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    • 7. 发明授权
    • 2-Azetidinone 4-carboxy derivatives and a process for producing the same
    • 2-氮杂环丁酮-4-羧基衍生物及其制备方法
    • US4322345A
    • 1982-03-30
    • US142542
    • 1980-04-21
    • Tadashi HirataAkira SatoNobuhiro Nakamizo
    • Tadashi HirataAkira SatoNobuhiro Nakamizo
    • C07D205/08C07D403/06
    • C07D205/08
    • A 2-azetidinone of formula (I): ##STR1## wherein R.sub.1 represents an aralkoxy, acyloxy, sulphonyloxy or amino group any of which may be substituted, or hydrogen, hydroxy, alkoxy or azido;R.sub.2 represents an alkyl or aralkyl group either of which may be substituted, or hydrogen;R.sub.3 represents an alkyl, aryl, aralkyl, alkenyl, aralkenyl, alkynyl, aralkynyl, acyl or heterocyclic group any of groups may be substituted;andR.sub.4 represents an alkyl, alkenyl, aryl or aralkyl group any of which may be substituted;or formula (I'): ##STR2## wherein R.sub.1 ' is the same as R.sub.1 above;R.sub.2 ' represents an alkyl, aralkyl or trialkylsilyl group any of which may be substituted, or hydrogen;R.sub.3 ' is the same as R.sub.3 above;andR.sub.4 ' represents an alkyl, aralkyl or trialkylsilyl group any of which may be substituted, or hydrogen; provided that when R.sub.1 ' represents azido or optionally substituted amino, R.sub.2 ' represents hydrogen or CH.sub.2 CCl.sub.3 and R.sub.4 ' represents ##STR3## R.sub.3 ' represents other than ##STR4## or a pharmaceutically acceptable salt thereof is disclosed. The derivatives exhibit .beta.-lactamase inhibiting activity and are thus of interest as anti-bacterial agents, used alone or together with known antibiotic subtances.
    • 式(I)的2-氮杂环丁酮:其中R 1表示可以被取代的芳烷氧基,酰氧基,磺酰氧基或氨基,或氢,羟基,烷氧基或叠氮基; R2表示可以被取代的烷基或芳烷基,或氢; R 3表示烷基,芳基,芳烷基,烯基,芳烯基,炔基,芳炔基,酰基或杂环基,任何基团可以被取代; 并且R 4表示任何可以被取代的烷基,烯基,芳基或芳烷基; 或式(I'):其中R 1'与上述R 1相同; R 2'表示任何可以被取代的烷基,芳烷基或三烷基甲硅烷基,或氢; R3'与上述R3相同; 和R 4'表示任何可以被取代的烷基,芳烷基或三烷基甲硅烷基,或氢; 条件是当R 1'表示叠氮基或任选被取代的氨基时,R 2'表示氢或CH 2 ClCl 3,并且R 4'表示除了“IMAGE”以外的R 3'或其药学上可接受的盐。 衍生物表现出β-内酰胺酶抑制活性,因此作为抗菌剂是有意义的,单独使用或与已知的抗生素偶联使用。