Patent ID: 6177588
Filing Date: 2001-01-23
Classification: A61P,C07C,C07F

Abstract:
A compound having the structure selected from formula (1) and formula (2) ##STR9##where R.sub.1 is alkyl of 1 to 10 carbons, (R.sub.4).sub.p -phenyl, RCO, or C.sub.1 -C.sub.6 trialkylsilyl;W.sub.1 of Formula 1 is O or S with the proviso that W.sub.1 is not S when R.sub.1 is RCO;W.sub.2 of Formula 2 is CH.sub.2 OR.sub.2, R.sub.2 CO, CO.sub.2 R.sub.2 or CON(R.sub.2).sub.2 ;p is an integer having the values 0 to 5;R is H, lower alkyl of 1 to 10 carbons, cycloalkyl of 3 to 10 carbons, halogen, (C.sub.1-10 -lower alkyl).sub.3 -silyl, C.sub.1-10 -lower alkylphenyl, or phenyl-C.sub.1-10 -lower alkyl;R.sub.2 and R.sub.3 independently are H, lower alkyl of 1 to 10 carbons, cycloalkyl of 3 to 10 carbons, (C.sub.1-10 -lower alkyl).sub.3 -silyl, C.sub.1-10 -lower alkylphenyl, or phenyl-C.sub.1-10 -lower alkyl;R.sub.4 is alkyl of 1 to 10 carbons, F, Cl, Br, I, NO.sub.2, (CH.sub.2).sub.p COOH, (CH.sub.2).sub.p COOR;n is an integer having the values of 0 to 6;X is C.tbd.C, C(O)O, CONR, CSNR, and (CR.dbd.CR).sub.n' where n' is an integer having the values 1 to 5;Y is a phenyl or naphthyl group, said phenyl and naphthyl groups being optionally substituted with one or two R groups, orwhen X is --(CR.dbd.CR).sub.n' -- and n' is 3, 4 or 5 then Y represents a direct valence bond between said (CR.dbd.CR).sub.n' group and B;A is (CH.sub.2).sub.q where q is 0-5, lower branched chain alkyl having 3-6 carbons, cycloalkyl having 3-6 carbons, alkenyl having 2-6 carbons and 1 or 2 double bonds, alkynyl having 2-6 carbons and 1 or 2 triple bonds;B is hydrogen, COOH or a pharmaceutically acceptable salt thereof, COOR.sub.8, CONR.sub.9 R,.sub.10, --CH.sub.2 OH, CH.sub.2 OR.sub.11, CH.sub.2 OCOR .sub.11, CHO, CH(OR.sub.12).sub.2, CHOR.sub.13 O, --COR.sub.7, CR.sub.7 (OR.sub.12).sub.2, CR.sub.7 OR.sub.13 O, or tri-lower alkylsilyl, where R.sub.7 is an alkyl, cycloalkyl or alkenyl group containing 1 to 5 carbons, R.sub.8 is an alkyl group of 1 to 10 carbons or (trimethylsilyl)alkyl where the alkyl group has 1 to 10 carbons, or a cycloalkyl group of 5 to 10 carbons, or R.sub.8 is phenyl or lower alkylphenyl, R.sub.9 and R.sub.10 independently are hydrogen, an alkyl group of 1 to 10 carbons, or a cycloalkyl group of 5-10 carbons, or phenyl or lower alkylphenyl, R.sub.11 is lower alkyl, phenyl or lower alkylphenyl, R.sub.12 is lower alkyl, and R.sub.3 is divalent alkyl radical of 2-5 carbons, or a pharmaceutically acceptable salt of said compound.