SG11201406468YA - Salt form of a human hi stone methyltransf erase ezh2 inhibitor - Google Patents

Abstract

(12) INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (43) International Publication Date 17 October 2013 (17.10.2013) WIPOIPCT (10) International Publication Number WO 2013/155317 A1 (51) International Patent Classification: C07D 407/12 (2006.01) A61P 35/00 (2006.01) A61K31/444 ( 2006.01) (21) International Application Number: PCT/US2013/036193 (22) International Filing Date: 11 April 2013 (11.04.2013) (25) Filing Language: English (26) Publication Language: English (30) Priority Data: 61/624,215 13 April 2012 (13.04.2012) US (71) Applicants: EPIZYME, INC. [US/US]; 400 Technology Square, 4th Floor, Cambridge, MA 02139 (US). EISAI R&D MANAGEMENT CO.LTD. [JP/JP]; 6-10, Koishi- kawa 4-chome, Bunkyo-ku, Tokyo 112-8088 (JP). (72) Inventors: KUNTZ, Kevin, Wayne; 8 New Village Road, Woburn, MA 01801 (US). HUANG, Kuan-chun; c/o Eisai, 4 Corporate Drive, Andover, MA 01810 (US). CHOI, Hyeong, Wook; c/o Eisai, Corporate Drive, 4 An­ dover, MA 01810 (US). SANDERS, Kristen; c/o Eisai, 4 Corporate Drive, Andover, MA 01810 (US). MATHIEU, Steven; c/o Eisai, 4 Corporate Drive, Andover, MA 01810 (US). CHANDA, Arani; c/o Eisai, Corporate Drive, 4 An­ dover, MA 01810 (US). FANG, Frank; c/o Eisai, 4 Cor­ porate Drive, Andover, MA 01810 (US). (74) Agents: BAUER, John, A. et al.; Mintz Levin Cohn Ferris Glovsky and Popeo, P.C., One Financial Center, Boston, MA 02111 (US). (81) Designated States (unless otherwise indicated, for every kind of national protection available)'. AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IS, JP, KE, KG, KM, KN, KP, KR, KZ, LA, LC, LK, LR, LS, LT, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW. (84) Designated States (unless otherwise indicated, for every kind of regional protection available)'. ARIPO (BW, GH, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, SZ, TZ, UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, RU, TJ, TM), European (AL, AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, SM, TR), OAPI (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, ML, MR, NE, SN, TD, TG). Published: — with international search report (Art. 21(3)) (54) Title: SALT FORM OF A HUMAN HI STONE METHYLTRANSF ERASE EZH2 INHIBITOR Polymorph A l> T-H m T-H rn i-H (57) Abstract: Provided herein is N-((4,6-dimethyl-2-oxo-l,2-dihydropyridin-3-yl)methyl)-5-(ethyl(tetrahydro-2H-pyran-4- O yl)amino)-4-methyl-4'-(morpholinomethyl)-[l,r-biphenyl]-3-carboxamide hydrobromide. Also provided herein is a particular poly- ^ morph form of this compound. Two-Theta (deg) FIG. 1