Patent ID: 6265434
Filing Date: 2001-07-24
Classification: A61P,C07D

Abstract:
A compound of the formula I: ##STR291##wherein:R.sup.1 is --CO.sub.2 H;R.sup.2 is: ##STR292##whereinR.sup.7 is selected from:(1) hydrogen,(2) C.sub.1-6 alkyl, which is unsubstituted or substituted with 1-4 substituents where the substituents are independently selected from: hydroxy, cyano, and halo,(3) cyano,(4) hydroxy, and(5) halo,whereinX is selected from:C.sub.1-10 alkyl and -(C.sub.0-6 alkyl)C.sub.3-6 cycloalkyl(C.sub.0-6 alkyl)-,which is unsubstituted or substituted with 1-7 substituents where the substituents are independently selected from:(a) halo,(b) hydroxy,(c) --O--C.sub.1-3 alkyl,(d) trifluoromethyl,(e)-(C.sub.1-3 alkyl)hydroxy, and(f) ethylenedioxyand whereinR.sup.8 is selected from:phenyl, naphthyl, biphenyl, indanyl, tetrahydronapthyl and heterocycle,which is unsubstituted or substituted with 1-7 of R.sup.11 where R.sup.11 is independently selected from:(a) halo,(b) cyano,(c) hydroxy,(d) C.sub.1-6 alkyl, which is unsubstituted or substituted with 1-5 of R.sup.12 where R.sup.12 is independently selected from: halo, cyano, hydroxy, C.sub.1-6 alkoxy, --CO.sub.2 H, --CO.sub.2 (C.sub.1-6 alkyl), phenyl, trifluoromethyl, and --NR.sup.9 R.sup.10, wherein R.sup.9 is defined above and R.sup.10 is independently selected from the definitions of R.sup.9,(e) --O--C.sub.1-6 alkyl, which is unsubstituted or substituted with 1-5 of R.sup.12,(f) --CF.sub.3,(g) --CHF.sub.2,(h) --CH.sub.2 F,(i) --NO.sub.2,(j) phenyl,(k) --CO.sub.2 R.sup.9,(l) tetrazolyl,(m) --NR.sup.9 R.sup.10,(n) --NR.sup.9 --COR.sup.10,(o) --NR.sup.9 --CO.sub.2 R.sup.10,(p) --CO--NR.sup.9 R.sup.10,(q) --OCO--NR.sup.9 R.sup.10,(r) --NR.sup.9 CO--NR.sup.9 R.sup.10,(s) --S(O).sub.m --R.sup.9,wherein m is an integer selected from 0, 1 and 2,(t) --S(O).sub.2 --NR.sup.9 R.sup.10,(u) --NR.sup.9 S(O).sub.2 --R.sup.10,(v) --NR.sup.9 S(O).sub.2 --NR.sup.9 R.sup.10, and(w) C.sub.1-6 fluoroalkoxy;R.sup.3 is selected from the group consisting of:phenyl and thienyl,which is unsubstituted or substituted with 1 7 substituents where the substituents are independently selected from:(a) halo,(b) trifluoromethyl,(c) hydroxy,(d) C.sub.1-3 alkyl,(e) --O--C.sub.1-3 alkyl,(f) --CO.sub.2 R.sup.9,(g) --NR.sup.9 R.sup.10, and(h) --CONR.sup.9 R.sup.10 ;R.sup.4 is selected from:C.sub.1-10 alkyl, C.sub.3-8 cycloalkyl, -(C.sub.1-3 alkyl)-C.sub.3-8 cycloalkyl,C.sub.2-10 alkenyl, C.sub.2-10 alkynyl, phenyl, -(C.sub.1-6 alkyl)-phenyl, naphthyl, biphenyl, hydrogen, cyclohexenyl,dihydronaphthyl, tetrahydronaphthyl, and octahydronaphthyl,which is unsubstituted or substituted with 1-7 of R.sup.11 where R.sup.11 is independently as defined above;R.sup.5 is selected from:hydrogen or C.sub.1-6 alkyl, wherein the alkyl is unsubstituted or substituted with 1-7 substituents where the substituents are independently selected from:(a) halo,(b) trifluoromethyl,(c) hydroxy,(d) C.sub.1-3 alkyl,(e) --O--C.sub.1-3 alkyl,(f) --CO.sub.2 R.sup.9,(g) --NR.sup.9 R.sup.10, and(h) --CONR.sup.9 R.sup.10,or where R.sup.4 and R.sup.5 may be joined together to form a C.sub.3-8 cycloalkyl ring which may be unsubstituted or substituted with 1-7 of R.sup.11 ;R.sup.6 is independently selected from:hydrogen or C.sub.1-6 alkyl, wherein the alkyl is unsubstituted or substituted with 1-7 substituents where the substituents are independently selected from:(a) halo,(b) trifluoromethyl,(c) hydroxy,(d) C.sub.1-3 alkyl,(e) --O--C.sub.1-3 alkyl,(f) --CO.sub.2 R.sup.9,(g) --NR.sup.9 R.sup.10, and(h) --CONR.sup.9 R.sup.10 ;n is an integer selected from 0, 1, 2 and 3;and pharmaceutically acceptable salts thereof and individual diastereomers thereof.