Patent SG-11201810967V-A (SG)
Title: Radio-pharmaceutical complexes
Inventor: CUTHBERTSON ALAN
IPC: A61K51/04
Filed: 2017-06-06
Abstract: INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property 111111111111111111 111111111111111111111111111111111111111111111111111111111111111111111 Organization International Bureau (10) International Publication Number (43) International Publication Date ......0\"\" WO 2017/211809 Al 14 December 2017 (14.12.2017) WIP0 I PCT (51) International Patent Classification: TR), OAPI (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, A61K 51/04 (2006.01) C07D 213/81 (2006.01) KM, ML, MR, NE, SN, TD, TG). A61K 51/10 (2006.01) A61P 35/00 (2006.01) (21) International Application Number: Declarations under Rule 4.17: PCT/EP2017/063689 — as to applicant's entitlement to apply for and be granted a patent (Rule 4.1700) (22) International Filing Date: 06 June 2017 (06.06.2017) Published: — with international search report (Art. 21(3)) (25) Filing Language: English — with sequence listing part of description (Rule 5.2(a)) (26) Publication Language: English (30) Priority Data: 16173874.5 10 June 2016 (10.06.2016) EP (71) Applicants: BAYER PHARMA AKTIENGESEL- LSCHAFT [DE/DE]; Miillerstr. 178, 13353 Berlin (DE). BAYER AS [NO/NO]; Drammensveien 288, 0283 Oslo (NO). (72) Inventors: CUTHBERTSON, Alan; Orreveien 14, 0789 _ Oslo (NO). TRAUTWEIN, Mark; 100 Bayer Boule- yard, Whippany, NJ 07981-0000 (US). WEBER, Ernst; — = Hermann-Kohl-StraBe 1, 40764 Langenfeld (DE). KAR- - LSSON, Jenny; Ullevalsveien 56C, 0454 Oslo (NO). = HAMMER, Stefanie; Neue Welt 12, 10247 Berlin (DE). (74) Agent: BIP PATENTS; Alfred-Nobel-Str. 10, 40789 Mon- = _ heim am Rhein NRW (DE). = = (81) Designated States (unless otherwise indicated, for every kind AE, AG, AL, AM, of national protection available): 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, 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 ARIPO of regional protection available): (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 AT, BE, BG, CH, CY, CZ, DE, DK, (AL, 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, 1-1 ON (54) Title: RADIO-PHARMACEUTICAL COMPLEXES of (57) : The invention provides a method for the formation of a tissue-targeting thorium complex, said method comprising; Il a) forming an octadentate chelator comprising four hydroxypyridinone (HOPO) moieties, substituted in the N-position with a methyl N group, and a coupling moiety terminating in a carboxylic acid group; b) coupling said octadentate chelator to at least one tissue-targeting —. moiety targeting prolyl endopeptidase FAP; and c) contacting said tissue-targeting chelator with an aqueous solution comprising an ion I r ----- of at least one alpha-emitting thorium isotope. A method of treatment of a neoplastic or hyperplastic disease comprising admistration 1-1 © of such a tissue-targeting thorium complex, as well as the complex and corresponding pharmaceutical formulations are also provided. ei O