Patent SG-11201808728Q-A (SG)
Title: Mdm2 protein degraders
Inventor: WANG SHAOMENG
IPC: C07D487/10
Filed: 2017-04-06
Abstract: INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property -, Organization 11M11111011101 111111111101011111011101011111111111111001111111111111110111111 International Bureau ... .... ..Yjd (10) International Publication Number (43) International Publication Date ..... ...,/ WO 2017/176957 Al 12 October 2017(12.10.2017) WIPO I PCT (51) International Patent Classification: (74) Agent: NAPOLI, James, J.; Marshall, Gerstein & Borun CO7D 401/04 (2006.01) A61K 31/4745 (2006.01) LLP, 233 S. Wacker Drive, 6300 Willis Tower, Chicago, CO7D 487/10 (2006.01) A61P 35/00 (2006.01) IL 60606-6357 (US). (21) International Application Number: (81) Designated States (unless otherwise indicated, for every PCT/US2017/026274 kind AO, of national protection available): AE, AG, AL, AM, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, (22) International Filing Date: BZ, 6 April 2017 (06.04.2017) DO, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DJ, DK, DM, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, (25) Filing Language: English HN, KP, HR, HU, ID, IL, IN, IR, IS, JP, KE, KG, KH, KN, KR, KW, KZ, LA, LC, LK, LR, LS, LU, LY, MA, (26) Publication Language: English MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, (30) Priority Data: NI, 62/318,974 6 April 2016 (06.04.2016) US RU, 62/393,874 13 September 2016 (13.09.2016) US TH, NO, NZ, OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, RW, SA, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, 62/409,571 18 October 2016 (18.10.2016) US ZA, ZM, ZW. (71) Applicant: THE REGENTS OF THE UNIVERSITY (84) Designated States (unless otherwise indicated, for every OF MICHIGAN [US/US]; Office of Technology Transfer, kind 1600 Huron Parkway, 2nd Floor, Ann Arbor, MI 48109- GM, of regional protection available): ARIPO (BW, GH, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, 2590 (US). TZ, UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, RU, TJ, TM), European (AL, AT, BE, BG, CH, CY, CZ, DE, (72) Inventors: WANG, Shaomeng; 3336 Stirling Ct., Superi- DK, or Township, MI 49198 (US). LI, Yangbing; 1600 Huron LV, Parkway, NCRC/Building 520, Room 1245, Ann Arbor MI SM, 48109 (GB). YANG, Jiuling; 2424 Leslie Circle, Ann Ar- GW, KM, ML, MR, NE, SN, TD, TG). bor, MI 48105 (US). AGUILAR, Angelo; 2364 Stone Rd., EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, TR), OAPI (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, — _ = Ann Arbor, 48105 (US). ZHOU, Bing; 555 Zu Chong Zhi Published: Road, Shanghai Institute of Materia Medica, Room 3508, — with international search report (Art. 21(3)) _ _ = Shanghai, 201203 (CN). HU, Jiantao; 3005 Whisperwood before the expiration of the time limit for amending the Dr., Apartment 280, Ann Arbor, MI 48105 (US). XU, claims and to be republished in the event of receipt of Fuming; 3111 International Dr., Apt. 2203A, Ypsilanti, amendments (Rule 48.2(h)) MI 48197 (US). REJ, Rohan; 3655 Greenbrier Blvd, Apartment 139B, Ann Arbor, MI 48105 (US). HAN, Xin; — 2327 Arrowwood Trail, Ann Arbor, MI 48105 (US). = = = = = = = = Il IN kin tz. ,tD IN 1-1 IN 1-1 (54) Title: MDM2 PROTEIN DEGRADERS 0 ei (57) : The present disclosure provides compounds represented by Formula I-A: A 1 — L 1 —B 1 I-A and the pharmaceutically ea.. ) acceptable salts, hydrates, and solvates thereof, wherein A 1 , B, and Ll are as 1 defined as set forth in the specification. The present disclosure also provides compounds of Formula I-A for use to treat a condition or disorder responsive to degradation of MDM2 pro - 5 tein such as cancer.