6,11-bridged erythromycin derivatives
    2.
    发明授权
    6,11-bridged erythromycin derivatives 有权
    6,11桥梁红霉素衍生物

    公开(公告)号:US6046171A

    公开(公告)日:2000-04-04

    申请号:US158459

    申请日:1998-09-22

    IPC分类号: C07H17/08 A61K31/70 C07H1/00

    CPC分类号: C07H17/08

    摘要: Novel 6,11-bridged erythromycin compounds and pharmaceutically acceptable salts and esters thereof having antibacterial activity having a formula ##STR1## compositions comprising a therapeutically effective amount of a compound of the invention in combination with a pharmaceutically acceptable carrier, a method for treating bacterial infections by administering to a mammal a pharmaceutical composition containing a therapeutically-effective amount of a compound of the invention, and processes for their preparation.

    摘要翻译: 具有抗细菌活性的新型6,11-桥接的红霉素化合物及其药学上可接受的盐和酯,其组成包括治疗有效量的本发明化合物与药学上可接受的载体的组合,通过给予 哺乳动物含有治疗有效量的本发明化合物的药物组合物及其制备方法。

    Process for preparation of chiral 3-amino-pyrrolidine and analogous
bicyclic compounds
    4.
    发明授权
    Process for preparation of chiral 3-amino-pyrrolidine and analogous bicyclic compounds 失效
    手性3-氨基 - 吡咯烷和类似双环化合物的制备方法

    公开(公告)号:US5703244A

    公开(公告)日:1997-12-30

    申请号:US754641

    申请日:1996-11-21

    摘要: A process for the preparation of chiral 3-aminopyrrolidine and analogous bicyclic derivatives from dihydroxy olefins by treatment with titanium isopropoxide, an optically active tartrate ester and tert-butyl hydroperoxide, followed by subsequent alkylation of the intermediate with an alkyl or alkenyl magnesium halide, then pyrrolidine ring formation by condensation with an arylmethylamine, subsequent chiral replacement of a ring hydroxyl group with an amino group with further protection thereof, optional additional substitution closing of the second ring, and hydrogenolysis to remove a ring-nitrogen protecting group.

    摘要翻译: 通过用异丙醇钛,光学活性酒石酸酯和叔丁基过氧化氢处理二羟基烯烃手性3-氨基吡咯烷和类似双环衍生物的方法,然后用烷基或链烯基卤化镁随后烷基化中间体,然后 通过与芳基甲胺缩合形成吡咯烷环,随后进一步保护具有氨基的环羟基的手性取代,任选的第二环的另外的取代封闭,以及氢解除去环 - 氮保护基。

    Method of producing quinoline-3-carboxylic acids
    7.
    发明授权
    Method of producing quinoline-3-carboxylic acids 失效
    喹啉-3-羧酸的制备方法

    公开(公告)号:US5262559A

    公开(公告)日:1993-11-16

    申请号:US642615

    申请日:1991-01-17

    申请人: Daniel T. Chu

    发明人: Daniel T. Chu

    摘要: A process for producing a 1,4-dihydro-4-oxo-quinoline-3-carboxylic acid by reacting an acctophenone with a dialkoxycarbonate to obtain the corresponding .beta.-ketoester, treating the .beta.-ketoester with a trialkylorthoformate in the presence of an acid anhydride followed by treatment with a substituted or unsubstituted amine to obtain the corresponding enaminoketoester, and then reacting the enaminoketoester with a strong base to obtain the corresponding quinoline-3-carboxylic acid ester. The acid ester may then be hydrolyzed, if desired, to obtain the quinoline-3-carboxylic acid. Also disclosed herein are compounds useful as intermediates useful in the production of quinoline-3-carboxylic acid.

    摘要翻译: 通过使acctophenone与二烷氧基碳酸酯反应制得1,4-二氢-4-氧代喹啉-3-羧酸的方法,得到相应的β-酮酯,在酸存在下用三烷基原甲酸酯处理β-酮酯 酐,然后用取代或未取代的胺处理,得到相应的烯胺酮酯,然后使烯胺酮与强碱反应,得到相应的喹啉-3-羧酸酯。 如果需要,可以将酸酯水解,得到喹啉-3-羧酸。 本文还公开了可用作生产喹啉-3-羧酸的中间体的化合物。

    Process for preparation of racemate and optically active ofloxacin and
related derivatives
    9.
    发明授权
    Process for preparation of racemate and optically active ofloxacin and related derivatives 失效
    外消旋物和光学活性氧氟沙星及相关衍生物的制备方法

    公开(公告)号:US4777253A

    公开(公告)日:1988-10-11

    申请号:US858532

    申请日:1986-04-25

    IPC分类号: C07D498/06

    CPC分类号: C07D498/06

    摘要: A process for producing racemic or optically active compounds of the formula: ##STR1## wherein R.sub.1 is hydrogen, C.sub.1 to C.sub.6 alkyl or benzyl; and Z is amino or substituted amino.Also disclosed are intermediates useful in the process and methods for producing the intermediates.

    摘要翻译: 制备下式的外消旋或光学活性化合物的方法:其中R1是氢,C1-C6烷基或苄基; Z是氨基或取代的氨基。 还公开了可用于制备中间体的方法和方法的中间体。

    3-'N-modified 6-O-substituted erythromycin ketolide derivatives having
antibacterial activity
    10.
    发明授权
    3-'N-modified 6-O-substituted erythromycin ketolide derivatives having antibacterial activity 有权
    具有抗菌活性的3-N改性的6-O-取代的红霉素酮内酯衍生物

    公开(公告)号:US06034069A

    公开(公告)日:2000-03-07

    申请号:US132256

    申请日:1998-08-11

    IPC分类号: C07H17/08 A61K31/70 C07H1/00

    CPC分类号: C07H17/08

    摘要: Novel 3'-N-modified 6-O-substituted erythromycin ketolide compounds and pharmaceutically acceptable salts and esters thereof having antibacterial activity having a formula ##STR1## compositions comprising a therapeutically effective amount of a compound of the invention in combination with a pharmaceutically acceptable carrier, as well as a method for treating bacterial infections by administering to a mammal a pharmaceutical composition containing a therapeutically-effective amount of a compound of the invention.

    摘要翻译: 具有抗细菌活性的新颖的3'-N-修饰的6-O-取代的红霉素酮内酯化合物及其药学上可接受的盐和酯,其具有包含治疗有效量的本发明化合物与药学上可接受的载体的组成的式 作为通过向哺乳动物施用含有治疗有效量的本发明化合物的药物组合物来治疗细菌感染的方法。