PYRROLIDINE AND THIAZOLE DERIVATIVES WITH ANTIBACTERIAL AND METALLO-BETA-LACTAMASE INHIBITORY PROPERTIES

阅读量:

25

申请(专利)号:

PCT/EP1996/004014

申请日期:

19960909

公开/公告号:

WO1997010225A1

申请(专利权)人:

发明人:

GilpinMartinP LeonardDavidB JohnJohnHargreaves

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国省代号:

WO

摘要:

A method of treatment of bacterial infections in humans or animals with comprises administering, in combination with a beta-lactam antibiotic, a therapeutically effective amount of a thiazolidine or proline derivative of formula (I) or a pharmaceutically acceptable salt, solvate or in vivo hydrolysable ester thereof. Compounds (IA) falling within the scope of formula (I) are also claimed; in formula (I): X is S, S(O)n or CH2; n is 1 or 2; R is hydrogen, a salt forming cation or an in vivo hydrolysable ester-forming group; R1 and R2 are each hydrogen or an organic substituent group; R3 is hydrogen, (C1-6)alkyl optionally substituted by up to three halogen atoms, (C2-6)alkenyl, (C2-6)alkynyl, aryl, aryl(C1-6)alkyl, heterocyclyl or heterocyclyl(C1-6)alkyl; and R4 is hydrogen, or an in vivo hydrolysable acyl group. In compounds (IA) R31 represents (C1-6)alkyl substituted by up to three halogen atoms, aryl, aryl(C1-6)alkyl, heterocyclyl or heterocyclyl(C1-6)alkyl and X is S.

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