Labeled molecular imaging agents and methods of use

Patent metadata

Field	Value
Publication number	US-9468693-B2
Application number	US-201414161863-A
Country	US
Kind code	B2
Filing date	Jan 23, 2014
Priority date	Jan 23, 2014
Publication date	Oct 18, 2016
Grant date	Oct 18, 2016

Abstract

Imaging agents are described that comprise labeled substrates capable of being introduced into cells via the cystine/glutamate antiporter. The substrates may be used for imaging or detecting oxidative stress in cells by introducing the labeled agents into cells via the cystine/glutamate antiporter and subsequent detection.

First claim

The invention claimed is:

1. An imaging agent comprising a compound of Formula I

wherein X is 18 F, 3 H, —(CH 2 ) m Z, —CH 2 —O—(CH 2 ) m Z, or —O—(CH 2 ) m Z;
Z is 18 F or 3 H;
m is an integer between 1 and 5;
Y is O—CH 2 , CH 2 —O, CH 2 —CH 2 , CH 2 —CH 2 —CH 2 , O—CH 2 —CH 2 , or CH 2 —O—CH 2 ; and
Ar is a 3-substituted phenyl, 4-substituted phenyl, 4-substituted naphthalene-1-yl, 5-substituted naphthalene-1-yl, or 6-substituted naphthalene-2-yl.

2. The agent of claim 1 wherein X is —O—(CH 2 ) m Z.

3. The agent of claim 2 wherein Z is 18 F or 3 H.

4. The agent of claim 3 wherein Z is a singularly occurring 18 F.

5. The agent of claim 1 wherein Formula I is

6. The agent of claim 1 wherein Formula I is

7. The agent of claim 1 wherein Formula I is

Assignees

• Gen Electric

Inventors

• Hay Bruce Allan
• Webster Jack Mathew

Classifications

• A61K49/0004 Primary

  Screening or testing of compounds for diagnosis of disorders, assessment of conditions, e.g. renal clearance, gastric emptying, testing for diabetes, allergy, rheuma, pancreas functions · CPC title

• G01N33/5091

  for testing the pathological state of an organism · CPC title

• A61K51/0446 Primary

  having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil · CPC title

• C07B59/002

  Heterocyclic compounds · CPC title

• A61K51/0406 Primary

  Amines, polyamines, e.g. spermine, spermidine, amino acids, (bis)guanidines · CPC title