University of Michigan

Yang Hu

Shaomeng Wang

Bing Zhou

Longchuan Bai

Chong Qin

Donna McEachern

Angelo Aguilar

Fuming Xu

Jiantao Hu

Arul M Chinnaiyan

Duxin Sun

Liu Liu

Chao-Yie Yang

Jeanne Stuckey

Yujun Zhao

Jennifer Lynn Meagher

Irfan A Asangani

Ruijuan Luo

Ester Fernandez-Salas

Xu Ran

Weiguo Xiang

Bo Wen

Ting Zhao

Rohan Rej

Jiuling Yang

Yangbing Li

Zhuo Chen

Xin Han

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

The present disclosure provides substituted 9H-pyrimido[4,5-b]indoles and 5H-pyrido[4,3-b]indoles and related analogs represented by Formula I: and the pharmaceutically acceptable salts, hydrates, and solvates thereof, wherein R, A, B, B, G, X, Y, Y, and Yare 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. Compounds of the present disclosure are especially useful for treating cancer.

9H-pyrimido [4,5-b]indoles and related analogs as BET bromodomain inhibitors

9H-pyrimido[4,5-B]indoles and related analogs as BET bromodomain inhibitors

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Ann Arbor, MI, United States of America

Yang Hu