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公开(公告)号:US20120071684A1
公开(公告)日:2012-03-22
申请号:US13306043
申请日:2011-11-29
IPC分类号: C07C255/47
CPC分类号: A61K31/70
摘要: A triterpenoid compound, methyl 2-cyano-3,12-dioxoleana-1,9(11)-dien-28-oate (CDDO methyl ester), has a non-crystalline, glassy solid form and a non-hydrous crystalline form that can prepared, for example, from a saturated methanol solution. The glassy form displays an enhanced bioavailability over the non-hydrous crystalline form. Each form of CDDO methyl ester is a superior candidate for use, typically in solid dosage form, for treating a variety of disease states, generally associated with inflammation.
摘要翻译: 三萜化合物,2-氰基-3,12-二氧杂环戊烯-1,9(11) - 二烯-28-甲酸甲酯(CDDO甲酯)具有非结晶的玻璃状固体形式和非水合结晶形式, 可以例如由饱和甲醇溶液制备。 玻璃状的形式显示了非含水结晶形式的增强的生物利用度。 每种形式的CDDO甲酯是通常用于固体剂型的优选候选药物,用于治疗通常与炎症相关的各种疾病状态。
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公开(公告)号:US20120330050A1
公开(公告)日:2012-12-27
申请号:US13537583
申请日:2012-06-29
IPC分类号: C07C255/47
CPC分类号: A61K31/70
摘要: A triterpenoid compound, methyl 2-cyano-3,12-dioxoleana-1,9(11)-dien-28-oate (CDDO methyl ester), has a non-crystalline, glassy solid form and a non-hydrous crystalline form that can prepared, for example, from a saturated methanol solution. The glassy form displays an enhanced bioavailability over the non-hydrous crystalline form. Each form of CDDO methyl ester is a superior candidate for use, typically in solid dosage form, for treating a variety of disease states, generally associated with inflammation.
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公开(公告)号:US20090048204A1
公开(公告)日:2009-02-19
申请号:US12191176
申请日:2008-08-13
IPC分类号: A61K31/215 , C07C69/753 , A61K31/7068 , A61P35/00
CPC分类号: A61K31/70
摘要: A triterpenoid compound, methyl 2-cyano-3,12-dioxoleana-1,9(11)-dien-28-oate (CDDO methyl ester), has a non-crystalline, glassy solid form and a non-hydrous crystalline form that can prepared, for example, from a saturated methanol solution. The glassy form displays an enhanced bioavailability over the non-hydrous crystalline form. Each form of CDDO methyl ester is a superior candidate for use, typically in solid dosage form, for treating a variety of disease states, generally associated with inflammation.
摘要翻译: 三萜化合物,2-氰基-3,12-二氧杂环戊烯-1,9(11) - 二烯-28-甲酸甲酯(CDDO甲酯)具有非结晶的玻璃状固体形式和非水合结晶形式, 可以例如由饱和甲醇溶液制备。 玻璃状的形式显示了非含水结晶形式的增强的生物利用度。 每种形式的CDDO甲酯是通常用于固体剂型的优选候选药物,用于治疗通常与炎症相关的各种疾病状态。
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4.
公开(公告)号:US20120283450A1
公开(公告)日:2012-11-08
申请号:US13552530
申请日:2012-07-18
申请人: Eric Anderson , Gary L. Bolton , Deborah A. Ferguson , Xin Jiang , Robert M. Kral, JR. , Patrick M. O'Brien , Melean Visnick
发明人: Eric Anderson , Gary L. Bolton , Deborah A. Ferguson , Xin Jiang , Robert M. Kral, JR. , Patrick M. O'Brien , Melean Visnick
IPC分类号: C07C255/46 , C07F7/10 , C07J21/00 , C07J71/00 , C07J41/00 , C07D317/30 , C07D311/62
CPC分类号: C07C255/46 , C07C2601/16 , C07D311/74 , C07D317/26 , C07D493/10 , C07F7/1804 , C07J21/003 , C07J41/0055 , C07J41/0094 , C07J53/001 , C07J71/0005
摘要: This invention provides novel compounds comprising the following anti-inflammatory pharmacore: wherein X, R1 and R2 are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds, methods and intermediates useful for making the compounds, and methods of using the compounds and compositions.
摘要翻译: 本发明提供包含以下抗炎药物的新化合物:其中X,R 1和R 2在本文中定义。 还提供了包含这种化合物的药物组合物,试剂盒和制品,用于制备化合物的方法和中间体,以及使用该化合物和组合物的方法。
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公开(公告)号:US20120101149A1
公开(公告)日:2012-04-26
申请号:US13127551
申请日:2009-10-29
申请人: Tadashi Honda , Michael B. Sporn , Karen T. Liby , Gordon W. Gribble , Robert M. Kral, JR. , Melean Visnick
发明人: Tadashi Honda , Michael B. Sporn , Karen T. Liby , Gordon W. Gribble , Robert M. Kral, JR. , Melean Visnick
IPC分类号: A61K31/277 , A61K48/00 , A61P35/00 , A61N5/00 , A61P3/06 , A61P9/12 , A61P25/00 , A61P13/12 , C07C255/47 , A61P29/00
CPC分类号: C07J41/0033 , C07J41/0055
摘要: This invention features betulinic acid derivatives having the formula: wherein the variables are defined herein. The invention also provides related compounds and intermediates thereof, as well as pharmaceutical compositions, kits, and articles of manufacture comprising such compounds. Treatment methods and methods of manufacture are also provided.
摘要翻译: 本发明的特征在于具有下式的桦木酸衍生物:其中变量在本文中定义。 本发明还提供了相关的化合物及其中间体,以及包含这些化合物的药物组合物,试剂盒和制品。 还提供了处理方法和制造方法。
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6.
公开(公告)号:US20090048205A1
公开(公告)日:2009-02-19
申请号:US12192710
申请日:2008-08-15
IPC分类号: A61K31/7064 , A61P35/00
CPC分类号: A61K31/122 , A61K31/7068 , C07B2200/13 , C07J63/008 , A61K2300/00
摘要: The present invention concerns methods for treating cancer, such as pancreatic cancer, using combination therapies, including the combination of a synthetic triterpenoid, e.g., CDDO-Me, and gemcitabine.
摘要翻译: 本发明涉及使用组合疗法(包括合成三萜类化合物例如CDDO-Me和吉西他滨)的组合治疗癌症如胰腺癌的方法。
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7.
公开(公告)号:US20100048887A1
公开(公告)日:2010-02-25
申请号:US12426889
申请日:2009-04-20
申请人: Eric Anderson , Gary L. Bolton , Deborah A. Ferguson , Xin Jiang , Robert M. Kral, JR. , Patrick M. O'Brien , Melean Visnick
发明人: Eric Anderson , Gary L. Bolton , Deborah A. Ferguson , Xin Jiang , Robert M. Kral, JR. , Patrick M. O'Brien , Melean Visnick
IPC分类号: C07J21/00 , C07C49/203 , C07D317/10 , C07F7/02 , C07C39/205 , C07C49/603 , C07D311/02 , C07J71/00 , C07J1/00 , C07J51/00
CPC分类号: C07C255/46 , C07C2601/16 , C07D311/74 , C07D317/26 , C07D493/10 , C07F7/1804 , C07J21/003 , C07J41/0055 , C07J41/0094 , C07J53/001 , C07J71/0005
摘要: This invention provides novel compounds comprising the following anti-inflammatory pharmacore: wherein X, R1 and R2 are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds, methods and intermediates useful for making the compounds, and methods of using the compounds and compositions.
摘要翻译: 本发明提供包含以下抗炎药物的新化合物:其中X,R 1和R 2在本文中定义。 还提供了包含这种化合物的药物组合物,试剂盒和制品,用于制备化合物的方法和中间体,以及使用该化合物和组合物的方法。
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