Patent SG-11201809714T-A (SG)
Title: Piperidines as menin inhibitors
Inventor: WANG SHAOMENG
IPC: C07D405/04
Filed: 2017-05-02
Abstract: INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization 1111111111111111111111111111110111111111111111111111111111111111110111111111 International Bureau (10) International Publication Number (43) International Publication Date .....0\"\" WO 2017/192543 Al 09 November 2017 (09.11.2017) W I P0 I P C T (51) International Patent Classification: C07D 401/04 (2006.01) A61K 31/4523 (2006.01) CO7D 401/14 (2006.01) A61K 31/454 (2006.01) CO7D 405/04 (2006.01) A61K 31/4545 (2006.01) CO7D 211/34 (2006.01) A61P 35/00 (2006.01) (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, (21) International Application Number: PCT/US2017/030577 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, (22) International Filing Date: KM, ML, MR, NE, SN, TD, TG). 02 May 2017 (02.05.2017) (25) Filing Language: English Published: — with international search report (Art. 21(3)) (26) Publication Language: English (30) Priority Data: 62/330,350 02 May 2016 (02.05.2016) US (71) Applicant: 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 49198 (US). AGUILAR, Angelo; 2364 - = Stone Rd., Ann Arbor, 48105 (US). ZHANG, Ke; 2411 Stone Rd., Ann Arbor, MI 48105 (US). XU, Shilin; 3578 =_ Green Brier Blvd., Apartment 405C, Ann Arbor, MI 48105 (US). XU, Tianfeng; 2153 Arbor Circle West, Apartment 205, Ypsilanti, 48197 (US). BERNARD, Denzil; 1803 = Pointe Crossing St., Apartment 101, Ann Arbor, MI 48105 = (US). HUANG, Liyue; 3170 Otter Creek Ct., Ann Arbor, MI 48105 (US). = (74) Agent: NAPOLI, James J.; Marshall, Gerstein & Borun = LLP, 233 S. Wacker Drive, 6300 Willis 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, 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. = 1-1 en (54) Title: PIPERIDINES AS MENIN INHIBITORS in ei (57) : The present disclosure provides compounds represented by Formula (I): (Formula(I)) R3b cT - and the pharmaceutically acceptable salts, hydrates, and solvates thereof, wherein R 2 , R 3a , R 3b , A, G, CP x , ,„ X, and Y are as defined as set forth in the specification. The present disclosure also provides compounds IN R 3 R 2 of Formula (I) for use to treat a condition or disorder responsive to menin inhibition such as cancer. 1-1 0 ei G O