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1. 发明授权

US5464616A 6.beta.-substituted penicillanic acids as beta-lactamase inhibitors 失效
标题翻译： 6β-取代的青霉烷酸作为β-内酰胺酶抑制剂
公开(公告)号：US5464616A
公开(公告)日：1995-11-07
申请号：US285670
申请日：1994-08-04
申请人： Kazuharu Noguchi , Ronald G. Micetich , Mohsen Daneshtalab
发明人： Kazuharu Noguchi , Ronald G. Micetich , Mohsen Daneshtalab
IPC分类号： C07D499/10 , A61K31/43 , A61P31/04 , C07D499/00 , C07D499/70 , C07D499/72 , C07D499/76 , A61K31/425
CPC分类号： C07D499/00
摘要： A 6.beta.-substituted penicillanic acid of the formula XII: ##STR1## or a pharmaceutically acceptable salt or ester thereof, whereinA and B are each hydrogen wherein the carbon atoms to which A and B are attached are linked by a single bond, or A and B together form a bond, wherein the carbon atoms to which A and B are attached are linked by a double bond,R1 is selected from the group consisting of a) hydrogen, b) a pharmaceutically acceptable salt and c) a pharmaceutically acceptable group selected from the group consisting of C.sub.1-10 alkyl, C.sub.2-10 alkenyl, C.sub.2-10 alkynyl, C.sub.3-10 cycloalkyl, C.sub.3-10 cycloalkenyl, allyl, aryl, aralkyl, aralkenyl, aralkynyl, heterocyclyl, heterocyclylalkyl, heterocyclylalkenyl, heterocyclylalkynyl and alkylheterocyclyl; wherein said group c) is unsubstituted or substituted with a substituent selected from the group consisting of floro, chloro, bromo, iodo, azido, nitro, monoalkyl substituted amino, dialkyl substituted amino, aryl substituted amino, alkanoylamino, arylcarbonylamino, cyano, hydroxy, alkoxy, aryloxy, alkanoyloxy, arylcarbonyloxy, mercapto, alkylthio, arylthio, alkanoylthio, arylcarbonylthio, oxyimino, alkoxyimino and carboxy, andn is an integer between 0 and 2.
摘要翻译：式XII的6β-取代的青霉烷酸：其中A和B各自为氢，其中A和B所连接的碳原子通过单键连接，或 A和B一起形成键，其中A和B连接的碳原子通过双键连接，R 1选自a）氢，b）药学上可接受的盐，和c）药学上可接受的盐选自C1-10烷基，C2-10烯基，C2-10炔基，C3-10环烷基，C3-10环烯基，烯丙基，芳基，芳烷基，芳烯基，芳炔基，杂环基，杂环基烷基，杂环基烯基，杂环基炔基和烷基杂环基其中所述基团c）未被取代或被选自以下的取代基取代：氟，氯，溴，碘，叠氮基，硝基，单烷基取代的氨基，二烷基取代的氨基，芳基取代的氨基，烷酰基氨基，芳基羰基氨基，氰基，羟基，烷氧基，芳氧基，烷酰氧基，芳基羰氧基，巯基，烷硫基，芳硫基，烷酰硫基，芳基羰硫基，氧亚氨基，烷氧基亚氨基和羧基，n为0〜2的整数。

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