| abstract |
Cyano- or amidino-aryl substituted bicyclic heterocycles of formula RaAHetArE (I) and their tautomers, regio-isomers and/or salts are new. A = phenylene-(1-3C) alkylene (optionally ring-substituted), 2-6C n-alkylene (optionally substituted) or 5-7C cycloalkylene-(1-3C) alkylene where methylene bonded to Ra is replaced by N (A groups are bonded to Het via alkylene moiety); E = CN or RbC(=NH); Rb = H, OH, alkyl or in vivo cleavable group; Ar = phenylene or naphthylene (both optionally substituted) or thienylene, thiazolylene, pyridinylene, pyrimidinylene, pyrazinylene or pyridazinylene (all optionally C-substituted); Het = indole, benzimidazole, quinolone or quinazolone derivative e.g. of formula (a); R1 = H, 1-4C alkyl or CF3; R2,R3 = H, H, A', COOH or COOA'; X = N, CH or C-(1-4C alkyl); A' = 1-3C alkyl; and Ra = e.g. phenyl-(1-3C)alkoxy, N-(phenyl-(1-3C)alkyl)-amino (optionally further N-substituted), N-(diphenyl-(1-3C)alkylcarbonyl)-amino (optionally further N-substituted by A') or phenylaminocarbonyl (optionally N-substituted) (alkyl substituents are optionally substituted). |