首页> 外国专利> Particulates of the CRTH2 antagonist { 4,6-bis(dimethylamino)-2-(4-(4-(trifluoromethyl)benzamido)-benzyl)pyrimidin-5-yl} acetic acid

Particulates of the CRTH2 antagonist { 4,6-bis(dimethylamino)-2-(4-(4-(trifluoromethyl)benzamido)-benzyl)pyrimidin-5-yl} acetic acid

机译:CRTH2拮抗剂{4,6-双(二甲基氨基)-2-(4-(4-(三氟甲基)苯甲酰胺基)-苄基)嘧啶-5-基}乙酸的颗粒

摘要

Disclosed are particulates of { 4,6-bis(dimethylamino)-2-(4-(4-(trifluoromethyl)benzamido)- benzyl)pyrimidin-5-yl} acetic acid, in crystalline Form I; wherein the crystalline Form I has a differential scanning calorimetric thermogram with an endotherm at a peak temperature of about 224 ºC and an onset temperature of about 220 ºC, wherein the differential scanning calorimetric thermogram is obtained at a heating rate of 10 ºC/min; and the particulates have an average particle size ranging from about 0.1 to about 150 mm; and wherein: the crystalline Form I has an X-ray powder diffraction pattern with one or more peaks expressed in two-theta at approximately 9.8, 13.1, 22.0, and 26.4º. Further disclosed is a process for the preparation of the particulates of { 4,6-bis(dimethylamino)-2-(4-(4-(trifluoromethyl)benzamido)-benzyl)pyrimidin-5-yl} acetic acid in crystalline Form I, comprising contacting { 4,6-bis(dimethylamino)-2-(4-(4-(trifluoromethyl)benzamido)benzyl)- pyrimidin-5-yl} acetic acid with a solvent such as acetonitrile, chloroform, dichloromethane, 1,4-dioxane, 2-methoxyethanol, MIBK, toluene, hexane(s), acetone, 1-butanol, DMSO, ethanol, ethyl acetate, ethyl formate, heptane, isobutyl acetate, 1-propanol, IPA, MEK, THF, water, and mixtures thereof.
机译:公开了结晶形式I的{4,6-双(二甲基氨基)-2-(4-(4-(三氟甲基)苯甲酰胺基)-苄基)嘧啶-5-基}乙酸的颗粒;其中晶型I具有差示扫描量热法热谱图,其吸热峰温度为约224℃,起始温度为约220℃,其中差示扫描量热法热谱图以10℃/ min的加热速率获得;所述颗粒的平均粒径为约0.1至约150mm;并且其中:晶型I具有X射线粉末衍射图,该X射线粉末衍射图具有在约9.8、13.1、22.0和26.4°处以两个θ表示的一个或多个峰。还公开了一种制备晶型I的{4,6-双(二甲基氨基)-2-(4-(4-(三氟甲基)苯甲酰胺基)-苄基)嘧啶-5-基}乙酸颗粒的方法,其包括使{4,6-双(二甲基氨基)-2-(4-(4-(4-(三氟甲基)苯甲酰胺基)苄基)-嘧啶基-5-基})乙酸与溶剂如乙腈,氯仿,二氯甲烷, 4-二恶烷,2-甲氧基乙醇,MIBK,甲苯,己烷,丙酮,1-丁醇,DMSO,乙醇,乙酸乙酯,甲酸乙酯,庚烷,乙酸异丁酯,1-丙醇,IPA,MEK,THF,水,及其混合物。

著录项

  • 公开/公告号NZ581811A

    专利类型

  • 公开/公告日2012-11-30

    原文格式PDF

  • 申请/专利权人 ACTIMIS PHARMACEUTICALS INC.;

    申请/专利号NZ20080581811

  • 发明设计人 LY TAI WEI;LI HUI-YIN;

    申请日2008-06-18

  • 分类号C07D239/48;A61K31/33;A61P11/06;A61P29;

  • 国家 NZ

  • 入库时间 2022-08-21 16:40:32

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