IP Library Granted Patent US 9,765,089
Granted Patent B2
US 9,765,089 · App. 14/890,344 · Granted Sep 19, 2017

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
C07D513/04A01N43/90C07D487/04C07D495/04
View Patent ↗
Loading inventors, assignments & file history…
Monitor This Case
Get email alerts when status or documents change.
Order Certified Copies
Most orders are placed with the USPTO same day — all within 24 business hours.
Order via The Patent Place →
Pre-filled with this patent's details
Quick Facts
Patent No.
US 9,765,089
App. No.
14/890,344
Granted
Sep 19, 2017
Kind
B2
Abstract

The present invention provides compounds useful as inhibitors of Acetyl CoA Carboxylase (ACC), compositions thereof, and methods of using the same.

Claims (17)

1. A compound of formula I-h:

or a pharmaceutically acceptable salt thereof, wherein:

R 1 is hydrogen or C 1-4 aliphatic, optionally substituted with one or more halogens, —OR, —SR, —N(R) 2 , —N(R)C(O)R, —C(O)N(R) 2 , —N(R)C(O)N(R) 2 , —N(R)C(O)OR, —OC(O)N(R) 2 , —N(R)SO 2 R, —SO 2 RN(R) 2 , —C(O)R, —C(O)OR, —OC(O)R, —C(O)OR, —S(O)R, or —SO 2 R;

R 2 is selected from 4-8 membered saturated or partially unsaturated monocyclic heterocyclic ring having 1-2 heteroatoms independently selected from nitrogen, oxygen, or sulfur, a 5-6 membered monocyclic heteroaromatic ring having 1-4 heteroatoms independently selected from nitrogen, oxygen, or sulfur, and an 8-10 membered bicyclic heteroaromatic ring having 1-5 heteroatoms independently selected from nitrogen, oxygen, or sulfur;

L 1 is a 1-6 membered straight or branched bivalent hydrocarbon chain optionally substituted with R 5 and R 5′ ;

L 2 is a 1-6 membered straight or branched bivalent hydrocarbon chain optionally substituted with R 7 and R 7′ ;

R 3 is halogen, —CN, —OR, —SR, —N(R) 2 , —N(R)C(O)R, —C(O)N(R) 2 , —C(O)N(R)S(O) 2 R, —N(R)C(O)N(R) 2 , —N(R)C(O)OR, —OC(O)N(R) 2 , —N(R)SO 2 R, —SO 2 N(R) 2 , —C(O)R, —C(O)OR, —OC(O)R, —S(O)R, —SO 2 R, —B(OR) 2 , or an optionally substituted ring selected from phenyl or 5-6 membered heteroaryl having 1-4 heteroatoms independently selected from nitrogen, oxygen, or sulfur;

R 4 is hydrogen or a ring selected from a 3-8 membered monocyclic saturated or partially unsaturated carbocyclic ring, a 4-8 membered monocyclic saturated or partially unsaturated heterocyclic ring having 1-2 heteroatoms independently selected from nitrogen, oxygen, or sulfur, phenyl, an 8-10 membered bicyclic aryl ring, a 5-6 membered monocyclic heteroaryl ring having 1-4 heteroatoms independently selected from nitrogen, oxygen, or sulfur, or an 8-10 membered bicyclic heteroaryl ring having 1-4 heteroatoms independently selected from nitrogen, oxygen, or sulfur; wherein said ring is optionally substituted with n instances of R 8 ;

each of R 5 and R 5′ is independently —R, —OR, —SR, —N(R) 2 , —N(R)C(O)R, —C(O)N(R) 2 , —N(R)C(O)N(R) 2 , —N(R)C(O)OR, —OC(O)N(R) 2 , —N(R)SO 2 R, —SO 2 N(R) 2 , —C(O)R, —C(O)OR, —OC(O)R, —S(O)R, or —SO 2 R; or R 5 and R 5′ are taken together to form a cyclopropylenyl, cyclobutylenyl, or oxetanyl group;

each of R 7 and R 7′ is independently, —R, —OR 6 , —SR, —N(R) 2 , —N(R)C(O)R, —C(O)N(R) 2 , —N(R)C(O)N(R) 2 , —N(R)C(O)OR, —OC(O)N(R) 2 , —N(R)SO 2 R, —SO 2 N(R) 2 , —C(O)R, —C(O)OR, —OC(O)R, —S(O)R, —SO 2 R, or —B(OR) 2 ; or R 7 and R 7′ are taken together to form a 3-8 membered saturated or partially unsaturated monocyclic carbocyclic ring, or a 4-8 membered saturated or partially unsaturated monocyclic heterocyclic ring having 1-2 heteroatoms independently selected from nitrogen, oxygen, or sulfur;

R 6 is —R, —C(O)N(R) 2 , or —C(O)R;

each R 8 is independently selected from halogen, —R, —OR, —SR, —N(R) 2 or deuterium;

each R is independently hydrogen, deuterium, or an optionally substituted group selected from C 1-6 aliphatic, a 3-8 membered saturated or partially unsaturated monocyclic carbocyclic ring, phenyl, and 8-10 membered bicyclic aromatic carbocyclic ring; a 4-8 membered saturated or partially unsaturated monocyclic heterocyclic ring having 1-2 heteroatoms independently selected from nitrogen, oxygen, or sulfur, a 5-6 membered monocyclic heteroaromatic ring having 1-4 heteroatoms independently selected from nitrogen, oxygen, or sulfur, or an 8-10 membered bicyclic heteroaromatic ring having 1-5 heteroatoms independently selected from nitrogen, oxygen, or sulfur; and

n is 0-5.

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

3. A compound of formula:

or a pharmaceutically acceptable salt thereof.

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 037075/0636 →
Continuity (2)
Provisional Application 61821829 · May 10, 2013
Related Publication 20160185799A1 · Jun 30, 2016