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Quinazolin-4(3H)-one Derivatives as NOX-2 Inhibitors: Composition of Matter, Methods of Preparation and Their Use
Application
Quinazolin-4(3H)-one derivatives as selective NOX-2 inhibitors to prevent oxidative damage.
Key Benefits
Small molecule NOX-2 specific inhibitor.
Prevents excessive reactive oxygen species (ROS) generation rather than removing them.
Selective NOX-2 inhibition offers significant advantages to development of an effective therapy against...
Published: 7/29/2022
Contributor(s): Thota Ganesh, Radhika Amaradhi, Jacek Zielonka
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Discovery of A Dual Inhibitor of NQO1 and GSTP1 for Treating Malignant Glioblastoma
Application
A small molecule compound to treat Malignant Glioblastoma multiforme.
Key Benefits
Dual inhibition of NQO1 and GSTP1 induces cell death in glioblastoma cells.
Inhibition of NQO1 and GSTP1 by MNPC suppresses tumor growth and elongates the life span of the animals with GBM.
Market Summary
Approximately 30% of patients diagnosed...
Published: 7/29/2022
Contributor(s): Keqiang Ye
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Use of miRNA-483 and its Target Genes in Treatment of Cardiovascular and Inflammatory Diseases
Application
Therapeutic use of miR-483 mimic for treating aortic valve clarification.
Key Benefits
MiR-483 or mimics of miR-483 could be used as a therapeutic.
Could also be a target for additional drug development toward a non-invasive therapy for aortic valve calcification.
Market Summary
Aortic stenosis (AS) is the most common type...
Published: 7/6/2022
Contributor(s): Hanjoong Jo, Joan Fernandez Esmerats, Nicolas (Nico) Villa-Roel
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Use of MAST1 Inhibitor in Treatment of Platinum-Based Chemotherapy
Application
A combination therapy product for treatment of patients having cisplatin-resistant cancer.
Key Benefits
Identified the use of MAST1 inhibitors (such as lestaurtinib) to target cisplatin-resistant cancer.
Lestaurtinib sensitized cells to cisplatin treatment the most using a concentration that attenuates cell viability by less...
Published: 7/6/2022
Contributor(s): Sumin Kang, Jing Chen, Lingtao Jin
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Novel Piperidine-Amide Derivatives as CXCR4 Modulators
Application
A new class of CXCR4 modulators for metastasis and inflammation.
Key Benefits
Selective for only one allosteric site on CXCR4.
Lower adverse effects.
Market Summary
Activation of the CXCR4 receptor triggers multiple signaling pathways that orchestrate cell migration, hematopoiesis and cell homing, and retention in the bone...
Published: 5/17/2022
Contributor(s): Hyunsuk Shim, Yoon-Hyeun Oum
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Targeting SREBP1 for Managing Acquired Resistance to Osimertinib/AZD9291 and Other EGFR Inhibitors for Non-small Cell Lung Cancer Treatment
Application
Small molecule combination therapy (adjuvant, sensitizing agent) for Osimertinib (to treat non-small cell lung cancer with common EGFR activating mutations and T790M resistant mutation).
Key Benefits
Therapy against EGFR-TKI resistant tumors with mutant EGFR (e.g., T790M).
Potential to reduce toxicity of EGFR medicines by requiring...
Published: 5/13/2022
Contributor(s): Shi-Yong Sun, Zhen Chen
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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: 5/13/2022
Contributor(s): Dennis Liotta, Stephen Traynelis, Hongjie Yuan, Matthew Epplin, Samantha Summer, David Menaldino, Leon Jacobs, Adam McCallum
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Small Molecules as Disinfectants and Antiseptics
Application
Anti-microbial molecules with broad spectrum activities.
Key Benefits
Effective antimicrobial scaffolds with improved broad-spectrum activities compares to current commercial disinfectants.
Market Summary
There is an increased effort in developing new antibiotics, antiseptics, and disinfectants to overcome the current resistance...
Published: 3/16/2022
Contributor(s): William (Bill) Wuest, Kevin Minbiole
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IACS-0107059 for Sensitizing Resistant Multiple Myeloma (MM) for Venetoclax Therapy
Application
Combinatorial drug therapy for resistant multiple myeloma.
Key Benefits
Clinically approved drugs to repurpose for multiple myeloma.
Therapies for multiple myeloma that is resistant to other therapies.
Market Summary
Multiple myeloma (MM) is a plasma cell malignancy. Despite the use of next generation immunomodulatory drugs...
Published: 3/16/2022
Contributor(s): Malathy (mala) Shanmugam, Aditi Sharma
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Small Molecule TrkB Agonist to Prevent Blindness from Eye Injuries
Application
Small molecule HIOC derivatives as a therapeutic for preventing vision loss in traumatic eye injuries.
Key Benefits
Reduces blindness in a model of traumatic optical injury.
May be administered systemically and penetrates tissues in and adjacent to the brain.
This treatment method has potential for indications outside of retinal injury.
Market...
Published: 5/5/2021
Contributor(s): Paul Iuvone, Frank Mcdonald, Christopher Walker
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