University of British Columbia

Other

The Governors of the University of Alberta

Michel Roberge

Raymond John Andersen

Edward Piers

John Coleman

Dilip De Silva

Debra Wallace

Fangming Kong

Theresa M Allen

Robert Britton

Jasbinder Sanghera

E Dilip De Silva

Bruno Cinel

Xin-Hui Huang

Roberto Gs Berlinck

Grant Mauk

Daniel Leung

Teresa Allen

Eduardo Vottero

James Nieman

Alban Pereira

Aruna Balgi

Robert A Britton

Inhibitors of indoleamine 2,3-dioxygenase (IDO) are provided as are pharmaceutical compositions containing such inhibitors as well as the use of such inhibitors and compositions for the treatment of a condition in a mammalian subject characterized by pathology of the IDO-mediated tryptophan metabolic pathway. Such conditions may involve suppression of T-cell mediated immune response or may directly result from depletion of tryptophan or accumulation of a product of tryptophan degradation. Specific disease conditions include cataracts, age-related yellowing in the eye, neurodegenerative disorders, mood disorders, cancer and various bacterial/viral infections. IDO inhibitors of this invention are substituted naphthalene and anthracene diones. Novel compounds of this invention include the following taurine-substituted naphthaquinone structure. 

Indoleamine 2,3-dioxygenase (IDO) inhibitors

This invention relates to derivatives of hemiasterlin or Geodiamolide G having anti-mitotic activities and useful in treating cancer. These derivatives are represented by general formula I, wherein Y, n, R, R, R, R, R, R, R, R, R, and Rare as defined in the specification.

Biologically active peptides and compositions, their use

This invention provides analogs of hemiasterlin, methods of synthesis of the analogs and use of the analogs as cytotoxic and anti-mitotic agents.

Hemiasterlin analogs

Derivatives of hemiasterlin or Geodiamolide G having anti-mitotic activities and useful in treating cancer. These derivatives are represented by formula I wherein Y, n, R, R, R, R, R, R, R, R, and Rare as defined in the specification.

This invention provides analogs of eleutherobin and the eleuthesides modified at the C-11 position or comprising an epoxide functionality from C-11 to C-12. C-11 to C-12 is an ideal location for conjugating functional moieties to the eleutherobin pharmacophore without significant loss of antimitotic activity. Moieties that may be conjugated at C-11 include those intended to increase the solubility of the pharmacophore, to facilitate drug formulation, or to facilitate in vivo delivery or targeting.

Antimitotic eleuthesides

Antimitotic terpenoid compounds including sarcodictyin A and as eleutherobin may be obtained from organisms of the order Gorgonacea. Methods of preparing such compounds provided, as are novel antimitotic diterpene compounds having formula (I).

Antimitotic compounds

Novel granulatimide compounds and pharmaceutical formulations thereof are provided. Compounds of this invention have the general formula:

Granulatimide compounds and uses thereof

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Vancouver, Canada

Michel Roberge