Patent ID: 6166037
Filing Date: 2000-12-26
Classification: C07D

Abstract:
A compound of the formula I: ##STR91## wherein: R.sup.1 is --X--R.sup.8, wherein X is selected from the group consisting of:(1) --CH.sub.2 --,(2) --CH.sub.2 CH.sub.2 --,(3) --CH.sub.2 CH.sub.2 CH.sub.2 --,(4) --CH(C.sub.1-6 alkyl)--,(5) --CO--,(6) -SO.sub.2 --,(7) --CONH.sub.2 --, and(8) --CONH(C.sub.1-6 alkyl)--,and wherein R.sup.8 is a selected from:phenyl, naphthyl, biphenyl, fluorenyl, dihydronaphthyl, tetrahydronaphthyl, octahydronaphthyl, C.sub.1-6 alkyl, C.sub.5-8 cycloalkyl, cyclohexenyl, adamantyl, and heteroaryl, which may be unsubstituted or substituted, where the substituents are independently selected from:(a) hydroxy,(b) C.sub.1-3 alkyl,(c) --O--C.sub.1-3 alkyl,(d) halogen,(e) trifluoromethyl,(f) phenyl(g) --CO.sub.2 (C.sub.1-6 alkyl), and(h) --CONH.sub.2 ;R.sup.2 is selected from the group consisting of: ##STR92## wherein R.sup.5 is a selected from: (1) --NR.sup.6 CO--O--R.sup.7, wherein R.sup.6 is hydrogen, C.sub.1-6 alkyl or C.sub.1-6 alkyl-C.sub.5-6 cycloalkyl, and R.sup.7 is C.sub.1-6 alkyl, C.sub.5-6 cycloalkyl, benzyl or phenyl, which is unsubsituted or substituted with halo, C.sub.1-3 alkyl, C.sub.1-3 alkoxy or trifluoromethyl,(2) --phenyl, which is unsubstituted or substituted with halo, C.sub.1-3 alkyl, C.sub.1-3 alkoxy or trifluoromethyl,(3) --C.sub.1-6 alkyl-phenyl, which is unsubsituted or substituted with halo, C.sub.1-3 alkyl, C.sub.1-3 alkoxy or trifluoromethyl,(4) --O--C.sub.1-6 alkyl-phenyl, which is unsubsituted or substituted with halo, C.sub.1-3 alkyl, C.sub.1-3 alkoxy or trifluoromethyl,(5) --C.sub.1-4 alkyl--O--C.sub.1-4 alkyl-phenyl, which is unsubsituted or substituted with halo, C.sub.1-3 alkyl, C.sub.1-3 alkoxy or trifluoromethyl,(6) --hydrogen,(7) --C.sub.1-6 alkyl,(8) --OH,(9) --CO.sub.2 (C.sub.1-6 alkyl), and(10) --CO--NR.sup.6 --(C.sub.0-3 alkyl)--R.sup.7 ;R.sup.3 is selected from the group consisting of:phenyl, naphthyl, biphenyl, fluorenyl, dihydronaphthyl, tetrahydronaphthyl, octahydronaphthyl, C.sub.1-6 alkyl, C.sub.5-8 cycloalkyl, cyclohexenyl, adamantyl, and heteroaryl, which may be unsubstituted or substituted, where the substituents are independently selected from:(a) hydroxy,(b) C.sub.1-3 alkyl,(c) --O--C.sub.1-3 alkyl,(d) halogen,(e) trifluoromethyl,(f) phenyl(g) --CO.sub.2 (C.sub.1-6 alkyl), and(h) --CONH.sub.2 ;R.sup.4a, R.sup.4b, R.sup.4c, R.sup.4d, R.sup.4e, R.sup.4f, R.sup.4g, and R.sup.4h are independently selected from the group consisting of:(1) hydrogen, and(2) C.sub.1-6 alkyl;m is 1 and n is 1;x is an integer selected from 0, 1, 2 and 3;y is an integer selected from 0, 1 and 2;and pharmaceutically acceptable salts thereof and individual diastereomers thereof.