Claims for Patent: 9,809,559

Summary for Patent: 9,809,559

Title:	(N-(cyanomethyl)-4-(2-(4-morpholinophenylamino)pyrimidin-4-yl)benzamide
Abstract:	The present invention relates to stable novel salt forms of N-(cyanomethyl)-4-(2-(4-morpholinophenylamino)pyrimidin-4-yl)benzamide that are suitable for the preparation of pharmaceutical formulations thereof, and their therapeutic use.
Inventor(s):	Brown Brandon H., Carra Ernest A., Hemenway Jeffrey N., Morrison Henry, Reynolds Troy, Shi Bing, Stefanidis Dimitrios, Wang Fang, Warr Matthew Robert, Whitney James Andrew, Xin Yan
Assignee:	GILEAD SCIENCES, INC.
Application Number:	US15231411
Patent Claims:	1. A method of treating myelofibrosis or polycythemia vera comprising administering to a subject in need thereof a compound selected from the group consisting of:N-(cyanomethyl)-4-(2-(4-morpholinophenylamino)pyrimidin-4-yl)benzamide dihydrochloride monohydrate Form II;N-(cyanomethyl)-4-(2-(4-morpholinophenylamino)pyrimidin-4-yl)benzamide monohydrochloride anhydrous Form I; andN-(cyanomethyl)-4-(2-(4-morpholinophenylamino)pyrimidin-4-yl)benzamide monohydrochloride anhydrous Form III.2. The method of claim 1 , wherein the compound is in a crystalline form.3. The method of claim 2 , wherein the crystalline form is N-(cyanomethyl)-4-(2-(4-morpholinophenylamino)pyrimidin-4-yl)benzamide dihydrochloride monohydrate Form II.4. The method of claim 3 , wherein the crystals have unit cell parameters at T=100° K of: a=10.2837(6) Å claim 3 , b=10.4981(6) Å claim 3 , c=11.5143(7) Å claim 3 , α=83.297(2)° claim 3 , β=87.649(2)° claim 3 , γ=67.445(2)° claim 3 , and a triclinic P-1 space group.5. The method of claim 3 , wherein the crystalline form is characterized by an x-ray powder diffraction (XRPD) pattern substantially as set forth in .6. The method of claim 3 , wherein the crystalline form is characterized by an x-ray powder diffraction (XRPD) pattern having peaks at about 7.7° claim 3 , 19.3° claim 3 , 24.0° claim 3 , 25.7° claim 3 , and 29.6° 2-θ±0.2° 2-θ.7. The method of claim 3 , wherein the crystalline form is characterized by differential scanning calorimetry (DSC) pattern substantially as set forth in .8. The method of claim 3 , wherein the crystalline form is characterized by a dynamic vapor sorption (DVS) pattern substantially as set forth in .9. The method of claim 2 , wherein the crystalline form is crystalline N-(cyanomethyl)-4-(2-(4-morpholinophenylamino)pyrimidin-4-yl)benzamide monohydrochloride anhydrous Form I.10. The method of claim 9 , wherein the crystalline form is characterized by an x-ray powder diffraction (XRPD) pattern substantially as set forth in .11. The method of claim 9 , wherein the crystalline form is characterized by an X-ray powder diffraction (XRPD) pattern having peaks at about 13.5° claim 9 , 20.9° claim 9 , 26.1° claim 9 , 26.6° claim 9 , and 28.3° 2-θ±0.2° 2-θ.12. The method of claim 9 , wherein the crystalline form is characterized by a differential scanning calorimetry (DSC) pattern substantially as set forth in .13. The method of claim 2 , wherein the crystalline form is crystalline N-(cyanomethyl)-4-(2-(4-morpholinophenylamino)pyrimidin-4-yl)benzamide monohydrochloride anhydrous Form III.14. The method of claim 13 , wherein the crystalline form is characterized by an x-ray powder diffraction (XRPD) pattern substantially as set forth in .15. The method of claim 13 , wherein the crystalline form is characterized by an X-ray powder diffraction (XRPD) pattern having peaks at about 12.7° claim 13 , 14.6° claim 13 , 17.8° claim 13 , 19.7° claim 13 , and 23.3° 2-θ±0.2° 2-θ.16. The method of claim 13 , wherein the crystalline form is characterized by a differential scanning calorimetry (DSC) pattern substantially as set forth in .