Patent ID: 6051586
Filing Date: 2000-04-18
Classification: C07D

Abstract:
A compound of the formula I: ##STR107## wherein R is hydrogen, hydroxy, oxo, halo, C.sub.1 -C.sub.10 haloalkyl, C.sub.1 -C.sub.10 alkyl, cyano, nitro, NR.sup.1 R.sup.1, SR.sup.1, OR.sup.1, SO.sub.2 R.sup.2, OCOR.sup.2, NR.sup.1 COR.sup.2, COR.sup.2, NR.sup.1 SO.sub.2 R.sup.2, NR.sup.1 CO.sub.2 R.sup.1, pyrrole, or Ar.sup.2, each moiety being optionally substituted with hydroxy, halogen, cyano, NR.sup.1 R.sup.1, SR.sup.1, trifluoromethyl, OR.sup.1, C.sub.3 -C.sub.8 cycloaklyl, phenyl, NR.sup.1 COR.sup.2, COR.sup.2, SO.sub.2 R.sup.2, OCOR.sup.2, NR.sup.1 SO.sub.2 R.sup.2, or NR.sup.1 CO.sub.2 R.sup.1 ;R is hydrogen, C.sub.1 -C.sub.10 alkyl optionally substituted with 1 to 4 substituents selected from hydroxy, halogen, CO.sub.2 H, CO.sub.2 C.sub.1 -C.sub.10 alkyl, SO.sub.2 C.sub.1 -C.sub.10 alkyl, C.sub.1 -C.sub.10 alkoxy; or C.sub.3 -C.sub.8 cycloalkyl, phenyl or naphthyl, each optionally substituted with 1 to 4 substituents selected from halogen, nitro, oxo, C.sub.1 -C.sub.10 alkyl, C.sub.1 -C.sub.10 alkoxy, and C.sub.1 -C.sub.10 alkylthio;R.sup.2 is R.sup.1 or NR.sup.1 R.sup.1 ;R.sup.3 is hydrogen, C.sub.1 -C.sub.10 alkyl or ##STR108## Ar.sup.1 is Ar.sup.1 --O--CH.sub.2, phenyl, or a 5 or 6 membered heterocyclic ring with from 1 to 4 heteroatoms selected from O, S and N, each moiety being optionally fused to a 5 or 6 membered heterocyclic ring containing from 1 to 4 hetero atoms selected from O, S, and N, the fused heterocyclic ring being optionally fused to a phenyl ring or substituted with oxo;m is 1, 2 or 3;(CH.sub.2).sub.m may be optionally replaced with C--(O)--(CH.sub.2).sub.m ;X is SO.sub.2 -piperizinyl, NR.sup.3 --SO.sub.2, or SO.sub.2 --NR.sup.3 ;n is 0, 1, 2, 3, or 4;Ar.sup.2 is phenyl, or a 5 or 6 membered heterocyclic ring with from 1 to 4 heteroatoms selected from O, S and N, each moiety being optionally substituted with halogen, C.sub.1 -C.sub.10 alkyl, C.sub.1 -C.sub.10 alkoxy, and OR, or being fused to a 5 or 6 membered heterocyclic ring containing from 1 to 4 hetero atoms selected from O, S, and N, the fused heterocyclic ring being optionally fused to a phenyl ring or optionally substituted with oxo;Y is O--Y, NR.sup.1, NR.sup.1 CO, C.sub.3 -C.sub.8 cycloalkyl or a 5 or 6 membered heterocyclic ring with from 1 to 4 heteroatoms selected from O, S and N, each of which is optionally fused to phenyl, or optionally substituted with oxo;p is 0 or 1;R.sup.4 is hydrogen, R.sup.1, R.sup.2, oxo, C.sub.1 -C.sub.10 heteroalkyl, C.sub.1 -C.sub.10 alkyl, C.sub.1 -C.sub.10 haloalkyl, each being optionally substituted with C.sub.3 -C.sub.8 cycloalkyl, phenyl, naphthyl, benzofuran, carbazole, dibenzothiofuran, or a 5 or 6 membered heterocyclic ring with from 1 to 4 heteroatoms selected from O, S, and N, each ring structure being optionally substituted with halo and C.sub.1 -C.sub.10 alkyl,and pharmaceutically acceptable salts and esters thereof.