Patent ID: 6174883
Filing Date: 2001-01-16
Classification: A61P,C07D

Abstract:
A compound of the formula ##STR30##and the pharmaceutically-acceptable salts thereof, whereinX is H, F, Cl, Br, (C.sub.1 -C.sub.6)alkyl, (C.sub.3 -C.sub.8)cycloalkyl, NO.sub.2, CF.sub.3, CN, SH, S(O).sub.m R.sup.3, OR.sup.4, COR.sup.4 or CONR.sup.4 R.sup.5 ;Y is H, F, Cl, Br, (C.sub.1 -C.sub.6)alkyl, (C.sub.3 -C.sub.8)cycloalkyl, NO.sub.2, CF.sub.3, CN, SH, S(O).sub.q R.sup.17, OR.sup.18, COR.sup.18 or CONR.sup.18 R.sup.19 ;R.sup.1 is H, alkanoyl of two to ten carbon atoms, cycloalkylcarbonyl of five to seven carbon atoms, phenylalkanoyl of seven to ten carbon atoms, chlorobenzoyl, methoxybenzoyl, thenoyl, omega-alkoxycarbonylalkanoyl, said alkoxy having one to three carbon atoms and said alkanoyl having three to five carbon atoms, alkoxy carbonyl of two to ten carbon atoms, phenoxycarbonyl, 1-(acyloxy)alkyl wherein acyl has one to four carbon atoms and said alkyl has two to four carbon atoms, 1-(alkoxycarbonyloxy)alkyl wherein said alkoxy has two to five carbon atoms and said alkyl has one to four carbon atoms, alkyl of one to three carbon atoms, alkylsulfonyl of one to three carbon atoms, methylphenylsulfonyl or dialkylphosphonate wherein each of said alkyl is one to three carbon atoms;R.sup.2 is COR.sup.6, CONR.sup.7 R.sup.8, (C.sub.1 -C.sub.6)alkyl, (C.sub.3 -C.sub.8)cycloalkyl, phenyl or mono- or disubstituted phenyl wherein the substituent or substituents are each Cl, F, Br, (C.sub.1 -C.sub.6)alkyl, (C.sub.1 -C.sub.6)alkoxy or CF.sub.3 ; ##STR31##A is H, F, Cl, Br, I, CF.sub.3, OR.sup.9, S(O).sub.p R.sup.10, COOR.sup.11, CONR.sup.9 R.sup.11, CN, NO.sub.2, COR.sup.10, CH.sub.2 OR.sup.11, OCOR.sup.10, NR.sup.9 R.sup.11, N(R.sup.9)COR.sup.11, SO.sub.2 NR.sup.9 R.sup.11, ##STR32##B is H, F, Cl, Br, I, CF.sub.3, OR.sup.13, S(O).sub.t R.sup.14, COOR.sup.15, CONR.sup.13 R.sup.15, CN, NO.sub.2, COR.sup.14, CH.sub.2 OR.sup.15, OCOR.sup.14, NR.sup.13 R.sup.15, N(R.sup.13)COR.sup.15 or SO.sub.2 NR.sup.13 R.sup.15 ;provided that A and B cannot both be H, or A and B are taken together, bonded to the same ring carbon of Q.sup.1 and equal oxo, or when A is not H, B is as defined above or (C.sub.1 -C.sub.4)alkyl;Q.sup.1 is ##STR33##m, n, p, q and t are each zero, one or two;W and Z are each O, S or NR.sup.11 ;W.sup.1 and W.sup.2 are each O, S or NR.sup.10 provided that when one of W.sup.1 and W.sup.2 is O, S or NR.sup.10, the other is O or S;R.sup.3, R.sup.6, R.sup.10, R.sup.14 and R.sup.17 are each (C.sub.1 -C.sub.6)alkyl or phenyl; R.sup.5, R.sup.8, R.sup.11, R.sup.15 and R.sup.19 are each H, (C.sub.1 -C.sub.6)alkyl or phenyl; R.sup.4, R.sup.7, R.sup.9, R.sup.13 and R.sup.18 are each H or (C.sub.1 -C.sub.6)alkyl; and R.sup.12 is H, F, Cl, Br, CF.sub.3 or (C.sub.1 -C.sub.6) alkyl; provided that when Q.sup.1 is ##STR34##then A is not H, F, Cl, Br, I, CF.sub.3, OR.sup.9, S(O).sub.p R.sup.10, COOR.sup.11, CONR.sup.9 R.sup.11, CN, NO.sub.2, COR.sup.10, CH.sub.2 OR.sup.11, OCOR.sup.10, NR.sup.9 R.sup.11, N(R.sup.9)COR.sup.11, SO.sub.2 NR.sup.9 R.sup.11 or ##STR35##and A and B are not taken together to equal oxo.