Search Results - kenneth+jacobson

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Selective A3 Adenosine Receptor Agonists for the Treatment of Chronic Neuropathic Pain and Other Conditions

This technology includes the creation and use of A3 adenosine receptor (A3AR)-selective agonists for treating chemotherapy-induced peripheral neuropathy, chronic neuropathic pain, rheumatoid arthritis, psoriasis, and other conditions. A3 receptors for adenosine are found in most cells and endogenous activation of the A3 receptors can result in apoptosis,...

Published: 8/12/2024 | Inventor(s): Daniela Salvemini, Dilip Tosh, Kenneth Jacobson

Keywords(s):

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

A3 Adenosine Receptor Positive Allosteric Modulators

Selective A3AR agonists are sought as potential agents for treating inflammatory diseases, chronic pain, cancer and non-alcoholic steatohepatitis (NASH). NIDDK investigators have invented new chemical composition as positive allosteric modulators (PAMs) of the A3AR. These chemical compounds contain sterically constrained, bridged modifications and...

Published: 4/8/2024 | Inventor(s): Kenneth Jacobson, Lucas Fallot, Rama Ravi, Balaram Pradhan, John Auchampach, Courtney Fisher

Keywords(s):

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

New Heterocyclic Scaffold-Based Inhibitors of the Polo-Box Domain of Polo-like Kinase 1 for the Treatment of Cancer

Abstract: Polo-like kinase 1 (Plk1), a member of the Polo-like kinase family, plays a critical role in regulating mitosis and cell cycle progression. Aberrant expression of Plk1 has been observed in a variety of human cancers, and it is known to be associated with tumorigenesis as well as poor prognosis in cancer patients. Unlike normal cells, some...

Published: 4/8/2024 | Inventor(s): Kyung Lee, Kenneth Jacobson, Celeste Alverez, Jung-Eun Park

Keywords(s): CANCER, cell cycle, Heterocyclic Scaffold, Lee, mitosis, Oncology, PBD, plk1, Polo-Box Domain, Polo-Like Kinase 1, PRODRUGS, Triazoloquinazolinone

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

Potent Nucleotide Inhibitors of Ecto-5'-Nucleotidase (CD73)

These small molecules are novel nucleotide derivatives, containing either a purine or pyrimidine nucleobase, that competitively block the enzyme CD73, also known as ecto-5'-nucleotidase. This enzyme converts extracellular AMP (not a potent activator of adenosine receptors) to adenosine (the native activator of 4 subtypes of adenosine receptors. CD73...

Published: 7/25/2024 | Inventor(s): Christa Mueller, Anna Junker, Kenneth Jacobson

Keywords(s): CB5EXX, CD73, Ecto-5-nucleotidase, Inhibitors, Nucleotide, POTENT

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

Small Molecule MRS5474 with Anticonvulsant Activity for Treatment of Epilepsy

Adenosine modulates many physiological processes by activating specific adenosine receptors. These adenosine receptors play a critical role in the regulation of cellular signaling and are broadly distributed throughout the body. Thus, the ability to modulate adenosine receptor-mediated signaling is an attractive therapeutic strategy for a broad range...

Published: 7/25/2024 | Inventor(s): Dilip Tosh, Kenneth Jacobson

Keywords(s): A3, Activity, ADENOSINE, AGONISTS, Agonists:, Al, ANTAGONISTS, Anticonvulsant, Derivatives, Docking, IB1FXX, IB1XXX, IBXXXX, IXXXXX, NB1EXX, NB1HXX, NB1XXX, NBXXXX, N-Methanocarba, Nucleosides, NXXXXX, PARTIAL, Patent Category - Chemistry, POTENT, RECEPTOR, TRUNCATED

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

A3 Adenosine Receptor Agonists to Treat Chemotherapy-induced Peripheral Neuropathy

This invention claims species-independent agonists of A3AR, specifically (N)-methanocarba adenine nucleosides and related pharmaceutical compositions. The A3 adenosine receptor (A3AR) subtype has been linked with helping protect the heart from ischemia, controlling inflammation, and regulating cell proliferation. Agonists of the human A3AR subtype...

Published: 4/8/2024 | Inventor(s): Dilip Tosh, Kenneth Jacobson

Keywords(s): 2-Arylethynyl, A3, ADENOSINE, CB3CXX, CB3XXX, CBXXXX, CXXXXX, Design, N-Methanocarba, Nucleosides, Receptor-Selective, Structure-based

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

Antagonist of A3 Adenosine Receptor Fluorescent Probes for the Study of Diseases that Involve A3 Signaling

This molecular probe may serve as a companion tool to identify and stratify patient populations based on the prevalence of the target A3 adenosine receptors. Small molecule drugs, A3AR-selective agonists, are currently in advanced clinical trials for the treatment of hepatocellular carcinoma, autoimmune inflammatory diseases, such as rheumatoid arthritis,...

Published: 7/25/2024 | Inventor(s): Kenneth Jacobson

Keywords(s): A3, ADENOSINE, ANTAGONISTS, BINDING, CA1CXX, CA1XXX, CAXXXX, CXXXXX, fluorescent, IA2XXX, IA3XXX, IAXXXX, IXXXXX, Molecular, Novel, Probes, RECEPTOR

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

Triazole Derivatives of 4,7-disubstituted 2 naphthoic acid (PPTN) as P2Y14 Receptor Antagonists

The Molecular Recognition Section of NIDDK announces the availability of a novel triazole-based probes, structures which act as antagonists at human P2Y14 receptors. Although the physiologic functions of this receptor remain undefined, recently it has been strongly implicated in immune and inflammatory responses. Prior work with a 4,7-disubstituted...

Published: 7/25/2024 | Inventor(s): Evgeny Kiselev, Elisa Uliassi, Anna Junker, Kenneth Jacobson

Keywords(s): Alkyne, ANTAGONISTS, IB3XXX, IB4XXX, ID1XXX, P2Y14, Patent Category - Chemistry, Probe, RECEPTOR, small molecule, Structure-based, Triazole, VFXXXX, WIXXXX, WKXXXX, XHXXXX, YBXXXX

Category(s): Collaboration Sought > Collaboration, Application > Therapeutics, TherapeuticArea > Endocrinology, ResearchProducts > Research Equipment, TherapeuticArea > Immunology, TherapeuticArea > Pulmonology, Application > Research Materials

N-Methanocarba Adenosine Derivatives and Their Dendrimer Conjugates as A3 Receptor Agonists

This technology relates to specific (N)-methanocarba adenine nucleosides that have been developed and dendrimers that connect these compounds to create molecules with multiple targets. Dendrimers are essentially repeated molecular branches presenting the core receptor-binding molecules. The compounds synthesized function as agonists and antagonists...

Published: 7/25/2024 | Inventor(s): Dilip Tosh, Kenneth Jacobson

Keywords(s): A3, ADENOSINE, AGONISTS, CONJUGATES, DENDRIMER, Derivatives, IAXXXX, IBXXXX, IXXXXX, N-Methanocarba, OBXXXX, OXXXXX, Patent Category - Chemistry, RECEPTOR, Their

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

Truncated Methanocarba Adenosine Derivatives as A3 Adenosine Receptor Antagonists

Novel A3 adenosine antagonists available for licensing. A3 receptors are particularly highly expressed in inflammatory cells, making it a potentially desirable target for inflammatory diseases. This technology relates to highly specific antagonists and partial agonists of A3 adenosine receptors, which are negatively coupled to adenylate cyclase and...

Published: 9/3/2024 | Inventor(s): Kenneth Jacobson

Keywords(s): A3, ADENOSINE, ANTAGONISTS, Derivatives, IB3XXX, IBXXXX, IXXXXX, N-Methanocarba, Patent Category - Chemistry, RECEPTOR, TRUNCATED

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

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