IP Library › Granted Patent US 9,512,105
Granted Patent B2
US 9,512,105 · App. 14/364,003 · Granted Dec 6, 2016

1-substituted 4-arylpiperazine as kappa opioid receptor antagonists

Inventors: Frank I. Carroll (Durham, NC); James B. Thomas (Elfand, NC); Hernan A. Navarro (Chapel Hill, NC); S. Wayne Mascarella (Hillsborough, NC); Scott P. Runyon (Hillsborough, NC); Chunyang Jin (Apex, NC); Chad M. Kormos (Apex, NC)
Assignee: RESEARCH TRIANGLE INSTITUTE
C07D401/12C07D241/04C07D295/13
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Quick Facts
Patent No.
US 9,512,105
App. No.
14/364,003
Granted
Dec 6, 2016
Kind
B2
Abstract

Provided are compounds represented by the formula: where R, Y 3 , R 1 , R 2 , R 3 , R 4 , R 6 , G, R 7 , E 1 , E 2 , A, B, W, X, Y and Z are as defined herein.

Claims (13)

1. A compound represented by the formula:

wherein

W, X, Y and Z are, independently, hydrogen, C 1-3 alkyl, OC 1-3 alkyl, F, OH, Br, Cl, CN, CF 3 , NO 2 , SO 2 CH 3 , SO 2 CF 3 or SO 2 NH 2 .

2. The compound of claim 1 , wherein W, X, Y and Z are, independently, hydrogen, methyl, methoxy, F, Cl or OH.

3. The compound of claim 1 , wherein W, V, X, Y and Z are, independently, hydrogen, methyl, Cl or OH.

4. The compound of claim 1 , wherein W is hydrogen, methyl or Cl.

5. The compound of claim 1 , wherein X is hydrogen, methoxy or OH.

6. The compound of claim 1 , wherein Y is hydrogen, methyl or methoxy.

7. The compound of claim 1 , wherein Z is hydrogen, F, methyl or methoxy.

8. The compound of claim 1 , which is represented by the formula:

9. The compound of claim 1 , which is represented by the formula:

10. The compound of claim 1 , which is a pharmaceutically acceptable salt.

11. A pharmaceutical composition, comprising the compound of claim 1 and a pharmaceutically acceptable carrier.

Assignments (2)
CONFIRMATORY LICENSE Recorded Apr 1, 2015
From: RESEARCH TRIANGLE INSTITUTE
To: NATIONAL INSTITUTES OF HEALTH (NIH), U.S. DEPT. OF HEALTH AND HUMAN SERVICES (DHHS), U.S. GOVERNMENT
Reel/Frame 035357/0126 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 15, 2014
From: CARROLL, FRANK I.; THOMAS, JAMES B.; NAVARRO, HERNAN A.; MASCARELLA, S. WAYNE; RUNYON, SCOTT P.; JIN, CHUNYANG; KORMOS, CHAD M.
To: RESEARCH TRIANGLE INSTITUTE
Reel/Frame 033740/0019 →
Continuity (2)
Provisional Application 61568961 · Dec 9, 2011
Related Publication 20150005315A1 · Jan 1, 2015