Sanford Burnham Prebys Medical Discovery Institute

Sanford-burnham Medical Research Institute

Daiichi Sankyo Company, Limited

University of Michigan

Wayne State University

University of Kansas-ku Medical Center Research Institute

Ardea Biosciences, Inc

La Jolla Institute of Allergy & Immunology

National Institutes of Health, a Component of the US Dept. of Health & Human Services

Duke University

Mayo Foundation for Medical Education and Research

The Royal Institution for the Advancement of Learning/mcgill University

Boundless Bio, Inc.

Selexagen Therapeutics, Inc.

Sandford Burnham Prebys Medical Discovery Institute

Anthony B Pinkerton

Layton H Smith

Patrick R Maloney

Paul M Hershberger

Michael P Hedrick

Robert J Ardecky

Takashi Tsuji

Jiwen Zou

Danielle McAnally

Yuko Yamamoto

Shojiro Miyazaki

Satyamaheshwar Peddibhotla

Masanori Izumi

Masaharu Inui

Eduard A Sergienko

Kaori Soma

Santhi Reddy Ganji

Thomas D Y Chung

Yoshiyuki Kobayashi

Keisuke Suzuki

Osamu Suzuki

Jean-Michel Andre Vernier

Takuya Ikeda

Takahiro Nagayama

Nicholas D P Cosford

Russell Dahl

Jose Luis Millan

Naoki Miyoshi

Taeko Shinozaki

Jun Tanaka

Samedy Ouk

Jeffrey Aube

Jennifer Elizabeth Golden

Tsuyoshi Nakamura

Daniel Patrick Flaherty

Randal J Kaufman

Nunzio Bottini

Hampton Sessions

Stephanie M Stanford

Mayuko Akiu

Edward Hampton Sessions, Jr

Koji Terayama

Mika Yokoyama

Christian A Hassig

Yasunobu Kurosaki

Marcos Gonzalez-Lopez

Alex Shaginian

Stephen Gardell

Andrew M Fribley

Marc G Caron

William Charles Ripka

Lawrence S Barak

Stephanie Hopkins

Pierre-Yves Bounaud

Richard J Bram

Stephen Todd Meyer

Patrick O'Connor

Masamichi Kishida

Kevin Edward Brown

Michael R Jackson

John May

Ze'ev Ronai

Yongmei Feng

Ivan Topisirovic

Koutaro Ishibashi

Eduard Serguienko

Ian Pass

Jacques Mauger

Rachelle Janette Elsdon

Yen Pham Hong Truong

Lawrence Barak

Danielle Mcanally

Edward Hampton Sessions

Nicholas DP Cosford

Santhi R Ganji

Thomas Chung

Aleksandr Shaginian

Provided herein are small molecule agonists of the apelin receptor for the treatment of disease. The compounds disclosed herein are useful for the treatment of a range of cardiovascular, renal and metabolic conditions. The present invention is based on the seminal discovery of a series of potent small molecule agonists of the apelin receptor, which are useful for the treatment of diseases including heart failure, chronic kidney disease, hypertension, and metabolic disorders such as insulin resistance/diabetes and obesity. The compounds disclosed herein are highly specific for the apelin receptor versus the angiotensin II receptor (ATI).

Agonists of the apelin receptor and methods of use thereof

The present invention relates to a novel fused ring compound having urea structure that exhibits excellent NAMPT activating effect, and a method using the same for treating/preventing metabolic disorder, cardiovascular and kidney disease, mitochondrial disease, neurodegenerative disease, ocular disease, and muscle wasting disorder. The present invention provides a compound represented by following formula (I) or a pharmacologically acceptable salt:

Fused ring compound having urea structure

Provided herein are agonists of the apelin receptor for the treatment of disease. The compounds disclosed herein are useful for the treatment of a range of cardiovascular, renal and metabolic conditions.

Apelin receptor agonists and methods of use thereof

The present invention relates to a novel azole derivative as an apelin receptor agonist and a method for treating cardiovascular disease, diabetic disease, renal disease, hypertension, and arteriosclerosis, etc., using the same. The present invention provides a compound represented by formula (I) or a pharmacologically acceptable salt thereof wherein Xrepresents —N═ or —CH═, Xrepresents —CH═ or —N═, Rand Reach represent a Cto Calkoxy group or the like, Rrepresents a heteroaryl group (the heteroaryl group is optionally substituted by a methyl group or the like) or the like, and Rrepresents a Cto Calkylthio group or a Cto Calkenyl group (the Cto Calkylthio group and the Cto Calkenyl group are each optionally substituted by one carboxy group or the like) or the like.

Azole derivatives as apelin receptor agonist

The present application provides, inter alia, a compound of Formula (I): or a pharmaceutically acceptable salt thereof, wherein Y, Ar, X, X, X, R, R, R, R, R, and Rare as described herein. Methods of making these compounds and methods of using these compound for treating diseases such as cancer are also provided.

PIKfyve inhibitors

Provided herein are agonists of the apelin receptor of Formula (I): for the treatment of disease. The compounds disclosed herein are useful for the treatment of a range of cardiovascular, renal and metabolic conditions.

Substituted pyrazolo[1,5-a]pyrimidines as apelin receptor agonists

The present invention relates to a compound or a pharmacologically acceptable salt thereof having excellent tissue non-specific alkaline phosphatase inhibitory activity. The present invention provides a compound represented by the following formula (I): wherein Xrepresents a nitrogen atom or CR, Rrepresents a hydrogen atom, a C-Calkyl group, or a C-Calkoxy group, Rrepresents a halogen atom, Rrepresents a hydrogen atom or a halogen atom, Rrepresents a hydrogen atom or a halogen atom, and Rrepresents a C-Calkylsulfonyl group, a substituted C-Calkyl group, a substituted C-Chaloalkyl group, a substituted C-Calkoxy group, or a substituted C-Calkylamino group, or a pharmacologically acceptable salt thereof.

Biaryl derivative

The present invention relates to a novel fused ring compound having urea structure that exhibits excellent NAMPT activating effect, and a method using the same for treating/preventing metabolic disorder, cardiovascular and kidney disease, mitochondrial disease, neurodegenerative disease, ocular disease, and muscle wasting disorder. The present invention provides a compound represented by following formula (I) or a pharmacologically acceptable salt: Formula (I) wherein A, B, R, Rand Rrepresent the same meanings as in the claims.

Provided herein are small molecule activators of Nicotinamide Phosphoribosyltransferase (NAMPT), compositions comprising the compounds, and methods of using the compounds and compositions.

Small molecule activators of nicotinamide phosphoribosyltransferase (NAMPT) and uses thereof

Protein tyrosine phosphatases (PTPs) are key regulators of metabolism and insulin signaling. As a negative regulator of insulin signaling, the low molecular weight protein tyrosine phosphatase (LMPTP) is a target for insulin resistance and related conditions. Described herein are compounds capable of modulating the level of activity of low molecular weight protein tyrosine phosphatase (LMPTP) and compositions, and methods of using these compounds and compositions.

Inhibitors of low molecular weight protein tyrosine phosphatase (LMPTP) and uses thereof

Provided herein are compounds and methods for the treatment of cancer. The methods include administering to a subject in need a therapeutically effective amount of a Chk1 inhibitor disclosed herein.

Checkpoint kinase 1 (CHK1) inhibitors and uses thereof

Provided herein are small molecule neurotensin receptor agonists, compositions comprising the compounds, and methods of using the compounds and compositions comprising the compounds.

Small molecule agonists of neurotensin receptor 1

Growing community of inventors

La Jolla, CA, United States of America

Anthony B Pinkerton