IP Library › Granted Patent US 11,986,532
Granted Patent B2
US 11,986,532 · App. 17/721,916 · Granted May 21, 2024

Modulators of BCL6 proteolysis and associated methods of use

Inventor: Dan Sherman (Madison, CT)
Assignee: Arvinas Operations, Inc.
A61K47/55A61K45/06A61K47/545A61P35/00
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Quick Facts
Patent No.
US 11,986,532
App. No.
17/721,916
Granted
May 21, 2024
Kind
B2
Abstract

Bifunctional compounds, which find utility as modulators of B-cell lymphoma 6 protein (BCL6; target protein), are described herein. In particular, the bifunctional compounds of the present disclosure contain on one end a cereblon ligand that binds to the respective E3 ubiquitin ligase and on the other end a moiety which binds the target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The bifunctional compounds of the present disclosure exhibit a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aggregation or accumulation of the target protein are treated or prevented with compounds and compositions of the present disclosure.

Claims (4)

1. A compound, wherein the compound is:

2. A pharmaceutically acceptable salt of a compound, wherein the compound is:

3. A pharmaceutical composition comprising a compound and one or more pharmaceutically acceptable excipients, wherein the compound is:

4. A pharmaceutical composition comprising a pharmaceutically acceptable salt of a compound and one or more pharmaceutically acceptable excipients, wherein the compound is:

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 1, 2022
From: BERLIN, MICHAEL; DONG, HANQING; SHERMAN, DAN; SNYDER, LAWRENCE B.; WANG, JING; ZHANG, WEI
To: ARVINAS OPERATIONS, INC.
Reel/Frame 060423/0850 →
Continuity (2)
Provisional Application 63175678 · Apr 16, 2021
Related Publication 20220395576A1 · Dec 15, 2022
Cited By (1)
US 12,310,975