Dart Neuroscience, LLC

Other

Boehringer Ingelheim International Gmbh

Neurocrine Biosciences, Inc.

Senhwa Biosciences, Inc.

Vertex Pharmaceuticals, Inc.

Cylene Pharmaceuticals, Inc.

Joe Anh Tran

Brett C Bookser

Nicholas Brian Raffaele

Mustapha Haddach

Brian Dyck

Joe H Satcher, Jr

Chen Chen

Stephen M Lane

Fabrice Pierre

Aaron Craig Burns

Andrew Richard Hudson

Lino J Valdez

Benjamin Pratt

Suchitra Ravula

Michael I Weinhouse

David M Ryckman

Marco Peters

Pablo Garcia-Reynaga

Iriny Botrous

Christopher B Darrow

DeMichael Chung

Margaret McCarrick

Douglas R Cary

Dange Vijay Kumar

Aaron Thompson

Collin F Regan

Andrew Kleinke

Jillian Basinger Thompson

Scott Burley

Mark Thomas Miller

Jinglan Zhou

Sara Sabina Hadida Ruah

Jason McCartney

Peter Diederik Jan Grootenhuis

Haripada Khatuya

Timothy Richard Coon

Junko Tamiya

Neil Ashweek

Jeremy J Clemens

Troy Vickers

Nicole Harriott

Fabrice Jean Denis Pierre

Alexander Russell Abela

Florence Jovic

Yoshihiro Ishihara

Substituted furanopyrimidine chemical entities of Formula (I): wherein Rhas any of the values described herein, and compositions comprising such chemical entities; methods of making them; and their use in a wide range of methods, including metabolic and reaction kinetic studies; detection and imaging techniques; radioactive therapies; modulating and treating disorders mediated by PDE1 activity or dopaminergic signaling; treating neurological disorders, CNS disorders, dementia, neurodegenerative diseases, and trauma-dependent losses of function; treating stroke, including cognitive and motor deficits during stroke rehabilitation; facilitating neuroprotection and neurorecovery; enhancing the efficiency of cognitive and motor training, including animal skill training protocols; and treating peripheral disorders, including cardiovascular, renal, hematological, gastroenterological, liver, cancer, fertility, and metabolic disorders.

Substituted furanopyrimidine compounds as PDE1 inhibitors

Substituted cyclohexyl chemical entities of Formula (I):

Substituted cyclohexyl compounds as NOP inhibitors

Substituted furanopyrimidine chemical entities of Formula (I): wherein Rhas any of the values described herein, and compositions comprising such chemical entities; methods of making them; and their use in a wide range of methods, including metabolic and reaction kinetic studies; detection and imaging techniques; radioactive therapies; modulating and treating disorders mediated by PDE1 activity or dopaminergic signaling; treating neurological disorders, CNS disorders, dementia, neurodegenerative diseases, and trauma-dependent losses of function; treating stroke, including cognitive and motor deficits during stroke rehabilitation; facilitating neuroprotection and neurorecovery; enhancing the efficiency of cognitive and motor training, including animal skill training protocols; and treating peripheral disorders, including cardiovascular, renal, hematological, gastroenterological, liver, cancer, fertility, and metabolic disorders. 

This disclosure provides modulators of Cystic Fibrosis Transmembrane Conductance Regulator (CFTR), pharmaceutical compositions containing at least one such modulator, methods of treatment of cystic fibrosis by administering such modulators and pharmaceutical compositions, and processes for making such modulators.

Modulators of cystic fibrosis transmembrane conductance regulator, pharmaceutical compositions, methods of treatment, and process for making the modulator

Substituted cyclohexyl chemical entities of Formula (I): wherein R, G, and Rhave any of the values described herein, and compositions comprising such chemical entities; methods of making them; and their use in a wide range of methods, including metabolic and reaction kinetic studies; detection and imaging techniques; radioactive therapies; modulating and treating disorders mediated by nociceptin activity or dopamine signaling; treating neurological disorders, neurodegenerative diseases, depression, and schizophrenia; enhancing the efficiency of cognitive and motor training; and treating peripheral disorders, including renal, respiratory, gastrointestinal, liver, genitourinary, metabolic, and inflammatory disorders. 

Substituted cyclohexyl compounds as NOP inhibiiors

The invention provides compounds that inhibit protein kinase CK2 activity (CK2 activity), and compositions containing such compounds. These compounds and compositions are useful for treating proliferative disorders such as cancer, as well as other kinase-associated conditions including inflammation, pain, and certain immunological disorders, and have the following general formula: 

Pyrazolopyrimidines and related heterocycles as CK2 inhibitors

New compounds are disclosed which have utility in the treatment of a variety of metabolic related conditions in a patient. The compounds of this invention have the structure (I): wherein X, X, X, X, Y, Y, A, R, R, R, R, m, n, p, and q are as defined herein, including stereoisomers, esters, and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof in a patient in need thereof.

Compounds, pharmaceutical composition and methods relating thereto

The invention provides compounds of general formula (I) that inhibit selected kinases (Pim and/or CK2 kinases) and compositions containing such compounds. These compounds and compositions are useful for treating proliferative disorders such as cancer, as well as other kinase-associated conditions including inflammation, pain, and certain infections and immunological disorders. 

Pyrazolopyrimidines and related heterocycles as kinase inhibitors

New compounds are disclosed which have utility in the treatment of a variety of metabolic related conditions in a patient. The compounds of this invention have the structure (I): wherein R, R, R, n, p, q, and Ar are as defined herein, including stereoisomers, and pharmaceutically acceptable salts thereof. Also disclosed are pharmaceutical compositions comprising a compound of this invention, as well as methods relating to the use thereof in a patient in need thereof.

An analyte sensing fluorescent molecule that employs intramolecular electron transfer is designed to exhibit selected fluorescent properties in the presence of analytes such as saccharides. The selected fluorescent properties include excitation wavelength, emission wavelength, fluorescence lifetime, quantum yield, photostability, solubility, and temperature or pH sensitivity. The compound comprises an aryl or a substituted phenyl boronic acid that acts as a substrate recognition component, a fluorescence switch component, and a fluorophore. The fluorophore and switch component are selected such that the value of the free energy for electron transfer is less than about 3.0 kcal mol . Fluorescent compounds are described that are excited at wavelengths greater than 400 nm and emit at wavelengths greater than 450 nm, which is advantageous for optical transmission through skin. The fluorophore is typically selected from transition metal-ligand complexes and thiazine, oxazine, oxazone, or oxazine-one as well as anthracene compounds. The fluorescent compound can be immobilized in a glucose permeable biocompatible polymer matrix that is implantable below the skin.

Glucose sensing molecules having selected fluorescent properties

The present invention provides formulae for fluorescent compounds that have a number of properties which make them uniquely suited for use in sensors of analytes such as saccharides. The advantageous fluorescent properties include favorable excitation wavelengths, emission wavelengths, fluorescence lifetimes, and photostability. Additional advantageous properties include enhanced aqueous solubility, as well as temperature and pH sensitivity. The compound comprises an aryl or a substituted phenyl botonic acid that acts as a substrate recognition component, a fluorescence switch component, and a fluorophore. Fluorescent compounds are described that are excited at wavelengths greater than 400 nm and emit at wavelengths greater than 450 nm, which is advantageous for optical transmission through skin. The fluorophore is typically selected from transition metal-ligand complexes and thiazine, oxazine, oxazone, or oxazine-one as well as anthracene compounds. The fluorescent compound can be immobilized in a glucose permeable biocompatible polymer matrix that is implantable below the skin.

Saccharide sensing molecules having enhanced fluorescent properties

Growing community of inventors

San Marcos, CA, United States of America

Joe Anh Tran