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    • 2. 发明授权
    • Crystalline form of (3R,4R)-4-[3-(S)-hydroxy-3-(6 methoxyquinolin-4-propyl]-1-[2-2-thienylthio)ethyl] piperidine-3-carboxylic acid
    • (3R,4R)-4- [3-(S) - 羟基-3-(6-甲氧基喹啉-4-丙基)-1- [2-2-噻吩硫基)乙基]哌啶-3-甲酸的结晶形式
    • US06939970B2
    • 2005-09-06
    • US10739704
    • 2003-12-18
    • Jacques BourgetMarc Antoine PerrinBernd JanochaCarole NevesPascal BillotSylvaine Lafont
    • Jacques BourgetMarc Antoine PerrinBernd JanochaCarole NevesPascal BillotSylvaine Lafont
    • C07D409/14C07D215/12A61K31/47C07D215/18
    • C07D409/14
    • The present invention comprises monohydrated form C of (3R,4R)-4-[3-(S)-hydroxy-3-(6-methoxyquinolin-4-yl)propyl]-1-[2-(2-thienylthio)ethyl]piperidine-3-carboxylic acid, represented by the structure and as herein defined by powder X-ray diffraction, processes for preparing monohydrated form C from amorphorous (3R,4R)-4-[3-(S)-hydroxy-3-(6-methoxyquinolin-4-yl)propyl]-1-[2-(2-thienylthio)ethyl]piperidine-3-carboxylic acid or form A of (3R,4R)-4-[3-(S)-hydroxy-3-(6-methoxyquinolin-4-yl)propyl]-1-[2-(2-thienylthio)ethyl]piperidine-3-carboxylic acid, pharmaceutical compositions comprising monohydrated form C, pharmaceutical compositions comprising monohydrated form C and form A or form B of (3R,4R)-4-[3-(S)-hydroxy-3-(6-methoxyquinolin-4-yl)propyl]-1-[2-(2-thienylthio)ethyl]piperidine-3-carboxylic acid, pharmaceutical compositions comprising monohydrated form C, form A and form B, methods for treating bacterial infection with monohydrated form C, methods for treating bacterial infection with monohydrated form C and form A or form B, methods for treating bacterial infection with monohydrated form C, form A and form B, and a process for the preparation of form A from monohydrated form C.
    • 本发明包括(3R,4R)-4- [3-(S) - 羟基-3-(6-甲氧基喹啉-4-基)丙基] -1- [2-(2-噻吩硫基)乙基 (3R,4R)-4- [3-(S) - 羟基-3-(S) - 哌啶-3-羧酸,由结构表示,如本文中由粉末X射线衍射所定义) (6-甲氧基喹啉-4-基)丙基] -1- [2-(2-噻吩硫基)乙基]哌啶-3-甲酸或(3R,4R)-4- [3-(S) - 羟基 -3-(6-甲氧基喹啉-4-基)丙基] -1- [2-(2-噻吩硫基)乙基]哌啶-3-羧酸,包含一水合形式C的药物组合物,包含一水合形式C和形式A 或(3R,4R)-4- [3-(S) - 羟基-3-(6-甲氧基喹啉-4-基)丙基] -1- [2-(2-噻吩硫基)乙基]哌啶-3 - 羧酸,包含一水合形式C,形式A和形式B的药物组合物,用于一水合形式C治疗细菌感染的方法,用于治疗细菌感染的方法 一水合形式C和形式A或形式B,用于一水合形式C,形式A和形式B处理细菌感染的方法,以及从一水合形式C制备形式A的方法。