IP Library Granted Patent US 11,858,938
Granted Patent B2
US 11,858,938 · App. 17/071,273 · Granted Jan 2, 2024

Imidazo-fused heterocycles and uses thereof

Inventor: Lin Zhi (San Diego, CA)
Assignee: Ligand Pharmaceuticals, Inc.
C07D487/04
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Quick Facts
Patent No.
US 11,858,938
App. No.
17/071,273
Granted
Jan 2, 2024
Kind
B2
Abstract

Compounds and methods in the fields of chemistry and medicine are disclosed. Some of the disclosed embodiments include compounds, compositions and methods of using imidazole-fused heterocycle amines. Some of the disclosed embodiments include imidazo-fused heterocycle compounds useful to treat leukemia and other hematopoietic disorders.

Claims (27)

1. A compound of Formula (III):

or a pharmaceutically acceptable salt, ester, amide, or prodrug thereof,

wherein

R 1 is selected from the group consisting of an optionally substituted (5 to 7 membered heterocyclyl)alkyl, an optionally substituted aralkyl; and an optionally substituted (5 or 6 membered heteroaryl)alkyl;

each of R 2 , R 3 , and R 4a is independently selected from the group consisting of hydrogen, halogen, C 1-6 alkyl, OH, and C 1-6 alkoxy;

each of R 5a and R 5b is independently selected from the group consisting of hydrogen, halogen, —OR 6 , —CN, —NR 7 R 8 , —CH 2 OR 6 , an optionally substituted aryl, an optionally substituted 5 to 10 membered heteroaryl, an optionally substituted 5-10 membered heterocyclyl, an optionally substituted C 3-7 carbocyclyl, an optionally substituted C 1-6 alkyl, an optionally substituted C 1-6 haloalkyl, an optionally substituted C 1-6 heteroalkyl, —C(═O)R 6 , —C(═O)OR 6 , —C(═O)NR 7 R 8 , —NHC(═O)R 6 , —SO 2 R 6 , and —SO 2 NR 7 R 8 ;

each R 6 is independently hydrogen, an optionally substituted C 1-10 alkyl, an optionally substituted C 1-10 haloalkyl, or an optionally substituted C 1-6 heteroalkyl; and

each R 7 and R 8 is independently selected from hydrogen; an optionally substituted C 1-10 alkyl; an optionally substituted C 1-10 haloalkyl; or an optionally substituted C 1-6 heteroalkyl; or R 7 and R 8 are joined together with the nitrogen atom to which they are attached to form an optionally substituted C 3-7 cycloalkyl or 3 to 7 membered heterocyclyl ring.

2. The compound of claim 1 , wherein each of R 4a and R 5a is hydrogen.

3. The compound of claim 1 , wherein R 1 is an optionally substituted (5 to 7 membered heterocyclyl)alkyl.

4. The compound of claim 3 , wherein R 1 is an optionally substituted (5 membered heterocyclyl)alkyl.

5. The compound of claim 4 , wherein R 1 is pyrrolidyl-CH 2 —.

6. The compound of claim 3 , wherein R 1 is an optionally substituted (6 membered heterocyclyl)alkyl.

7. The compound of claim 6 , wherein R 1 is piperidinyl-CH 2 — or morpholine-CH 2 —.

8. The compound of claim 1 , wherein R 2 is hydrogen.

9. The compound of claim 1 , wherein R 3 is hydrogen.

10. The compound of claim 1 , wherein R 5b is an optionally substituted 5 to 10 membered heteroaryl.

11. The compound of claim 10 , wherein R 5b is an optionally substituted 6 membered heteroaryl.

12. The compound of claim 11 , wherein R 5b is pyridyl, pyrazinyl, pyridazinyl, or pyrimidyl.

13. The compound of claim 10 , wherein R 5b is an optionally substituted 5 membered heteroaryl.

14. The compound of claim 13 , wherein R 5b is pyrazolyl.

15. The compound claim 1 , having the structure

or a pharmaceutically acceptable salt, ester, amide, or prodrug thereof.

16. A pharmaceutical composition comprising an effective amount of a compound of claim 1 , or a pharmaceutically acceptable salt, ester, amide, or prodrug thereof, and one or more pharmaceutically acceptable carriers, diluents, excipients, or combinations thereof.

17. The compound of claim 2 , wherein R 1 is an optionally substituted (5 to 7 membered heterocyclyl)alkyl.

18. The compound of claim 17 , wherein R 1 is an optionally substituted (5 membered heterocyclyl)alkyl.

19. The compound of claim 18 , wherein R 1 is pyrrolidyl-CH 2 —.

Assignments (2)
SECURITY INTEREST Recorded Oct 18, 2023
From: CYDEX PHARMACEUTICALS, INC.; LIGAND PHARMACEUTICALS INCORPORATED; METABASIS THERAPEUTICS, INC.; PFENEX INC.
To: CITIBANK, N.A., AS ADMINISTRATIVE AGENT
Reel/Frame 065271/0025 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 4, 2022
From: ZHI, LIN
To: LIGAND PHARMACEUTICALS, INC.
Reel/Frame 061305/0780 →