CEPHEM COMPOUNDS AND PHARMACEUTICAL USE THEREOF

摘要

7-Arylalkanoylamido-3-heterocyclylthio-cephem carboxylates of formula (I) and their salts are new: R1 = aryl 1-6C alkyl (optionally containing 1-3 suitable substituents from hydroxy, halogen, or 1-6C alkyl which optionally forms a ring with the other alkyl), heterocyclyl 1-6C alkyl (optionally containing 1-3 substituents from halogen, amino (optionally protected), 2-6C alkenyl, or 1-6C alkylidene), or 3-7C cyanoalkenyl-thio 1-6C alkyl; R2 = a heterocyclyl containing 1-3 substituents from acyl 1-6C alkyl, 1-6C hydroxyalkyl or aminoalkyl (optionally protected), mono- or di- (1-6C alkyl)amino 1-6C alkyl, acyl, acylamino, carboxyaryl, and also optionally 1-6C alkyl; heterocyclyl 2-6C alkenyl, or heterocyclyl-thio 1-6C alkyl group (both optionally having 1-3 suitable substituents); pyridyl 1-6C alkyl; pyrazolyl-ethyl optionally substituted by aryl 1-6C alkyl; thiadiazolyl 1-6C alkyl; thiadiazolyl (optionally substituted by1-6C alkyl), or 5-aminothiazolyl; and R3 = carboxy (optionally protected); provided that (i) when R1 = arylalkyl and R2 = thiadiazolyl substituted by 1-6C alkyl, then R3 = acyloxy 2-7C alkoxycarbonyl; and (ii) when R1 = aryl 1-6C alkyl substituted by halogen, or aminothiazolyl 1-6C alkyl, then R2 is not thiadiazolyl substituted by 1-6C alkyl. Note; the word "having" which occurs several times in the definitions, is taken to mean "substituted by".