Patent SG-11201901954X-A (SG)
Title: 8-(azetidin-1-yl)-[1,2,4]triazolo[1,5-a]pyridinyl compounds, compositions and methods of use thereof
Inventor: GOODACRE SIMON CHARLES
IPC: C07D471/04
Filed: 2017-09-02
Abstract: INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property 111111411 01E101011M 3E1 0 011101 IMI 100 11101101110 11110 1111 OEN Organization International Bureau (10) International Publication Number (43) International Publication Date ......0\" WO 2018/046409 Al 15 March 2018 (15.03.2018) WIP0 I PCT (51) International Patent Classification: OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, CO7D 471/04 (2006.01) A61P 29/00 (2006.01) SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, A61K 31/437 (2006.01) TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW. (21) International Application Number: (84) Designated States (unless otherwise indicated, for every PCT/EP2017/072034 kind of regional protection available): ARIPO (BW, GH, (22) International Filing Date: GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, TZ, 02 September 2017 (02.09.2017) UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, RU, TJ, TM), European (AL, AT, BE, BG, CH, CY, CZ, DE, DK, (25) Filing Language: English EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, (26) Publication Language: English 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, (30) Priority Data: KM, ML, MR, NE, SN, TD, TG). PCT/CN2016/098215 06 September 2016 (06.09.2016) CN Declarations under Rule 4.17: — as to applicant's entitlement to apply for and be granted a (71) Applicant (for all designated States except US): F. HOFF- patent (Rule 4.17(ii)) MANN-LA ROCHE AG [CH/CH]; Grenzacherstrasse — as to the applicant's entitlement to claim the priority of the 124, 4070 Basel (CH). earlier application (Rule 4.17(iii)) (71) Applicant (for US only): GENENTECH, INC. [US/US]; — of inventorship (Rule 4.17(iv)) — 1 DNA Way, South San Francisco, California 94080 (US). Published: (72) Inventors: GOODACRE, Simon Charles; 8/9 Spire — with international search report (Art. 21(3)) = Green Centre, Flex Meadow, Harlow Essex CM195TR = (GB). ZAK, Mark; c/o Genentech, Inc., 1 DNA Way, South _ San Francisco, California 94080 (US). ROMERO, F. An- thony; Genentech, Inc., 1 DNA Way, South San Fran- = c/o cisco, California 94080 (US). CHENG, Yun-Xing; 6 Tai- _ he Road, BDA, Beijing 100176 (CN). CHENG, Limin; 6 = Tai-he Road, BDA, Beijing 100176 (CN). HUA, Rongbao; = = 6 Tai-he Road, BDA, Beijing 100176 (CN). (74) Agent: SCHIRLIN, Julien; Grenzacherstrasse 124, 4070 = Basel (CH). (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, = (54) Title: 8-(AZETIDIN-1-YL)41,2,4]TRIAZOLO[1,5-A]PYRIDINYL COMPOUNDS, COMPOSITIONS AND METHODS OF USE THEREOF Il R5 R5 4 C:r N 'N ''' R4 H N \" \"L-....-. 0 © 0 N N 1 1' N 3 RA N 0 N ---- 3 R 1 \" N 1 1' n R ic © ---.... N NC C Rz Il R 6 (1) R 6 (II) 0 N C (57) : Compounds of Formuula (I) and (II), or a stereoisomer, tautomer, solvate, prodrug or salt thereof, and methods of use as Janus kinase inhibitors are described herein.