| abstract |
This refers to thiazol-4-carboxamide derivatives of the general formula (1) and to methods for obtaining them, said compounds are useful as glutamate metabotropic receptor antagonists. Claim 1: Compounds of the formula (1) wherein R1 is aryl or heteroaryl, which are optionally substituted by one or more -OH, Cl, F, Br, cyano, C1-7 alkyl, C1-7 alkoxy, -O - (CO) -C1-7 alkyl, C3-6 cycloalkyl, - (CH2) m-Ra, wherein Ra is -OH, -CH2F, -CHF2, -CF3, - C1-7 alkoxy, C3-6 cycloalkyl , -NH (CO) -C 1-7 alkyl, or -O- (CO) -C 1-7 alkyl; R2 is H, C1-7 alkyl, - (CH2) m-O-C1-7 alkyl or C3-6 cycloalkyl; R3 is C1-7 alkyl, - (CH2) m-Rb, wherein Rb is -O-C1-7 alkyl, C3-6 cycloalkyl, 5- or 6-chain heterocycloalkyl, aryl optionally substituted by F, or optionally substituted heteroaryl by C1-7 alkyl; - (CO) -Rc, wherein Rc is -O- (CH2) m-C3-6 cycloalkyl, or aryl; C3-6 cycloalkyl; or heterocycloalkyl of 5 or 6 links; or aryl or heteroaryl which are optionally substituted by: cyano, Cl, F, Br, CF3, CHF2, C3-6 cycloalkyl, or -O-C1-7 alkyl; or - (CO) -Rd, wherein Rd is C1-7 alkyl, NH2, or -O-C1-7 alkyl; or - (CH2) m-Re, wherein Re is OH, C1-7 alkoxy, CHF2, CF3, NH2, - NH- (CO) -C1-7 alkyl; -NH- (CO) -O- C1-7 alkyl; or -NH- (CO) -C 1-7 alkyl; or -O-CH2F, -O-CHF2, -O-CF3; or -S (O) 2-Rf, wherein Rf is C1-7 alkyl, -NH2, -NH-C1-7 alkyl or -N-di (C1-7 alkyl), or heteroaryl optionally substituted by C1- alkyl 7; R4 is H, C1-7 alkyl or (C1-7 alkyl) -C3-6 cycloalkyl; m is a number from 1 to 4; as well as pharmaceutically acceptable salts thereof. |