利索-全球专利检索

  1. 登录
  2. 注册
发明授权
CN107949560B 吡啶取代的2-氨基吡啶类蛋白激酶抑制剂的结晶 有权 转让

吡啶取代的2-氨基吡啶类蛋白激酶抑制剂的结晶
摘要：
本发明公开了吡啶取代的2‑氨基吡啶类蛋白激酶抑制剂的结晶，具体涉及5‑((R)‑l‑(2,6‑二氯‑3‑氟苯基)乙氧基)‑4'‑甲氧基‑6'‑((S)‑2‑甲基哌嗪‑1‑基)‑3，3'‑联吡啶‑6‑胺的柠檬酸盐结晶、其制备方法、结晶组合物和药物组合物，还公开了式I化合物柠檬酸盐结晶与蛋白激酶有关疾病的用途，本发明的柠檬酸盐结晶在生物利用度、吸湿性、稳定性、溶解性、纯度、易制备等至少一方面优于5‑((R)‑l‑(2,6‑二氯‑3‑氟苯基)乙氧基)‑4'‑甲氧基‑6'‑((S)‑2‑甲基哌嗪‑1‑基)‑3,3'‑联吡啶‑6‑胺或5‑((R)‑l‑(2,6‑二氯‑3‑氟苯基)乙氧基)‑4'‑甲氧基‑6'‑((S)‑2‑甲基哌嗪‑1‑基)‑3,3'‑联吡啶‑6‑胺的其它盐。
摘要（英）：

The present invention discloses a crystal of citrate salt of pyridine-substituted 2-aminopyridine-based protein kinase inhibitors, in particular, to crystal of 5-((R)-1-(2,6-dichloro-3-fluorophenyl)ethoxy)-4'-methoxy-6'-((S)-2-methylpiperazin -1-yl)-3,3'-bipyridin-6-amine citrate salt, a method for preparation thereof, a crystalline composition and a pharmaceutical composition comprising the crystal, and further discloses the use of crystals of citrate salt of the compound of Formula I in protein kinase-related diseases. The crystals of citrate salt according to the present invention are superior to 5-((R)-1-(2,6-dichloro-3-fluorophenyl)ethoxy)-4'-methoxy-6'-((S)-2-methylpiperazin-1-yl)-3,3'-bipyridin-6-amine or other salts of 5-((R)-1-(2,6-dichloro-3-fluorophenyl)ethoxy)-4'-methoxy-6'-((S)-2-methylpiperazin-1-yl)-3,3'-bipyridin-6-amine in at least one aspect of bioavailability, hygroscopicity, stability, solubility, purity, ease of preparation, and the like.

公开/授权文献
0/0