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    7-substituted-amino-3-substituted-3-cephem-4-carboxylic acids
    31.
    发明授权
    7-substituted-amino-3-substituted-3-cephem-4-carboxylic acids 失效
    7-取代 - 氨基-3-取代-3-头孢烯-4-羧酸

    公开(公告)号：US5525599A

    公开(公告)日：1996-06-11

    申请号：US95383

    申请日：1993-07-21

    申请人： Ho-Shen Lin

    发明人： Ho-Shen Lin

    IPC分类号： C07D463/00 ,  C07D501/00 ,  C07D501/20 ,  C07D501/34 ,  C07D501/59 ,  C07D505/00 ,  C07D498/04 ,  A61K31/535

    CPC分类号： C07D505/00 ,  C07D463/18 ,  C07D501/00 ,  Y02P20/55

    摘要： The invention provides compounds of the formula ##STR1## wherein X is CH.sub.2, S or O; R.sub.1 is a 3 position substituent such as hydrogen, hydroxy, halo, trifluoromethyl, C.sub.2 F.sub.5, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 substituted alkyl, C.sub.1 -C.sub.6 alkenyl, C.sub.1 -C.sub.6 alkynyl, CH.sub.2 O(CO)R', CH.sub.2 O(CO)NH.sub.2, CO.sub.2 R', thio(C.sub.1 -C.sub.6)alkyl, thio(C.sub.1 C.sub.6)alkenyl, oxo(C.sub.1 -C.sub.6)alkyl, phosphine oxide, quaternary ammonium group, substituted or unsubstituted thiazolothio, or oxo(C.sub.1 -C.sub.6)alkenyl;wherein R' is hydrogen, C.sub.1 -C.sub.6 alkyl, or C.sub.1 -C.sub.6 alkenyl;R.sub.2 is hydrogen or a carboxy protecting group;R.sub.3 is ##STR2## (CH.sub.2).sub.n ; wherein R.sub.6 is hydrogen Me, CH.sub.2 F, CF.sub.3, C.sub.2 H.sub.5, CH.sub.2 CH.sub.2 F, CH.sub.2 CF.sub.3, C.sub.2 F.sub.5, CH.sub.2 CO.sub.2 R', CH.sub.2 CONH.sub.2, C(Me).sub.2 CO.sub.2 R', or C(Me).sub.2 CONH.sub.2 ; and n is 0-5;R.sub.4 is ##STR3## wherein Z is O, S, NH, or CH.sub.2 ; Y is CH or N; and R.sub.7 is hydrogen, C.sub.1 -C.sub.6 alkyl, CONH.sub.2, or CO.sub.2 R'; andR.sub.5 is ##STR4## wherein R.sub.8 is CH, N, COH, CO(C.sub.1 -C.sub.6 alkyl) CSH, or CNH.sub.2 ; and R.sub.9 is R.sub.8 as defined; said R.sub.5 optionally substituted 1-4 times with halo, OH, SH, NH.sub.2, NO.sub.2, CH.sub.3, C.sub.2 H.sub.5, CO.sub.2 R', CONH.sub.2, SO.sub.3 H, or SO.sub.2 NHR'; and salts thereof. Also, pharmaceutical formulations and methods for treating bacterial infections in man or other animals using the above compounds are disclosed.

    摘要翻译： 本发明提供式（I）的化合物，其中X是CH 2，S或O; R1是3位取代基，例如氢，羟基，卤素，三氟甲基，C2F5，C1-C6烷基，C1-C6取代的烷基，C1-C6烯基，C1-C6炔基，CH2O（CO）R'，CH2O（CO） NH 2，CO 2 R'，硫代（C 1 -C 6）烷基，硫代（C 1 -C 6）烯基，氧代（C 1 -C 6）烷基，氧化膦，季铵基，取代或未取代的噻唑硫基或氧代（C 1 -C 6） 其中R'是氢，C 1 -C 6烷基或C 1 -C 6烯基; R2是氢或羧基保护基; （CH2）n; 其中R 6是氢，CH 2 F，CF 3，C 2 H 5，CH 2 CH 2 F，CH 2 CF 3，C 2 F 5，CH 2 CO 2 R'，CH 2 CONH 2，C（Me）2 CO 2 R'或C（Me） n为0-5; R4是，其中Z是O，S，NH或CH2; Y是CH或N; 并且R 7是氢，C 1 -C 6烷基，CONH 2或CO 2 R'; 其中R 8是CH，N，COH，CO（C 1 -C 6烷基）CSH或CNH 2; 并且R 9是如所定义的R8; 所述R5任选被卤素，OH，SH，NH 2，NO 2，CH 3，C 2 H 5，CO 2 R'，CONH 2，SO 3 H或SO 2 NHR'取代1-4次; 及其盐。 此外，公开了使用上述化合物治疗人或其他动物中的细菌感染的药物制剂和方法。