University of Michigan

Yujun Zhao

Shaomeng Wang

Duxin Sun

Donna McEachern

Bing Zhou

Arul M Chinnaiyan

Liu Liu

Longchuan Bai

Jeanne Stuckey

Wei Sun

Jennifer Lynn Meagher

Irfan A Asangani

Xu Ran

Ruijuan Luo

Angelo Aguilar

Sanjeev Kumar

Shanghai Yu

Peng Zou

Chao-Yie Yang

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, W, 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 such as cancer. The present disclosure is also directed to the use of compound of Formula I as synthetic intermediates. 

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

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

Provided herein are compounds, compositions, and methods in the field of medicinal chemistry. The compounds and compositions provided herein relate to spiro-oxindoles which function as antagonists of the interaction between p53 and MDM2, and their use as therapeutics for the treatment of cancer and other diseases.

Spiro-oxindole MDM2 antagonists

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Ann Arbor, MI, United States of America

Yujun Zhao