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1. (WO2017196806) CHEMICAL CONJUGATES OF EVANS BLUE DERIVATIVES AND THEIR USE AS RADIOTHERAPY AND IMAGING AGENTS
Latest bibliographic data on file with the International BureauSubmit observation

Pub. No.: WO/2017/196806 International Application No.: PCT/US2017/031696
Publication Date: 16.11.2017 International Filing Date: 09.05.2017
IPC:
C07D 207/444 (2006.01) ,A61K 51/04 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
207
Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
02
with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
44
having three double bonds between ring members or between ring members and non-ring members
444
having two doubly-bound oxygen atoms directly attached in positions 2 and 5
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
51
Preparations containing radioactive substances for use in therapy or testing in vivo
02
characterised by the carrier
04
Organic compounds
Applicants:
THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES [US/US]; National Institutes of Health Office of Technology Transfer 6011 Executive Boulevard Suite 325, MSC 7660 Bethesda, Maryland 20892-7660, US
Inventors:
CHEN, Xiaoyuan; US
WEISS, Orit Jacobson; US
Agent:
GARABEDIAN, Todd E.; US
Priority Data:
62/333,42709.05.2016US
Title (EN) CHEMICAL CONJUGATES OF EVANS BLUE DERIVATIVES AND THEIR USE AS RADIOTHERAPY AND IMAGING AGENTS
(FR) CONJUGUÉS CHIMIQUES DE DÉRIVÉS DU BLEU D'EVANS ET LEUR UTILISATION COMME AGENTS DE RADIOTHÉRAPIE ET D'IMAGERIE
Abstract:
(EN) The present invention is directed to a compound of Formula I or Formula III or a pharmaceutically acceptable ester, amide, solvate, or salt thereof, or a salt of such an ester or amide or a solvate of such an ester amide or salt: wherein the definitions of R1-R13 and L1-L4 are provided in the disclosure, and wherein R14 is a peptide. The compounds of Formula I may be covalently bonded to a peptide via a linker to provide a compound of Formula III and thereby extend the half-life of the therapeutic compound. The invention is also directed to pharmaceutical compositions of the disclosed compounds, as well as their use in the diagnosis or treatment of diseases.
(FR) La présente invention concerne un composé de formule I ou de formule III ou un ester, amide, solvate ou sel pharmaceutiquement acceptable de ce dernier, ou un sel d'un tel ester ou amide ou un solvate d'un tel ester, amide, ou sel, dans lesquelles formules les définitions de R1 à R13 et L1 à L4 sont telles qu'indiquées dans la description et R14 est un peptide. ` Les composés de formule I peuvent être liés de manière covalente à un peptide par l'intermédiaire d'un groupe de liaison, pour fournir un composé de formule III et prolonger ainsi la demi-vie du composé thérapeutique. L'invention concerne également des compositions pharmaceutiques des composés de la présente invention, ainsi que leur utilisation dans le diagnostic ou le traitement de maladies.
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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, 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
African Regional Intellectual Property Organization (ARIPO) (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)