CARBOXILIC ACID AMIDAS OF REPLACED TIENOPIRROL, CARBOXILIC ACID AMIDES OF PIRROLOTIAZOL AND RELATED ANALOGS, AS INHIBITORS OF CASEINA QUINASA I EPSILON.

摘要

A compound of formula (I) or of formula (II): ** (See formula) ** in which X is S or S (O) n; R1 is H or C1-C6 alkyl; R2 is NR5R6; R3 is aryl or heterocycle; R4 is H, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, aryl- (C1-C6 alkyl), heterocycle- (C1-C6 alkyl), C1-C6 alkoxy, aryl- (C1-C6 alkoxy) , heterocycle- (C1-C6 alkoxy), CF3, halogen, SH, C1-6 alkylthio, aryl- (C1-C6 alkylthio), heterocycle- (C1-C6 alkylthio), NO2, NH2, NR5R6, aryl- (C1 alkylamino -C6), heterocycle- (C1-C6 alkylamino), or XR3, wherein X and R3 are as defined above; R5 is H or C1-C6 alkyl; R6 is H or C1-C6 alkyl; L is N or CR7 in which R7 is H or C1-C6 alkyl; M is S, O or NR8 in which R8 is H, C1-C6 alkyl, aryl- (C1-C6 alkyl), heterocycle- (C1-C6 alkyl) or acyl; n is 1 or 2; where aryl means any monocyclic, bicyclic or tricyclic carbon ring, of up to seven members in each ring, in which at least one ring is aromatic and is unsubstituted or substituted with one to three substituents selected from the group consisting of methylenedioxy, hydroxy, C1-C6 alkoxy, halogen, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, trifluoromethyl, trifluoromethoxy, -NO2, -NH2, -NH (C1-C6 alkyl), -N (C1-C6 alkyl ) 2, -NH-acyl and -N (C1-C6 alkyl) acyl. where acyl refers to a group H- (C = O) -, C1-C6 alkyl- (C = O) -, aryl- (C = O) -, aryl (C1-C6 alkyl) - (C = O) -, heterocyclo- (C = O) - or heterocycle (C1-C6 alkyl) - (C = O) -; where heterocycle means a stable 5 to 7 member monocyclic ring or 8 to 11 member stable bicyclic ring that is saturated or unsaturated, and consisting of carbon atoms and one to three heteroatoms selected from the group consisting of N, O and S, and where the nitrogen and sulfur heteroatoms may be optionally oxidized, and the nitrogen heteroatom may be optionally quaternized, and including any bicyclic group in which any of the heterocyclic rings defined above is fused to a benzene ring, the heterocycle being without replace or substituted with one to three substituents selected from the group consisting of C1-C6 alkoxy, hydroxy, halogen, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, trifluoromethyl, trifluoromethoxy, -NO2, -NH2, - NH (C1-C6 alkyl), -N (C1-C6 alkyl) 2, -NH-acyl and -N (C1-C6 alkyl) acyl; or a stereoisomer, enantiomer, racemate or tautomer thereof; or a pharmaceutically acceptable salt thereof.