Claims for Patent: 8,865,730

Summary for Patent: 8,865,730

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. (Redmond, WA)
Assignee:	Gilead Calistoga LLC (Foster City, CA)
Application Number:	13/786,222
Patent 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 I having an X-ray powder diffraction pattern comprising characteristic peaks plus or minus 0.2 degrees 2.theta., at 17.7 degrees 2.theta. and 24.9 degrees 2.theta.. 2. The polymorph of claim 1, wherein the X-ray powder diffraction pattern further comprises characteristic peaks plus or minus 0.2 degrees 2.theta., at 14.3 degrees 2.theta., 17.2 degrees 2.theta., 20.9 degrees 2.theta., and 23.9 degrees 2.theta.. 3. The polymorph of claim 1, wherein the polymorph has an X-ray powder diffraction pattern substantially as shown in FIG. 1A. 4. A polymorph of claim 1 obtained by: a) combining (S)-2-(1-(9H-purin-6-ylamino)propyl)-5-fluoro-3-phenylquinazolin-4(3H)-on- e with a solvent to form a mixture; b) heating the mixture to form a solution; and c) cooling the heated solution to form the polymorph of claim 1. 5. The polymorph of claim 4, wherein: the mixture is heated to a temperature of at least 50.degree. C.; and the heated solution is cooled to a temperature of at least about 30.degree. C. 6. A pharmaceutical composition comprising the polymorph of claim 1, and one or more pharmaceutically acceptable carriers or excipients. 7. The pharmaceutical composition of claim 6, wherein the pharmaceutical composition is a tablet. 8. A method of preparing the polymorph of claim 1, comprising: a) combining (S)-2-(1-(9H-purin-6-ylamino)propyl)-5-fluoro-3-phenylquinazoli- n-4(3H)-one with a solvent to form a mixture; b) heating the mixture to form a solution; and c) cooling the heated solution to form the polymorph of claim 1. 9. The method of claim 8, wherein: the mixture is heated to a temperature of at least about 50.degree. C.; and the solution is cooled to a temperature of at least about 30.degree. C. 10. A method of treating a human in need of a cancer treatment, comprising administering to the human a composition comprising the polymorph of claim 1, and one or more pharmaceutically acceptable carriers or excipients wherein the cancer is a hematologic malignancy. 11. A method of treating a human in need of a cancer treatment, comprising administering to the human a composition comprising the polymorph of claim 1, and one or more pharmaceutically acceptable carriers or excipients, wherein the cancer is selected from the group consisting of acute lymphocytic leukemia (ALL), acute myeloid leukemia (AML), chronic lymphocytic leukemia (CLL), small lymphocytic lymphoma (SLL), myelodysplastic syndrome (MDS), myeloproliferative disease (MPD), chronic myeloid leukemia (CML), multiple myeloma (MM), indolent non-Hodgkin's lymphoma (iNHL), refractory iNHL, non-Hodgkin's lymphoma (NHL), mantle cell lymphoma (MCL), follicular lymphoma, Waldestrom's macroglobulinemia (WM), T-cell lymphoma, B-cell lymphoma, and diffuse large B-cell lymphoma (DLBCL). 12. The method of claim 11, wherein the cancer is selected from the group consisting of chronic lymphocytic leukemia (CLL), indolent non-Hodgkin's lymphoma (iNHL), and refractory iNHL.