Patent SG-11201909924V-A (SG)
Title: Rapamycin analogs as mtor inhibitors
Inventor: SEMKO CHRISTOPHER
IPC: C07D498/18
Filed: 2018-05-01
Abstract: INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (43) International Publication Date 08 November 2018 (08.11.2018) WIPO I PCT ill 1111u°11111OlDIIl ono o Mo IIH mIIII111110uDIIIIII (10) International Publication Number WO 2018/204416 Al (51) International Patent Classification: C07D 498/18 (2006.01) A61P 25/00 (2006.01) A61K 31/436 (2006.01) A61P 35/00 (2006.01) A61K 31/519 (2006.01) A61P 37/00 (2006.01) CO7D 519/00 (2006.01) (21) International Application Number: PCT/US2018/030531 (22) International Filing Date: 01 May 2018 (01.05.2018) (25) Filing Language: English (26) Publication Language: English (30) Priority Data: 62/500,410 02 May 2017 (02.05.2017) US (71) Applicant: REVOLUTION MEDICINES, INC. [US/US]; 700 Saginaw Drive, Redwood City, CA 94063 (US). (72) Inventors; and (71) Applicants: SEMKO, Christopher [US/US]; c/o Revolu- tion Medicines, Inc., 700 Saginaw Drive, Redwood City, CA 94063 (US). PITZEN, Jennifer [DE/US]; c/o Revolu- tion Medicines, Inc., 700 Saginaw Drive, Redwood City, CA 94063 (US). WANG, Gang [CN/US]; c/o Revolution Medicines, Inc., 700 Saginaw Drive, Redwood City, CA 94063 (US). TIBREWAL, Nidhi [IN/US]; c/o Revolution Medicines, Inc., 700 Saginaw Drive, Redwood City, CA 94063 (US). (72) Inventors: AGGEN, James Bradley; c/o Revolution Med- icines, Inc., 700 Saginaw Drive, Redwood City, CA 94063 (US). THOTTUMKARA, Arun P.; c/o Revolution Medi- cines, Inc., 700 Saginaw Drive, Redwood City, CA 94063 (US). BURNETT, G. Leslie; c/o Revolution Medicines, Inc., 700 Saginaw Drive, Redwood City, CA 94063 (US). GLIEDT, Micah James Evans; c/o Revolution Medicines, Inc., 700 Saginaw Drive, Redwood City, CA 94063 (US). KISS, Gert; c/o Revolution Medicines, Inc., 700 Saginaw Drive, Redwood City, CA 94063 (US). WON, Walter; c/o Revolution Medicines, Inc., 700 Saginaw Drive, Redwood City, CA 94063 (US). LEE, Julie Chu-li; c/o Revolution Medicines, Inc., 700 Saginaw Drive, Redwood City, CA 94063 (US). GILL, Adrian Liam; c/o Revolution Medi- cines, Inc., 700 Saginaw Drive, Redwood City, CA 94063 (US). (74) Agent: TONG, Connie C. et al.; Cooley LLP, 1299 Penn- sylvania Avenue, NW, Suite 700, Washington, DC 20004 (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). (54) Title: RAPAMYCIN ANALOGS AS MTOR INHIBITORS (57) : The present disclosure relates to rapamycin analogs of the general Formula (I). The compounds are inhibitors of mTOR and Me OMe Me Me thus useful for the treatment of cancer, immune-mediated diseases and R 3M Rao age related conditions. e [Continued on next page] W O 20 18/ 20 4416 Al WO 2018/204416 Al O II 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))