Inhibitors and methods of use thereof

Details Inhibitors and methods of use thereof Inhibitors and methods of use thereof

C - Chemistry, Metallurgy

07

J

C07J 63/00 (2006.01) A61K 31/275 (2006.01) A61K 31/4172 (2006.01) A61K 31/4184 (2006.01) A61K 31/4196 (2006.01) A61K 31/56 (2006.01) A61K 31/704 (2006.01) A61P 25/28 (2006.01) A61P 29/00 (2006.01) A61P 35/00 (2006.01) C07D 233/54 (2006.01) C07D 233/68 (2006.01) C07D 235/06 (2006.01) C07D 249/08 (2006.01) C07D 317/34 (2006.01) C07H 15/24 (2006.01) C07J 53/00 (2006.01)

Patent

CA 2485565

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-.gamma. 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.

L'invention concerne la synthèse de nouveaux dérivés triterpénoïdes présentant des substituants variés en position C-17 position d'acide 2-cyano-3,12-dioxooléana-1,9(11)-diène-28-oique (CDDO). Parmi ceux-ci, l'invention concerne du 2-cyano-3,12-dioxooléana-1,9(11)-diène-28-onitrile (CNDDO), 1-(2-cyano-3,12-dioxooléana-1,9(11)-diène-28-oyl) imidazole, 1-(2-cyano-3,12-dioxooléana-1,9(11)-diène-28-oyl)-2-méthylimidazole, 1-(2-cyano-3,12-dioxooléana-1,9(11)-diène-28-oyl)-4-méthylimidazole présentant une activité inhibitrice extrêmement élevée (IC¿50? = 0,01-1 niveau pM) contre la production d'oxyde nitrique induite par l'interféron-.gamma. dans des macrophages de souris. Ces composés peuvent être utilisés pour prévenir ou pour traiter des maladies, notamment le cancer, la maladie d'Alzheimer, la maladie de Parkinson, la sclérose en plaques, l'arthrite rhumatoïde et d'autres maladies inflammatoires. Tous ces nouveaux dérivés triterpénoïdes sont plus puissants que les CDDO déjà connus.

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