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US 7,442,707 B2Granted
CCI-779 polymorph and use thereof
AssigneeWyeth
InventorSubodh S. Deshmukh
Life of this patent
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Abstract
The present invention provides CCI-779 polymorph Form II. This invention also provides processes for preparing CCI-779 polymorph Form II and pharmaceutical compositions including CCI-779 polymorph Form II.
Claims11
A CCI-779 polymorph having an X-ray diffraction peak pattern lacking peaks at 2θ values of 7.6, 9.5, 11.4, 15.0, 16.8, 18.2, 18.5, and 21.2, and characterized by
- a X-ray diffraction peak pattern comprising peaks at 2θ of about 6.6, 9.8, 14.0, 14.1, 14.5, and 18.8;
- a differential scanning calorimetry thermogram having an endotherm with an onset temperature of about 110° C.;
- and a thermogravimetric analysis of less than 1 wt % weight loss on heating from 25° C. to 150° C.
An isolated CCI-779 polymorph Form II obtainable by precipitating said CCI-779 polymorph Form II from a suspension comprising amorphous CCI-779 and t-butyl methyl ether.
A process for preparing CCI-779 polymorph Form II, comprising the steps of:
- (a) dissolving CCI-779 in an initial solvent comprising acetone;
- (b) removing said initial solvent in step (a) to form a solid foam;
- (c) mixing the solid foam with t-butyl methyl ether (t-BME) to form a suspension and stirring to afford CCI-779 polymorph Form II;
- and
- (d) collecting said CCI-779 polymorph Form II.
2 more elements
Dependencies are inferred from the claim text.