Small Molecule Compound to Treat Neurological Diseases
Application
NMDAR agents for the treatment of various neurological diseases.
Key Benefits
Exemplary compound EU1180-490 is a potent and selective potentiator of GluN1/GluN3 NMDARs.
The compound has excellent Lipinski drug-like properties including low molecular weight and cLogP, as well as water solubility.
The initial studies have determined...
Published: 9/5/2023
Contributor(s): Dennis Liotta, Stephen Traynelis, Hongjie Yuan, Matthew Epplin, Samantha Summer, David Menaldino, Leon Jacobs, Adam McCallum
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Subunit-Selective NMDAR Antagonists for Treatment of Neurological Disorders
Application
GluN2C/2D selective inhibitors that modulate N-methyl-D-aspartic acid receptors (NMDAR) in a subunit-selective manner for treatment of neurological disorders.
Key Benefits
Specifically targets NMDARs that contain the GluN2C/2D subunit.
Higher potency and efficacy compared to previously reported GluN2C/2D-selective modulators.
Market...
Published: 3/1/2024
Contributor(s): Yao Jing, Stephen Traynelis, Dennis Liotta
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Subunit-Selective Modulator for Treatment of Neurological Disorders
Application
Subunit-selective GluN2C and GluN2D positive allosteric modulators of N-methyl-D-aspartic acid receptors (NMDAR) for treatment of neurological disorders.
Key Benefits
Specifically targets GluN2C/D subunits for positive modulation of NMDAR activity.
Higher potency compared to non-selective modulators.
Improved drug-like properties...
Published: 1/10/2024
Contributor(s): Matthew Epplin, David Menaldino, Stephen Traynelis, Dennis Liotta
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PI3Kα Inhibitors for the Treatment of Cancer
Application
Compounds that inhibit the kinase activity of phospoinostidie 3-kinase (PI3Kα) for the treatment of cancer.
Key Benefits
Potential therapeutic targeted to pathway without a clinically approved inhibitor.
Provides a useful pharmacological probe for research purposes.
Market Summary
In order to grow, cancer cells must have the...
Published: 7/28/2023
Contributor(s): Qi Shi, Thomas Kaiser, Dennis Liotta, James Snyder, Zackery Dentmon, John Diraddo
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CXCR4 Antagonists for the Treatment of Cancer
Application
Small molecules containing either the piperidine or piperazine core which act as antagonists to C-X-C chemokine receptor type 4 (CXCR4) and may be orally administered.
Key Benefits
Orally administered CXCR4 antagonists with diverse clinical applications in oncology.
Mobilize white blood cells in mice in a dose-dependent manner.
Cause...
Published: 11/6/2023
Contributor(s): Lawrence (larry) Wilson, Dennis Liotta, John Wiseman, Michael Natchus
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Small Molecule Potentiators for Treatment of Central Nervous System Disorders
Application
Series of compounds for selectively potentiating N-methyl-D-aspartate (NMDA) receptor subunit NR2C for treating central nervous system impairment.
Key Benefits
Selectivity for NR2C may reduce possibility of adverse side effects.
Market Summary
N-methyl-D-aspartate (NMDA) receptors are widely dispersed in the central nervous system...
Published: 7/28/2023
Contributor(s): Stephen Traynelis, Praseeda Mullasseril, Ethel Garnier-Amblard, Dennis Liotta, Sommer Zimmerman
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Small Molecule Potentiators of NMDA Receptors for Treating Neurological Conditions
Application
Multiple series of small molecules that selectivity potentiate NMDA receptors composed of specific subunits including GluN2B, GluN2C, GluN2B/GluN2C/GluN2D, and GluN2C/GluN2D.
Key Benefits
Small molecule potentiators enhance endogenous signals without exogenous activation.
Subunit selectivity allows targeting of specific subtypes of...
Published: 7/28/2023
Contributor(s): Dennis Liotta, Ethel Garnier-Amblard, Gabriela Fernandez-Cuervo, Lanny Liebeskind, Pavan Kumar Reddy Gangireddy, Stephen Traynelis, Katie Strong, Rose Santangelo-Freel
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Multi-Target CCR5/CXCR4 Chemokine Compounds for the Treatment of HIV
Application
Chemical compounds that bind to both CCR5 and CXCR4 chemokine GPCRs as therapeutics to block HIV entry and infection.
Key Benefits
Targets both chemokine receptors used for cell entry by HIV: CCR5 & CXCR4.
Eliminates the requirement of a tropism pre-test used for drug administration of single chemokine agents.
Does not interfere...
Published: 3/11/2024
Contributor(s): Bryan Cox, Lawrence (larry) Wilson, Anthony Prosser, James Snyder, Dennis Liotta
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GluN2C/D-selective Antagonists for Treatment of Neurological Disorders
Application
A new series of compounds for selectively inhibiting N-methyl-D-aspartate (NMDA) receptor subunits for the treatment of Parkinson's disease, schizophrenia, treatment-resistant depression, and ischemia.
Key Benefits
Improved anatomical selectivity in NMDA receptor modulation may result in fewer adverse side effects.
Targeted antagonism...
Published: 11/6/2023
Contributor(s): Timothy Acker, Stephen Traynelis, Dennis Liotta
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CXCR4 Antagonists in Treatment of Cancer
Application
Nonpeptidic molecules that block the chemokine receptor, CXCR4, for treatment of proliferative disorders including inhibition of cancer metastasis.
Key Benefits
Modulate CXCR4 receptor activity by interfering with SDF-1 ligand binding.
Inhibit migration of metastatic cancer cells by blocking chemokine receptor signaling.
Show increased...
Published: 7/28/2023
Contributor(s): Dennis Liotta, James Snyder, Weiqiang Zhan
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