University of Michigan

Chong Qin

Shaomeng Wang

Bing Zhou

Yang Hu

Fuming Xu

Jiantao Hu

Chao-Yie Yang

Longchuan Bai

Weiguo Xiang

Ester Fernandez-Salas

Donna McEachern

Angelo Aguilar

Rohan Rej

Yangbing Li

Jiuling Yang

Xin Han

Zhuo Chen

Zhou Chen

The present disclosure provides fused 1,4-oxazepines and related analogs represented by Formula (I) and the pharmaceutically acceptable salts, hydrates, and solvates thereof, wherein R, R, R, R, R, R, R, A, and Y are as defined as set forth in the specification. The present disclosure is also directed to the use of compounds of Formula (I) to treat a condition or disorder responsive to inhibition of BET bromodomains such as cancer. 

Fused 1,4-oxazepines and related analogs as BET bromodomain inhibitors

The present disclosure provides compounds represented by Formula I and the pharmaceutically acceptable salts, hydrates, and solvates thereof, wherein R, R, R, R, R, R4, 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-oxazepines as BET protein degraders

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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Ann Arbor, MI, United States of America

Chong Qin