Patent SG-11201809856S-A (SG)
Title: Combination of pure 5-ht6 receptor antagonists with acetylcholinesterase inhibitors
Inventor: NIROGI RAMAKRISHNA
IPC: A61P25/28
Filed: 2016-08-03
Abstract: INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property -,' Organization 111111111111111111111111111111111111111111111111111111111111111011111111111110111111 International Bureau (10) International Publication Number (43) International Publication Date ...;;• WO 2017/199071 Al 23 November 2017 (23.11.2017) WIPO I PCT (51) International Patent Classification: Venkateswarlu; Serene Chambers, Road-5, Avenue — 7, A61K 31/31 (2006.01) A61P 25/28 (2006.01) Banjara Hills, Hyderabad,Telangana 500034 (IN). A61K 31/496 (2006.01) (74) Agent: KAPOOR, Divya et al.; Central Square, Suite-328, (21) International Application Number: Plaza III, 20 Manoharlal Khurana Marg, Bara Hindu Rao, PCT/IB2016/054673 (off Rani Jhansi Road), Delhi 110006 (IN). (22) International Filing Date: (81) Designated States (unless otherwise indicated, for every 03 August 2016 (03.08.2016) kind of national protection available): AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, BZ, (25) Filing Language: English CA, CH, CL, CN, CO, CR, CU, CZ, DE, DK, DM, DO, DZ, (26) Publication Language: English EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IR, IS, JP, KE, KG, KN, KP, KR, KZ, LA, (30) Priority Data: LC, LK, LR, LS, LU, LY, MA, MD, ME, MG, MK, MN, 201641017205 18 May 2016 (18.05.2016) IN MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PA, PE, (71) Applicant: SUVEN LIFE SCIENCES LIMITED PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, SC, SD, SE, [IN/IN]; Serene Chambers, Road-5, Avenue — 7, Banjara SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, TR, TT, TZ, Hills, Hyderabad,Telangana 500034 (IN). UA, UG, US, UZ, VC, VN, ZA, ZM, ZW. (72) Inventors: NIROGI, Ramakrishna; Serene Chambers, (84) Designated States (unless otherwise indicated, for every Road-5, Avenue — 7, Banjara Hills, Hyderabad,Telangana kind of regional protection available): ARIPO (BW, GH, _ 500034 (IN). SHINDE, Anil Karbhari; Serene Chambers, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, TZ, Road-5, Avenue — 7, Banjara Hills, Hyderabad,Telangana UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, RU, TJ, = 500034 (IN). JAYARAJAN, Pradeep; Serene Chambers, TM), European (AL, AT, BE, BG, CH, CY, CZ, DE, DK, Road-5, Avenue — 7, Banjara Hills, Hyderabad,Telangana EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, = 500034 (IN). BHYRAPUNENI, Gopinadh; Serene MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, SM, — Chambers, Road-5, Avenue — 7, Banjara Hills, TR), OAPI (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, = Hyderabad,Telangana 500034 (IN). KAMBHAMPATI, KM, ML, MR, NE, SN, TD, TG). Ramasastri; Serene Chambers, Road-5, Avenue — 7, Ban- _ jara Hills, Hyderabad,Telangana 500034 (IN). JASTI, = = (54) Title: COMBINATION = = = 25- = — c.7) 20- = ' ` = ..7.! 15- =— 0 y 1 = OF PURE Open column - Familiar Filled column ' - T 5-HT6 Nowl RECEPTOR ANTAGONISTS object object Figure la WITH ACETYLCHOLINESTERASE INHIBITORS -r- ••••••• _ — = - w — Vehicle Vehicle Compound 1 Compound 1 Compound 2 Compound 2 Compound 3 Compound 3 2 mr/kg, p.n. 2 mt./kg. p.n. 03 mg/kg. p.o. 0.3 mg/kg, p.o. 0.5 mg/kg, p.n. 0.5 mg/kg. p.o. 0.5 mg/kg, p.n. 0.5 mg/kg, p.o. 11 + 1- + + + Vehicle, Donepezil, Vehicle, Doncpzil, Vehicle, Doncpzil, Vehicle, Doncpzil, 1 mi/kg, i.p. 0.05 mg/kg. i.p. 1 14/ kg, i.p. 0.05 mg/kg, i.p. 1 mllkg. i.p. 0.05 mg/kg, i.p 1 mlikg, i.p. 0.05 mg/kg, ip. 11 Data represents Mean ± SEM of Exploration Time 0 01 **p<0.01Vs familiar object (Paired `t test). N=6-33 . 01 Il N .----- (57) : The present invention relates to pure 5-HT6 receptor antagonists, or the pharmaceutically acceptable salt(s) thereof in Il combination with or as adjunct to acetylcholinesterase inhibitors and their use in the treatment of cognitive disorders. The invention © further provides the pharmaceutical composition containing the said combination. ei C [Continued on next page] WO 2017/199071 Al MIDEDIMOMOIDEIROIDEMOMOHEIMONMOIllii0#011# 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))