Patent SG-11201807982U-A (SG)
Title: Substituted inhibitors of menin-mll and methods of use
Inventor: WU TAO
IPC: A61K31/535
Filed: 2017-03-15
Abstract: INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property -, Organization M1111101110101011111 HO 111110111011110110101101011110111110111011 11 International Bureau ... .jd ..... .,,,, (10) International Publication Number (43) International Publication Date WO 2017/161028 Al 21 September 2017 (21.09.2017) WIP0 I PCT (51) International Patent Classification: (US). GREMBECKA, Jolanta; 1600 Huron Parkway, A61K 31/535 (2006.01) 2nd Floor, Ann Arbor, MI 48109 (US). CIERPICKI, To- (21) International Application Number: masz; 1600 Huron Parkway, 2nd Floor, Ann Arbor, MI 48109 (US). KLOSSOWSKI, Szymon; 1600 Huron Park- PCT/US2017/022564 way, 2nd Floor, Ann Arbor, MI 48109 (US). POLLOCK, (22) International Filing Date: Jonathan; 1600 Huron Parkway, 2nd Floor, Ann Arbor, 15 March 2017 (15.03.2017) MI 48109 (US). BORKIN, Dmitry; 1600 Huron Parkway, 2nd Floor, Ann Arbor, MI 48109 (US). (25) Filing Language: English (74) Agents: CHANG, Andrew, L. et al.; Wilson Sonsini (26) Publication Language: English Goodrich & Rosati, 650 Page Mill Road, Palo Alto, CA (30) Priority Data: 94304-1050 (US). 62/309,372 16 March 2016 (16.03.2016) US (81) Designated States (unless otherwise indicated, for every 62/334,369 10 May 2016 (10.05.2016) US kind of national protection available): AE, AG, AL, AM, 62/431,389 7 December 2016 (07.12.2016) US AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, 62/446,640 16 January 2017 (16.01.2017) US BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DJ, DK, DM, — (71) Applicants: KURA ONCOLOGY, INC. [US/US]; 11119 DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, North Torrey Pines Road, Suite 125, La Jolla, CA 92037 HN, HR, HU, ID, IL, IN, IR, IS, JP, KE, KG, KH, KN, (US). THE REGENTS OF THE UNIVERSITY OF KP, KR, KW, KZ, LA, LC, LK, LR, LS, LU, LY, MA, MICHIGAN [US/US]; 1600 Huron Parkway, 2nd Floor, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, Ann Arbor, MI 48109 (US). 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, (72) Inventors: WU, Tao; 2355 Terraza Guitara, Carlsbad, CA TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, 92009 (US). LI, Liansheng; 13569 Arroyo Dale Lane, San ZA, ZM, ZW. Diego, CA 92130 (US). WANG, Yi; 7556 Charmant Drive, Apartment 1732, San Diego, CA 92122 (US). REN, (84) Designated States (unless otherwise indicated, for every Pingda; 5534 Havenridge Way, San Diego, CA 92130 kind of regional protection available): ARIPO (BW, GH, [Continued on next page] Title: SUBSTITUTED INHIBITORS OF MENIN-MLL AND METHODS OF USE (54) FIG. 4 MV4;11 s.c. model 2000 -0-vehicle Control 1500 --Compound B, 50 mg/kg/bid, po -9-Compound B, 100 mg/kg/bid, po E ) -IEI-Compound B, 200 mg/kg/qd, po > 1000 8 -0-Compound B, 200 mg/kg/bid, po E +., c w as 500 1-1 ei 2 © 0 2 4 6 8 10 12 14 16 18 1-1 Treatment period (day) 1-1 1-1 (57) : The present disclosure provides methods of inhibiting the interaction of menin with MLL1, MLL2 and MLL-fusion N oncoproteins. The methods are useful for the treatment of leukemia, solid cancers, diabetes and other diseases dependent on activity of MLL1, MLL2, MLL fusion proteins, and/or menin. Compositions for use in these methods are also provided. C WO 2017/161028 Al 1#110HOMOIDEIRMEMOMMIDEMIMMOIMEN GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, Published: TZ, UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, RU, TJ, TM), European (AL, AT, BE, BG, CH, CY, CZ, DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, DE, LT, — with international search report (Art. 21(3)) — before the expiration of the time limit for amending the LU, LV, MC, MK, MT, NL, NO, PL, PT, RO, RS, SI, SK, SM, TR), OAPI (BF, BJ, CF, CG, CI, CM, SE, GA, claims and to be republished in the event amendments (Rule 48.2(h)) of receipt of GN, GQ, GW, KM, ML, MR, NE, SN, TD, TG).