首页> 外国专利> R-7-(3-AMINOMETHYL-4-METHOXYIMINO-3-METHYL-PYRROLIDIN-1-YL)-1-CYCLOPROPYL-6-FLUORO-4-OXO-1,4-DIHYDRO-1,8NAPHTHYRIDINE-3-CARBOXYLIC ACID AND L-ASPARTIC ACID SALT, PROCESS FOR THE PREPARATION THEREOF AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME FOR ANTIMICROBIAL

R-7-(3-AMINOMETHYL-4-METHOXYIMINO-3-METHYL-PYRROLIDIN-1-YL)-1-CYCLOPROPYL-6-FLUORO-4-OXO-1,4-DIHYDRO-1,8NAPHTHYRIDINE-3-CARBOXYLIC ACID AND L-ASPARTIC ACID SALT, PROCESS FOR THE PREPARATION THEREOF AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME FOR ANTIMICROBIAL

机译：R-7-（3-氨基甲基-4-甲亚氨基-3-甲基-吡咯烷-1-基）-1-环丙基-6-氟-4-氧-1-4-1,4-二氢-[1,8]萘啶-3 -羧酸和L-戊二酸盐，其制备方法和组成相同的抗微生物药物

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摘要

Disclosed herein are R-7-(3-aminomethyl-4-methoxyimino-3-methyl-pyrrolidin-1-yl)-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydro-[1,8]naphthyridine-3-carboxylic acid and L-aspartic acid salt, process for the preparation thereof and pharmaceutical composition comprising the same for antimicrobial. Because the R-7-(3-aminomethyl-4-methoxyimino-3-methyl-pyrrolidin-1-yl)-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydro-[1,8]naphthyridine-3-carboxylic acid and L-aspartic acid salt is more soluble and less toxic and has less side effects as an antimicrobial agent than hydrochloride and the other salts (D-aspartate and phosphate) conventionally used, the salt may be useful for oral and injectable administration.

机译：本文公开了R-7-（3-氨基甲基-4-甲氧基亚氨基-3-甲基-吡咯烷-1-基）-1-环丙基-6-氟-4-氧代-1,4-二氢-[1,8]萘啶-3-羧酸和L-天冬氨酸盐，其制备方法和包含它们的药物组合物用于抗菌。因为R-7-（3-氨基甲基-4-甲氧基亚氨基-3-甲基-吡咯烷基-1-基）-1-环丙基-6-氟-4-氧代-1,4-二氢-[1,8]萘啶-3-羧酸和L-天冬氨酸盐比传统上使用的盐酸盐和其他盐（D-天冬氨酸盐和磷酸盐）更易溶且毒性较小，并且作为抗菌剂的副作用较小，该盐可用于口服和注射给药。

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公开/公告号US2016362377A1

专利类型
公开/公告日2016-12-15

原文格式PDF
申请/专利权人 ARIBIO CO. LTD.;
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申请/专利号US201615247686
发明设计人 DONG RACK CHOI;JIN YANG;SUE HYE YOON;SUNG JAE PYUN;SEUNG HWAN KIM;SEUNG KYOO SEONG;JEI MAN RYU;
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申请日2016-08-25
分类号C07D215/56;C07D471/04;C07C229/24;C07D498/06;
国家 US
入库时间 2022-08-21 13:49:58

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