Invention Grant
- Patent Title: EGFR proteolysis targeting chimeric molecules and associated methods of use
-
Application No.: US15852854Application Date: 2017-12-22
-
Publication No.: US10994015B2Publication Date: 2021-05-04
- Inventor: Andrew P. Crew , Kurt Zimmermann , Jing Wang , Craig M. Crews , Saul Jaime-Figueroa , George Burslem
- Applicant: Arvinas Operations, Inc. , Yale University
- Applicant Address: US CT New Haven; US CT New Haven
- Assignee: Arvinas Operations, Inc.,Yale University
- Current Assignee: Arvinas Operations, Inc.,Yale University
- Current Assignee Address: US CT New Haven; US CT New Haven
- Agency: Cantor Colburn LLP
- Agent Bryan D. Zerhusen, Esq.
- Main IPC: C07D471/04
- IPC: C07D471/04 ; A61P35/00 ; A61K31/506 ; A61K47/54 ; A61K47/55 ; A61K31/519 ; A61K31/427 ; A61K31/454 ; A61K31/517 ; A61K31/55 ; A61K31/496 ; A61K31/551 ; A61K45/06 ; A61K38/07 ; A61K31/52

Abstract:
The present disclosure relates to bifunctional compounds, which find utility as modulators of receptor tyrosine kinase (RTK) proteins. In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a ligand which binds to an E3 ubiquitin ligase and on the other end a moiety which binds a target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effectuate ubiquitination, and therefore, degradation (and inhibition) of the target protein. The present disclosure exhibits 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.
Public/Granted literature
- US20180193470A1 EGFR PROTEOLYSIS TARGETING CHIMERIC MOLECULES AND ASSOCIATED METHODS OF USE Public/Granted day:2018-07-12
Information query