Patent SG-11201901817S-A (SG)
Title: Blood-brain barrier-penetrant dopamine-b-hydroxylase inhibitors
Inventor: SOARES DA SILVA PATRÍCIO
IPC: A61P25/00
Filed: 2017-09-22
Abstract: WO 18/05 685 4 Al (12) INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (43) International Publication Date 29 March 2018 (29.03.2018) WIP0 I PCT omit VIII °nolo III m Kum H 100 Immo oimIE (10) International Publication Number WO 2018/056854 Al (51) International Patent Classification: A61K 31/40 (2006.01) A61K 31/4196 (2006.01) A61K 31/4025 (2006.01) A61K 31/451 (2006.01) A61K 31/403 (2006.01) A61P 25/00 (2006.01) A61K 31/4188 (2006.01) (21) International Application Number: PCT/PT2017/050022 (22) International Filing Date: 22 September 2017 (22.09.2017) (25) Filing Language: English (26) Publication Language: English (30) Priority Data: 1616201.8 23 September 2016 (23.09.2016) GB 1713779.5 29 August 2017 (29.08.2017) GB (71) Applicant: BIAL - PORTELA & Ca, S.A. [PT/PT]; A Av. da Siderurgia Nacional, 4745-457 S. Mamede do Coronado (PT). (72) Inventors: SOARES DA SILVA, Patricio; A Av. da Siderurgia Nacional, 4745-457 S. Mamede do Coronado (PT). ROSSI, Tino; A Av. da Siderurgia Nacional, S. Mamede do Coronado 4745-457 (PT). KISS, Laszlo Er- no; A Av. da Siderurgia Nacional, 4745-457 S. Mamede do Coronado (PT). BELIAEV, Alexander; A Av. da Siderur- gia Nacional, 4745-457 S. Mamede do Coronado (PT). LEAL PALMA, Pedro Nuno; A Av. da Siderurgia Na- cional, 4745-457 S. Mamede do Coronado (PT). (74) Agent: ALVES MOREIRA, Pedro; Rua do Patrocinio N.° 94, 1399-019 Lisboa (PT). (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 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: BLOOD-BRAIN BARRIER-PENETRANT DOPAMINE-B-HYDROXYLASE INHIBITORS (57) : This invention relates to: (a) compounds of formula (I) (with R 1 to R5, n and A as defined herein) and pharmaceutically acceptable salts or solvates thereof that are useful as dopamine-13-hydroxylase inhibitors; (b) pharmaceutical compositions comprising such compounds, salts or solvates; (c) the use of such compounds, salts or solvates in therapy; (d) therapeutic methods of treatment using such compounds, salts or solvates; and (e) processes and intermediates useful for the synthesis of such compounds.