首页> 外国专利> Crystal forms of (6 - 4 - (piperazin-1-yl Ethyl methyl) phenyl - 7h pyrrolo 2, 3-d pyrimidin-4-yl) - (R) - 1 - phenyl Ethyl Amine and the same in Amorphous State, Preparation methods the same, Pharmaceutical compositions containing them and the use of these forms Crist

Crystal forms of (6 - 4 - (piperazin-1-yl Ethyl methyl) phenyl - 7h pyrrolo 2, 3-d pyrimidin-4-yl) - (R) - 1 - phenyl Ethyl Amine and the same in Amorphous State, Preparation methods the same, Pharmaceutical compositions containing them and the use of these forms Crist

机译:(6- [4-(哌嗪-1-基乙基甲基)苯基] -7h吡咯并[2,3-d]嘧啶-4-基)-(R)-1-苯基乙基胺的晶体形式非晶态,相同的制备方法,包含它们的药物组合物以及这些形式的用途

摘要

Crystal forms of (6 - [4 - (ethyl - piperazin - 1 - methyl) phenyl] - 7h pyrrolo [2,3-d] pyrimidine II} - (4 - (R) - 1 - phenyl ethyl) Amine, the procedure for the preparation of these Crystalline forms of {6 - [4 - (ethyl - piperazin - 1 - methyl) phenyl] - 7h pyrrolo [2,3-d] pyrimidine II} - (4 - (R) - 1 - phenyl ethyl) amine.Compositions containing the Crystalline forms (6 - [4 - (ethyl - piperazin - 1 - methyl) phenyl] - 7h pyrrolo [2,3-d] pyrimidine II} - (4 - (R) - 1 - phenyl ethyl) Amine, and the use of these Crystalline forms {6 - [4 - (ethyl - piperazin - 1 - methyl) phenyl] - 7h pyrrolo [2,3-d] pyrimidine II} - (4 - (R) - 1 - phenyl ethyl) amine In the therapy of warm blooded Animals, especially humans.Claim 2: The Compound according to claim 1, which shows a diffraction Peak of x ray diffraction Angle 2 Theta 4.4u00b0 + - 0.2 degrees (%).Claim 1, a process for the preparation of Crystalline form of {6 - [4 - (ethyl - piperazin - 1 - methyl) phenyl] - 7h pyrrolo [2,3-d] pyrimidin-4-yl) - ((R) - 1 - phenyl ethyl) Amine which includes: (a) contacting {6 - [4 - (Ethyl - piperazin - 1 - methyl) phenyl] - 7h pyrrolo [2,3 - d] pyrimidin-4-yl) - ((R) - 1 - phenyl ethyl) Amine with a Solvent to form a precipitate; (b) to resuspend the pellet in a Second Solvent to form a Second precipitate; and (c) separating the second precipitate. Claim 1: The Compound according to claim 1, which shows a diffraction Peak of x-ray diffraction Angle 2 Theta 5.7u00b0 + - 0.2u00b0.Claim 31: a process for the preparation of Crystalline Form b {6 - [4 - (ethyl - piperazin - 1 - methyl) phenyl] - 7h pyrrolo [2,3-d] pyrimidine II} - (4 - (R) - 1 - phenyl ethyl) Amine which includes: (a) contacting {6 - [4 - (ethyl - piperazin - 1 - methyl) phenyl] - 7h pyrrolo [2,3 - d] pyrimidin-4-yl) - ((R) - 1 - phenyl ethyl) Amine with a Solvent to form a precipitate; and (b) separating the second precipitate. The Compound claim 35: According to claim 25, which shows a diffraction Peak of x-ray diffraction Angle 2 Theta 5.7u00b0 + - 0.2u00b0.Claim 47: a process for the preparation of Crystalline form c {6 - [4 - (ethyl - piperazin - 1 - methyl) phenyl] - 7h pyrrolo [2,3-d] pyrimidin-4-yl) - ((R) - 1 - phenyl ethyl) Amine which includes: (a) contacting {6 - [4 - (Ethyl - piperazin - 1 - methyl) phenyl] - 7h pyrrolo [2,3 - d] pyrimidin-4-yl) - ((R) - 1 - phenyl ethyl) Amine with a Solvent to form a precipitate; and (b) separating the second precipitate. The Compound claim 52: According to claim 51, which has substantially the same x-ray diffraction pattern as shown in Figure 11.
机译:(6- [4-(乙基-哌嗪-1-甲基)苯基] -7h吡咯并[2,3-d]嘧啶II}-(4-(R)-1-苯基乙基)胺的晶型,该方法制备{6- [4-(乙基-哌嗪-1-甲基)苯基] -7h吡咯并[2,3-d]嘧啶II}-(4-(R)-1-苯基乙基含有结晶形式(6- [4-(乙基-哌嗪-1-甲基)苯基] -7h吡咯并[2,3-d]嘧啶II}-(4-(R)-1-苯基乙基)胺,以及使用这些晶体形式的{6- [4--(乙基-哌嗪-1-甲基)苯基]-7h吡咯并[2,3-d]嘧啶II}-(4-(R)-1-权利要求2的化合物,其显示x射线衍射角2θ为4.4±0.2度(%)的衍射峰。权利要求1的化合物。 ,一种制备{6- [4-(乙基-哌嗪-1-甲基)苯基] -7h吡咯并[2,3-d]吡啶的晶型的方法Midin-4-yl)-((R)-苯乙基)胺,包括:(a)与{6- [4--(乙基-哌嗪-1-甲基)苯基]-7h吡咯并[2,3- d]嘧啶-4-基)-((R)-1-苯基乙基)胺与溶剂形成沉淀; (b)将沉淀重悬于第二溶剂中以形成第二沉淀物; (c)分离第二沉淀物。权利要求1的化合物,其显示x射线衍射角2θ为5.7 u00b0 + -0.2 u00b0的衍射峰。权利要求31:制备晶型b {6- [4-]的方法。 (乙基-哌嗪-1-甲基)苯基]-7h吡咯并[2,3-d]嘧啶II}-(4-(R)-1-苯基乙基)胺,包括:(a)与{6- [4 -(乙基-哌嗪-1-甲基)苯基] -7h吡咯并[2,3-d]嘧啶-4-基)-((R)-1-苯基乙基)胺与溶剂形成沉淀; (b)分离第二沉淀物。 35.根据权利要求25所述的化合物,其显示了x射线衍射角2θ5.7的衍射峰。5.7。u0.2b。47.一种制备晶型c {6- [4-]的方法。 (乙基-哌嗪-1-甲基)苯基] -7h吡咯并[2,3-d]嘧啶-4-基)-((R)-1-苯基乙基)胺,包括:(a)与{6- [ 4-(乙基-哌嗪-1-甲基)苯基] -7h吡咯并[2,3-d]嘧啶-4-基)-((R)-1-苯基乙基)胺与溶剂形成沉淀; (b)分离第二沉淀物。 52.根据权利要求51所述的化合物,其具有与图11所示基本相同的X射线衍射图。

著录项

  • 公开/公告号AR059090A1

    专利类型

  • 公开/公告日2008-03-12

    原文格式PDF

  • 申请/专利权人 NOVARTIS AG.;

    申请/专利号AR2007P100240

  • 发明设计人

    申请日2007-01-19

  • 分类号C07D487/04;A61K31/519;A61P35/00;C07D487/04;C07D239/00;C07D221/00;

  • 国家 AR

  • 入库时间 2022-08-21 20:08:57

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