发明名称 |
INHIBITORS AND METHODS OF USE THEREOF |
摘要 |
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. |
申请公布号 |
WO2004064723(A2) |
申请公布日期 |
2004.08.05 |
申请号 |
WO2003US14904 |
申请日期 |
2003.05.12 |
申请人 |
TRUSTEES OF DARTMOUTH COLLEGE;HONDA, TADASHI;HONDA, YUKIKO;GRIBBLE, GORDON, W.;SPORN, MICHAEL, B.;SUH, NANJOO |
发明人 |
HONDA, TADASHI;HONDA, YUKIKO;GRIBBLE, GORDON, W.;SPORN, MICHAEL, B.;SUH, NANJOO |
分类号 |
A61K31/275;A61K31/4172;A61K31/4184;A61K31/4196;A61K31/704;C07D233/54;C07D233/60;C07D233/68;C07D235/06;C07D249/08;C07D249/10;C07D317/34;C07H15/24 |
主分类号 |
A61K31/275 |
代理机构 |
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代理人 |
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