University of Michigan

Jiangsu Ascentage Biomed Development Inc.

Longchuan Bai

Shaomeng Wang

Donna McEachern

Liu Liu

Duxin Sun

Bing Zhou

Chao-Yie Yang

Angelo Aguilar

Jeanne Stuckey

Xiaoqin Li

Jennifer Lynn Meagher

Arul M Chinnaiyan

Yujun Zhao

Fuming Xu

Yang Hu

Irfan A Asangani

Ruijuan Luo

Xu Ran

Jiantao Hu

Jianfang Chen

Ester Fernandez-Salas

Hacer Karatas

Chong Qin

Weiguo Xiang

Ting Zhao

Bo Wen

Jianyong Chen

Dajun Yang

Yunlong Zhou

Yu Jing

Ming Guo

Lingling Jiao

Rohan Rej

Haibin Zhou

Yangbing Li

Jiuling Yang

Xin Han

Zhuo Chen

Xu Qian

Donna McEachem

Zhou Chen

Donna Mceacherm

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): Formula (I) and the pharmaceutically acceptable salts and solvates thereof, wherein R, R, R, R, R, R, Y, &#x2550;, Ar, W, L, and B are as defined as set forth in the specification. The present disclosure also provides compounds of Formula (I)I for use to treat a condition or disorder responsive to inhibition and/or degradation of BET bromodomains such as cancer. 

BET bromodomain protein degraders with cleavable linkers

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 compounds represented by Formula I: and the pharmaceutically acceptable salts, hydrates, and solvates thereof, wherein B, R, R, Q, Q&#x2033;, L, X, Y, and Z 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. 

BET protein degraders

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

Disclosed herein are certain indoloquinolone compounds, methods of preparation thereof, pharmaceutical compositions thereof, and uses thereof, such as their uses as ALK inhibitors.

Indoloquinolone compounds as anaplastic lymphoma kinase (ALK) inhibitors

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

Inhibitors of Bcl-2/Bcl-xL and compositions containing the same are disclosed. Methods of using the Bcl-2/Bcl-xL inhibitors in the treatment of diseases and conditions wherein inhibition of Bcl-2/Bcl-xL provides a benefit, like cancers, also are disclosed.

Bcl-2/Bcl-xL inhibitors and therapeutic methods using the same

BCL-2/BCL-XL inhibitors and therapeutic methods using the same

Growing community of inventors

Ann Arbor, MI, United States of America

Longchuan Bai