申请人:Zeneca Limited
公开号:US05571805A1
公开(公告)日:1996-11-05
The present invention relates to carbapenems and provides a compound of the formula (I) ##STR1## wherein: R.sup.1 is 1-hydroxyethyl, 1-fluoroethyl or hydroxyethyl; R.sup.2 is hydrogen or C.sub.1-4 alkyl; R.sup.3 is hydrogen or C.sub.1-4 alkyl; P is of the formula (IA), (IB) or (IC) ##STR2## and in the formula (IB) the naphthyl group may be bonded to the nitrogen of the linking carbamoyl group at either ring; Z is carboxy, sulfonic acid, sulfinic acid, C.sub.1-4 alkanamidosulfonyl (--SO.sub.2 NHCOC.sub.1-3 alkyl), benzamidosulfonyl, C.sub.1-4 alkylsulfonylcarbamoyl (--CONHSO.sub.2 C.sub.1-4 alkyl), phenylsulfonylcarbamoyl, C.sub.1-4 alkoxy carbamoyl, hydroxycarbamoyl, sulfoamino, N--C.sub.1-4 alkanesulfonamido, cyanocarbamoyl, cyanosulfamoyl, tetrazol-5-yl, 3-hydroxyisoxazol-4-yl and 3-hydroxyisoxazol-5-yl; and P is optionally further substituted provided that when P is of the formula (IA) or (IC), Z is not carboxy; or a pharmaceutically acceptable salt or in vivo hydrolysable ester thereof. Processes for their preparation, intermediates in their preparation, their use as therapeutic agents and pharmaceutical compositions containing them are also described.
本发明涉及碳青霉烯类药物,并提供了一种具有以下结构的化合物(I):
其中:R.sup.1为1-羟基乙基、1-氟乙基或羟基乙基;R.sup.2为氢或C.sub.1-4烷基;R.sup.3为氢或C.sub.1-4烷基;P为以下结构之一(IA)、(IB)或(IC):
在结构(IB)中,萘基可以与连接的碳酰胺基团的氮原子结合在任一环上;Z为羧基、磺酸、亚磺酸、C.sub.1-4烷基氨基磺酰(-SO.sub.2 NHCOC.sub.1-3烷基)、苯甲酰磺酰、C.sub.1-4烷基磺酰基碳酰胺(-CONHSO.sub.2 C.sub.1-4烷基)、苯基磺酰基碳酰胺、C.sub.1-4烷氧基碳酰胺、羟基碳酰胺、磺酰氨基、N-烷基磺酰氨基、氰基碳酰胺、氰基磺酰胺、四唑-5-基、3-羟基异噁唑-4-基和3-羟基异噁唑-5-基;P可进一步取代,但当P为结构(IA)或(IC)时,Z不为羧基;或其药学上可接受的盐或体内可水解的酯。还描述了其制备方法、制备中间体、作为治疗剂的用途以及含有它们的药物组合物。