Granted Patent B2

US 12,729,208 · App. 17/997,461 · Granted Sep 8, 2026

Inventors: Nicholas David Peter Cosford (San Diego, CA); Dominik Heimann (Hamm, DE); Peter Teriete (San Diego, CA); Sumit Kumar Chanda (La Jolla, CA); Lars Pache (San Diego, CA); Laurent Jean Stephane De Backer (San Diego, CA); Nicole Bata (San Diego, CA); Mitchell D. Vamos (Batavia, OH)

Assignee: SANFORD BURNHAM PREBYS MEDICAL DISCOVERY INSTITUTE

C07D498/04A61P35/00C07D487/04C07D487/22C07D513/04

Abstract

Claims (36)

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

wherein,

X is NR A , O, S, S(O), or S(O) 2 ;

R A is hydrogen;

R 2a , R 2b , R 3a , and R 3b are each hydrogen;

R 6a is —U;

R 6b is —U;

—U is C 1 -C 6 alkyl;

or R 6a and R 6b together with the carbon atom to which they are attached form a saturated or partially saturated 3- to 7-membered cycloalkyl or a saturated or partially saturated 3- to 7-membered heterocycloalkyl;

R 7a is hydrogen;

R 7b is hydrogen;

R 8 is Z, CH(Z) 2 , CH 2 CH(Z) 2 , CH(C 1 -C 6 alkyl)Z, or C(O)Z; and

Z is C 3 -C 10 cycloalkyl, 3- to 10-membered heterocycloalkyl, C 6 -C 10 aryl, or 5- to 10-membered heteroaryl; wherein each Z is optionally substituted with 1, 2, or 3 C 1 -C 4 alkyl, C 1 -C 4 haloalkyl, C 1 -C 4 alkoxy, C 1 -C 4 haloalkoxy, or 5- to 10-membered heteroaryl provided that when R 6a and Rob are both CH 3 or when R 6a and R 6b together with the carbon atom to which they are attached form an unsubstituted cyclopentyl or unsubstituted cyclopentenyl, then R 8 is not

2 . The compound of claim 1 , wherein X is O.

3 . The compound of claim 1 , wherein X is S or S(O) 2 .

4 . The compound of claim 1 , wherein X is S.

5 . The compound of claim 1 , wherein X is S(O) 2 .

6 . The compound of claim 1 , wherein X is NR A .

7 . The compound of claim 1 , having the structure of Formula (A-IV-a), (A-IV-b), or (A-IV-c):

8 . The compound of claim 1 , wherein R 6a and R 6b together with the carbon atom to which they are attached form a saturated or partially saturated 3- to 7-membered cycloalkyl ring.

9 . The compound of claim 8 , wherein R 6a and R 6b together with the carbon atom to which they are attached form a saturated or partially saturated 3- to 5-membered cycloalkyl ring.

10 . The compound of claim 1 , wherein R 6b is methyl, ethyl, 2-propenyl, or isopropyl.

11 . The compound of claim 1 , wherein R 6b is methyl.

12 . The compound of claim 1 , wherein R 6a and Rob are methyl.

13 . The compound of claim 1 , wherein R 8 is Z or CH(Z) 2 .

14 . The compound of claim 1 , wherein R 8 is Z.

15 . The compound of claim 1 , wherein Z is C 3 -C 10 cycloalkyl or 3- to 10-membered heterocycloalkyl.

16 . The compound of claim 1 , wherein Z is C 3 -C 10 cycloalkyl.

17 . The compound of claim 1 , wherein R 8 is:

18 . A compound or pharmaceutically acceptable salt thereof, having the structure:

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

20 . A method of treating cancer in an individual in need thereof comprising administering a therapeutically effective amount of a compound of claim 1 , or pharmaceutically acceptable salt thereof, to the individual.

21 . The compound of claim 18 , having the structure:

or pharmaceutically acceptable salt thereof.

22 . The compound of claim 18 , having the structure:

or pharmaceutically acceptable salt thereof.

Assignments (2)

Continuity (2)

References Cited (140)