Emory University

Fob Synthesis, Inc.

Neurop, Inc.

David Menaldino

Dennis C Liotta

Stephen F Traynelis

Matthew Epplin

Woo-Baeg Choi

Yesim Altas Tahirovic

Deog-Il Kim

Martin Bouygues

Rose M Freel

Michael W Hager

Kamalesh Poornachary

Katie L Strong

Scott Myers

Lawrence Wilson

Compounds that selectively inhibit GluN2B-containing N-methyl-D-aspartic acid receptors (NM/DARs) are disclosed. In some cases, the compounds selectively target GluN2B over GluN2A, GluN2C, and/or GluN2D. Generally, the compounds possess an enhanced potency to GluN2B at a pH that is more acidic compared to the physiological pH. Pharmaceutical formulations containing one or more of the compounds are also disclosed. Additionally, methods of treating a condition, disorder or disease using the compounds or their pharmaceutical formulations thereof are disclosed. Exemplary conditions, disorders, and diseases relevant to this disclosure include stroke, subarachnoid hemorrhage, cerebral ischemia, cerebral vasospasm, hypoxia, acute CNS injury, spinal cord injury, traumatic brain injury, coronary artery bypass graft, persistent or chronic cough, substance abuse disorder, opiate withdrawal, opiate tolerance, bipolar disorder, suicidal ideation, pain, fibromyalgia, depression, postpartum depression, resting tremor, dementia, epilepsy, seizure disorder, movement disorder, and neurodegenerative disease.

GluN2B-subunit selective antagonists of the N-methyl-D-aspartate receptors with enhanced potency at acidic pH

A series of subunit selective allosteric modulators of NMDA receptor function according to Formula (I) is provided herein. Also provided is a method of treating neurological disorders such as Alzheimer's disease Parkinson's disease, schizophrenia, depression, stroke, psychosis and the like using compounds of Formula (I), optionally in combination with one or more further active agent. Pharmaceutical compositions containing a compound of Formula (I) and optionally one or more active agent for treating such disorders may be provided in the form of a tablet, capsule, pill, gel, granules, aerosol, aqueous buffer or a nanoparticle formulation, emulsion, liposome, etc. (I)

N-methyl-D-aspartic acid receptor modulators

This disclosure relates to tetrahydroisoquinolines, salts, and derivatives useful for managing mental or cognitive diseases or conditions of the brain or central nervous system. In certain embodiments, the disclosure relates to compounds and compositions having formula I: prodrugs, esters, or salts thereof, wherein the substituents are described herein. 

N-methyl-D-aspartate receptor (NMDAR) potentiators, pharmaceutical compositions, and uses related thereto

The present invention provides &#x3b2;-methyl carbapenem compounds and pharmaceutical compositions useful in the treatment of bacterial infections and methods for treating such infections using such compounds and/or compositions, wherein the compounds are generally of the Formulae  The invention includes administering an effective amount of a carbapenem compound or salt and/or prodrug thereof to a host in need of such a treatment. The present invention is also in the field of synthetic organic chemistry and is specifically provides an improved method of synthesis of &#xff;-methyl carbapenems which are useful as antibacterial agents.

Gram-positive carbapenem antibacterials and processes for their preparation

Growing community of inventors

Atlanta, GA, United States of America

David Menaldino