Patent SG-11201908940U-A (SG)
Title: Isoquinolines as inhibitors of hpk1
Inventor: CHAN BRYAN
IPC: C07D417/04
Filed: 2018-03-30
Abstract: International Publication Date 04 October 2018 (04.10.2018) WIPO I PCT (51) International Patent Classification: C07D 401/14 (2006.01) C07D 417/04 (2006.01) C07D 405/14 (2006.01) CO7D 471/04 (2006.01) CO7D 413/14 (2006.01) CO7D 487/04 (2006.01) CO7D 487/14 (2006.01) CO7D 491/04 (2006.01) CO7D 217/22 (2006.01) CO7D 498/04 (2006.01) CO7D 401/04 (2006.01) CO7D 513/04 (2006.01) CO7D 409/14 (2006.01) CO7D 519/00 (2006.01) CO7D 413/04 (2006.01) (12) INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (21) International Application Number: PCT/US2018/025573 (22) International Filing Date: 30 March 2018 (30.03.2018) (25) Filing Language: English (26) Publication Language: English (30) Priority Data: PCT/CN2017/078790 30 March 2017 (30.03.2017) CN PCT/CN2018/076908 15 February 2018 (15.02.2018) CN (71) Applicants: GENENTECH, INC. [US/US]; 1 DNA Way, South San Francisco, California 94080 (US). F. HOFF- MANN-LA ROCHE AG [CH/CH]; Grenzacherstrasse 124, 4070 Basel (CH). (72) Inventors: CHAN, Bryan; c/o Genentech, Inc., 1 DNA Way, South San Francisco, California 94080 (US). DROB- NICK, Joy; c/o Genentech, Inc., 1 DNA Way, South San Francisco, California 94080 (US). GAZZARD, Lewis; c/ o Genentech, Inc., 1 DNA Way, South San Francisco, Cal- ifornia 94080 (US). HEFFRON, Timothy; c/o Genentech, Inc., 1 DNA Way, South San Francisco, California 94080 (US). LIANG, Jun; c/o Genentech, Inc., 1 DNA Way, South San Francisco, California 94080 (US). MALHO- TRA, Sushant; c/o Genentech, Inc., 1 DNA Way, South San Francisco, California 94080 (US). MENDONCA, Ro- han; c/o Genentech, Inc., 1 DNA Way, South San Fran- cisco, California 94080 (US). RAJAPAKSA, Naomi; c/o Genentech, Inc., 1 DNA Way, South San Francisco, Cali- fornia 94080 (US). STIVALA, Craig; c/o Genentech, Inc., 1 DNA Way, South San Francisco, California 94080 (US). TELLIS, John; c/o Genentech, Inc., 1 DNA Way, South San Francisco, California 94080 (US). WANG, Weiru; c/o Genentech, Inc., 1 DNA Way, South San Francisco, California 94080 (US). WEI, BinQing; c/o Genentech, Inc., 1 DNA Way, South San Francisco, California 94080 omit VIII °nolo OH mil moilooimiflo oimIE (10) International Publication Number WO 2018/183964 Al (US). ZHOU, Aihe; 1361 Stephen Way, San Jose, Cali- fornia 94129 (US). CARTWRIGHT, Matthew W.; 8-9 Spire Green, Flex Meadow, Harlow Essex CM19 5TR (GB). LAINCHBURY, Michael; 8-9 Spire Green, Flex Mead- ow, Harlow Essex CM19 5TR (GB). GANCIA, Emanuela; 8-9 Spire Green, Flex Meadow, Harlow Essex CM19 5TR (GB). SEWARD, Eileen; 8-9 Spire Green, Flex Meadow, Harlow Essex CM19 5TR (GB). MADIN, Andrew; 8-9 Spire Green, Flex Meadow, Harlow Essex CM19 5TR (GB). FAVOR, David; 5 Building, 998 Halei Road, Zhangjiang Hi-Tech Park, Pudong New Area, Shanghai 201203 (CN). FONG, Kin Chiu; 5 Building, 998 Halei Road, Zhangjiang Hi-Tech Park, Pudong New Area, Shanghai 201203 (CN). HU, Yonghan; 5 Building, 998 Halei Road, Zhangjiang Hi-Tech Park, Pudong New Area, Shanghai 201203 (CN). GOOD, Andrew; 5 Building, 998 Halei Road, Zhangjiang Hi-Tech Park, Pudong New Area, Shanghai 201203 (CN). (74) Agent: TIAN, Zong-Qiang Bill et al.; c/o Genentech, Inc., 1 DNA Way, South San Francisco, California 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). Declarations under Rule 4.17: as to applicant's entitlement to apply for and be granted a patent (Rule 4.17(ii)) as to the applicant's entitlement to claim the priority of the earlier application (Rule 4.17(iii)) 71' O\ GC (54) Title: ISOQUINOLINES AS INHIBITORS OF HPK1 (57) : Isoquinoline compounds and their use as inhibitors of HPK1 (hematopoietic kinase 1) are described. The compounds 00 are useful in treating HPK1 -dependent disorders and enhancing an immune response. Also described are methods of inhibiting HPK1, O methods of treating HPK1 -dependent disorders, methods for enhancing an immune response, and methods for preparing the isoquino- N line compounds. C [Continued on next page] WO 2018/183964 Al MIDEDIMOMMIDEFIEDEINIIIMEHNHIMEMOIMIE Published: — with international search report (Art. 21(3)) with sequence listing part of description (Rule 5.2(a))