Patent SG-11201811393W-A (SG)
Title: Phthalazine derivatives as inhibitors of parp1, parp2 and/or tubulin useful for the treatment of cancer
Inventor: TSANG TSZE
IPC: C07D403/10
Filed: 2017-06-23
Abstract: WO 17 / 2235 16 Al (I) 0 N ‘>-NH R 6 NH N (12) INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (43) International Publication Date 28 December 2017 (28.12.2017) WIPO I PCT o 1E1 olo VIII Holm o Hum! oil Em Hi m° lII ois (10) International Publication Number WO 2017/223516 Al (51) International Patent Classification: CO7D 403/10 (2006.01) CO7D 403/14 (2006.01) CO7D 405/14 (2006.01) A61K 31/502 (2006.01) C07D 471/04 (2006.01) A61P 35/00 (2006.01) C07D 401/14 (2006.01) (21) International Application Number: PCT/US2017/039119 (22) International Filing Date: 23 June 2017 (23.06.2017) (25) Filing Language: English (26) Publication Language: English (30) Priority Data: 62/354,449 24 June 2016 (24.06.2016) US 62/426,095 23 November 2016 (23.11.2016) US (71) Applicants: THE REGENTS OF THE UNIVERSI- TY OF CALIFORNIA [US/US]; 1111 Franklin Street, Twelfth Floor, Oakland, CA 94607-5200 (US). AT- LASMEDX, INC. [US/US]; UCSF Mission Bay Cam- pus,1700 4th Street, Byers Hall 214, MC 2522, San Fran- cisco, California 94158-2330 (US). (72) Inventors: TSANG, Tsze; 8367 Kent Drive, El Cerrito, CA 94530 (US). PETO, Csaba, J.; c/o UCSF Mt Zion Can- cer Research Bldg., 2340 Sutter Street, San Francisco, CA 94143 (US). JABLONS, David, M.; c/o UCSF Mt Zion Cancer Research Bldg., 2340 Sutter Street, San Francisco, CA 94143 (US). LEMJABBAR-ALAOUI, Hassan; c/o UCSF Mt Zion Cancer Research Bldg., 2340 Sutter Street, San Francisco, CA 94143 (US). (74) Agent: ESKER, Todd et al.; Morgan, Lewis & Bockius LLP, One Market, Spear Street Tower, San Francisco, CA 94105 (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)) Published: — with international search report (Art. 21(3)) (54) Title: PHTHALAZINE DERIVATIVES AS INHIBITORS OF PARP1, PARP2 AND/OR TUBULIN USEFUL FOR THE TREATMENT OF CANCER (57) : The application relates to phthalazine derivatives of formula (I) which are inhibitors of PARP1, PARP2 and/or tubulin and thus useful for the treatment of cancer. Also disclosed are pharmaceuti- cal formulations containing such compounds, as well as combinations of these compounds with at least one additional therapeutic agent.