IP Library Granted Patent US 8,987,303
Granted Patent B2
US 8,987,303 · App. 13/801,030 · Granted Mar 24, 2015

AMPK-activating heterocyclic compounds and methods for using the same

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Quick Facts
Patent No.
US 8,987,303
App. No.
13/801,030
Granted
Mar 24, 2015
Kind
B2
Abstract

Disclosed are substituted pyridine compounds as well as pharmaceutical compositions and methods of use. One embodiment is a compound having the structure wherein E, J, T, the ring system denoted by “B”, T, R 3 , R 4 , w and x are as described herein. In certain embodiments, a compound disclosed herein activates the AMPK pathway, and can be used to treat metabolism-related disorders and conditions.

Claims (30)

1. N-((trans)-1-(4-cyanobenzyl)-3-fluoropiperidin-4-yl)-6-(4-(4-methoxybenzoyl)piperidine-1-carbonyl)nicotinamide or a pharmaceutically acceptable salt or N-oxide thereof.

2. A pharmaceutical composition comprising:

at least one pharmaceutically acceptable carrier, diluent or excipient; and

a compound according to claim 1 or a pharmaceutically acceptable salt or N-oxide thereof.

3. A method for activating the AMPK pathway in a cell, the method comprising contacting the cell with an effective amount of a compound according to claim 1 or a pharmaceutically acceptable salt or N-oxide thereof.

4. A method for treating type II diabetes in a subject, the method comprising administering to the subject an effective amount of a compound according to claim 1 or a pharmaceutically acceptable salt or N-oxide thereof.

5. A method for treating atherosclerosis in a subject, the method comprising administering to the subject an effective amount of a compound according to claim 1 or a pharmaceutically acceptable salt or N-oxide thereof.

6. A method for improving exercise efficiency in a subject, the method comprising administering to the subject an effective amount of a compound according to claim 1 or a pharmaceutically acceptable salt or N-oxide thereof.

7. A method for treating intermittent claudication, the method comprising administering to the subject an effective amount of a compound according to claim 1 or a pharmaceutically acceptable salt or N-oxide thereof.

8. The compound of claim 1 , having the structural formula

9. A pharmaceutical composition comprising:

at least one pharmaceutically acceptable carrier, diluent or excipient; and

a compound according to claim 8 or a pharmaceutically acceptable salt or N-oxide thereof.

10. A method for activating the AMPK pathway in a cell, the method comprising contacting the cell with an effective amount of a compound according to claim 8 or a pharmaceutically acceptable salt or N-oxide thereof.

11. A method for treating type II diabetes in a subject, the method comprising administering to the subject an effective amount of a compound according to claim 8 or a pharmaceutically acceptable salt or N-oxide thereof.

12. A method for treating atherosclerosis in a subject, the method comprising administering to the subject an effective amount of a compound according to claim 8 or a pharmaceutically acceptable salt or N-oxide thereof.

13. A method for improving exercise efficiency in a subject, the method comprising administering to the subject an effective amount of a compound according to claim 8 or a pharmaceutically acceptable salt or N-oxide thereof.

14. A method for treating intermittent claudication, the method comprising administering to the subject an effective amount of a compound according to claim 8 or a pharmaceutically acceptable salt or N-oxide thereof.

15. The compound of claim 1 , having the structural formula

16. A pharmaceutical composition comprising:

at least one pharmaceutically acceptable carrier, diluent or excipient; and

a compound according to claim 15 or a pharmaceutically acceptable salt or N-oxide thereof.

17. A method for activating the AMPK pathway in a cell, the method comprising contacting the cell with an effective amount of a compound according to claim 15 or a pharmaceutically acceptable salt or N-oxide thereof.

18. A method for treating type II diabetes in a subject, the method comprising administering to the subject an effective amount of a compound according to claim 15 or a pharmaceutically acceptable salt or N-oxide thereof.

19. A method for treating atherosclerosis in a subject, the method comprising administering to the subject an effective amount of a compound according to claim 15 or a pharmaceutically acceptable salt or N-oxide thereof.

20. A method for improving exercise efficiency in a subject, the method comprising administering to the subject an effective amount of a compound according to claim 15 or a pharmaceutically acceptable salt or N-oxide thereof.

21. A method for treating intermittent claudication, the method comprising administering to the subject an effective amount of a compound according to claim 15 or a pharmaceutically acceptable salt or N-oxide thereof.

22. A compound according to claim 1 , wherein the compound is racemic.

23. A compound according to claim 8 , wherein the compound is substantially enantiomerically pure.

24. A compound according to claim 15 , wherein the compound is substantially enantiomerically pure.

Assignments (3)
SECURITY INTEREST Recorded May 8, 2026
From: RIGEL PHARMACEUTICALS, INC.
To: MIDCAP FUNDING IV TRUST
Reel/Frame 075576/0880 →
SECURITY INTEREST Recorded Aug 25, 2022
From: RIGEL PHARMACEUTICALS, INC.
To: MIDCAP FINANCIAL TRUST
Reel/Frame 061327/0712 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 25, 2013
From: GOFF, DANE; PAYAN, DONALD; SINGH, RAJINDER; SHAW, SIMON; CARROLL, DAVID; HITOSHI, YASUMICHI
To: RIGEL PHARMACEUTICALS, INC.
Reel/Frame 030078/0988 →