Elan Pharmaceuticals, Inc.

Srx Cardio, LLC

Onyx Therapeutics, Inc.

Imago Pharmaceuticals, Inc.

Other

Simeon Bowers

Anjali Pandey

Thomas E Barta

Roy K Hom

Jonathan William Bourne

Anh P Truong

Michael Mark Muehlemann

Kyle D Monroe

Andrei William Konradi

R Jeffrey Neitz

Gary D Probst

Albert W Garofalo

Jennifer Sealy

Hing L Sham

Dustin L McMinn

Henry Johnson

David C Moebius

Xiaocong Michael Ye

Christopher Michael Semko

Dean R Artis

Darren B Dressen

Ying-Zi Xu

Danielle Aubele

Marc Adler

Matthew N Mattson

Gergely Toth

Yong-Liang Zhu

Jing Wu

John P Anderson

Martin Neitzel

Robert Galemmo

Paul Beroza

Varghese John

Jay S Tung

Louis Brogley

Shendong Yuan

John Alan Tucker

Minghua Sun

Barbara Jagodzinska

Michael S Dappen

Michel Maillard

Jiang Zhu

Mark Karbarz

Jose Aquino

Neerav Shah

Robert A Galemmo, Jr

Raymond Ng

Danielle L Aubele

Maurizio Franzini

Dean Richard Artis, I

Dustin Mcminn

Anh Truong

The present disclosure relates to novel compounds capable of binding to PCSK9, thereby modulating PCSK9 biological activity. Also provided are compositions comprising these compounds, methods of preparing the compounds, and methods for use of the compounds in the treatment of PCSK9-related conditions and diseases.

Compounds for the modulation of proprotein convertase subtilisin/kexin type 9 (PCSK9)

This invention is related to the field of PCSK9 biology and the composition and methods of use of small organic compounds as ligands for modulation of PCSK9 biological activity. In particular, the invention provides compositions of small organic compounds that modulate circulating levels of low density lipoproteins by altering the conformation of the protein PCSK9. Binding these small organic compound ligands to PCSK9 alters the conformation of the protein, modifying the interaction between PCSK9 and an endogenous low density lipoprotein receptor, and can lead to reduced or increased levels of circulating LDL-cholesterol. High LDL-cholesterol levels are associated with increased risk for heart disease. Low LDL-cholesterol levels may be problematic in other conditions, such as liver dysfunctions; thus, there is also utility for small organic compound ligands and can raise LDL levels.

Composition and methods of use of tetrahydroisoquinoline small molecules to bind and modulate PCSK9 protein activity

This invention is related to the field of PCSK9 biology and the composition and methods of use of small organic compounds as ligands for modulation of PCSK9 biological activity. In particular, the invention provides compositions of small organic compounds that modulate circulating levels of low density lipoproteins by altering the conformation of the protein PCSK9. Binding these small organic compound ligands to PCSK9 alters the conformation of the protein, modifying the interaction between PCSK9 and an endogenous low density lipoprotein receptor, and can lead to reduced or increased levels of circulating LDL-cholesterol. High LDL-cholesterol levels are associated with increased risk for heart disease. Low LDL-cholesterol levels may be problematic in other conditions, such as liver dysfunction; thus, there is also utility for small organic compound ligands that can raise LDL levels.

Phenylalanine small organic compounds to directly modulate PCSK9 protein activity

Phenylpiperazine proprotein convertase subtilisin/kexin type 9 (PCSK9) modulators and their use

The present disclosure relates to novel compounds, methods, and compositions capable of binding to PCSK9, thereby modulating PCSK9 proprotein convertase enzyme activity, for treatment of a disease or condition mediated, at least in part, by PCSK9. The compounds of the disclosure include compounds Formula (I).

Compounds for binding proprotein convertase subtilisin/kexin type 9

Provided herein are tripeptide epoxy ketone protease inhibitors, methods of their preparation, related pharmaceutical compositions, and methods of using the same. For example, provided herein are compounds of Formula (X): and pharmaceutically acceptable salts and compositions including the same. The compounds and compositions provided herein may be used, for example, in the treatment of diseases including inflammation and neurodegenerative disease.

Tripeptide epoxy ketone protease inhibitors

Composition and methods of use of novel phenylalanine small organic compounds to directly modulate PCSK9 protein activity

Peptide epoxyketone immunoproteasome inhibitors

The present invention provides compounds having a structure according to Formula I: (I) or a salt or solvate thereof, wherein R1, R2, R3 and R4 are defined herein. The invention further provides pharmaceutical compositions including the compounds of the invention and methods of making and using the compounds and compositions of the invention, e.g., in the treatment and prevention of various disorders, such as Parkinson's disease. 

Substituted cinnolines as inhibitors of LRRK2 kinase activity

The present disclosure provides inhibitors of c-Jun N-terminal kinases (JNK) having a structure according to the following formula: or a salt or solvate thereof, wherein ring A, C, C, Z, R, W and Cy are defined herein. The disclosure further provides pharmaceutical compositions including the compounds of the present disclosure and methods of making and using the compounds and compositions of the present disclosure, e.g., in the treatment and prevention of various disorders, such as Alzheimer's disease.

Inhibitors of Jun N-terminal kinase

Compounds are provided having a structure according to Formula (I): wherein A, A, A, Y, R, R, R, R, R, R, m, n and p are defined herein. Further provided are pharmaceutical compositions including the compounds provided and methods of making and using the compounds and compositions as provided, e.g., in the treatment and prevention of various disorders, such as Alzheimer's disease. 

Spirocyclic dihydro-thiazine and dihydro-oxazine BACE inhibitors, and compositions and uses thereof

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Oakland, CA, United States of America

Simeon Bowers