University of Michigan

Xu Ran

Shaomeng Wang

Arul M Chinnaiyan

Duxin Sun

Liu Liu

Donna McEachern

Longchuan Bai

Bing Zhou

Jeanne Stuckey

Yujun Zhao

Jennifer Lynn Meagher

Irfan A Asangani

Ruijuan Luo

Chao-Yie Yang

Angelo Aguilar

Xiaoqin Li

Yang Hu

Hacer Karatas

Bo Wen

Ting Zhao

Inhibitors of BET bromodomains and compositions containing the same are disclosed. Methods of using the BET bromodomain inhibitors in the treatment of diseases and conditions wherein inhibition of BET bromodomain provides a benefit, like cancers, also are disclosed.

BET bromodomain inhibitors and therapeutic methods using the same

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

Xu Ran