Patent ID: 6232334
Filing Date: 2001-05-15
Classification: A61P,C07D

Abstract:
A compound of the formula: ##STR46##wherein the ring A is a benzene ring which may be substituted or unsubstituted in addition to the R' group; with a substituent selected from the group consisting of 1) halogen; 2) nitro; 3) cyano; 4) amino; 5) N--C.sub.1-4, alkylamino; 6) N--N--di--C.sub.1-4 alkylamino; 7) phenylamino; 8) naphthylamino; 9) benzylamino; 10) naphthylmethylamino; 11) morpholino; 12) piperidino; 13) piperazino; 14) N-phenylpiperazino;15) a group having the formula --W--R.sup.13 wherein W is i) a chemical bond, ii) --O--, iii) --S-- or iv) --C(.dbd.O)-- andR.sup.13 is i) hydrogen or ii) C.sub.1-4 alkyl optionally substituted with a) hydroxyl, b) amino, c) dimethylamino, d) diethylamino, e) piperidino, f) morpholino, g) halogen or h) C.sub.1-4 alkoxy;16) a group having a formula: --(CH.sub.2).sub.p --CO--D wherein p is 0 or 1, and D is i) hydrogen, ii) hydroxyl, iii) amino, iv) N--C.sub.1-4 alkylamino: v) N--N--di-C.sub.1-4 alkylamino; vi) C.sub.1-6 alkoxy optionally substituted with a) hydroxyl, b) amino, c) dimethylamino, d) diethylamino, e) piperidino, f) morpholino, g) halogen, h) C.sub.1-6 alkoxy, i) C.sub.1-6 alkylthio, j) dioxolenyl or k) 5-methyl-2-oxo-1,3-dioxolen4-yl on the alkyl moiety, orvii) a group having the formula: --OCH(R.sup.9) OCOR.sup.10 whereinR.sup.9 is a) hydrogen, b) straight or branched C.sub.1-6 alkyl, c) cyclopentyl, d) cyclohexyl, or e) cycloheptyl, andR.sup.10 is a) straight or branched C.sub.1-6 alkyl, b) straight or branched C.sub.2-8 alkenyl, c) cyclopentyl, d) cyclohexyl, e) cycloheptyl, f) C.sub.1-3 alkyl which is substituted with phenyl, p-chlorophenyl or C.sub.5-7 cycloalkyl, g) C.sub.2-3 alkenyl which is substituted with phenyl or C.sub.5-7 cycloalkyl, h) phenyl, i) p-tolyl, j) naphthyl, k) straight or branched C.sub.1-6 alkoxy, l) straight or branched C.sub.2-8 alkenyloxy, m) cyclopentyloxy, n) cyclohexyloxy, o) cycloheptyloxy, p) C.sub.1-3 alkoxy which is substituted with phenyl or C.sub.5-7 cycloalkyl, g) C.sub.2-3 alkenyloxy which is substituted with phenvl or C.sub.5-7 cycloalkyl, r) phenoxy, s) p-nitrophenoxy or t) naphthoxy;17) tetrazolyl optionally protected with i) C.sub.1-4 alkyl optionally substituted with C.sub.1-4 alkoxy or phenyl, ii) C.sub.2 -.sub.5 alkanoyl or iii) benzoyl;18) trifluoromethanesulfonic amido;19) phosphono (PO(OH).sub.2); and 20) sulfo (SO.sub.2 H);whereby one or two of these substituents may be substituted at various positions of the benzene ring, andwhereby when two substituents are present at the 4 and 5 or 5 and 6 positions on the ring A, they may be taken together to form a benzene ringwhereby such rings may be substituted with the same groups as for the ring A,R.sup.1 is1) hydrogen:2) C.sub.1-8 alkalyl, C.sub.2-8 alkenyl, C.sub.2-8 alknyl or C.sub.3-6 cycloalkyl group which groups may be substituted with i) hydroxyl, ii) amino, iii) methylamino iv) halogen or v) C.sub.1-4 alkoxy;3) phenyl optionally substituted with i) halogen, ii) nitro, iii) C.sub.1-4 alkoxy or C.sub.1-4 alkyl; or4) phenyl-C.sub.1-4 alkyl optionally substituted with i) haloen, ii) nitro, iii) C.sub.1-4 alkoxy or iv) C.sub.1-4 alkyl on the benzene ring; andR.sup.2 is1) carboxyl;2) tetrazolyl;3) trifluoromethanesulfonic amido;4) phosphono (PO(OH).sub.2);5) sulfo (SO.sub.3 H);6) cyano; or7) C.sub.1-4 alkoxycarbonyl; each of which may be protected with i) C.sub.1-4 alkyl optionally substituted with C.sub.1-4 alkoxy or phenyl, ii) C.sub.2-5 alkanoyl or iii) benzoyl;X is a chemical bond, C.sub.1-4 alkylene wherein the number of carbon atoms in the straight chain of said C.sub.1-4 alkylene is 1 or 2, --CO--, --O--, --S--, --NH--, --CONH--, --OCHI--, SCH.sub.2 -- or --CH.dbd.CH--;R' is a group of the formula: --CO--D' wherein D' is hydroxy or lower (C.sub.1-6) alkoxy optionally substituted with hydroxy, optionally substituted amino, halogen, lower (C.sub.1-6) alkoxy, lower (C.sub.1-6) alkylthio or optionally substituted dioxolenyl on the alkyl moiety; Y is --O--, --S(O).sub.m -- or --N(R.sup.4)-- wherein m is an integer of 0, 1 or 2 and R.sup.4 is hydrogen or optionally substituted alkyl group, wherein R.sup.1 and R.sup.4 may be taken together with the N atom to form a ring and n is an integer of 1 or 2; or a pharmaceutically acceptable salt thereof.