Patent SG-11201900680P-A (SG)
Title: Triple combination of histamine-3 receptor inverse agonists, acetylcholinesterase inhibitors and nmda receptor antagonist
Inventor: NIROGI RAMAKRISHNA
IPC: A61P25/28
Filed: 2017-08-14
Abstract: WO 18/0338 48 Al (12) INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (43) International Publication Date 22 February 2018 (22.02.2018) WIPO I PCT IiiimmomitiaotiolooluinommommomovoimIE (10) International Publication Number WO 2018/033848 Al (51) International Patent Classification: A61K 45/06 (2006.01) A61K 31/5377 (2006.01) A61K 31/13 (2006.01) A61K 31/55 (2006.01) A61K 31/27 (2006.01) A61P 25/28 (2006.01) A61K 31/445 (2006.01) (21) International Application Number: PCT/IB2017/054939 (22) International Filing Date: 14 August 2017 (14.08.2017) (25) Filing Language: English (26) Publication Language: English (30) Priority Data: 201641028165 18 August 2016 (18.08.2016) IN (71) Applicant: SUVEN LIFE SCIENCES LIMITED [IN/IN]; Serene Chambers, Road-5, Avenue — 7, Banjara Hills, Hyderabad, Telangana 500034 (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, Telan- gana 500034 (IN). MOHAMMED, Abdul Rasheed; Su- ven Life Sciences Limited, Serene Chambers, Road-5, Av- enue — 7, Banjara Hills, Hyderabad, Telangana 500034 (IN). JAYARAJAN, Pradeep; Suven Life Sciences Limit- ed, Serene Chambers, Road-5, Avenue — 7, Banjara Hills, Hyderabad, Telangana 500034 (IN). BHYRAPUNENI, Gopinadh; Serene Chambers, Road-5, Avenue — 7, Ban- jara 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: MAHLA, Aaysu et al.; Subramaniam & Associates, Central Square, Suite-328, Plaza 20 Manoharlal III, Khu- rana 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, 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, (54) Title: TRIPLE COMBINATION OF HISTAMINE-3 RECEPTOR INVERSE AGONISTS, ACETYLCHOLINESTERASE IN- HIBITORS AND NMDA RECEPTOR ANTAGONIST (57) : The present invention relates to a combination of histamine-3 re- ceptor inverse agonist, acetylcholinesterase inhibitor and NMDA receptor antag- onist. Also, the present invention provides histamine-3 receptor (H 3 R) inverse agonist, or the 10 pharmaceutically acceptable salt(s) thereof in combination with or as adjunct to acetylcholinesterase inhibitor and N-Methyl-D-aspartate (NM- DA) receptor antagonist and their use in the treatment of cognitive disorders. The present invention further provides the pharmaceutical composition containing the said combination. Vehicle, Vehicle. Vehicle. _mU Done,. Menmeinc 03 mail. Iiminand 03 ..8n.i+m Dcran 0 n 1 Mementine 03 m0/4 4 , , D. Mean ± SEM of Exploration Time. .P<0.0.9, .. 9 9.-0.001 Vs vehicle (Students paired test) n 6-9 B) Data represents Meant SEM of discriminative index. .p<0.05 Vs Nubian (Kruskal-Wallis followed by Dunn 's Multiple Comparison Test) n = 6-9 [Continued on next page] Figure la A) la WO 2018/033848 Al MIDEDIMOMOIDEIREIDIONINOMMOIEHMEHOIMI 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(11)) Published: — with international search report (Art. 21(3))