Patent SG-11201903803U-A (SG)
Title: Aldosterone synthase inhibitor
Inventor: SCHUMACHER CHRISTOPH
IPC: A61P5/38
Filed: 2017-10-26
Abstract: INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property MD 1101111 0 DOI HIM 011101 0 011111H111111111111111111111111111111111111 Organization International Bureau (10) International Publication Number (43) International Publication Date ......0\" WO 2018/078049 Al 03 May 2018 (03.05.2018) WIP0 I PCT (51) International Patent Classification: Declarations under Rule 4.17: A61K 31/437 (2006.01) A61P 9/04 (2006.01) A61P 5/38 (2006.01) CO7D 471/04 (2006.01) — as to applicant's entitlement to apply for and be granted a patent (Rule 4.17(H)) (21) International Application Number: PCT/EP2017/077511 Published: — with international search report (Art. 21(3)) (22) International Filing Date: 26 October 2017 (26.10.2017) (25) Filing Language: English (26) Publication Language: English (30) Priority Data: 62/413,635 27 October 2016 (27.10.2016) US 16205019.9 19 December 2016 (19.12.2016) EP (71) Applicant: DAMIAN PHARMA AG [CH/CH]; Haltli 6, 6318 Walchwil (CH). (72) Inventors: SCHUMACHER, Christoph; Haltli 6, 6318 Walchwil (CH). FUHRER, Walter; Im Budler 3, 4419 _ Lupsingen (CH). STEELE, Ronald, Edward; 101 Naugh- right Road, Long Valley, New Jersey 07853 (US). — = Agent: SPERRLE, Martin; Latscha Schollhorn Partner (74) AG, Austrasse 24, 4051 Basel (CH). = 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, (81) = = — 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. _ Designated States (unless otherwise indicated, for every — (84) _ _ 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). = 1-1 ON (54) Title: ALDOSTERONE SYNTHASE INHIBITOR C 71' (57) : The present invention relates to a compound selected from (R)-(+)-5-(p-cyanophenyl)- 5,6,7,8-tetrahydroimida- GP zo[1,5-a]pyridine and a pharmaceutically acceptable salt thereof, and in particular to the phosphate salt of (R)-(+)-5-(p-cyanopheny Ir- 1)-5,6,7,8-tetrahydroimidazo[1,5-a]pyridine, both having preferably an enantiomeric excess of the (R) form higher than or equal to 0 ---. 97%. Furthermore, the present invention relates to pharmaceutical compositions comprising the same, their use as a medicament and in GC methods of treatment of diseases and disorders in humans including women of child bearing potential and pediatric patients in which 1-1 c;;;;) aldosterone over-exposure contributes to the deleterious effects of said diseases or disorders, as well as processes for preparing said ei inventive compounds. C