Dart Neuroscience, (cayman) Ltd.

Helicon Therapeutics, Inc.

Dart Neuroscience, LLC

Alan P Kaplan

Terence P Keenan

Varsha Gupta

Andrew J McRiner

Mark E Wilson

Andrew Lindstrom

Jillian Basinger

Vincent Santora

Graeme Freestone

Venkataiah Bollu

James Breitenbucher

Robert Huerta Lemus

Dipanjan Sengupta

Troy Vickers

Lino J Valdez

Benjamin Pratt

James Zapf

Mi Chen

Rusiko Bourtchouladze

Michael I Weinhouse

Roderick E M Scott

Jan W F Wasley

Xianbo Zhou

Chi Ching Mak

William Charles Ripka

Joel Renick

Chi-Ching Mak

Andrew J Mcriner

Brett C Bookser

Andrew Richard Hudson

DeMichael Chung

James Na

Jan Wf Wasley

Terrence P Keenan

Roderick Em Scott

Andrew Mcriner

Lino Valdez

Roderick EM Scott

Andrew Mckriner

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

The invention provides a compound of formula I: wherein A, A, A, R, X, Y, and B 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 monoamine oxidase B (MAO-B) enzyme function and are useful for improving cognitive function and for treating psychiatric disorders in animals.

Therapeutic isoxazole compounds

The invention provides a chemical entity of Formula (I) wherein R, R, R, Y, and n have 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, and radioactive treatments; and therapies, including inhibiting MAO, and MAO-B selectively, 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 obesity, diabetes, and cardiometabolic disorders) and their associated co-morbidities.

Substituted naphthyridine and quinoline compounds as MAO inhibitors

The invention provides a chemical entity of Formula (I), wherein R, R, R, R, Rand X have 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 treatments; modulating and treating disorders mediated by GlyT1 activity; 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; and treating other disorders, including pain and alcohol-dependence. 

Substituted 2,4,5,6-tetrahydropyrrolo[3,4-c]pyrazole and 4,5,6,7-tetrahydro-2H-pyrazolo[4,3-c]pyridine compounds as GlyT1 inhibitors

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

The invention provides a chemical entity of Formula (I) whereinR, R, R, R, Y and Z have 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, 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.

The invention provides a chemical entity of Formula (I) 

The invention provides a chemical entity of Formula (I) wherein R, R, R, R, Y and Z have 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, 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.

The invention provides a novel chemical series of formula I, as well as methods of use thereof for binding to the benzodiazepine site of the GABAreceptor and negatively modulating the &#x3b1;5 subtype of GABA, and use of the compound of formula I in the manufacture of a medicament for the treatment of GABAreceptor associated disorders. The invention further provides a method of modulation of one or more GABAsubtypes in an animal comprising administering to the animal an effective amount of a compound of formula (I).

Therapeutic 5,6,5-tricyclic analogs

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Kings Park, CA, United States of America

Alan P Kaplan