公开(公告)号：US07538221B2

公开(公告)日：2009-05-26

申请号：US10578371

申请日：2004-11-10

申请人： Prasad Keshav Deshpande ,  Satish Baliram Bhavsar ,  Yati Chugh ,  Ravindra Dattatrya Yeole ,  Noel John De Souza ,  Mahesh Vithalbhai Patel

发明人： Prasad Keshav Deshpande ,  Satish Baliram Bhavsar ,  Yati Chugh ,  Ravindra Dattatrya Yeole ,  Noel John De Souza ,  Mahesh Vithalbhai Patel

IPC分类号： C07D215/38 ,  A61K31/44

CPC分类号： C07D401/04

摘要： A polymorphic forms of the hydrochloride salt and mesylate salt of racemic (±)-1-cyclopropyl-6-fluoro-8-methoxy-7-(4-amino-3,3-dimethylpiperidin-1-yl)-1,4-dihydro-4-oxo-quinoline-3-carboxylic acid, dextrorotatory R-(+)-1-cyclopropyl-6-fluoro-8-methoxy-7-(4-amino-3,3-dimethylpiperidin-1-yl)-1,4-dihydro-4-oxo-quinoline-3-carboxylic acid and S-(−)-1-cyclopropyl-6-fluoro-8-methoxy-7-(4-amino-3,3-dimethylpiperidin-1-yl)-1,4-dihydro-4-oxo-quinoline-3-carboxylic acid having formula (I) and (II) respectively are described. Processes for their preparation are also described. The invention further relates to methods of using, and pharmaceutical compositions comprising the compounds of the invention for treatment of bacterial infections in mammals.

摘要翻译： 外消旋（±）-1-环丙基-6-氟-8-甲氧基-7-（4-氨基-3,3-二甲基哌啶-1-基）-1,4-苯并二氢吡喃的盐酸盐和甲磺酸盐的多晶形式， -2,3-二氢-4-氧代 - 喹啉-3-羧酸，右旋R - （+）-1-环丙基-6-氟-8-甲氧基-7-（4-氨基-3,3-二甲基哌啶-1-基） - 1,4-二氢-4-氧代 - 喹啉-3-羧酸和S - （ - ） - 1-环丙基-6-氟-8-甲氧基-7-（4-氨基-3,3-二甲基哌啶-1-基） （I）和（II）的1,4-二氢-4-氧代 - 喹啉-3-羧酸。 还描述了其制备方法。 本发明还涉及包含本发明化合物用于治疗哺乳动物细菌感染的药物组合物的方法和药物组合物。