A SUBSTITUTED BENZIMIDAZOLE DERIVATIVE AS A MODULATOR OF TNF ACTIVITY

• Main Author: HEER, Jag Paul
• Format: Patent
• Language: English
• Published: 30.05.2019
• Subjects: CHEMISTRY; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

OO C (12) INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (43) International Publication Date 14 June 2018 (14.06.2018) WIPO I PCT omit VIII °nolo tommoillimiflo oimIE (10) International Publication Number WO 2018/104534 Al (51) International Patent Classification: CO7D 403/04 (2006.01) A61P 29/00 (2006.01) A61P 3/00 (2006.01) A61P 35/00 (2006.01) A61P 37/08 (2006.01) A61P 37/00 (2006.01) A61P 9/00 (2006.01) A61K 31/506 (2006.01) A61P 25/28 (2006.01) (21) International Application Number: PCT/EP2017/082092 (22) International Filing Date: 08 December 2017 (08.12.2017) (25) Filing Language: English (26) Publication Language: English (30) Priority Data: 1620948.8 09 December 2016 (09.12.2016) GB (71) Applicant: UCB BIOPHARMA SPRL [BE/BE]; Allee de la Recherche 60, B-1070 Brussels (BE). (72) Inventor: HEER, Jag Paul; c/o IPD, UCB Celltech, 208 Bath Road, Slough Berkshire SL1 3WE (GB). (74) Agent: J A KEMP; 14 South Square, Gray's Inn, London Greater London WC1R 5JJ (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, 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. (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: of inventorship (Rule 4.17(iv)) Published: - with international search report (Art. 21(3)) (54) Title: A SUBSTITUTED BENZIMIDAZOLE DERIVATIVE AS A MODULATOR OF TNF ACTIVITY (57) : 2-(5- {142-(Difluoromethoxy)-6-fluorobenzy1]-2-methyl-1H-benzimidazol-6- yl pyrimidin-2-yl)propan-2-ol, or a pharmaceutically acceptable salt thereof, being potent modulators of human TNF activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including autoimmune and inflammatory disorders; neurological and neurodegenerative disorders; pain and nociceptive disorders; cardiovascular disorders; metabolic disorders; ocular disorders; and oncological disorders.