| 摘要 |
Agent for treatment or prevention of glomerulopathy comprise a sulphonamide derivative of formula R4-R3-SO2-N(R2)C(R1)COY (I) or its salt or hydrate. R1, R2 = H or optionally substituted lower alkyl, aryl, aralkyl, heteroaryl or heteroarylalkyl; R3 = 4-phenylene or 2,5-thiophendiyl; R4 = OPh, Tet-Ph, Ctriple boundCPh, NHCOPh, Het-Ph, phenyl parasubstituted by R6 or 2-R5-thiophen-5-ylethynyl; Ph = phenyl para-substituted by R6; Tet = tetrazol-2,5-diyl; Het = oxazol-2,5-diyl or oxadiazol-3,5-diyl bonded to phenyl through the 5 and 3 positions respectively or thiophen-2,5-diyl; R5 = H, OH, lower alkylthio, SH, cycloalkyl, halo, COOH, lower alkoxycarbonyl, NO2, CN, lower haloalkyl, aryloxy, guanidino, lower alkenyl, lower alkynyl, acyl, acyloxy, CONRaRb, NRcCORd or optionally substituted lower alkoxy, amino, lower alkyl, unsaturated heterocyclyl or heteroaryl; Ra-Rc = H, lower alkyl or aralkyl; Rd = lower alkyl, aryl or aralkyl; R6 = cycloalkyl, lower alkoxy, halo, lower alkylthio, carboxy, lower alkoxycarbonyl, aryloxy, phenyl or optionally substituted lower alkyl, amino, unsaturated heterocyclyl or heteroaryl; Y = NHOH or OH. (I) are new when R4 = 2-R5-thiophen-5-ylethynyl, Ph-Tet or Ph-Het1 and R3 = 2,5-thiophen-diyl; or R4 = Ph-Het2 and R3 = 4-phenylene; Het1 = oxazol-2,5-diyl; Het2 = 2,5-thiophendiyl, tetrazol-2,5-diyl bonded to Ph through the 5 position or oxadiazol-3,5-yl; R5, R6 = H, lower alkylthio, halo or optionally substituted alkoxy, amino, alkyl or unsaturated heterocyclyl and R2 = H or lower alkyl. |
