IP Library › Granted Patent US 11,530,197
Granted Patent B2
US 11,530,197 · App. 17/678,301 · Granted Dec 20, 2022

Analogs for the treatment of disease

Inventors: Aleksandrs Zavoronkovs (Pak Shek Kok, HK); Aleksandr Aliper (Ramenskoye, RU); Vladimir Aladinskiy (Kaliningrad, RU); Andrey Kukharenko (Moscow, RU)
Assignee: Insilico Medicine IP Limited
C07D403/04
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Quick Facts
Patent No.
US 11,530,197
App. No.
17/678,301
Granted
Dec 20, 2022
Kind
B2
Abstract

The disclosure provides TNIK and/or MAP4K4 kinases inhibitors for the treatment of disease. In one aspect, disclosed herein are kinase inhibitors having a structure of Formula (A), (A*), (I), (IIA), or (IIB). Further described herein are pharmaceutical composition comprising these compounds and methods of using these compounds. In one aspect, disclosed herein are methods of treating a disease or condition by administering the kinases inhibitors described herein.

Claims (60)

1. A compound represented by Formula (IIA),

or a pharmaceutically acceptable salt thereof, wherein:

R 1 is piperazine, wherein the piperazine is optionally substituted with one or more substituents independently selected at each occurrence from oxo, —S(O 2 )NH 2 , and C 1-10 alkyl, wherein the C 1-10 alkyl is optionally substituted with one or more substituents independently selected at each occurrence from hydroxy, halogen, oxo, and —NH 2 ;

R 3 is phenyl, wherein the phenyl is optionally substituted with one or more halogen; and

R 4 is

2. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein R 3 is selected from

3. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein R 1 is piperazine substituted with one or more C 1-3 alkyl, wherein the C 1-3 alkyl is optionally substituted with one or more substituents independently selected at each occurrence from hydroxy, halogen, oxo, and —NH 2 .

4. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein R 1 is selected from

5. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein the compound is:

or a pharmaceutically acceptable salt thereof.

6. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein the compound is

or a pharmaceutically acceptable salt thereof.

7. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein the compound is

or a pharmaceutically acceptable salt thereof.

8. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein the compound is

or a pharmaceutically acceptable salt thereof.

9. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein the compound is

or a pharmaceutically acceptable salt thereof.

10. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein the compound is

or a pharmaceutically acceptable salt thereof.

11. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein the compound is

or a pharmaceutically acceptable salt thereof.

12. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein the compound is

or a pharmaceutically acceptable salt thereof.

13. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein the compound is

or a pharmaceutically acceptable salt thereof.

14. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein the compound is

or a pharmaceutically acceptable salt thereof.

15. A method of treating a fibrotic disease or condition, comprising administering a compound of claim 5 or a pharmaceutically acceptable salt thereof, to a subject in need thereof, wherein the fibrotic disease or condition is idiopathic pulmonary fibrosis (IPF).

16. A method of treating a fibrotic disease or condition, comprising administering a compound of claim 5 or a pharmaceutically acceptable salt thereof, to a subject in need thereof, wherein the fibrotic disease or condition is skin fibrosis.

17. A pharmaceutical composition comprising (i) a compound represented by Formula (IIA),

or a pharmaceutically acceptable salt thereof, wherein:

R 1 is piperazine, wherein the piperazine is optionally substituted with one or more substituents independently selected at each occurrence from oxo, —S(O 2 )NH 2 , and C 1-10 alkyl, wherein the C 1-10 alkyl is optionally substituted with one or more substituents independently selected at each occurrence from hydroxy, halogen, oxo, and —NH 2 ;

R 3 is phenyl, wherein the phenyl is optionally substituted with one or more halogen; and

R 4 is

and

(ii) a pharmaceutically acceptable excipient.

18. The pharmaceutical composition of claim 17 , wherein:

R 1 is selected from

R 3 is selected from

19. The pharmaceutical composition of claim 17 , wherein the compound is:

or a pharmaceutically acceptable salt thereof.

20. The pharmaceutical composition of claim 17 , wherein the compound is

or a pharmaceutically acceptable salt thereof.

21. The pharmaceutical composition of claim 17 , wherein the compound is

or a pharmaceutically acceptable salt thereof.

22. The pharmaceutical composition of claim 17 , wherein the compound is

or a pharmaceutically acceptable salt thereof.

23. The pharmaceutical composition of claim 17 , wherein the compound is

or a pharmaceutically acceptable salt thereof.

24. The pharmaceutical composition of claim 17 , wherein the compound is

or a pharmaceutically acceptable salt thereof.

25. The pharmaceutical composition of claim 17 , wherein the compound is

or a pharmaceutically acceptable salt thereof.

26. The pharmaceutical composition of claim 17 , wherein the compound is

or a pharmaceutically acceptable salt thereof.

27. The pharmaceutical composition of claim 17 , wherein the compound is

or a pharmaceutically acceptable salt thereof.

28. The pharmaceutical composition of claim 17 , wherein the compound is

or a pharmaceutically acceptable salt thereof.

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Apr 13, 2022
From: INSILICO MEDICINE HONG KONG LIMITED
To: INSILICO MEDICINE IP LIMITED
Reel/Frame 059589/0026 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Apr 1, 2022
From: ZAVORONKOVS, ALEKSANDRS; ALIPER, ALEKSANDR; ALADINSKIY, VLADIMIR; KUKHARENKO, ANDREY
To: INSILICO MEDICINE HONG KONG LIMITED
Reel/Frame 059477/0161 →
Priority Claims (2)
CN PCT/CN2021/077706 · Feb 24, 2021 · national
CN PCT/CN2021/142622 · Dec 29, 2021 · national
Continuity (1)
Related Publication 20220274959A1 · Sep 1, 2022
Cited By (2)
US 12,552,778 US 12,583,838