New 2-amino-thiazole derivs.

摘要

2-Aminothiazoles of formula (I) and their tautomers are new: R1 = NH2 or N=C(T1)-NT2T3; T1 = H, 1-6C alkyl or Ph; T2 and T3 = 1-6C alkyl, 5-7C cycloalkyl or Ph, or NT2T3 is a satd. 5- to 7-membered ring opt. contg. other heteroatoms; R3 = S(O)nX, SH or Y; n = 0-2; X = 3-8C cycloalkyl or opt. substd. 1-20C alkyl, 3-6C alkenyl, 3-6C alkynyl or phenyl; Y = 1-20C mono- or dialkylamino (opt. substd. and/or interrupted by O), 3-8C cycloalkylamino, adamantylamino, 2-12C mono- or dialkenylamino, 3-12C alkynylamino, N-(1-5C alkyl)anilino, pyrrolidino, piperidino, morpholino, thiomorpholino, 1-piperazinyl, 4-(1-4C alkyl)-1-piperazinyl, hexamethylenimino, 1-imidazolyl, 1-pyrazolyl, opt. substd. anilino, pyridylamino, thienylamino, NHNH2, 1-4C mono- or dialkylhydrazino or phenylhydrazino; R4 = 1-6C alkanoyl, benzoyl, CN, COT4 or C(T6)T5; T4 = OH, 1-6C alkoxy, NH2 or Y; T5 = H, 1-6C alkyl or Ph; T6 = NOH, NQ or the residue of a cpd. contg. a reactive CH2 gp.; Q = opt. substd. 1-20C alkyl (opt. interrupted by O), an opt. substd. 3-6C alkenyl, 3-6C alkynyl, 3-12C cycloalkyl or phenyl gp., pyridyl, 3-6C alkoxycarbonylmethyl, NH2, dialkylamino or anilino; provided that: (a) R3 is not SCH(COMe)COOETt or SCH(COMe)2 when R1 = NH2 and R4 = COMe or COOEt; (b) R3 is not SMe when R1 = NH2 and R4 = CN; (c) R1 is not NH2 when R3 = piperidino or morpholino and R4 = CN.