Patent SG-11201901141W-A (SG)
Title: Crystalline form of (s)-7-(1-acryloylpiperidin-4-yl)-2-(4-phenoxyphenyl)-4,5,6,7-tetra-hydropyrazolo[1,5-a]pyrimidine-3-carboxamide, preparation, and uses thereof
Inventor: SHI GONGYIN
IPC: C07D487/04
Filed: 2017-08-15
Abstract: INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (43) International Publication Date 22 February 2018 (22.02.2018) WIPO I PCT IiiimmomiolollmonoloomunomimiolinifloiliollIE (10) International Publication Number WO 2018/033853 A3 (51) International Patent Classification: MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, SM, CO7D 487/04 (2006.01) A61P 29/00 (2006.01) TR), OAPI (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, A61K 31/519 (2006.01) A61P 35/00 (2006.01) KM, ML, MR, NE, SN, TD, TG). A61P 37/00 (2006.01) Published: with international search report (Art. 21(3)) before the expiration of the time limit for amending the claims and to be republished in the event of receipt of amendments (Rule 48.2(h)) (88) Date of publication of the international search report: (26) Publication Language: English 01 November 2018 (01.11.2018) (30) Priority Data: PCT/CN2016/095510 16 August 2016 (16.08.2016) CN (71) Applicant: BEIGENE, LTD.; c/o Mourant Ozannes Cor- porate Services (Cayman) Limited, 94 Solaris Avenue, Ca- mana Bay, Grand Cayman KY1-1108 (KY). (72) Inventors; and (71) Applicants (for SC only): WANG, Zhiwei [US/CN]; No.30 Science Park Road, Zhongguancun Life Science Park, Changping, Beijing 102206 (CN). GUO, Yunhang [CN/CN]; No.30 Science Park Road, Zhongguancun Life Science Park, Changping, Beijing 102206 (CN). (72) Inventor: SHI, Gongyin; No.30 Science Park Road, Zhongguancun Life Science Park, Changping, Beijing 102206 (CN). = (74) Agent: WU, FENG & ZHANG CO.; Room 305, Tower B, Beijing Aerospace Cpmiec Building, Beijing 100080 (CN). (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, (54) Title: CRYSTALLINE FORM OF (S)-7-(1-ACRYLOYLPIPERIDIN-4-YL)-2-(4-PHENOXYPHENYL)-4,5,6,7-TETRA-HY- DROPYRAZOLO[1,5-A]PYRIMIDINE-3-CARBOXAMIDE, PREPARATION, AND USES THEREOF (57) : The present invention relates to a crystalline form of (S)-7-(1-acryloylpiperidin-4-y1)-2-(4-phenoxypheny1)-4,5,6,7-tetr a-hydropyrazolo[1,5-a]pyrimi dine-3-carboxamide for inhibiting Btk, methods of preparation thereof and pharmaceutical compositions, and use of the crystalline form above in the treatment of a disease, or in the manufacturing of a medicament for the treatment of a disease. (21) International Application Number: PCT/IB2017/054955 (22) International Filing Date: 15 August 2017 (15.08.2017) (25) Filing Language: English W O 20 18/03385 3 A3