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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
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
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
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
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
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
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
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
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
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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