Patent SG-11201907546W-A (SG)
Title: Pyrazole derivatives as bromodomain inhibitors
Inventor: ATKINSON STEPHEN JOHN
IPC: C07D471/04
Filed: 2018-02-27
Abstract: Filing Language: (26) Publication Language: (30) Priority Data: 1703283.0 1716374.2 27 February 2018 (27.02.2018) English English 01 March 2017 (01.03.2017) GB 06 October 2017 (06.10.2017) GB (12) INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (43) International Publication Date 07 September 2018 (07.09.2018) WIPO I PCT onion °nolo HE VIII in oimIE (10) International Publication Number WO 2018/158212 Al (51) International Patent Classification: C07D 231/14 (2006.01) C07D 405/12 (2006.01) C07D 403/12 (2006.01) C07D 413/12 (2006.01) C07D 401/14 (2006.01) C07D 417/12 (2006.01) C07D 405/14 (2006.01) C07D 471/04 (2006.01) C07D 401/12 (2006.01) A61K 31/415 (2006.01) C07D 403/14 (2006.01) A61K 31/4155 (2006.01) (21) International Application Number: PCT/EP2018/054733 (22) International Filing Date: (71) Applicant: GLAXOSMITHKLINE INTELLECTUAL PROPERTY (NO.2) LIMITED [GB/GB]; 980 Great West Road, Brentford Middlesex TW8 9GS (GB). (72) Inventors: ATKINSON, Stephen John; GlaxoSmithK- line, Gunnels Wood Road, Stevenage Hertfordshire SG1 2NY (GB). DEMONT, Emmanuel Hubert; Glax- oSmithKline, Gunnels Wood Road, Stevenage Hertford- shire SG1 2NY (GB). HARRISON, Lee Andrew; Glax- oSmithKline, Gunnels Wood Road, Stevenage Hertford- shire SG1 2NY (GB). LIWICKI, Gemma Michele; GlaxoSmithKline, Gunnels Wood Road, Stevenage Hert- fordshire SG1 2NY (GB). LUCAS, Simon Christopher Cranko; GlaxoSmithKline, Gunnels Wood Road, Steve- nage Hertfordshire SG1 2NY (GB). PRESTON, Alexan- der G; GlaxoSmithKline, Gunnels Wood Road, Steve- nage Hertfordshire SG1 2NY (GB). SEAL, Jonathan, Thomas; GlaxoSmithKline, Gunnels Wood Road, Steve- nage Hertfordshire SG1 2NY (GB). WALL, Ian David; GlaxoSmithKline, Gunnels Wood Road, Stevenage Hert- fordshire SG1 2NY (GB). WATSON, Robert J; Glax- oSmithKline, Gunnels Wood Road, Stevenage Hertford- shire SG1 2NY (GB). (74) Agent: SHORE, Andrew David; GlaxoSmithKline, Glob- al Patents (CN925.1), 980 Great West Road, Brentford Mid- dlesex TW8 9GS (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, N CA, CH, CL, CN, CO, CR, CU, CZ, DE, DJ, DK, DM, DO, 1-1 DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, co 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, 1-1 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 applicant's entitlement to apply for and be granted a patent (Rule 4.17(ii)) 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)) O (57) : The present invention is directed to pyrazole derivatives, pharmaceutical compositions comprising the compounds and 0 the use of the compounds or the compositions in the treatment of various diseases (54) Title: PYRAZOLE DERIVATIVES AS BROMODOMAIN INHIBITORS