Arvinas Operations, Inc.

Merck Sharp + Dohme Corp.

Schering Corporation

Yale University

Schering-plough Corporation

Schering Coporation

Genentech, Inc.

Michael Berlin

Robert G Aslanian

Kevin D McCormick

Jing Wang

Andrew Philip Crew

Hanqing Dong

Pauline C Ting

Christopher W Boyce

Manuel De Lera Ruiz

Yimin Qian

Junying Zheng

Wing C Tom

Pietro Mangiaracina

Neng-Yang Shih

Stuart B Rosenblum

Lawrence B Snyder

Daniel M Solomon

Younong Yu

Craig M Crews

Rongze Kuang

Kurt Zimmermann

Jianhua Chao

Yeon-Hee Lim

Xianhai Huang

Xin Chen

Anandan Palani

Amjad Ali

Dong Xiao

Purakkattle J Biju

Meizhong Jin

Ashwin Umesh Rao

Andrew William Stamford

John J Piwinski

Michael Man-Chu Lo

Jayaram R Tagat

Joseph A Kozlowski

Peter Scott Dragovich

Huifen Chen

Mwangi W Mutahi

Xiaohong Zhu

Heping Wu

Qingbei Zeng

Yonglian Zhang

Leanna Staben

Walter Won

Steven M Sparks

Wei Zhang

Jie Wu

Henry A Vaccaro

Gang Zhou

Salem Fevrier

Jianhua Cao

Ning Shao

Li Dong

Hongwu Wang

Caterina Ferraro

Kam Siu

Joseph Michael Kelly

Tao Yu

Qiaolin Deng

Wei Zhou

Jae-Hun Kim

Erika Araujo

Erika Marina Vieira Araujo

Ying Huang

Guoqing Li

Rajan Anand

Timothy J Henderson

Keith R Hornberger

Paul Tempest

Tanweer A Khan

Nicolas Zorn

Chia-Yu Huang

Angela Marie Cacace

Bo Liang

John A Hey

Joe F Lee

Gioconda V Gallo

David Kim

Sylvia Joanna Degrado

Chander Shekher Celly

Gioconda V Gallo-Etienne

Liwu Hong

Dan Sherman

John C Anthes

Hongwu Yang

Yoon Joo Lee

Rema Danielle Bitar

Stephanie Louise Ciesla

Youngong Yu

David Won-Shik Kim

Alexander L Tung

Alexey Ishchenko

Dong Won-Shik Kim

Yushi Xiao

Julian T Chandler

Bifunctional compounds, which find utility as modulators of non-receptor Leucine-rich repeat kinase 2 (LRRK2), are described herein. In particular, the bifunctional compounds of the present disclosure contain on one end a moiety that binds to the cereblon E3 ubiquitin ligase and on the other end a moiety which binds LRRK2, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The bifunctional compounds of the present disclosure exhibit a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aberrant regulation of the target protein are treated or prevented with compounds and compositions of the present disclosure.

Selective modulators of mutant LRRK2 proteolysis and associated methods of use

The description relates to cereblon E3 ligase binding compounds, including bifunctional compounds comprising the same, which find utility as modulators of targeted ubiquitination, especially inhibitors of a variety of polypeptides and other proteins which are degraded and/or otherwise inhibited by bifunctional compounds according to the present disclosure. In particular, the description provides compounds, which contain on one end a ligand which binds to the cereblon E3 ubiquitin ligase and on the other end a moiety which binds a target protein such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of that protein. Compounds can be synthesized that exhibit a broad range of pharmacological activities consistent with the degradation/inhibition of targeted polypeptides of nearly any type.

Cereblon ligands and bifunctional compounds comprising the same

Bifunctional compounds, which find utility as modulators of B-cell lymphoma 6 protein (BCL6; target protein), are described herein. In particular, the bifunctional compounds of the present disclosure contain on one end a Von Hippel-Lindau, cereblon, Inhibitors of Apotosis Proteins or mouse double-minute homolog 2 ligand that binds to the respective E3 ubiquitin ligase and on the other end a moiety which binds the target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The bifunctional compounds of the present disclosure exhibit a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aggregation or accumulation of the target protein are treated or prevented with compounds and compositions of the present disclosure.

Modulators of BCL6 proteolysis and associated methods of use

The present invention relates to bifunctional compounds, which find utility as modulators of targeted ubiquitination, especially inhibitors of a variety of polypeptides and other proteins which are degraded and/or otherwise inhibited by bifunctional compounds according to the present invention. In particular, the present invention is directed to compounds, which contain on one end a VHL ligand which binds to the ubiquitin ligase and on the other end a moiety which binds a target protein such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of that protein. The present invention exhibits a broad range of pharmacological activities associated with compounds according to the present invention, consistent with the degradation/inhibition of targeted polypeptides.

Compounds and methods for the enhanced degradation of targeted proteins

Compounds and methods for the targeted degradation of bromodomain- containing proteins

Bifunctional compounds, which find utility as modulators of leucine-rich repeat kinase 2 (LRRK2), are described herein. In particular, the hetero-bifunctional compounds of the present disclosure contain on one end a moiety that binds to the cereblon E3 ubiquitin ligase and on the other end a moiety which binds LRRK2, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The hetero-bifunctional compounds of the present disclosure exhibit a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aberrant regulation of the target protein are treated or prevented with compounds and compositions of the present disclosure.

Indazole based compounds and associated methods of use

The present disclosure relates to bifunctional compounds, which find utility as modulators of tau protein. In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a VHL or cereblon ligand which binds to the E3 ubiquitin ligase and on the other end a moiety which binds tau protein, such that tau protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of tau. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of tau protein. Diseases or disorders that result from aggregation or accumulation of tau protein are treated or prevented with compounds and compositions of the present disclosure.

Tau-protein targeting compounds and associated

The present disclosure relates to bifunctional compounds, which find utility as modulators of enhancer of zeste homolog 2 (target protein). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a Von Hippel-Lindau, cereblon, Inhibitors of Apotosis Proteins or mouse double-minute homolog 2 ligand which binds to the respective E3 ubiquitin ligase and on the other end a moiety which binds the target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aggregation or accumulation of the target protein are treated or prevented with compounds and compositions of the present disclosure.

Compounds and methods for the targeted degradation of enhancer of zeste homolog 2 polypeptide

The present disclosure relates to bifunctional compounds, which find utility as modulators of &#x3b1;-synuclein (target protein). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a Von Hippel-Lindau, cereblon. Inhibitors of Apotosis Proteins or mouse double-minute homolog 2 ligand which binds to the respective E3 ubiquitin ligase and on the other end a moiety which binds the target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aggregation or accumulation of the target protein are treated or prevented with compounds and compositions of the present disclosure.

Modulators of alpha-synuclein proteolysis and associated methods of use

Compounds and methods for the targeted degradation of bromodomain-containing proteins

Disclosed are compounds having the structure of Formula I, or a pharmaceutically acceptable salt of any thereof: wherein: 'Z' and Rare defined herein, which compounds are believed suitable for use in selectively antagonizing the A2a receptors, for example, those found in high density in the basal ganglia. Such compounds and pharmaceutical formulations are believed to be useful in treatment or management of neurodegenerative diseases, for example, Parkinson's disease, or movement disorders arising from use of certain medications used in the treatment or management of Parkinson's disease. 

Substituted imidazo[1,2-c]quinazolines as A2A antagonists

Tau-protein targeting PROTACs and associated methods of use

Growing community of inventors

Flemington, NJ, United States of America

Michael Berlin