IP Library Granted Patent US 10,807,983
Granted Patent B2
US 10,807,983 · App. 15/070,718 · Granted Oct 20, 2020

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 10,807,983
App. No.
15/070,718
Granted
Oct 20, 2020
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 imizazo-fused heterocycle compounds useful to treat leukemia and other hematopoietic disorders.

Claims (31)

1. A compound of Formula I:

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

wherein

X is CR 4a ;

X′ is CR 4b ;

Y is N;

Y′ is CR 5b ;

R 1 is selected from the group consisting of hydrogen, halogen, —OR 6 , —CN, —NR 7 R 8 , —CH 2 OR 6 , —CH 2 NR 7 R 8 , an optionally substituted C 1-6 alkyl, an optionally substituted C 1-6 haloalkyl, an optionally substituted C 2-6 alkenyl, an optionally substituted C 2-6 alkynyl, an optionally substituted (5 to 7 membered heterocyclyl)alkyl, an optionally substituted 5 to 7 membered heterocyclyl, an optionally substituted aralkyl; an optionally substituted (5 or 6 membered heteroaryl)alkyl, 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 of R 2 , R 3 , R 4a and R 4b is independently selected from the group consisting of hydrogen, halogen, C 1-6 alkyl, OH, and C 1-6 alkoxy;

R 5b is selected from the group consisting of 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;

each R 6 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; 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 R 4a and R 4b 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 selected from piperidinyl-CH 2 — or morpholine-CH 2 —.

8. The compound of claim 1 , wherein R 1 is an optionally substituted 5 to 7 membered heterocyclyl.

9. The compound of claim 8 , wherein R 1 is an optionally substituted 6 membered heterocyclyl.

10. The compound of claim 9 , wherein R 1 is selected from optionally substituted morpholinyl, optionally substituted piperazinyl, or optionally substituted piperidinyl.

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

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

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

14. The compound of claim 13 , wherein R 5b is an optionally substituted 6 membered heteroaryl.

15. The compound of claim 14 , wherein R 5b is selected from pyridyl, pyrazinyl, pyridazinyl, or pyrimidyl.

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

17. The compound of claim 16 , wherein R 5b is pyrazolyl.

18. The compound claim 1 , selected from

pharmaceutically acceptable salts, esters, amides, or prodrugs thereof.

19. A pharmaceutical composition comprising an effective amount of a compound of claim 1 , or a pharmaceutically acceptable salt, ester, amide, or prodrug thereof, and a pharmaceutically acceptable carrier, diluent, excipient or combinations thereof.

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 Sep 16, 2020
From: ZHI, LIN
To: LIGAND PHARMACEUTICALS, INC.
Reel/Frame 053794/0293 →