IP Library › Granted Patent US 11,760,728
Granted Patent B2
US 11,760,728 · App. 17/646,787 · Granted Sep 19, 2023

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
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Quick Facts
Patent No.
US 11,760,728
App. No.
17/646,787
Granted
Sep 19, 2023
Kind
B2
Abstract

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

Claims (41)

1. A method for treating mesothelioma in a patient, comprising administering to the patient 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 method of claim 1 , wherein L 1 is —NH—CH 2 —.

3. The method of claim 1 , wherein Ring A is phenyl, optionally substituted 1-2 times by —C 1-6 aliphatic substituted 0-6 times by halogen.

4. The method of claim 1 , wherein R 2 is

and R is unsubstituted —C 1-6 aliphatic.

5. The method of claim 1 , wherein R 1 is —S(O) 2 NHR.

6. The method of claim 1 , wherein R 6 is —H.

7. The method of claim 1 , 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 method of claim 1 , 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 method of claim 1 , 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 method of claim 1 , 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 method of claim 1 , wherein the compound is of Formula (XIVa-1) or (XIVa-2):

wherein L 1 is —NH—CH 2 —.

12. The method of claim 1 , wherein the compound is of Formulas (XVa-1), or (XVa-2):

13. The method of claim 1 , wherein the compound is of Formulas (XVIa-1), or (XVIa-2):

14. The method of claim 1 , wherein the compound is of Formula (II):

wherein L 1 is —NH—CH 2 —, le is —H, -halogen, —CN, —NO 2 , or —C 1-6 aliphatic, and R 7 is —H, -halogen, —CN, —NO 2 , or —C1-6 aliphatic.

15. The method of claim 1 , wherein R 2 is

16. The method of claim 1 , wherein R 4 is —S(O) 2 NH—CH 3 .

17. The method of claim 1 , wherein the compound is selected from:

or a pharmaceutically acceptable salt thereof.

18. The method of claim 1 , wherein the compound is:

or a pharmaceutically acceptable salt thereof.

19. The method of claim 1 , wherein the compound is:

or a pharmaceutically acceptable salt thereof.

20. The method of claim 1 , wherein the compound is:

or a pharmaceutically acceptable salt thereof.

21. The method of claim 1 , wherein the compound is:

or a pharmaceutically acceptable salt thereof.

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 Mar 2, 2022
From: CASTRO, ALFREDO C.
To: IKENA ONCOLOGY, INC.
Reel/Frame 059144/0960 →
Continuity (6)
Division 16886926 · May 29, 2020
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 20220251048A1 · Aug 11, 2022
Cited By (1)
US 12,577,208