Glaxosmithkline Intellectual Property Development Limited

Yale University

Cambridge Enterprise Limited University of Cambridge

Astex Therapeutics Limited

Ian Edward David Smith

Gordon Saxty

Afjal Hussain Miah

Craig M Crews

Joelle Le

Rodolfo Cadilla

John David Harling

Stephen Andrew Thomson

Linda N Casillas

Sebastien Andre Campos

Mark David Rackham

William L Jorgensen

Simon Teanby Hodgson

Denton Wade Hoyer

Joseph Wendell Wilson

Heather Hobbs

Julien Michel

Peter C Gareiss

Anke G Roth

Dennis Buckley

Christie Schulte

Alessio Ciulli

Inge Van Molle

Jeffrey Gustafson

Hyun-Seop Tae

Ashley Paul Hancock

Daniel J Price

Lee T Schaller

Andrew L Larkin

Dave Norman Deaton

Paul N Mortenson

The present invention relates to compounds, compositions, combinations and medicaments containing said compounds and processes for their preparation. The invention also relates to the use of said compounds, combinations, compositions and medicaments, for example as inhibitors of the activity of RIP2 kinase, including degrading RIP2 kinase, the treatment of diseases and conditions mediated by the RIP2 kinase, in particular for the treatment of inflammatory diseases or conditions.

Conjugates comprising RIPK2 inhibitors

The present invention relates to bifunctional compounds, which find utility as modulators of targeted ubiquitination, especially inhibitors of a variety of polypeptides and other proteins that are degraded and/or otherwise inhibited by bifunctional compounds of the present invention. In particular, the present invention is directed to compounds, which contain on one end a VHL ligand that binds to the ubiquitin ligase and on the other end a moiety that binds a target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of that protein. The present invention exhibits a broad range of pharmacological activities associated with compounds of the present invention, consistent with the degradation/inhibition of targeted polypeptides.

Compounds and methods for the enhanced degradation of targeted proteins and other polypeptides by an E3 ubiquitin ligase

Compounds

1AP E3 ligase directed proteolysis targeting chimeric molecules

A compound of formula (I): or a pharmaceutically acceptable salt thereof, compositions, combinations and medicaments containing said compounds and processes for their preparation. The invention also relates to the use of said compounds, combinations, compositions and medicaments, for example as inhibitors of the activity of the estrogen receptor, including degrading the estrogen receptor, the treatment of diseases and conditions mediated by the estrogen receptor.

Benzothiophene derivatives as estrogen receptor inhibitors

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Stevenage, United Kingdom

Ian Edward David Smith