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    • 4. 发明申请
    • 2-ACYLAMINOTHIAZOLE COMPOUND CRYSTALS
    • 2-氨基苯并噻唑化合物
    • WO2013018362A1
    • 2013-02-07
    • PCT/JP2012/004885
    • 2012-08-01
    • ASTELLAS PHARMA INC.SUGASAWA, KeizoMIYAFUJI, AkioSUZUKI, KenichiAWAMURA, Yuji
    • SUGASAWA, KeizoMIYAFUJI, AkioSUZUKI, KenichiAWAMURA, Yuji
    • C07D417/14A61K31/496A61P7/04
    • C07D417/14
    • The purpose of the present invention is to provide crystals of 1-(3-chloro-5-{[4-(4-chlorothiophen-2-yl)-5-(4-cyclohexyl piperazin-1-yl) thiazol-2-yl] carbamoyl} pyridin-2-yl) piperidine-4-carboxylic acid maleic acid salt that can ensure constant quality and constant effects as a drug substance for medicines, and that can be stably supplied in mass production such as industrial production. The present invention relates to crystals of 1-(3-chloro-5-{[4-(4-chlorothiophen-2-yl)-5-(4-cyclohexyl piperazin-1-yl) thiazol-2-yl] carbamoyl} pyridin-2-yl) piperidine-4-carboxylic acid maleic acid salt with endothermic peak top temperatures in differential scanning calorimeter analysis of between approximately 229 and 232 degree C, and between approximately 300 and 303 degree C. The crystals of the present invention are with excellent oral absorption, can be stably supplied in mass production such as industrial production or the like, and can be used as an active ingredient in a pharmaceutical composition for preventing and/or treating various types of thrombocytopenia.
    • 本发明的目的是提供1-(3-氯-5 - {[4-(4-氯噻吩-2-基)-5-(4-环己基哌嗪-1-基)噻唑-2-基] 吡啶-2-基)哌啶-4-甲酸马来酸盐,其能够确保作为药物的药物的质量和恒定的效果,并且可以在大规模生产例如工业生产中稳定供应。 本发明涉及1-(3-氯-5 - {[4-(4-氯噻吩-2-基)-5-(4-环己基哌嗪-1-基)噻唑-2-基]氨基甲酰基} 吡啶-2-基)哌啶-4-甲酸马来酸盐,差示扫描量热分析仪的吸热峰顶温度在229和232摄氏度之间,在约300和303摄氏度之间。本发明的晶体是 具有优异的口服吸收性,可以在工业化生产等的批量生产中稳定供给,可以作为预防和/或治疗各种血小板减少症的药物组合物中的活性成分使用。