Patent SG-11201907435P-A (SG)
Title: Combinations of a 4-pyrimidinesulfamide derivative with active ingredients for the treatment of endothelin related diseases
Inventor: BELLET MARC
IPC: A61K31/4422
Filed: 2017-11-06
Abstract: O C (12) 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 oimitia °nolo °H0111 m offiniou oimIE (10) International Publication Number WO 2018/153513 Al (51) International Patent Classification: A61K 31/41 (2006.01) A61K 31/549 (2006.01) A61K 31/4422 (2006.01) A61P 9/12 (2006.01) A61K 31/513 (2006.01) (21) International Application Number: PCT/EP2017/078371 (22) International Filing Date: 06 November 2017 (06.11.2017) (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: BELLET, Marc; c/o Idorsia Pharmaceuticals Ltd, Hegenheimermattweg 91, 4123 Allschwil (CH). BOL- LI, Martin; c/o Idorsia Pharmaceuticals Ltd, Hegenheimer- mattweg 91, 4123 Allschwil (CH). CLOZEL, Martine; c/ o Idorsia Pharmaceuticals Ltd, Hegenheimermattweg 91, 4123 Allschwil (CH). IGLARZ, Marc; c/o Idorsia Phar- maceuticals 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). (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, 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. 21(3)) (54) Title: COMBINATIONS OF A 4-PYRIMIDINESULFAMIDE DERIVATIVE WITH ACTIVE INGREDIENTS FOR THE TREATMENT OF ENDOTHELIN RELATED DISEASES (57) : The present invention concerns the compound aprocitentan, {5-(4-bromo-phenyl)-642-(5-bromo-pyrimidin-2-yloxy)- ethoxy]-pyrimidin-4-yll -sulfamide, and its use as endothelin receptor antagonist, in combination with other active ingredients or ther- apeutic agents including an angiotenin receptor blocker, and/or a calcium channel blocker, and preferably a diuretic which is a thi- azide-like diuretic, in the prophylaxis or treatment of certain endothelin related diseases. The invention further relates to pharmaceutical compositions comprising aprocitentan in combination with said other active ingredients or therapeutic agents. The invention further relates to such pharmaceutical compositions comprising novel crystalline forms of aprocitentan.