Patent SG-11201810976T-A (SG)
Title: Pharmaceutical salts of n-(2-(2-(dimethylamino)ethoxy)-4-methoxy-5-((4-(1-methyl-1h-indol-3-yl)pyrimidin-2-yl)amino)phenyl)acrylamide and crystalline forms thereof
Inventor: GRECO MICHAEL
IPC: A61K31/506
Filed: 2017-06-16
Abstract: INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (43) International Publication Date 21 December 2017 (21.12.2017) WIP0 I PCT Iiiimmoimiolollmolomm oimIE (10) International Publication Number WO 2017/218892 Al (51) International Patent Classification: A61K 31/506 (2006.01) C07D 403/04 (2006.01) (21) International Application Number: PCT/US2017/037872 (22) International Filing Date: Published: — with international search report (Art. 21(3)) 16 June 2017 (16.06.2017) (25) Filing Language: English (26) Publication Language: English (30) Priority Data: 62/351,749 17 June 2016 (17.06.2016) US (71) Applicant: BETA PHARMA, INC. [US/US]; 1000 N. West Street, Suite 1200, Wilmington, DE 19801 (US). (72) Inventors: GRECO, Michael, Nicholas; 1634 Clearbrook Road, Lansdale, PA 19446 (US). COSTANZO, Michael, John; 14 Breckenridge Drive, Warminster, PA 18974 (US). GREEN, Michael, Alan; 1184 Dewalt Drive, Easton, PA 18040 (US). PENG, Jirong; 11019 North Kensington Dr., Mequon, WI 53097 (US). WILDE, Victoria, Lynn; 50 Pine Street, Apt. 41, Montclair, NJ 07042 (US). ZHANG, Don; 9 Kensington Court, Princeton, NJ 08540 (US). (74) Agent: LIU, Wansheng Jerry et al.; Fox Rothschild LLP, 997 Lenox Drive, Building 3, Lawrenceville, NJ 08648-2311 (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, DJ, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IR, IS, JO, JP, KE, KG, KH, KN, KP, KR, KW, KZ, LA, LC, LK, LR, LS, 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, SA, 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, ST, 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, 1-1 KM, ML, MR, NE, SN, TD, TG). co co (54) Title: PHARMACEUTICAL SALTS OF N-(2-(2-(DIMETHYLAMINO)ETHOXY)-4-METHOXY-544-(1-METHYL-1H-IN- DOL-3-YL)PYRIMIDIN-2-YL)AMINO)PHENYL)ACRYLAMIDE AND CRYSTALLINE FORMS THEREOF (57) : Crystalline forms of N-(2-(2-(dimethylamino)ethoxy)-4-methoxy-54(4-(1-methyl-1H- indo1-3-yl)pyrimidin-2- © yl)amino)phenyl)acrylamide (1) and its pharmaceutically acceptable salts and compositions thereof useful for the treatment or preven- tion of diseases or medical conditions mediated through mutated forms of epidermal growth factor receptor (EGFR), such as various 0 cancers, are disclosed.