PROCESS FOR THE PREPARATION OF THIAZOLES AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM

摘要

Thiazoles of formula (I) and their acid addn. salts are new, where R1 = H, CF3, 1-6C alkyl, 3-6C cycloalkyl, 3-6C cycloalkyl(1-3C)alkyl, phenyl or phenyl(1-3C)alkyl; R2 is R1, but not CF3, or R1+R2 are together tri-, tetra- or penta-methylene opt. substd. on same or different C by 1 or 2 Me) or (CH3)2C.O.C(CH3)2; W = 2-6C alkylene, 4-6C alkenylene or alkynylene, the multiple bond not being on the C atom bonded to N; X-Y = NCH2, C=CH or CH2CH2; R3 is one of the gps. (i)-(xiv) and when X-Y = NCH2, R3 can also be -NR8R9; A = CR4R5, NR6, O or S; B = CR4R5 or CO; m = 0 or 1; R4 and R4' = H or 1-4C alkyl; R5 and R5' = H, 1-4C alkyl, phenyl or phenyl(1-4C)alkyl; t = 4 or 5; R6 = H or 1-3C alkyl; R7 = H, 1-3C alkyl, phenyl(1-3C)alkyl or phenoxy(1-3C)alkyl; U=L = N=CR5 or CR5=N; A' = CR4R5 or NR6; D = CR4R5, CO, NR6, S or O; E = N or CH; M-V = CR4R5-CR4R5 or CR5=CR5; R8 = H or 1-3C alkyl; R9 = COR10, CONR11R12, SO2R10 or SO2NR11R12; R10 = 1-6C alkyl, 3-6C cycloalkyl, phenyl or phenyl(1-3C)alkyl (opt. phenyl rings substd. by 1-3 of halo, 1-3C alkyl, OH, MeO, methylenedioxy, NH2 or CF3); R11 and R12 = H or 1-3C alkyl, or together they complete tetra- or penta-methylene; at least one of R1, R2 and R8 is other than H when W = (CH2)2 and R9 = 4-aminophenylcarbonyl.