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    • 4. 发明专利
    • MANUFACTURE OF TRANS-[TETRACHLOROBIS(1H-INDAZOLE)RUTHENATE (III)] AND COMPOSITIONS THEREOF
    • SG11201910043PA
    • 2019-11-28
    • SG11201910043P
    • 2018-05-07
    • INTEZYNE TECHNOLOGIES INCVOJKOVSKY TOMASSILL KEVINCARIE ADAM
    • VOJKOVSKY TOMASSILL KEVINCARIE ADAM
    • A61K31/555A61K31/416A61K33/24
    • INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (43) International Publication Date 08 November 2018 (08.11.2018) WIPO I PCT Iiiimmoimiolollmonolooloviimiflinomovom (10) International Publication Number WO 2018/204930 Al (51) International Patent Classification: A61K 31/416 (2006.01) A61K 33/24 (2006.01) A61K 31/555 (2006.01) (21) International Application Number: PCT/US2018/031436 (22) International Filing Date: 07 May 2018 (07.05.2018) (25) Filing Language: English (26) Publication Language: English (30) Priority Data: 62/501,984 05 May 2017 (05.05.2017) US (71) Applicant: INTEZYNE TECHNOLOGIES, INC. [US/US]; 3720 Spectrum Blvd., Suite 104, Tampa, Florida 33612 (US). (72) Inventors; and (71) Applicants: VOJKOVSKY, Tomas [ /US]; 23 Shelby Lane, Palm Beach Gardens, Florida 33418 (US). SILL, Kevin [ /US]; 16308 Royal Park Ct., Tampa, Florida 33647 (US). CARIE, Adam [ /US]; 4206 Knob Lake Ct., Tampa, FL 33619 (US). (74) Agent: REID, Andrea L.C. et al.; One International Place, 100 Oliver Street, 40th Floor, Boston, Massachusetts 02110-2605 (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, (54) Title: MANUFACTURE OF TRANS-[TETRACHLOROBIS(1H-INDAZOLE)RUTHENATE (III)] AND COMPOSITIONS = THEREOF 120 100 IT- 139 Drug Su b O cr O 1 \ \ 80 1 \ 1 \ \ 60 7 1 \\ \ \ \ 40d \ , 1 20 1 \\ \ 1 01 1 0 10 20 IT-139 2-8°C - -0- - IT-13918-22°C 30 40 50 60 Time (h) Figure 1 1-1 (57) : The present invention relates to the preparation of compositions comprising sodium trans-[tetrachlorobis(1H- ei • mdazole)ruthenate (III)]. Synthesis and formulation preparation is detailed. Impurity profiles are also discussed. Compositions herein C are useful for anti-cancer applications. [Continued on next page] WO 2018/204930 Al MIDEDIMOMMIDIRE10100101011fifilIMIHMEMOIS 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))