IP Library Granted Patent US 8,895,560
Granted Patent B2
US 8,895,560 · App. 14/202,390 · Granted Nov 25, 2014

Opioid antagonists

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Quick Facts
Patent No.
US 8,895,560
App. No.
14/202,390
Granted
Nov 25, 2014
Kind
B2
Abstract

Certain quinolizidine and octahydropyridopyrazine compounds, pharmaceutical compositions, and methods of their use, inter alia, as opioid receptor antagonists are disclosed.

Claims (14)

1. A compound of formula I:

wherein:

R 1 is —C(═O)NH 2 ;

X is N—C(═O)-aryl;

or a pharmaceutically acceptable salt thereof.

2. The compound of claim 1 , wherein said aryl is substituted with halo.

3. The compound of claim 2 , wherein said aryl is substituted with fluoro.

4. A method for binding delta opioid receptors, comprising the step of contacting one or more delta opioid receptors with a compound of formula (I) or a salt thereof in an amount effective to bind to the opioid receptor,

wherein:

R 1 is —C(═O)NH 2 ;

X is N—C(═O)-aryl;

or a pharmaceutically acceptable salt thereof.

5. The method of claim 4 , wherein said aryl is substituted with halo.

6. The method of claim 5 , wherein said aryl is substituted with fluoro.

Assignments (2)
MERGER Recorded Aug 8, 2022
From: MERCK SHARP & DOHME CORP.
To: MERCK SHARP & DOHME LLC
Reel/Frame 061102/0145 →
NUNC PRO TUNC ASSIGNMENT Recorded Jul 9, 2015
From: ADOLOR CORPORATION
To: MERCK SHARP & DOHME CORP.
Reel/Frame 036046/0153 →