Search Results - ajit+jadhav

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Creation and Use of 12-LO inhibitors (4-((2-hydroxy-3-methoxybenzyl)amino)benzenesulfonamide derivatives) for the Treatment of Diabetes and Large Platelet-Derived Clots

This technology includes the discovery and use of novel selective 12-LO (lipoxygenase) inhibitors, 4-((2-hydroxy-3-methoxybenzyl)amino)benzenesulfonamide derivatives, for attenuating large clots and for the treatment of Type 1/2 diabetes. A 12-LO inhibitor could be a potent intracellular approach to block platelets from forming large clots in response...

Published: 10/28/2024 | Inventor(s): Ajit Jadhav, Anton Simeonov, Adam Yasgar, Diane Luci, Michael Holinstat, Theodore Holman, Jerry Nadler, David Taylor-Fishwick, David Maloney

Keywords(s): 12-Lipoxygenase., 4-2-hydroxy-3-methoxybenzylaminobenzenesulfon, Derivatives, Discovery, Human, Inhibitors, Listed LPM Nguyen-Antczak as of 4/15/2015, Post LPM Assignment Set 20150420, POTENT, Pre LPM working set 20150418, SELECTIVE, VDXXXX, VFXXXX, WKXXXX, XEXXXX

Category(s): TherapeuticArea > Cardiology, TherapeuticArea > Endocrinology, Application > Therapeutics

Inhibition of Thioredoxin Reductase 1 (Trxr1) by Pyridine Compounds for Cancer Treatment

This technology includes the use of pyridines for anticancer treatment. A common feature of cancer cells is a high level of reactive oxygen species with a concomitant increase of two antioxidative systems to combat the toxicity: the glutathione and thioredoxin systems. Inhibiting either, or both, of these systems is a promising avenue to target cancer...

Published: 10/28/2024 | Inventor(s): Ajit Jadhav, Diane Luci, Thomas Dexheimer, Anton Simeonov, Nathan Coussens, David Maloney

Keywords(s): CANCER, Novel, PYRIDINES, Their, treatment, VCXXXX, WIXXXX, WKXXXX, XEXXXX

Category(s): Application > Research Materials, TherapeuticArea > Oncology, Application > Therapeutics

Identification and Use of 12/15-Lipoxygenase (LOX) Inhibitors for Post-Strike Treatment

This technology includes the identification and use of 12/15-lipoxygenase (LOX) inhibitors, including ML351 and related analogs, for post-stroke treatment. The 12/15-LOX directly oxidizes lipid membranes leading to their direct attack. After a stroke, the activity of 12/15-LOX is upregulated and is thought to contribute to increased neuronal loss and...

Published: 10/28/2024 | Inventor(s): Theodore Holman, David Maloney, Ganesha Rai Bantukallu, Ajit Jadhav, Anton Simeonov, Klaus Van Leyen

Keywords(s): 12/15-Li, 12/15-Lipoxygenase, Enase, Inhibitors, Ox, VEXXXX, WIXXXX, WKXXXX, XEXXXX

Category(s): Application > Research Materials, TherapeuticArea > Neurology, Application > Therapeutics

Small Molecule Inhibitors of the p53/S100B Interaction for Treating Cancer

This technology includes newly identified best-in-class inhibitors of the p53-S100B interaction that plays a role in malignant melanoma. S100B contributes to cancer cell proliferation (particularly malignant melanoma) by binding to p53 and inhibiting its tumor suppressor function. A high-throughput screen was used to find p53-S100B inhibitors, leading...

Published: 10/28/2024 | Inventor(s): Anton Simeonov, David Maloney, Daniel Jansen, Hongmao Sun, Diane Luci, Ajit Jadhav, Stephen Kales

Keywords(s): Inhibitors, MOLECULE, P53-S100B, Small, VCXXXX, WKXXXX, XEXXXX

Category(s): Application > Therapeutics, TherapeuticArea > Oncology

A Novel Chemical Series for Inhibiting Bromodomain-containing Protein 4 (BRD4) for Treating Cancer

This technology includes the design, synthesis, and use of a novel chemical series for multiple treatments, including for treating cancer. A series of substituted bicyclic heteroaryl small molecules were found to be a potent inhibitor of bromodomain-containing protein 4 (BRD4) for multiple uses, including cancer. A BRD4 inhibitor is in a class of drugs...

Published: 10/28/2024 | Inventor(s): David Maloney, Shyh-Ming Yang, Ajit Jadhav, Daniel Urban, Makoto Yoshioka, Jeffrey Strovel

Keywords(s): BICYCLIC, Brd4, Bromodomain-containing, Heteroaryl, Inhibitors, Protein, Substituted, VCXXXX, WKXXXX, XEXXXX

Category(s): TherapeuticArea > Oncology, Application > Therapeutics

Highly Potent and Selective Deubiquitinating Enzyme Inhibitor

Available for licensing are inhibitors that target the USP1/ UAF1 deubiquitinating enzyme (DUB) complex. The FDA approval and commercial success of Velcade®, a small molecule proteasome inhibitor, has established the ubiquitin-proteasome system (UPS) as a valid target for anticancer treatment. However, proteasome inhibitors in general suffer from...

Published: 10/28/2024 | Inventor(s): Andrew Rosenthal, Ajit Jadhav, Thomas Dexheimer, Anton Simeonov, Qin Liang, Zhihao Zhuang, David Maloney

Keywords(s): CANCER, CANCER THERAPEUTICS, CB5XXX, CB7XXX, CBXXXX, Combination Therapy, CXXXXX, Deubiquitinase, Inhibitors, POTENT, protease inhibitors, SELECTIVE, small molecule, USP1/UAF1

Category(s): Collaboration Sought > Collaboration, Collaboration Sought > Licensing, TherapeuticArea > Oncology, Application > Therapeutics

Selective 12-Human Lipoxygenase Inhibitors for the Treatment of Diabetes and Clotting

This invention discloses small molecule inhibitors of human 12-lipoxygenase (12-hLO). 12-lipoxygenase expression, activation, and lipid metabolites have been implicated in type 1 and type 2 diabetes, cardiovascular disease, hypertension, Alzheimer’s, and Parkinson’s disease. The development of 12-hLO inhibitors may be a potent intracellular approach...

Published: 10/28/2024 | Inventor(s): Jerry Nadler, Michael Holinstat, Anton Simeonov, Ajit Jadhav, Theodore Holman, David Maloney

Keywords(s): 12-human, Cardiovascular, CAUSED, Clot, DIABETES, Discovery, Disease, Formation, IA1AXX, IA1XXX, IAXXXX, Inhibitors, IXXXXX, LIPOXYGENASE, Platelet-mediated, Prevention, SELECTIVE, treatment

Category(s): Collaboration Sought > Licensing, Application > Research Materials, TherapeuticArea > Cardiology, Application > Therapeutics, Application > Diagnostics