发明名称 2-OXOAZETIDINE DERIVATIVES, THEIR PRODUCTION AND USE
摘要 <p>This invention relates to a novel compound of the formula and its production process, < IMG > ¢I! wherein R1 is an amino group which may be acylated or protected; X is hydrogen or a methoxyl group; R4 is (1) a sulfamoyl group, (2) a group of the formula, -S-Y-Z where Y is alkylene or alkenylene with up to 3 C atoms, and Z is ? alkanoyloxy with 2 to 4 C atoms, ? carbamoyl optionally substituted by sulfo, ? a carbamoyloxy or haloacetyl-carbamoyloxy, ? sulfocarbamoyloxy, or ? amino optionally substituted by sulfo, alkanoyl or aralkyloxycarbonyl, (3) triazolyl which is bonded with the azetidine ring on a nitrogen atom of the triazol ring, optionally substituted by alkoxycarbonyl, or (4) azido, with the proviso that when R4 is azido, R1 is a group, < IMG > where Q is alkylene with 1 to 3 C atoms, and T is optionally esterified carboxyl, the ester residue being lower alkyl optionally substituted by trimethylsilyl, or a pharmaceutically acceptable salt or ester thereof. The compound ¢I!, and a pharmaceutically acceptable salt or ester thereof exhibit excellent antimicrobial activity against gram-positive and gram-negative bacteria, and .beta.-lactamase inhibitory activity, thus being of value as a prophylactic or therapeutic agent for infectious diseases in mammals.</p>
申请公布号 CA1206968(A) 申请公布日期 1986.07.01
申请号 CA19830429158 申请日期 1983.05.30
申请人 TAKEDA CHEMICAL INDUSTRIES, LTD. 发明人 OCHIAI, MICHIHIKO;MATSUO, TAISUKE, (DECEASED)
分类号 C07D205/08;A61K31/395;A61K31/397;A61K31/41;A61K31/425;A61P31/04;C07D205/095;C07D403/04;C07D403/12;C07D417/12;C07D417/14;C07F7/08;C07F7/10;(IPC1-7):C07D205/08 主分类号 C07D205/08
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