Glutarimides for medical treatment

Patent metadata

Field	Value
Publication number	US-11802131-B2
Application number	US-202016809336-A
Country	US
Kind code	B2
Filing date	Mar 4, 2020
Priority date	Sep 4, 2017
Publication date	Oct 31, 2023
Grant date	Oct 31, 2023

Abstract

The present invention provides selected glutarimides 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.

First claim

We claim:

1. A compound of the formula:

or a pharmaceutically acceptable salt thereof
wherein
R 2 is hydrogen or C 1 -C 6 alkyl;
R 1 is 2,3-dihydro-1H-pyrrolo[2,3-b]pyridinyl; and
n is 0 or 1.

2. The compound of claim 1 , wherein R 2 is hydrogen.

3. The compound of claim 1 , wherein R 2 is methyl.

4. The compound of claim 1 wherein n is 0.

5. The compound of claim 1 , wherein n is 1.

6. The compound of claim 1 of the formula:

or a pharmaceutically acceptable salt thereof.

7. A pharmaceutical composition comprising a compound or pharmaceutically acceptable salt thereof of claim 1 optionally in a pharmaceutically acceptable carrier.

8. The compound of claim 6 of the formula:

or a pharmaceutically acceptable salt thereof.

9. The compound of claim 6 of the formula:

or a pharmaceutically acceptable salt thereof.

Assignees

• C4 Therapeutics Inc

Inventors

• Norcross Roger
• Goergler Annick
• Schmid Philipp
• Dey Fabian
• Kusznir Eric Andre

Classifications

• A61P35/00

  Antineoplastic agents · CPC title

• C07D487/04

  Ortho-condensed systems · CPC title

• C07D211/88 Primary

  attached in positions 2 and 6, e.g. glutarimide · CPC title

• C07D471/04

  Ortho-condensed systems · CPC title

• C07D401/12 Primary

  linked by a chain containing hetero atoms as chain links · CPC title