Patent SG-11201803489S-A (SG)
Title: 4-(biphen-3-yl)-1h-pyrazolo[3,4-c]pyridazine derivatives of formula (i) as gaba receptor modulators for use in the treatment of epilepsy and pain
Inventor: OWEN ROBERT MCKENZIE
IPC: C07D487/04
Filed: 2016-11-22
Abstract: INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (43) International Publication Date 15 June 2017 (15.06.2017) WIPOIPCT (10) International Publication Number WO 2017/098367 A1 (51) International Patent Classification: C07D 487/04 (2006.01) A61P 25/00 (2006.01) A61K31/5025 (2006.01) (21) International Application Number: PCT/IB2016/05 7049 (22) International Filing Date: (25) Filing Language: (26) Publication Language 22 November 2016 (22.11.2016) English English (30) Priority Data: 62/265,572 10 December 2015 (10.12.2015) US (71) Applicant: PFIZER LIMITED [GB/GB]; 748 Ramsgate Road, Sandwich Kent CT13 9NJ (GB). (72) Inventors: OWEN, Robert McKenzie; c/o Neusentis, Portway Building, Granta Park, Great Abington Cambridge CB21 6GS (GB). PRYDE, David Cameron; c/o Neusentis, Portway Building, Granta Park, Great Abington Cambridge CB21 6GS (GB). DACK, Kevin Neil; c/o Pf­ izer Limited, Ramsgate Road, Sandwich Kent CT13 9NJ (GB). (74) Agent: LANE, Graham M .; Pfizer Limited, 748 Ramsgate Road, Sandwich Kent CT13 9NJ (GB). (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, JP, KE, KG, 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. (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 the identity of the inventor (Rule 4.17(i)) as to applicant's entitlement to apply for and be granted a patent (Rule 4.17(H)) as to the applicant's entitlement to claim the priority of the earlier application (Rule 4.17(iii)) Published: with international search report (Art. 21(3)) < 00 ON n O (54) Title: 4-(BIPHEN-3-YL)-lH-PYRAZOLO[3,4-C]PYRIDAZINE DERIVATIVES OF FORMULA (I) AS GABA RECEPTOR MODULATORS FOR USE IN THE TREATMENT OF EPILEPSY AND PAIN R (I) (57) : The present invention relates to pyrazolopyridazine derivatives. More particularly, it relates to 4-(biphenyl-3-yl)-lH- pyrazolo[3,4-c]pyridazine derivatives of formula (I), and pharmaceutically acceptable salts thereof, wherein X, R1, R2, R3, R4 and R5 are as defined in the description. The pyrazolopyridazine derivatives of the present invention modulate the activity of the GABAA re­ ceptor. They may useful in the treatment of a number of conditions, including pain and epilepsy.