Patent SG-11201805154Y-A (SG)
Title: Tetrahydropyranyl amino-pyrrolopyrimidinone and methods of use thereof
Inventor: LAPIERRE JEAN-MARC
IPC: C07D487/04
Filed: 2015-12-23
Abstract: INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property -, Organization 1111111101111011101010111110101111101110111011101011111111011111111101111011111 International Bureau 0.. .... .. (10) International Publication Number (43) International Publication Date ..... ..or::,,, WO 2017/111787 Al 29 June 2017(29.06.2017) WIPO I PCT (51) International Patent Classification: CHI SANKYO COMPANY, LIMITED, 3-5-1, Nihonbashi C07D 487/04 (2006.01) A61P 35/00 (2006.01) Honcho, Chuo-ku, Tokyo 103-8426 (JP). C07D 405/12 (2006.01) A61P 29/00 (2006.01) A61K 31/519 (2006.01) A61P 31/12 (2006.01) (74) Agents: ELRIFI, Ivor et al.; Cooley LLP, 1299 Pennsylvania Avenue, N.W., Washington, District of (21) International Application Number: Columbia 20004 (US). PCT/US2015/000285 (81) Designated States (unless otherwise indicated, for every (22) International Filing Date: 23 December 2015 (23.12.2015) 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, (25) Filing Language: English DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, (26) Publication Language: English HN, HR, HU, ID, IL, IN, IR, IS, JP, KE, KG, KN, KP, KR, KZ, LA, LC, LK, LR, LS, LU, LY, MA, MD, ME, MG, (71) Applicant: ARQULE, INC. [US/US]; One Wall Street, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, Burlington, Massachusetts 01803 (US). PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, SC, (72) Inventors: LAPIERRE, Jean-Marc; 1 Alexandra Drive, SD, SE, SG, SK, SL, 5M, ST, 5V, 5Y, TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW. Pelham, New Hampshire 03076 (US). EATHIRAJ, Sud- harshan; 24 Ptarmigan Drive, Shrewsbury, Massachusetts (84) Designated States (unless otherwise indicated, for every 01545 (US). NAMDEV, Nivedita; 18 Briarwood Drive, kind of regional protection available): ARIPO (BW, GH, Westford, Massachusetts 01545 (US). SCHWARTZ, Bri- an; 18 October Hill Rd., Woodbridge, Connecticut 06525 GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, TZ, UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, RU, (US). OTA, Yusuke; c/o DAIICHI SANKYO COM- TJ, TM), European (AL, AT, BE, BG, CH, CY, CZ, DE, PANY, LIMITED, 3-5-1, Nihonbashi Honcho, Chuo-ku, DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, Tokyo 103-8426 (JP). MOMOSE, Takayuki; c/o DAII- LV, MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, CHI SANKYO COMPANY, LIMITED, 3-5-1, Nihonbashi SM, TR), OAPI (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, = Honcho, Chuo-ku, Tokyo 103-8426 (JP). TSUNEMI, To- GW, KM, ML, MR, NE, SN, TD, TG). — moyuki; c/o DAIICHI SANKYO COMPANY, LIMITED, 3-5-1, Nihonbashi Honcho, Chuo-ku, Tokyo 103-8426 Published: (JP). INAGAKI, Hiroaki; c/o DAIICHI SANKYO COM- — with international search report (Art. 21(3)) PANY, LIMITED, 3-5-1, Nihonbashi Honcho, Chuo-ku, _ _ Tokyo 103-8426 (JP). NAKAYAMA, Kiyoshi; c/o DAII- = = = = = = Title: TETRAHYDROPYRANYL AMINO-PYRROLOPYRIMIDINONE AND METHODS OF USE THEREOF = (54) = C) HO CI — '`-''''NH 0 1-1 ® OPh (I) IN N GO LI ,, IN 1-1 N N H 1-1 1-1 IN 1-1 (57) : The application relates to a compound of Formula (I): or a pharmaceutically acceptable salt thereof, tautomer, prod- = mg, solvate, metabolite, polymorph, analog or derivative thereof, which modulates the activity of BTK, a pharmaceutical composi - \" tion comprising the compound of Formula (I), and a method of treating or preventing a disease in which BTK plays a role.