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61.发明授权Compounds for inhibiting &bgr;-amyloid peptide release and/or its synthesis 失效用于抑制β-淀粉样蛋白肽释放和/或其合成的化合物公开(公告)号：US06476263B1
公开(公告)日：2002-11-05
申请号：US09826412
申请日：2001-04-03
申请人： Jing Wu , Jay S. Tung , Eugene D. Thorsett , Jon K. Reel , Warren J. Porter , Jeffrey S. Nissen , Thomas E. Mabry , Lee H. Latimer , Varghese John , Beverly K. Folmer , James J. Droste , Thomas C. Britton , James E. Audia
发明人： Jing Wu , Jay S. Tung , Eugene D. Thorsett , Jon K. Reel , Warren J. Porter , Jeffrey S. Nissen , Thomas E. Mabry , Lee H. Latimer , Varghese John , Beverly K. Folmer , James J. Droste , Thomas C. Britton , James E. Audia
IPC分类号： C07C23300
CPC分类号： C07K5/06191 , A61K31/00 , A61K38/05 , A61K38/06 , C07K5/06078
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.
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-淀粉样肽释放和/或其合成的化合物的药物组合物。
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公开(公告)号：US06333351B1
公开(公告)日：2001-12-25
申请号：US09303655
申请日：1999-05-03
申请人： Jing Wu , Eugene D. Thorsett , Jeffrey S. Nissen , Thomas E. Mabry , Lee H. Latimer , Varghese John , Lawrence Y. Fang , James E. Audia
发明人： Jing Wu , Eugene D. Thorsett , Jeffrey S. Nissen , Thomas E. Mabry , Lee H. Latimer , Varghese John , Lawrence Y. Fang , James E. Audia
IPC分类号： C07C22906
CPC分类号： A61K31/198 , A61K31/223 , A61K31/277
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 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.
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63.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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64.发明授权Methods and compounds for inhibiting β-amyloid peptide release and/or its synthesis 失效用于抑制β-淀粉样蛋白肽释放和/或其合成的方法和化合物公开(公告)号：US06888022B2
公开(公告)日：2005-05-03
申请号：US09789487
申请日：2001-02-20
申请人： James E. Audia , Thomas C. Britton , James J. Droste , Beverly K. Folmer , George W. Huffman , Varghese John , Lee H. Latimer , Thomas E. Mabry , Jeffrey S. Nissen , Warren J. Porter , Jon K. Reel , Eugene D. Thorsett , Jay S. Tung , Jing Wu , Clark Norman Eid , William Leonard Scott
发明人： James E. Audia , Thomas C. Britton , James J. Droste , Beverly K. Folmer , George W. Huffman , Varghese John , Lee H. Latimer , Thomas E. Mabry , Jeffrey S. Nissen , Warren J. Porter , Jon K. Reel , Eugene D. Thorsett , Jay S. Tung , Jing Wu , Clark Norman Eid , William Leonard Scott
CPC分类号： C07K5/06191 , A61K31/00 , A61K31/4015 , A61K31/405 , A61K31/445 , A61K31/47 , A61K38/05 , A61K38/06 , C07K5/06078
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 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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公开(公告)号：US06211235B1
公开(公告)日：2001-04-03
申请号：US09164448
申请日：1998-09-30
申请人： Jing Wu , Jay S. Tung , Eugene D. Thorsett , Jon K. Reel , Warren J. Porter , Jeffrey S. Nissen , Thomas E. Mabry , Lee H. Latimer , Varghese John , Beverly K. Folmer , James J. Droste , Thomas C. Britton , James E. Audia
发明人： Jing Wu , Jay S. Tung , Eugene D. Thorsett , Jon K. Reel , Warren J. Porter , Jeffrey S. Nissen , Thomas E. Mabry , Lee H. Latimer , Varghese John , Beverly K. Folmer , James J. Droste , Thomas C. Britton , James E. Audia
IPC分类号： A01N3712
CPC分类号： C07K5/06191 , A61K31/00 , A61K38/05 , A61K38/06 , C07K5/06078
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.
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66.发明授权N-(aryl/heteroarylacetyl) amino acid esters, 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/杂芳基乙酰基）氨基酸酯，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：US06767918B2
公开(公告)日：2004-07-27
申请号：US10314221
申请日：2002-12-09
申请人： Jing Wu , Eugene D. Thorsett , Jeffrey S. Nissen , Thomas E. Mabry , Lee H. Latimer , Varghese John , Lawrence Y. Fang , James E. Audia
发明人： Jing Wu , Eugene D. Thorsett , Jeffrey S. Nissen , Thomas E. Mabry , Lee H. Latimer , Varghese John , Lawrence Y. Fang , James E. Audia
IPC分类号： A61K3138
CPC分类号： A61K31/198 , A61K31/223 , A61K31/277
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 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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67.发明授权N-(aryl/heteroarylacety) amino acid esters, 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）氨基酸酯，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：US06642261B2
公开(公告)日：2003-11-04
申请号：US09984834
申请日：2001-10-31
申请人： Jing Wu , Eugene D. Thorsett , Jeffrey S. Nissen , Thomas E. Mabry , Lee H. Latimer , Varghese John , Lawrence Y. Fang , James E. Audia
发明人： Jing Wu , Eugene D. Thorsett , Jeffrey S. Nissen , Thomas E. Mabry , Lee H. Latimer , Varghese John , Lawrence Y. Fang , James E. Audia
IPC分类号： A61K3144
CPC分类号： A61K31/198 , A61K31/223 , A61K31/277
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 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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68.发明授权N(aryl/heteroarylacetyl) amino acid esters, 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/杂芳基乙酰基）氨基酸酯，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：US06313152B1
公开(公告)日：2001-11-06
申请号：US09390692
申请日：1999-09-07
申请人： Jing Wu , Eugene D. Thorsett , Jeffrey S. Nissen , Thomas E. Mabry , Lee H. Latimer , Varghese John , Lawrence Y. Fang , James E. Audia
发明人： Jing Wu , Eugene D. Thorsett , Jeffrey S. Nissen , Thomas E. Mabry , Lee H. Latimer , Varghese John , Lawrence Y. Fang , James E. Audia
IPC分类号： A61K3144
CPC分类号： A61K31/198 , A61K31/223 , A61K31/277
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 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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69.发明授权N-(aryl/heteroarylacetyl) amino acid esters, pharmaceutical compositions comprising same, and methods for use 失效N-（芳基/杂芳基乙酰基）氨基酸酯，包含其的药物组合物和使用方法
公开(公告)号：US6117901A
公开(公告)日：2000-09-12
申请号：US976179
申请日：1997-11-21
申请人： Jing Wu , Eugene D. Thorsett , Jeffrey S. Nissen , Thomas E. Mabry , Lee H. Latimer , Varghese John , Lawrence Y. Fang , James E. Audia
发明人： Jing Wu , Eugene D. Thorsett , Jeffrey S. Nissen , Thomas E. Mabry , Lee H. Latimer , Varghese John , Lawrence Y. Fang , James E. Audia
IPC分类号： A61K31/198 , A61K31/223 , A61K31/277 , A61K31/16
CPC分类号： A61K31/198 , A61K31/223 , A61K31/277
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 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治疗方法。
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公开(公告)号：US11325904B2
公开(公告)日：2022-05-10
申请号：US14235405
申请日：2012-08-01
申请人： Varghese John , Dale E. Bredesen
发明人： Varghese John , Dale E. Bredesen
IPC分类号： C07D453/02 , C07D451/12 , A61K31/439 , A61K31/444 , A61K45/06
摘要： In various embodiments, compositions and methods are provided for treatment and/or prevention of amyloidogenic diseases. In certain embodiments, the methods entail administering an effective amount of a tropinol ester to a subject in need thereof for prophylactic or therapeutic effect. The methods are particularly useful for prophylactic and therapeutic treatment of Alzheimer's disease. In certain embodiments, methods of reducing the risk, lessening the severity, or delaying the progression or onset of a disease characterized by beta-amyloid deposits in the brain of a mammal are also provided. In certain embodiments, methods of directly or indirectly inhibiting the C-terminal cleavage of APP resulting in the formation of APP-C31 peptide and APPneo (AP-P664) in a mammal are provided.
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