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：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：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：EP1807396A1

公开(公告)日：2007-07-18

申请号：EP05851361.5

申请日：2005-10-25

申请人： Merck & Co., Inc.

发明人： COBURN, Craig, A. ,  HOLLOWAY, M. Katharine ,  STACHEL, Shawn, J.

IPC分类号： C07D211/72 ,  A61K31/44

CPC分类号： C07D213/73

摘要： The present invention is directed to 2-aminopyridine 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：EP1732906A1

公开(公告)日：2006-12-20

申请号：EP05733551.5

申请日：2005-03-25

申请人： Merck & Co., Inc.

发明人： COBURN, Craig, A. ,  ESPESETH, Amy, S. ,  STACHEL, Shawn, J. ,  OLSEN, David, B. ,  HAZUDA, Daria, J. ,  HOLLOWAY, M. Katharine

IPC分类号： C07D277/60

CPC分类号： C07D417/14 ,  C07D277/40 ,  C07D277/60 ,  C07D277/82 ,  C07D277/84 ,  C07D417/04 ,  C07D417/06 ,  C07D417/08

摘要： The present invention is directed to 2-aminothiazole compounds which are aspartyl protease inhibitors, and are inhibitors of both the beta-secretase enzyme and HIV protease, and that are useful in the treatment of diseases in which the beta-secretase enzyme and HIV are involved, such as Alzheimer's disease, HIV Infection and AIDS. 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 and HIV protease are involved.

公开(公告)号：EP1855679A2

公开(公告)日：2007-11-21

申请号：EP06718443.2

申请日：2006-01-13

申请人： Merck & Co., Inc.

发明人： COBURN, Craig, A. ,  NANTERMET, Philippe, G. ,  RAJAPAKSE, Hemaka, A. ,  SELNICK, Harold, G. ,  STAUFFER, Shaun, R.

IPC分类号： A61K31/4745 ,  C07D271/06

CPC分类号： C07D413/06 ,  C07D271/10

摘要： The present invention is directed to aminomethyl 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：EP1743170A2

公开(公告)日：2007-01-17

申请号：EP05732580.5

申请日：2005-03-29

申请人： Merck & Co., Inc.

发明人： COBURN, Craig, A. ,  ESPESETH, Amy, S. ,  HAZUDA, Daria, J.

IPC分类号： G01N33/50

CPC分类号： G01N33/6896 ,  C07D307/79 ,  C07D405/12 ,  G01N2333/4709 ,  G01N2500/00

摘要： Disclosed are methods for identifying and evaluating the binding properties of substances to the amyoid precursor protein (APP) or to β-amyloid (Aβ) fragments of APP. Also disclosed is a class of benzofuran derivatives of formula (I), which interact specifically with APP or Aβ, and block interaction of APP or Aβ with secreatase or APP or Aβ binding antibodies.

公开(公告)号：EP1583750A2

公开(公告)日：2005-10-12

申请号：EP04700071.6

申请日：2004-01-02

申请人： Merck & Co., Inc.

发明人： COBURN, Craig, A. ,  STACHEL, Shawn, J. ,  VACCA, Joseph, P.

IPC分类号： C07D267/22 ,  A61K31/33 ,  A61P25/28

CPC分类号： C07D273/02

摘要： The present invention is directed to compounds which are inhibitors of the beta-secretase enzyme and that are useful in the treatment or prevention 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 prevention or treatment of such diseases in which the beta-secretase enzyme is involved.