IP Library Granted Patent US 11,622,968
Granted Patent B2
US 11,622,968 · App. 16/838,753 · Granted Apr 11, 2023

Heterocyclic modulators of lipid synthesis

Inventors: Douglas Buckley (San Mateo, CA); Gregory Duke (San Mateo, CA); Allan S. Wagman (San Maeo, CA); Marc Evanchik (San Jose, CA); Robert S. McDowell (San Francisco, CA)
Assignee: Sagimet Biosciences Inc.
A61K31/55A61K31/437A61K31/451A61K31/453A61K31/454A61K31/4525A61K31/4545A61K31/496A61K31/501A61K31/506A61K31/5377C07D401/04C07D401/06C07D401/10C07D401/12C07D401/14C07D405/04C07D405/10C07D405/12C07D405/14C07D413/10C07D413/14C07D471/04C07D487/04C07D491/048C07D491/052C07D491/10C07D491/107C07D513/04
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Quick Facts
Patent No.
US 11,622,968
App. No.
16/838,753
Granted
Apr 11, 2023
Kind
B2
Abstract

Compounds that are fatty acid synthesis modulators are provided. The compounds may be used to treat disorders characterized by disregulation of the fatty acid synthase function by modulating the function and/or the fatty acid synthase pathway. Methods are provided for treating such disorders including viral infections, such as hepatitis C infection, cancer and metabolic disorders, such as non-alcoholic steatohepatitis (NASH).

Claims (31)

1. A compound having Structure (VI-J):

or a pharmaceutically acceptable salt thereof, wherein:

R 1 is H, —CN, halogen, C 1 -C 4 straight or branched alkyl, —O—(C 3 -C 5 cycloalkyl), or —O—(C 1 -C 4 straight or branched alkyl), wherein:

the C 3 -C 5 cycloalkyl optionally includes an oxygen or nitrogen heteroatom; and when R 1 is not H, —CN or halogen, it is optionally substituted with one or more halogens;

each R 2 is independently H, halogen or C 1 -C 4 straight or branched alkyl;

R 3 is H, —OH, or halogen;

R 21 is cyclobutyl, azetidin-1-yl, or cyclopropyl;

R 22 is H, halogen, or C 1 -C 2 alkyl;

R 35 is —C(O)—R 351 , —C(O)—NHR 351 , —C(O)—O—R 351 or S(O) 2 R 351 ; and

R 351 is C 1 -C 6 straight or branched alkyl, cycloalkyl, heterocyclyl, aryl or heteroaryl, wherein alkyl is optionally substituted with one or two substituents selected from cycloalkyl, heterocycle, aryl, and heteroaryl.

2. The compound of claim 1 , wherein R 3 is H or halogen.

3. The compound of claim 2 , wherein R 21 is cyclobutyl.

4. The compound of claim 3 , wherein R 1 is —CN.

5. The compound of claim 4 , wherein R 22 is H.

6. The compound of claim 5 , wherein R 35 is —C(O)—NH—R 351 .

7. The compound of claim 6 , wherein R 351 is (R)-3-tetrahydrofuranyl, (S)-3-tetrahydrofuranyl, (R)-(tetrahydrofuran-2-yl)methyl or (S)-(tetrahydrofuran-2-yl)methyl.

8. The compound of claim 5 , wherein R 35 is —C(O)—O—R 351 .

9. The compound of claim 8 , wherein R 351 is (R)-3-tetrahydrofuranyl or (S)-3-tetrahydrofuranyl.

10. The compound of claim 1 , having a formula selected from the group consisting of:

11. The compound of claim 6 , wherein R 351 is C 1 -C 6 straight or branched alkyl optionally substituted with one or two substituents selected from cycloalkyl, heterocycle, aryl, and heteroaryl.

12. The compound of claim 6 , wherein R 351 is (R)-(tetrahydrofuran-2-yl)methyl or (S) (tetrahydrofuran-2-yl)methyl.

13. The compound of claim 6 , wherein is R 351 is cycloalkyl, heterocyclyl, aryl or heteroaryl.

14. The compound of claim 1 , wherein R 35 is —C(O)—NH—R 351 .

15. The compound of claim 14 , wherein R 351 is C 1 -C 6 straight or branched alkyl optionally substituted with one or two substituents selected from cycloalkyl, heterocycle, aryl, and heteroaryl.

16. The compound of claim 14 , wherein R 351 is (R)-(tetrahydrofuran-2-yl)methyl or (S)-(tetrahydrofuran-2-yl)methyl.

17. The compound of claim 1 , having a formula selected from

or a pharmaceutically acceptable salt thereof.

18. The compound of claim 1 , having a formula selected from

or a pharmaceutically acceptable salt thereof.

19. The compound of claim 1 , having a formula selected from

or a pharmaceutically acceptable salt thereof.

Assignments (3)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Apr 15, 2020
From: BUCKLEY, DOUGLAS I.; DUKE, GREGORY; WAGMAN, ALLAN S.
To: 3-V BIOSCIENCES, INC.
Reel/Frame 052405/0367 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Apr 15, 2020
From: EVANCHIK, MARC; MCDOWELL, ROBERT S.
To: 3-V BIOSCIENCES, INC.
Reel/Frame 052405/0488 →
CHANGE OF NAME Recorded Apr 15, 2020
From: 3-V BIOSCIENCES, INC.
To: SAGIMET BIOSCIENCES INC.
Reel/Frame 052408/0556 →
Continuity (18)
Continuation 16157672 · Oct 11, 2018
Continuation 15349960 · Nov 11, 2016
Continuation In Part 15110154
Continuation In Part 15201824 · Jul 5, 2016
Division 14587908 · Dec 31, 2014
Continuation PCTUS2013048950 · Jul 1, 2013
Continuation In Part 14874961 · Oct 5, 2015
Continuation 14315133 · Jun 25, 2014
Continuation 13415660 · Mar 8, 2012
Provisional Application 61924520 · Jan 7, 2014
Provisional Application 61785933 · Mar 14, 2013
Provisional Application 61699819 · Sep 11, 2012
Provisional Application 61698511 · Sep 7, 2012
Provisional Application 61667894 · Jul 3, 2012
Provisional Application 61585642 · Jan 11, 2012
Provisional Application 61508611 · Jul 16, 2011
Provisional Application 61450561 · Mar 8, 2011
Related Publication 20220296605A1 · Sep 22, 2022
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