University of Michigan

Ascentage Pharma (suzhou) Co., Ltd.

Ascentage Pharma Group Corp Limited

University of Kansas

Jiangsu Ascentage Biomed Development Inc.

Jianyong Chen

Shaomeng Wang

Chao-Yie Yang

Lingling Jiao

Liang Xin Xu

Liu Liu

Zaneta Nikolovska-Coleska

Donna McEachern

Dajun Yang

Haiying Sun

James H Woods

Gregory Collins

John F W Keana

Yunlong Zhou

Yu Jing

Ming Guo

Guozhi Tang

Beth Levant

Longchuan Bai

Dongguang Qin

Chao Li

Shanghai Yu

Hao Chen

Xuyuan Dong

Zengjian Hu

Naoyuki G Saito

Chengzhe Wu

Leilei Zhao

Liugen Li

Binghua Sheng

Xu Qian

Wenliang Hu

The present disclosure provides compounds having Formula I-A: and the pharmaceutically acceptable salts and solvates thereof, wherein A, X, X, XR, R, E, andare as defined as set forth in the specification. The present disclosure also provides compounds of Formula I-A for use to treat a disease, disorder, or condition responsive to Bcl-2 protein inhibition such as cancer.

N-(phenylsulfonyl)benzamides and related compounds as Bcl-2 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: wherein R, A, A, A, A, E, E, E, L, Q, Z, and are as defined in the specification, and the pharmaceutically acceptable salts and solvates thereof. Compounds of Formula I are KRAS inhibitors and are thus useful to treat cancer and other diseases.

Spirocyclic tetrahydroquinazolines

The present disclosure provides compounds represented by Formula I: and the pharmaceutically acceptable salts, hydrates, and solvates thereof, wherein R, R, R, R, R, R, R, R, and Rare 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.

Aminopyrimidines as ALK inhibitors

The present disclosure provides compounds having Formula I-A: and the pharmaceutically acceptable salts and solvates thereof, wherein A, X, X, XR, RE, and = are as defined as set forth in the specification. The present disclosure also provides compounds of Formula I-A for use to treat a disease, disorder, or condition responsive to Bcl-2 protein inhibition such as cancer. 

N-(phenylsulfonyl)benzamides and related compounds as bcl-2 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

N-(phenylsulfonyl)benzamides and related compounds as BCL-2 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

Potent and selective ligands for the dopamine 3 (D) receptor are disclosed. The Dreceptor ligands have a structural formula: wherein Ris Calkyl or Ccycloalkyl; or wherein Ris substituted with one or two halogen(s) or OCalkyl.

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Potent and selective ligands for the dopamine 3 (D) receptor are disclosed. The D3 receptor ligands have a structural formula (I) wherein X is C&#x2550;O or SO, Ris Calkyl, Ris aryl, heteroaryl, aryl, &#x2014;(CH)aryl, or &#x2014;(CH)heteroaryl, and n is 0 or 1. Methods of using the Dreceptor ligands in the treatment of diseases and conditions wherein modulation of the Dreceptor provides a benefit also are disclosed. 

The invention relates to small molecules which function as inhibitors of the interaction between p53 and MDM2. The invention also relates to the use of these compounds for inhibiting cell growth, inducing cell death, inducing cell cycle arrest and/or sensitizing cells to additional agent(s).

Small molecule inhibitors of MDM2 and the uses thereof

The present invention relates to naturally occurring and chemically synthesized small molecule antagonists of XIAP family proteins. In particular, the present invention provides embelin and other XIAP inhibitors and methods of using these compounds as antagonists of the anti-apoptotic effects of XIAP family member proteins. The present invention also provides methods for treating diseases and pathologies (e.g., neoplastic diseases).

Small molecule antagonists of XIAP family proteins

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

This invention relates to relates to methods for producing gossypol acetic acid co-crystals and (&#x2212;)-gossypol acetic acid co-crystals. The invention also relates to pharmaceutical compositions comprising gossypol acetic acid co-crystals and (&#x2212;)-gossypol acetic acid co-crystals and the use of gossypol acetic acid co-crystals and (&#x2212;)-gossypol acetic acid co-crystals for inducing apoptosis in cells and for sensitizing cells to the induction of apoptotic cell death.

Growing community of inventors

Ann Arbor, MI, United States of America

Jianyong Chen