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US 8,507,005 B2Granted
Particulates of a CRTH2 antagonist
AssigneeActimis Pharmaceuticals, Inc.
InventorsTai Wei Ly, Hui-Yin Li
Life of this patent
Estimating the term…
Abstract
Provided herein are particulates of {4,6-bis(dimethylamino)-2-(4-(4-(trifluoromethyl)benzamido)benzyl)pyrimidin-5-yl}acetic acid in amorphous or crystalline forms, processes for their preparation, pharmaceutical compositions comprising them, and methods of their use for treating, preventing, or ameliorating one or more symptoms of a CRTH2-mediated disorder or disease.
Claims11
Particulates of {4,6-bis(dimethylamino)-2-(4-(4-(trifluoromethyl)benzamido)-benzyl)pyrimidin-5-yl}acetic acid of Formula I:
- in crystalline Form I;
- wherein the particulates have one or more characteristics, selected from the group consisting of:
- (i) having an average particle size ranging from about 0.1 to about 150 μm;
- (ii) having a uniformity coefficient ranging from about 1 to about 20;
- (iii) having a tapped bulk density ranging from about 0.1 to about 1.0 g/mL;
- (iv) containing no less than about 95% by weight of the acid of Formula I;
- (v) having a residual organic solvent content of no greater than about 5% by weight;
- (vi) having a residual methanol content of no greater than about 100,000 ppm;
- (vii) containing no less than about 90% by weight of the particulates in Form I;
- and
- wherein the particulates have a differential scanning calorimetric thermogram with an endotherm at a peak temperature of about 224° C. and an onset temperature of about 220° C.
8 more elements
4,6-Bis(dimethylamino)-2-(4-(4-(trifluoromethyl)benzamido)-benzyl)pyrimidin-5-yl}acetic acid in crystalline Form I;
- wherein the crystalline form 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 26.4°;
- and wherein the particulates have a differential scanning calorimetric thermogram with an endotherm at a peak temperature of about 224° C. and an onset temperature of about 220° C.
Dependencies are inferred from the claim text.