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公开(公告)号：US08778990B2
公开(公告)日：2014-07-15
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 , A61N5/00 , A61P35/00
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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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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公开(公告)号：US08129429B2
公开(公告)日：2012-03-06
申请号：US12352473
申请日：2009-01-12
申请人： Michael B. Sporn , Karen T. Liby , Gordon W. Gribble , Tadashi Honda , Robert M. Kral , Colin J. Meyer
发明人： Michael B. Sporn , Karen T. Liby , Gordon W. Gribble , Tadashi Honda , Robert M. Kral , Colin J. Meyer
IPC分类号： A61K31/21
CPC分类号： A61K31/4174 , A61K31/275 , A61K31/277 , A61K31/4164 , A61K2300/00
摘要： The present invention concerns methods for treating and preventing renal/kidney disease, insulin resistance/diabetes, fatty liver disease, and/or endothelial dysfunction/cardiovascular disease using synthetic triterpenoids, optionally in combination with a second treatment or prophylaxis.
摘要翻译： 本发明涉及使用合成三萜类化合物治疗和预防肾/肾病，胰岛素抵抗/糖尿病，脂肪肝疾病和/或内皮功能障碍/心血管疾病的方法，任选地与第二次治疗或预防联合使用。
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公开(公告)号：US20120220652A1
公开(公告)日：2012-08-30
申请号：US13359381
申请日：2012-01-26
申请人： Michael B. Sporn , Karen T. Liby , Gordon W. Gribble , Tadashi Honda , Robert M. Kral , Colin J. Meyer
发明人： Michael B. Sporn , Karen T. Liby , Gordon W. Gribble , Tadashi Honda , Robert M. Kral , Colin J. Meyer
IPC分类号： A61K31/277 , A61P13/12
CPC分类号： A61K31/4174 , A61K31/275 , A61K31/277 , A61K31/4164 , A61K2300/00
摘要： The present invention concerns methods for treating and preventing renal/kidney disease, insulin resistance/diabetes, fatty liver disease, and/or endothelial dysfunction/cardiovascular disease using synthetic triterpenoids, optionally in combination with a second treatment or prophylaxis.
摘要翻译： 本发明涉及使用合成三萜类化合物治疗和预防肾/肾病，胰岛素抵抗/糖尿病，脂肪肝疾病和/或内皮功能障碍/心血管疾病的方法，任选地与第二治疗或预防组合。
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5.发明授权公开(公告)号：US08067394B2
公开(公告)日：2011-11-29
申请号：US12777120
申请日：2010-05-10
IPC分类号： A61K31/695 , A61K31/277 , A61K31/4164 , A61K31/40 , A61P35/00 , A61P35/02
CPC分类号： C07F7/0812 , C07C49/743 , C07C255/47 , C07C2603/26 , C07D207/337 , C07D209/08 , C07D233/64 , C07D295/145 , C07F7/081
摘要： This invention describes novel tricyclic-bis-enone derivatives (TBEs), such as TBE-31, TBE-34, TBE-45 and water-soluble TBEs. The methods of preparing these compounds are also disclosed. The inventors demonstrate the ability of these new TBEs to inhibit proliferation of human myeloma cells, inhibit the induction of iNOS in cells stimulated with interferon-γ, induce heme oxygenase-1 (HO-1), induce CD11b expression—a leukemia differentiation marker, inhibit proliferation of leukemia cells, induce apoptosis in human lung cancer, and induce apoptosis in other cancerous cells. The TBEs of this invention are expected to be useful agents for the treatment and prevention of many diseases, including cancer, neurological disorders, inflammation, and pathologies involving oxidative stress.
摘要翻译： 本发明描述了新型三环双烯衍生物（TBE），如TBE-31，TBE-34，TBE-45和水溶性TBE。 还公开了制备这些化合物的方法。 本发明人证明了这些新型TBE抑制人骨髓瘤细胞增殖的能力，抑制了用干扰素-γ刺激的细胞中诱导iNOS，诱导血红素加氧酶-1（HO-1），诱导CD11b表达 - 白血病分化标记， 抑制白血病细胞增殖，诱导人肺癌细胞凋亡，诱导其他癌细胞凋亡。 预期本发明的TBE可用于治疗和预防许多疾病，包括癌症，神经障碍，炎症和涉及氧化应激的病理学的有用试剂。
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公开(公告)号：US08455544B2
公开(公告)日：2013-06-04
申请号：US13359381
申请日：2012-01-26
申请人： Michael B. Sporn , Karen T. Liby , Gordon W. Gribble , Tadashi Honda , Robert M. Kral , Colin J. Meyer
发明人： Michael B. Sporn , Karen T. Liby , Gordon W. Gribble , Tadashi Honda , Robert M. Kral , Colin J. Meyer
IPC分类号： A61K31/21
CPC分类号： A61K31/4174 , A61K31/275 , A61K31/277 , A61K31/4164 , A61K2300/00
摘要： The present invention concerns methods for treating and preventing renal/kidney disease, insulin resistance/diabetes, fatty liver disease, and/or endothelial dysfunction/cardiovascular disease using synthetic triterpenoids, optionally in combination with a second treatment or prophylaxis.
摘要翻译： 本发明涉及使用合成三萜类化合物治疗和预防肾/肾病，胰岛素抵抗/糖尿病，脂肪肝疾病和/或内皮功能障碍/心血管疾病的方法，任选地与第二次治疗或预防联合使用。
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7.发明授权Synthetic triterpenoids and tricyclic-bis-enones for use in stimulating bone and cartilage growth 有权用于刺激骨和软骨生长的合成三萜类化合物和三环双烯酮公开(公告)号：US08299046B2
公开(公告)日：2012-10-30
申请号：US11941723
申请日：2007-11-16
申请人： Michael B. Sporn , Karen T. Liby , Tadashi Honda , Gregory Mundy , Ross Garrett , Hari Reddi , Gordon W. Gribble , Takahiro Niikura
发明人： Michael B. Sporn , Karen T. Liby , Tadashi Honda , Gregory Mundy , Ross Garrett , Hari Reddi , Gordon W. Gribble , Takahiro Niikura
IPC分类号： C07D233/02
CPC分类号： A61K31/4164 , A61K9/00 , A61K31/26 , A61K31/277 , A61K35/32 , A61K38/1841 , C12N5/0655 , C12N2501/999 , Y02A50/395 , A61K2300/00
摘要： The present invention concerns methods for stimulating the growth and repair of bone and cartilage using synthetic triterpenoids and tricyclic-bis-enones. Examples of suitable triterpenoids include CDDO, CDDO-Me, CDDO-Im, and CDDO-Ethylamide. Examples of tricyclic-bis-enones include TBE-31 and TBE-34.
摘要翻译： 本发明涉及使用合成三萜类化合物和三环双酮刺激骨和软骨的生长和修复的方法。 合适的三萜类化合物的实例包括CDDO，CDDO-Me，CDDO-Im和CDDO-乙酰胺。 三环双酮的实例包括TBE-31和TBE-34。
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8.发明申请公开(公告)号：US20090326063A1
公开(公告)日：2009-12-31
申请号：US12352473
申请日：2009-01-12
申请人： Michael B. Sporn , Karen T. Liby , Gordon W. Gribble , Tadashi Honda , Robert M. Kral , Colin J. Meyer
发明人： Michael B. Sporn , Karen T. Liby , Gordon W. Gribble , Tadashi Honda , Robert M. Kral , Colin J. Meyer
IPC分类号： A61K31/215 , A61P13/12
CPC分类号： A61K31/4174 , A61K31/275 , A61K31/277 , A61K31/4164 , A61K2300/00
摘要： The present invention concerns methods for treating and preventing renal/kidney disease, insulin resistance/diabetes, fatty liver disease, and/or endothelial dysfunction/cardiovascular disease using synthetic triterpenoids, optionally in combination with a second treatment or prophylaxis.
摘要翻译： 本发明涉及使用合成三萜类化合物治疗和预防肾/肾病，胰岛素抵抗/糖尿病，脂肪肝疾病和/或内皮功能障碍/心血管疾病的方法，任选地与第二次治疗或预防联合使用。
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9.发明申请Novel synthetic triterpenoids and methods of use in the treatment and prevention of multiple scleroris 审中-公开新型合成三萜类化合物及其用于治疗和预防多发性巩膜的方法公开(公告)号：US20090060873A1
公开(公告)日：2009-03-05
申请号：US12151425
申请日：2008-05-05
IPC分类号： A61K38/21 , C07C233/64 , A61K31/166 , A61K31/513 , A61K39/395 , A61K31/7028 , A61K31/337 , A61P25/28 , A61P35/00 , A61K31/519 , A61K31/437 , A61K31/403 , A61K31/366 , A61K31/60
CPC分类号： C07J63/008
摘要： The present invention overcomes limitations of the prior art by providing new compounds and methods for the treatment of conditions, such as neurodegenerative diseases (e.g., multiple sclerosis), psychiatric disorders (e.g., psychosis, bipolar disorder, depression, neuropathic pain), conditions involving CNS-mediated chronic pain, spinal cord injuries, and other diseases or injuries.
摘要翻译： 本发明通过提供新的化合物和治疗诸如神经变性疾病（例如多发性硬化症），精神病学障碍（例如精神病，双相情感障碍，抑郁症，神经性疼痛）等疾病的方法来克服现有技术的局限性， CNS介导的慢性疼痛，脊髓损伤等疾病或损伤。
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10.发明申请SYNTHESIS AND BIOLOGICAL ACTIVITIES OF NEW TRICYCLIC-BIS-ENONES (TBES) 有权新TRICYCLIC-BIS-ENONES（TBES）的合成和生物活性公开(公告)号：US20080261985A1
公开(公告)日：2008-10-23
申请号：US11941820
申请日：2007-11-16
IPC分类号： C07C255/47 , A61K31/13 , C07D233/66 , A61K31/4164 , C07D211/06 , A61K31/445 , A61K31/495 , C07D241/04 , C07D265/30 , A61K31/5375 , A61K31/40 , C07D207/00 , A61P35/00
CPC分类号： C07F7/0812 , C07C49/743 , C07C255/47 , C07C2603/26 , C07D207/337 , C07D209/08 , C07D233/64 , C07D295/145 , C07F7/081
摘要： This invention describes novel tricyclic-bis-enone derivatives (TBEs), such as TBE-31, TBE-34, TBE-45 and water-soluble TBEs. The methods of preparing these compounds are also disclosed. The inventors demonstrate the ability of these new TBEs to inhibit proliferation of human myeloma cells, inhibit the induction of iNOS in cells stimulated with interferon-γ, induce heme oxygenase-1 (HO-1), induce CD11b expression—a leukemia differentiation marker, inhibit proliferation of leukemia cells, induce apoptosis in human lung cancer, and induce apoptosis in other cancerous cells. The TBEs of this invention are expected to be useful agents for the treatment and prevention of many diseases, including cancer, neurological disorders, inflammation, and pathologies involving oxidative stress.
摘要翻译： 本发明描述了新型三环双烯衍生物（TBE），如TBE-31，TBE-34，TBE-45和水溶性TBE。 还公开了制备这些化合物的方法。 发明人证明了这些新型TBE抑制人骨髓瘤细胞增殖的能力，抑制了用干扰素-γ刺激的细胞中诱导iNOS，诱导血红素加氧酶-1（HO-1），诱导CD11b表达 - 白血病分化标记， 抑制白血病细胞增殖，诱导人肺癌细胞凋亡，诱导其他癌细胞凋亡。 预期本发明的TBE可用于治疗和预防许多疾病，包括癌症，神经障碍，炎症和涉及氧化应激的病理学的有用试剂。
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