Patent SG-11201806548U-A (SG)
Title: Radio-pharmaceutical complexes
Inventor: LINDEN LARS
IPC: C07K16/32
Filed: 2017-03-20
Abstract: INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (10) International Publication Number (43) International Publication Date WO 2017/162555 Al 28 September 2017 (28.09.2017) WIPO I PCT 111111111111110111011111111111010111110111011111111011111111111111111111111111110111111 (51) International Patent Classification: A61K 51/10 (2006.01) A61K 103/40 (2006.01) C07K 16/32 (2006.01) A61P 35/00 (2006.01) (21) International Application Number: PCT/EP2017/056503 (22) International Filing Date: 20 March 2017 (20.03.2017) (25) Filing Language: English (26) Publication Language: English (30) Priority Data: 16162123.0 24 March 2016 (24.03.2016) EP (71) Applicants: BAYER PHARMA AKTIENGESELL- SCHAFT [DE/DE]; Miillerstr. 178, 13353 Berlin (DE). BAYER AS [NO/NO]; Drammensveien 288, N-0283 Oslo (NO). (72) Inventors: LINDEN, Lars; Am Altenlande 2, 58285 Gevelsberg (DE). CUTHBERTSON, Alan; Orrevein 14, N-9789 Oslo (NO). (74) Agent: BIP PATENTS; Alfred-Nobel-Str. 10, 40789 Monheim am Rhein (DE). (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, Published: with international search report (Art. 21(3)) with sequence listing part of description (Rule 5.2(a)) 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, 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, TR), OAPI (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, KM, ML, MR, NE, SN, TD, TG). Declarations under Rule 4.17: as to applicant's entitlement to apply for and be granted a patent (Rule 4.1700) W O 20 17 / 16 2555 Al (54) Title: RADIO-PHARMACEUTICAL COMPLEXES (57) : The invention provides a method for the formation of a tissue-targeting thorium complex, said method comprising; a) forming an octadentate chelator comprising four hydroxypyridinone (HOPO) moieties, substituted in the N-position with a methyl group, and a coupling moiety terminating in a carboxylic acid group; b) coupling said octadentate chelator to at least one tissue-tar - geting moiety targeting HER2; and c) contacting said tissue-targeting chelator with an aqueous solution comprising an ion of at least one alpha-emitting thorium isotope. A method of treatment of a neoplastic or hyperplastic disease comprising admistration of such a tissue-targeting thorium complex, as well as the complex and corresponding pharmaceutical formulations are also provided