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    • 4. 发明授权
    • 2-(substituted pyrrolidinylthio)carbapenem derivatives
    • 2-(取代的吡咯烷硫基)碳青霉烯衍生物
    • US5374720A
    • 1994-12-20
    • US780142
    • 1991-10-21
    • Susumu NakagawaNorikazu OhtakeFumio NakanoKoji YamadaRyosuke UshijimaSatoshi MuraseHiroshi Fukatsu
    • Susumu NakagawaNorikazu OhtakeFumio NakanoKoji YamadaRyosuke UshijimaSatoshi MuraseHiroshi Fukatsu
    • C07D477/20C07D487/04A61K31/40
    • C07D477/20
    • A compound of the formula: ##STR1## wherein R is a hydrogen atom or a methyl group, R.sup.1 is a hydrogen atom or a negative charge, each of R.sup.2 and R.sup.3 which may be the same or different, is a hydrogen atom, a lower alkyl group, a hydroxy lower alkyl group, a formimidoyl group, an acetoimidoyl group, --COOR.sup.4, --CON(R.sup.5)R.sup.6, --N(R.sup.5)R.sup.6, --CH.sub.2 COOR.sup.4, --CH.sub.2 N(R.sup.5)R.sup.6 or --CH.sub.2 CON(R.sup.5)R.sup.6 (wherein R.sup.4 is a hydrogen atom or a lower alkyl group, each of R.sup.5 and R.sup.6 which may be the same or different, is a hydrogen atom or a lower alkyl group, or R.sup.5 and R.sup.6 form together with the adjacent nitrogen atom a heterocyclic group selected from the group consisting of an aziridinyl group, an azetidinyl group, a pyrrolidinyl group and a piperidyl group), A is .dbd.NR.sup.7, .dbd.N.sup.+ (R.sup.7)R.sup.8, wherein each of R.sup.7 and R.sup.8 which may be the same or different, is a hydrogen atom, a lower alkyl group, a hydroxy lower alkyl group, a formimidoyl group, an acetoimidoyl group, --COOR.sup.4, --CON(R.sup.5)R.sup.6, --N(R.sup.5)R.sup.6, --CH.sub.2 COOR.sup.4, --CH.sub.2 N(R.sup.5)R.sup.6 or --CH.sub.2 CON(R.sup.5)R.sup.6 (wherein R.sup.4, R.sup.5 and R.sup.6 are as defined above), p is an integer of from 0 to 3, and q is an integer of from 1 to 3; or a pharmaceutically acceptable salt or ester thereof.
    • 下式的化合物:其中R是氢原子或甲基,R 1是氢原子或负电荷,R 2和R 3可以相同或不同,为氢原子 ,低级烷基,羟基低级烷基,亚氨基,亚氨酰基,-COOR4,-CON(R5)R6,-N(R5)R6,-CH2COOR4,-CH2N(R5)R6或-CH2CON( R5)R6(其中R4是氢原子或低级烷基,R5和R6各自可以相同或不同,是氢原子或低级烷基,或R5和R6与相邻的氮原子一起形成) 选自氮丙啶基,氮杂环丁烷基,吡咯烷基和哌啶基的杂环基),A为= NR 7 = N +(R 7)R 8,其中R 7和R 8可以相同或不同, 不同的是氢原子,低级烷基,羟基低级烷基,亚氨基,亚氨代乙酰基,-COOR4,-CON(R5)R6,-N(R5)R6,-CH2COOR4,-CH2N(R5 )R6或-CH2CON(R5)R6(其中 在R4中,R5和R6如上所定义),p是0-3的整数,q是1至3的整数; 或其药学上可接受的盐或酯。