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IMIDAZOLE CARBONYL COMPOUNDS
专利权人:
发明人:
SONEDA, TSUYOSHI,曾根田刚,曾根田剛,TAKESHITA, HIROSHI,竹下裕,竹下裕,KAGOSHIMA, YOSHIKO,神子岛佳子,神子島佳子,YAMAMOTO, YUKO,山本裕子,山本裕子,HOSOKAWA, TAKAFUMI,细川贵史,細川貴史,KONOSU, TOSHIYUKI,鸿巢俊之,鴻巢俊之,MASUDA, NOBUHISA,增田修久,增田修久,UCHIDA
申请号:
TW097150632
公开号:
TWI498115B
申请日:
2008.12.25
申请国别(地区):
TW
年份:
2015
代理人:
摘要:
In order to create the antibiotic with the new active machenism, the present inventors searched for the compound having the physical properties with high water solubility and weak cell toxicity, that have the action inhibiting both the GyrB subunit of DNA Gyrase and the ParE subunit of topoisomerase IV, and have sufficient anti-bacterium activity. Finally, the compound of general formula (1) of this invention, the pharmaceutically acceptable salt, or the prodrug thereof with the preferable character was found, and the present invention was completed. The present invention provides a pharmaceutical composition (especially, the composition for prevention or the treatment of the infectious disease disease) that contains the compound of general formula (1), the pharmaceutically acceptable salt, or the prodrug thereof as an active ingredient, a use of the compound of general formula (1), the pharmaceutically acceptable salt, or the prodrug thereof for preparing the pharmaceutical composition (especially, the composition for prevention or the treatment of the infectious disease disease), and a preventing or treating method of the disease (especially, infectious disease disease) that administers a pharmaceutical effective amount of the compound of general formula (1), the pharmaceutically acceptable salt, or the prodrug thereof to the warm-blooded animal (especially, human).A compound of the following general formula (1) :the pharmaceutically acceptable salt, or the hydrate thereof, and a medicine that contains those compound as active ingredient.發明者等為創製具有新穎作用機制之抗生素,探索細胞毒性弱,而具有對水之溶解度大之物性,和抑制DNA促旋酶(DNA gyrase)之GyrB子單元(Subunit)及拓樸異構酶(topoisomerase)IV之ParE子單元之兩方之作用,且具有充分抗菌活性之化合物之結果,發現本發明之式(1)化合物、其藥理容許鹽、及其前藥具有所望性質,終於完成本發明。本發明提供式(1)化合物、其藥理容許鹽、及以其前藥為有效成分含有之醫藥組成物(尤其預防或治療感染症疾病之組成物)、製造醫藥組成物(尤其預防或治療感染症疾病之組成物)之式(1)化合物、其藥理容許鹽、及其前藥之使用,將式(1)化合物、其藥理容許鹽、及其前藥之藥理有效量投與溫血動物(尤其人)之疾病(尤其感染症疾病)之預防或治療方法。如下式(I)化合物、其藥理容許鹽、或彼等之水合物:、及以該化合物為有效成分含有之醫藥。
来源网站:
中国工程科技知识中心
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