN.sub.4 H OH, OH5745 NH(CNH)NH.sub.2 H (CH.sub.2)CN.sub.4 H OH, OH5746 OMe H H (+)-pin5747 OMe H H OH, OH5748 NH(CNH)H H H (+)-pin5749 NH(CNH)H H H OH, OH5750 CH.sub.2 NH.sub.2 CH.sub.2 CN H (+)-pin5751 CH.sub.2 NH.sub.2 CH.sub.2 CN H OH, OH5752 NH(CNH)NH.sub.2 (CH.sub.2).sub.2 COOH H (+)-pin5753 NH(CNH)NH.sub.2 (CH.sub.2).sub.2 COOH H OH, OH5754 OMe CH.sub.2 COOMe H (+)-pin5755 OMe CH.sub.2 COOMe H OH, OH5756 NH(CNH)H (CH.sub.2).sub.2 CN.sub.4 H H OH, OH5757 NH(CNH)H (CH.sub.2).sub.2 CN.sub.4 H H (+)-pin__________________________________________________________________________ TABLE 53______________________________________ ##STR148##Ex X R.sup.13 R.sup.14 Y.sup.1 Y.sup.2 Phys. Data______________________________________5762 CH.sub.2 NH.sub.2 H H (+)-pin5763 CH.sub.2 NH.sub.2 H H OH, OH5764 NH(CNH)NH.sub.2 H H (+)-pin5765 NH(CNH)NH.sub.2 H H OH, OH5766 OMe H H (+)-pin5767 OMe H H OH, OH5768 NH(CNH)H H H OH, OH5769 NH(CNH)H H H (+)-pin5770 CH.sub.2 NH.sub.2 CH.sub.2 CN H (+)-pin5771 CH.sub.2 NH.sub.2 CH.sub.2 CN H OH, OH5772 NH(CNH)NH.sub.2 (CH.sub.2)COOH H (+)-pin5773 NH(CNH)NH.sub.2 (CH.sub.2)COOH H OH, OH5774 OMe CH.sub.2 COOMe H (+)-pin5775 OMe CH.sub.2 COOMe H OH, OH5776 NH(CNH)H (CH.sub.2)CN.sub.4 H H OH, OH5777 NH(CNH)H (CH.sub.2)CN.sub.4 H H (+)-pin______________________________________ TABLE 54______________________________________ ##STR149##Ex X R.sup.13 R.sup.14 Y.sup.1 Y.sup.2 Phys. Data______________________________________5782 CH.sub.2 NH.sub.2 H H (+)-pin5783 CH.sub.2 NH.sub.2 H H OH, OH5784 NH(CNH)NH.sub.2 H H (+)-pin5785 NH(CNH)NH.sub.2 H H OH, OH5786 OMe H H (+)-pin5787 OMe H H OH, OH5788 NH(CNH)H H H OH, OH5789 NH(CNH)H H H (+)-pin5790 CH.sub.2 NH.sub.2 CH.sub.2 CN H (+)-pin5791 CH.sub.2 NH.sub.2 CH.sub.2 CN H OH, OH5792 NH(CNH)NH.sub.2 (CH.sub.2)COOH H (+)-pin5793 NH(CNH)NH.sub.2 (CH.sub.2)COOH H OH, OH5794 OMe CH.sub.2 COOMe H (+)-pin5795 OMe CH.sub.2 COOMe H OH, OH5796 NH(CNH)H (CH.sub.2)CN.sub.4 H H OH, OH5797 NH(CNH)H (CH.sub.2)CN.sub.4 H H (+)-pin______________________________________ TABLE 55______________________________________ ##STR150##Ex X R.sup.13 R.sup.14 Y.sup.1 Y.sup.2 Phys. Data______________________________________5802 CH.sub.2 NH.sub.2 H H (+)-pin5803 CH.sub.2 NH.sub.2 H H OH, OH5804 NH(CNH)NH.sub.2 H H (+)-pin5805 NH(CNH)NH.sub.2 H H OH, OH5806 OMe H H (+)-pin5807 OMe H H OH, OH5808 NH(CNH)H H H OH, OH5809 NH(CNH)H H H (+)-pin5810 CH.sub.2 NH.sub.2 CH.sub.2 CN H (+)-pin5811 CH.sub.2 NH.sub.2 CH.sub.2 CN H OH, OH5812 NH(CNH)NH.sub.2 (CH.sub.2)COOH H (+)-pin5813 NH(CNH)NH.sub.2 (CH.sub.2)COOH H OH, OH5814 OMe CH.sub.2 COOMe H (+)-pin5815 OMe CH.sub.2 COOMe H OH, OH5816 NH(CNH)H (CH.sub.2)CN.sub.4 H H OH, OH5817 NH(CNH)H (CH.sub.2)CN.sub.4 H H (+)-pin______________________________________ TABLE 56______________________________________ ##STR151##Ex X R.sup.13 R.sup.14 Y.sup.1 Y.sup.2 Phys. Data______________________________________5822 CH.sub.2 NH.sub.2 H H (+)-pin5823 CH.sub.2 NH.sub.2 H H OH, OH5824 NH(CNH)NH.sub.2 H H (+)-pin5825 NH(CNH)NH.sub.2 H H OH, OH5826 OMe H H (+)-pin5827 OMe H H OH, OH5828 NH(CNH)H H H OH, OH5829 NH(CNH)H H H (+)-pin5830 CH.sub.2 NH.sub.2 CH.sub.2 CN H (+)-pin5831 CH.sub.2 NH.sub.2 CH.sub.2 CN H OH, OH5832 NH(CNH)NH.sub.2 (CH.sub.2)COOH H (+)-pin5833 NH(CNH)NH.sub.2 (CH.sub.2)COOH H OH, OH5834 OMe CH.sub.2 COOMe H (+)-pin5835 OMe CH.sub.2 COOMe H OH, OH5836 NH(CNH)H (CH.sub.2)CN.sub.4 H H OH, OH5837 NH(CNH)H (CH.sub.2)CN.sub.4 H H (+)-pin______________________________________ TABLE 57______________________________________ ##STR152##Ex X R.sup.13 R.sup.14 Y.sup.1 Y.sup.2 Phys. Data______________________________________m = 15842 CH.sub.2 NH.sub.2 H H (+)-pin5843 CH.sub.2 NH.sub.2 H H OH, OH5844 NH(CNH)NH.sub.2 H H (+)-pin5845 NH(CNH)NH.sub.2 H H OH, OH5846 OMe H H (+)-pin5847 OMe H H OH, OH5848 NH(CNH)H H H OH, OH5849 NH(CNH)H H H (+)-pin5850 CH.sub.2 NH.sub.2 CH.sub.2 CN H (+)-pin5851 CH.sub.2 NH.sub.2 CH.sub.2 CN H OH, OH5852 NH(CNH)NH.sub.2 (CH.sub.2)COOH H (+)-pin5853 NH(CNH)NH.sub.2 (CH.sub.2)COOH H OH, OH5854 OMe CH.sub.2 COOMe H (+)-pin5855 OMe CH.sub.2 COOMe H OH, OH5856 NH(CNH)H (CH.sub.2)CN.sub.4 H H OH, OH5857 NH(CNH)H (CH.sub.2)CN.sub.4 H H (+)-pinm = 05858 CH.sub.2 NH.sub.2 H H (+)-pin5859 CH.sub.2 NH.sub.2 H H OH, OH5860 NH(CNH)NH.sub.2 H H (+)-pin5861 NH(CNH)NH.sub.2 H H OH, OH5862 OMe H H (+)-pin5863 OMe H H OH, OH5864 NH(CNH)H H H OH, OH5865 NH(CNH)H H H (+)-pin5866 CH.sub.2 NH.sub.2 CH.sub.2 CN H (+)-pin5867 CH.sub.2 NH.sub.2 CH.sub.2 CN H OH, OH5868 NH(CNH)NH.sub.2 (CH.sub.2)COOH H (+)-pin5869 NH(CNH)NH.sub.2 (CH.sub.2)COOH H OH, OH5870 OMe CH.sub.2 COOMe H (+)-pin5871 OMe CH.sub.2 COOMe H OH, OH5872 NH(CNH)H (CH.sub.2)CN.sub.4 H H OH, OH5873 NH(CNH)H (CH.sub.2)CN.sub.4 H H (+)-pin______________________________________ TABLE 58______________________________________ ##STR153##Ex X R.sup.13 R.sup.14 Y.sup.1 Y.sup.2 Phys. Data______________________________________m = 15878 CH.sub.2 NH.sub.2 H H (+)-pin5879 CH.sub.2 NH.sub.2 H H OH, OH5880 NH(CNH)NH.sub.2 H H (+)-pin5881 NH(CNH)NH.sub.2 H H OH, OH5882 OMe H H (+)-pin5883 OMe H H OH, OH5884 NH(CNH)H H H OH, OH5885 NH(CNH)H H H (+)-pin5886 CH.sub.2 NH.sub.2 CH.sub.2 CN H (+)-pin5887 CH.sub.2 NH.sub.2 CH.sub.2 CN H OH, OH5888 NH(CNH)NH.sub.2 (CH.sub.2)COOH H (+)-pin5889 NH(CNH)NH.sub.2 (CH.sub.2)COOH H OH, OH5890 OMe CH.sub.2 COOMe H (+)-pin5891 OMe CH.sub.2 COOMe H OH, OH5892 NH(CNH)H (CH.sub.2)CN.sub.4 H H OH, OH5893 NH(CNH)H (CH.sub.2)CN.sub.4 H H (+)-pinm = 05894 CH.sub.2 NH.sub.2 H H (+)-pin5895 CH.sub.2 NH.sub.2 H H OH, OH5896 NH(CNH)NH.sub.2 H H (+)-pin5897 NH(CNH)NH.sub.2 H H OH, OH5898 OMe H H (+)-pin5899 OMe H H OH, OH5900 NH(CNH)H H H OH, OH5901 NH(CNH)H H H (+)-pin5902 CH.sub.2 NH.sub.2 CH.sub.2 CN H (+)-pin5903 CH.sub.2 NH.sub.2 CH.sub.2 CN H OH, OH5904 NH(CNH)NH.sub.2 (CH.sub.2)COOH H (+)-pin5905 NH(CNH)NH.sub.2 (CH.sub.2)COOH H OH, OH5906 OMe CH.sub.2 COOMe H (+)-pin5907 OMe CH.sub.2 COOMe H OH, OH5908 NH(CNH)H (CH.sub.2)CN.sub.4 H H OH, OH5909 NH(CNH)H (CH.sub.2)CN.sub.4 H H (+)-pin______________________________________ TABLE 59______________________________________ ##STR154##Ex H U Y.sup.1 Y.sup.2 Phys. Data______________________________________m = 15914 CH.sub.2 NH.sub.2 S (+)-pin5915 NHC(NH)NH.sub.2 S (+)-pin5916 SC(NH)NH.sub.2 S (+)-pin5917 CH.sub.2 NH.sub.2 S OH, OH5918 NHC(NH)NH.sub.2 S OH, OH5919 SC(NH)NH.sub.2 S OH, OH5920 CH.sub.2 NH.sub.2 O (+)-pin5921 NHC(NH)NH.sub.2 O (+)-pin5922 SC(NH)NH.sub.2 O (+)-pin5923 CH.sub.2 NH.sub.2 O OH, OH5924 NHC(NH)NH.sub.2 O OH, OH5925 SC(NH)NH.sub.2 O OH, OHm = 25926 CH.sub.2 NH.sub.2 S (+)-pin CA5927 NHC(NH)NH.sub.2 S (+)-pin5928 SC(NH)NH.sub.2 S (+)-pin5929 CH.sub.2 NH.sub.2 S OH, OH5930 NHC(NH)NH.sub.2 S OH, OH5931 SC(NH)NH.sub.2 S OH, OH5932 CH.sub.2 NH.sub.2 O (+)-pin5933 NHC(NH)NH.sub.2 O (+)-pin5934 SC(NH)NH.sub.2 O (+)-pin5935 CH.sub.2 NH.sub.2 O OH, OH5936 NHC(NH)NH.sub.2 O OH, OH5937 SC(NH)NH.sub.2 O OH, OH______________________________________ CA: HRMS Calc.: 543.2635, Found: 543.2643 TABLE 60______________________________________ ##STR155##Ex H U Y.sup.1 Y.sup.2 Phys. Data______________________________________m = 15942 CH.sub.2 NH.sub.2 S (+)-pin5943 NHC(NH)NH.sub.2 S (+)-pin5944 SC(NH)NH.sub.2 S (+)-pin5945 CH.sub.2 NH.sub.2 S OH, OH5946 NHC(NH)NH.sub.2 S OH, OH5947 SC(NH)NH.sub.2 S OH, OH5948 CH.sub.2 NH.sub.2 O (+)-pin5949 NHC(NH)NH.sub.2 O (+)-pin5950 SC(NH)NH.sub.2 O (+)-pin5951 CH.sub.2 NH.sub.2 O OH, OH5952 NHC(NH)NH.sub.2 O OH, OH5953 SC(NH)NH.sub.2 O OH, OHm = 25954 CH.sub.2 NH.sub.2 S (+)-pin5955 NHC(NH)NH.sub.2 S (+)-pin5956 SC(NH)NH.sub.2 S (+)-pin5957 CH.sub.2 NH.sub.2 S OH, OH5958 NHC(NH)NH.sub.2 S OH, OH5959 SC(NH)NH.sub.2 S OH, OH5960 CH.sub.2 NH.sub.2 O (+)-pin5961 NHC(NH)NH.sub.2 O (+)-pin5962 SC(NH)NH.sub.2 O (+)-pin5963 CH.sub.2 NH.sub.2 O OH, OH5964 NHC(NH)NH.sub.2 O OH, OH5965 SC(NH)NH.sub.2 O OH, OH______________________________________ TABLE 61______________________________________ ##STR156## PhysEx X R.sup.A R.sup.C R.sup.D Y.sup.1, Y.sup.2 Data______________________________________5970 NHC(NH)NH.sub.2 Me Ph OMe (+)-pin5971 NHC(NH)NH.sub.2 Me Ph CONH.sub.2 (+)-pin5972 NHC(NH)NH.sub.2 Me Ph F (+)-pin5973 NHC(NH)NH.sub.2 Me Ph CF.sub.3 (+)-pin5974 NHC(NH)NH.sub.2 Me Ph Cl (+)-pin5975 NHC(NH)NH.sub.2 Me Ph OH (+)-pin5976 NHC(NH)NH.sub.2 Me 4-C.sub.6 H.sub.4 CO.sub.2 H OMe (+)-pin5977 NHC(NH)NH.sub.2 Me 4-C.sub.6 H.sub.4 CO.sub.2 H CONH.sub.2 (+)-pin5978 NHC(NH)NH.sub.2 Me 4-C.sub.6 H.sub.4 CO.sub.2 H F (+)-pin5979 NHC(NH)NH.sub.2 Me 4-C.sub.6 H.sub.4 CO.sub.2 H CF.sub.3 (+)-pin5980 NHC(NH)NH.sub.2 Me 4-C.sub.6 H.sub.4 CO.sub.2 H Cl (+)-pin5981 NHC(NH)NH.sub.2 Me 4-C.sub.6 H.sub.4 CO.sub.2 H OH (+)-pin5982 SC(NH)NH.sub.2 Me Ph OMe (+)-pin5983 SC(NH)NH.sub.2 Me Ph CONH.sub.2 (+)-pin5984 SC(NH)NH.sub.2 Me Ph F (+)-pin5985 SC(NH)NH.sub.2 Me Ph CF.sub.3 (+)-pin5986 SC(NH)NH.sub.2 Me Ph Cl (+)-pin5987 SC(NH)NH.sub.2 Me Ph OH (+)-pin5988 SC(NH)NH.sub.2 Me 4-C.sub.6 H.sub.4 CO.sub.2 H OMe (+)-pin5989 SC(NH)NH.sub.2 Me 4-C.sub.6 H.sub.4 CO.sub.2 H CONH.sub.2 (+)-pin5990 SC(NH)NH.sub.2 Me 4-C.sub.6 H.sub.4 CO.sub.2 H F (+)-pin5991 SC(NH)NH.sub.2 Me 4-C.sub.6 H.sub.4 CO.sub.2 H CF.sub.3 (+)-pin5992 SC(NH)NH.sub.2 Me 4-C.sub.6 H.sub.4 CO.sub.2 H Cl (+)-pin5993 SC(NH)NH.sub.2 Me 4-C.sub.6 H.sub.4 CO.sub.2 H OH (+)-pin5994 CH.sub.2 NH.sub.2 Me Ph OMe (+)-pin5995 CH.sub.2 NH.sub.2 Me Ph CONH.sub.2 (+)-pin5996 CH.sub.2 NH.sub.2 Me Ph F (+)-pin5997 CH.sub.2 NH.sub.2 Me Ph CF.sub.3 (+)-pin5998 CH.sub.2 NH.sub.2 Me Ph Cl (+)-pin5999 CH.sub.2 NH.sub.2 Me Ph OH (+)-pin6000 CH.sub.2 NH.sub.2 Me 4-C.sub.6 H.sub.4 CO.sub.2 H OMe (+)-pin6001 CH.sub.2 NH.sub.2 Me 4-C.sub.6 H.sub.4 CO.sub.2 H CONH.sub.2 (+)-pin6002 CH.sub.2 NH.sub.2 Me 4-C.sub.6 H.sub.4 CO.sub.2 H F (+)-pin6003 CH.sub.2 NH.sub.2 Me 4-C.sub.6 H.sub.4 CO.sub.2 H CF.sub.3 (+)-pin6004 CH.sub.2 NH.sub.2 Me 4-C.sub.6 H.sub.4 CO.sub.2 H Cl (+)-pin6005 CH.sub.2 NH.sub.2 Me 4-C.sub.6 H.sub.4 CO.sub.2 H OH (+)-pin6006 NHC(NH)NH.sub.2 Me Ph OMe OH, OH6007 NHC(NH)NH.sub.2 Me Ph CONH.sub.2 OH, OH6008 NHC(NH)NH.sub.2 Me Ph F OH, OH6009 NHC(NH)NH.sub.2 Me Ph CF.sub.3 OH, OH6010 NHC(NH)NH.sub.2 Me Ph Cl OH, OH6011 NHC(NH)NH.sub.2 Me Ph OH OH, OH6012 NHC(NH)NH.sub.2 Me 4-C.sub.6 H.sub.4 CO.sub.2 H OMe OH, OH6013 NHC(NH)NH.sub.2 Me 4-C.sub.6 H.sub.4 CO.sub.2 H CONH.sub.2 OH, OH6014 NHC(NH)NH.sub.2 Me 4-C.sub.6 H.sub.4 CO.sub.2 H F OH, OH6015 NHC(NH)NH.sub.2 Me 4-C.sub.6 H.sub.4 CO.sub.2 H CF.sub.3 OH, OH6016 NHC(NH)NH.sub.2 Me 4-C.sub.6 H.sub.4 CO.sub.2 H Cl OH, OH6017 NHC(NH)NH.sub.2 Me 4-C.sub.6 H.sub.4 CO.sub.2 H OH OH, OH6018 SC(NH)NH.sub.2 Me Ph OMe OH, OH6019 SC(NH)NH.sub.2 Me Ph CONH.sub.2 OH, OH6020 SC(NH)NH.sub.2 Me Ph F OH, OH6021 SC(NH)NH.sub.2 Me Ph CF.sub.3 OH, OH6022 SC(NH)NH.sub.2 Me Ph Cl OH, OH6023 SC(NH)NH.sub.2 Me Ph OH OH, OH6024 SC(NH)NH.sub.2 Me 4-C.sub.6 H.sub.4 CO.sub.2 H OMe OH, OH6025 SC(NH)NH.sub.2 Me 4-C.sub.6 H.sub.4 CO.sub.2 H CONH.sub.2 OH, OH6026 SC(NH)NH.sub.2 Me 4-C.sub.6 H.sub.4 CO.sub.2 H F OH, OH6027 SC(NH)NH.sub.2 Me 4-C.sub.6 H.sub.4 CO.sub.2 H CF.sub.3 OH, OH6028 SC(NH)NH.sub.2 Me 4-C.sub.6 H.sub.4 CO.sub.2 H Cl OH, OH6029 SC(NH)NH.sub.2 Me 4-C.sub.6 H.sub.4 CO.sub.2 H OH OH, OH6030 CH.sub.2 NH.sub.2 Me Ph OMe OH, OH6031 CH.sub.2 NH.sub.2 Me Ph CONH.sub.2 OH, OH6032 CH.sub.2 NH.sub.2 Me Ph F OH, OH6033 CH.sub.2 NH.sub.2 Me Ph CF.sub.3 OH, OH6034 CH.sub.2 NH.sub.2 Me Ph Cl OH, OH6035 CH.sub.2 NH.sub.2 Me Ph OH OH, OH6036 CH.sub.2 NH.sub.2 Me 4-C.sub.6 H.sub.4 CO.sub.2 H OMe OH, OH6037 CH.sub.2 NH.sub.2 Me 4-C.sub.6 H.sub.4 CO.sub.2 H CONH.sub.2 OH, OH6038 CH.sub.2 NH.sub.2 Me 4-C.sub.6 H.sub.4 CO.sub.2 H F OH, OH6039 CH.sub.2 NH.sub.2 Me 4-C.sub.6 H.sub.4 CO.sub.2 H CF.sub.3 OH, OH6040 CH.sub.2 NH.sub.2 Me 4-C.sub.6 H.sub.4 CO.sub.2 H Cl OH, OH6041 CH.sub.2 NH.sub.2 Me 4-C.sub.6 H.sub.4 CO.sub.2 H OH OH, OH______________________________________

UTILITY

The compounds of formula (I) are useful as inhibitors of trypsin-like enzymes, notably human thrombin, Factor VIIa, Factor IXa, Factor Xa, plasma kallikrein and plasmin. Because of their inhibitory action, these compounds are indicated for use in the prevention or treatment of physiological reactions catalyzed by the aforesaid enzymes such as blood coagulation and inflammation. These compounds are also useful as anticoagulants for the processing of blood for therapeutic or diagnostic purposes or for the production of blood products of fragments, since contact of blood with the surfaces commonly used for blood collection and storage causes activation of coagulation leading to thrombin formation and clot formation.

The effectiveness of compounds of the present invention as inhibitors of blood coagulation proteases was determined using purified human proteases and synthetic substrates following procedures similar to those described in Kettner et al. (1990).

For these assays, the rate of enzymatic (thrombin, Factor Xa, and Factor VIIa) hydrolysis of chromogenic substrates (S2238 (H-D-Phe-Pip-Arg-pNA), S2222, and S2288, respectively; Kabi Pharmacia, Franklin, Ohio.) was measured both in the absence and presence of compounds of the present invention. Hydrolysis of the substrate resulted in the release of pNA, which was monitored spectrophotometrically by measuring the increase in absorbance at 405 nM. A decrease in the rate of absorbance change at 405 nm in the presence of inhibitor is indicative of enzyme inhibition. The results of this assay are expressed as inhibitory constant, K.sub.i.

Thrombin and Xa determinations were made in 0.10M sodium phosphate buffer, pH 7.5, containing 0.20M NaCl, and 0.5% PEG 8000. VIIa determinations were made in 0.05M tris buffer, pH 7.6, containing 0.10M NaCl, 4 mM CaCl.sub.2, and 0.1% bovine serum albumin. The Michaelis constant, K.sub.m, for substrate hydrolysis was determined at 5.degree. C. using the method of Lineweaver and Burk.

Values of K.sub.i were determined by allowing 0.2-0.5 nM human thrombin or human factor Xa (Enzyme Research Laboratories, South Bend, Ind.), or 50 nM human factor VIIa (BiosPacific, Emeryville, Calif.) react with the substrate (0.20 mM-1 mM) in the presence of inhibitor. Reactions were allowed to go for 30 minutes and the velocities (rate of absorbance change vs time) were measured in the time frame of 25-30 minutes. The following relationship was used to calculate K.sub.i values. ##EQU1## where: v.sub.o is the velocity of the control in the absence of inhibitor;

v.sub.s is the velocity in the presence of inhibitor; I is the concentration of inhibitor; K.sub.i is the dissociation constant of the enzyme: inhibitor complex; S is the concentration of substrate; K.sub.m is the Michaelis constant.

Using the methodology described above, representative compounds of this invention were evaluated and found to exhibit a Ki of less 500 .mu.M thereby confirming the utility of compounds of the invention as effective inhibitors of human blood coagulation proteases. The results of these assays are summarized in Table 62, where +++ indicates a K.sub.i <500 nM; ++ indicates a K.sub.i <50,000 nM; and + indicates a K.sub.i 500,000<nM; - indicates inactive.

TABLE 62______________________________________K.sub.i values for inhibition of SerineProteases by compounds of the present invention.EXAMPLE Thrombin Factor Xa Factor VIIa______________________________________1 +++ ++ NT2 +++ +++ +++29 +++ NT NT35 +++ +++ ++68 ++ ++ +++129 +++ +++ NT199 +++ +++ +++203 +++ +++ +++224 +++ +++ +++227 +++ +++ ++231 +++ +++ ++261 +++ +++ +++262 +++ +++ +++263 +++ +++ +++283 +++ +++ ++286 +++ +++ +++288 +++ NT +++298 +++ +++ +++299 +++ +++ +++302 +++ +++ ++303 +++ ++ ++304 ++ ++ ++305 ++ ++ ++468 ++ ++ ++474 ++ ++ ++887 +++ NT NT888 +++ ++ ++890 +++ ++ ++892 +++ ++ ++898 +++ ++ ++905 ++ ++ -913 +++ - ++914 +++ ++ ++917 +++ ++ ++920 +++ NT NT921 +++ ++ ++923 +++ ++ ++931 +++ ++ ++967 +++ ++ +++969 +++ ++ ++977 +++ NT NT1352 +++ ++ NT1431 +++ NT NT1459 ++ ++ ++1467 +++ NT ++1521 +++ NT NT1557 +++ NT ++2066 NT NT NT2067 +++ NT NT2068 ++ ++ ++2073 +++ ++ ++2074 +++ ++ ++2411 +++ NT NT2412 +++ ++ ++2414 +++ ++ ++2416 +++ ++ ++2422 +++ ++ ++2430 ++ ++ -2439 +++ ++ ++2440 +++ ++ ++2443 +++ ++ ++2446 +++ ++ ++2447 +++ ++ ++2490 +++ ++ +++2491 +++ +++ ++2499 +++ ++ ++2533 +++ ++ -2752 +++ NT NT2780 +++ ++ +++2781 +++ ++ ++2837 ++ NT NT3349 +++ ++ NT3458 +++ - ++3465 +++ ++ ++3538 +++ ++ ++4064 ++ ++ ++4065 ++ ++ ++5426 +++ +++ NT5529 +++ +++ NT5551 NT NT NT______________________________________

The final concentration of thrombin was 4 NIH units/mL. The effectiveness of compounds in prolonging clotting times is reported as K.sub.i TT (nM; level of inhibitor required to prolong clotting to the time observed for 2 NIH units/mL thrombin in the absence of inhibitor) o Compounds of the present invention were found to have K.sub.i TT values in the range of 100-6000 nm.

Generally, these compounds may be administered orally or parenterally to a hose to obtain an anti-thrombogenic effect. The dosage of the active compound depends on the mammalian species, body weight, age, and mode of administration as will be obvious to one skilled in the art. In the case of large mammals such as humans, the compounds may be administered alone or in combination with pharmaceutical carriers or diluents at a dose of from 0.02 to 15 mg/Kg to obtain the anti-thrombogenic effect, and may be given as a single dose or in divided doses or as a sustained release formulation.

Pharmaceutical carriers or diluents are well known and include sugars, starches and water, which may be used to make tablets, capsules, injectable solutions or the like which can serve as suitable dosage forms for administration of the compounds of this invention. Remington's Pharmaceutical Sciences, A. Osol, is a standard reference text which discloses suitable pharmaceutical carriers and dosage forms. The disclosure of this text is hereby incorporated by reference for a more complete teaching of suitable dosage forms for administration of the compounds of this invention.

Claims

1. A compound of formula:

R.sup.1 --Z--CHR.sup.2 --A (I)

wherein:

A is -BY.sup.1 Y.sup.2 ;

Y.sup.1 and Y.sup.2 are independently

a) --OH,

b) --F

c) --NR.sup.3 R.sup.4, or

d) C.sub.1 -C.sub.8 alkoxy;

Y.sup.1 and y.sup.2 are taken together to form:

e) a cyclic boron ester where said chain or ring contains from 2 to 20 carbon atoms and, from 0-3 heteroatoms which are N, S, or O,

f) a cyclic boron amide where said chain or ring contains from 2 to 20 carbon atoms and, from 0-3 heteroatoms which are N, S, or O,

g) a cyclic boron amide-ester where said chain or ring contains from 2 to 20 carbon atoms and from 0-3 heteroatoms which are N, S, or O;

Z is

a) --(CH.sub.2).sub.m CONR.sup.8 --,

b) --(CH.sub.2).sub.m CSNR.sup.8 --,

c) --(CH.sub.2).sub.m SO.sub.2 NR.sup.8 --,

d) --(CH.sub.2).sub.m CO.sub.2 --,

e) --(CH.sub.2).sub.m C(S)O--, or

f) --(CH.sub.2).sub.m SO.sub.2 O--;

R.sup.1 is --(CH.sub.2).sub.p -aryl, wherein aryl is phenyl, naphthyl or biphenyl substituted with one, two or three substituents selected from the group consisting of:

halo, methylenedioxy, -R.sup.8, --NR.sup.8 COR.sup.9, C.sub.2 -C.sub.6 -alkenyl, C.sub.2 -C.sub.6 -alkynyl, --(CH.sub.2).sub.w --OR.sup.8, -(C.sub.1 -C.sub.6)-perfluoroalkyl, --(CH.sub.2).sub.w CN, --(CH.sub.2).sub.w NC, --(CH.sub.2).sub.w NO.sub.2, --(CH.sub.2).sub.w CF.sub.3, --(CH.sub.2).sub.w S(O).sub.r R.sup.7, --(CH.sub.2).sub.w NR.sup.8 R.sup.9, --(CH.sub.2).sub.w COR.sup.8, --(CH.sub.2).sub.w CHO; --(CH.sub.2).sub.w CO.sub.2 R.sup.8, --(CH.sub.2).sub.w CONR.sup.8 R.sup.9, --(CH.sub.2).sub.w SO.sub.2 NH--(C.sub.1 -C.sub.5)-alkyl, --(CH.sub.2).sub.w SO.sub.2 NH.sub.2, --(CH.sub.2).sub.w SO.sub.2 NH--CO--(C.sub.1 -C.sub.6)-alkyl, --(CH.sub.2).sub.w SO.sub.2 NH--CO.sub.2 --(C.sub.1 -C.sub.6)-alkyl, --(CH.sub.2).sub.w NHSO.sub.2 --(C.sub.1 -C.sub.6)-alkyl, --(CH.sub.2).sub.w NHSO.sub.2 --(C.sub.1 -C.sub.6)-perfluoroalkyl, --(CH.sub.2).sub.w NHSO.sub.2 -phenyl, --(CH.sub.2).sub.w NHSO.sub.2 -perfluorophenyl, --(CH.sub.2).sub.w CN.sub.4 H, --O(CH.sub.2).sub.w CN, --NH(CH.sub.2).sub.w CN, --S(CH.sub.2).sub.w CN, --(CH.sub.2).sub.w NH--CO--(C.sub.1 -C.sub.6 -alkyl), --(CH.sub.2).sub.w NH--CO--(C.sub.1 -C.sub.6 -perfluoroalkyl), --(CH.sub.2).sub.w NH--CO--(phenyl), --(CH.sub.2).sub.w NH--CO.sub.2 --(C.sub.1 -C.sub.6 -alkyl), --(CH.sub.2).sub.w NH--CO.sub.2 --(C.sub.1 -C.sub.6 -perfluoroalkyl), --(CH.sub.2).sub.w NH--CO.sub.2 --(phenyl), --O(C.dbd.O)--(C.sub.1 -C.sub.5 -alkyl), ##STR157## R.sup.2 is a) -(C.sub.1 -C.sub.12 alkyl)-X,

b) -(C.sub.2 -C.sub.12 alkenyl)-X, or ##STR158## X is a) halogen,

b) --CN,

c) --NO.sub.2,

d) --CF.sub.3,

e) --S(O).sub.r R14,

f) --NHR.sup.14

g) --NHS(O).sub.r R.sup.14,

h) --NHC(NH)H,

i) --NHC(NH)NHOH,

j) --NHC(NH)NHCN,

k) --NHC(NH)NHR.sup.14,

l) --NHC(NH)NHCOR.sup.14,

m) --C(NH)NHR.sup.14,

n) --C(NH)NHCOR.sup.14,

o) --C(O)NHR.sup.14,

p) --C(O)NHC(O)R.sup.14,

q) --C(O)OR.sup.14,

r) --OR.sup.14,

s) --OC(O)R.sup.14,

t) --OC(O)OR.sup.14,

u) --OC(O)NHR.sup.14,

v) --OC(O)NHC(O)R.sup.14,

w) --SC(.dbd.NH).sup.NHR.sup.14, or

x) --SC(.dbd.NH)NHC(.dbd.O)R.sup.14 ;

R.sup.3 is

a) hydrogen,

b) C.sub.1 -C.sub.8 alkyl,

c) -(C.sub.1 -C.sub.4 alkyl)-aryl,

d) C.sub.5 -C.sub.7 cycloalkyl, or

e) phenyl;

R.sup.4 is

a) hydrogen,

b) C.sub.1 -C.sub.8 alkyl,

c) --(C.sub.1 -C.sub.4 alkyl)-aryl,

d) C.sub.5 -C.sub.7 cycloalkyl,

e) phenyl, or

f) phenylsulfonyl;

R.sup.7 is

a) phenyl,

b) C.sub.1 -C.sub.8 -alkyl,

c) C.sub.1 -C.sub.4 -alkoxy,

d) --CF.sub.3, or

e) benzyl;

R.sup.8 and R.sup.9 are independently

a) H, ##STR159## c) C.sub.3 -C.sub.7 cycloalkyl, d) C.sub.1 -C.sub.8 -alkyl, or

R.sup.11 is

a) halo,

b) --CN,

c) C.sub.1 -C.sub.10 -alkyl,

d) C.sub.3 -C.sub.8 -cycloalkyl,

e) C.sub.2 -C.sub.10 -alkenyl,

f) C.sub.2 -C.sub.10 -alkynyl,

g) --OR.sup.8,

h) --NO.sub.2,

i) --CF.sub.3,

j) --S(O).sub.r R.sup.7,

k) --NR.sup.8 R.sup.9,

m) --CO.sub.2 R.sup.8,

l) --COR.sup.9,

n) --CONR.sup.8 R.sup.9, or

o) H

R.sup.12 is H, C.sub.1 -C.sub.4 alkyl, phenyl, benzyl, --COR.sup.7, or --S(O).sub.r R.sup.7 ;

R14 is

a) --H,

b) --CF.sub.3

c) --C.sub.1 -C.sub.4 alkyl,

d) --(CH.sub.2).sub.q -aryl, wherein aryl is phenyl, biphenyl, naphthyl, or fluorenyl unsubstituted or substituted with one to three substituents selected from the group consisting of:

halogen,

--CF.sub.3,

-(C.sub.1 -C.sub.4 alkyl),

--(CH.sub.2).sub.x R.sup.15,

--(CH.sub.2).sub.x CO(CH.sub.2).sub.y R.sup.15,

--(CH.sub.2).sub.x C(O)O(CH.sub.2).sub.y R.sup.15,

--(CH.sub.2).sub.x C(O)N�(CH.sub.2).sub.y R.sup.15 !�(CH.sub.2).sub.y R.sup.16 !,

-methylenedioxy,

-(C.sub.1 -C.sub.4 alkoxy),

--(CH.sub.2).sub.x O(CH.sub.2).sub.y R.sup.15,

--(CH.sub.2).sub.x OCO(CH.sub.2).sub.y R.sup.15,

--(CH.sub.2).sub.x OC(O)O(CH.sub.2).sub.y R.sup.15,

--(CH.sub.2).sub.x OC(O)N�(CH.sub.2).sub.y R.sup.15 !�(CH.sub.2).sub.y R.sup.16 !,

--(CH.sub.2).sub.x OC(O)N�(CH.sub.2).sub.y R.sup.15 !�CO(CH.sub.2).sub.y R.sup.16 !,

--(CH.sub.2).sub.x S(O).sub.r (CH.sub.2).sub.y R.sup.15,

--(CH.sub.2).sub.x S(O).sub.r (CH.sub.2).sub.y COR.sup.15,

--(CH.sub.2).sub.x S(O).sub.r (CH.sub.2).sub.y C(O)OR.sup.15,

--(CH.sub.2).sub.x S(O).sub.r N�(CH.sub.2).sub.y R.sup.15 !�(CH.sub.2).sub.y R.sup.16 !

--(CH.sub.2).sub.x N�(CH.sub.2).sub.y R.sup.15 !�(CH.sub.2).sub.y R.sup.16 !,

--(CH.sub.2).sub.x N�(CH.sub.2).sub.y R.sup.15 !�CO(CH.sub.2).sub.y R.sup.16 !,

--(CH.sub.2).sub.x N�(CH.sub.2).sub.y R.sup.15 !�C(O)O(CH.sub.2).sub.y R.sup.16 !,

--(CH.sub.2).sub.x N�(CH.sub.2).sub.y R.sup.15 !CON�(CH.sub.2).sub.y R.sup.15 !�(CH.sub.2).sub.y R.sup.16 !,

--(CH.sub.2).sub.x N�(CH.sub.2).sub.y R.sup.15 !CON�(CH.sub.2).sub.y R.sup.15 !--�CO(CH.sub.2).sub.y R.sup.16 !,

--(CH.sub.2).sub.x N�(CH.sub.2).sub.y R.sup.15 !�S(O).sub.r (CH.sub.2).sub.y R.sup.16 !;

R.sup.15 and R.sup.16 are independently

a) hydrogen,

b) C.sub.1 -C.sub.8 alkyl,

c) -(C.sub.1 -C.sub.4 alkyl)-aryl, where aryl is defined above,

d) C.sub.5 -C.sub.7 cycloalkyl,

e) phenyl, substituted by 0-3 R.sup.18,

f) benzyl, substituted by 0-3 R.sup.18, or

g) --(C.sub.1 -C.sub.4 alkoxy);

R.sup.15 and R.sup.16 are taken together to form a ring: ##STR160## m is 0 to 6; n is 1 to 2;

p is 0 to 2;

q is 0 to 4.

r is 0 to 2;

s is 0 to 3;

t is 1 to 5;

u is 0 to 5;

w is 0 to 5;

x is 0 to 6;

y is 0 to 6;

W is

a) --O--,

b) --S(O).sub.r,

c) --NR.sup.4 --,

d) --NC(.dbd.O)R.sup.3 --,

e) a bond, or

f) --(CH.sub.2).sub.n --;

or pharmaceutically acceptable salts thereof.

2. A compound of claim 1 wherein:

Z is

a) --(CH.sub.2).sub.m CONR.sup.8 --,

b) --(CH.sub.2).sub.m CSNR.sup.8 --,

c) --(CH.sub.2).sub.m SO.sub.2 NR.sup.8 --,

R.sup.1 is --(CH.sub.2).sub.p -aryl, wherein aryl is phenyl, naphthyl or biphenyl substituted with one, two or three substituents selected from the group consisting of:

halo, methylenedioxy, -R.sup.8, --NR.sup.8 COR.sup.9, C.sub.2 -C.sub.6 -alkenyl, C.sub.2 -C.sub.6 -alkynyl, --(CH.sub.2).sub.w --OR.sup.8, --(C.sub.1 -C.sub.6)-perfluoroalkyl, --(CH.sub.2).sub.w CN, --(CH.sub.2).sub.w NC, --(CH.sub.2).sub.w NO.sub.2, --(CH.sub.2).sub.w CF.sub.3, --(CH.sub.2).sub.w S(O).sub.r R.sup.7, --(CH.sub.2).sub.w NR.sup.8 R.sup.9, --(CH.sub.2).sub.w COR.sup.8, --(CH.sub.2).sub.w CO.sub.2 R.sup.8, --(CH.sub.2).sub.w CONR.sup.8 R.sup.9. --(CH.sub.2).sub.w SO.sub.2 NH--(C.sub.1 -C.sub.6)-alkyl, --(CH.sub.2).sub.w SO.sub.2 NH.sub.2, --(CH.sub.2).sub.w SO.sub.2 NH--CO--(C.sub.1 -C.sub.6)--alkyl, --(CH.sub.2).sub.w SO.sub.2 NH--CO.sub.2 --(C.sub.1 -C.sub.6)-alkyl, --(CH.sub.2).sub.w NHSO.sub.2 --(C.sub.1 -C.sub.6)-alkyl, --(CH.sub.2).sub.w NHSO.sub.2 --(C.sub.1 -C.sub.6)-perfluoroalkyl, --(CH.sub.2).sub.w NHSO.sub.2 -phenyl, --(CH.sub.2).sub.w NHSO.sub.2 -perfluorophenyl, --(CH.sub.2).sub.w CN.sub.4 H, --O(CH.sub.2).sub.w CN, --NH(CH.sub.2).sub.w CN, --S(CH.sub.2).sub.w CN, --(CH.sub.2).sub.w NH--CO--(C.sub.1 -C.sub.6 -alkyl), --(CH.sub.2).sub.w NH--CO--(C.sub.1 -C.sub.6 -perfluoroalkyl), --(CH.sub.2).sub.w NH--CO--(phenyl), --(CH.sub.2).sub.w NH--CO.sub.2 --(C.sub.1 -C.sub.6 -alkyl), --(CH.sub.2).sub.w NH--CO.sub.2 --(C.sub.1 -C.sub.6 -perfluoroalkyl), or --(CH.sub.2).sub.w NH--CO.sub.2 --(phenyl), --O(C.dbd.O--(C.sub.1 -C.sub.5 alkyl);

R.sup.14 is:

a) --H,

b) --CF.sub.3

c) -C.sub.1 -C.sub.4 alkyl,

d) --(CH.sub.2).sub.q -aryl, wherein aryl is phenyl, biphenyl, naphthyl, or fluorenyl unsubstituted or substituted with one to three substituents selected from the group consisting of:

halogen

--CF.sub.3,

-(C.sub.1 -C.sub.4 alkyl),

-methylenedioxy,

-(C.sub.1 -C.sub.4 alkoxy),

--(CH.sub.2).sub.x N�(CH.sub.2).sub.y R.sup.15 !�(CH.sub.2).sub.y R.sup.16 !; and all other required substituents of formula (I) are as defined in claim 1.

3. A compound of claim 2 wherein

A is -BY.sup.1 Y.sup.2 ;

Y.sup.1 and Y.sup.2 are independently

a) --OH, or

b) C.sub.1 -C.sub.8 alkoxy;

Y.sup.1 and Y.sup.2 are taken together to form

a cyclic boron ester where said chain or ring contains from 2 to 20 carbon atoms and from 0-3 heteroatoms which are N, S, or O,

X is

a) halogen

b) --CN,

c) --NO.sub.2,

d) --CF.sub.3,

e) --NHR.sup.14

f) --NHS(O).sub.r R.sup.14,

g) --NHC(NH)H,

h) --NHC(NH)NHOH,

i) --NHC(NH)NHCN,

j) --NHC(NH)NHR.sup.14,

k) --NHC(NH)NHCOR.sup.14,

l) --C(NH)NHR.sup.14,

m) --C(NH)NHCOR.sup.14,

n) --C(O)NHR.sup.14,

o) --C(O)NHC(O) R.sup.14,

p) --C(O)OR.sup.14,

q) --OR.sup.14,

r) --OC(O)R.sup.14,

s) --OC(O)OR.sup.14,

t) --OC(O)NHR.sup.14,

u) --OC(O)NHC(O) R.sup.14,

v) --SC(.dbd.NH)NHR.sup.14, or

w) --SC(.dbd.NH)NHC(.dbd.O) R.sup.14 ;

W is

a) --O--,

b) --NR.sup.4 --,

c) a bond, or

d) --(CH.sub.2).sub.n --;

and all other required substituents of formula (I) are as in claim 2.

4. A compound of claim 3 wherein:

Z is --(CH.sub.2).sub.m CONR.sup.8 --;

R.sup.2 is

a) -(C1-C12 alkyl)-X, or ##STR161## X is a) halogen (F, Cl, Br, I),

b) --CN,

c) --NHR.sup.14

d) --NHC(NH) H,

e) --NHC(NH) NHR.sup.14,

f) --C(NH)NHR.sup.14,

g) --OR.sup.14, or

h) --SC(.dbd.NH) NHR.sup.14 ;

R.sup.14 is --H;

and all other required substituents of formula (I) are defined as in claim 3.

5. A compound of claim 4 selected from the group consisting of:

N.sup.1 -(4-phenylbenzoyl)-(R)-boroarginine, hydrochloride

N.sup.1 -(3-phenoxybenzoyl)-(R)-boroarginine, hydrochloride

N.sup.1 -(1-fluorenonyl)-(R)-boroarginine, hydrochloride

N.sup.1 -(4-�1-butyl!benzoyl)-(R)-boroarginine, hydrochloride

N.sup.1 -(2-benzoylbenzoyl)-(R)-boroarginine, hydrochloride

N.sup.1 -(3-�N-benzyloxycarbonyl-N-methylamino!-4-�1-butyl!-benzoyl)-(R)-boroarginine, hydrochloride

N.sup.1 -(4-cyclohexylbenzoyl)-(R)-boroarginine, hydrochloride

N.sup.1 -(2-methyl-4-phenylbenzoyl)-(R)-boroarginine, hydrochloride

N.sup.1 -�4-phenyl-2-nitrobenzoyl!boroArg, (+)-pinanediol ester

N.sup.1 -�4-phenyl-2-fluorobenzoyl!boroArg, (+)-pinanediol ester

N.sup.1 -�4-phenyl-2-aminobenzoyl!boroArg, (+)-pinanediol ester

N.sup.1 -�4-phenyl-2-(methylsulfonamido)benzoyl!boroArg, (+)-pinanediol ester

N.sup.1 -�4-phenyl-2-(cyanomethylamino)benzoyl!boroArg, (+)-pinanediol ester

N.sup.1 -�4-phenyl-2-(cyanomethyl)benzoyl!boroArg, (+)-pinanediol ester

N.sup.1 -�4-phenyl-2-(diethylamino)benzoyl!boroArg, (+)-pinanediol ester

N.sup.1 -�4-�2-(t-butylaminosulfonyl)phenyl!-2-methyl-benzoyl!boroArg, (+)pinanediol ester

N.sup.1 -�4-�2-(aminosulfonyl)phenyl!-2-methyl-benzoyl!boroArg, (+)pinanediol ester

N.sup.1 -�4-�2-(methoxycarbonylaminosulfonyl)phenyl!-2-methyl-benzoyl!boroArg, (+)-pinanediol ester

N.sup.1 -�4-�2-(t-butylaminosulfonyl)phenyl!benzoyl!boroArg, (+)-pinanediol ester

N.sup.1 -�4-�2-(t-butylaminosulfonyl)phenyl!benzoyl!boroArg--OH

N.sup.1 -�4-�2-(n-butoxycarbonylaminosulfonyl)phenyl!-2-methyl-benzoyl!boroArg, (+)-pinanediol ester

N.sup.1 -�4-�2-(diethylaminosulfonyl)phenyl!-2-methyl-benzoyl!boroArg, (+)pinanediol ester

N.sup.1 -�4-�2-(t-butylaminosulfonyl)phenyl!-2-fluoro-benzoyl!boroArg, (+)pinanediol ester

N.sup.1 -�4-�2-(aminosulfonyl)phenyl!-2-fluoro-benzoyl!boroArg, (+)pinanediol ester

N.sup.1 -�4-�2-(methoxycarbonylaminosulfonyl)phenyl!-2-fluoro-benzoyl!boroArg, (+)-pinanediol ester

N.sup.1 -�4-�2-(t-butylaminosulfonyl)phenyl!-2-nitro-benzoyl!boroArg, (+)pinanediol ester

N.sup.1 -�4-�2-(aminosulfonyl)phenyl!-2-nitro-benzoyl!boroArg, (+)pinanediol ester

N.sup.1 -�4-�2-(methoxycarbonylaminosulfonyl)phenyl!-2-nitro-benzoyl!boroArg, (+)-pinanediol ester

N.sup.1 -(3-phenylbenzoyl)boroarg, (+)-pinanediol

N.sup.1 -�4-(3-BOCNHphenyl).sub.2 -methylbenzoyl!boroarg, (+)-pinanediol

N.sup.1 -�4-(3-nitrophenyl)benzoyl!boroarg, (+)-pinanediol

N.sup.1 -�4-(3-aminophenyl)benzoyl!boroarg, (+)-pinanediol

N.sup.1 -(3-phenylbenzoyl)borolys, (+)-pinanediol and

N.sup.1 -(3-phenylbenzoyl)boroIrg, (+)-pinanediol.

6. A pharmaceutical composition comprising a pharmaceutically acceptable carrier and a therapeutically effective amount of a compound of any one of claims 1 through 5.

7. A method of treating a physiological disorder in a warm blooded animal catalyzed by trypsin-like enzymes comprising administering to an animal in need of such treatment an effective amount of a compound of any one of claims 1 through 5.