Patent ID: 6043358
Filing Date: 2000-03-28
Classification: A61P,C07D

Abstract:
A compound of Formula I ##STR30## or a pharmaceutically acceptable salt thereof wherein: side a or side b has a double bond,X is O,R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are each independently selected from the group consisting of:(a) hydrogen,(b) hydroxy,(c) amino,(d) cyano,(e) fluoro, chloro, bromo and iodo,(f) trifluoromethyl,(g) C.sub.1-6 alkyl,(h) C.sub.1-6 alkoxy,(i) C.sub.1-6 alkylthio,(j) C.sub.1-6 alkylcarbonyl,(k) mono- and di-C.sub.1-6 alkylamino,(l) aryl, where aryl is phenyl and naphthyl,(m) aryloxy, where aryl is phenyl and naphthyl, and(n) heteroaryl, wherein heteroaryl is selected from the group consisting of:(1) pyridyl,(2) furanyl,(3) thienyl,(4) pyrazinyl,(5) pyrimidyl,(6) thiazolyl and(7) triazolyl,each of (g) to (n) being optionally mono- or di- substituted, the substituents being independently selected from:(1) hydroxy,(2) C.sub.1-4 alkyl,(3) C.sub.1-3 alkoxy,(4) amino,(5) mono- and di-C.sub.1-6 alkylamino,(6) carboxyl,(7) C.sub.1-3 alkylthio,(8) C.sub.1-3 alkyl-S(O).sub.k --, where k is 1 or 2,(9) C.sub.1-4 alkoxycarbonyl,(10) halo selected from fluoro, chloro, bromo, and iodo,(11) oxo and(12) amidino,R.sub.5 is selected from the group consisting of:(a) hydrogen,(b) C.sub.1-6 alkylcarbonyl,(c) aroyl, wherein the aroyl group is benzoyl,(d) aroylaminocarbonyl, wherein the aroyl group is benzoyl and naphthoyl, and(e) R.sub.6 R.sub.7 N--SO.sub.O.sub.2 --NH--C(.dbd.O)--, wherein R.sub.6 and R.sub.7 are independently selected from the group consisting of:(1) hydrogen,(2) C.sub.1-6 alkyl and(3) aryl, wherein the aryl group is selected from phenyl,each of (b) to (e) being mono- or di- substituted, the substituents being independently selected from:(1) hydroxy,(2) C.sub.1-3 alkoxy,(3) amino,(4) mono- and di-C.sub.1-6 alkylamino,(5) carboxyl,(6) C.sub.1-3 alkylthio,(7) C.sub.1-3 alkyl-S(O).sub.k --, where k is 1 or 2,(8) C.sub.1-4 alkoxycarbonyl,(9) halo selected from fluoro, chloro, bromo, and iodo,(10) oxo and(11) amidino.