Michigan State University

The University of Texas System

Jetze J Tepe

Satyamaheshwar Peddibhotla

Theresa A Lansdell

Evert Njomen

Corey Lee Jones

Thomas J Pinnavaia

James Marino Hamby

Pawel A Osmulski

Maria Gaczynska

Aaron L Odom

Matt Giletto

Aaron Odom

Peddibhotla Satyamaheshwar

Described herein are quinoline compounds useful for, among other things, inhibition of the proteasome and for treatment of cancer and inflammation.

Quinoline-based proteasome inhibitors and uses thereof

The disclosure is directed to substituted dibenzo[b,f]azepines of the formula (II):

Substituted dibenzo[b, f]azepines as proteasome activators

The disclosure is directed to compounds of the formula (I): and uses of such compounds to treat neurodegenerative diseases and cancers.

Substituted phenothiazines as proteasome activators

The present disclosure relates to chemical compounds that modulate proteasome activity, pharmaceutical compositions containing such compounds, and use of these compounds and compositions for the treatment of disorders of uncontrolled cellular proliferation such as, for example, a cancer. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

Pipecolic esters for inhibition of the proteasome

A new class of imidazolines as 4-position esters with very potent anti-inflammatory as well as antimicrobial activity is described. The synthesis of these imidazolines includes a multicomponent reaction applicable to a combinatorial synthetic approach. The combination of these two key characteristics provides an effective therapeutic drug in the treatment of septic shock as well as many other inflammatory (arthritis and asthma) and infectious disorders. The use of this novel class of non-steroidal agents as anti-inflammatory agents (for the treatment of asthma, etc.), antibacterial agents, and antiseptic agents is described. The compounds are also useful in the treatment of tumors (such as cancers). The imidazolines are potent inhibitors of the transcription factor NF-&#x3ba;B as well as potent activity against the Gram (+) bacterium. The compositions are also useful for treating autoimmune diseases and for inhibiting rejection of organ and tissue transplants.

NF-&#x3ba;B inhibitors and uses thereof

The invention relates to compositions comprising substituted imidazoline compounds including prodrugs, and salts thereof. In some embodiments, the invention relates to the use of these compositions as therapeutic agents, preferably for the treatment of arthritis or cancer. In further embodiments, The invention relates to the pharmaceutical compositions with effective amounts of substituted imidazoline compounds disclosed herein that function as agonist or antagonists of the genetic expression or interactions with transcription factor NF-&#x3ba;B.

Substituted imidazoline compounds

A new class of imidazolines as 4-position acids or esters with very potent anti-inflammatory as well as antimicrobial activity is described. The synthesis of these imidazolines includes a multicomponent reaction applicable to a combinatorial synthetic approach. The combination of these two key characteristics provides an effective therapeutic drug in the treatment of septic shock as well as many other inflammatory (arthritis and asthma) and infectious disorders. The use of this novel class of non-steroidal agents as anti-inflammatory agents (for the treatment of asthma etc.), antibacterial agents and antiseptic agents is described. The compounds are also useful in the treatment of tumors (such as cancers). The imidazolines are potent inhibitors of the transcription factor NF-&#x3ba;B as well as potent activity against the Gram (+) bacteriumandwith MIC values in the range of 50 &#x3bc;m/mL.

Multi-substituted imidazolines and method of use thereof

The synthesis and biological activity of indoloazepines and acid amine salts thereof which are structurally related to naturally-occurring hymenialdisine is disclosed. Naturally-occurring hymenialdisine obtained from the sponge is a potent inhibitor of production of cytokines interleukin-2 (IL-2) and tumor necrosis factor-&#x3b1; (TNF-&#x3b1;). The chemically-synthesized indoloazepines of the invention also inhibit production of IL-2 and TNF-&#x3b1;. The indoloazepines are useful for treating inflammatory diseases, particularly diseases associated with kinases NF-&#x3ba;B or GSK-3&#x3b2; activation or NF-&#x3ba;B activated gene expression products. The indoloazepines are useful for the treatment of cancer by the inhibition of kinases CHK1 and CHK2.

Preparation of hymenialdisine derivatives and use thereof

NF-kappaB inhibitors and uses thereof

A method for the separation and assay of phosphorylated peptides or proteins from complex mixtures of proteins and peptides is described. The method uses a diazo moiety linked by an organic group to a substrate. Kits for performing the assay are also described. The method and kits are particularly useful for detecting changes in phosphorylates produced in living cells.

Method for the enrichment and characterization of phosphorylated peptides or proteins

A new class of imidazolines as 4-position acids or esters with very potent anti-inflammatory as well as antimicrobial activity is described. The synthesis of these imidazolines includes a multicomponent reaction applicable to a combinatorial synthetic approach. The combination of these two key characteristics provides an effective therapeutic drug in the treatment of septic shock as well as many other inflammatory (arthritis and asthma) and infectious disorders. The use of this novel class of non-steroidal agents as anti-inflammatory agents (for the treatment of asthma, etc.), antibacterial agents, and antiseptic agents is described. The compounds are also useful in the treatment of tumors (such as cancers). The imidazolines are potent inhibitors of the transcription factor NF-&#x3ba;B as well as potent activity against the Gram (+) bacterium. The compositions are also useful for treating autoimmune diseases and for inhibiting rejection of organ and tissue transplants.

Growing community of inventors

East Lansing, MI, United States of America

Jetze J Tepe