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31.发明授权Heterocyclic compounds, pharmaceutical compositions comprising same, and methods for inhibiting &bgr;-amyloid peptide release and/or its synthesis by use of such compounds 失效杂环化合物，包含其的药物组合物，以及通过使用这些化合物抑制β-淀粉样蛋白肽释放和/或其合成的方法公开(公告)号：US06506782B1
公开(公告)日：2003-01-14
申请号：US09032019
申请日：1998-02-27
申请人： Eugene D. Thorsett , Warren J. Porter , Jeffrey S. Nissen , Lee H. Latimer , James E. Audia , James Droste
发明人： Eugene D. Thorsett , Warren J. Porter , Jeffrey S. Nissen , Lee H. Latimer , James E. Audia , James Droste
IPC分类号： A61K314245
CPC分类号： A61K31/4245
摘要： Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.
摘要翻译： 公开了抑制β-淀粉样蛋白肽释放和/或其合成的化合物，因此具有治疗阿尔茨海默病的效用。 还公开了包含抑制β-淀粉样蛋白肽释放和/或其合成的化合物的药物组合物以及用这种药物组合物预防性和治疗性地治疗阿尔茨海默病的方法。
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32.发明授权N-(aryl/heteroaryl) amino acid derivatives, pharmaceutical compositions comprising same, and methods for inhibiting &bgr;-amyloid peptide release and/or its synthesis by use of such compounds 失效N-（芳基/杂芳基）氨基酸衍生物，包含其的药物组合物，以及通过使用这些化合物抑制β-淀粉样蛋白肽释放和/或其合成的方法公开(公告)号：US06495693B2
公开(公告)日：2002-12-17
申请号：US09280966
申请日：1999-03-30
申请人： James E. Audia , Beverly K. Folmer , Varghese John , Lee H. Latimer , Jeffrey S. Nissen , Warren J. Porter , Eugene D. Thorsett , Jing Wu
发明人： James E. Audia , Beverly K. Folmer , Varghese John , Lee H. Latimer , Jeffrey S. Nissen , Warren J. Porter , Eugene D. Thorsett , Jing Wu
IPC分类号： C07D27782
CPC分类号： C07D215/38 , A61K31/00 , A61K31/198 , A61K31/223 , C07C237/08 , C07C237/10 , C07C237/12 , C07C271/22 , C07D209/20 , C07D233/64 , C07D277/62 , C07D277/82
摘要： Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.
摘要翻译： 公开了抑制β-淀粉样蛋白肽释放和/或其合成的化合物，因此具有治疗阿尔茨海默病的效用。 还公开了包含抑制β-淀粉样蛋白肽释放和/或其合成的化合物的药物组合物以及用这种药物组合物预防性和治疗性地治疗阿尔茨海默病的方法。
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33.发明授权Heterocyclic compounds, pharmaceutical compositions comprising same, and methods for inhibiting β-amyloid peptide release and/or its synthesis by use of such compounds 失效杂环化合物，包含其的药物组合物，以及通过使用这些化合物抑制β-淀粉样蛋白肽释放和/或其合成的方法公开(公告)号：US06849650B2
公开(公告)日：2005-02-01
申请号：US10246558
申请日：2002-09-19
申请人： Eugene D. Thorsett , Warren J. Porter , Jeffrey S. Nissen , Lee H. Latimer , James E. Audia , James Droste
发明人： Eugene D. Thorsett , Warren J. Porter , Jeffrey S. Nissen , Lee H. Latimer , James E. Audia , James Droste
IPC分类号： A61K31/4245 , A61K31/41 , C07D271/06
CPC分类号： A61K31/4245
摘要： Disclosed are compounds which inhibit β-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits β-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.
摘要翻译： 公开了抑制β-淀粉样蛋白肽释放和/或其合成的化合物，因此具有治疗阿尔茨海默病的效用。 还公开了包含抑制β-淀粉样蛋白肽释放和/或其合成的化合物的药物组合物以及用这种药物组合物预防性和治疗性地治疗阿尔茨海默病的方法。
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34.发明授权N-(aryl/heteroaryl) amino acid derivatives pharmaceutical compositions comprising same and methods for inhibiting .beta.-amyloid peptide release and/or its synthesis by use of such compounds 失效包含其的N-（芳基/杂芳基）氨基酸衍生物药物组合物和通过使用这些化合物抑制β-淀粉样蛋白肽释放和/或其合成的方法
公开(公告)号：US06096782A
公开(公告)日：2000-08-01
申请号：US976191
申请日：1997-11-21
申请人： James E. Audia , Beverly K. Folmer , Varghese John , Lee H. Latimer , Jeffrey S. Nissen , Warren J. Porter , Eugene D. Thorsett , Jing Wu
发明人： James E. Audia , Beverly K. Folmer , Varghese John , Lee H. Latimer , Jeffrey S. Nissen , Warren J. Porter , Eugene D. Thorsett , Jing Wu
IPC分类号： A61K31/00 , A61K31/198 , A61K31/223 , C07C237/08 , C07C237/10 , C07C237/12 , C07C271/22 , C07D209/20 , C07D215/38 , C07D233/54 , C07D233/61 , C07D277/62 , C07D277/82 , A01N37/20 , A01N43/50 , C07C229/24
CPC分类号： C07D215/38 , A61K31/00 , A61K31/198 , A61K31/223 , C07C237/08 , C07C237/10 , C07C237/12 , C07C271/22 , C07D209/20 , C07D233/64 , C07D277/62 , C07D277/82
摘要： Disclosed are compounds which inhibit .beta.-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits .beta.-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.
摘要翻译： 公开了抑制β-淀粉样蛋白肽释放和/或其合成的化合物，因此具有治疗阿尔茨海默氏病的效用。 还公开了包含抑制β-淀粉样蛋白肽释放和/或其合成的化合物的药物组合物以及预防和治疗这些药物组合物的阿尔茨海默氏病的方法。
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35.发明授权Biological reagents and methods for determining the mechanism in the generation of &bgr;-amyloid peptide 失效用于确定β-淀粉样蛋白肽生成机制的生物试剂和方法公开(公告)号：US06486350B1
公开(公告)日：2002-11-26
申请号：US09408283
申请日：1999-09-29
申请人： James E. Audia , Paul A. Hyslop , Jeffrey S. Nissen , Richard C. Thompson , Jay S. Tung , Laura I. Tanner
发明人： James E. Audia , Paul A. Hyslop , Jeffrey S. Nissen , Richard C. Thompson , Jay S. Tung , Laura I. Tanner
IPC分类号： C07C23305
CPC分类号： C07C235/34 , C07C271/16 , C07C271/20 , C07K5/06191 , G01N33/6896
摘要： Disclosed are biological reagents which comprise compounds that inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in determining the cellular mechanism involved in the generation of &bgr;-amyloid peptide.
摘要翻译： 公开了包含抑制β-淀粉样蛋白肽释放和/或其合成的化合物的生物试剂，因此具有用于确定参与β-淀粉样蛋白肽生成的细胞机制。
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公开(公告)号：US6090945A
公开(公告)日：2000-07-18
申请号：US187066
申请日：1998-11-05
申请人： James E. Audia , David L. Nelson
发明人： James E. Audia , David L. Nelson
IPC分类号： A61K31/40 , A61K31/403 , A61K31/404 , A61K31/405 , A61K31/435 , A61K31/44 , A61K31/475 , A61P1/00 , A61P1/10 , A61P13/02 , A61P15/00 , A61P25/04 , A61P25/18 , A61P25/20 , A61P25/24 , A61P25/26 , C07D209/14 , C07D209/60 , C07D211/72 , C07D471/04
CPC分类号： C07D471/04 , C07D209/14 , C07D209/60
摘要： The present invention provides novel tetrahydro-beta-carboline compounds having useful central nervous system activity. Further, there is provided 3-ethanamine and 3-ethanamine related compounds which are useful intermediates and have beneficial central nervous system activity. The invention provides formulations and methods for using the novel tetrahydro-beta-carboline and related compounds.
摘要翻译： 本发明提供具有有用的中枢神经系统活性的新颖的四氢-β-咔啉化合物。 此外，提供了3-乙胺和3-乙胺相关的化合物，其是有用的中间体并具有有益的中枢神经系统活性。 本发明提供了使用新型四氢-β-咔啉及相关化合物的配方和方法。
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公开(公告)号：US5861409A
公开(公告)日：1999-01-19
申请号：US835774
申请日：1997-04-08
申请人： James E. Audia , Stephen Richard Baker , Jesus Ezquerra Carrera , Carlos Lamas Peteira , Concepcion Pedregal Tercero
发明人： James E. Audia , Stephen Richard Baker , Jesus Ezquerra Carrera , Carlos Lamas Peteira , Concepcion Pedregal Tercero
IPC分类号： C07D471/04 , A61K31/44
CPC分类号： C07D471/04
摘要： The present invention provides novel tetrahydro-beta-carboline compounds having useful central nervous system activity. Further, there is provided tetrahydro-beta-carboline related compounds which are useful intermediates and have beneficial central nervous system activity. The invention provides formulations and methods for using the novel tetrahydro-beta-carboline and related compounds. Such compounds are particularly useful for the modulation of a 5-HT.sub.2B receptor.
摘要翻译： 本发明提供具有有用的中枢神经系统活性的新颖的四氢-β-咔啉化合物。 此外，提供了四氢-β-咔啉相关化合物，其是有用的中间体并具有有益的中枢神经系统活性。 本发明提供了使用新型四氢-β-咔啉及相关化合物的配方和方法。 这些化合物特别可用于5-HT 2B受体的调节。
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公开(公告)号：US5710163A
公开(公告)日：1998-01-20
申请号：US683750
申请日：1996-07-17
申请人： James E. Audia
发明人： James E. Audia
IPC分类号： A61K31/47 , A61K31/435 , A61K31/473 , A61P13/08 , A61P17/00 , A61P17/08 , A61P17/10 , A61P17/14 , A61P35/00 , A61P43/00 , C07C45/00 , C07C45/51 , C07C45/56 , C07C49/697 , C07C49/737 , C07C49/747 , C07C49/755 , C07C205/45 , C07C229/46 , C07D211/00 , C07D221/06 , C07D221/10 , C12N9/99 , C07D215/227 , C07D215/12
CPC分类号： C07D221/10 , C07C227/16 , C07C229/46 , C07C41/16 , C07C45/00 , C07C45/513 , C07C45/562 , C07C49/697 , C07C49/747 , C07C49/755 , C07C59/255 , C07C2102/10 , C07C2103/70
摘要： This invention relates to hexa- and octahydrobenzo�f!quinolin-3-ones, pharmaceutical formulations containing those compounds and methods of their use as steroid 5.alpha.-reductase inhibitors.
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公开(公告)号：US5495021A
公开(公告)日：1996-02-27
申请号：US223884
申请日：1994-04-06
IPC分类号： A61K31/47 , A61K31/435 , A61K31/473 , A61P13/08 , A61P17/00 , A61P17/08 , A61P17/10 , A61P17/14 , A61P35/00 , A61P43/00 , C07C45/00 , C07C45/51 , C07C45/56 , C07C49/697 , C07C49/737 , C07C49/747 , C07C49/755 , C07C205/45 , C07C229/46 , C07D211/00 , C07D221/06 , C07D221/10 , C12N9/99 , C07D215/227 , C07D215/38
CPC分类号： C07D221/10 , C07C227/16 , C07C229/46 , C07C41/16 , C07C45/00 , C07C45/513 , C07C45/562 , C07C49/697 , C07C49/747 , C07C49/755 , C07C59/255 , C07C2102/10 , C07C2103/70
摘要： This invention relates to hexa- and octahydrobenzo[f]quinolin-3-ones, pharmaceutical formulations containing those compounds and methods of their use as steroid 5.alpha.-reductase inhibitors.
摘要翻译： 本发明涉及六氢和八氢苯并[f]喹啉-3-酮，含有这些化合物的药物制剂及其用作类固醇5α-还原酶抑制剂的方法。
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公开(公告)号：US08796261B2
公开(公告)日：2014-08-05
申请号：US13309646
申请日：2011-12-02
申请人： Brian K. Albrecht , James E. Audia , Alexandre Côté , Victor S. Gehling , Jean-Christophe Harmange , Michael C. Hewitt , Yves Leblanc , Christopher G. Nasveschuk , Alexander M. Taylor , Rishi G. Vaswani
发明人： Brian K. Albrecht , James E. Audia , Alexandre Côté , Victor S. Gehling , Jean-Christophe Harmange , Michael C. Hewitt , Yves Leblanc , Christopher G. Nasveschuk , Alexander M. Taylor , Rishi G. Vaswani
IPC分类号： A61K31/55 , C07D498/04 , C07D498/20 , C07K14/47 , C07D498/14 , C07D498/22
CPC分类号： C07D498/04 , A61K31/424 , A61K31/55 , C07D498/14 , C07D498/20 , C07D498/22 , C07K14/4702
摘要： The present invention relates to compounds useful as inhibitors of bromodomain-containing proteins. The invention also provides pharmaceutically acceptable compositions comprising compounds of the present invention and methods of using said compositions in the treatment of various disorders.
摘要翻译： 本发明涉及可用作含溴结构域蛋白质的抑制剂的化合物。 本发明还提供包含本发明化合物的药学上可接受的组合物和使用所述组合物治疗各种疾病的方法。
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