Patent SG-11201906222W-A (SG)
Title: Jak1 selective inhibitors
Inventor: NILSSON KARL
IPC: A61P17/14
Filed: 2018-01-16
Abstract: pn s p<1.01 p.9.01 p.9.001 7% 68% 61% 97% 2 (12) INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (43) International Publication Date 26 July 2018 (26.07.2018) WIPO I PCT omit VIII °nolo o1111 111 OH min mom ow (10) International Publication Number WO 2018/134213 Al (51) International Patent Classification: CO7D 403/04 (2006.01) A61P 17/14 (2006.01) CO7D 403/14 (2006.01) A61P 37/00 (2006.01) A61K 31/506 (2006.01) (21) International Application Number: PCT/EP2018/051038 (22) International Filing Date: 16 January 2018 (16.01.2018) (25) Filing Language: English (26) Publication Language: English (30) Priority Data: 62/447,057 17 January 2017 (17.01.2017) US (71) Applicant: ASTRAZENECA AB [SE/SE]; 151 85 Sodertalje (SE). (72) Inventors: NILSSON, Karl, Magnus; AstraZeneca, 431 83 Molndal (SE). ASTRAND, Annika, Birgitta, Mar- gareta; AstraZeneca, 431 83 Molndal (SE). BERGGREN, Anna, Ingrid, Kristina; AstraZeneca, 431 83 Molndal (SE). JOHANSSON, Johan, R.; AstraZeneca, 431 83 Mol- ndal (SE). LEPISTO, Matti, Juhani; AstraZeneca, 431 83 Molndal (SE). KAWATKAR, Sameer, Pralhad; As- trazeneca Pharmaceuticals LP, 1800 Concord Pike, Wilm- ington, DE 19803 (US). SU, Qibin; Astrazeneca Pharma- ceuticals LP, 1800 Concord Pike, Wilmington, DE 19803 (US). KETTLE, Jason, Grant; 1 Francis Crick Avenue, Cambridge Biomedical Campus, Cambridge CB2 OAA (GB). (74) Agent: ASTRAZENECA; Milstein Building Granta Park, Cambridge Cambridgeshire CB21 6GH (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, (54) Title: JAK1 SELECTIVE INHIBITORS Eosinophils in BAL 4 (57) : Disclosed herein are compounds of Formula (I), and pharmaceutically acceptable salts thereof, wherein R-Rg have any 1 of the meanings defined herein. Also disclosed are pharmaceutical compositions comprising compounds of Formula (I) and methods of using the same. Group 1 Group 2 Group 3 Group 4 Group 5 Group 6 Group Group 8 .08µg/ g 0.11,41kg 0.6µg/kg 4.8µg/k Budesonide 300µg/kg )(2 FIG. 3 W O 20 18/ 13 4213 Al (1) [Continued on next page] WO 2018/134213 Al MIDEDIMOMOIDEIREIO I II III 0111 VIII VIII VIII 0111 DOMEHOIMIE 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(11)) Published: — with international search report (Art. 21(3))