Imaging agents for detecting neurological dysfunction

Patent metadata

Field	Value
Publication number	US-8932557-B2
Application number	US-201213477095-A
Country	US
Kind code	B2
Filing date	May 22, 2012
Priority date	Feb 14, 2008
Publication date	Jan 13, 2015
Grant date	Jan 13, 2015

Abstract

Disclosed here in are compounds and methods of diagnosing Alzheimer's Disease or a predisposition thereto in a mammal, the method comprising administering to the mammal a diagnostically effective amount of a radiolabeled compound, wherein the compound is selected from the group consisting of radiolabeled carbazoles and derivatives thereof and triazoles derivatives, allowing the compound to distribute into the brain tissue, and imaging the brain tissue, wherein an increase in binding of the compound to the brain tissue compared to a normal control level of binding indicates that the mammal is suffering from or is at risk of developing Alzheimer's Disease.

First claim

We claim:

1. A compound that is:

or pharmaceutically acceptable salts thereof,
wherein R 21 is selected from the group consisting of F, Cl, Br, I, 18 F, 77 Br, 123 I, 124 I, 125 I, 131 I, and NO 2 .

2. A compound which is:
7-(6-Nitropyridine-3-yl)-5H-pyrido[4,3-b]indole;
or pharmaceutically acceptable salts thereof.

3. A compound that is 7-[6-( 18 F)fluoropyridin-3-yl]-5H-pyrido[4,3-b]indole:

or a pharmaceutically acceptable salt thereof.

4. A compound that is 7-[6-fluoropyridin-3-yl]-5H-pyrido[4,3-b]indole:

or a pharmaceutically acceptable salt thereof.

5. A process for the preparation of 7-[6-( 18 F)fluoropyridin-3-yl]-5H-pyrido[4,3-b]indole, comprising reacting 7-(6-nitropyridine-3-yl)-5H-pyrido[4,3-b]indole with anhydrous [F-18]fluoride ion.

Assignees

• Chen Gang
• Gangadharmath Umesh B
• Kasi Dhanalakshmi
• Sinha Anjana
• Zhang Wei
• Chen Kai
• Mocharla Vani P
• Lilly Co Eli

Inventors

• Chen Gang
• Gangadharmath Umesh B
• Kasi Dhanalakshmi
• Sinha Anjana
• Zhang Wei
• Chen Kai
• Mocharla Vani P

Classifications

• C07D471/14

  Ortho-condensed systems · CPC title

• C07B59/002 Primary

  Heterocyclic compounds · CPC title

• C07D471/04

  Ortho-condensed systems · CPC title

• A61K51/0455 Primary

  having six-membered rings with one nitrogen as the only ring hetero atom · CPC title

• A61K51/0446

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