IP Library Granted Patent US 8,871,790
Granted Patent B2
US 8,871,790 · App. 13/415,660 · Granted Oct 28, 2014

Heterocyclic modulators of lipid synthesis

Inventors: Johan D. Oslob (Sunnyvale, CA); Robert S. McDowell (San Francisco, CA); Russell Johnson (San Mateo, CA); Hanbiao Yang (Sunnyvale, CA); Marc Evanchik (San Jose, CA); Cristiana A. Zaharia (Redwood City, CA); Haiying Cai (Cupertino, CA); Lily W. Hu (Palo Alto, CA)
Assignee: 3-V Biosciences, Inc.
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Quick Facts
Patent No.
US 8,871,790
App. No.
13/415,660
Granted
Oct 28, 2014
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.

Claims (36)

1. A compound of Structure (IX):

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), —O—(C 1 -C 4 straight or branched alkyl) wherein:

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 hydrogen, halogen or C 1 -C 4 straight or branched alkyl;

R 3 is H, —OH, or halogen;

R 21 is H, halogen, C 1 -C 4 straight or branched alkyl, C 3 -C 5 cycloalkyl wherein the C 3 -C 5 cycloalkyl optionally includes an oxygen or nitrogen heteroatom;

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

R 24 is H, C 1 -C 4 straight or branched alkyl, —(C 1 -C 4 alkyl) t —OH,

—(C 1 -C 4 alkyl) t —O t —(C 3 -C 5 cycloalkyl), or

—(C 1 -C 4 alkyl) t —O—(C 1 -C 4 straight or branched alkyl) wherein:

t is 0 or 1;

the C 3 -C 5 cycloalkyl optionally includes an oxygen or nitrogen heteroatom;

L 1 is N; and

L 2 is N.

2. The compound of claim 1 wherein R 24 is C 1 -C 4 straight or branched alkyl or —(C 1 -C 4 alkyl) t —O—(C 1 -C 4 straight or branched alkyl) wherein t is 0 or 1.

3. The compound of claim 2 wherein R 24 is C 1 -C 4 straight or branched alkyl.

4. The compound of claim 3 wherein R 24 is methyl.

5. The compound of claim 1 wherein R 21 is halogen, C 1 -C 4 straight or branched alkyl or C 3 -C 5 cycloalkyl wherein the C 3 -C 5 cycloalkyl optionally includes an oxygen or nitrogen heteroatom.

6. The compound of claim 5 wherein R 21 is C 3 -C 5 cycloalkyl.

7. The compound of claim 6 l wherein R 21 is cyclobutyl.

8. The compound of claim 1 wherein R 22 is H, methyl or ethyl.

9. The compound of claim 8 wherein R 22 is methyl.

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

11. The compound of claim 10 wherein R 3 is H.

12. The compound of claim 1 wherein each R 2 is H.

13. The compound of claim 1 wherein R 1 is halogen, —CN or C 1 -C 2 haloalkyl.

14. The compound of claim 13 l wherein R 1 is —CN.

15. The compound of claim 1 wherein R 21 is C 1 -C 2 alkyl or C 3 -C 5 cycloalkyl and R 22 is C 1 -C 2 alkyl.

16. The compound of claim 15 wherein R 21 is C 3 -C 5 cycloalkyl and R 22 is C 1 -C 2 alkyl.

17. The compound of claim 16 wherein R 24 is C 1 -C 2 alkyl.

18. The compound of claim 1 wherein R 1 is —CN, each R 2 is H, R 3 is H or F, R 21 is C 3 -C 4 cycloalkyl, R 22 is methyl, and R 24 is methyl, ethyl, hydroxymethyl, methoxymethyl, or 2-methoxyethyl.

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

20. The compound of claim 1 having the following formula:

21. A pharmaceutical composition comprising a compound of claim 1 and a pharmaceutically acceptable carrier, excipient, or diluent.

Assignments (4)
CHANGE OF NAME Recorded Jan 24, 2020
From: 3-V BIOSCIENCES, INC.
To: SAGIMET BIOSCIENCES INC.
Reel/Frame 051695/0631 →
RELEASE OF SECURITY INTEREST Recorded Aug 9, 2019
From: PACIFIC WESTERN BANK
To: 3-V BIOSCIENCES, INC.
Reel/Frame 050014/0541 →
SECURITY INTEREST Recorded Jun 21, 2018
From: 3-V BIOSCIENCES, INC.
To: PACIFIC WESTERN BANK
Reel/Frame 046168/0452 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 16, 2012
From: OSLOB, JOHAN D.; MCDOWELL, ROBERT S.; JOHNSON, RUSSELL; YANG, HANBIAO; EVANCHIK, MARC; ZAHARIA, CRISTIANA A.; CAI, HAIYING; HU, LILY W.
To: 3-V BIOSCIENCES, INC.
Reel/Frame 028560/0125 →
Continuity (4)
Provisional Application 61585642 · Jan 11, 2012
Provisional Application 61508611 · Jul 16, 2011
Provisional Application 61450561 · Mar 8, 2011
Related Publication 20120264737A1 · Oct 18, 2012