# US 6,723,746 B2 · Functional radiographic imaging methods and agents

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- Number: US 6,723,746 B2
- Document ID: US6723746B2
- Status: Granted
- Kind: B2
- Application number: 09/809,870
- Filed: 2001-03-15
- Published: 2001-10-18
- Granted: 2004-04-20
- Earliest claimed: 1998-09-08
- Assignees: Veritas Pharmaceuticals, Inc.
- Inventors: Jesse Salb; Nicholas Cairns
- Web page: https://patentgrep.com/patent/US6723746B2

## CPC

- A61K 49/0438: {Organic X-ray contrast-enhancing agent comprising an iodinated group or an iodine atom, e.g. iopamidol}
- A61B 6/4035: {the source being combined with a filter or grating}
- A61B 6/4241: {using energy resolving detectors, e.g. photon counting}
- A61K 49/0433: {containing an organic halogenated X-ray contrast-enhancing agent}
- A61K 51/04: Organic 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)
- A61B: DIAGNOSIS; SURGERY; IDENTIFICATION (usefulness limited to only animals A61D)

## Abstract

Systems and methods for radiographic imaging of tissue using a radio-opaque imaging agent that in one embodiment accumulates intracellularly in tissue in proportion to its functional, or physiological, activity. In one embodiment, the imaging agent is a cell membrane-permeable, radio-opaque, high affinity ligand for an intracellular target. The imaging agent is administered to a patient, and after an accumulation interval, radiographic images are acquired. The imaging agent preferentially accumulates in certain types of tissue and increases its radio-opacity. The tissue being examined is transilluminated by X-ray beams with preselected different mean energy spectra, and a separate radiographic image is acquired during transillumination by each beam. An image processing system may perform a weighted combination of the acquired images to produce a single displayed image. The system and method thus provides a functional image displayed with the anatomical detail and spatial resolution of a radiographic image. Functional and anatomical information are displayed in complete registration, facilitating localization of abnormal tissue in relation to nearby anatomical structures.

## Claims

### Claim 1

A compound having the general formula S-L-X wherein:
the X moiety is selected from alkyl, alkoxy, alkylthio, alkenyl, alkylamino and aryl, and is substituted with at least one atom having a K-absorption edge of about 13 keV to about 90 keV;
the S moiety is selected from pyranose and furanose; and
the L moiety is selected from aryl, arylamido, alkylamido, alkyl, and thioamido, and is bonded to said X moiety and to said S moiety.

### Claim 2 (depends on 1)

The compound of claim 1 wherein said at least one atom of said X moiety is selected from Br, I, and Bi.

### Claim 3 (depends on 1)

The compound of claim 1 wherein said X moiety is further substituted with at least one group selected from hydroxyalkyl, alkoxy, alkloxyalkyl, alkylamido, hydroxyalkylamido, and polyhydroxyalkylamido.

### Claim 4 (depends on 1)

The compound of claim 1 wherein said L moiety is an unsubstituted or substituted arylamido and is N-bonded to said S moiety.

### Claim 5 (depends on 1)

The compound of claim 1 wherein said L moiety is further substituted with at least one group selected from nitro, amino, methyl, methoxy, and hydroxy.

### Claim 6 (depends on 1)

The compound of claim 1 wherein said L moiety contains at least one N atom and is N-bonded to the S moiety.

### Claim 7 (depends on 1)

The compound of claims 1 wherein said S moiety is hydroxy-substituted.

### Claim 8 (depends on 1)

The compound of claim 1 wherein said S moiety is 2-hydroxy-substituted.

### Claim 9 (depends on 1)

The compound of claim 1 which is 2-Amino-4-[3′,5′-bis(N-acetamido)-2′,4′,6′-triiodophenyl]-benzoyl-D-glucosamine.

### Claim 10 (depends on 1)

The compound of claim 1 which is 2,6-Diamino-4-[3′,5′-bis(N-methylacetamido)-2′,4′,6′-triiodophenyl]-benzoyl-D-glucosamine.

### Claim 11 (depends on 1)

The compound of claim 1 which is 2-Amino-4-[3′,5′-bis(2,3-dihydroxypropylmethylcarbamoyl)2′,4′,6′-triiodophenyl]-benzoyl-D-glucosamine.

### Claim 12 (depends on 1)

The compound of claim 1 wherein said X moiety is substituted with at least one atom of a radioisotope.

### Claim 13 (depends on 1)

The compound of claim 1 wherein said X moiety is substituted with at least one atom of 123I.

### Claim 14 (depends on 1)

The compound of claim 1 which is [123I]-2-Amino-4-[3′,5′-bis(N-acetamido)-2′,4′,6′-triiodophenyl]-benzoyl-D-glucosamine.

### Claim 15 (depends on 1)

The compound of claim 1 which is [123I]-2-Diamino-4-[3′,5′-bis(N-methylacetamido)-2′,4′,6′-triiodophenyl]benzoyl-D-glucosamine.

### Claim 16 (depends on 1)

The compound of claim 1 which is [123I]-2-Amino-4-[3′,5′-bis(2,3-dihydroxypropylmethylcarbamoyl)-2′,4′,6′triiodophenyl]benzoyl-D-glucosamine.