公开(公告)号：EP1924593B8

公开(公告)日：2009-11-18

申请号：EP06787475.0

申请日：2006-07-14

申请人： Merck & Co., Inc.

发明人： HOLLOWAY, M. Katharine ,  LIVERTON, Nigel, J. ,  LUDMERER, Steven, W. ,  MCCAULEY, John, A. ,  OLSEN, David, B. ,  RUDD, Michael, T. ,  VACCA, Joseph, P. ,  MCINTYRE, Charles, J.

IPC分类号： C07K5/08 ,  A61P31/14 ,  A61K38/06

CPC分类号： C07K5/0808 ,  A61K38/00 ,  C07K5/0812 ,  C07K5/0827

摘要： The present invention relates to macrocyclic compounds of formula (I) that are useful as inhibitors of the hepatitis C virus (HCV) NS3 protease, their synthesis, and their use for treating or preventing HCV infections.

公开(公告)号：EP1912963A2

公开(公告)日：2008-04-23

申请号：EP06789003.8

申请日：2006-07-28

申请人： Merck & Co., Inc.

发明人： NANTERMET, Philippe, G. ,  VACCA, Joseph, P.

IPC分类号： C07D307/22 ,  A61K31/443 ,  A61K31/341

CPC分类号： C07D307/22 ,  C07D405/12

摘要： The present invention is directed to cyclic ketal 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：EP1879607A2

公开(公告)日：2008-01-23

申请号：EP06751833.2

申请日：2006-04-28

申请人： Merck & Co., Inc.

发明人： HOLLOWAY, M. Katharine ,  LIVERTON, Nigel, J. ,  LUDMERER, Steven, W. ,  MCCAULEY, John, A. ,  OLSEN, David, B. ,  RUDD, Michael, T. ,  VACCA, Joseph, P.

IPC分类号： A61K38/12

CPC分类号： C07K5/0808 ,  C07K5/0806 ,  C07K5/0812 ,  C07K5/0815 ,  C07K5/0821

摘要： The present invention relates to macrocyclic compounds of formula (I) that are useful as inhibitors of the hepatitis C virus (HCV) NS3 protease, their synthesis, and their use for treating or preventing HCV infections. I

摘要翻译： 本发明涉及可用作丙型肝炎病毒（HCV）NS3蛋白酶抑制剂的有用的式（I）的大环化合物，它们的合成及其用于治疗或预防HCV感染的用途。 一世

公开(公告)号：EP1656359A2

公开(公告)日：2006-05-17

申请号：EP04780598.1

申请日：2004-08-10

申请人： Merck & Co., Inc.

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

IPC分类号： C07D267/22 ,  C07D225/04 ,  A61K31/33 ,  A61P25/28

CPC分类号： C07D267/00 ,  C07D225/08

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.

公开(公告)号：EP0949926A1

公开(公告)日：1999-10-20

申请号：EP97911906.0

申请日：1997-10-27

申请人： MERCK & CO., INC.

发明人： BELL, Ian, M. ,  GUARE, James, P., Jr. ,  HAZUDA, Daria, Jean ,  MUNSON, Peter, M. ,  THOMPSON, Wayne, J. ,  VACCA, Joseph, P.

IPC分类号： A61K31 ,  C07D243 ,  C07D403

CPC分类号： C07D403/12 ,  A61K31/5513 ,  C07D243/20

摘要： Compounds having a benzodiazepine hydrazide core are described. These compounds are useful in the inhibition of HIV integrase, 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.

摘要翻译： 描述了具有苯并二氮杂肼核心的化合物。 这些化合物可用作抑制HIV整合酶，预防或治疗HIV感染和治疗AIDS，作为化合物，药学上可接受的盐，药物组合物成分，不论是否与其他抗病毒剂，免疫调节剂，抗生素或 疫苗。 还描述了治疗AIDS的方法和预防或治疗HIV感染的方法。

公开(公告)号：EP0923372A1

公开(公告)日：1999-06-23

申请号：EP97906633.0

申请日：1997-02-18

申请人： MERCK & CO., INC.

发明人： SANDERSON, Philip, E. ,  LYLE, Terry, A. ,  VACCA, Joseph, P. ,  LUMMA, William, C. ,  BRADY, Stephen, F. ,  TUCKER, Thomas, J.

IPC分类号： C07D213 ,  A61K31 ,  C07K5

CPC分类号： C07D213/75 ,  C07K5/06139

摘要： Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions and have structure (I), for example (II).

公开(公告)号：EP0696277A1

公开(公告)日：1996-02-14

申请号：EP94915427.0

申请日：1994-04-26

申请人： MERCK & CO. INC.

发明人： VACCA, Joseph, P. ,  DORSEY, Bruce, D. ,  GUARE, James, P. ,  HOLLOWAY, M., Katharine ,  HUNGATE, Randall, W. ,  LEVIN, Rhonda, B.

IPC分类号： A61K31 ,  A61K45 ,  A61P31 ,  A61P37 ,  C07C237 ,  C07D207 ,  C07D211 ,  C07D217 ,  C07D241 ,  C07D401 ,  C07D403 ,  C07D405 ,  C07D409 ,  C07D417

CPC分类号： C07D401/06 ,  A61K31/70 ,  A61K45/06 ,  C07C237/20 ,  C07C2602/08 ,  C07D207/16 ,  C07D211/60 ,  C07D217/26 ,  C07D241/04 ,  C07D401/12 ,  C07D403/12 ,  C07D405/06 ,  C07D405/12 ,  C07D409/12 ,  C07D417/12 ,  A61K2300/00

摘要： Compounds of formula (I), where R?1 and R2¿ are independently hydrogen or optionally-substituted C¿1-4?alkyl or aryl, and R?1¿ also forms a heterocycle or heterocycle-C¿1-4?alkyl, are HIV protease inhibitors. These compounds are useful in the prevention or treatment of infection by HIV and in 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.

摘要翻译： 其中R 1和R 2独立地为氢或任选取代的C 1-4烷基或芳基，或R 1和R 2连接在一起形成单环或双环环系的式“IMAGE”的化合物是HIV蛋白酶抑制剂。 这些化合物可用于治疗艾滋病毒和艾滋病感染，作为化合物，药学上可接受的盐，药物组合物成分，无论是否与其他抗病毒剂，免疫调节剂，抗生素或疫苗结合使用。 还描述了治疗艾滋病的方法和治疗HIV感染的方法。

公开(公告)号：EP1913016A1

公开(公告)日：2008-04-23

申请号：EP06800513.1

申请日：2006-07-28

申请人： Merck & Co., Inc.

发明人： HOLLOWAY, M., Katharine ,  LIVERTON, Nigel, J. ,  MCCAULEY, John, A. ,  RUDD, Michael, T. ,  VACCA, Joseph, P. ,  LUDMERER, Steven, W. ,  OLSEN, David, B.

IPC分类号： C07K5/08 ,  C07K5/10 ,  C07K7/06 ,  A61K38/06 ,  A61K38/07 ,  A61K38/08 ,  A61P31/14

CPC分类号： C07K5/0812 ,  A61K38/00 ,  C07K5/0827

摘要： The present invention relates to macrocyclic compounds of formula (I) that are useful as inhibitors of the hepatitis C virus (HCV) NS3 protease, their synthesis, and their use for treating or preventing HCV infections. Formula (I).

公开(公告)号：EP1910404A1

公开(公告)日：2008-04-16

申请号：EP06787698.7

申请日：2006-07-14

申请人： Merck & Co., Inc.

发明人： HOLLOWAY, M., Katharine ,  LIVERTON, Nigel, J. ,  LUDMERER, Steven, W. ,  MCCAULEY, John, A. ,  OLSEN, David, B. ,  RUDD, Michael, T. ,  VACCA, Joseph, P. ,  MCINTYRE, Charles, J.

IPC分类号： C07K5/08 ,  A61P31/14 ,  A61K38/06

CPC分类号： C07K5/0808 ,  A61K38/00 ,  C07K5/0812 ,  C07K5/0827

摘要： The present invention relates to macrocyclic compounds of formula (I) that are useful as inhibitors of the hepatitis C virus (HCV) NS3 protease, their synthesis, and their use for treating or preventing HCV infections.

公开(公告)号：EP1817311A2

公开(公告)日：2007-08-15

申请号：EP05851916.6

申请日：2005-11-18

申请人： Merck & Co., Inc.

发明人： NANTERMET, Philippe, G. ,  STANTON, Matthew, G. ,  RAJAPAKSE, Hemaka, A. ,  SELNICK, Harold, G. ,  BARROW, James, C. ,  STAUFFER, Shaun, R. ,  VACCA, Joseph, P. ,  MOORE, Keith, P. ,  STACHEL, Shawn, J.

IPC分类号： C07D413/04

CPC分类号： C07D413/04 ,  C07D413/14

摘要： The present invention is directed to 2,3,4,6-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.