IP Library › Granted Patent US 11,377,431
Granted Patent B2
US 11,377,431 · App. 17/498,530 · Granted Jul 5, 2022

Inhibitors of RAF kinases

Inventors: Stephen W. Kaldor (San Diego, CA); Toufike Kanouni (Rancho Santa Fe, CA); Eric Murphy (San Marcos, CA); Jason Cox (Rancho Santa Fe, CA); Robert Kania (Del Mar, CA)
Assignee: KINNATE BIOPHARMA INC.
C07D295/155C07D401/12C07D405/12
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Quick Facts
Patent No.
US 11,377,431
App. No.
17/498,530
Granted
Jul 5, 2022
Kind
B2
Abstract

Provided herein are inhibitors of receptor tyrosine kinase effector, RAF, pharmaceutical compositions comprising said compounds, and methods for using said compounds for the treatment of diseases.

Claims (37)

1. A compound, or pharmaceutically acceptable salt or solvate thereof, having the structure of Formula (I):

wherein,

X is N or C—H;

R 1 is selected from H, optionally substituted C1-C6 alkyl, or optionally substituted C3-C7 cycloalkyl;

R 2 is selected from H, optionally substituted C1-C6 alkyl, or optionally substituted C3-C7 cycloalkyl; or optionally, R 1 and R 2 join to form a ring;

R 3 is selected from H, —OH, —OR 4 , —NH 2 , —NHR 4 , —N(R 4 ) 2 , optionally substituted heterocyclyl, or optionally substituted heteroaryl;

each R 4 is independently selected from optionally substituted C1-C6 alkyl, optionally substituted C1-C6 acyl or optionally, R 2 and R 4 join to form a ring; and

Z is an optionally substituted aryl or heteroaryl.

2. The compound of claim 1 , or pharmaceutically acceptable salt or solvate thereof, wherein X is N.

3. The compound of claim 1 , or pharmaceutically acceptable salt or solvate thereof, wherein X is C—H.

4. The compound of claim 1 , or pharmaceutically acceptable salt or solvate thereof, wherein R 1 is H.

5. The compound of claim 1 , or pharmaceutically acceptable salt or solvate thereof, wherein R 1 is optionally substituted C1-C6 alkyl.

6. The compound of claim 5 , or pharmaceutically acceptable salt or solvate thereof, wherein the optionally substituted alkyl is substituted with at least one halogen.

7. The compound claim 5 , or pharmaceutically acceptable salt or solvate thereof, wherein R 1 is CH 3 .

8. The compound of claim 6 , or pharmaceutically acceptable salt or solvate thereof, wherein R 1 is CF 3 .

9. The compound of claim 1 , or pharmaceutically acceptable salt or solvate thereof, wherein R 1 is optionally substituted C3-C7 cycloalkyl.

10. The compound claim 1 , or pharmaceutically acceptable salt or solvate thereof, wherein R 2 is H.

11. The compound of claim 1 , or pharmaceutically acceptable salt or solvate thereof, wherein R 2 is optionally substituted C1-C6 alkyl.

12. The compound of claim 1 , or pharmaceutically acceptable salt or solvate thereof, wherein R 2 is optionally substituted C3-C7 cycloalkyl.

13. The compound of claim 1 , or pharmaceutically acceptable salt or solvate thereof, wherein R 1 and R 2 join to form a ring.

14. The compound of claim 1 , or pharmaceutically acceptable salt or solvate thereof, wherein R 3 is —OH.

15. The compound of claim 1 , or pharmaceutically acceptable salt or solvate thereof, wherein R 3 is —OR 4 , —NH 2 , —NHR 4 , or —N(R 4 ) 2 .

16. The compound of claim 1 , or pharmaceutically acceptable salt or solvate thereof, wherein R 3 is optionally substituted heterocyclyl.

17. The compound of claim 1 , or pharmaceutically acceptable salt or solvate thereof, wherein R 3 is optionally substituted heteroaryl.

18. The compound of claim 15 , or pharmaceutically acceptable salt or solvate thereof, wherein R 4 is optionally substituted C1-C6 alkyl.

19. The compound of claim 15 , or pharmaceutically acceptable salt or solvate thereof, wherein R 4 is optionally substituted C1-C6 acyl.

20. The compound of claim 1 , or pharmaceutically acceptable salt or solvate thereof, wherein R 2 and R 4 join to form a ring.

21. The compound of claim 1 , or pharmaceutically acceptable salt or solvate thereof, wherein Z is an optionally substituted aryl.

22. The compound of claim 21 , or pharmaceutically acceptable salt or solvate thereof, wherein the optionally substituted aryl is an optionally substituted phenyl.

23. The compound of claim 22 , or pharmaceutically acceptable salt or solvate thereof, wherein the optionally substituted phenyl is an optionally substituted 3-(trifluoromethyl)phenyl.

24. The compound of claim 1 , or pharmaceutically acceptable salt or solvate thereof, wherein Z is a 3-(trifluoromethyl)phenyl.

25. The compound of claim 1 , or pharmaceutically acceptable salt or solvate thereof, wherein Z is an optionally substituted heteroaryl.

26. The compound of claim 25 , or pharmaceutically acceptable salt or solvate thereof, wherein the optionally substituted heteroaryl is an optionally substituted six-membered heteroaryl.

27. The compound of claim 26 , or pharmaceutically acceptable salt or solvate thereof, wherein the optionally substituted six-membered heteroaryl is an optionally substituted pyridyl.

28. The compound of claim 27 , or pharmaceutically acceptable salt or solvate thereof, wherein the optionally substituted pyridyl is an optionally substituted 2-(trifluoromethyl)pyrid-4-yl.

29. The compound of claim 1 , or pharmaceutically acceptable salt or solvate thereof, wherein Z is a 2-(trifluoromethyl)pyrid-4-yl.

30. A pharmaceutical composition comprising a compound, or pharmaceutically acceptable salt or solvate thereof, as described in claim 1 , and a pharmaceutically acceptable excipient.

Assignments (3)
CORRECTIVE ASSIGNMENT TO CORRECT THE CORRECT THE RECEIVING PARTY DATA COMPANY NAME IS: PIERRE FABRE MEDICAMENT PREVIOUSLY RECORDED AT REEL: 66638 FRAME: 147. ASSIGNOR(S) HEREBY CONFIRMS THE ASSIGNMENT. Recorded Sep 11, 2024
From: KINNATE BIOPHARMA INC.
To: PIERRE FABRE MÉDICAMENT
Reel/Frame 068939/0656 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 4, 2024
From: KINNATE BIOPHARMA INC.
To: PIERRE FABRE MÉDICAMENT, SAS
Reel/Frame 066638/0147 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Apr 6, 2022
From: KALDOR, STEPHEN W.; KANOUNI, TOUFIKE; MURPHY, ERIC; COX, JASON; KANIA, ROBERT
To: KINNATE BIOPHARMA INC.
Reel/Frame 059520/0874 →
Continuity (2)
Provisional Application 63090623 · Oct 12, 2020
Related Publication 20220112170A1 · Apr 14, 2022
Cited By (4)
US 12,312,336 US 12,319,655 US 12,569,496 US 12,692,248