Dart Neuroscience, (cayman) Ltd.

Dart Neuroscience, LLC

Corvas International, Inc.

Dendreon Corporation

Michael I Weinhouse

Brian Dyck

Laurent Gomez

James Breitenbucher

Bryan James Branstetter

Troy Vickers

Marco Peters

Tami Jo Marrone

Andrew Richard Hudson

Alan P Kaplan

Mark E Wilson

Andrew Lindstrom

Mi Chen

William Charles Ripka

Terence P Keenan

Brett C Bookser

Aaron Craig Burns

Nicholas Brian Raffaele

Joe Anh Tran

Iriny Botrous

DeMichael Chung

Margaret McCarrick

Dange Vijay Kumar

Andrew Kleinke

Edwin L Madison

Joseph Edward Semple

Odile Esther Levy

Venkataiah Bollu

Robert Huerta Lemus

James Zapf

Amy Lynn Allan

Andrew K Lindstrom

Daniel Vanna Siev

Amir P Tamiz

J Edward Semple

Bryan Branstetter

Tammi Jo Marrone

Amy Allan

Robert Lemus

Alan Kaplan

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 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. 

The invention provides a chemical entity of Formula (I), 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, and radioactive treatments; and therapies, including inhibiting PDE4, enhancing neuronal plasticity, treating neurological disorders, providing neuroprotection, treating a cognitive impairment associated with a CNS disorder, enhancing the efficiency of cognitive and motor training, providing neurorecovery and neurorehabilitation, enhancing the efficiency of non-human animal training protocols, and treating peripheral disorders, including inflammatory and renal disorders.

Substituted pyridine and pyrazine compounds as PDE4 inhibitors

Described herein are compounds of Formula I and Formula II, methods of their synthesis, compositions comprising the compounds, and use of the compounds and compositions in treating numerous diseases and disorders, including cognitive deficits associated with CNS diseases and disorders.

Therapeutic thiophene-, furan-, and pyridine-fused azolopyrimidin-5-(6H)-ones

Therapeutic thiophene-, furan-, and pyridine-fused azolopyrimidin-5-(6h)-ones

The invention includes a compound of formula I: wherein R, Y, A, n, Rand Z have any of the values described herein, as well as salts of such compounds, compositions comprising such compounds, and therapeutic methods that comprise the administration of such compounds. The compounds are inhibitors of PDE4 function and are useful for improving cognitive function and/or treating cognitive disorders or impairment, traumatic and/or ischemic injuries of the central and peripheral nervous system and/or psychiatric disorders in animals, especially humans.

Therapeutic piperazines

Described herein are compounds and chemical entities of Formula (I), methods of their synthesis, compositions comprising them, and their use in treating numerous diseases and disorders, including cognitive deficits associated with CNS diseases and disorders. 

Substituted pyrido[3,2-e][1,2,4]triazolo[1,5-c]pyrimidines, pyrido[2,3-e][1,2,4]triazolo[1,5-c]pyrimidines and/or [1,2,4]triazolo[1,5-c]pteridines for treatment of central nervous system diseases and disorders

This invention provides a method for producing a derivatized resin useful in the arts of solid-phase peptide synthesis, combinatorial chemistry, and peptide or protein purification and separation. Methods for synthesizing the derivatized resin, the prototypical example of which is hydrazyl-carbonyl-amino methylated polystyrene, are provided by this invention disclosure.

Resin derivatization method and uses thereof

Novel compounds having activity as non-covalent inhibitors of urokinase and having activity in reducing or inhibiting blood vessel formation are provided. These compounds have P1 a group having an amidino or guanidino moiety or derivative thereof. These compounds are useful in vitro for monitoring plasminogen activator levels and in vivo in treatment of conditions which are ameliorated by inhibition of or decreased activity of urokinase and in treating pathologic conditions wherein blood vessel formation is related to a pathologic condition.

Non-covalent inhibitors of urokinase and blood vessel formation

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San Diego, CA, United States of America

Michael I Weinhouse