Dart Neuroscience, (cayman) Ltd.

Helicon Therapeutics, Inc.

Dart Neuroscience, LLC

Varsha Gupta

Alan P Kaplan

Jillian Basinger

Graeme Freestone

Vincent Santora

Dipanjan Sengupta

Lino J Valdez

Benjamin Pratt

Jan W F Wasley

Chi Ching Mak

Joel Renick

Chi-Ching Mak

Mi Chen

Brett C Bookser

Andrew Richard Hudson

DeMichael Chung

James Na

Jan Wf Wasley

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 provides a chemical entity of Formula (I) 

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

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 modulating GABA, and use of the compound of formula I for the treatment of GABAreceptor associated disorders. The general structure of formula I is shown below and can exist in tautomeric forms:  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 pyrazoloquinoline derivatives

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 for the treatment of GABAreceptor associated disorders. The general structure of formula I is shown below: 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 pyrazolonaphthyridine derivatives

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 modulating GABA, and use of the compound of formula I for the treatment of GABAreceptor associated disorders. The general structure of formula I is shown below:  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).

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Encinitas, CA, United States of America

Varsha Gupta