Icahn School of Medicine at Mount Sinai

The University of North Carolina at Chapel Hill

Glaxo Group Limited

Glaxosmithkline LLC

Duke University

Jian Jin

Paul Adrian Wyman

Brian W Budzik

David G Cooper

Ian Thomson Forbes

Jing Liu

Dongchuan Shi

Graham Walker

Vincenzo Garzya

Ramon Parsons

Paul William Smith

Xiaobao Yang

Kevin J Duffy

Stephen Frye

Antony N Shaw

Kenneth Wiggall

Bryan Leo Roth

Duke M Fitch

Ronggang Liu

Xufen Yu

Ilias Stratikopoulos

Anqi Ma

Kyle Butler

Nate Hathaway

Michael R Palovich

Dramane Ibrahim Laine

Brent W McCleland

Ralph A Rivero

Matthew Robert Redinbo

Chongjie Zhu

Anthony W J Cooper

Yonghui Wang

Poulikos Poulikakos

Lindsey James

He Chen

Jianping Hu

Dongxu Li

Gang Wang

Jieli Wei

Anna Chiarella

Joshua Brody

Md Kabir

Hyerin Yim

Steven Burakoff

Sansana Sawasdikosol

Nina Bhardwaj

H Umit Kaniskan

Jia Xu

Haibo Xie

Ian MacDonald

Hyeong-min Lee

Yuna Kim

Yong-hui Jiang

Tamer Ahmed

Xuewei Wu

Zoi Karoulia

Yan Xiong

Ranathunga Arachchillage Yamuna Ariyarathna

Sam Pellock

David Gwyn Cooper

Yann Louchart

Disclosed are Hematopoietic Progenitor Kinase 1 (HPK1) degradation/disruption compounds including a HPK1 ligand, a degradation/disruption tag and a linker, and methods for use of such compounds in the treatment of HPK1-mediated diseases.

Heterobifunctional compounds as degraders of HPK1

Methods for designing bivalent compounds which selectively degrade/disrupt EZH2 and compositions and methods of using such degraders/disruptors to treat EZH2-mediated cancer are provided.

Compositions and methods for treating EZH2-mediated cancer

Disclosed herein are WD40 repeat domain protein 5 (WDR5) degradation/disruption compounds including a WDR5 ligand, a degradation/disruption tag, and a linker, and methods of using such compounds in the treatment of WDR5-mediated diseases.

WD40 repeat domain protein 5 (WDR5) degradation/disruption compounds and methods of use

This disclosure relates to heterobifunctional compounds (e.g., bi-functional small molecule compounds), compositions comprising one or more of the heterobifunctional compounds, and to methods of use the heterobifunctional compounds for the treatment of certain disease in a subject in need thereof. The disclosure also relates to methods for identifying such heterobifunctional compounds.

Mitogen-activated protein kinase kinase (MEK) degradation compounds and methods of use

The present disclosure relates to bifunctional chemical epigenetic modifiers, and methods of making, kits and using the bifunctional chemical epigenetic modifiers. The bifunctional chemical epigenetic modifiers can include a FK506 molecule or derivative thereof, a linker and a bifunctional ligand. The bifunctional ligand can be a histone deacetylase inhibitor.

Bifunction chemical epigenetic modifiers and methods of use

The invention described herein relates to certain pyrimidinetrione N-substituted glycine derivatives of formula (I) which are antagonists of HIF prolyl hydroxylases and are useful for treating diseases benefiting from the inhibition of this enzyme, anemia being one example.

Prolyl hydroxylase inhibitors

Methods for designing heterobifunctional small molecules which selectively degrade/disrupt CDK4/6 and compositions and methods of using such degraders/disruptors to treat CDK4/6-mediated cancer are provided.

Compositions and methods for treating CDK4/6-mediated cancer

Disclosed herein are serine threonine kinase (AKT) degradation/disruption compounds including an AKT ligand, a degradation/disruption tag, and a linker, and methods of using such compounds in the treatment of AKT-mediated diseases.

Serine threonine kinase (AKT) degradation / disruption compounds and methods of use

Compounds and compositions are provided that comprise selective b-glucuronidase inhibitors. The compounds and compositions can ameliorate the side effects of chemotherapeutic agents and can improve the efficacy of such agents, including irinotecan and non-steroidal anti-inflammatory drugs.

Inhibitors of microbial beta-glucuronidase enzymes and uses thereof

The invention provides pharmaceutical compositions and methods of use thereof for treating Prader-Willi syndrome. More specifically, the invention provides pharmaceutical compositions that when administered inhibit the G9a driven methylation of histone H3 lysine 9.

Compositions and methods for the treatment of Prader-Willi syndrome

The present disclosure relates to chemical compounds that inhibit HP1-mediated heterochromatin formation, pharmaceutical compositions containing such compounds, methods of identifying such compounds, and their use in the treatment of disorders related to heterochromatin formation such as, for example, a disorder of cellular proliferation (e.g., cancer). This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

Heterochromatin gene repression inhibitors

The present invention relates to novel functionally selective ligands of dopamine Dreceptors, including agonists, antagonists, and inverse agonists. The invention further relates to the use of these compounds for treating central nervous system disorders related to Dreceptors.

[object Object]

Compounds of formula (I) and salts and solvates are provided: wherein Ris fluoro, Ris selected from hydrogen, halogen, cyano, Calkyl, Calkyl substituted with one or more fluorine atoms, Calkoxy, and Calkoxy substituted with one or more fluorine atoms; and Ris selected from halogen, cyano, Calkyl, Calkyl substituted with one or more fluorine atoms, Ccycloalkyl, Ccycloalkyl substituted with one or more fluorine atoms, Calkoxy and Calkoxy substituted with one or more fluorine atoms, and Q is hydrogen or Calkyl. The compounds are expected to be useful for therapy, for example in the treatment of psychotic disorders and cognitive impairment.

Compounds which have activity at M1 receptor and their uses in medicine

Growing community of inventors

New York, NY, United States of America

Jian Jin