University of Michigan

Ascentage Pharma (suzhou) Co., Ltd.

Ascentage Pharma Group Corp Limited

Jiangsu Ascentage Biomed Development Inc.

Ascentage Pharma Co., Ltd.

Chao-Yie Yang

Shaomeng Wang

Liu Liu

Longchuan Bai

Bing Zhou

Donna McEachern

Jianyong Chen

Jeanne Stuckey

Duxin Sun

Xiaoqin Li

Yunlong Zhou

Yu Jing

Jennifer Lynn Meagher

Arul M Chinnaiyan

Liang Xin Xu

Zaneta Nikolovska-Coleska

Angelo Aguilar

Haiying Sun

Yujun Zhao

Fuming Xu

Yang Hu

Jiantao Hu

Lingling Jiao

Irfan A Asangani

Hao Chen

Guozhi Tang

Ruijuan Luo

Ester Fernandez-Salas

Dajun Yang

Jianfeng Lu

Ming Guo

Xu Ran

Chong Qin

Rohan Rej

Hacer Karatas

Dongbo Li

Wenming Chen

Chao Li

Haibin Zhou

Liyue Huang

Jianfang Chen

Jiuling Yang

Yangbing Li

Weiguo Xiang

Xin Han

Zhuo Chen

Mi Wang

Liugen Li

Xianchan Zha

Changwei Wang

Binghua Sheng

Wenliang Hu

Leilei Zhao

Chengzhe Wu

Naoyuki G Saito

Dengyou Zhang

Donna McEachem

Canhui Zheng

Xu Qian

Xuyuan Dong

Donna Mceacherm

Provided are compounds represented by Formula IA: (IA), and the pharmaceutically acceptable salts and solvates thereof, wherein R, R, R, L, L, L, X, A, B and C are as defined as set forth in the specification. Also provided compounds of Formula IA for use to treat a condition or disorder responsive to Mcl-1 inhibition such as cancer.

Macrocyclic fused pyrazoles as Mcl-1 inhibitors

The present disclosure provides compounds represented by Formula I: wherein R, R, R, and Rare as defined in the specification, and the salts and solvates thereof. Compounds of Formula I are EED inhibitors. EED inhibitors are useful for the treatment of cancer and other diseases.

Imidazopyrimidines as EED inhibitors and the use thereof

Disclosed is compound of formula I and the pharmaceutically acceptable salts and solvates thereof, wherein R, R, R, R, L, L, #, #, # are as defined as set forth in the re) specification. Disclosed is compound of formula I for use to treat a condition or disorder responsive to Mcl-1 inhibition such as cancer.

Macrocyclic indoles as Mcl-1 inhibitors

The present disclosure provides fused 1,4-oxazepines and related analogs represented by Formula (I) and the pharmaceutically acceptable salts, hydrates, and solvates thereof, wherein R, R, R, R, R, R, R, A, and Y are 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. 

Fused 1,4-oxazepines and related analogs as BET bromodomain inhibitors

Provided are compounds represented by Formula (I-A) and the pharmaceutically acceptable salts and solvates thereof, wherein R, R, R, R, R, X, Y, Z, Z, W, and (aa) are as defined as set forth in the specification. Provided are also compounds of Formula (I-A) for use to treat a condition or disorder responsive to Mcl-1 inhibition such as cancer. 

Macrocyclic spiroethers as Mcl-1 inhibitors

The present disclosure provides compounds represented by Formula I and II: and the pharmaceutically acceptable salts and solvates thereof, wherein R, R, R, X, W, Y, and Z are as defined as set forth in the specification. The present disclosure also provides compounds of Formula I and II for use to treat a condition or disorder responsive to LSD1 inhibition such as cancer. 

Pyrrolo[2,3-C]pyridines and related analogs as LSD-1 inhibitors

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

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

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 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

The invention relates to conformationally constrained mimetics of Smac which function as inhibitors of Inhibitor of Apoptosis Proteins. The invention also relates to the use of these mimetics for inducing apoptotic cell death and for sensitizing cells to inducers of apoptosis.

Conformationally constrained Smac mimetics and the uses thereof

Growing community of inventors

Ann Arbor, MI, United States of America

Chao-Yie Yang