公开(公告)号：EP1083897A1

公开(公告)日：2001-03-21

申请号：EP99926096.1

申请日：1999-06-01

申请人： MERCK & CO., INC. ,  Tularik Inc.

发明人： SELNICK, Harold, G. ,  HAZUDA, Daria, Jean ,  EGBERTSON, Melissa ,  GUARE, James, P., Jr. ,  WAI, John, S. ,  YOUNG, Steven, D. ,  CLARK, David, L. ,  MEDINA, Julio, C.

IPC分类号： A61K31/40 ,  A61K31/415 ,  A61K31/445 ,  C07D207/30 ,  C07D207/333 ,  C07D209/04 ,  C07D209/12 ,  C07D211/18 ,  C07D211/26 ,  C07D211/28 ,  C07D211/32 ,  C07D211/40 ,  C07D231/10 ,  C07D231/12 ,  C07D233/54 ,  C07D233/64 ,  C07D401/04

CPC分类号： C07D207/333 ,  A61K31/40 ,  A61K45/06 ,  C07D207/34 ,  C07D209/12 ,  C07D231/12 ,  C07D401/04 ,  A61K2300/00

摘要： Nitrogen-containing heteroaryl dioxo-butyric acid derivatives are described as inhibitors of HIV integrase and inhibitors of HIV replication. These compounds are useful in the prevention or treatment of infection by HIV and the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.

公开(公告)号：EP2134342A2

公开(公告)日：2009-12-23

申请号：EP08726587.2

申请日：2008-03-07

申请人： Merck & Co., Inc.

发明人： BELL, Ian, M. ,  STUMP, Craig, A. ,  SELNICK, Harold, G.

IPC分类号： A61K31/44 ,  A61K31/40

CPC分类号： C07D471/20 ,  C07D403/12 ,  C07D471/10 ,  C07D519/00

摘要： The present invention is directed to compounds of Formula I: I (where variables A1, A2, B, J, K, m, n, R4, R5a, R5b and R5c are as defined herein) useful as antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache. 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 CGRP is involved.

公开(公告)号：EP0854870B1

公开(公告)日：2009-06-10

申请号：EP96937654.0

申请日：1996-10-02

申请人： Merck & Co., Inc.

发明人： SELNICK, Harold, G. ,  CLAREMON, David, A. ,  LIVERTON, Nigel, J.

IPC分类号： C07D401/14 ,  A61K31/415 ,  A61K31/44 ,  A61K31/445 ,  C07D417/14

CPC分类号： C07D401/14 ,  C07D417/14 ,  Y02P20/55

摘要： Compounds represented by formula (I), are disclosed. AR represents an aromatic group containing 6-10 atoms; and (a) represents a 4 to 10 membered non-aromatic heterocycle containing at least one N atom, and optionally containing 1-2 additional N atoms and 0-1 O or S atom. A pharmaceutical composition is also included. Methods of treating cancer and cytokine mediated diseases are also included.

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：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：EP1689713A1

公开(公告)日：2006-08-16

申请号：EP04811618.0

申请日：2004-11-19

申请人： Merck & Co., Inc.

发明人： NANTERMET, Philippe, G. ,  RAJAPAKSE, Hemaka, A. ,  SELNICK, Harold, G. ,  STAUFFER, Shaun, R. ,  YOUNG, Mary Beth

IPC分类号： C07D213/02 ,  A61K31/44

CPC分类号： C07C255/46 ,  C07C311/08 ,  C07C2601/02 ,  C07C2601/08 ,  C07D207/06 ,  C07D213/76 ,  C07D295/192 ,  C07D401/06

摘要： The present invention is directed to benzylether and benzylamino 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：EP0863757B1

公开(公告)日：2003-03-26

申请号：EP96928097.3

申请日：1996-08-08

申请人： MERCK & CO., INC.

发明人： DE LASZLO, Stephen, E. ,  MANTLO, Nathan, B. ,  PONTICELLO, Gerald, S. ,  SELNICK, Harold, G. ,  LIVERTON, Nigel, J.

IPC分类号： A61K31/44 ,  A61K31/50 ,  A61K31/445 ,  A61K31/495 ,  A61K31/505 ,  A61K31/535 ,  C07D211/68 ,  C07D211/80 ,  C07D213/02 ,  C07D239/02 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04

CPC分类号： C07D401/04 ,  C07D401/14 ,  C07D403/04

摘要： The present invention addresses 2-substituted aryl pyrroles, as well as compositions containing such compounds and methods of treatment. Cytokine mediated diseases refers to diseases or conditions in which excessive or unregulated production or activity of one or more cytokines occurs. Interleukin-1 (IL-1), Interleukin-6 (IL-6), Interleukin-8 (IL-8) and Tumor Necrosis Factor (TNF) are cytokines which are involved.

公开(公告)号：EP0833819B1

公开(公告)日：2003-03-26

申请号：EP96916988.7

申请日：1996-06-03

申请人： MERCK & CO., INC.

发明人： CLAREMON, David, A. ,  FREIDINGER, Roger, M. ,  LIVERTON, Nigel ,  SELNICK, Harold, G. ,  SMITH, Garry, R.

IPC分类号： C07D243/12 ,  A61K31/55

CPC分类号： C07D243/12

摘要： This invention is concerned with novel compounds represented by structural formula (I), which are useful in the treatment of arrhythmia.

公开(公告)号：EP0854870A1

公开(公告)日：1998-07-29

申请号：EP96937654.0

申请日：1996-10-02

申请人： MERCK & CO., INC.

发明人： SELNICK, Harold, G. ,  CLAREMON, David, A. ,  LIVERTON, Nigel, J.

IPC分类号： A61K31 ,  A61P7 ,  A61P17 ,  A61P19 ,  A61P29 ,  A61P31 ,  A61P35 ,  A61P37 ,  A61P43 ,  C07D233 ,  C07D401 ,  C07D405 ,  C07D413 ,  C07D417

CPC分类号： C07D401/14 ,  C07D417/14 ,  Y02P20/55

摘要： Compounds represented by formula (I), are disclosed. AR represents an aromatic group containing 6-10 atoms; and (a) represents a 4 to 10 membered non-aromatic heterocycle containing at least one N atom, and optionally containing 1-2 additional N atoms and 0-1 O or S atom. A pharmaceutical composition is also included. Methods of treating cancer and cytokine mediated diseases are also included.

公开(公告)号：EP0842156A1

公开(公告)日：1998-05-20

申请号：EP96916954.0

申请日：1996-06-03

申请人： MERCK & CO., INC.

发明人： CLAREMON, David, A. ,  LIVERTON, Nigel ,  SELNICK, Harold, G.

IPC分类号： A61K31 ,  A61P9 ,  C07D243

CPC分类号： C07D243/12

摘要： This invention is concerned with novel compounds represented by structural formula (I) which are useful in the treatment of arrhythmia.

摘要翻译： 本发明涉及用于治疗心律失常的由结构式（I）表示的新颖化合物。