Molecular probes for imaging of myelin

Patent metadata

Field	Value
Publication number	US-11382991-B2
Application number	US-201816000717-A
Country	US
Kind code	B2
Filing date	Jun 5, 2018
Priority date	Sep 30, 2008
Publication date	Jul 12, 2022
Grant date	Jul 12, 2022

Abstract

A molecular probe for labeling myelin includes a fluorescent trans-stilbene derivative.

First claim

Having described the invention, the following is claimed:

1. A method of detecting myelin in vivo in an animal, the method comprising:
(i) administering to the animal a molecular probe including a compound having the general formula:

wherein R 1 and R 2 are each independently selected from the group consisting of H, NO 2 , NH 2 , NHCH 3 , N(CH 3 ) 2 , OH, OCH 3 , COOCH 3 , SH, SCH 3 , alkyl derivatives thereof, a halo group, a radiolabel, a chelating group, and a near infrared group, provided that at least one of R 1 or R 2 is NH 2 , NHCH 3 , or N(CH 3 ) 2 ; wherein X 1 is a double or triple bond; each R 4 -R 13 are independently H; or a pharmaceutically acceptable salt thereof;
(ii) detecting the molecular probe in the animal using an in vivo imaging modality to determine the myelinated regions in the animal, wherein the compound binds to myelin and the detected molecular probe that is bound to myelin is indicative of myelinated regions of the animal.

2. The method of claim 1 , the in vivo imaging modality comprising a Positron Emission Tomography (PET) imaging modality.

3. The method of claim 1 , the in vivo imaging modality comprising a micro Positron Emission Tomography (microPET) imaging modality.

4. The method of claim 1 , further comprising the step of administering the molecular probe to the animal parenterally.

5. The method of claim 1 , wherein the molecular probe further comprises a radiolabel.

6. The method of claim 5 , the radiolabel including a 3 H, 125 I, 11 C, or 18 F.

7. The method of claim 1 , wherein the molecular probe further comprises a chelating group or a near infrared imaging group.

8. The method of claim 1 , wherein X 1 is a double bond.

9. The method of claim 1 , wherein R 1 and R 2 are amines or alkyl derivatives thereof.

10. The method of claim 1 , the molecular probe comprising at least one compound including the following general structures:

or pharmaceutically acceptable salts thereof.

Assignees

• Univ Case Western Reserve

Inventors

• Wang Yanming
• Wu Chunying

Classifications

• A61K51/04

  Organic compounds · CPC title

• A61K49/0021

  the fluorescent group being a small organic molecule · CPC title

• A61K49/0032

  Methine dyes, e.g. cyanine dyes · CPC title

• G01N33/92

  involving lipids, e.g. cholesterol {, lipoproteins, or their receptors (steroid hormones G01N33/743)} · CPC title

• A61K49/085 Primary

  conjugated systems · CPC title