Abrégé

Anti-infective quinolone compound, preparation method thereof and use thereof. The present invention disclosed the pharmaceutically acceptable salt of 6-fluoro-1-methyl-4-oxo-7- (1- piperazinyl) - 4H -[1,3]thiazeto[3,2-a]quinoline-3-carboxylic acid (I) , which is separated out by solvent crystallization following the reaction of compound (I) with pharmaceutically acceptable acids X using water or water containing organic solvent as solvents. The obtained compound has a definitive structure. It is stable and has confirmed anti-bacterial effect. The water solubility of compound (I) has been improved by this way, and it is convenient to make appropriate dosage forms for clinic use to expand the extension of clinic use. By preparing the pharmaceutically acceptable salt of compound (I), the toxicity of the active compound (I) has been reduced and the safety of its clinic use has been improved.

Classes IPC  ?

• C07D 513/04 - Systèmes condensés en ortho
• A61K 31/47 - QuinoléinesIsoquinoléines
• A61K 31/495 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à six chaînons avec deux azote comme seuls hétéro-atomes d'un cycle, p. ex. pipérazine
• C07D 221/00 - Composés hétérocycliques contenant des cycles à six chaînons ne comportant qu'un atome d'azote comme unique hétéro-atome du cycle, non prévus par les groupes
• C07D 285/00 - Composés hétérocycliques contenant des cycles comportant des atomes d'azote et de soufre comme uniques hétéro-atomes du cycle, non prévus par les groupes

Abrégé

Anti-infective compound, preparation method thereof and use thereof. The present invention disclosed a crystal of 6-fluoro-1-methyl-4-oxo-7-(1-piperazinyl)-4H-[1,3]thiazeto[3,2-a]quinoline-3-carboxylic acid (II) methanesulfonate, which is separated out by solvent crystallization following the reaction of compound (II) with pharmaceutical methanesulfonic acid using water or water containing organic solvent as solvents. The obtained compound has a definitive structure. It is stable and has confirmed anti-bacterial effect. The water solubility of compound (II) has been improved by this way, and it is convenient to make appropriate dosage forms for clinic use to expand the extension of clinic use. By preparing the methanesulfonate of compound (II), the toxicity of the active compound (II) has been reduced and the safety of its clinic use has been improved.

Classes IPC  ?

• C07D 513/04 - Systèmes condensés en ortho
• A61K 31/47 - QuinoléinesIsoquinoléines
• A61K 31/495 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à six chaînons avec deux azote comme seuls hétéro-atomes d'un cycle, p. ex. pipérazine
• C07D 221/00 - Composés hétérocycliques contenant des cycles à six chaînons ne comportant qu'un atome d'azote comme unique hétéro-atome du cycle, non prévus par les groupes
• C07D 285/00 - Composés hétérocycliques contenant des cycles comportant des atomes d'azote et de soufre comme uniques hétéro-atomes du cycle, non prévus par les groupes