公开(公告)号：US06951854B1

公开(公告)日：2005-10-04

申请号：US10951992

申请日：2004-09-29

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: A61K31/40 ,  A61K31/4015 ,  A61K31/445 ,  A61K31/55 ,  A61K38/04 ,  A61K38/05 ,  A61P25/28 ,  C07D223/18 ,  C07D471/04 ,  C07D471/06 ,  C07D471/08

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.

公开(公告)号：US06888022B2

公开(公告)日：2005-05-03

申请号：US09789487

申请日：2001-02-20

Applicant: 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

Inventor： 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: A61K31/00 ,  A61K38/05 ,  A61K38/06 ,  C07K5/06 ,  C07K5/065 ,  C07C229/00

CPC classification number: C07K5/06191 ,  A61K31/00 ,  A61K31/4015 ,  A61K31/405 ,  A61K31/445 ,  A61K31/47 ,  A61K38/05 ,  A61K38/06 ,  C07K5/06078

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 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.

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。

公开(公告)号：US06683075B1

公开(公告)日：2004-01-27

申请号：US10336806

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: A61K3155

CPC classification number: C07D471/04 ,  A61K31/55 ,  C07D223/18 ,  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.

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。

公开(公告)号：US06653303B1

公开(公告)日：2003-11-25

申请号：US10336824

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: 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.

公开(公告)号：US07858642B2

公开(公告)日：2010-12-28

申请号：US12396989

申请日：2009-03-03

Applicant: Varghese John ,  Michel Maillard ,  John Tucker ,  Jose Aquino ,  Barbara Jagodzinska ,  Louis Brogley ,  Jay S. Tung ,  Simeon Bowers ,  Darren Dressen ,  Gary Probst ,  Neerav Shah

Inventor： Varghese John ,  Michel Maillard ,  John Tucker ,  Jose Aquino ,  Barbara Jagodzinska ,  Louis Brogley ,  Jay S. Tung ,  Simeon Bowers ,  Darren Dressen ,  Gary Probst ,  Neerav Shah

IPC: A61K31/427 ,  A61K31/4709 ,  C07D215/58 ,  C07D285/04

CPC classification number: C07D419/12 ,  C07C215/28 ,  C07C215/50 ,  C07C217/30 ,  C07C217/34 ,  C07C217/48 ,  C07C217/52 ,  C07C217/58 ,  C07C225/06 ,  C07C225/20 ,  C07C229/16 ,  C07C229/42 ,  C07C229/60 ,  C07C233/43 ,  C07C237/20 ,  C07C237/30 ,  C07C271/12 ,  C07C311/24 ,  C07C317/28 ,  C07C323/25 ,  C07C323/30 ,  C07C323/32 ,  C07C2601/02 ,  C07C2601/14 ,  C07C2602/04 ,  C07C2602/10 ,  C07C2602/42 ,  C07C2603/18 ,  C07C2603/74 ,  C07D207/323 ,  C07D207/325 ,  C07D213/38 ,  C07D215/42 ,  C07D231/12 ,  C07D231/38 ,  C07D233/54 ,  C07D233/64 ,  C07D233/88 ,  C07D239/42 ,  C07D239/48 ,  C07D249/04 ,  C07D249/06 ,  C07D249/14 ,  C07D257/04 ,  C07D263/34 ,  C07D271/113 ,  C07D275/02 ,  C07D277/42 ,  C07D285/08 ,  C07D285/10 ,  C07D285/135 ,  C07D307/52 ,  C07D309/14 ,  C07D311/74 ,  C07D333/36 ,  C07D335/06 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/04 ,  C07D413/12 ,  C07D417/12 ,  C07D495/04

Abstract: The invention relates to novel compounds and also to methods of treating at least one disease, disorder, or condition associated with amyloidosis using such compounds. Amyloidosis refers to a collection of diseases, disorders, and conditions associated with abnormal deposition of A-beta protein.

Abstract translation: 本发明涉及新化合物，还涉及使用这些化合物治疗与淀粉样变性相关的至少一种疾病，病症或病症的方法。 淀粉样变性是指与A-β蛋白异常沉积相关的疾病，病症和病症的集合。

公开(公告)号：US20100280066A1

公开(公告)日：2010-11-04

申请号：US12833758

申请日：2010-07-09

Applicant: 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

Inventor： 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: A61K31/4725 ,  C07D231/38 ,  C07D401/12 ,  C07D407/04 ,  C07D401/04 ,  C07D403/12 ,  A61P25/28 ,  A61K31/415 ,  A61K31/4439 ,  A61K31/454 ,  C12N5/07

CPC classification number: C07D231/40 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D405/04 ,  C07D405/12 ,  C07D409/12

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US07514408B1

公开(公告)日：2009-04-07

申请号：US09730329

申请日：2000-12-04

Applicant: Varghese John ,  Sukanto Sinha ,  Jay S. Tung

Inventor： Varghese John ,  Sukanto Sinha ,  Jay S. Tung

IPC: C07K7/00

CPC classification number: C07K7/02 ,  G01N33/6896

Abstract: Disclosed is an active, isolated β-secretase enzyme in purified and recombinant form. This enzyme is implicated in the production of amyloid plaque components which accumulate in the brains of individuals afflicted with Alzheimer's disease. Recombinant cells that produce this enzyme either alone or in combination with some of its natural substrates (APP and APPsw) are also disclosed. These compositions are useful for use in methods of selecting compounds that modulate β-secretase. Inhibitors of β-secretase are implicated as therapeutics in the treatment of neurodegenerative diseases, such as Alzheimer's disease.

Abstract translation: 公开了纯化和重组形式的活性，分离的β-分泌酶。 这种酶涉及积聚在患有阿尔茨海默病的个体的脑中的淀粉样蛋白斑块成分的产生。 也公开了单独或与其一些天然底物（APP和APPsw）组合产生该酶的重组细胞。 这些组合物可用于选择调节β-分泌酶的化合物的方法。 β-分泌酶的抑制剂涉及作为治疗神经变性疾病如阿尔茨海默病的治疗剂。

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.

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。

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.