University of Michigan

Bo Wen

Shaomeng Wang

Arul M Chinnaiyan

Duxin Sun

Liu Liu

Donna McEachern

Angelo Aguilar

Longchuan Bai

Bing Zhou

Jeanne Stuckey

Yujun Zhao

Yang Hu

Jennifer Lynn Meagher

Irfan A Asangani

Xu Ran

Ruijuan Luo

Ting Zhao

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

Bo Wen