Patent SG-11201809726U-A (SG)
Title: Triple combination of pure 5-ht6 receptor antagonists, acetylcholinesterase inhibitors and nmda receptor antagonist
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 International Bureau (43) International Publication Date 23 November 2017 (23.11.2017) WIPO PCT Hu omit VIII Hot 0 VIII 110 110111111 oimIE (10) International Publication Number WO 2017/199070 Al (51) International Patent Classification: A61K 31/13 (2006.01) A61K 31/496 (2006.01) A61K 31/445 (2006.01) A61P 25/28 (2006.01) (21) International Application Number: PCT/IB2016/054672 (22) International Filing Date: 03 August 2016 (03.08.2016) (25) Filing Language: English (26) Publication Language: English (30) Priority Data: 201641017204 18 May 2016 (18.05.2016) IN (71) Applicant: SUVEN LIFE SCIENCES LIMITED [IN/IN]; Serene Chambers, Road - 5, Avenue — 7, Banjara Hills, Hyderabad,Telangana 500 034 (IN). (72) Inventors: NIROGI, Ramakrishna; Suven Life Sciences Limited,Serene Chambers, Road-5, Avenue — 7, Banjara Hills, Hyderabad, Telangana 500034 (IN). SHINDE, Anil Karbhari; Suven Life Sciences Limited,Serene Cham- bers, Road-5, Avenue — 7, Banjara Hills, Hyderabad, Telangana, 500034 (IN). JAYARAJAN, Pradeep; Su- ven Life Sciences Limited,Serene Chambers, Road-5, Av- enue — 7, Banjara Hills, Hyderabad, Telangana 500034 (IN). BHYRAPUNENI, Gopinadh; Suven Life Sciences Limited,Serene Chambers, Road-5, Avenue — 7, Banjara Hills, Hyderabad, Telangana 500034 (IN). KAMBHAM- PATI, Ramasastri; Suven Life Sciences Limited,Serene Chambers, Road-5, Avenue — 7, Banjara Hills, Hyderabad, Telangana 500034 (IN). JASTI, Venkateswarlu; Suven Life Sciences Limited,Serene Chambers, Road-5, Avenue — 7, Banjara Hills, Hyderabad, Telangana 500034 (IN). (74) Agent: GANDHI, Ritu et al.; Central Square, Suite-328, Plaza III, 20 Manoharlal Khurana Marg, Bara Hindu Rao, (off Rani Jhansi Road), Delhi 110006 (IN). (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, DK, DM, DO, DZ, 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, LC, LK, LR, LS, LU, LY, MA, MD, ME, MG, MK, MN, (54) Title: TRIPLE COMBINATION OF PURE 5-HT6 RECEPTOR ANTAGONISTS, ACETYLCHOLINESTERASE INHIBITORS = AND NMDA RECEPTOR ANTAGONIST Figure la 0.7— 7, 0.6- o ' OA Vehicle, Vehicle, Compound I 2 mL/kg,p.o. 2 naL/kg,p.o. 1 mg/kg, p.o. Vehicle, Donepezil Donepezil 1 mL/kg, s.e. 0.3 mg/kg, s.c. 0.3 mg/kg, s.c. Vehicle, Memantine Memantine 1 mL/kg, i.p. 0.3 mg/kg. i.p. 0.3 mg/kg, i.p. 1-1 O N O 1-1 N 1-1 O C Data represents Mean ± SEM of discriminative index. *p<0.05 Vs vehicle (Kruskal-Wallis followed by Dunn's Multiple Comparison Test) N=11-12 (57) : The present invention relates to a combination of pure 5-HT6 receptor antagonist, acetylcholinesterase inhibitor and NMDA receptor antagonist. Also, the present invention provides pure 5-HT6 receptor (5-HT6R) antagonists, or the pharmaceutically acceptable salt(s) thereof in combination with or as adjunct to acetylcholinesterase inhibitor and N- Methyl-D-aspartate (NMDA) receptor antagonist and their use in the treatment of cognitive disorders. The present invention further provides the pharmaceutical composition containing the said combination. [Continued on next page] WO 2017/199070 Al MIDEDIMOMOIDEIROIDEMOMOHEIMONEIHMEMOIMIE 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 applicant's entitlement to apply for and be granted a patent (Rule 4.17(H)) Published: — with international search report (Art. 21(3))