Patent SG-11201908517X-A (SG)
Title: Pyrimidinyl-pyridyloxy-naphthyl compounds and methods of treating ire1-related diseases and disorders
Inventor: BRAUN MARIE-GABRIELLE
IPC: A61K31/506
Filed: 2018-03-16
Abstract: DISEASESAND DISORDERS cc kr) ,•\"% h N SD (R ), 0 1-1 O C RA N H R 7 1 (12) INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (43) International Publication Date 20 September 2018 (20.09.2018) WIPO I PCT oimitia °nolo OilIIIII0111IIIIIOH o imio oimIE (10) International Publication Number WO 2018/166528 Al (51) International Patent Classification: CO7D 403/04 (2006.01) A61K 31/445 (2006.01) CO7D 403/14 (2006.01) A61K 31/506 (2006.01) A61K 31/4545 (2006.01) A61P 35/00 (2006.01) (21) International Application Number: PCT/CN2018/079292 (22) International Filing Date: 16 March 2018 (16.03.2018) (25) Filing Language: English (26) Publication Language: English (30) Priority Data: PCT/CN2017/077059 17 March 2017 (17.03.2017) CN (71) Applicants: GENENTECH, INC. [US/US]; 1 DNA Way, South San Francisco, California 94080 (US). THE RE- GENTS OF THE UNIVERSITY OF CALIFORNIA [US/US]; 1111 Franklin Street, Twelfth Floor, Oakland, California 94607 (US). = (72) Inventors; and (71) Applicants (for MN only): BRAUN, Marie-Gabrielle [FR/US]; 1 DNA Way, South San Francisco, California 94080 (US). GIBBONS, Paul [US/US]; 1 DNA Way, South San Francisco, California 94080 (US). LEE, Wendy [US/US]; 1 DNA Way, South San Francisco, California 94080 (US). LY, Cuong [US/US]; 1 DNA Way, South San Francisco, California 94080 (US). RUDOLPH, Joachim [DE/US]; 1 DNA Way, South San Francisco, California 94080 (US). SCHWARZ, Jacob [US/US]; 1 DNA Way, South San Francisco, California 94080 (US). ASHKE- NAZI, Avi [US/US]; 1 DNA Way, South San Francisco, California 94080 (US). FU, Leo [CN/CN]; 288 Fute Zhong Road, Waigaoqiao Free Trade Zone, Shanghai 200131 (CN). LAI, Tommy [CN/CN]; 288 Fute Zhong Road, Waigaoqiao Free Trade Zone, Shanghai 200131 (CN). WANG, Fei [CN/CN]; 288 Fute Zhong Road, Waigaoqiao Free Trade Zone, Shanghai 200131 (CN). BEVERIDGE, Ramsay [CA/CA]; 2525 Avenue Marie-Curie, Montreal, Quebec H4S 2E1 (CA). ZHAO, Liang [CA/CA]; 2525 Av- enue Marie-Curie, Montreal, Quebec H4S 2E1 (CA). (74) Agent: WU, FENG & ZHANG; 3 FL, Building 2, Yard 3, Fengxiuzhonglu Road, Haidian District, Beijing 100094 (CN). (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)) (54) Title: PYRIMIDINYL-PYRIDYLOXY-NAPHTHYL COMPOUNDS AND METHODS OF TREATING IRE1-RELATED (57) : Described herein are pyrimidinyl-pyridyloxy-naphthyl compounds with inositol requiring enzyme 1 (IRE1) modulation activity or function having the Formu- la (I) or (I') structure : or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, and with the substituents and structural features described herein. Also described are pharmaceutical compositions and medicaments that include the Formula (I) or (I') compounds, as well as methods of using such IRE1 modulators, alone and in combina- tion with other therapeutic agents, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.