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    • 4. 发明申请
    • 3-SUBSTITUTED CARBACEPHEMS
    • 3-取代的碳水化合物
    • WO1993025551A1
    • 1993-12-23
    • PCT/GB1993001092
    • 1993-05-26
    • SMITHKLINE BEECHAM PLCBURTON, GeorgeNAYLOR, Antoinette
    • SMITHKLINE BEECHAM PLC
    • C07D463/00
    • C07D463/22Y02P20/55
    • A compound of formula (I) or a salt thereof, wherein R is hydrogen, methoxy or formamido; R is an acyl group, in particular that of an antibacterially active cephalosporin; CO2R is a carboxy group or a carboxylate anion, or R is a readily removable carboxy protecting group or a pharmaceutically acceptable salt-forming group or in vivo hydrolysable ester group; R represents hydrogen or up to four substituents, which may be present on any of the carbon atoms in the ring system shown, selected from alkyl, alkenyl, alkynyl, alkoxy, hydroxy, halogen, amino, alkylamino, acylamino, dialkylamino, CO2R, CONR2, SO2NR2 where R is hydrogen or alkyl, aryl and heterocyclyl, which may be the same or different and wherein any R alkyl substituent is optionally substituted by one or more substituents selected from the list from which R is selected; Y is O, S, SO or SO2; and m is 1 or 2, a process for its preparation, use as an antibiotic and intermediates thereto.
    • 式(I)化合物或其盐,其中R 1是氢,甲氧基或甲酰氨基; R 2是酰基,特别是抗菌活性头孢菌素的酰基; CO 2 R 3是羧基或羧酸根阴离子,或R 3是容易除去的羧基保护基或药学上可接受的成盐基团或体内可水解的酯基; R 4表示氢或至多四个取代基,其可以存在于所示的环体系中的任何碳原子上,所述环系统选自烷基,烯基,炔基,烷氧基,羟基,卤素,氨基,烷基氨基,酰氨基,二烷基氨基, CO 2 R,CONR 2,SO 2 NR 2,其中R是氢或烷基,芳基和杂环基,其可以相同或不同,并且其中任何R 4烷基取代基任选被一个或多个选自以下的取代基取代:其中R 4, 被选中 Y是O,S,SO或SO 2; m为1或2,其制备方法,用作抗生素及其中间体。