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公开(公告)号：US08653273B2
公开(公告)日：2014-02-18
申请号：US13178117
申请日：2011-07-07
申请人： Kirsten Alison Rinderspacher , Donald W. Landry , Yuli Xie , Yidong Liu , Gangli Gong , Shi-Xian Deng
发明人： Kirsten Alison Rinderspacher , Donald W. Landry , Yuli Xie , Yidong Liu , Gangli Gong , Shi-Xian Deng
IPC分类号： C07D211/62
CPC分类号： C07D211/96 , C07D211/62 , C07D401/12 , C07D409/12 , C07F9/59 , C12N9/99
摘要： The present invention relates to compounds that exhibit vasodilatory and anti-inflammatory effects by inhibiting the activity of soluble epoxide hydrolase (sEH). The present invention is also directed to methods of identifying such compounds, and use of such compounds for the treatment of diseases related to dysfunction of vasodilation, inflammation, and/or endothelial cells. In particular non-limiting embodiments, components of the invention may be used to treat hypertension.
摘要翻译： 本发明涉及通过抑制可溶性环氧化物水解酶（sEH）的活性而显示血管扩张和抗炎作用的化合物。 本发明还涉及鉴定这些化合物的方法，以及这些化合物用于治疗与血管舒张功能障碍，炎症和/或内皮细胞相关的疾病的用途。 特别是非限制性实施方案，本发明的组分可用于治疗高血压。
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公开(公告)号：US20120029022A1
公开(公告)日：2012-02-02
申请号：US13178117
申请日：2011-07-07
申请人： Donald W. Landry , Yuli Xie , Yidong Liu , Gangli Gong , Shi-Xian Deng , Kirsten Alison Rinderspacher
发明人： Donald W. Landry , Yuli Xie , Yidong Liu , Gangli Gong , Shi-Xian Deng , Kirsten Alison Rinderspacher
IPC分类号： A61K31/445 , A61P9/12 , A61P29/00 , C07D211/62 , A61P9/00
CPC分类号： C07D211/96 , C07D211/62 , C07D401/12 , C07D409/12 , C07F9/59 , C12N9/99
摘要： The present invention relates to compounds that exhibit vasodilatory and anti-inflammatory effects by inhibiting the activity of soluble epoxide hydrolase (sEH). The present invention is also directed to methods of identifying such compounds, and use of such compounds for the treatment of diseases related to dysfunction of vasodilation, inflammation, and/or endothelial cells. In particular non-limiting embodiments, components of the invention may be used to treat hypertension.
摘要翻译： 本发明涉及通过抑制可溶性环氧化物水解酶（sEH）的活性而显示血管扩张和抗炎作用的化合物。 本发明还涉及鉴定这些化合物的方法，以及这些化合物用于治疗与血管舒张功能障碍，炎症和/或内皮细胞相关的疾病的用途。 特别是非限制性实施方案，本发明的组分可用于治疗高血压。
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公开(公告)号：US08685963B2
公开(公告)日：2014-04-01
申请号：US13094504
申请日：2011-04-26
申请人： Donald W. Landry , Shi Xian Deng , Gangli Gong , Yuli Xie , Yidong Liu , K. Alison Rinderspacher
发明人： Donald W. Landry , Shi Xian Deng , Gangli Gong , Yuli Xie , Yidong Liu , K. Alison Rinderspacher
IPC分类号： A61K31/54 , A01N43/42 , A61K31/47 , C07D215/36
CPC分类号： C07D215/40 , A61K31/47 , C07D401/12 , C07D409/12
摘要： The present invention relates to compounds with activity as BACE1 and NFκB modulators, and methods for treating, preventing, or ameliorating neurodegenerative diseases, such as Alzheimer's disease. The present invention is also directed to the treatment of diseases related to dysfunction of cell proliferation, the immune system and/or inflammation using such compounds or pharmaceutical compositions containing such candidate compounds.
摘要翻译： 本发明涉及具有BACE1和NFκB调节剂活性的化合物，以及治疗，预防或改善神经变性疾病如阿尔茨海默氏病的方法。 本发明还涉及使用这些化合物或包含这些候选化合物的药物组合物治疗与细胞增殖功能障碍，免疫系统和/或炎症有关的疾病。
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公开(公告)号：US20120064099A1
公开(公告)日：2012-03-15
申请号：US13094504
申请日：2011-04-26
申请人： Donald W. Landry , Tae-Wan Kim , Shi Xian Deng , Gangli Gong , Jeremy C. Hwang , Yuli Xie , Yidong Liu , K. Alison Rinderspacher
发明人： Donald W. Landry , Tae-Wan Kim , Shi Xian Deng , Gangli Gong , Jeremy C. Hwang , Yuli Xie , Yidong Liu , K. Alison Rinderspacher
IPC分类号： A61K39/00 , A61K31/542 , A61K31/47 , A61P29/00 , C07D215/36 , A61P35/00 , A61P25/28 , A61P37/02 , C12N5/02 , C07D513/04
CPC分类号： C07D215/40 , A61K31/47 , C07D401/12 , C07D409/12
摘要： The present invention relates to compounds with activity as BACE1 and NFκB modulators, and methods for treating, preventing, or ameliorating neurodegenerative diseases, such as Alzheimer's disease. The present invention is also directed to the treatment of diseases related to dysfunction of cell proliferation, the immune system and/or inflammation using such compounds or pharmaceutical compositions containing such candidate compounds.
摘要翻译： 本发明涉及具有BACE1和NFκB调节剂活性的化合物，以及治疗，预防或改善神经变性疾病如阿尔茨海默氏病的方法。 本发明还涉及使用这些化合物或包含这些候选化合物的药物组合物治疗与细胞增殖功能障碍，免疫系统和/或炎症有关的疾病。
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5.发明申请公开(公告)号：US20110071124A1
公开(公告)日：2011-03-24
申请号：US12858837
申请日：2010-08-18
申请人： Tae-wan Kim , Donald W. Landry , Jeremy C. Hwang , Shi Xian Deng , Gangli Gong , Yuli Xie , Yidong Liu , Alison Rinderspacher
发明人： Tae-wan Kim , Donald W. Landry , Jeremy C. Hwang , Shi Xian Deng , Gangli Gong , Yuli Xie , Yidong Liu , Alison Rinderspacher
IPC分类号： A61K31/40 , A61K31/445 , A61K31/397 , A61K31/165 , A61K31/138 , A61K31/495 , A61K31/41 , A61K31/4184 , A61K31/35 , A61P25/28 , C12N9/99
CPC分类号： A61K31/535 , A61K31/351 , A61K31/395 , A61K31/40 , A61K31/4178 , A61K31/496
摘要： The present invention relates to compounds with activity as inhibitors of sAPPβ and Aβ production, and methods for treating, preventing, or ameliorating neurodegenerative diseases, such as Alzheimer's disease and pharmaceutical compositions containing such candidate compounds.
摘要翻译： 本发明涉及具有作为sAPP和bgr的抑制剂活性的化合物。 和A＆bgr 生产和治疗，预防或改善神经变性疾病如阿尔茨海默氏病的方法和含有这些候选化合物的药物组合物。
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公开(公告)号：US20210047337A1
公开(公告)日：2021-02-18
申请号：US17085791
申请日：2020-10-30
申请人： Konstantin Petrukhin , Kirsten Alison Rinderspacher , Shi-Xian Deng , Andras Varadi , Boglarka Racz , Peter Bernstein , Patricia C. Weber , Donald W. Landry , Andrew S. Wasmuth
发明人： Konstantin Petrukhin , Kirsten Alison Rinderspacher , Shi-Xian Deng , Andras Varadi , Boglarka Racz , Peter Bernstein , Patricia C. Weber , Donald W. Landry , Andrew S. Wasmuth
IPC分类号： C07D487/04 , C07D519/00 , A61P27/02
摘要： The present invention provides a compound having the structure: wherein R1, R2, R3, R4, and R5 are each independently H, halogen, CF3, C1-C4 alkyl, aryl or heteroaryl; X is N or CR6, wherein R6 is H, OH, or halogen; A is absent or present, and when present is B has the structure: or a pharmaceutically acceptable salt thereof.
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公开(公告)号：US20080176920A1
公开(公告)日：2008-07-24
申请号：US11674965
申请日：2007-02-14
申请人： Richard Ambron , Ying-Ju Sung , Jeremy Greenwood , Leah Frye , Shi-Xian Deng , Yuli Xie , Donald W. Landry
发明人： Richard Ambron , Ying-Ju Sung , Jeremy Greenwood , Leah Frye , Shi-Xian Deng , Yuli Xie , Donald W. Landry
IPC分类号： A61K31/416 , A61K31/352 , A61K31/4035 , A61P43/00 , A61K31/215 , A61K31/40
CPC分类号： A61K31/40 , A61K31/235 , A61K31/335
摘要： The present invention relates to compounds that may be used to inhibit activation of protein kinase G (“PKG”). It is based, at least in part, on the discovery of the tertiary structure of PKG and the identification of molecules that either bind to the active site of PKG and/or are analogs of balanol.
摘要翻译： 本发明涉及可用于抑制蛋白激酶G（“PKG”）活化的化合物。 至少部分基于PKG的三级结构的发现以及与PKG的活性位点结合的分子的鉴定和/或是平衡醇的类似物。
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公开(公告)号：US08846742B2
公开(公告)日：2014-09-30
申请号：US11674965
申请日：2007-02-14
申请人： Richard Ambron , Ying-Ju Sung , Jeremy Greenwood , Leah Frye , Shi-Xian Deng , Yuli Xie , Donald W. Landry
发明人： Richard Ambron , Ying-Ju Sung , Jeremy Greenwood , Leah Frye , Shi-Xian Deng , Yuli Xie , Donald W. Landry
IPC分类号： A61K31/415 , A61K31/335
CPC分类号： A61K31/40 , A61K31/235 , A61K31/335
摘要： The present invention relates to compounds that may be used to inhibit activation of protein kinase G (“PKG”). It is based, at least in part, on the discovery of the tertiary structure of PKG and the identification of molecules that either bind to the active site of PKG and/or are analogs of balanol.
摘要翻译： 本发明涉及可用于抑制蛋白激酶G（“PKG”）活化的化合物。 至少部分基于PKG的三级结构的发现以及与PKG的活性位点结合的分子的鉴定和/或是平衡醇的类似物。
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公开(公告)号：US20120295853A1
公开(公告)日：2012-11-22
申请号：US13569510
申请日：2012-08-08
申请人： Richard Ambron , Ying-Ju Sung , Donald W. Landry , Shi-Xian Deng
发明人： Richard Ambron , Ying-Ju Sung , Donald W. Landry , Shi-Xian Deng
CPC分类号： A61K38/06 , A61K9/0014 , A61K9/7023 , A61K31/352 , A61K31/4422 , A61K31/55 , A61K38/02 , A61K38/07 , A61K38/465 , A61K47/64 , C12N9/1205 , C12Y301/04017
摘要： The present invention relates to the discovery of a novel molecular pathway involved in long-term hyperexcitability of sensory neurons, which, in higher animals, is associated with persistent pain. It is based on the discovery that, following injury to an axon of a neuron, an increase in nitric oxide synthase activity results in increased nitric oxide production, which, in turn, activates guanylyl cyclase, thereby increasing levels of cGMP. Increased cGMP results in activation of protein kinase G (“PKG”), which then is retrogradely transported along the axon to the neuron cell body, where it phosphorylates MAPKerk.
摘要翻译： 本发明涉及发现涉及感觉神经元的长期兴奋性的新型分子途径，其在高等动物中与持续性疼痛相关。 基于这样的发现，在神经元轴突损伤之后，一氧化氮合酶活性的增加导致一氧化氮产生增加，这反过来激活鸟苷酸环化酶，从而增加cGMP的水平。 增加的cGMP导致蛋白激酶G（PKG）的激活，其然后沿着轴突逆行转运到神经元细胞体，其中磷酸化MAPKerk。
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公开(公告)号：US09173874B2
公开(公告)日：2015-11-03
申请号：US13452019
申请日：2012-04-20
CPC分类号： A61K39/0013 , A61K31/44 , A61K39/385 , A61K47/643 , A61K47/646 , A61K2039/505 , A61K2039/55566 , A61K2039/6056 , A61K2039/6081
摘要： The present invention relates to anti-drug vaccines based on conjugates between the drug and a non-immunogenic carrier protein. In preferred embodiments, it provides for anti-cocaine vaccines and their use to diminish the effects and/or use of cocaine in a subject.
摘要翻译： 本发明涉及基于药物和非免疫原性载体蛋白质之间的缀合物的抗药物疫苗。 在优选的实施方案中，它提供了抗可卡因疫苗及其用于减少受试者中可卡因的作用和/或使用的用途。
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