Dart Neuroscience, (cayman) Ltd.

Akarna Therapeutics, Ltd.

Dart Neuroscience, LLC

Exelixis Patent Company LLC

Recurium IP Holdings, LLC

Pratt, Benjamin Anthony

Benjamin Pratt

Raju Mohan

Lino J Valdez

Alan P Kaplan

Dipanjan Sengupta

Varsha Gupta

Jillian Basinger

Vincent Santora

Graeme Freestone

Brant Clayton Boren

Michael M Morrissey

Chi Ching Mak

Venkataiah Bollu

Brenton Todd Flatt

Brett C Bookser

Andrew Richard Hudson

Jackaline Dalgard Julien

Joe Anh Tran

Marco Peters

Pablo Garcia-Reynaga

Nadia Haq

Sarah Hudson

Chi-Ching Mak

Aaron Thompson

Scott Burley

Jillian Basinger Thompson

Richard Martin

Kevin Duane Bunker

Peter Qinhua Huang

Tie-Lin Wang

Sunny Abraham

Xiao-Hui Gu

Aditya Krishnan Unni

Sobhana Babu Boga

Lino Valdez

Thompson Jillian Basinger

Joe Tran

Disclosed herein are methods for preparing tertiary alcohols from an optionally substituted phenyl ketone or an optionally substituted pyridinyl ketone that includes the use of a chiral ligand and boron trifluoride diethyl etherate. Tertiary alcohols can be used to prepare synthetic versions of natural products and/or pharmaceuticals.

Chiral synthesis of a tertiary alcohol

Substituted cyclohexyl chemical entities of Formula (I):

Substituted cyclohexyl compounds as NOP inhibitors

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

Described herein are fused bicyclic compounds, compositions, and methods for their use for the treatment of disease.

Fused bicyclic compounds for the treatment of disease

A compound having the Formula (I), or a pharmaceutically acceptable salt or solvate thereof: 

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) 

TGR5 agonists of structural formula VIII(Q), wherein X, R, R, and Rare defined in the specification, pharmaceutically acceptable salts thereof, compositions thereof, and use of the compounds and compositions for treating diseases. The invention also comprises use of the compounds in and for the manufacture of medicaments, particularly for treating diseases. 

TGR5 agonists

The present invention comprises TGR5 agonists of structural formula I, wherein X, R, R, and Rare defined herein, as well as N-oxides of them and pharmaceutically acceptable salts thereof. The invention further comprises composition comprising the compounds, N-oxides, and/or pharmaceutically acceptable salts thereof. The invention also comprises use of the compounds and compositions for treating diseases in which TGR5 is a mediator or is implicated. The invention also comprises use of the compounds in and for the manufacture of medicaments, particularly for treating diseases in which TGR5 is a mediator or is implicated.

Triazole and imidazole derivatives for use as TGR5 agonists in the treatment of diabetes and obesity

Growing community of inventors

Encinitas, CA, United States of America

Benjamin Pratt