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Last Updated: December 15, 2025

Claims for Patent: 9,469,643

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Summary for Patent: 9,469,643

Title:	Polymorphic forms of (S)-2-(1-(9H-purin-6-ylamino)propyl)-5-fluoro-3-phenylquinazolin-4(3H)-one
Abstract:	Polymorphs of (S)-2-(1-(9H-purin-6-ylamino)propyl)-5-fluoro-3-phenylquinazolin-4(3H)-one, compositions thereof, methods for their preparation, and methods for their use are disclosed.
Inventor(s):	Ernest CARRA, Michael Gerber, Bing Shi, Keiko Sujino, Duong Tran, Fang Wang, Jerry B. Evarts
Assignee:	Gilead Calistoga LLC
Application Number:	US14/493,261
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 9,469,643
Patent Claims:	1. A polymorph of (S)-2-(1-(9H-purin-6-ylamino)propyl)-5-fluoro-3-phenylquinazolin-4(3H)-one, wherein the polymorph is Form II having an X-ray powder diffraction pattern comprising characteristic peaks, plus or minus 0.2 degrees 2θ, at 14.0 degrees 2θ, 18.6 degrees 2θ, and 24.3 degrees 2θ. 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)-one; 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° C. and 25° 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)-one 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.

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