University of Michigan

Jiangsu Ascentage Biomed Development Inc.

Donna McEachern

Shaomeng Wang

Liu Liu

Duxin Sun

Longchuan Bai

Yujun Zhao

Angelo Aguilar

Bing Zhou

Arul M Chinnaiyan

Chao-Yie Yang

Jeanne Stuckey

Xiaoqin Li

Jennifer Lynn Meagher

Irfan A Asangani

Xu Ran

Ruijuan Luo

Sanjeev Kumar

Wei Sun

Yang Hu

Shanghai Yu

Peng Zou

Ester Fernandez-Salas

Jianyong Chen

Jianfeng Lu

Fuming Xu

Hacer Karatas

Jianfang Chen

Ting Zhao

Bo Wen

Dajun Yang

Haiying Sun

Ming Guo

Yu Jing

Yunlong Zhou

Lingling Jiao

Jiantao Hu

Chong Qin

Weiguo Xiang

Yangbing Li

Jiuling Yang

Zhuo Chen

Xu Qian

Rong Sheng

Xuyuan Dong

Zhou Chen

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: wherein R, R, R, R, R, R, R, A, 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 cancer or any other disease, condition, or disorder that is responsive to degradation of MDM2 protein.

Small molecule MDM2 protein degraders

The present disclosure provides compounds represented by Formula (I), and the pharmaceutically acceptable salts and solvates thereof wherein R, R, R, R, R, R, R, R, R, E 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 inhibition of ALK such as cancer. and &#xae;

5,6-dihydro-11H-indolo[2,3-B]quinolin-11-ones as alk inhibitors

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

Inhibitors of MDM2 and MDM2-related proteins and compositions containing the same are disclosed. Methods of using the MDM2 inhibitors in the treatment of diseases and conditions wherein inhibition of an interaction between p53 and MDM2 provides a benefit, like cancers, also are disclosed.

MDM2 inhibitors and therapeutic methods using the same

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

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

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

Bivalent inhibitors of IAP proteins and therapeutic methods using the same

Growing community of inventors

Ann Arbor, MI, United States of America

Donna McEachern