公开(公告)号：US20080015233A1

公开(公告)日：2008-01-17

申请号：US11547994

申请日：2005-04-20

申请人： James Barrow ,  Georgia McGaughey ,  Philippe Nantermet ,  Hemaka Rajapakse ,  Harold Selnick ,  Shaun Stauffer ,  Joseph Vacca ,  Shawn Stachel ,  Craig Coburn ,  Matthew Stanton

发明人： James Barrow ,  Georgia McGaughey ,  Philippe Nantermet ,  Hemaka Rajapakse ,  Harold Selnick ,  Shaun Stauffer ,  Joseph Vacca ,  Shawn Stachel ,  Craig Coburn ,  Matthew Stanton

IPC分类号： A61K31/4439 ,  A61P25/28 ,  C07D401/04 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04

CPC分类号： C07D413/04 ,  C07D401/04 ,  C07D413/14 ,  C07D417/04 ,  C07D417/14

摘要： The present invention is directed to 2,4,6-substituted pyridyl derivative compounds which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.

摘要翻译： 本发明涉及作为β-分泌酶的抑制剂并可用于治疗其中涉及β-分泌酶的疾病如阿尔茨海默氏病的2,4,6-取代的吡啶衍生物化合物。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在治疗涉及β-分泌酶的疾病中的用途。

公开(公告)号：US20070244119A1

公开(公告)日：2007-10-18

申请号：US11578559

申请日：2005-04-15

申请人： James Barrow ,  Georgia McGaughey ,  Philippe Nantermet ,  Hemaka Rajapakse ,  Harold Selnick ,  Shaun Stauffer ,  Craig Coburn

发明人： James Barrow ,  Georgia McGaughey ,  Philippe Nantermet ,  Hemaka Rajapakse ,  Harold Selnick ,  Shaun Stauffer ,  Craig Coburn

IPC分类号： A61K31/4245 ,  A61K31/341 ,  A61K31/433 ,  A61K31/5377 ,  C07D263/30 ,  C07D285/12 ,  C07D413/04 ,  C07D307/02 ,  C07D271/10 ,  C07D253/02 ,  A61K31/4418 ,  A61K31/421

CPC分类号： C07D271/10 ,  C07D249/06 ,  C07D249/08 ,  C07D263/32 ,  C07D263/62 ,  C07D271/06 ,  C07D285/12 ,  C07D307/14 ,  C07D307/42 ,  C07D307/44 ,  C07D307/52 ,  C07D307/54 ,  C07D413/04 ,  C07D413/10 ,  C07D413/12 ,  C07D413/14

摘要： The present invention is directed to 1,3,5-phenyl substituted derivative compounds which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.

摘要翻译： 本发明涉及作为β-分泌酶的抑制剂并可用于治疗其中涉及β-分泌酶的疾病如阿尔茨海默氏病的1,3,5-苯基取代的衍生物化合物。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在治疗涉及β-分泌酶的疾病中的用途。

公开(公告)号：US20070021454A1

公开(公告)日：2007-01-25

申请号：US11487229

申请日：2006-07-14

申请人： Craig Coburn ,  Melissa Egbertson ,  Samuel Graham ,  Georgia McGaughey ,  Shaun Stauffer ,  Hemaka Rajapakse ,  Philippe Nantermet ,  Shawn Stachel ,  Wenjin Yang ,  Wanli Lu ,  Bruce Fahr

发明人： Craig Coburn ,  Melissa Egbertson ,  Samuel Graham ,  Georgia McGaughey ,  Shaun Stauffer ,  Hemaka Rajapakse ,  Philippe Nantermet ,  Shawn Stachel ,  Wenjin Yang ,  Wanli Lu ,  Bruce Fahr

IPC分类号： A61K31/4747 ,  C07D471/10

CPC分类号： C07D471/10

摘要： The present invention is directed to spiropiperidine compounds of formula (I) and tautomers thereof, which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.

摘要翻译： 本发明涉及式（I）的螺哌啶化合物及其互变异构体，其是β-分泌酶的抑制剂，并且其可用于治疗涉及β-分泌酶的疾病，例如阿尔茨海默氏病。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在治疗涉及β-分泌酶的疾病中的用途。

公开(公告)号：US20070197571A1

公开(公告)日：2007-08-23

申请号：US11663388

申请日：2005-10-12

申请人： James Barrow ,  Craig Coburn ,  Melissa Egbertson ,  Georgia McGaughey ,  Melody McWherter ,  Lou Neilson ,  Kenneth Rittle ,  Harold Selnick ,  Shaun Stauffer ,  Zhi-Qiang Yang ,  Wenjin Yang ,  Wanli Lu ,  Bruce Fahr

发明人： James Barrow ,  Craig Coburn ,  Melissa Egbertson ,  Georgia McGaughey ,  Melody McWherter ,  Lou Neilson ,  Kenneth Rittle ,  Harold Selnick ,  Shaun Stauffer ,  Zhi-Qiang Yang ,  Wenjin Yang ,  Wanli Lu ,  Bruce Fahr

IPC分类号： A61K31/4747 ,  C07D471/10

CPC分类号： C07D471/10

摘要： The present invention is directed to spiropiperidine compounds of formula (I) which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.

摘要翻译： 本发明涉及作为β-分泌酶的抑制剂并且可用于治疗其中涉及β-分泌酶的疾病如阿尔茨海默氏病的式（I）的哌啶哌啶化合物。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在治疗涉及β-分泌酶的疾病中的用途。

公开(公告)号：US20060057694A1

公开(公告)日：2006-03-16

申请号：US10541814

申请日：2004-01-23

申请人： Kenneth Thomas ,  Bo-Sheng Pan ,  Georgia McGaughey

发明人： Kenneth Thomas ,  Bo-Sheng Pan ,  Georgia McGaughey

IPC分类号： C12N9/12 ,  C07H21/04 ,  C12P21/06 ,  C12N5/06

CPC分类号： C07K14/705

摘要： An isolated nucleic acid molecule encoding an optimized rat receptor type tyrosine kinase, KDR, is disclosed. The isolation of this KDR cDNA sequence results in disclosure of purified forms of rat KDR protein, recombinant vectors and recombinant hosts which express rat KDR.

摘要翻译： 公开了编码优化的大鼠受体型酪氨酸激酶KDR的分离的核酸分子。 这种KDR cDNA序列的分离导致纯化形式的大鼠KDR蛋白，重组载体和表达大鼠KDR的重组宿主的公开。