SG11201908128YA - Subcutaneous administration of a p2y12 receptor antagonist - Google Patents

Abstract

INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (43) International Publication Date 20 September 2018 (20.09.2018) WIPO I PCT ill~~~~~~~~ 011101010VIIIOH olo omioom minnow° oimIE (10) International Publication Number WO 2018/167139 Al (51) International Patent Classification: A61K 31/506 (2006.01) A61P 7/02 (2006.01) (21) International Application Number: PCT/EP2018/056372 (22) International Filing Date: 14 March 2018 (14.03.2018) (25) Filing Language: English (26) Publication Language: English (30) Priority Data: PCT/EP2017/056175 15 March 2017 (15.03.2017) EP (71) Applicant: IDORSIA PHARMACEUTICALS LTD [CH/CH]; Hegenheimermattweg 91, 4123 Allschwil (CH). (72) Inventors: BAUMANN, Martine; c/o Idorsia Pharma- ceuticals Ltd, Hegenheimermattweg 91, 4123 Allschwil (CH). KRAMBERG, Markus; c/o Idorsia Pharmaceuticals Ltd, Hegenheimermattweg 91, 4123 Allschwil (CH). REY, Markus; c/o Idorsia Pharmaceuticals Ltd, Hegenheimer- mattweg 91, 4123 Allschwil (CH). RIEDERER, Markus; c/o Idorsia Pharmaceuticals Ltd, Hegenheimermattweg 91, 4123 Allschwil (CH). ROUX, Sebastien; c/o Idorsia Phar- maceuticals Ltd, Hegenheimermattweg 91, 4123 Allschwil (CH). 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 4.1700) 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)) 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)) (74) Agent: KOBERSTEIN, Ralf; 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, (54) Title: SUBCUTANEOUS ADMINISTRATION OF A P2Y12 RECEPTOR ANTAGONIST (57) : The present invention relates to a P2Y12 receptor antagonist selected from the group consisting of4-((R)-2- { [6-((S)-3-methoxy-pyrrolidin-l-y1)-2-phenyl-pyrimidine-4-carbony1]-aminol -3-phosphono-propiony1)-piperazine-l-carboxylic acid butyl ester, (1 S,2 S,3R,5 S)-3- [7- [(1R,25)-2-(3,4 -difluorophenyl)cyclopropylamino] -5 -(propylthio)-3H- [1,2,3]triazolo [4,5 -d]pyrim idin-3-y1]-5-(2-hydroxyethoxy)cyclopentane-1,2-diol, and (1S,2R,3S,4R)-4-[7- [(1R,25)-2-(3,4-difluorophenyl)cyclopropylami- no]-5-(propylthio)-3H41,2,3]triazolo[4,5-d]pyrimidin-3-yl]cyclopentane-1,2,3-triol, or a pharmaceutically acceptable salt thereof, for use as a medicament by subcutaneous or intradermal administration. 1-1 N 00 O C