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公开(公告)号：US06916784B2
公开(公告)日：2005-07-12
申请号：US10378004
申请日：2003-02-27
Applicant: Frederick J. Burkhardt , Manuel Debono , Jeffrey S. Nissen , William W. Turner, Jr.
Inventor： Frederick J. Burkhardt , Manuel Debono , Jeffrey S. Nissen , William W. Turner, Jr.
Abstract: Provided are compounds of the formula (1): wherein R′ is hydrogen, methyl or NH2C(O)CH2—; R″ and R′″ are independently methyl or hydrogen; R adn Ry are independently hydroxy or hydrogen; R1 is hydroxy, hydrogen, or hydroxysulfonyloxy; R7 is hydroxy, hydrogen, hydroxysulfonyloxy or phosphonooxy; R2 is a novel acyl side chain. Also provided are novel formulations, methods of inhibiting fungal and parasitic activity, and a process for preparing dideoxy (R═H) forms of the compounds.
Abstract translation: 提供式（1）的化合物：其中R'是氢，甲基或NH 2 C（O）CH 2 - ; R“和R”'独立地是甲基或氢; R adn R y独立地是羟基或氢; R 1是羟基，氢或羟基磺酰氧基; R 7是羟基，氢，羟基磺酰氧基或膦酰氧基; R 2是新的酰基侧链。 还提供了新的制剂，抑制真菌和寄生虫活性的方法，以及制备化合物的二脱氧（R-H）形式的方法。
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公开(公告)号：US06559141B2
公开(公告)日：2003-05-06
申请号：US09915564
申请日：2001-07-27
Applicant: Jing Wu , Jay S. Tung , Eugene D. Thorsett , Michael A. Pleiss , Jeffrey S. Nissen , R. Jeffrey Neitz , Lee H. Latimer , Varghese John , Stephen Freedman , Thomas C. Britton , James A. Audia , Jon K. Reel , Thomas E. Mabry , Bruce A. Dressman , Cynthia L. Cwi , James J. Droste , Steven S. Henry , Stacey L. McDaniel , William Leonard Scott , Russell D. Stucky , Warren J. Porter
Inventor： Jing Wu , Jay S. Tung , Eugene D. Thorsett , Michael A. Pleiss , Jeffrey S. Nissen , R. Jeffrey Neitz , Lee H. Latimer , Varghese John , Stephen Freedman , Thomas C. Britton , James A. Audia , Jon K. Reel , Thomas E. Mabry , Bruce A. Dressman , Cynthia L. Cwi , James J. Droste , Steven S. Henry , Stacey L. McDaniel , William Leonard Scott , Russell D. Stucky , Warren J. Porter
IPC: A61K3155
CPC classification number: C07D471/04 , A61K31/40 , A61K31/4015 , A61K31/445 , A61K31/5513 , A61K38/05 , C07C237/22 , C07C2603/32 , C07D223/18 , C07D307/33 , C07D311/76 , C07D471/06 , C07D471/08
Abstract: 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.
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3.发明授权N-(aryl/heteroaryl/alkylacetyl) amino acid amides, 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/烷基乙酰基）氨基酸酰胺，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：US06262302B1
公开(公告)日：2001-07-17
申请号：US09398211
申请日：1999-09-17
Applicant: Jing Wu , Jay S. Tung , Jeffrey S. Nissen , Thomas E. Mabry , Lee H. Latimer , Clark N. Eid , James E. Audia
Inventor： Jing Wu , Jay S. Tung , Jeffrey S. Nissen , Thomas E. Mabry , Lee H. Latimer , Clark N. Eid , James E. Audia
IPC: C07C22938
CPC classification number: A61K31/277 , A61K31/198 , A61K31/223 , A61K31/44
Abstract: 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.
Abstract translation: 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
Applicant: 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
Inventor： 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: A01N3712
CPC classification number: C07K5/06191 , A61K31/00 , A61K38/05 , A61K38/06 , C07K5/06078
Abstract: 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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公开(公告)号：US5846982A
公开(公告)日：1998-12-08
申请号：US862208
申请日：1997-05-22
Applicant: James E. Audia , Daniel J. Koch , Thomas E. Mabry , Jeffrey S. Nissen , Vincent P. Rocco , Yao-Chang Xu
Inventor： James E. Audia , Daniel J. Koch , Thomas E. Mabry , Jeffrey S. Nissen , Vincent P. Rocco , Yao-Chang Xu
IPC: A61K31/00 , A61K31/44 , A61K31/4427 , A61K31/4433 , A61K31/4436 , A61K31/4439 , A61K31/445 , A61K31/4465 , A61K31/4523 , A61K31/454 , A61P25/04 , A61P43/00 , C07D211/68 , C07D333/58 , C07D401/04 , C07D401/14 , C07D409/04 , C07D409/14 , C07D417/14 , A61K31/43
CPC classification number: C07D401/04 , C07D401/14 , C07D409/04 , C07D409/14 , C07D417/14
Abstract: This invention provides compounds and a method for the inhibition of serotonin reuptake in mammals.
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Patent Agency Ranking
公开(公告)号：US07153847B2
公开(公告)日：2006-12-26
申请号：US10733877
申请日：2003-12-12
Applicant: Jing Wu , Jay S. Tung , Jeffrey S. Nissen , R. Jeffrey Neitz , James A. Audia , Thomas E. Mabry
Inventor： Jing Wu , Jay S. Tung , Jeffrey S. Nissen , R. Jeffrey Neitz , James A. Audia , Thomas E. Mabry
IPC: C07D487/00 , C07D491/00 , A61K31/55
CPC classification number: C07D471/04 , A61K31/40 , A61K31/4015 , A61K31/445 , A61K31/5513 , A61K38/05 , C07C237/22 , C07C2603/32 , C07D223/18 , C07D307/33 , C07D311/76 , C07D471/06 , C07D471/08
Abstract: 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.
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7.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
Applicant: Jing Wu , Eugene D. Thorsett , Jeffrey S. Nissen , Thomas E. Mabry , Lee H. Latimer , Varghese John , Lawrence Y. Fang , James E. Audia
Inventor： Jing Wu , Eugene D. Thorsett , Jeffrey S. Nissen , Thomas E. Mabry , Lee H. Latimer , Varghese John , Lawrence Y. Fang , James E. Audia
IPC: A61K3138
CPC classification number: A61K31/198 , A61K31/223 , A61K31/277
Abstract: 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.
Abstract translation: 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：US06667305B1
公开(公告)日：2003-12-23
申请号：US10336745
申请日：2003-01-06
Applicant: Jing Wu , Jay S. Tung , Eugene D. Thorsett , Michael A. Pleiss , Jeffrey S. Nissen , R. Jeffrey Neitz , Lee H. Latimer , Varghese John , Stephen Freedman , Thomas C. Britton , James A. Audia , Jon K. Reel , Thomas E. Mabry , Bruce A. Dressman , Cynthia L. Cwi , James J. Droste , Steven S. Henry , Stacey L. McDaniel , William Leonard Scott , Russell D. Stucky , Warren J. Porter
Inventor： Jing Wu , Jay S. Tung , Eugene D. Thorsett , Michael A. Pleiss , Jeffrey S. Nissen , R. Jeffrey Neitz , Lee H. Latimer , Varghese John , Stephen Freedman , Thomas C. Britton , James A. Audia , Jon K. Reel , Thomas E. Mabry , Bruce A. Dressman , Cynthia L. Cwi , James J. Droste , Steven S. Henry , Stacey L. McDaniel , William Leonard Scott , Russell D. Stucky , Warren J. Porter
IPC: A61P2528
CPC classification number: C07D471/04 , A61K31/40 , A61K31/4015 , A61K31/445 , A61K31/5513 , A61K38/05 , C07C237/22 , C07C2603/32 , C07D223/18 , C07D307/33 , C07D311/76 , C07D471/06 , C07D471/08
Abstract: 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.
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9.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
Applicant: Jing Wu , Eugene D. Thorsett , Jeffrey S. Nissen , Thomas E. Mabry , Lee H. Latimer , Varghese John , Lawrence Y. Fang , James E. Audia
Inventor： Jing Wu , Eugene D. Thorsett , Jeffrey S. Nissen , Thomas E. Mabry , Lee H. Latimer , Varghese John , Lawrence Y. Fang , James E. Audia
IPC: A61K3144
CPC classification number: A61K31/198 , A61K31/223 , A61K31/277
Abstract: 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.
Abstract translation: 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：US06579867B2
公开(公告)日：2003-06-17
申请号：US09915379
申请日：2001-07-27
Applicant: Jing Wu , Jay S. Tung , Eugene D. Thorsett , Michael A. Pleiss , Jeffrey S. Nissen , Jeffrey Neitz , Lee H. Latimer , Varghese John , Stephen Freedman , Thomas C. Britton , James A. Audia , Jon K. Reel , Thomas E. Mabry , Bruce A. Dressman , James J. Droste , Steven S. Henry , Stacey L. McDaniel , Russell D. Stucky , Warren J. Porter
Inventor： Jing Wu , Jay S. Tung , Eugene D. Thorsett , Michael A. Pleiss , Jeffrey S. Nissen , Jeffrey Neitz , Lee H. Latimer , Varghese John , Stephen Freedman , Thomas C. Britton , James A. Audia , Jon K. Reel , Thomas E. Mabry , Bruce A. Dressman , James J. Droste , Steven S. Henry , Stacey L. McDaniel , Russell D. Stucky , Warren J. Porter
IPC: A61K3155
CPC classification number: C07D471/04 , A61K31/40 , A61K31/4015 , A61K31/445 , A61K31/5513 , A61K38/05 , C07C237/22 , C07C2603/32 , C07D223/18 , C07D307/33 , C07D311/76 , C07D471/06 , C07D471/08
Abstract: 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.
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