Abstract

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.

IPC Classes  ?

• C07D 513/04 - Ortho-condensed systems
• A61K 31/47 - QuinolinesIsoquinolines
• A61K 31/495 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
• C07D 221/00 - Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups
• C07D 285/00 - Heterocyclic compounds containing rings having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by groups

Abstract

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.

IPC Classes  ?

• C07D 513/04 - Ortho-condensed systems
• A61K 31/47 - QuinolinesIsoquinolines
• A61K 31/495 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
• C07D 221/00 - Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups
• C07D 285/00 - Heterocyclic compounds containing rings having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by groups