Rigel Pharmaceuticals, Incorporated

Sarkiz D Issakani

Jianing Huang

Julie Sheung

Todd R Pray

Rajinder Paul Singh

Simon Shaw

Gary Charles Look

Usha V Ramesh

Donald G Payan

Dane A Goff

David Carroll

Matthew Duncton

Xiang Xu

Thomas Weitao Sun

Arvinder Sran

Yasumichi Hitoshi

Henry Lu

Nan Lin

Lyuben Tsvetkov

Disclosed are benzimidazole compounds, as well as pharmaceutical compositions and methods of use thereof. One embodiment is a compound having the structure and pharmaceutically acceptable salts, prodrugs and N-oxides thereof (and solvates and hydrates thereof), wherein R, R, R, R, Y and X are as described herein. In certain embodiments, a compound disclosed herein activates AMPK, and can be used to treat disease by activating the AMPK pathway.

Direct AMPK activators

Disclosed are sulfonamidoquinoline compounds, as well as pharmaceutical compositions and methods of use. One embodiment is a compound having the structure and pharmaceutically acceptable salts, prodrugs and N-oxides thereof (and solvates and hydrates thereof), wherein R, R, Rand Rare as described herein. In certain embodiments, a compound disclosed herein inhibits ubiquitination, and can be used to treat disease by blocking the degradation of tumor suppressors.

Ubiquitination inhibitors

This invention describes compounds useful as ubiquitin ligase inhibitors. The compounds of the invention are useful as inhibitors of the biochemical pathways of organisms in which ubiquitination is involved. The invention also provides for pharmaceutical compositions comprising the compounds described in the invention for the treatment of conditions that require inhibition of ubiquitin ligases. Furthermore, the invention provides for methods of inhibiting ubiquitination in a cell comprising contacting a cell in which inhibition of ubiquitination is desired with a compound according to the invention.

Ubiquitin ligase inhibitors

The invention relates to assays for measuring ubiquitin ligase activity and for identifying modulators of ubiquitin ligase enzymes.

Ubiquitin ligase assay

This invention describes compounds and pharmaceutical compositions useful as inhibitors of ubiquitination. The compounds and compositions of the invention are useful as inhibitors of the biochemical pathways of organisms in which ubiquitination is involved. In particular, the compounds and compositions are useful for treating diseases caused by viruses such as poxviruses and retroviruses. The invention further provides for methods of treating smallpox, Herpes virus and HIV infection in patients using the compounds and compositions of the invention.

Rhodanine compositions for use as antiviral agents

Provided are methods and compositions for assaying for ubiquitin agents that are enzymatic components of ubiquitin-mediated proteolysis and, more particularly, methods and compositions for assaying for agents that modulate the activity of such ubiquitin agents.

Assays for identifying ubiquitin agents and for identifying agents that modify the activity of ubiquitin agents

The present invention relates to substituted diphenyl heterocycle compounds and pharmaceutical compositions thereof that inhibit replication of HCV virus. The present invention also relates to the use of the compounds and/or compositions to inhibit HCV replication and/or proliferation and to treat or prevent HCV infections.

Substituted diphenyl heterocycles useful for treating HCV infection

Ubiquitin conjugation assays

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San Jose, CA, United States of America

Sarkiz D Issakani