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：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：EP1515944A1

公开(公告)日：2005-03-23

申请号：EP03741998.3

申请日：2003-06-16

申请人： Sunesis Pharmaceuticals, Inc.

发明人： YANG, Wenjin ,  CARY, Douglas, R. ,  JACOBS, Jeffrey, W. ,  LU, Wanli ,  LU, Yafan ,  SUN, Jian ,  ZHONG, Min

IPC分类号： C07C237/22 ,  C07C237/12 ,  C07C237/14 ,  C07D333/02 ,  C07D307/02 ,  C07D277/02 ,  C07D263/02 ,  C07D211/04 ,  C07D209/02 ,  C07D249/08 ,  C07C311/16 ,  C07C311/08 ,  C07D275/02 ,  C07D285/06 ,  C07D285/18

CPC分类号： C07D207/08 ,  C07C233/78 ,  C07C235/50 ,  C07C237/22 ,  C07C271/54 ,  C07C311/08 ,  C07C311/16 ,  C07C311/21 ,  C07C2601/02 ,  C07C2601/08 ,  C07C2601/14 ,  C07D213/81 ,  C07D213/82 ,  C07D217/14 ,  C07D241/08 ,  C07D263/32 ,  C07D275/02 ,  C07D277/30 ,  C07D285/06 ,  C07D285/10 ,  C07D285/16 ,  C07D285/18 ,  C07D295/192 ,  C07D307/54 ,  C07D333/24 ,  C07D333/38 ,  C07D401/06 ,  C07D409/06

摘要： The present invention provides compounds having formula (I): wherein R', R , R , X , R , R , R ', X , X , and R4 are as defined herein, and pharmaceuticals compositions thereof. The present invention also provides methods of inhibiting proteases, more specially aspartyl proteases. In certain embodiments, compounds inhibit BACE (beta-site APP-cleaving enzyme), and thus are useful in the treatment or prevention of a disease characterized by beta-amyloid deposits in the brain (including, but not limited to, Alzheimer's Disease). The present invention also provides methods for preparing compounds of the invention.

摘要翻译： 本发明提供具有式（I）的化合物：其中R 1，R 0，R 1，X 1，R 2， R 3，R 3，R 3，X 2，X 3和R 3， 4和本文所定义的药物组合物。 本发明还提供了抑制蛋白酶，更具体而言是天冬氨酰蛋白酶的方法。 在某些实施方案中，化合物抑制BACE（β-位点APP切割酶），因此可用于治疗或预防以脑中β-淀粉样蛋白沉积为特征的疾病（包括但不限于阿尔茨海默氏病）。 本发明还提供了制备本发明化合物的方法。

公开(公告)号：EP2063889A2

公开(公告)日：2009-06-03

申请号：EP07811660.5

申请日：2007-09-04

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

发明人： EGBERTSON, Melissa, S. ,  STAUFFER, Shaun, R. ,  COBURN, Craig, A. ,  BARROW, James, C. ,  YANG, Wenjin ,  LU, Wanli ,  FAHR, Bruce ,  NEILSON, Lou Anne ,  WAI, Jenny M.

IPC分类号： A61K31/438 ,  C07D471/10 ,  C07D498/10

CPC分类号： C07D471/10 ,  C07D498/10

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：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.