HETEROCYCLYLMETHYL SUBSTITUTED DERIVATIVES OF PYRAZOLE, PROCESS OF THEIR PREPARATION, PHARMACEUTICAL COMPOSITIONS CONTAINING THEREOF AND THEIR USE FOR PREPARING MEDICAMENTS

摘要

1-(Benzyl or heterocyclylmethyl)-3-(substituted (hetero)aromatic)-fused pyrazole compounds of formula (I) are new. X = O, S NH or CH=CH, and the X-containing ring is optionally substituted by R14; R1 = phenyl, 2-thienyl, 2-pyrrolyl or 2-furanyl, all substituted by R4; R4 = CHOHCH3, 2-6C alkyl (substituted by OH or 1-4C alkoxy), CHO, 1-6C acyl, NO2, 1-6C alkyl (optionally substituted by NH2, N3 or OR5), CH2OR13, or a group of formula (a) or (b); A = phenyl (optionally mono-, di- or trisubstituted by alkyl, alkoxy, alkoxycarbonyl, (each with up to 6C), COOH, NO2, CN, CF3, N3 or halo; R5 = 1-5C acyl, SiR6R7R8, CH2OR10 or a group of formula (c); R6-R8 = 6-10C aryl, 1-6C alkyl; R9, R13 = H or 1-3C alkyl; R10-R12 = H or 1-4C alkyl; R14 = OH, halo, 1-4C alkoxy or 1-4C alkyl; a = 1-3: provided that when R4 = CH2OR13, then A = substituted phenyl where the substituents include alkoxycarbonyl, COOH, NO2, CN, CF3 or N3.