公开(公告)号：EP1804794A2

公开(公告)日：2007-07-11

申请号：EP05812233.4

申请日：2005-10-12

申请人： Merck & Co., Inc. ,  Sunesis Pharmaceuticals, Inc.

发明人： BARROW, James, C. ,  COBURN, Craig, A. ,  EGBERTSON, Melissa, S. ,  MCGAUGHEY, Georgia, B. ,  MCWHERTER, Melody, A. ,  NEILSON, Lou, Anne ,  SELNICK, Harold, G. ,  STAUFFER, Shaun, R. ,  YANG, Zhi-Qiang ,  YANG, Wenjin ,  LU, Wanli ,  FAHR, Bruce ,  RITTLE, Kenneth, E.

IPC分类号： A61K31/438 ,  C07D401/04

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.

公开(公告)号：EP1910364A2

公开(公告)日：2008-04-16

申请号：EP06787495.8

申请日：2006-07-14

申请人： Merck & Co., Inc. ,  Sunesis Pharmaceuticals, Inc.

发明人： COBURN, Craig, A. ,  EGBERTSON, Melissa, S. ,  GRAHAM, Samuel, L. ,  MCGAUGHEY, Georgia, B. ,  STAUFFER, Shaun, R. ,  RAJAPAKSE, Hemaka, A. ,  NANTERMET, Philippe, G. ,  STACHEL, Shawn, R. ,  YANG, Wenjin ,  LU, Wanli ,  FAHR, Bruce

IPC分类号： C07D471/10 ,  A61K31/438 ,  A61P25/28

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.

公开(公告)号：EP1804794B1

公开(公告)日：2013-07-31

申请号：EP05812233.4

申请日：2005-10-12

申请人： Merck Sharp & Dohme Corp. ,  Sunesis Pharmaceuticals, Inc.

发明人： BARROW, James, C. ,  COBURN, Craig, A. ,  EGBERTSON, Melissa, S. ,  MCGAUGHEY, Georgia, B. ,  MCWHERTER, Melody, A. ,  NEILSON, Lou, Anne ,  SELNICK, Harold, G. ,  STAUFFER, Shaun, R. ,  YANG, Zhi-Qiang ,  YANG, Wenjin ,  LU, Wanli ,  FAHR, Bruce ,  RITTLE, Kenneth, E.

IPC分类号： A61K31/438 ,  C07D401/04

CPC分类号： C07D471/10

公开(公告)号：EP1910364B1

公开(公告)日：2012-03-21

申请号：EP06787495.8

申请日：2006-07-14

申请人： Merck Sharp & Dohme Corp. ,  Sunesis Pharmaceuticals, Inc.

发明人： COBURN, Craig, A. ,  EGBERTSON, Melissa, S. ,  GRAHAM, Samuel, L. ,  MCGAUGHEY, Georgia, B. ,  STAUFFER, Shaun, R. ,  RAJAPAKSE, Hemaka, A. ,  NANTERMET, Philippe, G. ,  STACHEL, Shawn, R. ,  YANG, Wenjin ,  LU, Wanli ,  FAHR, Bruce

IPC分类号： C07D471/10 ,  A61K31/438 ,  A61P25/28

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.

公开(公告)号：EP1740559A1

公开(公告)日：2007-01-10

申请号：EP05738682.3

申请日：2005-04-15

申请人： Merck & Co., Inc.

发明人： BARROW, James, C. ,  MCGAUGHEY, Georgia, B. ,  NANTERMET, Philippe, G. ,  RAJAPAKSE, Hemaka, A. ,  SELNICK, Harold, G. ,  STAUFFER, Shaun, R. ,  COBURN, Craig, A.

IPC分类号： C07D271/10

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.

公开(公告)号：EP2049110A2

公开(公告)日：2009-04-22

申请号：EP07796851.9

申请日：2007-07-13

申请人： Merck & Co., Inc.

发明人： COLEMAN, Paul, J. ,  COX, Christopher, D. ,  MCGAUGHEY, Georgia, B. ,  ROECKER, Anthony, J. ,  SCHREIER, John, D.

IPC分类号： A61K31/44 ,  C07D471/08 ,  A61P3/04

CPC分类号： C07D471/08 ,  C07D487/08

摘要： The present invention is directed to bridged diazepan compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which orexin receptors are involved.

摘要翻译： 本发明涉及作为食欲素受体拮抗剂的桥联二氮杂环庚烷化合物，其可用于治疗或预防涉及食欲肽受体的神经和精神疾病和疾病。 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预防或治疗涉及食欲素受体的这些疾病中的用途。

公开(公告)号：EP1841426A1

公开(公告)日：2007-10-10

申请号：EP06718444.0

申请日：2006-01-13

申请人： Merck & Co., Inc.

发明人： MCGAUGHEY, Georgia, B. ,  NANTERMET, Philippe, G. ,  RAJAPAKSE, Hemaka, A. ,  STAUFFER, Shaun, R.

IPC分类号： A61K31/4245 ,  C07D271/06

CPC分类号： C07D413/04 ,  C07D271/10 ,  C07D271/107 ,  C07D405/04 ,  C07D413/06 ,  C07D413/08 ,  C07D413/10 ,  C07D413/14 ,  C07D417/04 ,  C07D417/06 ,  C07D451/02 ,  C07D453/02 ,  C07D471/04 ,  C07D487/04 ,  C07D513/04

摘要： The present invention is directed to tertiary carbinamine compounds having substituted heterocycles, which are inhibitors of the beta-secretase enzyme, and 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.

公开(公告)号：EP1590436A2

公开(公告)日：2005-11-02

申请号：EP04704947.3

申请日：2004-01-23

申请人： Merck & Co., Inc.

发明人： THOMAS, Kenneth, A., Jr. ,  PAN, Bo-Sheng ,  MCGAUGHEY, Georgia, B.

IPC分类号： C12N1/00

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.