University of Michigan

Georgetown University

Ascentage Pharma (Suzhou) Co., Ltd.

Ascentage Pharma Group Corp Limited

Sanofi

University of Kansas

Adherex Technologies, Inc.

Jiangsu Ascentage Biomed Development Inc.

Ascenta Licensing Corporation

Ascentage Pharma Co., Ltd.

Shaomeng Wang

Donna McEachern

Chao-Yie Yang

Liu Liu

Jianyong Chen

Longchuan Bai

Angelo Aguilar

Zaneta Nikolovska-Coleska

Bing Zhou

Duxin Sun

Haiying Sun

Dajun Yang

Jeanne Stuckey

Jianfeng Lu

Yujun Zhao

Su Qiu

Dongguang Qin

Fuming Xu

Liang Xin Xu

Istvan J Enyedy

Yang Hu

Jiantao Hu

Sanjeev Kumar

Wei Sun

Xiaoqin Li

Jennifer Lynn Meagher

Guoping Wang

Shanghai Yu

Arul M Chinnaiyan

Ke Ding

Irfan A Asangani

Haibin Zhou

Qian Cai

Xu Ran

Hacer Karatas

Ruijuan Luo

Chong Qin

Rohan Rej

Yuefeng Peng

Denzil Bernard

Alan P Kozikowski

Ester Fernandez-Salas

Chen-Yong Lin

Yunlong Zhou

Robert B Dickson

Guozhi Tang

Peng Zou

Yipin Lu

Jiuling Yang

Weiguo Xiang

Liyue Huang

Jiangyong Chen

Jianfang Chen

Yangbing Li

James H Woods

Lingling Jiao

Lixin Qiao

Hao Chen

Michael D Johnson

Bo Wen

Zhuo Chen

Yi Sun

Gregory Collins

Beth Levant

Shilin Xu

Ting Zhao

Tianfeng Xu

Wenming Chen

Dongbo Li

Xin Han

Yali Dou

Elizabeth Townsend

Orest W Blaschuk

Barbara J Gour

John F W Keana

Yu Jing

Ming Guo

Marc E Lippman

Feng Ni

Zhigang Chen

Chao Li

Anmar Ali

Stephanie Denise Michaud

Liangyou Rui

Zenjian Hu

Canhui Zheng

Fang Cao

Rong Sheng

Donna McEachem

Carlos Garcia-Echeverria

Renxiao Wang

Zengjian Hu

Naoyuki G Saito

Chengzhe Wu

Leilei Zhao

Binghua Sheng

Wenliang Hu

The present disclosure provides compounds represented by Formula (I) and the pharmaceutically acceptable salts and solvates thereof, wherein R, R, R, R, A, E, E, M, and Q are as set forth in the specification. Compounds of Formula (I) are STAT protein degraders and thus are useful for the treatment of cancer and other diseases.

Small molecule STAT protein degraders

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

Compounds of formula (I) as inhibitors of DCN1 and compositions containing the same are disclosed. Methods of using the DCN1 inhibitors in the treatment of diseases and conditions wherein inhibition of DCN1 provides a benefit, like oxidative stress-related diseases and conditions, neurodegenerative diseases and conditions, metabolic disorders, and muscular nerve degeneration, also are disclosed.

Small molecule DCN1 inhibitors and therapeutic methods using the same

The present disclosure provides compounds represented by Formula I: and the pharmaceutically acceptable salts and solvates thereof, wherein 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 LSD1 inhibition such as cancer.

Imidazo[4,5-c]pyridine compounds as LSD-1 inhibitors

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

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 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-A: A-L-BI-A and the pharmaceutically acceptable salts, hydrates, and solvates thereof, wherein A, B, and L1 are as defined as set forth in the specification. The present disclosure also provides compounds of Formula I-A for use to treat a condition or disorder responsive to degradation of MDM2 protein such as cancer.

MDM2 protein degraders

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, 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 fused 1,4-diazepines represented by Formula (I): and the pharmaceutically acceptable salts and solvates thereof, wherein A, E, R, R, R, R, R, and Ar are as defined as set forth in the specification. The present disclosure is also directed to the use of compounds having Formula (I) to treat diseases, conditions, or disorders responsive to inhibition of BET bromodomain proteins such as cancer. 

Fused 1,4-diazepines as BET bromodomain inhibitors

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Saline, MI, United States of America

Shaomeng Wang