IP Library Granted Patent US 8,431,582
Granted Patent B2
US 8,431,582 · App. 13/571,667 · Granted Apr 30, 2013

Inhibitors of fatty acid uptake and methods of use

Inventors: Concetta DiRusso (Lincoln, NE); Paul Black (Lincoln, NE)
Assignee: NUtech Ventures
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Quick Facts
Patent No.
US 8,431,582
App. No.
13/571,667
Granted
Apr 30, 2013
Kind
B2
Abstract

The present disclosure describes inhibitors of fatty acid uptake and methods of using such inhibitors. Specifically, the present disclosure describes inhibitors with specificity for FATP2.

Claims (39)

1. A method of inhibiting fatty acid uptake by cells, comprising:

contacting said cells with a compound having the formula:

or a pharmaceutically acceptable salt form thereof, wherein:

R 1 is H or NO 2 ; and

R 2 is selected from the group consisting of: H, Cl, and OCH 3 .

2. The method of claim 1 , wherein said cells are selected from the group consisting of intestinal epithelial cells and hepatocytes.

3. The method of claim 1 , wherein said contacting is in vitro.

4. The method of claim 1 , wherein said inhibition is reversible.

5. The method of claim 1 , wherein R 1 is NO 2 .

6. The method of claim 1 , wherein R 2 is Cl.

7. The method of claim 1 , wherein the compound is selected from the group consisting of:

or a pharmaceutically acceptable salt form thereof.

8. The method of claim 1 , wherein the compound is:

or a pharmaceutically acceptable salt form thereof.

9. A method of treating a disease selected from the group consisting of obesity, metabolic syndrome, insulin resistant diabetes, cardiovascular disease, and non-alcoholic fatty liver disease in an individual, comprising:

administering, to said individual, a compound having the formula:

or a pharmaceutically acceptable salt form thereof, wherein:

R 1 is H or NO 2 ; and

R 2 is selected from the group consisting of: H, CI, and OCH 3 .

10. The method of claim 9 , wherein R 1 is NO 2 .

11. The method of claim 9 , wherein R 2 is Cl.

12. The method of claim 9 , wherein the compound is selected from the group consisting of:

or a pharmaceutically acceptable salt form thereof.

13. The method of claim 9 , wherein the compound is:

or a pharmaceutically acceptable salt form thereof.

14. A method of inhibiting FATP2 in a cell, the method comprising:

contacting said cell with a compound having the formula:

or a pharmaceutically acceptable salt form thereof, wherein:

R 1 is H or NO 2 ; and

R 2 is selected from the group consisting of: H, Cl, and OCH 3 .

15. The method of claim 14 , wherein said cell is selected from the group consisting of intestinal epithelial cells and hepatocytes.

16. The method of claim 14 , wherein said contacting is in vitro.

17. The method of claim 14 , wherein said inhibition is reversible.

18. The method of claim 14 , wherein R 1 is NO 2 .

19. The method of claim 14 , wherein R 2 is Cl.

20. The method of claim 14 , wherein the compound is selected from the group consisting of:

or a pharmaceutically acceptable salt form thereof.

21. The method of claim 14 , wherein the compound is:

or a pharmaceutically acceptable salt form thereof.

Assignments (5)
GOVERNMENT INTEREST AGREEMENT Recorded Mar 19, 2018
From: NATIONAL INSTITUTES OF HEALTH
To: NATIONAL INSTITUTES OF HEALTH
Reel/Frame 045629/0922 →
CONFIRMATORY LICENSE Recorded Sep 18, 2015
From: UNIVERSITY OF NEBRASKA-LINCOLN / NUTECH VENTURES
To: NATIONAL INSTITUTES OF HEALTH - DIRECTOR DEITR
Reel/Frame 036598/0121 →
CONFIRMATORY LICENSE Recorded Aug 5, 2013
From: BOARD OF REGENTS ON BEHALF OF THE UNIVERSITY OF NEBRASKA LINCOLN
To: NATIONAL INSTITUTES OF HEALTH (NIH), U.S. DEPT. OF HEALTH AND HUMAN SERVICES (DHHS), U.S. GOVERNMENT
Reel/Frame 030955/0357 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Dec 13, 2012
From: DIRUSSO, CONCETTA; BLACK, PAUL
To: BOARD OF REGENTS OF THE UNIVERSITY OF NEBRASKA
Reel/Frame 029458/0630 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Dec 13, 2012
From: BOARD OF REGENTS OF THE UNIVERSITY OF NEBRASKA
To: NUTECH VENTURES
Reel/Frame 029458/0655 →
Continuity (3)
Continuation 12791323 · Jun 1, 2010
Provisional Application 61217498 · Jun 1, 2009
Related Publication 20120309772A1 · Dec 6, 2012