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1. US20110313130 - Bifunctional chelating agents

Office
United States of America
Application Number 13030766
Application Date 18.02.2011
Publication Number 20110313130
Publication Date 22.12.2011
Grant Number 08772446
Grant Date 08.07.2014
Publication Kind B2
IPC
A61K 38/12
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
38Medicinal preparations containing peptides
04Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
12Cyclic peptides
C07K 5/00
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
KPEPTIDES
5Peptides having up to four amino acids in a fully defined sequence; Derivatives thereof
CPC
C07D 213/79
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
213Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
02having three double bonds between ring members or between ring members and non-ring members
04having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
60with heteroatoms or with carbon atoms having three bonds to hetero atoms, with at the most one to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
78Carbon atoms having three bonds to hetero atoms, with at the most one to halogen, e.g. ester or nitrile radicals
79Acids; Esters
A61K 51/0478
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
0474complexes or complex-forming compounds, i.e. wherein a radioactive metal (e.g. 111In3+) is complexed or chelated by, e.g. a N2S2, N3S, NS3, N4 chelating group
0478complexes from non-cyclic ligands, e.g. EDTA, MAG3
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 or proteins
Applicants Adam Mike
Nordion (Canada) Inc.
Boros Eszter
Ferreira Cara L.
Orvig Chris
Price Eric William
Inventors Adam Mike
Boros Eszter
Ferreira Cara L.
Orvig Chris
Price Eric William
Agents Arent Fox LLP
Title
(EN) Bifunctional chelating agents
Abstract
(EN)

A bifunctional chelating agent of the formula (I):

embedded image
wherein the variables R1, R1′, Q1, Q2 and M are as defined in the description of the present application. Also described is a complex of the above chelating agent to an ion of a stable or radioactive metal; a conjugate of the complex covalently attached to a biological carrier; and a pharmaceutical composition containing the conjugate.


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