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11. 发明授权

US5385923A 2-saccharinylmethyl aryl and aryloxy acetates useful as proteolytic enzyme inhibitors 失效
标题翻译： 2-糖基甲基芳基和芳氧基乙酸酯可用作蛋白水解酶抑制剂
公开(公告)号：US5385923A
公开(公告)日：1995-01-31
申请号：US109849
申请日：1993-08-20
申请人： Lee H. Latimer , Richard P. Dunlap
发明人： Lee H. Latimer , Richard P. Dunlap
IPC分类号： A61K9/48 , A61K31/425 , A61K31/428 , A61K31/44 , A61P1/00 , A61P11/00 , A61P35/00 , A61P43/00 , C07D275/06 , C07D417/04 , C07D417/12 , C07D513/04 , C07D275/04
CPC分类号： C07D275/06 , A61K31/425 , C07D513/04
摘要： 4-R.sup.4 --R.sup.5 -2-Saccharinylmethyl aryl and aryloxy acetates, useful in the treatment of degenerative diseases, are prepared by reacting a 4-R.sup.4 --R.sup.5 -2-halomethylsaccharin with an aryl or aryloxyacetic acid in the presence of an acid-acceptor.
摘要翻译：可用于治疗退行性疾病的4-R4-R5-2-糖基甲基芳基和芳氧基乙酸酯通过在酸 - 受体存在下使4-R 4 -R 5 - 2-卤代甲基糖精与芳基或芳氧基乙酸反应来制备。

12. 发明授权

US5382682A Nitroanilides and their preparation 失效
标题翻译：硝基酰苯胺及其制备方法
公开(公告)号：US5382682A
公开(公告)日：1995-01-17
申请号：US920573
申请日：1992-08-18
申请人： Paul R. Buckland , Lee H. Latimer
发明人： Paul R. Buckland , Lee H. Latimer
IPC分类号： C07C231/12 , C07C233/15 , C07C233/25 , C07C233/66 , C07C233/75
CPC分类号： C07C233/75 , C07C231/12 , C07C233/25
摘要： Novel aryloxy-nitroanilides of formula ##STR1## wherein R is alkyl from 1 to 5 carbon atoms or unsubstituted or substituted aryl of from 6 to 10 carbon atoms; one of R.sup.1 and R.sup.2 is a hydrogen atom and the other is aryloxy, wherein the aryl is unsubstituted or substituted with one or more alkyl of from 1 to 10 carbon atoms, with the proviso that when R is methyl, R.sup.1 may not be unsubstituted phenoxy and when R is 2-hydroxy-5-chlorophenyl, R.sup.2 may not be unsubstituted or chloro or methyl substituted phenoxy, and a method of preparing them. The compounds are suitable as intermediates for the preparation of anilines, required in the preparation of useful photographic and pharmaceutical compounds.
摘要翻译： PCT No.PCT / EP91 / 02417 371日期1982年8月18日 102（e）日期1992年8月18日PCT 1991年12月16日PCT PCT。公开号WO92 / 11230 日期：1992年7月9日。新颖的式（Ia）的芳氧基 - 硝基酰苯胺，其中R是1至5个碳原子的烷基或6至10个碳原子的未取代或取代的芳基; R1和R2中的一个是氢原子，另一个是芳氧基，其中芳基是未取代的或被一个或多个1-10个碳原子的烷基取代，条件是当R是甲基时，R 1可以不是未被取代的苯氧基当R是2-羟基-5-氯苯基时，R 2可以不是未取代的或氯或甲基取代的苯氧基，以及它们的制备方法。该化合物适合用作制备有用的照相和药物化合物所需的苯胺的中间体。

13. 发明授权

US5376653A 2-saccharinylmethyl heterocyclic carboxylates useful as proteolytic enzyme inhibitors 失效
标题翻译：可用作蛋白水解酶抑制剂的2-糖基甲基杂环羧酸盐
公开(公告)号：US5376653A
公开(公告)日：1994-12-27
申请号：US109411
申请日：1993-08-19
申请人： Richard P. Dunlap , Lee H. Latimer , Chakrapani Subramanyam
发明人： Richard P. Dunlap , Lee H. Latimer , Chakrapani Subramanyam
IPC分类号： A61K31/425 , A61K9/20 , A61K9/48 , A61K31/428 , A61K31/44 , A61P1/00 , A61P11/00 , A61P35/00 , A61P43/00 , C07D275/06 , C07D417/12 , C07D275/04
CPC分类号： C07D417/12
摘要： 4-R.sup.4 -R.sup.5 -2-Saccharinylmethyl heterocyclic carboxylates, useful in the treatment of degenerative diseases, are prepared by reacting a 4-R.sup.4 -R.sup.5 -2-halomethylsaccharin with either a heterocyclic carboxylic acid in the presence of an acid-acceptor or the alkali metal salt of a heterocyclic carboxylic acid.
摘要翻译：可用于治疗退行性疾病的4-R4-R5-2-糖基甲基杂环羧酸盐通过在酸受体存在下使4-R 4 -R 5 -2-卤代甲基糖精与杂环羧酸反应来制备，杂环羧酸的碱金属盐。

14. 发明授权

US07759382B2 Acylated amino acid amidyl pyrazoles and related compounds 失效
标题翻译：酰化氨基酸氨基吡唑和相关化合物
公开(公告)号：US07759382B2
公开(公告)日：2010-07-20
申请号：US10559823
申请日：2004-06-04
申请人： Jay S. Tung , Lee H. Latimer , Jing Wu , Albert Garofalo , Michael A. Pleiss , Darren Dressen , Ashley Guinn , Scott A. Jenkins , Jennifer Sealy , John Tucker , David W. G. Wone
发明人： Jay S. Tung , Lee H. Latimer , Jing Wu , Albert Garofalo , Michael A. Pleiss , Darren Dressen , Ashley Guinn , Scott A. Jenkins , Jennifer Sealy , John Tucker , David W. G. Wone
IPC分类号： A61K31/415 , C07D231/10
CPC分类号： C07D231/40 , C07D401/04 , C07D401/06 , C07D401/12 , C07D405/04 , C07D405/12 , C07D409/12
摘要： This invention is directed to acylated amino acid amidyl pyrazoles and related compounds of Formula I. The invention is also directed to a pharmaceutical formation comprising such compound or in a pharmaceutically acceptable salt form thereof. The invention is further directed to a method for inhibiting β-amyloid peptide release and/or synthesis, a method for inhibiting γ-secretase activity, and a method for treating neurological disorders associated with β-amyloid peptide production. The method comprises administering to a host a pharmaceutical formulation comprising an effective amount of a compound of Formula I. The compounds of Formula I are useful in the prevention and treatment of Alzheimer's disease.
摘要翻译：本发明涉及酰化氨基酸酰氨基吡唑和式I的相关化合物。本发明还涉及包含这种化合物或其药学上可接受的盐形式的药物组合物。本发明进一步涉及一种抑制β-淀粉样蛋白肽释放和/或合成的方法，一种抑制γ-分泌酶活性的方法，以及用于治疗与β-淀粉样蛋白肽生产相关的神经障碍的方法。该方法包括向宿主施用包含有效量的式I化合物的药物制剂。式I化合物可用于预防和治疗阿尔茨海默氏病。

15. 发明授权

US06861558B2 Methods and compounds for inhibiting β-amyloid peptide release and/or its synthesis 失效
公开(公告)号：US06861558B2
公开(公告)日：2005-03-01
申请号：US10309569
申请日：2002-12-03
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
IPC分类号： A61K31/00 , A61K38/05 , A61K38/06 , C07K5/06 , C07K5/065 , C02C233/00
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.

16. 发明授权

US06849650B2 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
标题翻译：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。

17. 发明授权

US06635632B1 Cycloalkyl, lactam, lactone and related compounds, pharmaceutical compositions comprising same, and methods for inhibiting &bgr;-amyloid peptide release and/or its synthesis by use of such compounds 失效
公开(公告)号：US06635632B1
公开(公告)日：2003-10-21
申请号：US08996422
申请日：1997-12-22
申请人： 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
发明人： 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分类号： A61K3155
CPC分类号： 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
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.

18. 发明授权

US06632811B2 Cycloalkyl, lactam, lactone and related compounds, pharmaceutical compositions comprising same, and methods for inhibiting &bgr;-amyloid peptide release and/or its synthesis by use of such compounds 失效
标题翻译：环烷基，内酰胺，内酯和相关化合物，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：US06632811B2
公开(公告)日：2003-10-14
申请号：US09915342
申请日：2001-07-27
申请人： 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
发明人： 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分类号： A61K3155
CPC分类号： 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
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，以及预防和治疗阿尔茨海默病的方法，该药物组合物均为该药物组合物。

19. 发明授权

US06544978B2 Cycloalkyl, lactam, lactone and related compounds, pharmaceutical compositions comprising same, and methods for inhibiting &bgr;-amyloid peptide release and/or its synthesis by use of such compounds 失效
公开(公告)号：US06544978B2
公开(公告)日：2003-04-08
申请号：US09915480
申请日：2001-07-27
申请人： 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
发明人： 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分类号： A61K3155
CPC分类号： 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
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.

20. 发明授权

US06541466B2 Cycloalkyl, lactam, lactone and related compounds, pharmaceutical compositions comprising same, and methods for inhibiting &bgr;-amyloid peptide release and/or its synthesis by use of such compounds 失效
公开(公告)号：US06541466B2
公开(公告)日：2003-04-01
申请号：US09915362
申请日：2001-07-27
申请人： 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
发明人： 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分类号： A61K3155
CPC分类号： 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
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.

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