Claims
- 1. A compound of formula (I): ##STR154## or a pharmaceutically acceptable salt thereof, wherein: L is connected with J or K to form an aromatic ring as defined below;
- J and L are connected together to form a 6 carbon aromatic ring substituted with R.sup.7a, R.sup.7b, R.sup.8a and R.sup.8b ;
- K is --C(.dbd.O)--;
- R.sup.1 is --SO.sub.2 NHCO.sub.2 R.sup.23 ;
- R.sup.2a and R.sup.2b are each independently
- (a) H,
- (b) halogen, (Cl, Br, I, F),
- (c) NO.sub.2,
- (d) NH.sub.2,
- (e) C.sub.1 -C.sub.4 -alkylamino,
- (f) di(C.sub.1 -C.sub.4 -alkyl)amino,
- (g) SO.sub.2 NHR.sup.9,
- (h) CF.sub.3,
- (i) C.sub.1 -C.sub.6 -alkyl,
- (j) C.sub.1 -C.sub.6 -alkoxy,
- (k) (C.sub.1 -C.sub.6 -alkoxy)--CH.sub.2 --,
- (l) (C.sub.1 -C.sub.6 -alkyl-S)--CH.sub.2 --,
- (m) C.sub.1 -C.sub.6 -alkyl--S--,
- (n) --CH.sub.2 NR.sup.9 R.sup.9,
- (o) C.sub.2 -C.sub.6 -alkenyl,
- (p) C.sub.2 -C.sub.6 -alkynyl;
- (q) aryl as defined below,
- (r) aryl(C.sub.1 -C.sub.4 -alkyl), or
- (s) C.sub.3 -C.sub.7 -cycloalkyl;
- R.sup.3a is
- (a) H,
- (b) halogen (Cl, Br, I, F),
- (c) C.sub.1 -C.sub.6 -alkyl,
- (d) C.sub.1 -C.sub.6 -alkoxy, or
- (e) C.sub.1 -C.sub.6 -alkoxyalkyl;
- R.sup.3b is
- (a) H,
- (b) halogen (Cl, Br, I, F),
- (c) NO.sub.2,
- (d) C.sub.1 -C.sub.6 -alkyl,
- (e) C.sub.1 -C.sub.6 -acyloxy, or
- (f) C.sub.3 -C.sub.7 -cycloalkyl,
- (g) C.sub.1 -C.sub.6 -alkoxy,
- (h) --NHSO.sub.2 R.sup.4,
- (i) hydroxy(C.sub.1 -C.sub.4 -alkyl),
- (j) aryl(C.sub.1 -C.sub.4 -alkyl),
- (k) C.sub.1 -C.sub.4 -alkylthio,
- (l) C.sub.1 -C.sub.4 -alkyl sulfinyl,
- (m) C.sub.1 -C.sub.4 -alkyl sulfonyl,
- (n) NH.sub.2,
- (o) C.sub.1 -C.sub.4 -alkylamino,
- (p) di(C.sub.1 -C.sub.4 -alkyl)amino,
- (q) fluoro-C.sub.1 -C.sub.4 -alkyl-,
- (r) --SO.sub.2 --NHR.sup.9,
- (s) aryl as defined below,
- (t) furyl,
- (u) CF.sub.3,
- (v) C.sub.2 -C.sub.6 -alkenyl, or
- (w) C.sub.2 -C.sub.6 -alkynyl;
- wherein aryl is phenyl or naphthyl optionally substituted with one or two substituents selected from the group consisting of halogen(Cl, Br, I, F), N(R.sup.4).sub.2, CO.sub.2 R.sup.4, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkoxy, NO.sub.2, CF.sub.3, C.sub.1 -C.sub.4 -alkylthio, OH, --SO.sub.2 NR.sup.9 R.sup.10, C.sub.3 -C.sub.7 -cycloalkyl, C.sub.3 -C.sub.10 -alkenyl, and --S(O).sub.x (C.sub.1 -C.sub.4 -alkyl);
- R.sup.4 is H, aryl as defined above, straight chain or branched C.sub.1 -C.sub.6 alkyl optionally substituted with aryl as defined above, or heteroaryl, wherein heteroaryl is an unsubstituted, monosubstituted or disubstituted heteroaromatic 5 or 6 membered ring which can contain one or two heteroatoms selected from the group consisting of N, O, and S, and wherein the substituents are members selected from the group consisting of --OH, --SH, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkoxy, --CF.sub.3, halogen (Cl, Br, I, F), and NO.sub.2 ;
- R.sup.4a is aryl as defined above, C.sub.1 -C.sub.6 -alkyl, or aryl-C.sub.1 -C.sub.6 -alkyl
- R.sup.5 is H, ##STR155## E is a single bond, --NR.sup.13 (CH.sub.2).sub.s --, --S(O).sub.x (CH.sub.2).sub.s -- where x is 0 to 2 and s is 0 to 5, --CH(OH)--, --O--, or CO--;
- R.sup.6 is
- (a) aryl,
- (b) straight chain or branched C.sub.1 -C.sub.6 -alkyl, C.sub.2 -C.sub.5 -alkenyl or C.sub.2 -C.sub.5 -alkynyl each of which can be optionally substituted with a substituent selected from the group consisting of aryl as defined above, C.sub.3 -C.sub.7 -cycloalkyl, halogen (Cl, Br, I, F), CF.sub.3, CF.sub.2 CF.sub.3, --NH.sub.2, --NH(C.sub.1 -C.sub.4 -alkyl), --OR.sup.4 --N(C.sub.1 -C.sub.4 -alkyl).sub.2, --NH--SO.sub.2 R.sup.4, --COOR.sup.4, and --SO.sub.2 NHR.sup.9,
- (c) heteroaryl as defined hereinabove,
- (d) C.sub.3 -C.sub.7 -cycloalkyl,
- (e) perfluoro-C.sub.1 -C.sub.4 -alkyl, or
- (f) H;
- R.sup.7a and R.sup.7b are independently
- (a) H,
- (b) straight chain or branched C.sub.1 -C.sub.6 -alkyl, C.sub.2 -C.sub.6 -alkenyl or C.sub.2 -C.sub.6 -alkynyl,
- (c) halogen (Cl, Br, I, F),
- (d) CF.sub.3, or
- (e) when R.sup.7a and R.sup.7b are bonded to adjacent carbon atoms, they can be joined to form a phenyl ring;
- R.sup.8a and R.sup.8b are independently
- (a) H,
- (b) C.sub.1 -C.sub.6 -alkyl optionally substituted with a substituent selected from the group consisting of --OH, -guanidino, C.sub.1 -C.sub.4 -alkoxy, --N(R.sup.4).sub.2, COOR.sup.4, --CON(R.sup.4).sub.2, --O--COR.sup.4, -aryl, -heteroaryl, --S(O).sub.x --R.sup.23, -tetrazol-5-yl, --CONHSO.sub.2 R.sup.23, --SO.sub.2 NH-heteroaryl, --SO.sub.2 NHCOR.sup.23, --PO(OR.sup.4).sub.2, --PO(OR.sup.4)R.sup.9, --SO.sub.2 NH--CN, --NR.sup.10 COOR.sup.23, morpholino, --N--(C.sub.1 -C.sub.6 -alkyl)piperazine, --COR.sup.4, ##STR156## (c) --CO-aryl, (d) --C.sub.3 -C.sub.7 -cycloalkyl,
- (e) halogen (Cl, Br, I, F),
- (f) --OH,
- (g) --OR.sup.23,
- (h) --C.sub.1 -C.sub.4 -perfluoroalkyl,
- (i) --S(O).sub.x --R.sup.23,
- (j) --COOR.sup.4,
- (k) --SO.sub.3 H,
- (l) --NR.sup.4 R.sup.23,
- (m) --NR.sup.24 COR.sup.23,
- (n) --NR.sup.24 COOR.sup.23,
- (o) --SO.sub.2 NR.sup.9 R.sup.10,
- (p) --NO.sub.2,
- (q) --NR.sup.24 SO.sub.2 R.sup.23,
- (r) --NR.sup.24 CONR.sup.4 R.sup.23,
- (s) ##STR157## (t) -aryl or -heteroaryl as defined above, (u) --NR.sup.24 SO.sub.2 CF.sub.3,
- (v) --SO.sub.2 NH-heteroaryl,
- (w) --SO.sub.2 NHCOR.sup.23,
- (x) --CONHSO.sub.2 R.sup.23,
- (y) --PO(OR.sup.4).sub.2,
- (z) --PO(OR.sup.4)R.sup.9,
- (aa) -tetrazol-5-yl,
- (bb) --CONH(tetrazol-5-yl),
- (cc) --COR.sup.4,
- (dd) --SO.sub.2 NHCN
- (ff) --CO-heteroraryl,
- (gg) --NR.sup.24 SO.sub.2 NR.sup.23 R.sup.9,
- (hh) ##STR158## (ii) ##STR159## (jj) ##STR160## (kk) ##STR161## (ll) ##STR162## (mm) ##STR163## (nn) ##STR164## or (oo) ##STR165## R.sup.9 is H, C.sub.1 -C.sub.5 -alkyl, aryl or arylmethyl; R.sup.10 is H, C.sub.1 -C.sub.4 -alkyl;
- R.sup.11 is H, C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.4 -alkenyl, C.sub.1 -C.sub.4 -alkoxy alkyl, or ##STR166## R.sup.12 is --CN, --NO.sub.2, --CF.sub.3 or --CO.sub.2 R.sup.4 ; R.sup.13 is H, (C.sub.1 -C.sub.4 -alkyl)CO--, C.sub.1 -C.sub.6 -alkyl, allyl, C.sub.3 -C.sub.6 -cycloalkyl, aryl or arylmethyl;
- R.sup.14 is H, C.sub.1 -C.sub.8 -alkyl, C.sub.1 -C.sub.8 -perfluoroalkyl, C.sub.3 -C.sub.6 -cycloalkyl, aryl or arylmethyl;
- R.sup.15 is H, C.sub.1 -C.sub.6 -alkyl;
- R.sup.16 is H, C.sub.1 -C.sub.6 -alkyl, C.sub.3 -C.sub.6 -cycloalkyl, aryl or arylmethyl;
- R.sup.17 is --NR.sup.9 R.sup.10, --OR.sup.10, --NHCONH.sub.2, --NHCSNH.sub.2, ##STR167## R.sup.18 and R.sup.19 are independently C.sub.1 -C.sub.4 -alkyl or taken together are --(CH.sub.2).sub.q - where q is 2 or 3;
- R.sup.20 is H, --NO.sub.2, --NH.sub.2, --OH or --OCH.sub.3 ;
- R.sup.21 is H, aryl, or C.sub.1 -C.sub.4 -alkyl optionally substituted with aryl, --NH.sub.2, --NH(C.sub.1 -C.sub.4 -alkyl), --N(C.sub.1 -C.sub.4 -alkyl).sub.2, --CO.sub.2 R.sup.4, --OH, --SO.sub.3 H, or --SO.sub.2 NH.sub.2 ;
- R.sup.22 is
- (a) aryl as defined above,
- (b) heteroaryl as defined above, or
- (c) C.sub.1 -C.sub.4 -alkyl optionally substituted with a substituent selected from the group consisting of aryl as defined above, heteroaryl as defined above, --OH, --NH.sub.2, --NH(C.sub.1 -C.sub.4 -alkyl), --N(C.sub.1 -C.sub.4 -alkyl).sub.2, --CO.sub.2 R.sup.4, halogen (Cl, Br, F, I), and --CF.sub.3 ;
- R.sup.23 is
- (a) aryl as defined above,
- (b) heteroaryl as defined above,
- (c) C.sub.3 -C.sub.7 -cycloalkyl,
- (d) C.sub.1 -C.sub.6 -alkyl optionally substituted with a substituent selected from the group consisting of aryl as defined above, heteroaryl as defined above, --OH, --SH, C.sub.1 -C.sub.4 -alkyl, --O(C.sub.1 -C.sub.4 -alkyl), C.sub.3 -C.sub.7 -cycloalkyl, --S(O).sub.x (C.sub.1 -C.sub.4 -alkyl), --CF.sub.3, halogen (Cl, Br, F, I), --NO.sub.2, --CO.sub.2 H, CO.sub.2 --C.sub.1 -C.sub.4 -alkyl, --NH.sub.2, --NH(C.sub.1 -C.sub.4 -alkyl), --N(C.sub.1 -C.sub.4 -alkyl).sub.2, --PO.sub.3 H.sub.2, --PO(OH)(O--C.sub.1 -C.sub.4 -alkyl), --N(C.sub.1 -C.sub.4 -alkyl)COR.sup.4a, --CON(C.sub.1 -C.sub.4 -alkyl).sub.2, or --PO(OR.sup.4)R.sup.9,
- (e) perfluoro-C.sub.1 -C.sub.4 -alkyl, or
- (f) CH(aryl).sub.2 ;
- R.sup.24 is
- (a) C.sub.1 -C.sub.6 alkyl,
- (b) substituted C.sub.1 -C.sub.6 alkyl in which the substituent is C.sub.3 -C.sub.7 cycloalkyl, C.sub.1 -C.sub.4 alkoxy, hydroxy, di-(C.sub.1 -C.sub.4 alkyl)amino, CO.sub.2 R.sup.2, morpholinyl, C.sub.1 -C.sub.4 alkylpiperazinyl, CF.sub.3, C.sub.1 -C.sub.4 alkylthio, C.sub.1 -C.sub.4 alkylsulfinyl or C.sub.1 -C.sub.4 alkyl sulfonyl,
- (c) C.sub.2 -C.sub.6 alkenyl,
- (d) phenyl C.sub.1 -C.sub.6 alkyl,
- (e) substituted phenyl C.sub.1 -C.sub.6 alkyl, in which the substituent on the phenyl group is hydroxy, C.sub.1 -C.sub.4 alkoxy, F, Cl, NO.sub.2, cyano, CO.sub.2 R.sup.2, di(C.sub.1 -C.sub.4 alkyl)amino, CF.sub.3, phenyl C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 alkylthio, C.sub.1 -C.sub.4 alkylsulfinyl, or C.sub.1 -C.sub.4 alkylsulfonyl,
- (f) heteroaryl C.sub.1 -C.sub.6 alkyl,
- (g) substituted heteroaryl C.sub.1 -C.sub.6 alkyl, in which the substituent on the heteroaryl group is F, Cl, NO.sub.2, CO.sub.2 R.sup.2, or di-(C.sub.1 -C.sub.4 alkyl)amino, and
- (h) H;
- R.sup.25 is
- (a) H,
- (b) aryl as defined above, or
- (c) C.sub.1 -C.sub.6 -alkyl optionally substituted with aryl, F, Cl, Br, --OH, --NH.sub.2, --NH(C.sub.1 -C.sub.4 -alkyl), --N(C.sub.1 -C.sub.4 -alkyl).sub.2, or CF.sub.3 ;
- R.sup.26 is
- (a) aryl as defined above,
- (b) C.sub.1 -C.sub.6 -alkyl optionally substituted with aryl, F, Cl, Br, --OH, --NH.sub.2, --NH(C.sub.1 -C.sub.4 -alkyl), --N(C.sub.1 -C.sub.4 -alkyl).sub.2, CF.sub.3, --COOR.sup.4, or CN,
- (c) --OCH(R.sup.4)--O--CO--R.sup.4a, or
- (d) --OH or --O--C.sub.1 -C.sub.6 -alkyl wherein alkyl is as defined in (b);
- R.sup.27 is
- (a) H,
- (b) C.sub.1 -C.sub.6 -alkyl optionally substituted with aryl, F, Cl, Br, --OH, --NH.sub.2, --NH(C.sub.1 -C.sub.4 -alkyl), --N(C.sub.1 -C.sub.4 -alkyl).sub.2, CF.sub.3, --COOR.sup.4, or CN, or
- (c) F, Cl, Br;
- X is
- (a) a carbon-carbon single bond,
- (b) --CO--,
- (c) --O--,
- (d) --S--,
- (e) ##STR168## (f) ##STR169## (g) ##STR170## (h) --OCH.sub.2 --, (i) --CH.sub.2 O--,
- (j) --SCH.sub.2 --,
- (k) --CH.sub.2 S--,
- (l) --NHC(R.sup.9)(R.sup.10),
- (m) --NR.sup.9 SO.sub.2 --,
- (n) --SO.sub.2 NR.sup.9 --,
- (o) --C(R.sup.9)(R.sup.10)NH--,
- (p) --CH.dbd.CH--,
- (q) --CF.dbd.CF--,
- (r) --CH.dbd.CF--,
- (s) --CF.dbd.CH--,
- (t) --CH.sub.2 CH.sub.2 --,
- (u) --CF.sub.2 CF.sub.2 --,
- (v) ##STR171## (w) ##STR172## (x) ##STR173## (y) ##STR174## or (z) ##STR175## n is 1 to 3; r is 1 or 2; and
- x is 0 to 2.
- 2. The compound according to claim 1 wherein:
- K is --C(O)--;
- J and L are connected together to form a 6 carbon aromatic ring substituted with R.sup.7a, R.sup.7b, R.sup.8a and R.sup.8b ;
- R.sup.1 is --SO.sub.2 NHCO.sub.2 R.sup.23 ;
- X is a single bond;
- R.sup.2a is H;
- R.sup.2b is H, F, Cl, CF.sub.3, C.sub.1 -C.sub.6 -alkyl, C.sub.2 -C.sub.4 -alkenyl, or C.sub.2 -C.sub.4 -alkynyl;
- R.sup.3a is H;
- R.sup.3b is H, F, Cl, CF.sub.3, C.sub.1 -C.sub.4 -alkyl, C.sub.2 -C.sub.4 -alkenyl, C.sub.2 -C.sub.4 -alkynyl, C.sub.5 -C.sub.6 -cycloalkyl, --COOCH.sub.3, --COOC.sub.2 H.sub.5, --SO.sub.2 -CH.sub.3, NH.sub.2, --N(C.sub.1 -C.sub.4 -alkyl).sub.2 or --NH--SO.sub.2 CH.sub.3 ;
- E is a single bond, --O-- or --S--;
- R.sup.6 is
- (a) C.sub.1 -C.sub.5 alkyl optionally substituted with a substituent selected from the group consisting of C.sub.3 -C.sub.5 -cycloalkyl, Cl, CF.sub.3, CCl.sub.3, --O--CH.sub.3, --OC.sub.2 H.sub.5, --S--CH.sub.3, --S--C.sub.2 H.sub.5, phenyl, or F,
- (b) C.sub.2 -C.sub.5 -alkenyl or C.sub.2 -C.sub.5 -alkynyl, or,
- (c) C.sub.3 -C.sub.5 -cycloalkyl;
- R.sup.7a and R.sup.7b are each H;
- R.sup.8a and R.sup.8b are independently
- (a) H,
- (b) C.sub.1 -C.sub.4 -alkyl optionally substituted with COOR.sup.4, OCOR.sup.4a, OH, aryl, heteroaryl, morpholinyl, ##STR176## (c) C.sub.2 -C.sub.4 -alkenyl, (d) --OH,
- (e) --NO.sub.2,
- (f) --NR.sup.24 COR.sup.23,
- (g) --C.sub.1 -C.sub.4 -alkoxy,
- (h) --NR.sup.24 CO.sub.2 R.sup.23,
- (i) --NR.sup.4 R.sup.23,
- (j) halogen (Cl, F, Br),
- (k) --CF.sub.3,
- (1) --CO.sub.2 R.sup.4,
- (m) --CO--aryl as defined above,
- (n) heteroaryl,
- (o) --S(O).sub.x --C.sub.1 -C.sub.4 -alkyl,
- (p) --SO.sub.2 --NH--C.sub.1 -C.sub.4 -alkyl,
- (q) --SO.sub.2 --NH-aryl as defined above,
- (r) --NR.sup.24 SO.sub.2 CH.sub.3,
- (s) aryl as defined above,
- (t) --NR.sup.24 CONR.sup.4 R.sup.23, (u) ##STR177## (v) ##STR178## (w) ##STR179## or (x) ##STR180## X is a single bond; r is one; and
- x is 0 to 2.
- 3. The compound according to claim 2 wherein:
- R.sup.1 is: --SO.sub.2 NHCO.sub.2 R.sup.23 ; and
- X is a single bond;
- E is a single bond;
- r is one;
- x is 0 to 2;
- R.sup.2a, R.sup.2b, R.sup.3a and R.sup.3b are each H, --C.sub.1 -C.sub.6 -alkyl, --C.sub.2 -C.sub.4 -alkynyl, --Cl, --F, --NO.sub.2, or --CF.sub.3 ;
- R.sup.6 is methyl, ethyl, -n-propyl, isopropyl, -n-butyl, -trans-2-butenyl, CH.sub.2 CH.sub.2 CF.sub.3, --CH.sub.2 CH.sub.2 CH.sub.2 CF.sub.3, -cyclopropyl, or -cyclopropylmethyl;
- R.sup.8a and R.sup.8b are each independently H, --NO.sub.2, --C.sub.1 -C.sub.4 -alkyl, --NHR.sup.4, --NR.sup.24 CO--R.sup.23, --S(O).sub.x -(C.sub.1 -C.sub.4 -alkyl), --N(CH.sub.3).sub.2, --OCH.sub.3, --NR.sup.24 COCH.sub.2 NH.sub.2, --NR.sup.24 COCH.sub.2 N(CH.sub.3).sub.2, --COOH, --COOCH.sub.3, --CH.sub.2 OCOCH.sub.3, Cl, --CH.sub.2 COOCH.sub.3, --NR.sup.24 CON(R.sup.4).sub.2, --NR.sup.24 CON-furoyl, --NR.sup.24 CO.sub.2 R.sup.4, --CH.sub.2 COOH, CH.sub.2 OH, aryl, heteroaryl, --CH.sub.2 -heteroaryl, ##STR181##
- 4. The compound according to claim 3 wherein:
- R.sup.1 is --SO.sub.2 NHCO.sub.2 R.sup.23 ;
- X is a single bond;
- R.sup.2a, R.sup.2b, R.sup.3a and R.sup.3b are each H, --C.sub.1 -C.sub.4 -alkyl, --Cl or F;
- R.sup.6 is methyl, ethyl, -n-propyl, isopropyl, -n-butyl, -trans-2-butenyl, CH.sub.2 CH.sub.2 CF.sub.3, --CH.sub.2 CH.sub.2 CH.sub.2 CF.sub.3, -cyclopropyl, or -cyclopropylmethyl;
- R.sup.8a and R.sup.8b are each independently H, --NO.sub.2, --C.sub.1 -C.sub.4 -alkyl, --NHR.sup.4, --NR.sup.24 CO--R.sup.23, --S(O).sub.x -(C.sub.1 -C.sub.4 -alkyl), --N(CH.sub.3).sub.2, --OCH.sub.3, --NR.sup.24 COCH.sub.2 NH.sub.2, --NR.sup.24 CON-furoyl, --NR.sup.24 COCH.sub.2 N(CH.sub.3).sub.2, --COOH, --COOCH.sub.3, --CH.sub.2 OCOCH.sub.3, Cl, --CH.sub.2 COOCH.sub.3, --NR.sup.24 CON(R.sup.4).sub.2, --NR.sup.24 CO.sub.2 R.sup.4, --CH.sub.2 COOH, CH.sub.2 OH, aryl, heteroaryl, --CH.sub.2 -heteroaryl, ##STR182##
- 5. The compound according to claim 4 which is
- ______________________________________ ##STR183##wherein:R.sup.x R.sup.y R.sup.z______________________________________Pr butyl NO.sub.2Pr butyl NH.sub.2Pr butyl BuNHCONHPr butyl EtNHCONHPr 2-dimethyaminoethyl EtNHCONHBu butyl iPrN(Me)CONHPr butyl iPrNHCONHPr propyl iPrNHCONHPr pentyl iPrNHCONHPr butyl MeNHCONHPr 3-methylbutyl EtNHCONHPr 3-methylbutyl MeNHCONHPr butyl n-PrNHCONHPr 2-cyclopropylethyl EtNHCONHPr 3,3-dimethylbutyl EtNHCONHBu pentyl iPrNHCONHBu butyl iPrNHCONHBu 2-methoxyethyl iPrNHCONHEt 3-methylbutyl EtNHCONHBu 2-cyclopropylethyl morpholinylCONHBu 3-methylbutyl EtNHCONHEt 2-cyclopropylethyl EtNHCONHPr 2-cyclopentylmethyl EtNHCONHBu 2-methoxyethyl EtNHCONHPr Butyl 2-pyridyl-Pr Butyl 3-pyridyl-Pr Butyl 4-MePh-Pr Butyl methyl(piperazinyl-N- acetyl)Pr Butyl methyl(piperazinyl-N- cyclopropylcarbonyl)Pr Butylmethyl(N1-imidazolyl)Pr benzyl EtNHCONHPr 2-methoxybenzyl EtNHCONHBu butyl EtNHCONHPr ethoxyethyl EtNHCONHPr benzyl nPrNHCONHPr 3-methylbutylyl 2-pyridylPr 3-methylbutyl 2-furoyl-CONH orEt benzyl EtNHCONH.______________________________________
- 6. A pharmaceutical composition useful in the treatment of hypertension which comprises a pharmaceutically acceptable carrier and a pharmaceutically effective amount of a compound of claim 1.
- 7. A method of treating hypertension which comprises administering to a patient in need of such treatment a pharmaceutically effective amount of a compound of claim 1.
- 8. An ophthalmological formulation for the treatment of ocular hypertension comprising an ophthalmologically acceptable carrier and an effective ocular antihypertensive amount of a compound of claim 1.
- 9. A method of treating ocular hypertension comprising administering to a patient in need of such treatment an effective ocular antihypertensive amount of a compound of claim 1.
RELATED APPLICATION
The present patent application is a continuation-is-part of copending application Ser. No. 698,506, filed May 10, 1991 now abandoned.
Foreign Referenced Citations (3)
Number |
Date |
Country |
5869690 |
Jan 1991 |
AUX |
407342 |
Jul 1989 |
EPX |
0411766 |
Feb 1991 |
EPX |
Continuation in Parts (1)
|
Number |
Date |
Country |
Parent |
698506 |
May 1991 |
|