University of Michigan

Weiguo Xiang

Shaomeng Wang

Fuming Xu

Longchuan Bai

Bing Zhou

Jiantao Hu

Yang Hu

Chong Qin

Ester Fernandez-Salas

Donna McEachern

Chao-Yie Yang

Angelo Aguilar

Rohan Rej

Yangbing Li

Jiuling Yang

Xin Han

The present disclosure provides compounds represented by Formula (I): Formula (I) and the pharmaceutically acceptable salts and solvates thereof, wherein R, R, R, R, R, R, Y, &#x2550;, Ar, W, L, and B are as defined as set forth in the specification. The present disclosure also provides compounds of Formula (I)I for use to treat a condition or disorder responsive to inhibition and/or degradation of BET bromodomains such as cancer. 

BET bromodomain protein degraders with cleavable linkers

The present disclosure provides compounds represented by Formula I: I, and the pharmaceutically acceptable salts, hydrates, and solvates thereof, wherein R, R, R, R, R, Ar, L, X, Y, and B are as defined as set forth in the specification. The present disclosure also provides compounds of Formula I for use to treat a condition or disorder responsive to degradation of BET bromodomains such as cancer. 

Fused 1,4-diazepines as BET protein degraders

The present disclosure provides compounds represented by Formula I: and the salts or solvates thereof, wherein X, L, Y, and B are as defined in the specification. Compounds having Formula I are immunomodulators and/or monofunctional synthetic intermediates that can be used to prepare small-molecule drug conjugates. 

Monofunctional intermediates for ligand-dependent target protein degradation

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Ypsilanti, MI, United States of America

Weiguo Xiang