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    2-aza substituted-1-carbadethiapen-2-em-3-carboxylic acids
    6.
    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。

    2-aza-substituted 1-carbadethiapen-2-em-3 carboxylic acids
    7.
    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。

    13-Halo and 13-deoxy C-076 compounds
    8.
    发明授权
    13-Halo and 13-deoxy C-076 compounds 失效
    13-Halo和13-deoxy C-076化合物

    公开(公告)号：US4171314A

    公开(公告)日：1979-10-16

    申请号：US861810

    申请日：1977-12-19

    申请人： John C. Chabala ,  Michael H. Fisher ,  Helmut H. Mrozik

    发明人： John C. Chabala ,  Michael H. Fisher ,  Helmut H. Mrozik

    IPC分类号： A01N43/22 ,  C07D493/22 ,  C07F7/18 ,  C07H17/08 ,  C12P19/62

    CPC分类号： C07D493/22 ,  A01N43/22 ,  C07F7/1856 ,  C07H17/08 ,  C12P19/623 ,  C12R1/465

    摘要： Derivatives of the C-076 compounds are disclosed wherein the 13-position is unsubstituted or substituted by a halogen atom. The compounds are prepared by removing the glycosyl groups on the 13-position of the C-076 compounds isolated from the fermentation broth of Streptomyces avermitilis. This is followed by substitution of the 13-hydroxy group with a halogen, and subsequent removal of the halogen. The disclosed compounds are antiparasitic, anthelmintic, insecticidal and acaracidal agents.

    摘要翻译： 公开了C-076化合物的衍生物，其中13位未被取代或被卤素原子取代。 通过除去分离自阿维链霉菌发酵液的C-076化合物的13位上的糖基来制备化合物。 然后用卤素取代13-羟基，随后除去卤素。 所公开的化合物是抗寄生虫，驱虫虫，杀虫剂和杀螨剂。