Details for Patent: 9,469,643
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Title: | Polymorphic forms of (S)-2-(1-(9H-purin-6-ylamino)propyl)-5-fluoro-3-phenylquinazolin-4(3H)-on- e |
Abstract: | Polymorphs of (S)-2-(1-(9H-purin-6-ylamino)propyl)-5-fluoro-3-phenylquinazolin-4(3H)-on- e, compositions thereof, methods for their preparation, and methods for their use are disclosed. |
Inventor(s): | Carra; Ernest (Foster City, CA), Gerber; Michael (Oakland, CA), Shi; Bing (Redwood City, CA), Sujino; Keiko (Edmonton, CA), Tran; Duong (Edmonton, CA), Wang; Fang (Foster City, CA), Evarts; Jerry B. (Seattle, WA) |
Assignee: | Gilead Calistoga, LLC. (Foster City, CA) |
Filing Date: | Sep 22, 2014 |
Application Number: | 14/493,261 |
Claims: | 1. A polymorph of (S)-2-(1-(9H-purin-6-ylamino)propyl)-5-fluoro-3-phenylquinazolin-4(3H)-on- e, wherein the polymorph is Form II having an X-ray powder diffraction pattern comprising characteristic peaks, plus or minus 0.2 degrees 2.theta., at 14.0 degrees 2.theta., 18.6 degrees 2.theta., and 24.3 degrees 2.theta.. 2. The polymorph of claim 1, wherein the polymorph has an X-ray powder diffraction pattern substantially as shown in FIG. 2A. 3. A polymorph of claim 1 obtained by: a) grinding polymorphic Form I of (S)-2-(1-(9H-purin-6-ylamino)propyl)-5-fluoro-3-phenylquinazolin-4(3H)-on- e; and b) stirring the ground polymorphic Form I in a solvent to form the polymorph of claim 1. 4. The polymorph of claim 3, wherein the ground polymorphic Form I is stirred in the solvent at a temperature of between about 10.degree. C. and 25.degree. C. 5. The polymorph of claim 3, wherein the grinding is performed using a mortar and pestle, a high shear wet mill, a high shear dry mixer, a jet mill, a ball mill, or a combination thereof. 6. A polymorph of claim 1 obtained by compressing polymorphic Form I of (S)-2-(1-(9H-purin-6-ylamino)propyl)-5-fluoro-3-phenylquinazolin-4(3H)-on- e at a pressure of between about 500 psi and 5000 psi to convert at least a portion of the polymorphic Form I to a polymorph of claim 1. |