IP Library Patent Application 15999505
Patent Application
App. No. 15/999,505

Triazole ACC inhibitors and uses thereof

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Quick Facts
Patent No.
US None
App. No.
15/999,505
Abstract

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

Claims (20)

1 . A compound of formula I:

or a pharmaceutically acceptable salt or agriculturally acceptable salt thereof, wherein:

X is —O—, —S—, or —NR—;

R 1 is hydrogen, C 1-4 aliphatic optionally substituted with 1-4 halogen, —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)S(O) 2 R, —S(O) 2 N(R) 2 , —C(O)R, —C(O)OR, —OC(O)R, —S(O)R, or —S(O) 2 R;

each instance of R 2 , R 6 , R 7 , and R 8 is independently oxo; halogen; —CN; —OR; —R a , —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)S(O) 2 R; —S(O) 2 N(R) 2 ; —C(O)R; —C(O)OR; —OC(O)R; —S(O)R; or —S(O) 2 R;

each R is independently hydrogen or R a ;

each R a is independently an optionally substituted group selected from C 1-6 aliphatic, a 3-8 membered saturated or partially unsaturated monocyclic carbocyclic ring, phenyl, an 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;

L 1 is a covalent bond; a 1-6 membered straight or branched bivalent hydrocarbon chain; cyclopropylenyl; cyclobutylenyl; or oxetanylenyl;

L 2 is a covalent bond or a 1-6 membered straight or branched bivalent hydrocarbon chain; wherein L 2 is substituted by n instances of R 9 ;

R 3 is —OR, —C(O)OR, —N(R)C(O)OR, —OC(O)N(R) 2 , —C(O)N(R)OR, —C(O)NH 2 , —C(O)NHR a , C(O)N(R a ) 2 , or —C(O)Hy;

Hy is a 3-8 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; wherein Hy is substituted by p instances of R 6 ;

R 4 is 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, and an 8-10 membered bicyclic heteroaryl ring having 1-4 heteroatoms independently selected from nitrogen, oxygen, or sulfur; wherein R 4 is substituted by q instances of R 7 ;

each R 5 is independently hydrogen, C 1-4 aliphatic, 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 each R 5 is substituted with r instances of R 8 ;

each R 9 is independently oxo or —OR 5 ;

m is 0, 1, 2, or 3;

n is 0, 1, or 2;

p is 0, 1, 2, 3, or 4;

q is 0, 1, 2, 3, 4, or 5; and

r is 0, 1, 2, 3, or 4.

2 .- 26 . (canceled)

Assignments (9)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 18, 2019
From: NIMBUS DISCOVERY, INC.
To: NIMBUS APOLLO, INC.
Reel/Frame 049504/0948 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 18, 2019
From: SCHRÖDINGER, INC.
To: SCHRÖDINGER, L.L.C.
Reel/Frame 049505/0006 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 18, 2019
From: SCHRÖDINGER, L.L.C.
To: NIMBUS DISCOVERY, INC.
Reel/Frame 049505/0061 →
CHANGE OF NAME Recorded Jun 18, 2019
From: NIMBUS APOLLO, INC.
To: GILEAD APOLLO, INC.
Reel/Frame 049510/0756 →
CHANGE OF NAME Recorded Jun 18, 2019
From: GILEAD APOLLO, INC.
To: GILEAD APOLLO, LLC
Reel/Frame 049510/0835 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Apr 25, 2019
From: GHOSH, SHOMIR
To: NIMBUS APOLLO, INC.
Reel/Frame 048999/0206 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Apr 25, 2019
From: GREENWOOD, JEREMY ROBERT
To: SCHRODINGER, INC.
Reel/Frame 048999/0262 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Apr 25, 2019
From: DE MORADEI, SILVANA MARCEL LEIT
To: NIMBUS APOLLO, INC.
Reel/Frame 049001/0502 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Apr 25, 2019
From: HARRIMAN, GERALDINE C.
To: NIMBUS DISCOVERY, INC.
Reel/Frame 049007/0964 →