IP Library Granted Patent US 9,469,629
Granted Patent B2
US 9,469,629 · App. 14/304,163 · Granted Oct 18, 2016

NK

Inventors: Anandan Palani (Bridgewater, NJ); Xianhai Huang (Warren, NJ); Dong Xiao (Warren, NJ); Sunil Paliwal (Monroe Township, NJ); Hon-Chung Tsui (East Brunswick, NJ); Michelle Laci Wrobleski (Whitehouse Station, NJ); Ashwin U. Rao (Avenel, NJ); Cheng Wang (King of Prussia, PA); Sapna S. Shah (Jamesburg, NJ); Neng-Yang Shih (Warren, NJ)
Assignee: OPKO Health, Inc.
C07D417/04A61K31/451A61K31/454A61K31/4523A61K31/4545A61K45/06C07D211/60C07D211/66C07D211/76C07D401/04C07D413/04C07D498/20
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Quick Facts
Patent No.
US 9,469,629
App. No.
14/304,163
Granted
Oct 18, 2016
Kind
B2
Abstract

A compound having the general structure shown in Formula I: or pharmaceutically acceptable salts and/or solvates thereof are useful in treating diseases or conditions mediated by NK 1 receptors, for example various physiological disorders, symptoms or diseases, including emesis, depression, anxiety and cough.

Claims (18)

1. A compound selected from

or a pharmaceutically acceptable salt thereof.

2. The compound of claim 1 having the following structure:

3. The compound of claim 1 having the following structure:

4. The compound of claim 1 having the following structure:

5. The compound of claim 1 having the following structure:

6. The compound of claim 1 having the following structure:

7. The compound of claim 1 having the following structure:

8. The compound of claim 1 having the following structure:

9. A pharmaceutical composition comprising:

at least one compound of claim 1 or a pharmaceutically acceptable salt and/or solvate thereof, and at least one pharmaceutically acceptable carrier.

10. A pharmaceutical composition comprising a pharmaceutically acceptable carrier, at least one serotonin reuptake inhibitor, and at least one compound of claim 1 .

11. A kit, comprising:

two or more separate containers in a single package, wherein each container comprises a pharmaceutical composition;

wherein a first container of said package comprises a first pharmaceutical composition comprising an effective amount of a compound of claim 1 and/or a pharmaceutically acceptable salt and/or solvate thereof in a pharmaceutically acceptable carrier,

a second container of said package comprises a second pharmaceutical composition comprising another therapeutic agent in a pharmaceutically acceptable carrier, and

the other therapeutic agent is selected from the group consisting of SSRIs, other types of NK 1 receptor antagonists, prostanoids, H 1 receptor antagonists, α-adrenergic receptor agonists, dopamine receptor agonists, melanocortin receptor agonists, endothelin receptor antagonists, endothelin converting enzyme inhibitors, angiotensin II receptor antagonists, angiotensin converting enzyme inhibitors, neutral metalloendopeptidase inhibitors, ETA antagonists, renin inhibitors, serotonin 5-HT 3 receptor antagonists, serotonin 5-HT 2c receptor agonists, nociceptin receptor agonists, glucocorticoids, rho kinase inhibitors, potassium channel modulators and inhibitors of multi-drug resistance protein 5.

12. A purified compound according to claim 1 .

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 10, 2016
From: SCHERING CORPORATION
To: OPKO HEALTH, INC.
Reel/Frame 039395/0167 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 10, 2016
From: PALANI, ANANDAN; HUANG, XIANHAI; XIAO, DONG; PALIWAL, SUNIL; TSUI, HON-CHUNG; WROBLESKI, MICHELLE LACI; RAO, ASHWIN U.; WANG, CHENG; SHAH, SAPNA S.; SHIH, NENG-YANG
To: SCHERING CORPORATION
Reel/Frame 039710/0273 →
Continuity (5)
Continuation 13245403 · Sep 26, 2011
Continuation 12750420 · Mar 30, 2010
Division 11172289 · Jun 30, 2005
Provisional Application 60584502 · Jul 1, 2004
Related Publication 20140296196A1 · Oct 2, 2014