University of Dundee

Boehringer Ingelheim International Gmbh

Amphista Therapeutics Limited

Alessio Ciulli

Andrea Testa

Steffen Steurer

Michael Roy

Michael Zengerle

Scott Hughes

Emelyne Diers

Nicole Trainor

William Farnaby

Steven Peter Butcher

Kwok-Ho Chan

Chiara Maniaci

Scott J Hughes

Christian Dank

The present invention encompasses compounds of formula (1) wherein the groups R, A, G, LK and t have the meanings given in the claims and specification, their use as degraders of SMARCA2 and/or SMARCA4, pharmaceutical compositions which contain compounds of this kind and their use as medicaments/medical uses, especially as agents for treatment and/or prevention of oncological diseases.

Proteolysis targeting chimera (PROTACS) as degraders of SMARCA2 and /or SMARCA4

The invention provides for bifunctional molecules comprising an Rpn11 binding partner and a target protein binding partner. A bifunctional molecule according to the invention binds to Rpn11 and to the target protein, thereby facilitating degradation of the target protein bound to the target protein binding partner. The invention also provides for use of a bifunctional molecule for preventing or treating disease.

Bifunctional molecules for targeting Rpn11

Compounds having the general structure A-L-B are presented wherein A and B are independently an E3 ubiquitin ligase protein binding ligand compound of formula 1A or 1B. Pharmaceutical compositions comprising these compounds and methods of use are also presented.

Small molecules

There is provided novel small molecule E3 ubiquitin ligase protein binding ligand compounds, and to their utility in PROteolysis Targeted Chimeras (PROTACs), as well as processes for their preparation thereof, and use in medicine. There is particularly provided novel small molecule E3 ubiquitin ligase protein binding inhibitor compounds based on a fluorohydroxyproline scaffold, to their utility as ligands in synthesizing novel PROTACs, and to synthetic methods therefor.

Fluorohydroxyproline derivatives useful in the preparation of proteolysis targeted chimeras

There is provided novel small molecule E3 ubiquitin ligase protein binding ligand compounds, having utility in PROteolysis Targeted Chimeras (PROTACs), as well as processes for the preparation thereof, and use in medicine. There is particularly provided PROTACs which bind to a protein within the bromo- and Extra-terminal (BET) family of proteins, and especially to PROTACs including novel small molecule E3 ubiquitin ligase protein binding ligand compounds which selectively induce degradation of the BRD4 protein within the bromodomain of the BET family of proteins.

Derivatives of 1-[(cyclopentyl or 2-pyrrolidinyl)carbonylaminomethyl]-4-(l,3-thiazol-5-yl) benzene which are useful for the treatment of proliferative, autoimmune or inflammatory diseases

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Dundee, United Kingdom

Alessio Ciulli