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：EP0900207A1

公开(公告)日：1999-03-10

申请号：EP97918780.0

申请日：1997-04-18

申请人： MERCK & CO., INC.

发明人： SANDERSON, Philip, E. ,  LYLE, Terry, A. ,  DORSEY, Bruce, D. ,  VARSOLONA, Richard, J.

IPC分类号： A61K31 ,  A61P7 ,  C07D241 ,  C07D401 ,  C07D405 ,  C07D409

CPC分类号： C07D401/12 ,  C07D241/20 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14

摘要： Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having structure (a), for example (b).

公开(公告)号：EP0900207B1

公开(公告)日：2001-11-21

申请号：EP97918780.4

申请日：1997-04-18

申请人： MERCK & CO., INC.

发明人： SANDERSON, Philip, E. ,  LYLE, Terry, A. ,  DORSEY, Bruce, D. ,  VARSOLONA, Richard, J.

IPC分类号： C07D241/20 ,  C07D401/12 ,  C07D405/14 ,  A61K31/495

CPC分类号： C07D401/12 ,  C07D241/20 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14

公开(公告)号：EP1124822A1

公开(公告)日：2001-08-22

申请号：EP99958684.5

申请日：1999-10-28

申请人： Merck & Co., Inc. ,  Barrow, James C.

发明人： SANDERSON, Philip, E. ,  LYLE, Terry, A. ,  DORSEY, Bruce, D. ,  STANTON, Matthew, G. ,  STAAS, Donnette ,  COBURN, Craig ,  NAYLOR-OLSEN, Adel, M. ,  MORRISSETTE, Matthew, M. ,  SELNICK, Harold, G. ,  NANTERMET, Philippe, G. ,  WILLIAMS, Peter, D. ,  STAUFFER, Kenneth, J. ,  BURGEY, Christopher ,  ISAACS, Richard

IPC分类号： C07D403/12 ,  C07D401/12 ,  A61K31/437 ,  A61K31/4375 ,  A61K31/4995

CPC分类号： C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D405/14 ,  C07D413/14 ,  C07D471/04

摘要： Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the structure (I) or a pharmaceutically acceptable salt thereof, wherein b is NY1 or O; c is CY2 or N; d is CY3 or N; e is CY4 or N; f is CY5 or N; g is CY6 or N; Y?4, Y5, and Y6¿ are independently hydrogen, C¿1-4? alkyl, or halogen; Y?1 and Y2¿ are independently hydrogen, C¿1-4? alkyl, C3-7 cycloalkyl, halogen, NH2, OH or C1-4 alkoxy, and Y?3¿ is hydrogen, C¿1-4? alkyl, C3-7 cycloalkyl, halogen, -CN, NH2, OH or C1-4 alkoxy; A is (II), (III), (IV), (V) or (VI); and W, W?1, R1, R3, R4, R5¿, X and Z are defined in the specification.

摘要翻译： 本发明化合物可用于抑制具有结构（I）的凝血酶和相关的血栓形成性闭塞物或其药学上可接受的盐，其中b是NY1或O; c是CY2或N; d是CY3或N; e是CY4或N; f是CY5或N; g是CY6或N; Y 4，Y 5和Y 6独立地是氢，C 1-4 - 烷基或卤素; Y 1和Y 2独立地是氢，C 1-4 - 烷基，C 3-7环烷基，卤素，NH 2，OH或C 1-4烷氧基，Y 3是氢，C 1-4 - 烷基，C 3-7环烷基，卤素，-CN，NH 2，OH或C 1-4烷氧基; A是（II），（III），（IV），（V）或（VI）; W，W 1，R 1，R 3，R 4，R 5'，X和Z在说明书中定义。

公开(公告)号：EP1942736A2

公开(公告)日：2008-07-16

申请号：EP06836463.7

申请日：2006-10-23

申请人： Merck & Co., Inc.

发明人： WAI, John, S. ,  WILLIAMS, Peter, D. ,  LYLE, Terry, A.

IPC分类号： A01N43/58 ,  A01N43/60 ,  A61K31/50

CPC分类号： C07D487/04

摘要： Substituted hydroxytetrahydropyrrolopyrazinone and substituted hydroxytetrahydro-pyrazolopyrazinone compounds of Formula (I) are inhibitors of HIV integrase and inhibitors of HIV replication: (I) wherein R1, R2, R3, R4; R5, X, ring A, and Q are as defined herein. The compounds are useful in the prevention and treatment of infection by HIV and in the prevention, delay in the onset, and treatment of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.

摘要翻译： 式（I）的取代的羟基四氢吡咯并吡嗪酮和取代的羟基四氢吡唑并吡喃酮化合物是HIV整合酶抑制剂和HIV复制抑制剂：（I）其中R1，R2，R3，R4; R5，X，环A和Q如本文所定义。 这些化合物可用于预防和治疗HIV感染以及预防，延缓艾滋病的发作和治疗。 这些化合物本身作为化合物或以药学上可接受的盐的形式用于抗HIV感染和AIDS。 化合物及其盐可以用作药物组合物中的成分，任选地与其他抗病毒剂，免疫调节剂，抗生素或疫苗组合使用。

公开(公告)号：EP1189899A1

公开(公告)日：2002-03-27

申请号：EP00939492.5

申请日：2000-06-01

申请人： Merck & Co., Inc.

发明人： BURGEY, Christopher, S. ,  ROBINSON, Kyle, A. ,  WILLIAMS, Peter, D. ,  COBURN, Craig, A. ,  LYLE, Terry, A. ,  SANDERSON, Philip, E.

IPC分类号： C07D401/12 ,  C07D401/14 ,  A61K31/495

CPC分类号： C07D401/12 ,  A61K31/495 ,  C07D401/14 ,  A61K31/00 ,  A61K2300/00

摘要： Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having structure (I): where A is (II), (III), or (IV) wherein Y?1 and Y2¿ are independently hydrogen, C¿1-4? alkyl, C1-4 alkoxy, FuHvC(CH2)0-1 O-, wherein u and v are either 1 or 2, provided that when u is 1, v is 2, and when u is 2, v is 1; C3-7 cycloalkyl, thio C1-4 alkyl, C1-4 sulfinylalkyl, C1-4 sulfonylalkyl, halogen, cyano, or trifluoromethyl, and wherein b is 0 or 1.

公开(公告)号：EP1549315A2

公开(公告)日：2005-07-06

申请号：EP03749574.4

申请日：2003-09-10

申请人： Merck & Co., Inc.

发明人： WAI, John, S. ,  KIM, Boyoung ,  FISHER, Thorsten, E. ,  ZHUANG, Linghang ,  WILLIAMS, Peter, D. ,  LYLE, Terry, A. ,  LANGFORD, H. Marie ,  ROBINSON, Kyle, A.

IPC分类号： A61K31/4985 ,  A61K31/5377 ,  A61K31/541 ,  C07D487/04 ,  C07D487/14

CPC分类号： C07D471/14 ,  C07D471/04

摘要： 8,9-Dihydroxydihydropyridopyrazine-1,6-diones and 8,9-dihydroxypyridopyrazine-1,6-diones are inhibitors of HIV integrase and inhibitors of HIV replication. In one embodiment, the pyridopyrazinediones are of Formula (I): (I),wherein R1, R2, R3, R4 and R5 are defined herein. The compounds are useful in the prevention and treatment of infection by HIV and in the prevention, delay in the onset, and treatment of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of preventing, treating or delaying the onset of AIDS and methods of preventing or treating infection by HIV are described.

公开(公告)号：EP1189899B1

公开(公告)日：2003-02-12

申请号：EP00939492.5

申请日：2000-06-01

申请人： Merck & Co., Inc.

发明人： BURGEY, Christopher, S. ,  ROBINSON, Kyle, A. ,  WILLIAMS, Peter, D. ,  COBURN, Craig, A. ,  LYLE, Terry, A. ,  SANDERSON, Philip, E.

IPC分类号： C07D401/12 ,  C07D401/14 ,  A61K31/495

CPC分类号： C07D401/12 ,  A61K31/495 ,  C07D401/14 ,  A61K31/00 ,  A61K2300/00

公开(公告)号：EP1017393A1

公开(公告)日：2000-07-12

申请号：EP98946835.0

申请日：1998-09-03

申请人： MERCK & CO., INC.

发明人： SANDERSON, Philip, E. ,  LYLE, Terry, A. ,  DORSEY, Bruce, D.

IPC分类号： A61K31/495 ,  C07D241/20 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D405/14

CPC分类号： C07D401/12 ,  C07D401/14 ,  C07D405/14

摘要： Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having structure (a), for example, structure (17-1).

公开(公告)号：EP0971891A1

公开(公告)日：2000-01-19

申请号：EP98902807.1

申请日：1998-01-16

申请人： MERCK & CO., INC.

发明人： SANDERSON, Philip, E. ,  LYLE, Terry, A. ,  COBURN, Craig

IPC分类号： C07D211/80 ,  C07D401/02 ,  A61K31/44

CPC分类号： C07D213/73 ,  C07D213/75 ,  C07D409/14 ,  C07K5/06139

摘要： A compound which inhibits human thrombin and where has structure (a) such as (b).

摘要翻译： 抑制人凝血酶的化合物，其中具有（b）的结构（a）的化合物。