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公开(公告)号:US20130237721A1
公开(公告)日:2013-09-12
申请号:US13217127
申请日:2011-08-24
申请人: Gordon W. Gribble , Tadashi Honda , Michael B. Sporn , Nanjoo Suh
发明人: Gordon W. Gribble , Tadashi Honda , Michael B. Sporn , Nanjoo Suh
IPC分类号: C07C255/47
CPC分类号: C07C255/47 , A61K31/19 , A61K31/275 , A61K31/277 , A61K31/35
摘要: Compounds and methods useful for chemopreventative treatment of diseases such as cancer, Alzheimer's disease, Parkinson's disease, inflammatory bowel diseases, and multiple sclerosis.
摘要翻译: 用于化学预防性治疗诸如癌症,阿尔茨海默氏病,帕金森病,炎性肠病和多发性硬化症的化合物和方法。
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公开(公告)号:US06552075B2
公开(公告)日:2003-04-22
申请号:US09927081
申请日:2001-08-09
申请人: Gordon W. Gribble , Tadashi Honda , Michael B. Sporn , Nanjoo Suh
发明人: Gordon W. Gribble , Tadashi Honda , Michael B. Sporn , Nanjoo Suh
IPC分类号: A61K31275
CPC分类号: C07C255/47 , A61K31/19 , A61K31/275 , A61K31/277 , A61K31/35
摘要: Compounds and methods useful for chemopreventative treatment of diseases such as cancer, Alzheimer's disease, Parkinson's disease, inflammatory bowel diseases, and multiple sclerosis.
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公开(公告)号:US06326507B1
公开(公告)日:2001-12-04
申请号:US09335003
申请日:1999-06-17
申请人: Gordon W. Gribble , Tadashi Honda , Michael B. Sporn , Nanjoo Suh
发明人: Gordon W. Gribble , Tadashi Honda , Michael B. Sporn , Nanjoo Suh
IPC分类号: A61K31275
CPC分类号: C07C255/47 , A61K31/19 , A61K31/275 , A61K31/277 , A61K31/35
摘要: Compounds and methods useful for chemopreventative treatment of diseases such as cancer, Alzheimer's disease, Parkinson's disease, inflammatory bowel diseases, and multiple sclerosis.
摘要翻译: 用于化学预防性治疗诸如癌症,阿尔茨海默氏病,帕金森病,炎性肠病和多发性硬化症的化合物和方法。
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公开(公告)号:US07288568B2
公开(公告)日:2007-10-30
申请号:US10395372
申请日:2003-03-24
申请人: Gordon W. Gribble , Tadashi Honda , Michael B. Sporn , Nanjoo Suh
发明人: Gordon W. Gribble , Tadashi Honda , Michael B. Sporn , Nanjoo Suh
IPC分类号: A61K31/275 , A61K31/19
CPC分类号: C07C255/47 , A61K31/19 , A61K31/275 , A61K31/277 , A61K31/35
摘要: Compounds and methods useful for chemopreventative treatment of diseases such as cancer, Alzheimer's disease, Parkinson's disease, inflammatory bowel diseases, and multiple sclerosis.
摘要翻译: 用于化学预防性治疗诸如癌症,阿尔茨海默氏病,帕金森病,炎性肠病和多发性硬化症的化合物和方法。
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公开(公告)号:US08586775B2
公开(公告)日:2013-11-19
申请号:US13217127
申请日:2011-08-24
申请人: Gordon W. Gribble , Tadashi Honda , Michael B. Sporn , Nanjoo Suh
发明人: Gordon W. Gribble , Tadashi Honda , Michael B. Sporn , Nanjoo Suh
IPC分类号: C07C255/49
CPC分类号: C07C255/47 , A61K31/19 , A61K31/275 , A61K31/277 , A61K31/35
摘要: Compounds and methods useful for chemopreventative treatment of diseases such as cancer, Alzheimer's disease, Parkinson's disease, inflammatory bowel diseases, and multiple sclerosis.
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公开(公告)号:US08067465B2
公开(公告)日:2011-11-29
申请号:US12722053
申请日:2010-03-11
IPC分类号: A61K31/275 , C07C255/47
CPC分类号: C07C62/38 , C07C225/12 , C07C255/47 , C07C271/18 , C07C2603/00 , C07C2603/26 , C07F7/1804
摘要: Novel tricyclic-bis-enone derivatives (TBEs) as well as the process for the preparation of such TBEs are provided. Also provided are methods for prevention and/or treatment of cancer, Alzheimer's disease, Parkinson's disease, multiple sclerosis, amyotropic lateral sclerosis, rheumatoid arthritis, inflammatory bowel disease, and all other diseases whose pathogenesis is believed to involve excessive production of either nitric oxide (NO) or prostaglandins or the overexpression of iNOS or COX-2 genes or gene products. Further, methods for the synthesis of the TBE compounds of the invention utilize cheap commercially available reagents and are highly cost effective and amenable to scale-up. Additional high efficiency synthetic methods that utilize novel intermediates as well as the synthesis of these intermediates are also provided. Furthermore, the invention also provides methods for designing novel and water-soluble TBEs.
摘要翻译: 提供了新的三环双烯衍生物(TBE)以及制备这种TBE的方法。 还提供了用于预防和/或治疗癌症,阿尔茨海默氏病,帕金森病,多发性硬化,肌萎缩性侧索硬化,类风湿性关节炎,炎症性肠病以及其发病机制被认为涉及过量产生一氧化氮的所有其它疾病的方法 NO)或前列腺素或iNOS或COX-2基因或基因产物的过表达。 此外,用于合成本发明的TBE化合物的方法使用便宜的市售试剂,并且是高成本有效的并且适于放大。 还提供了利用新型中间体以及这些中间体的合成的其它高效合成方法。 此外,本发明还提供了设计新型和水溶性TBE的方法。
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公开(公告)号:US20080220057A1
公开(公告)日:2008-09-11
申请号:US11927418
申请日:2007-10-29
申请人: Gordon W. Gribble , Tadashi Honda , Michael B. Sporn , Nanjoo Suh
发明人: Gordon W. Gribble , Tadashi Honda , Michael B. Sporn , Nanjoo Suh
IPC分类号: A61K9/127 , C07C255/57 , A61K31/135 , A61P35/04 , A61P1/00 , A61P9/00 , A61P19/02 , A61P25/00 , C07D261/20 , A61K9/48
CPC分类号: C07C255/47 , A61K31/19 , A61K31/275 , A61K31/277 , A61K31/35
摘要: Compounds and methods useful for chemopreventative treatment of diseases such as cancer, Alzheimer's disease, Parkinson's disease, inflammatory bowel diseases, and multiple sclerosis.
摘要翻译: 用于化学预防性治疗诸如癌症,阿尔茨海默氏病,帕金森病,炎性肠病和多发性硬化症的化合物和方法。
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公开(公告)号:US07176237B2
公开(公告)日:2007-02-13
申请号:US10345053
申请日:2003-01-15
IPC分类号: A61K31/275 , C07C255/47
CPC分类号: C07C62/38 , C07C225/12 , C07C255/47 , C07C271/18 , C07C2603/00 , C07C2603/26 , C07F7/1804
摘要: Novel tricyclic-bis-enone derivatives (TBEs) as well as the process for the preparation of such TBEs are provided. Also provided are methods for prevention and/or treatment of cancer, Alzheimer's disease, Parkinson's disease, multiple sclerosis, amyotropic lateral sclerosis, rheumatoid arthritis, inflammatory bowel disease, and all other diseases whose pathogenesis is believed to involve excessive production of either nitric oxide (NO) or prostaglandins or the overexpression of iNOS or COX-2 genes or gene products. Further, methods for the synthesis of the TBE compounds of the invention utilize cheap commercially available reagents and are highly cost effective and amenable to scale-up. Additional high efficiency synthetic methods that utilize novel intermediates as well as the synthesis of these intermediates are also provided. Furthermore, the invention also provides methods for designing novel and water-soluble TBEs.
摘要翻译: 提供了新的三环双烯衍生物(TBE)以及制备这种TBE的方法。 还提供了用于预防和/或治疗癌症,阿尔茨海默氏病,帕金森病,多发性硬化,肌萎缩性侧索硬化,类风湿性关节炎,炎症性肠病以及其发病机制被认为涉及过量产生一氧化氮的所有其它疾病的方法 NO)或前列腺素或iNOS或COX-2基因或基因产物的过表达。 此外,用于合成本发明的TBE化合物的方法使用便宜的市售试剂,并且是高成本有效的并且适于放大。 还提供了利用新型中间体以及这些中间体的合成的其它高效合成方法。 此外,本发明还提供了设计新型和水溶性TBE的方法。
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公开(公告)号:US06974801B2
公开(公告)日:2005-12-13
申请号:US10435925
申请日:2003-05-12
申请人: Tadashi Honda , Yukiko Honda , Gordon W. Gribble , Michael B. Sporn , Nanjoo Suh
发明人: Tadashi Honda , Yukiko Honda , Gordon W. Gribble , Michael B. Sporn , Nanjoo Suh
IPC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 , A61K31/70 , A61K31/4164 , C07H13/08
CPC分类号: C07D233/54 , A61K31/275 , A61K31/4172 , A61K31/4184 , A61K31/4196 , A61K31/704 , C07D233/68 , C07D235/06 , C07D249/08 , C07D317/34 , C07H15/24
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-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.
摘要翻译: 合成了在2-氰基-3,12-二氧代噻吩-1,9(11) - 二 - 二十八酸(CDDO)的C-17位具有各种取代基的新三萜衍生物。 其中,2-氰基-3,12-二氧代噻吩-1,9(11) - 二烯-28-腈(CNDDO),1-(2-氰基-3,12-二氧杂环戊烯-1,9(11) - 二烯 -2-甲基咪唑,1-(2-氰基-3,12-二氧杂环戊烯-1,9(11) - 二烯-28-基)-2-甲基咪唑,1-(2-氰基-3,12-二氧代噻唑 -1,9(11) - 二烯-28-基)-4-甲基咪唑显示出对干扰素-γ诱导的一氧化氮产生的极高的抑制活性(IC 50> 0.01-1pM水平) 在小鼠巨噬细胞。 这些化合物可用于预防或治疗诸如癌症,阿尔茨海默氏病,帕金森病,多发性硬化症,类风湿性关节炎和其它炎性疾病的疾病。 所有新的三萜衍生物比先前已知的CDDO更有效。
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公开(公告)号:US08034955B2
公开(公告)日:2011-10-11
申请号:US11927418
申请日:2007-10-29
申请人: Gordon W. Gribble , Tadashi Honda , Michael B. Sporn , Nanjoo Suh
发明人: Gordon W. Gribble , Tadashi Honda , Michael B. Sporn , Nanjoo Suh
IPC分类号: A61K31/275 , A61K31/255 , C07C69/76 , C07C255/49
CPC分类号: C07C255/47 , A61K31/19 , A61K31/275 , A61K31/277 , A61K31/35
摘要: Compounds and methods useful for chemopreventative treatment of diseases such as cancer, Alzheimer's disease, Parkinson's disease, inflammatory bowel diseases, and multiple sclerosis.
摘要翻译: 用于化学预防性治疗诸如癌症,阿尔茨海默氏病,帕金森病,炎性肠病和多发性硬化症的化合物和方法。
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