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    • 2. 发明专利
    • Method for producing acylaminothiazole derivative
    • 制备酰氨基噻唑衍生物的方法
    • JP2006219481A
    • 2006-08-24
    • JP2006003657
    • 2006-01-11
    • Astellas Pharma Incアステラス製薬株式会社
    • SUGASAWA KEIZOUKOGA YUJIKOHITSU KAZUYOSHIOKUDA TAKAOHARADA KOICHIROKUBOTA HIDEKIHIRAYAMA FUKUSHIABE MASAKISUZUKI KENICHI
    • C07D417/04A61K31/427A61K31/4439A61K31/4545A61P7/04C07D417/14
    • PROBLEM TO BE SOLVED: To provide a method for producing a 2-acylaminothiazole derivative or its pharmaceutically allowable salt which has thrombocytosis activity based on excellent human c-mpl-Ba/F3 cell proliferation action and megakaryocyte colony formation acceleration action and is useful for curing thrombocytopenia. SOLUTION: The method produces a 2-acylaminothiazole derivative represented by formula (I) or its pharmaceutically allowable salt. In formula (I), -R 1 is a lower alkyl group or a cycloalkyl group; -A= is -N= or -CH=; -X is a halogen; (a) when -A= is -N=, then -Y- is -NR 3 - and (b) when -A= is -CH=, then -Y- is -O-; -R 2 is a substituted lower alkyl group; and -R 3 is -H or a lower alkyl group; and optionally, R 2 and R 3 may be united with an adjacent nitrogen atom to form a substituted piperidin-1-yl group or a piperazin-1-yl group substituted by an oxo group. COPYRIGHT: (C)2006,JPO&NCIPI
    • 待解决的问题:提供一种基于优异的人c-mpl-Ba / F3细胞增殖作用和巨核细胞集落形成加速作用产生具有血小板增多活性的2-酰基氨基噻唑衍生物或其药学上允许的盐的方法,并且是 可用于治疗血小板减少症。 方法:该方法产生由式(I)表示的2-酰基氨基噻唑衍生物或其药学上可允许的盐。 在式(I)中,-R SP 1是低级烷基或环烷基; -A = = -N =或-CH =; -X是卤素; (a)当-A =为-N =时,-Y-为-NR 3,和(b)当-A =为-CH =时,-Y-为-O-; -R 2 是取代的低级烷基; 且R 3 = H或低级烷基; 并且任选地,R“SP”2和R“3”可以与相邻的氮原子一起形成取代的哌啶-1-基或被哌嗪-1-基取代的哌嗪-1-基, 氧代基团。 版权所有(C)2006,JPO&NCIPI