IP Library Granted Patent US 10,081,616
Granted Patent B2
US 10,081,616 · App. 15/504,223 · Granted Sep 25, 2018

Soluble epoxide hydrolase inhibitors and uses thereof

Inventors: Ying Zhang (Lexington, MA); Anthony D. Keefe (Cambridge, MA); Christoph Dumelin (Zurich, CH)
C07D401/12A61K31/4412C07D213/81
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Quick Facts
Patent No.
US 10,081,616
App. No.
15/504,223
Granted
Sep 25, 2018
Kind
B2
Abstract

The present invention features compounds having soluble epoxide hydrolase inhibitory activity. The compounds of the invention, alone or in combination with other pharmaceutically active agents, can be used for treating or preventing various medical conditions, such as cardiovascular diseases, respiratory diseases, inflammation, and diabetes.

Claims (21)

1. A compound having the structure:

wherein one of X 1 or X 2 is N and the other is CH;

R 1 is hydrogen, C 1 -C 6 acyl, C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, C 1 -C 6 heteroalkyl, C 2 -C 6 heteroalkenyl, C 2 -C 6 heteroalkynyl, C 3 -C 10 carbocyclyl, C 6 -C 10 aryl, C 6 -C 10 aryl C 1 -C 6 alkyl, C 2 -C 9 heterocyclyl, or C 2 -C 9 heterocyclyl C 1 -C 6 alkyl;

R 2 is hydrogen or C 1 -C 6 alkyl;

R 3 is C(O)NHR 4 ; and

R 4 is hydrogen, C 1 -C 6 acyl, C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, C 1 -C 6 heteroalkyl, C 2 -C 6 heteroalkenyl, C 2 -C 6 heteroalkynyl, C 3 -C 10 carbocyclyl, C 6 -C 10 aryl, C 6 -C 10 aryl C 1 -C 6 alkyl, C 2 -C 9 heterocyclyl, C 2 -C 9 heterocyclyl C 1 -C 6 alkyl;

or a pharmaceutically acceptable salt thereof.

2. The compound of claim 1 , wherein said compound has the structure:

3. The compound of claim 1 , wherein R 4 is C 3 -C 10 carbocyclyl or C 6 -C 10 aryl C 1 -C 6 alkyl.

4. The compound of claim 3 , wherein R 4 is C 3 -C 10 carbocyclyl.

5. The compound of claim 4 , wherein said C 3 -C 10 carbocyclyl is cyclohexyl.

6. The compound of claim 3 , wherein R 4 is C 6 -C 10 aryl C 1 -C 6 alkyl.

7. The compound of claim 6 , wherein said C 6 -C 10 aryl C 1 -C 6 alkyl is benzyl.

8. The compound of claim 1 , wherein R 2 is C 1 -C 6 alkyl.

9. The compound of claim 8 , wherein said C 1 -C 6 alkyl is methyl.

10. The compound of claim 1 , wherein X 1 is N and X 2 is CH.

11. The compound of claim 1 , wherein X 1 is CH and X 2 is N.

12. The compound of claim 1 , wherein R 1 is C 2 -C 9 heterocyclyl C 1 -C 6 alkyl.

13. A compound having the structure:

or a pharmaceutically acceptable salt thereof.

14. A pharmaceutical composition comprising the compound of claim 1 and a pharmaceutically acceptable excipient.

Assignments (2)
SECURITY INTEREST Recorded Dec 11, 2020
From: X-CHEM, INC.
To: MIDCAP FINANCIAL TRUST
Reel/Frame 054619/0407 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 25, 2018
From: ZHANG, YING; KEEFE, ANTHONY D.; DUMELIN, CHRISTOPH
To: X-CHEM, INC.
Reel/Frame 046964/0523 →
Continuity (2)
Provisional Application 62043275 · Aug 28, 2014
Related Publication 20170240526A1 · Aug 24, 2017