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1. WO2017196806 - CHEMICAL CONJUGATES OF EVANS BLUE DERIVATIVES AND THEIR USE AS RADIOTHERAPY AND IMAGING AGENTS

Publication Number WO/2017/196806
Publication Date 16.11.2017
International Application No. PCT/US2017/031696
International Filing Date 09.05.2017
IPC
C07D 207/444 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
207Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
02with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
44having three double bonds between ring members or between ring members and non-ring members
444having two doubly-bound oxygen atoms directly attached in positions 2 and 5
A61K 51/04 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
51Preparations containing radioactive substances for use in therapy or testing in vivo
02characterised by the carrier
04Organic compounds
CPC
A61K 51/0497
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
51Preparations containing radioactive substances for use in therapy or testing in vivo
02characterised by the carrier ; , i.e. characterised by the agent or material covalently linked or complexing the radioactive nucleus
04Organic compounds
0497conjugates with a carrier being an organic compounds
A61K 51/082
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
51Preparations containing radioactive substances for use in therapy or testing in vivo
02characterised by the carrier ; , i.e. characterised by the agent or material covalently linked or complexing the radioactive nucleus
04Organic compounds
08Peptides, e.g. proteins ; , carriers being peptides, polyamino acids, proteins
082the peptide being a RGD-containing peptide
A61K 51/088
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
51Preparations containing radioactive substances for use in therapy or testing in vivo
02characterised by the carrier ; , i.e. characterised by the agent or material covalently linked or complexing the radioactive nucleus
04Organic compounds
08Peptides, e.g. proteins ; , carriers being peptides, polyamino acids, proteins
088conjugates with carriers being peptides, polyamino acids, proteins
A61P 35/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
C07B 2200/05
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
2200Indexing scheme relating to specific properties of organic compounds
05Isotopically modified compounds, e.g. labelled
C07B 59/002
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
59Introduction of isotopes of elements into organic compounds ; ; Labelled organic compounds per se
002Heterocyclic compounds
Applicants
  • THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES [US]/[US]
Inventors
  • CHEN, Xiaoyuan
  • WEISS, Orit Jacobson
Agents
  • GARABEDIAN, Todd E.
Priority Data
62/333,42709.05.2016US
Publication Language English (EN)
Filing Language English (EN)
Designated States
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.
Also published as
SG11201809982R
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