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Particulates of the CRTH2 antagonist { 4,6-bis(dimethylamino)-2-(4-(4-(trifluoromethyl)benzamido)-benzyl)pyrimidin-5-yl} acetic acid
专利权人:
ACTIMIS PHARMACEUTICALS; INC.
发明人:
LY, TAI, WEI,LI, HUI-YIN
申请号:
NZ58181108
公开号:
NZ581811A
申请日:
2008.06.18
申请国别(地区):
NZ
年份:
2012
代理人:
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.
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