Back to results
US 2025/0084055 A1Published application
Dihydroquinolinones for medical treatment
AssigneeC4 Therapeutics, Inc.
InventorsRoger Norcross, Adrian Britschgi, Fabian Dey, Annick Goergler, Eric Andre Kusznir, Moreno Attilio Wichert
Life of this patent
Estimating the term…
Abstract
The present invention provides dihydroquinolinone compounds which bind to the ubiquitously expressed E3 ligase protein cereblon (CRBN) and alter the substrate specificity of the CRBN E3 ubiquitin ligase complex, resulting in breakdown of intrinsic downstream proteins. The disclosed compounds are useful for the treatment of cancer.
Claims1
A compound of formula:
- or a pharmaceutically acceptable salt thereof,
- wherein
- X is CH or N,
- R1 is —C(O)—R6,
- R2 is H,
- or R1 and R2 together with the nitrogen they are attached to form a heteroaryl, which can be substituted by 1 or 2 substituents selected from R3,
- R3 is selected from the group consisting of
- i) —(CH2)0-1-aryl substituted by 1-2 substituents selected from R4
- ii) —(CH2)0-1-aryl,
- iii) —C(═O)N(R3a,R3b),
- iv) —C(═O)O—C1-6alkyl,
- v) —C(C3-7cycloalkyl)-aryl
- vi) C1-6alkyl,
- vii) —C3-7cycloalkyl
- viii) —CH2—O—(CH2)0-1-aryl,
- ix) heteroaryl substituted by 1-2 substituents selected from R4,
- x) hydroxy-C1-6alkyl, and
- xi) unsubstituted heteroaryl,
- R3a is selected from the group consisting of H and C1-6alkyl,
- R3b is selected from the group consisting of H, C1-6alkyl, and —C3-7cycloalkyl,
- or R3a and R3b form together with the nitrogen they are attached to a heterocycloalkyl,
- R4 is selected from the group consisting of unsubstituted heteroaryl, heteroaryl substituted by 1-2 substituents selected from R5, and C1-6alkoxy,
- R5 is C1-6alkyl,
- R6 is selected from the group consisting of unsubstituted heteroaryl and heteroaryl substituted by 1-2 substituents selected from R7,
- R7 is selected from the group consisting of unsubstituted heteroaryl and heteroaryl substituted by 1-2 substituents selected from R8,
- R8 is C1-6alkyl,
- with the proviso that 6-imidazol-1-yl-3,4-dihydro-1H-quinolin-2-one is excluded.
24 more elements
Dependencies are inferred from the claim text.