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.

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。

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.

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.

公开(公告)号：US06525026B2

公开(公告)日：2003-02-25

申请号：US09987900

申请日：2001-11-16

申请人： Eugene D. Thorsett ,  Christopher M. Semko ,  Dimitrios Sarantakis ,  Michael A. Pleiss ,  Anthony Kreft ,  Andrei W. Konradi ,  Francine S. Grant ,  Darren B. Dressen ,  Susan Ashwell ,  Reinhardt Bernhard Baudy ,  Louis John Lombardo

发明人： Eugene D. Thorsett ,  Christopher M. Semko ,  Dimitrios Sarantakis ,  Michael A. Pleiss ,  Anthony Kreft ,  Andrei W. Konradi ,  Francine S. Grant ,  Darren B. Dressen ,  Susan Ashwell ,  Reinhardt Bernhard Baudy ,  Louis John Lombardo

IPC分类号： C07K506

CPC分类号： A61K31/397 ,  A61K31/4015 ,  A61K31/404 ,  A61K31/495 ,  A61K31/54 ,  A61K38/00 ,  C07K5/0215 ,  C07K5/06026 ,  C07K5/06139 ,  C07K5/06165 ,  C07K5/06191

摘要： Disclosed are compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.

公开(公告)号：US06479492B1

公开(公告)日：2002-11-12

申请号：US09489378

申请日：2000-01-21

申请人： Andrei W. Konradi ,  Michael A. Pleiss ,  Eugene D. Thorsett ,  Susan Ashwell ,  Dimitrios Sarantakis ,  Gregory S. Welmaker ,  Anthony Kreft ,  Christopher Semko ,  Robert Warren Sullivan ,  Christopher Joseph Soares ,  Kiev Sui Ly ,  Christine M. Tarby

发明人： Andrei W. Konradi ,  Michael A. Pleiss ,  Eugene D. Thorsett ,  Susan Ashwell ,  Dimitrios Sarantakis ,  Gregory S. Welmaker ,  Anthony Kreft ,  Christopher Semko ,  Robert Warren Sullivan ,  Christopher Joseph Soares ,  Kiev Sui Ly ,  Christine M. Tarby

IPC分类号： A61K3153

CPC分类号： A61K31/425 ,  A61K31/41 ,  A61K31/427 ,  A61K31/433 ,  A61K31/44 ,  A61K31/4439 ,  A61K31/445 ,  A61K31/495 ,  A61K31/496 ,  A61K31/4965 ,  A61K31/497 ,  A61K31/50 ,  A61K31/505 ,  A61K31/506 ,  A61K31/53 ,  A61K31/535 ,  A61K31/54 ,  C07D211/58 ,  C07D213/74 ,  C07D213/76 ,  C07D233/88 ,  C07D239/32 ,  C07D239/42 ,  C07D239/47 ,  C07D239/48 ,  C07D239/52 ,  C07D241/20 ,  C07D249/06 ,  C07D251/18 ,  C07D251/48 ,  C07D251/50 ,  C07D251/52 ,  C07D251/54 ,  C07D257/06 ,  C07D285/06 ,  C07D285/10 ,  C07D333/36 ,  C07D333/48 ,  C07D401/04 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/04 ,  C07D413/12 ,  C07D417/12 ,  Y02A50/463 ,  A61K2300/00

摘要： Disclosed are compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.

摘要翻译： 公开了结合VLA-4的化合物。 这些化合物中的某些也抑制白细胞粘附，特别是由VLA-4介导的白细胞粘附。 这样的化合物可用于治疗哺乳动物患者，例如人类例如哮喘，阿尔茨海默氏病，动脉粥样硬化，艾滋病痴呆，糖尿病，炎性肠病，类风湿性关节炎，组织移植，肿瘤转移和心肌缺血等炎性疾病。 化合物也可以用于治疗炎性脑疾病如多发性硬化症。

公开(公告)号：US06291453B1

公开(公告)日：2001-09-18

申请号：US09126091

申请日：1998-07-30

申请人： Susan Ashwell ,  Francine S. Grant ,  Andrei W. Konradi ,  Anthony Kreft ,  Louis John Lombardo ,  Michael A. Pleiss ,  Dimitrios Sarantakis ,  Christopher M. Semko ,  Eugene D. Thorsett

发明人： Susan Ashwell ,  Francine S. Grant ,  Andrei W. Konradi ,  Anthony Kreft ,  Louis John Lombardo ,  Michael A. Pleiss ,  Dimitrios Sarantakis ,  Christopher M. Semko ,  Eugene D. Thorsett

IPC分类号： A61K31541

CPC分类号： C07D401/12 ,  C07D207/48 ,  C07D403/12 ,  C07D417/12

摘要： Disclosed are compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.

摘要翻译： 公开了结合VLA-4的化合物。 这些化合物中的某些也抑制白细胞粘附，特别是由VLA-4介导的白细胞粘附。 这样的化合物可用于治疗哺乳动物患者，例如人类例如哮喘，阿尔茨海默氏病，动脉粥样硬化，艾滋病痴呆，糖尿病，炎性肠病，类风湿性关节炎，组织移植，肿瘤转移和心肌缺血等炎性疾病。 化合物也可以用于治疗炎性脑疾病如多发性硬化症。