US20110313130 Bifunctional chelating agents

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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

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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, R^1′, Q¹, Q²and 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.

A	HUMAN NECESSITIES
61	MEDICAL OR VETERINARY SCIENCE; HYGIENE
K	PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
38	Medicinal preparations containing peptides
04	Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
12	Cyclic peptides

C	CHEMISTRY; METALLURGY
07	ORGANIC CHEMISTRY
K	PEPTIDES
5	Peptides having up to four amino acids in a fully defined sequence; Derivatives thereof

A	HUMAN NECESSITIES
61	MEDICAL OR VETERINARY SCIENCE; HYGIENE
K	PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
38	Medicinal preparations containing peptides
04	Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
12	Cyclic peptides

C	CHEMISTRY; METALLURGY
07	ORGANIC CHEMISTRY
K	PEPTIDES
5	Peptides having up to four amino acids in a fully defined sequence; Derivatives thereof

C	CHEMISTRY; METALLURGY
07	ORGANIC CHEMISTRY
D	HETEROCYCLIC COMPOUNDS
213	Heterocyclic 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
02	having three double bonds between ring members or between ring members and non-ring members
04	having 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
60	with 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
78	Carbon atoms having three bonds to hetero atoms, with at the most one to halogen, e.g. ester or nitrile radicals
79	Acids; Esters

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1. US20110313130 - Bifunctional chelating agents

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 ; , i.e. characterised by the agent or material covalently linked or complexing the radioactive nucleus
04	Organic compounds
0474	complexes 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
0478	complexes from non-cyclic ligands, e.g. EDTA, MAG3

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 ; , i.e. characterised by the agent or material covalently linked or complexing the radioactive nucleus
04	Organic compounds
08	Peptides, e.g. proteins ; , carriers being peptides, polyamino acids, proteins
082	the peptide being a RGD-containing peptide

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 ; , i.e. characterised by the agent or material covalently linked or complexing the radioactive nucleus
04	Organic compounds
08	Peptides, e.g. proteins ; , carriers being peptides, polyamino acids, proteins
088	conjugates with carriers being peptides, polyamino acids or proteins

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 ; , i.e. characterised by the agent or material covalently linked or complexing the radioactive nucleus
04	Organic compounds
0474	complexes 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
0478	complexes from non-cyclic ligands, e.g. EDTA, MAG3