Patent SG-11201907604U-A (SG)
Title: Crystalline forms of the 4-pyrimidinesulfamide derivative aprocitentan
Inventor: BOLLI MARTIN
IPC: A61P9/12
Filed: 2018-02-26
Abstract: INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (43) International Publication Date 30 August 2018 (30.08.2018) WIPO I PCT omit VIII °nolo OH 100TH O II oimIE (10) International Publication Number WO 2018/154101 Al (51) International Patent Classification: A61K 31/513 (2006.01) A61P 9/12 (2006.01) (21) International Application Number: PCT/EP2018/054627 (22) International Filing Date: 26 February 2018 (26.02.2018) (25) Filing Language: English (26) Publication Language: English (30) Priority Data: PCT/EP2017/054489 27 February 2017 (27.02.2017) EP PCT/EP2017/061487 12 May 2017 (12.05.2017) EP (71) Applicant: IDORSIA PHARMACEUTICALS LTD [CH/CH]; Hegenheimermattweg 91, 4123 Allschwil (CH). (72) Inventors: BOLLI, Martin; c/o Idorsia Pharmaceuti- cals Ltd, Hegenheimermattweg 91, 4123 Allschwil (CH). KOHLER, Philipp; c/o Idorsia Pharmaceuticals Ltd, Hegenheimermattweg 91, 4123 Allschwil (CH). SCHIN- DELHOLZ, Ivan; c/o Idorsia Pharmaceuticals Ltd, Hegen- heimermattweg 91, 4123 Allschwil (CH). VON RAUMER, Markus; c/o Idorsia Pharmaceuticals Ltd, Hegenheimer- mattweg 91, 4123 Allschwil (CH). TR), OAPI (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, KM, ML, MR, NE, SN, TD, TG). Declarations under Rule 4.17: as to applicant's entitlement to apply for and be granted a patent (Rule 4.17(ii)) as to the applicant's entitlement to claim the priority of the earlier application (Rule 4.17(iii)) Published: — with international search report (Art. 2 I (3)) (74) Agent: VELKER, Jorg; c/o Idorsia Pharmaceuticals Ltd, Hegenheimermattweg 91, 4123 Allschwil (CH). (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, (54) Title: CRYSTALLINE FORMS OF THE 4-PYRIMIDINESULFAMIDE DERIVATIVE APROCITENTAN (57) : The present invention concerns novel crystalline forms of {5-(4-bromo-phenyl)-642-(5-bromo-pyrimidin-2-yloxy)- ethoxy]-pyrimidin-4-yll -sulfamide, processes for the preparation thereof, pharmaceutical compositions comprising said crystalline forms, pharmaceutical compositions prepared from such crystalline forms, and their use as endothelin receptor antagonists. It also relates to new uses of {5-(4-bromo-phenyl)-642-(5-bromo-pyrimidin-2-yloxy)-ethoxy]-pyrimidin-4-yll -sulfamide, either alone or in combination with other active ingredients or therapeutic agents.