Claims for Patent: 11,491,163

Summary for Patent: 11,491,163

Title:	Salt form of a human histone methyltransferase EZH2 inhibitor
Abstract:	Provided herein is N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-5-(ethyl (tetrahydro-2H-pyran-4-yl)amino)-4-methyl-4′-(morpholinomethyl)-[1,1′-biphenyl]-3-carboxamide hydrobromide. Also provided herein is a particular polymorph form of this compound.
Inventor(s):	Kevin Wayne Kuntz, Kuan-Chun Huang, Hyeong Wook Choi, Kristen Sanders, Steven Mathieu, Arani Chanda, Francis Fang
Assignee:	Eisai R&D Management Co Ltd , Epizyme Inc
Application Number:	US17/032,432
Patent Claims:	1. A method of treating a cancer, comprising administering to a subject in need thereof a therapeutically effective amount of a polymorph of N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-5-(ethyl(tetrahydro-2H-pyran-4-yl)amino)-4-methyl-4′-(morpholinomethyl)-[1,1′-biphenyl]-3-carboxamide hydrobromide, wherein the polymorph exhibits an X-ray powder diffraction pattern having a peak at 10.1+/−0.3 degrees and one or more characteristic peaks expressed in degrees 2-theta selected from peaks at about 17.5+/−0.3 degrees and about 22.0+/−0.3 degrees 2-theta. 2. The method of claim 1, wherein the cancer is lymphoma, leukemia, melanoma, sarcoma, prostate cancer, or breast cancer. 3. The method of claim 2, wherein the cancer is lymphoma. 4. The method of claim 3, wherein the lymphoma is non-Hodgkin lymphoma, follicular lymphoma, or diffuse large B-cell lymphoma (DLBCL). 5. The method of claim 4, wherein the lymphoma is non-Hodgkin lymphoma. 6. The method of claim 4, wherein the lymphoma is follicular lymphoma. 7. The method of claim 4, wherein the lymphoma is diffuse large B-cell lymphoma (DLBCL). 8. The method of claim 2, wherein the cancer is sarcoma. 9. The method of claim 8, wherein the sarcoma is selected soft tissue sarcoma, osteosarcoma, rhabdomyosarcoma, Kaposi sarcoma, uterine sarcoma, or a sarcoma belonging to the Ewing family of sarcoma tumors. 10. A method of treating follicular lymphoma, comprising administering to a subject in need thereof a therapeutically effective amount of a polymorph of N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-5-(ethyl(tetrahydro-2H-pyran-4-yl)amino)-4-methyl-4′-(morpholinomethyl)-[1,1′-biphenyl]-3-carboxamide hydrobromide, wherein the polymorph exhibits an X-ray powder diffraction pattern having one or more characteristic peaks expressed in degrees 2-theta selected from peaks at about 10.1+/−0.3 degrees, about 17.5+/−0.3 degrees, and about 22.0+/−0.3 degrees 2-theta.