Patent SG-11201809342Y-A (SG)
Title: Pyrimidine compounds as jak kinase inhibitors
Inventor: HUDSON RYAN
IPC: C07D451/14
Filed: 2017-04-27
Abstract: INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property 111111101111 0 DOI 010111110101111 0 111 01111101111111010111011111110 HOE lil Organization International Bureau (10) International Publication Number (43) International Publication Date .....0\"\"\" WO 2017/189822 Al 02 November 2017 (02.11.2017) W I PO I PCT (51) International Patent Classification: SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, TR, C07D 451/14 (2006.01) A61K 31/506 (2006.01) TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW. C07D 451/04 (2006.01) (84) Designated States (unless otherwise indicated, for every (21) International Application Number: kind of regional protection available): ARIPO (BW, GH, PCT/US2017/029796 GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, TZ, (22) International Filing Date: UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, RU, TJ, 27 April 2017 (27.04.2017) 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, (25) Filing Language: English MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, SM, (26) Publication Language: English TR), OAPI (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, KM, ML, MR, NE, SN, TD, TG). (30) Priority Data: 62/328,737 28 April 2016 (28.04.2016) US Published: (71) — Applicant: THERAVANCE BIOPHARMA R&D IP, with international search report (Art. 21(3)) LLC [US/US]; 901 Gateway Boulevard, South San Fran- cisco, California 94080 (US). (72) Inventors: HUDSON, Ryan; 1454 Walbrook Drive, San Jose, California 95129 (US). KOZAK, Jennifer; 771 _ Prairie Creek Drive, Pacifica, California 94044 (US). FLEURY, Melissa; 47D Joy Avenue, Brisbane, California — 94005 (US). FATHEREE, Paul R.; 921 Minnesota Street, San Francisco, California 94107 (US). BEAUSOLEIL, Anne-Marie; 600 Brewster Avenue, Apt. 306, Redwood = =_ City, California 94063 (US). PODESTO, Dante D.; 1122 = Trinity Avenue, Modesto, California 95350 (US). HUANG, Xiaojun; 513 Granger Terrace, Sunnyvale, California 94087 (US). = (74) Agent: HAGENAH, Jeffrey A. et al.; THERAVANCE BIOPHARMA US, INC., 901 Gateway Boulevard, South = — _ San Francisco, California 94080 (US). (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, 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, = = (54) Title: PYRIMIDINE COMPOUNDS AS JAK KINASE INHIBITORS _ 1-1 (57) : The invention provides compounds of formula (I): wherein the variables are defined HO R1 in the specification, or a pharmaceutically-acceptable salt thereof,that are inhibitors of JAK kinases. I .4 HN N fl The invention also provides pharmaceutical compositions comprising such compounds, methods of ei ei N , , \ using such compounds to treat gastrointestinal and other inflammatory diseases, and processes and intermediates useful for preparing such compounds. GC 01 HN,_ ; ,,N., N, R 2 GC 1 i 11 • --).„ N 0 O