Patent ID: 6225288
Filing Date: 2001-05-01
Classification: A61P,C07C,C07D

Abstract:
A compound represented by formula I: ##STR198##or a pharmaceutically acceptable salt, ester or hydrate thereof, wherein:a is 0 or 1:m is 1:n is 0, 1 or 2;Z is selected from the group consisting of:1) C.sub.1-18 alkyl,2) C.sub.3-11 cycloalkyl, said alkyl and cycloalkyl groups being optionally substituted with 1-4 halo groups,3) phenyl or naphthyl, optionally substituted by one or two groups selected from the group consisting of: halo, nitro, C.sub.1-4 alkyl and C.sub.1-4 alkoxy, said alkyl and alkoxy groups being optionally substituted with 1-3 halo groups, and4) HET.sup.1 wherein HET.sup.1 represents a 5 or 6 membered aromatic or non-aromatic ring, and the benzofused analogs thereof, containing from 1-3 heteroatoms selected from O, S and N, and optionally substituted with 1-2 groups selected from halo, C.sub.1-4 alkyl and C.sub.1-4 acyl:R.sup.1 represents a member selected from the group consisting of: H, aryl,C.sub.1-6 alkyl optionally substituted by OR.sup.7, and C.sub.5-7 cycloalkyl optionally containing one heteroatom selected from O, S and NR.sup.8,andR.sup.2 represents H,or in the alternative, R.sup.1 and R.sup.2 are taken in combination and represent a ring of 4-7 members, said ring optionally containing one heteroatom selected from O, S and NR.sup.8 ;R.sup.7 is selected from the group consisting of: H, C.sub.1-5 alkyl and benzyl optionally substituted with 1-2 groups selected from halo, C.sub.1-4 alkyl and C.sub.1-4 alkoxy; andR.sup.8 is H or C.sub.1-4 alkyl;each R.sup.3 is independently selected from the group consisting of: H, C.sub.1-6 alkyl optionally containing 1-2 oxo groups, C.sub.1-4 alkoxy and halo;R.sup.4, R.sup.5 and R.sup.6 are independently selected from the group consisting of:1) H,2) halo,3) C.sub.1-4 alkoxy optionally substituted with 1-3 halo atoms,4) NO.sub.2 S5) OH,6) benzyloxy, the benzyl portion of which is optionally substituted with 1-2 members selected from the group consisting of: halo, CN, C.sub.1-4 alkyl and C.sub.1-4 alkoxy, said alkyl and alkoxy being optionally substituted with 1-3 halo groups,7) NH--C.sub.1-4 acyl,8) C.sub.1-4 acyl,9) O--C.sub.1-4 alkyl-CO.sub.2 H, optionally esterified with a C.sub.1-6 alkyl or C.sub.5-7 cycloalkyl group,10) CH.dbd.CH--CO.sub.2 H,11) C.sub.0-5 alkylCO.sub.2 H,12) C.sub.0-5 alkylC(O)NH.sub.2, optionally substituted on the nitrogen atom by 1-2 C.sub.1-4 alkyl groups;13) C.sub.0-2 alkylS(O).sub.0-2 C.sub.1-4 alkyl14) S(O).sub.0-2 -C.sub.1-6 alkyl or S(O).sub.0-2 -phenyl, said alkyl and phenyl portions thereof being optionally substituted with 1-3 members selected from the group consisting of: halo, CN, C.sub.1-4 alkyl and C.sub.1-4 alkoxy, said alkyl and alkoxy being optionally substituted by 1-3 halo groups,15) benzoyl optionally substituted by 1-2 members selected from the group consisting of: halo, CN, C.sub.1-4 alkyl and C.sub.1-4 alkoxy, said alkyl and alkoxy groups being optionally substituted by 1-3 halo groups,16) phenyl or naphthyl, optionally substituted with 1-2 members selected from the group consisting of: halo, CN, C.sub.1-4 alkyl and C 1-4alkoxy, said alkyl and alkoxy being optionally substituted with 1-3 halo groups,17) CN,18) --C.sub.1-4 alkyl-HET.sup.2, wherein HET.sup.2 represents a 5-7 membered aromatic or non-aromatic ring containing 1-4 heteroatoms selected from O, S and NR.sup.8 and optionally containing 1-2 oxo groups, and optionally substituted with 1-3 C.sub.1-4 alkyl, OH, halo or C.sub.1-4 acyl groups;19) --OC.sub.0-4 alkyl-HET.sup.3, wherein HET.sup.3 is a 5 or 6 membered aromatic or non-aromatic ring containing from 1 to 3 heteroatoms selected from O, S and N, and optionally substituted with one or two groups selected from halo and C.sub.1-4 alkyl, and optionally containing 1-2 oxo groups, and20) HET.sup.4, wherein HET.sup.4 is a 5 or 6 membered aromatic or non-aromatic ring, and the benzofused analogs thereof, containing from 1 to 4 heteroatoms selected from O, S and N, and is optionally substituted by one or two groups selected from halo, C.sub.1-4 alkyl and C.sub.1-4 acyl, orR.sup.4 and R.sup.5 are taken in combination and represent a fused heteroaryl ring as shown below: ##STR199##wherein Y is selected from the group consisting of CH and N, and X is selected from O, S and NH, and R.sup.6 is as defined above.