abstract |
International Patent Classification: C07D 403/12 (2006.01) C07D 413/14 (2006.01) C07D 413/12 (2006.01) C07D 417/12 (2006.01) C07D 471/04 (2006.01) C07D 261/18 (2006.01) C07D 487/04 (2006.01) C07D 491/048 (2006.01) CO7D 495/04 (2006.01) CO7D 498/04 (2006.01) CO7D 498/14 (2006.01) CO7D 513/04 (2006.01) (12) INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (43) International Publication Date 10 August 2017 (10.08.2017) WIPO I PCT (10) International Publication Number WO 2017/136727 A3 111111111111110111011111111111010111110 01110111100111110101111111111111110111111 CENTE FIDALGO, Javier; c/o Denali Therapeutics Inc., 151 Oyster Point Blvd., 2nd Floor, South San Francisco, California 94080 (US). (74) Agents: TANNER, Lorna L. et al.; Sheppard Mullin Richter & Hampton LLP, 379 Lytton Avenue, Palo Alto, California 94301-1479 (US). (21) International Application Number: PCT/US2017/016509 (22) International Filing Date: 3 February 2017 (03.02.2017) (25) Filing Language: English (26) Publication Language: English (30) Priority Data: 62/292,202 5 February 2016 (05.02.2016) 62/341,019 24 May 2016 (24.05.2016) 62/363,775 18 July 2016 (18.07.2016) 62/385,217 8 September 2016 (08.09.2016) 62/417,219 3 November 2016 (03.11.2016) (71) Applicant: DENALI THERAPEUTICS INC. [US/US]; 151 Oyster Point Blvd., 2nd Floor, South San Francisco, California 94080 (US). (72) Inventors: ESTRADA, Anthony A.; c/o Denali Thera- peutics Inc., 151 Oyster Point Blvd., 2nd Floor, South San Francisco, California 94080 (US). FENG, Jianwen A.; c/o Denali Therapeutics Inc., 151 Oyster Point Blvd., 2nd Floor, South San Francisco, California 94080 (US). FOX, Brian; c/o Denali Therapeutics Inc., 151 Oyster Point Blvd., 2nd Floor, South San Francisco, California 94080 (US). LESLIE, Colin Philip; c/o Denali Therapeutics Inc., 151 Oyster Point Blvd., 2nd Floor, South San Francisco, California 94080 (US). LYSSIKATOS, Joseph P.; c/o Denali Therapeutics Inc., 151 Oyster Point Blvd., 2nd Floor, South San Francisco, California 94080 (US). POZZAN, Alfonso; c/o Denali Therapeutics Inc., 151 Oyster Point Blvd., 2nd Floor, South San Francisco, Cali- fornia 94080 (US). SWEENEY, Zachary K.; c/o Denali Therapeutics Inc., 151 Oyster Point Blvd., 2nd Floor, South San Francisco, California 94080 (US). DE VI- (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, 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. 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). Declarations under Rule 4.17: — as to the applicant's entitlement to claim the priority of the earlier application (Rule 4.17(iii)) Published: with international search report (Art. 21(3)) before the expiration of the time limit for amending the claims and to be republished in the event of receipt of amendments (Rule 48.2(h)) (88) Date of publication of the international search report: 8 September 2017 US US US US (84) US W O 20 17 / 1367 27 A3 (54) Title: INHIBITORS OF RECEPTOR-INTERACTING PROTEIN KINASE 1 (57) : The present disclosure relates generally to N-azepinyl-carboxamide derivatives and compositions, and their use as in- hibitors of receptor-interacting protein kinase 1 which is a key regulator of inflammation, apoptosis and necroptosis. |