Patent SG-11201900681S-A (SG)
Title: Combination of histamine-3 receptor inverse agonists with acetylcholinesterase inhibitors
Inventor: NIROGI RAMAKRISHNA
IPC: A61P25/28
Filed: 2017-08-14
Abstract: Compound0.5 mg/kg, p. o. Vehicle 2 mL/kg, s.c. Vehicle 2 mL/kg, p. o. Donepezil 0.5mg/kg, s. e. Compound 1 0.5 mg/kg, p. o. Donepezil 0.5 mg/kg, s.c Vehicle 2 mL/kg, p. o. Vehicle 2 mL/kg, s.c. Open Column-Familiar Closed Column-Novel object 5' (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 °mons °nolo oluinommomommo oimIE (10) International Publication Number WO 2018/033847 Al (51) International Patent Classification: A61K 31/27 (2006.01) A61K 31/55 (2006.01) A61K 31/445 (2006.01) A61P 25/28 (2006.01) A61K 31/5377 (2006.01) (21) International Application Number: PCT/IB2017/054938 (22) International Filing Date: 14 August 2017 (14.08.2017) (25) Filing Language: English (26) Publication Language: English (30) Priority Data: 201641028166 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; Suven Life Sciences Limited, Serene Cham- bers, Road-5, Avenue — 7, Banjara Hills, Hyderabad, Telan- gana 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.; Subramaniam & Associates, Central Square, Suite-328, Plaza III, 20 Manoharlal 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, 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. (54) Title: COMBINATION OF HISTAMINE-3 RECEPTOR INVERSE AGONISTS WITH ACETYLCHOLINESTERASE INHIBI- TORS Figure la: Data represents Mean ± SEM of Exploration Time (*p<0.05 Vs familiar object, Students 71' paired `t' test), n=8-10. 00 O (57) : The present invention relates to the combination of histamine-3 receptor inverse agonist and acetylcholinesterase in- hibitor. Also, the present invention provides histamine-3 receptor (HR) inverse agonist, or the pharmaceutically acceptable salt(s) 3 © thereof in combination with or as adjunct to acetylcholinesterase inhibitor and their use in the treatment of cognitive disorders. The C present invention further provides the pharmaceutical composition containing the said combination. [Continued on next page] WO 2018/033847 Al MIDEDIMOMMIDIRENHEIHOMMOHOHnin (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(ii)) Published: — with international search report (Art. 21(3))