IP Library Granted Patent US 10,208,063
Granted Patent B2
US 10,208,063 · App. 14/890,320 · Granted Feb 19, 2019

ACC inhibitors and uses thereof

Inventors: Jeremy Robert Greenwood (Brooklyn, NY); Geraldine C. Harriman (Charlestown, RI); George Borg (Somerville, MA); Craig E. Masse (Cambridge, MA)
Assignee: GILEAD APOLLO, LLC
C07D513/04A01N43/90C07D471/04C07D487/04C07D498/04
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Quick Facts
Patent No.
US 10,208,063
App. No.
14/890,320
Granted
Feb 19, 2019
Kind
B2
Abstract

The present invention provides compounds useful as inhibitors of Acetyl CoA Carboxylase (ACC), compositions thereof, and methods of using the same. Specifically, bicyclic heteroaryl derivatives containing a imidazole, thiazole or oxazole fused to a pyridinone, pyrimidinone or pyrimidindione are provided. These compounds have therapeutic utility toward treating an ACC enzyme mediated disorder such as obesity in a subject, upon administration in an effective amount to said subject.

Claims (14)

1. A compound of formula:

or a pharmaceutically acceptable salt thereof.

2. A composition comprising a compound according to claim 1 and a pharmaceutically acceptable carrier, adjuvant, or vehicle.

3. A method of inhibiting ACC in a biological sample, comprising contacting the biological sample with an effective amount of the compound according to claim 1 .

4. A method of inhibiting ACC in a plant, comprising contacting the plant with an effective amount of the compound according to claim 1 .

5. A method for treating non-alcoholic steatohepatitis (NASH) in a patient in need thereof, comprising administering to said patient an effective amount of the composition according to claim 2 .

6. A method of inhibiting Acetyl-CoA carboxylase (ACC) in a patient in need thereof, comprising administering to said patient an effective amount of the composition according to claim 2 .

7. A method for treating a metabolic disorder susceptible to treatment with an ACC inhibitor in a patient in need thereof, comprising administering to said patient an effective amount of the composition according to claim 2 .

8. The method according to claim 7 , wherein the metabolic disorder is obesity.

9. The method according to claim 8 , wherein the obesity is a symptom of Prader-Willi syndrome, Bardet-Biedl syndrome, Cohen syndrome or Macrosomia, Obesity, Macrocephaly, and Ocular (“MOMO”) syndrome.

10. The method according to claim 8 , wherein the obesity is a side effect of the administration of another medication selected from insulin, a sulfonylurea, a thiazolidinedione, an antipsychotic, an antidepressant, a steroid, an anticonvulsant, pizotifen, and a hormonal contraceptive.

11. The method according to claim 7 , wherein the metabolic disorder is dyslipidemia or hyperlipidemia.

12. A method of treating a cancer or other proliferative disorder susceptible to treatment with an ACC inhibitor in a patient in need thereof, comprising administering to said patient an effective amount of the composition according to claim 2 .

13. A method of treating a fungal, parasitic, or bacterial infection susceptible to treatment with an ACC inhibitor in a patient in need thereof, comprising administering to said patient an effective amount of the composition according to claim 2 .

Assignments (3)
CHANGE OF NAME Recorded Oct 3, 2016
From: GILEAD APOLLO, INC.
To: GILEAD APOLLO, LLC
Reel/Frame 040209/0033 →
MERGER AND CHANGE OF NAME Recorded Jul 27, 2016
From: NIMBUS APOLLO, INC.; GILEAD APOLLO, INC.
To: GILEAD APOLLO, INC.
Reel/Frame 039490/0648 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 18, 2015
From: GREENWOOD, JEREMY ROBERT; HARRIMAN, GERALDINE C.; BORG, GEORGE; MASSE, CRAIG E.
To: NIMBUS APOLLO, INC.
Reel/Frame 037145/0752 →
Continuity (2)
Provisional Application 61821828 · May 10, 2013
Related Publication 20160108061A1 · Apr 21, 2016