# US 8,784,774 B2 · Labeled molecular imaging agents and methods of use

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- Number: US 8,784,774 B2
- Document ID: US8784774B2
- Status: Granted
- Kind: B2
- Application number: 13/234,210
- Filed: 2011-09-16
- Published: 2013-03-21
- Granted: 2014-07-22
- Earliest claimed: 2011-09-16
- Assignees: General Electric Company
- Applicants: Jack Mathew Webster; Bruce Fletcher Johnson; Brian Duh-Lan Lee; Chittari Pabba; Michael James Rishel
- Inventors: Jack Mathew Webster; Bruce Fletcher Johnson; Brian Duh-Lan Lee; Chittari Pabba; Michael James Rishel
- Web page: https://patentgrep.com/patent/US8784774B2

## CPC

- A61K 51/0406: {Amines, polyamines, e.g. spermine, spermidine, amino acids, (bis)guanidines}
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- C07B 59/001: {Acyclic or carbocyclic compounds}
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- C07B: GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR (preparation of carboxylic acid esters by telomerisation C07C67/47; telomerisation C08F)

## 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.

## Claims

### Claim 1

A cystine/glutamate transporter imaging agent comprising a 18F labeled derivative of Formula I
wherein:
Formula I is a L-enantiomeric form;
R2 is independently at each occurrence H and 18F wherein 18F is singularly occurring; and
n is 5.

### Claim 2 (depends on 1)

A method for imaging a target having a cystine/glutamate transporter comprising:
introducing into the target an imaging agent of claim 1 comprising a 18F labeled derivative of Formula I
wherein;
X is independently at each occurrence H, and 18F wherein 18F is singularly occurring;
n is an integer between 3 and 7; and
detecting the labeled derivative in the target.

### Claim 3 (depends on 2)

The method of claim 2, wherein the labeled derivative comprises a compound of Formula II
wherein R2 is independently at each occurrence H, 18F, —(CH2)mR3, or —O—(CH2)mR3;
R3 is 18F or wherein R2 is a singularly occurring 18F
n is an integer between 3 and 7; and
m is an integer between 1 and 3.

### Claim 4 (depends on 3)

The method of claim 3 wherein R2 is 18F and n is equal to 5.

### Claim 5 (depends on 2)

The method of claim 2 wherein the imaging agent is detected in apoptotic cells.

### Claim 6 (depends on 2)

The method of claim 2 wherein the imaging agent is detected in cells with high cystine uptake.

### Claim 7 (depends on 2)

The method of claim 2 wherein the detecting step comprises detecting the imaging agent using one or more of positron emission tomography (PET), autoradiography, scintillation detection, or a combination thereof.