Patent SG-11201909083U-A (SG)
Title: Piperidines as covalent menin inhibitors
Inventor: WANG SHAOMENG
IPC: A61K31/445
Filed: 2018-03-30
Abstract: 1 (54) Title: PIPERIDINES AS COVALENT MENIN INHIBITORS IN ir) R id Ot 1 R1° en N1 ) , GC R 8b ''''''' . - 71 'R i j e V r1 N Il A 0 .... 1 . 5 ° R8a o x, z2 (I) (57) : The present disclosure provides compounds represented by Formula (I): and the pharmaceutically acceptable salts and solvates thereof, wherein A, R la , R ib R ic , R id , R 2 , R , R 3 8a , R , R 8b 10 , m, and n are as defined as set forth in the specification. The present disclosure also provides compounds of Formula (I) for use to treat a condition or disorder responsive to menin inhibition such as cancer. (12) INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (43) International Publication Date 04 October 2018 (04.10.2018) W I PO I PC T oimiolo VIII °nolo III OH H ioo Imo oimIE (10) International Publication Number WO 2018/183857 Al (51) International Patent Classification: A61K 31/445 (2006.01) C07D 401/06 (2006.01) C07D 211/26 (2006.01) (21) International Application Number: PCT/US2018/025417 (22) International Filing Date: 30 March 2018 (30.03.2018) (25) Filing Language: English (26) Publication Language: English (30) Priority Data: 62/479,520 31 March 2017 (31.03.2017) US (71) Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGAN [US/US]; Office of Technology Trans- fer, 1600 Huron Parkway, 2nd Floor, Ann Arbor, MI 48109-2590 (US). (72) Inventors: WANG, Shaomeng; 3336 Stirling Ct., Superi- or Township, MI 48198 (US). AGUILAR, Angelo; 2364 Stone Rd., Ann Arbor, MI 48105 (US). XU, Shilin; 3578 Green Brier Blvd., Apartment 405C, Ann Arbor, MI 48105 (US). HUANG, Liyue; 3170 Otter Creek Ct., Ann Arbor, MI 48105 (US). STUCKEY, Jeanne; 13536 Lakebrook Drive, Fenton, MI 48430 (US). TIANFENG, Xu; 2153 Ar- bor Circle West, Apartment 205, Ypsilanti, MI 48197 (US). (74) Agent: NAPOLI, James, J.; Marshall, Gerstein & Borun LLP, 233 S. Wacker Drive, 6300 Wills Tower, Chicago, IL 60606-6357 (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). Published: with international search report (Art. 2 I (3)) C