Rhodanine derivatives and pharmaceutical compositions.

摘要

Disclosed is a rhodanine derivative of formula (I). A rhodanine derivative of formula (I) <CHEM> wherein R<1> is hydrogen, C1-C8 alkyl, carboxyl(C1-C4)alkyl or (C1-C4)alkoxycarbonyl(C1-C4)alkyl; R<2> is -CH2-CH2-R<3>, &lparstr& CH=CH &rparstr& @R<3> (m is 0 or 1), - @=CH-R<4> (R is C1-C3 alkyl) or &lparstr& CH2 &rparstr& @CONHR<4> (n is 0 or 1-4); R<3> is a thienyl or furyl group which may be substituted by C1-C3 alkyl or halogen; a pyrrolyl group which may be substituted by carboxy(C1-C3)alkyl on the nitrogen atom; or a phenyl group which may be substituted by one or more substituents selected from the group consisting of C1-C3 alkyl, C1-C3 alkoxy, hydroxyl, halogen, trifluoromethyl, carboxyl, (C1-C3)alkoxycarbonyl, cyano, carboxy(C1-C3)alkoxy, (C1-C6)alkoxycarbonyl(C1-C3)alkoxy, benzyloxycarbonyl(C1-C3)alkoxy, piperidinylcarbonyl(C1-C3)alkoxy, 2H-tetrazolyl, 2H-tetrazolyl-(C1-C4)alkoxy, carboxy(C2-C4)alkenyl, (C1-C3)alkoxycarbonyl(C2-C4)alkenyl, carboxy(C1-C3)alkyl and (C1-C3)alkoxycarbonyl(C1-C3)alkyl; and R<4> is a phenyl group which may be substituted by one or more of the same substituents as defined above, or a pharmaceutically acceptable salt thereof. The derivatives are of an inhibitory activity against aldose reductase and useful for the prevention or treatment of complications of diabetes.