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AssigneeTrustees of Dartmouth College
InventorsTadashi Honda, Yukiko Honda, Gordon W. Gribble, Michael B. Sporn, Nanjoo Suh
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New triterpenoid derivatives with various substituents at the C-17 position of 2-cyano-3,12-dioxooleana-1,9(11)-dien-28-oic acid (CDDO) were synthesized. Among them, 2-cyano-3,12-dioxooleana-1,9(11)-dien-28-onitrile (CNDDO), 1-(2-cyano-3,12-dioxooleana-1,9(11)-dien-28-oyl) imidazole, 1-(2-cyano-3,12-dioxooleana-1,9(11)-dien-28-oyl)-2-methylimidazole, 1-(2-cyano-3,12-dioxooleana-1,9(11)-dien-28-oyl)-4-methylimidazole show extremely high inhibitory activity (IC50=0.01-1 pM level) against production of nitric oxide induced by interferon-γ in mouse macrophages. These compounds can be used in the prevention or treatment of diseases such as cancer, Alzheimer's disease, Parkinson's disease, multiple sclerosis, rheumatoid arthritis, and other inflammatory diseases. All the new triterpenoid derivatives are more potent than previously known CDDO.
A composition of matter having the formula:
A triterpenoid derivative effective for inhibiting IFN-γ-induced NO production in macrophages or RAW cells, said composition having an IC50 value from 0.00006 nM to 0.43 nM.
A method of preventing or treating a disorder in a subject, comprising administering to a subject a pharmaceutically effective amount of a composition having the formula:
A method of modulating excessive nitric oxide or prostaglandin formation in a subject, comprising administering to said subject a pharmaceutically effective amount of a composition having the formula:
A method of modulating transcription or translation of iNOS or COX-2 genes, comprising administering to a subject a pharmaceutically effective amount of a composition having the formula:
Dependencies are inferred from the claim text.