Search Results - inhibitors

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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: 7/25/2024 | 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

Development and Use of O-linked beta-N-acetylglucosamine (O-GlcNAc) Transferase (OGT) Inhibitors for Multiple Conditions, Including Cancer

This technology includes the development and use of small molecules that inhibit O-linked beta-N-acetylglucosamine (O-GlcNAc) transferase (OGT) for a variety of pathologies, including Alzheimer's disease, cancer, cancer, diabetes, and neurodegenerative disorders the treatment of cancer and as a potential antiviral. OGT is a ubiquitous enzyme that catalyzes...

Published: 7/25/2024 | Inventor(s): Sara Martin Schwanger, Craig Thomas, Damien Duveau, Suzanne Walker

Keywords(s): 0-GlcNAc, Development, Developmtent, Inhibitors, OGT, THEREOF, TRANSFERASE, USES, VEXXXX, WIXXXX, WKXXXX

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

Repurposing CDK Inhibitors for the Treatment of Zika Virus Infection

This invention includes the discovery and use of a group of CDK inhibitors that were found during a drug repurposing screen designed to find compounds that inhibit Zika virus caused cell death. The identified CDK inhibitors have all previously been used in clinical trials for other diseases, potentially reducing the long time course needed for new drug...

Published: 7/25/2024 | Inventor(s): Ruili Huang, Miao Xu, Wenwei Huang, Hengli Tang, Emily Lee, Cheng YiChen, Yi Zhou, Hongjun Song, Guo-Li Ming, Zhexing Wen, Wei Zheng

Keywords(s): CDK, Infection, Inhibitors, Repurposing, treatment, VEXXXX, virus, VLXXXX, WIXXXX, WKXXXX, Zika

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

Novel ACRV1/ALK2 Inhibitors and Methods for Inhibiting BMP Signaling for the Treatment of Fibrodysplasia Ossificans Progressiva (FOP)

This technology includes the identification and use of novel ACRV1/ALK2 inhibitors for the treatment of fibrodysplasia ossificans progressiva (FOP), an autosomal-dominant rare disease that affects one person in every 1-2 million. FOP is characterized by malformation of the great (big) toes during embryonic development and by progressive heterotopic...

Published: 7/25/2024 | Inventor(s): Jian-kang Jiang, Khalida Shamim, Philip Sanderson, Wei Zheng, Xiuli Huang, Gregory Tawa, Asaf Alimardanov, Arthur Lee, Junfeng Huang, Wenwei Huang

Keywords(s): ALK2, BMP, INHIBITING, Inhibitors, Methods, Novel, SIGNALING, VGXXXX, WIXXXX, WKXXXX, XEXXXX

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

Creation of a High-density Screening Format and the Identification of Small Molecule Inhibitors of the SIX/EYA Interaction for the Treatment of Cancers

The technology includes the creation of a high-throughput assay and the identification and use of small molecules that inhibit the SIX/EYA interaction as a treatment for cancer. The Eya proteins are phosphatases that form a complex and are activated by the Six family of homeobox transcription factors. The interaction of Eya and Six mediates breast cancer...

Published: 7/25/2024 | Inventor(s): Marc Ferrer-Alegre, Xin Hu, Juan Marugan, Lesley Mathews, Heide Ford, Melanie Blevins, Rebecca Mull, Rui Zhao

Keywords(s): cancers, Identification, Identifying, Inhibitors, INTERACTION, Listed LPM Vathyam as of 4/15/2015, Method, MOLECULE, Post LPM Assignment Set 20150420, Pre LPM working set 20150418, SIX/EYA, Small, treatment, VCXXXX, WIXXXX, WKXXXX, XEXXXX

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

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: 7/25/2024 | 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

Treatment of Acute Myeloid Leukemia (AML) with the Multi-kinase FLT3-IRAK1/4 Inhibitor, NCGC1481, to Avoid Adaptive Resistance

This technology includes the identification and use of a novel small molecule, NCGC1481, to inhibit both the FLT3 and IRAK1/4 kinase pathways for treating acute myeloid leukemia (AML). An activating mutation of the FMS-like receptor kinase 3 (FMT3) occurs in approximately 25% of AML cases. Consequently, FLT3 inhibitors (FLT3i) have a good initial clinical...

Published: 7/25/2024 | Inventor(s): Jian-kang Jiang, Craig Thomas

Keywords(s): FTL3/IRAK, Inhibitors, MOLECULE, Small, VCXXXX, WIXXXX, WKXXXX, XEXXXX

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

Treatment of primary hyperoxalurias with small molecule lactate dehydrogenase inhibitors such as WO2018005807A1

This technology includes the use of novel lactate dehydrogenase (LDH) inhibitors, including WO2018005807A1, for the treatment of primary hyperoxalurias (PHs). PHs are rare autosomal recessive disorders caused by overproduction of oxalate, leading to recurrent calcium oxalate kidney stone disease, and in some cases end-stage renal disease. One potential...

Published: 7/25/2024 | Inventor(s): Daniel Urban, Leonard Neckers, Ross Holmes, David Wood, Matthew Hall

Keywords(s): DEHYDROGENASE, Hyperoxalurias, Inhibitors, LACTATE, MOLECULE, Primary, Small, TREATING, VPXXXX, WIXXXX, WKXXXX, XEXXXX

Category(s): TherapeuticArea > Cardiology, TherapeuticArea > Oncology, TherapeuticArea > Infectious Disease, Application > Therapeutics, TherapeuticArea > Ophthalmology, TherapeuticArea > Endocrinology, TherapeuticArea > Dental, Application > Research Materials

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: 7/25/2024 | 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: 7/25/2024 | 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

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