IP Library Granted Patent US 7,354,935
Granted Patent B2
US 7,354,935 · App. 10/528,888 · Granted Apr 8, 2008

Radiolabeled neurokinin-1 receptor antagonists

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Quick Facts
Patent No.
US 7,354,935
App. No.
10/528,888
Granted
Apr 8, 2008
Kind
B2
Abstract

The present invention is directed to radiolabeled neurokinin-1 receptor antagonists which are useful for the labeling and diagnostic imaging of neurokinin-1 receptors in mammals.

Claims (13)

1. A compound of the formula:

wherein:

A is —CD 2 — or —CH 2 CH 2 —;

or a pharmaceutically acceptable salt thereof.

2. A compound which is:

[ 18 F][2-fluorodideuteromethoxy-5-(5-trifluoromethyl-tetrazol-1-yl)-benzyl]-([2S,3S]-2-phenyl-piperidin-3-yl)-amine;

or a pharmaceutically acceptable salt thereof.

3. A compound which is:

[ 18 F][3-fluoroethoxy-5-(5-trifluoromethyl-tetrazol-1-yl)-benzyl]-([2S,3S]-2-phenyl-piperidin-3-yl)-amine;

or a pharmaceutically acceptable salt thereof.

4. A radiopharmaceutical composition which comprises the compound of claim 1 and a pharmaceutically acceptable carrier or excipient.

5. A method for the imaging of neurokinin-1 receptor in the brain in a mammal which comprises administering to a mammal in need of such diagnostic imaging an effective amount of the compound of claim 1 , and obtaining an image of the brain in the mammal using positron emission tomography.

6. The method of claim 5 wherein the mammal is a human.

Assignments (4)
CHANGE OF NAME Recorded Aug 29, 2012
From: SCHERING CORPORATION
To: MERCK SHARP & DOHME CORP.
Reel/Frame 028866/0511 →
MERGER Recorded Aug 27, 2012
From: MERCK SHARP & DOHME CORP.
To: SCHERING CORPORATION
Reel/Frame 028850/0515 →
CHANGE OF NAME Recorded Jan 29, 2010
From: MERCK & CO., INC.
To: MERCK SHARP & DOHME CORP.
Reel/Frame 023861/0910 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jan 12, 2007
From: BURNS, H. DONALD; GIBSON, RAYMOND E.; ENG, WAI-SI; HAMILL, TERENCE G.
To: MERCK & CO., INC.
Reel/Frame 018764/0353 →