Patent SG-11201809792T-A (SG)
Title: Treatment of neurological disorders
Inventor: RAGEOT DENISE
IPC: A61P25/28
Filed: 2017-05-17
Abstract: INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property 11111111111111111111101011111111111 01110111111111111100111111101111111111110111111 Organization International Bureau (10) International Publication Number (43) International Publication Date .....0\"\" WO 2017/198346 Al 23 November 2017 (23.11.2017) WIPO I PCT (51) International Patent Classification: 8102 Oberengstringen (CH). NGUYEN, Hoa Huu Phuc; A61K 31/5377 (2006.01) A61P 25/08 (2006.01) Ursrainer Ring 39, 72076 Tiibingen (DE). LOSCHER, A61K 31/5386 (2006.01) A61P 25/28 (2006.01) Wolfgang; Kaulbachstrasse 5a, 30625 Hannover (DE). A61K 31/541 (2006.01) BRANDT, Claudia; Vor den Kampen 24, 30851 Langen- (21) International Application Number: hagen (DE). SELE, Alexander, Markus; Amerbachstrasse 86, 4057 Basel (CH). PCT/EP2017/025136 (22) International Filing Date: (74) Agent: SPERRLE, Martin; Latscha Schollhorn Partner 17 May 2017 (17.05.2017) AG, Austrasse 24, CH-4051 Basel (CH). (25) Filing Language: English (81) Designated States (unless otherwise indicated, for every kind of national protection available): AE, AG, AL, AM, (26) Publication Language: English AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, BZ, (30) Priority Data: CA, CH, CL, CN, CO, CR, CU, CZ, DE, DJ, DK, DM, DO, 16170107.3 18 May 2016 (18.05.2016) EP DZ, EC, EE, EG, ES, FL GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IR, IS, JP, KE, KG, KH, KN, KP, KR, (71) Applicants: PIQUR THERAPEUTICS AG [CH/CH]; KW, KZ, LA, LC, LK, LR, LS, LU, LY, MA, MD, ME, MG, Hochbergerstrasse 60C, CH-4057 Basel (CH). UNIVERSI- MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, TAT BASEL [CH/CH]; Vizerektorat Forschung, Peters- PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, SC, graben 35, CH-4003 Basel (CH). 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. (72) Inventors: RAGEOT, Denise; 18 Rue de la Tuilerie, 68300 Saint-Louis (CH). HEBEISEN, Paul; St. Al- (84) Designated States (unless otherwise indicated, for every banring 184, CH-4052 Basel (CH). BEAUFILS, Flo- kind of regional protection available): ARIPO (BW, GH, rent; 28 Rue des Ecureuils, F-68870 Bartenheim (FR). GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, TZ, FABBRO, Doriano; Im Lee 54, CH-4144 Arleshiem UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, RU, TJ, (CH). HILLMANN-WULLNER, Petra; Dorfstrasse 49b, TM), European (AL, AT, BE, BG, CH, CY, CZ, DE, DK, = =_ Title: TREATMENT OF NEUROLOGICAL DISORDERS (54) = = R 2 = F ..,..,„- R3 ro R4 = .--,..-- - -:• Y N ) R t = _ + (H) N NH2 = (I) = A A . = = = = : The present invention is relates to a compound of formula (I), wherein X 1 , X 2 andX 3 are, independently of each other, or CH; with the proviso that at least two of X 1 X 2 andX 3 areN; Y is N or CH; R 1 and R 2 are independently of each other (iii)a of formula (II) wherein the arrow denotes the bond in formula (I); and wherein R and R are independently of each other 3 4 (57) — morpholinyl N - H, C1-C3alkyl optionally substituted with one or two OH, C1-C2fhioroalkyl, C1-C2alkoxy, C1-C2alkoxyCi-C3alkyl, CN, or C(0)0-C1- C2alkyl; or R3 and R4 form together a bivalent residue -R5R6- selected from Ci-C3alkylene optionally substituted with 1 to 4 F, -CH2-0- Z CH2-, -CH2-NH-CH2-, or any of the structures wherein the arrows denote the bonds in formula (II); or (iv) a saturated 6-membered 71' en heterocyclic ring Z selected from thiomorpholinyl and piperazinyl, optionally substituted by 1 to 3 R 7 ; wherein R7 is independently at c)1 : each occurrence Ci-C3alkyl optionally substituted with one or two OH, C 1 -C 2 fluoroalkyl, C - C2alkoxyC 1 l -C 3 alkyl, C -C 3 6 cycloalkyl; 01 Il or two R 7 substituents form together a bivalent residue -R 8 R 9 - selected from C1-C3alkylene optionally substituted with 1 to 4 F, -CH2-0- IN CH2- or -0- CH2CH2-0-; with the proviso that at least one of R 1 and R 2 is a morpholinyl of formula II; and prodrugs, metabolites, 1-1 © tautomers, solvates and pharmaceutically acceptable salts thereof, for use in the prevention or treatment of a neurological disorder in N a subject. o [Continued on next page] WO 2017/198346 Al MIDEDIMOMOIDEIROIDEMOMMUNDOMEOMEMOIMIE 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 patent (Rule 4.17(H)) for and be granted a Published: — with international search report (Art. 21(3))