ANTI-INFECTIVE COMPOUND, PREPARATION METHOD THEREOF AND USE THEREOF

WIPO Patent Application WO/2007/082471

A1

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.

CHEN MAO (CN)
ZHU SHAOXUAN (CN)
LIU XUEBIN (CN)
ZHENG LIZHEN (CN)
XU SHUWEN (CN)
LIU DANQING (CN)

PCT/CN2007/000179

July 26, 2007

January 18, 2007

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GUANGZHOU BAIYUNSHAN PHARMACEU (CN)
GUANGZHOU PHARMACEUTICAL IND R (CN)
CHEN MAO (CN)
ZHU SHAOXUAN (CN)
LIU XUEBIN (CN)
ZHENG LIZHEN (CN)
XU SHUWEN (CN)
LIU DANQING (CN)

C07D513/04; A61K31/47; A61K31/495; C07D221/00; C07D285/00

US4843070A	1989-06-27
CN1033055A	1989-05-24

DAI S.-C. ET AL.: "Improved Synthesis of Danofloxacin Mesylate", CHINESE JOURNAL OF PHARMACEUTICALS, vol. 31, no. 3, 2000, pages 103 - 104

GUANGZHOU SCIHEAD PATENT AGENT CO., LTD. (Huihua Commercial & Trade Building No 80, XianLie Zhong Roa, Guangzhou Guangdong 0, CN)

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