Patent ID: 6048856
Filing Date: 2000-04-11
Classification: C07D

Abstract:
A compound of formula I ##STR18## wherein R.sup.1, R.sup.1a, R.sup.2 and R.sup.2a independently are hydrogen, halogen, cyano, trifluoromethyl, methylthio, hydroxy, C.sub.1-6 -alkyl or C.sub.1-6 -alkoxy;X is ortho-phenylene, --CH.sub.2 CH.sub.2 --, --CH.dbd.CH--CH.sub.2 --, --CH.sub.2 --CH.dbd.CH--, --CH.sub.2 --(C.dbd.O)--, --(C.dbd.O)--CH.sub.2 --, --CH.sub.2 CH.sub.2 CH.sub.2 --, --CH.dbd.CH--, --N(R.sup.5)--(C.dbd.O)--, --(C.dbd.O)--N(R.sup.5)--, --O--CH.sub.2 --O--, --CH.sub.2 --O--CH.sub.2 --, --(CH.sub.2)N(R.sup.5)--, --N(R.sup.5)(CH.sub.2)--, --N(CH.sub.3)SO.sub.2 --, --SO.sub.2 N(CH.sub.3)--, --CH(R.sup.6)CH.sub.2 --, --CH.sub.2 CH(R.sup.6)--, --(C.dbd.O)-- or --N(R.sup.7)-- wherein R.sup.5 and R.sup.7 independently are hydrogen or C.sub.1-6 -alkyl and wherein R.sup.6 is C.sub.1-6 -alkyl or phenyl;Y is >N--, >CH--, >N--(C.dbd.O)-- or >C.dbd.C(R.sup.8)-- wherein only the underscored atom participates in the ring system and wherein R.sup.8 is hydrogen or C.sub.1-6 -alkyl;A is --CH.dbd.CR.sup.9 --, --CR.sup.9 .dbd.CH--, --C.dbd.C--, --(C.dbd.O)--, --(C.dbd.CH.sub.2)--, --(CR.sup.9 R.sup.10)--, --CH(OR.sup.11)--, --CH(NHR.sup.11)--, phenylene, C.sub.3-7 -cycloalkylene or the completion of a bond wherein R.sup.9 and R.sup.10 independently are hydrogen, C.sub.1-6 -unbranched alkyl, C.sub.3-6 -branched alkyl or C.sub.3-8 -cycloalkyl and wherein R.sup.11 is hydrogen or C.sub.1-6 -alkyl;r and s independently are 0, 1, 2, 3 or 4;R.sup.12 is hydrogen, --(CH.sub.2).sub.N OH or --(CH.sub.2).sub.p COR.sup.17 wherein n is 1, 2, 3, 4, 5 or 6 and wherein p is 0 or 1 and wherein R.sup.17 is --OH, --NHR.sup.20 or C.sub.1-6 -alkoxy wherein R.sup.20 is hydrogen or C.sub.1-6 -alkyl; andR.sup.13 is cyano, --NR.sup.5 --Z or --(CHR.sup.21).sub.q --Z wherein R.sup.5 is as defined above and wherein q is 0, 1, 2, 3, 4, 5 or 6, and wherein R.sup.21 is hydrogen, halogen, cyano, trifluoromethyl, hydroxy, C.sub.1-6 -alkyl, C.sub.1-6 -alkoxy, --NR.sup.5 R.sup.7 or --COOH, and wherein Z is C.sub.3-8 -cycloalkyl, phenyl, naphthyl or pyrrolidinyl, which rings may optionally be substituted with one or more of halogen, cyano, trifluoromethyl, hydroxy, methylthio, C.sub.1-6 -alkyl or C.sub.1-6 -alkoxy; ora pharmaceutically acceptable salt thereof.