2-(6-甲基-吡啶-2-基)-3-基-[6-酰胺基-喹啉-4-基]-5,6-二氢-4H-吡咯并[1,2-b]吡唑的共晶,其制备方法和药物组合物

文档序号:1721752 发布日期:2019-12-17 浏览:36次 >En<

阅读说明:本技术 2-(6-甲基-吡啶-2-基)-3-基-[6-酰胺基-喹啉-4-基]-5,6-二氢-4H-吡咯并[1,2-b]吡唑的共晶,其制备方法和药物组合物 (Co-crystals of 2- (6-methyl-pyridin-2-yl) -3-yl- [ 6-amido-quinolin-4-yl ] -5, 6-dihydro-4H-pyrrolo [1,2-b ] pyrazole, processes for their preparation and pharmaceutical compositions containing them ) 是由 盛晓红 盛晓霞 汪晶 于 2017-03-21 设计创作,主要内容包括:本发明涉及式(I)所示的2-(6-甲基-吡啶-2-基)-3-基-[6-酰胺基-喹啉-4-基]-5,6-二氢-4H-吡咯并[1,2-b]吡唑(Galunisertib或LY2157299)与共晶形成物形成的共晶,与Galunisertib已知的固体形式相比,本发明的共晶在稳定性、溶解度等方面具有优势。本发明还涉及所述共晶的晶型及其制备方法,其药物组合物及其在制备用于预防和/或治疗与TGF-β有关的疾病中的用途。&lt;Image he="472" wi="700" file="DDA0002259668310000011.GIF" imgContent="drawing" imgFormat="GIF" orientation="portrait" inline="no"&gt;&lt;/Image&gt;(The invention relates to 2- (6-methyl-pyridine-2-yl) -3-yl- [ 6-amido-quinoline-4-yl group shown as the formula (I)]-5, 6-dihydro-4H-pyrrolo [1,2-b]The co-crystals formed by pyrazole (gallunertinib or LY2157299) with the co-crystal composition have advantages in terms of stability, solubility, etc. compared to the known solid forms of gallunertinib. The invention also relates to a crystal form of the eutectic crystal, a preparation method thereof, a pharmaceutical composition thereof and application thereof in preparing medicines for preventing and/or treating TGF-beta related diseases.)

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