Patent SG-11201900090T-A (SG)
Title: Treatment of cancer
Inventor: NIESMAN MICHAEL
IPC: C07D487/04
Filed: 2017-07-13
Abstract: INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization 1#11101111 0 11101 HOE 3E1 0 0111111 0111 OM 11011101 IMO 1111 HE International Bureau (10) International Publication Number (43) International Publication Date .....0\"\"\"1 WO 2018/013862 Al 18 January 2018 (18.01.2018) W I PO I PC T (51) International Patent Classification: CA, CH, CL, CN, CO, CR, CU, CZ, DE, DJ, DK, DM, DO, A61K 31/52 (2006.01) C07D 487/04 (2006.01) DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, (21) International Application Number: HR, HU, ID, IL, IN, IR, IS, JO, JP, KE, KG, KH, KN, KP, PCT/US2017/042011 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, (22) International Filing Date: OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, 13 July 2017 (13.07.2017) 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. (25) Filing Language: English (26) Publication Language: English (84) Designated States (unless otherwise indicated, for every kind of regional protection available): ARIPO (BW, GH, (30) Priority Data: GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, TZ, 62/362,369 14 July 2016 (14.07.2016) US UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, RU, TJ, (71) Applicant: MINGSIGHT PHARMACEUTICALS, 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, INC. [US/US]; P.O. Box 261208, San Diego, California MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, SM, 92196 (US). TR), OAPI (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, (72) Inventors: NIESMAN, Michael; P.O. Box 261208, San KM, ML, MR, NE, SN, TD, TG). Diego, California 92196 (US). ZHANG, Kai; P.O. Box 261208, San Diego, California 92196 (US). Declarations under Rule 4.17: — as to applicant's entitlement to apply for and be granted a (74) Agent: FLOYD, Jennifer; Wilson Sonsini Goodrich & Ro- sait, 650 Page Mill Road, Palo Alto, California 94304 (US). — = as to the applicant's entitlement to claim the priority of the patent (Rule 4.17(0 _ Designated States (unless otherwise indicated, for every earlier application (Rule 4.17(iii)) _ (81) kind of national protection available): AE, AG, AL, AM, = _ AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, BZ, _ = Title: TREATMENT OF CANCER = (54) = Cell Proliferation cmpd A plus Ibrutinib = —o— —•— 1.25 nM — o — Cmpd A only = 0.3125 nM —0—.625 nM = 120% ,, --- = 0 110% U = = 48 oill11111111111 -112 `• BO% . Q' i i I 1 11 I I I I i • I I , , . J = = _ = 60% --- ji lk lvi = a) 40% 20% — 0_ c.) —......w.m r--- \"• 111 + 4 -...1 1 1.11 ,* Ill • • - 0 0% 0.01 0.10 1.00 N Cm pd A Drug Concentration (OA) GC en ,—, © FIG. 3C 00 1-1 (57) : Provided herein are compositions and methods for the treatment of a hematological malignancy. Also disclosed herein C:::: ) are compositions and methods for the treatment of Ewings Sarcoma. Said compositions comprise isoform selective pyrrolo-pyrazole el PKC inhibitors. C [Continued on next page] WO 2018/013862 Al MIDEDIMOM0101011EFIENIIEMIDERIEDIDIIIMEHOIS 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 amendments (Rule 48.2(h)) of receipt of