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1. (WO2016178852) 211-ASTATINE CONTAINING RADIOTHERAPEUTICS FOR THE TREATMENT OF CANCER
Latest bibliographic data on file with the International Bureau   

Pub. No.:    WO/2016/178852    International Application No.:    PCT/US2016/029289
Publication Date: 10.11.2016 International Filing Date: 26.04.2016
IPC:
A61K 31/47 (2006.01), A61K 51/04 (2006.01), C07D 217/04 (2006.01), G21H 5/02 (2006.01)
Applicants: THE TRUSTEES OF THE UNIVERSITY OF PENNSYLVANIA [US/US]; 3160 Chestnut Street, Suite 200 Philadelphia, PA 19104 (US)
Inventors: PRYMA, Daniel, A.; (US).
LIEBERMAN, Brian, P.; (US).
MAKVANDI, Mehran; (US).
MACH, Robert, H.; (US)
Agent: CALDWELL, John W.; (US)
Priority Data:
62/156,534 04.05.2015 US
Title (EN) 211-ASTATINE CONTAINING RADIOTHERAPEUTICS FOR THE TREATMENT OF CANCER
(FR) AGENTS RADIOTHÉRAPEUTIQUES CONTENANT DU 211-ASTATINE POUR LE TRAITEMENT DU CANCER
Abstract: front page image
(EN)Described herein is an alpha-emitting radionuclide, 211At, which has been incorporated into a selective sigma-2 ligand moiety to provide cytotoxic capabilities to a chemical compound. As described herein, a compound of formula (I), wherein R1-R4, m, and n are defined herein, was prepared and utilized in in vitro and in vivo tumor targeting of alpha-emitting sigma-2 ligand in a breast cancer model. In one embodiment, the compound is 5-(211At)-N-(4-(6,7-dimethoxy-3,4- dihydroisoquinolin-2(lH)-yl)butyl)-2,3-dimethoxybenzamide.
(FR)L'invention concerne un radionucléide émetteur d'alpha, 211At, qui a été incorporé dans un fragment de ligand sigma-2 sélectif pour fournir des capacités cytotoxiques à un composé chimique. Comme décrit ici, un composé de formule (I), dans laquelle 1-R4, m et n sont définis ici, a été préparé et utilisé dans un ciblage tumoral in vitro et in vivo de ligand sigma-2 émetteur d'alpha dans un modèle de cancer du sein. Selon un mode de réalisation, le composé est du 5-(211At)-N-(4-(6,7-diméthoxy-3,4- dihydroisoquinoline-2(lH)-yl)butyl)-2,3-diméthoxybenzamide.
Designated States: 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, 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, KN, KP, KR, 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.
African Regional Intellectual Property Organization (BW, GH, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, TZ, UG, ZM, ZW)
Eurasian Patent Organization (AM, AZ, BY, KG, KZ, RU, TJ, TM)
European Patent Office (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, TR)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, KM, ML, MR, NE, SN, TD, TG).
Publication Language: English (EN)
Filing Language: English (EN)