IP Library Granted Patent US 7,413,727
Granted Patent B2
US 7,413,727 · App. 10/462,836 · Granted Aug 19, 2008

Contrast agents

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Quick Facts
Patent No.
US 7,413,727
App. No.
10/462,836
Granted
Aug 19, 2008
Kind
B2
Abstract

The invention provides a composition of matter of the formula (I): V-L-R, where V is a vector moiety having affinity for an angiogenesis-related endothelias cell receptor, L is a linker moiety or a bond and R is a detectable moiety, characterised in that V is a non-peptidic organic group, or V is peptidic and R is a macromolecular or particulate species providing a multiplicity of labels detectable in in vivo imaging.

Claims (20)

1. A composition of matter of formula I

V-L-R  (Formula I)

wherein

L is a linker moiety or a bond;

R is a moiety comprising one to ten detectable labels; and

V is selected from the list of non-peptidic organic groups consisting of:

N 2 -[3S-hydroxy-4-(N-hydroxyamino)2R-isobutylsuccinyl]-L-(4-oxymethylcarboxy)phenylalanine-N 1 -methylamide,

N-(4-octylphenyl)-3-(2-carboxyethyl)-6,7-dihydro-5H-thiazolo[3,2-a]pyrimidine-2-carboxamide,

N 2 -[3S-hydroxy-4-hydroxyamino)-2R-isobutylsuccinyl]-L-phenylalanine-N 1 -methylamide,

N-(6-aminohexyl)-[4-(6,7-dimethoxy-quinazolin-4-ylamino)phenyl]acetamide hydrochloride,

3-Oxo-2-[2-(pyridin-2-ylamino)-ethyl]-2,3-dihydro-1H-isoindole-5-carboxylic acid [2-(2-amino-ethylcarbamoyl)-ethyl]-amide, and

N-(6-amino-hexyl)-2-{3-[2-(4-chloro-benzyloxy)-2-(2,4-dichloro-phenyl)-ethyl]-3H-imidazol-1-yl}-acetamide.

2. A composition of matter of claim 1 labelled with Gd(III), 99m Tc or 111 In chelates of DTPA.

3. A composition of matter as claimed in claim 1 wherein R is a radionuclide.

4. A composition of matter as claimed in claim 3 wherein R is an iodine or metal radionuclide.

5. A pharmaceutical composition comprising a composition of matter of formula I as defined in claim 1 together with at least one pharmaceutically acceptable carrier or excipient.

6. A method of generating an image of an animate human or non-human animal subject involving administering a contrast agent to said subject and generating an image of at least a part of said subject to which said contrast agent has distributed, characterised in that as said contrast agent is used as a composition of matter of formula I as defined in claim 1 .

7. A process for the preparation of a composition of a matter of formula I

V-L-R

of claim 1 , said process comprising conjugating moiety V with moiety R via the linker or bond L.

Assignments (2)
CHANGE OF NAME Recorded Aug 2, 2006
From: AMERSHAM HEALTH AS; NYCOMED IMAGING AS
To: GE HEALTHCARE AS
Reel/Frame 018039/0537 →
CHANGE OF NAME Recorded Nov 13, 2003
From: NYCOMED IMAGING AS
To: AMERHSHAM HEALTH AS
Reel/Frame 014122/0831 →