Patent SG-11201903431S-A (SG)
Title: Sstr-targeted conjugates and particles and formulations thereof
Inventor: SHINDE RAJESH R
IPC: A61P35/00
Filed: 2017-10-27
Abstract: INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property MUNRO III HO I1111 011001 0 01111111111111111111111111111111111111 Organization International Bureau (10) International Publication Number (43) International Publication Date .....0\"\"\" WO 2018/081521 Al 03 May 2018 (03.05.2018) WIP0 I PCT (51) International Patent Classification: House Rd, Bernardsville, New Jersey 07924 (US). SEARS, A61K 47/64 (2017.01) C07K 14/72 (2006.01) Chris; 3 Leslie Rd., Belmont, Massachusetts 02478 (US). A61P 35/00 (2006.01) (74) Agent: WARD, Donna T. et al.; DT WARD, PC, 142A (21) International Application Number: Main Street, Groton, Massachusetts 01450 (US). PCT/US2017/058701 (81) Designated States (unless otherwise indicated, for every (22) International Filing Date: kind of national protection available): AE, AG, AL, AM, 27 October 2017 (27.10.2017) 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, (25) Filing Language: English DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, (26) Publication Language: English HR, HU, ID, IL, IN, IR, IS, JO, JP, KE, KG, KH, KN, KP, (30) Priority Data: KR, KW, KZ, LA, LC, LK, LR, LS, LU, LY, MA, MD, ME, 62/414,481 28 October 2016 (28.10.2016) US 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, (71) Applicant: TARVEDA THERAPEUTICS, INC. SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, [US/US]; 134 Coolidge Avenue, Watertown, Massachusetts TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW. 02472 (US). (84) Designated States (unless otherwise indicated, for every (72) Inventors: SHINDE, Rajesh R.; 110 Stearns Hill Rd, kind of regional protection available): ARIPO (BW, GH, Waltham, Massachusetts 02451 (US). ALARGOVA, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, TZ, _ Rossitza G.; 148 Newton St., Apt.4, Brighton, Massachu- UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, RU, TJ, setts 02135 (US). LIM SOO, Patrick; 64 Garfield Place, TM), European (AL, AT, BE, BG, CH, CY, CZ, DE, DK, = Unit B, Ridgewood, New Jersey 07450 (US). SWERY- 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, DA-KRAWIEC, Beata; 46 Littlefield Lane, Marlborough, = Massachusetts 01752 (US). ALLAND, Leila; 102 Carriage = (54) Title: SSTR-TARGETED CONJUGATES AND PARTICLES AND FORMULATIONS THEREOF Fig. 3 HCC-33 Xenograft efficacy Vehicle 4 wikm. = 2000 *).0.:. Conj. 57 1.0mg/kg = — 1800 .. % 1600 i Conj. 57 0.5mg/kg = — E 1400 . Conj. 57 0.33mg/kg ..,,,.. ' I ' = 1200 i , ...e. , Conj. 57 O.Smg/kg2x's/week = '5 1000 > Conj. 57 0.25mg/kg2x's/week E 800 = 2 - 600 = (i.i °.° 400 • w 200 > .' _ — 0 ,. , 1-1 0 3 6 9 12 15 18 21 24 27 30 Days 1-1 ei kr) 1-1 (57) : Conjugates of an active agent such as DM1 attached to a targeting moiety, such as a somatostatin receptor binding C moiety, via a linker, and particles comprising such conjugates have been designed. Such conjugates and particles can provide improved - --- GC temporospatial delivery of the active agent, improved biodistribution and penetration in tumor, and/or decreased toxicity. Methods of , 1 making the conjugates, the particles, and the formulations thereof are provided. Methods of administering the formulations to a subject 0 in need thereof are provided, for example, to treat or prevent cancer. ei O [Continued on next page] WO 2018/081521 Al MIDEDIMOM0101011EFIDINIRMEOHOIHOIIIMEMOIS 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. 21(3))