IP Library › Granted Patent US 11,274,082
Granted Patent B2
US 11,274,082 · App. 16/886,926 · Granted Mar 15, 2022

Tead inhibitors and uses thereof

Inventor: Alfredo C. Castro (Somerville, MA)
Assignee: IKENA ONCOLOGY, INC.
C07D233/58A61P35/00C07C317/14C07D231/12C07D249/08C07D257/04C07D271/10C07D401/04C07D401/12C07D403/12C07D405/12C07D417/12C07F5/025
View Patent ↗
Loading inventors, assignments & file history…
Monitor This Case
Get email alerts when status or documents change.
Order Certified Copies
Most orders are placed with the USPTO same day — all within 24 business hours.
Order via The Patent Place →
Pre-filled with this patent's details
Quick Facts
Patent No.
US 11,274,082
App. No.
16/886,926
Granted
Mar 15, 2022
Kind
B2
Abstract

The present invention provides compounds, compositions thereof, and methods of using the same.

Claims (47)

1. A compound of Formula I:

or a pharmaceutically acceptable salt thereof, wherein:

L 1 is —NH—CH 2 — or —NH—C(O)—;

Ring A is phenyl, optionally substituted 1-2 times by halogen, —CN, —NO 2 , or —C 1-6 aliphatic substituted 0-6 times by halogen, —CN, or —NO 2 ;

R 2 is an optionally substituted 5-membered heteroaryl ring having 2 nitrogen atoms;

R 3 is —H;

R 4 is halogen, —S(O) 2 N(R) 2 , —S(O)N(R) 2 , or —C(O)N(R) 2 ;

R 6 is —H or —C 1-6 aliphatic substituted 0-6 times by halogen, —CN, or —NO 2 ; and

each R is independently —H or optionally substituted —C 1-6 aliphatic.

2. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein L 1 is NH—CH 2 —.

3. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein Ring A is phenyl, optionally substituted 1-2 times by —C 1-6 aliphatic substituted 0-6 times by halogen.

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

and R is unsubstituted —C 1-6 aliphatic.

5. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein R 4 is —S(O) 2 NHR.

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

7. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein the compound is of Formulas (IXa-1), (IXa-2), (Xa-1), or (Xa-2):

wherein L 1 is —NH—CH 2 —, and each R is independently —H or —C 1-6 aliphatic substituted 0-6 times by halogen, —CN, or —NO 2 .

8. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein the compound is of Formula (XIa-1) or (XIa-2):

wherein L 1 is —NH—CH 2 —, and each R is independently —H or —C 1-6 aliphatic substituted 0-6 times by halogen, —CN, or —NO 2 .

9. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein the compound is of Formula (XIIa-1) or (XIIa-2):

wherein L 1 is —NH—CH 2 —, and R is —C 1-3 aliphatic substituted 1, 2, 3, 4, 5, or 6 times by F.

10. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein the compound is of Formula (XIIIa-1) or (XIIIa-2):

wherein L 1 is —NH—CH 2 —, and R is optionally substituted —C 1-6 aliphatic.

11. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein the compound is of Formula (XIVa-1) or (XIVa-2):

wherein L 1 is —NH—CH 2 −.

12. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein the compound is of Formulas (XVa-1), or (XVa 2):

13. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein the compound is of Formulas (XVIa-1), or (XVIa 2):

14. The compound of claim 1 , which is selected from:

or a pharmaceutically acceptable salt thereof.

15. A pharmaceutical composition comprising a compound of claim 1 , or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, adjuvant, or vehicle.

16. A pharmaceutical composition comprising the compound of claim 14 , or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, adjuvant, or vehicle.

17. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein the compound is of Formula (II):

wherein L 1 is —NH—CH 2 —, R 1 is —H, -halogen, —CN, —NO 2 , or —C 1-6 aliphatic, and R 7 is —H, -halogen, —CN, —NO 2 , or —C 1-6 aliphatic.

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

19. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein R 4 is —S(O) 2 NH—CH 3 .

20. A compound:

or a pharmaceutically acceptable salt thereof.

21. A pharmaceutical composition comprising the compound of claim 20 , or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, adjuvant, or vehicle.

22. A compound:

or a pharmaceutically acceptable salt thereof.

23. A pharmaceutical composition comprising the compound of claim 22 , or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, adjuvant, or vehicle.

24. A compound:

or a pharmaceutically acceptable salt thereof.

25. A pharmaceutical composition comprising the compound of claim 24 , or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, adjuvant, or vehicle.

26. A compound:

or a pharmaceutically acceptable salt thereof.

27. A pharmaceutical composition comprising the compound of claim 26 , or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, adjuvant, or vehicle.

Assignments (3)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 11, 2026
From: IMAGENEBIO, INC.
To: THE EHE FOUNDATION
Reel/Frame 073758/0595 →
CHANGE OF NAME Recorded Dec 23, 2025
From: IKENA ONCOLOGY, INC.
To: IMAGENEBIO, INC.
Reel/Frame 073522/0031 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 21, 2020
From: CASTRO, ALFREDO C.
To: IKENA ONCOLOGY, INC.
Reel/Frame 053260/0711 →
Continuity (5)
Provisional Application 63025219 · May 15, 2020
Provisional Application 62944567 · Dec 6, 2019
Provisional Application 62928931 · Oct 31, 2019
Provisional Application 62855082 · May 31, 2019
Related Publication 20200407327A1 · Dec 31, 2020
Cited By (1)
US 12,577,208