IP Library Granted Patent US 8,263,640
Granted Patent B2
US 8,263,640 · App. 12/791,323 · Granted Sep 11, 2012

Inhibitors of fatty acid uptake and methods of use

Assignee: NUtech Ventures
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Quick Facts
Patent No.
US 8,263,640
App. No.
12/791,323
Granted
Sep 11, 2012
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 (31)

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

contacting said cells with a compound of Formula (IV):

or a pharmaceutically acceptable salt form thereof, wherein:

R 1 and R 2 are independently selected from the group consisting of: H, F, Cl, Br, I, OH, and O(C 1-6 alkyl).

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 R 1 is selected from H and OH.

4. The method of claim 1 , wherein R 2 is selected from H and Br.

5. The method of claim 1 , wherein a compound of Formula (IV) is selected from the group consisting of:

or a pharmaceutically acceptable salt form thereof.

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

contacting said cells with a compound selected from the group consisting of:

or a pharmaceutically acceptable salt form thereof.

7. The method of claim 6 , wherein said cells are selected from the group consisting of intestinal epithelial cells and hepatocytes.

8. A method of treating a disease associated with dyslipidemias and lipotoxicity in an individual in need thereof, comprising: administering, to the individual, a compound of Formula (IV):

or a pharmaceutically acceptable salt form thereof, wherein:

R 1 and R 2 are independently selected from the group consisting of: H, F, Cl, Br, I, OH, and O(C 1-6 alkyl).

9. The method of claim 8 , wherein said disease is selected from the group consisting of obesity, metabolic syndrome, insulin resistant diabetes, cardiovascular disease, and non-alcoholic fatty liver disease.

10. A method of treating a disease associated with dyslipidemias and lipotoxicity in an individual in need thereof, comprising:

Administering, to the individual, a compound selected from the group consisting of:

or a pharmaceutically acceptable salt form thereof.

11. The method of claim 10 , wherein said disease is selected from the group consisting of obesity, metabolic syndrome, insulin resistant diabetes, cardiovascular disease, and non-alcoholic fatty liver disease.

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

contacting said cell with a compound of Formula (IV):

or a pharmaceutically acceptable salt form thereof, wherein:

R 1 and R 2 are independently selected from the group consisting of: H, F, Cl, Br, I, OH, and O(C 1-6 alkyl).

13. The method of claim 12 , wherein said cell is selected from the group consisting of intestinal epithelial cells and hepatocytes.

14. The method of claim 12 , wherein R 1 is selected from H and OH.

15. The method of claim 12 , wherein R 2 is selected from H and Br.

16. The method of claim 12 , wherein a compound of Formula (IV) is selected from the group consisting of:

or a pharmaceutically acceptable salt form thereof.

17. The method of claim 12 , wherein said contacting is in vitro.

Assignments (3)
CONFIRMATORY LICENSE Recorded Aug 31, 2010
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 024913/0420 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 26, 2010
From: DIRUSSO, CONCETTA; BLACK, PAUL
To: BOARD OF REGENTS OF THE UNIVERSITY OF NEBRASKA
Reel/Frame 024739/0362 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 26, 2010
From: BOARD OF REGENTS OF THE UNIVERSITY OF NEBRASKA
To: NUTECH VENTURES
Reel/Frame 024739/0389 →
Continuity (2)
Provisional Application 61217498 · Jun 1, 2009
Related Publication 20100305106A1 · Dec 2, 2010