Patent SG-11201907544V-A (SG)
Title: Jak inhibitors containing a 4-membered heterocyclic amide
Inventor: FATHEREE PAUL R
IPC: A61P11/00
Filed: 2018-03-08
Abstract: Title: JAK INHIBITORS CONTAINING A 4-MEMBERED HETEROCYCLIC AMIDE (57) : The invention provides compounds of formula (I): which contain a 4-membered heterocyclic amide, where the variables are defined in the specifica- HO tion, or a pharmaceutically-acceptable salt thereof, that are useful as JAK kinase in- hibitors. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat respiratory diseases, and (1) processes and intermediates useful for preparing such compounds. N 00 C HN-N (12) INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (43) International Publication Date 13 September 2018 (13.09.2018) WIP0 I PCT omit IIl °nolo oimIE (10) International Publication Number WO 2018/165392 Al (51) International Patent Classification: CO7D 471/04 (2006.01) A61K 31/437 (2006.01) A61P 11/00 (2006.01) A61K 31/397 (2006.01) (21) International Application Number: PCT/US2018/021489 (22) International Filing Date: 08 March 2018 (08.03.2018) (25) Filing Language: English (26) Publication Language: English (30) Priority Data: 62/469,073 09 March 2017 (09.03.2017) US (71) Applicant: THERAVANCE BIOPHARMA R&D IP, LLC [US/US]; 901 Gateway Boulevard, South San Fran- cisco, California 94080 (US). (72) Inventors: FATHEREE, Paul R.; 921 Minnesota Street, San Francisco, California 94107 (US). BRANDT, Gary E.L.; 2160 Buena Vista Avenue, Alameda, California 94501 (US). SMITH, Cameron; 4256 Shelter Creek Lane, San Bruno, California 94066 (US). SULLIVAN, Steven D.E.; 1417 17th Avenue, San Francisco, California 94122 (US). VAN ORDEN, Lori Jean; 362 ParkStreet, San Fran- cisco, California 94110 (US). KLEINSCHEK, Melanie A.; 30 Elizabeth Street, San Francisco, California 94110 (US). CRATER, Glenn D.; 7108 Rippling Stone Ln, Raleigh, North Carolina 27612 (US). (74) Agent: HAGENAH, Jeffrey A. et al.; THERAVANCE, INC., 901 Gateway Boulevard, South San Francisco, Cali- fornia 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, 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). Published: — with international search report (Art. 21(3))