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    2-aza-substituted 1-carbadethiapen-2-em-3-carboxylic acids
    24.
    发明授权
    2-aza-substituted 1-carbadethiapen-2-em-3-carboxylic acids 失效
    2-氮杂取代的1-碳代萘二烯-2-烯-3-羧酸

    公开(公告)号：US5140030A

    公开(公告)日：1992-08-18

    申请号：US569257

    申请日：1990-08-16

    申请人： Burton G. Christensen ,  Ronald W. Ratcliffe ,  John C. Chabala

    发明人： Burton G. Christensen ,  Ronald W. Ratcliffe ,  John C. Chabala

    IPC分类号： C07D477/22 ,  C07F9/6561

    CPC分类号： C07F9/65611 ,  C07D477/22 ,  Y02P20/55

    摘要： Disclosed are 2-aza-substituted 1-carbadethiapen-2-em-3-carboxylic acids. I, where the generic 2-aza group includes azido, acylamino, amino, alkylamino, dialkylamino, triazolyl, triazolinyl, aziridinyl, and their pharmaceutically acceptable salt, ester, anhydride and amide derivatives which are useful as antibiotics. Also disclosed are processes for the preparation of I from the known, appropriately substituted bicyclic keto ester II via the 2-azido central intermediate III: ##STR1## wherein R.sup.16 is H or CH.sub.3, preferably beta-methyl; R.sup.6, and R.sup.7 are independently hydrogen, linear, branched or cyclic C.sub.1 -C.sub.5 alkyl, which can be substituted with fluoro, hydroxy, protected hydroxy, sulfoxy, amino, protected amino, wherein R.sup.6 and R.sup.7 taken together can also be C.sub.2 -C.sub.4 alkylidene, similarly substituted; with the proviso that both R.sup.6 and R.sup.7 are not unsubstituted alkyl, R.sup.1 and R.sup.2 are, inter alia, hydrogen, alkyl, acyl, and can be joined to form a ring comprising 3 to 7 atoms; R.sup.a is hydrogen, a salt cation, a removable protecting group, or a pharmaceutically acceptable ester moiety.Also disclosed are processes for the preparation of such compounds; pharmaceutical compositions comprising such compounds; and methods of treatment comprising administering such compounds and compositions when an antibiotic effect is indicated.

    摘要翻译： 披露的是2-氮杂取代的1-碳代萘二烯-2-烯-3-羧酸。 I，其中通用2-氮杂基团包括可用作抗生素的叠氮基，酰氨基，氨基，烷基氨基，二烷基氨基，三唑基，三唑啉基，氮丙啶基及其药学上可接受的盐，酯，酸酐和酰胺衍生物。 还公开了通过2-叠氮中心中间体III从已知的适当取代的双环酮酯II制备I的方法：其中R 16是H或CH 3，优选β- 甲基; R 6和R 7独立地是氢，直链，支链或环状的C 1 -C 5烷基，其可以被氟，羟基，保护的羟基，亚磺氧基，氨基，保护的氨基取代，其中R 6和R 7一起也可以是C 2 -C 4亚烷基， 同样取代; 条件是R6和R7都不是未取代的烷基，R1和R2特别是氢，烷基，酰基，并且可以连接形成包含3至7个原子的环; Ra是氢，盐阳离子，可除去的保护基或药学上可接受的酯部分。 还公开了制备这些化合物的方法; 包含这些化合物的药物组合物; 和治疗方法，包括当指出抗生素效应时施用这些化合物和组合物。

    2-aza-substituted 1-carbadethiapen-2-em-3-carboxylic acids
    26.
    发明授权
    2-aza-substituted 1-carbadethiapen-2-em-3-carboxylic acids 失效
    2-氮杂取代的1-碳代萘二烯-2-烯-3-羧酸

    公开(公告)号：US4783453A

    公开(公告)日：1988-11-08

    申请号：US97348

    申请日：1987-09-08

    申请人： Burton G. Christensen ,  Ronald W. Ratcliffe ,  John C. Chabala

    发明人： Burton G. Christensen ,  Ronald W. Ratcliffe ,  John C. Chabala

    IPC分类号： C07D477/22 ,  C07F9/6561 ,  C07D487/04 ,  A61K31/40

    CPC分类号： C07D477/22 ,  C07F9/65611 ,  Y02P20/55

    摘要： Disclosed are 2-aza-substituted 1-carbadethiapen-2-em-3-carboxylic acids I, where the generic 2-aza group includes azido, acylamino, amino, alkylamino, dialkylamino, triazolyl, triazolinyl, aziridinyl, and their pharmaceutically acceptable salt, ester, anhydride and amide derivatives which are useful as antibiotics. Also disclosed are processes for the preparation of I from the known, appropriately substituted bicyclic keto ester II via the 2-azido central intermediate III: ##STR1## wherein R.sup.16 is H or CH.sub.3, preferably beta-methyl; R.sup.6, and R.sup.7 are independently hydrogen, linear, branched or cyclic C.sub.1 -C.sub.5 alkyl, which can be substituted with fluoro, hydroxy, protected hydroxy, sulfoxy, amino, protected amino, wherein R.sup.6 and R.sup.7 taken together can also be C.sub.2 -C.sub.4 alkylidene, similarly substituted; with the proviso that both R.sup.6 and R.sup.7 are not unsubstituted alkyl, R.sup.1 and R.sup.2 are, inter alia, hydrogen, alkyl, acyl, and can be joined to form a ring comprising 3 to 7 atoms; R.sup.a is hydrogen, a salt cation, a removable protecting group, or a pharmaceutically acceptable ester moiety.Also disclosed are processes for the preparation of such compounds; pharmaceutical compositions comprising such compounds; and methods of treatment comprising administering such compounds and compositions when an antibiotic effect is indicated.

    摘要翻译： 披露的是2-氮杂取代的1-碳代萘二甲酸-2-烯-3-羧酸I，其中通用的2-氮杂基团包括叠氮基，酰氨基，氨基，烷基氨基，二烷基氨基，三唑基，三唑基，氮丙啶基及其药学上可接受的盐 ，可用作抗生素的酯，酸酐和酰胺衍生物。 还公开了通过2-叠氮中心中间体III从已知的适当取代的双环酮酯II制备I的方法：其中R 16是H或CH 3，优选β- 甲基; R 6和R 7独立地是氢，直链，支链或环状的C 1 -C 5烷基，其可以被氟，羟基，保护的羟基，亚磺氧基，氨基，保护的氨基取代，其中R 6和R 7一起也可以是C 2 -C 4亚烷基， 同样取代; 条件是R6和R7都不是未取代的烷基，R1和R2特别是氢，烷基，酰基，并且可以连接形成包含3至7个原子的环; Ra是氢，盐阳离子，可除去的保护基或药学上可接受的酯部分。 还公开了制备这些化合物的方法; 包含这些化合物的药物组合物; 和治疗方法，包括当指出抗生素效应时施用这些化合物和组合物。