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72 条记录 (耗时 0.032 秒)

    Process for preparing 3-substituted-6-substituted-7-oxo-1-azabicyclo[3.2.0]hept-2-ene-2-carbox ylic acid
    31.
    发明授权
    Process for preparing 3-substituted-6-substituted-7-oxo-1-azabicyclo[3.2.0]hept-2-ene-2-carbox ylic acid 失效
    制备3-取代-6-取代-7-氧代-1-氮杂双环[3.2.0]庚-2-烯-2-羧酸的方法

    公开(公告)号：US4745188A

    公开(公告)日：1988-05-17

    申请号：US759721

    申请日：1985-07-29

    申请人： Burton G. Christensen ,  Ronald W. Ratcliffe

    发明人： Burton G. Christensen ,  Ronald W. Ratcliffe

    IPC分类号： C07D477/02 ,  C07D487/04 ,  A61K31/40

    CPC分类号： C07D477/02

    摘要： Disclosed is a process for preparing 3- and 6-substituted-7-oxo-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acids: ##STR1## wherein: X is a leaving group such as chloro, bromo, tosyl, mesyl or the like; and R.sup.6, R.sup.7 and R.sup.8 are, inter alia, independently selected from the group consisting of hydrogen, alkyl, alkenyl, aryl and aralkyl. Such compounds (I), as well as their pharmaceutically acceptable salt, ester and amide derivatives, are useful as antibiotics.

    摘要翻译： 公开了制备3-和6-取代-7-氧代-1-氮杂双环[3.2.0]庚-2-烯-2-羧酸的方法：其中：X是离开 例如氯，溴，甲苯磺酰，甲磺酰等; R 6，R 7和R 8特别独立地选自氢，烷基，烯基，芳基和芳烷基。 这些化合物（I）及其药学上可接受的盐，酯和酰胺衍生物可用作抗生素。

    2-aza substituted-1-carbadethiapen-2-em-3-carboxylic acids
    37.
    发明授权
    2-aza substituted-1-carbadethiapen-2-em-3-carboxylic acids 失效
    2-氮杂的取代的-1-碳代萘二烯-2-烯-3-羧酸

    公开(公告)号：US4892869A

    公开(公告)日：1990-01-09

    申请号：US300738

    申请日：1989-01-19

    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 1 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1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。

    Process for preparing 3-substituted-6-substituted-7-oxo-1-azabicycl(3.2.0)-hept-2-ene-2-carbox ylic acid
    38.
    发明授权
    Process for preparing 3-substituted-6-substituted-7-oxo-1-azabicycl(3.2.0)-hept-2-ene-2-carbox ylic acid 失效
    制备3-取代-6-取代-7-氧代-1-氮杂双环（3.2.0） - 庚-2-烯-2-羧酸的方法

    公开(公告)号：US4820817A

    公开(公告)日：1989-04-11

    申请号：US787018

    申请日：1985-10-15

    申请人： Burton G. Christensen ,  Ronald W. Ratcliffe

    发明人： Burton G. Christensen ,  Ronald W. Ratcliffe

    IPC分类号： C07D477/02 ,  A61K31/40

    CPC分类号： C07D477/02

    摘要： Disclosed is a process for preparing 3-substituted-thio-6-(1'-hydroxyethyl)-7-oxo-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acids (I) ##STR1## wherein X is a leaving group such as chloro, bromo, tosyl, mesyl or the like; and R.sup.8 is, inter alia, selected from the group consisting of hydrogen, alkyl, alkenyl, aryl and aralkyl. The compounds I as well as their pharmaceutically acceptable O- and carboxyl derivatives are useful as antibiotics.

    摘要翻译： 公开了制备3-取代的硫代-6-（1'-羟乙基）-7-氧代-1-氮杂双环[3.2.0]庚-2-烯-2-羧酸（I）的方法， 其中X是离去基团如氯，溴，甲苯磺酰基，甲磺酰等; R8尤其选自氢，烷基，烯基，芳基和芳烷基。 化合物I及其药学上可接受的O-和羧基衍生物可用作抗生素。

    2-aza-substituted 1-carbadethiapen-2-em-3 carboxylic acids
    39.
    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-基-3-羧酸

    公开(公告)号：US4782051A

    公开(公告)日：1988-11-01

    申请号：US87978

    申请日：1987-08-17

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

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

    IPC分类号： C07D477/22 ,  C07D487/04 ,  A61K31/495

    CPC分类号： 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, trizolyl, 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： 公开了2-氮杂取代的1-碳代萘二甲酸-2-烯-3-羧酸I，其中通用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。