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：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：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：EP0820453A1

公开(公告)日：1998-01-28

申请号：EP96911520.0

申请日：1996-04-01

申请人： MERCK & CO., INC.

发明人： FENG, Dong-Mei ,  BOCK, Mark, G. ,  FREIDINGER, Roger, M. ,  VACCA, Joseph, P. ,  DORSEY, Bruce, D.

IPC分类号： A61K38 ,  A61P7 ,  A61P43 ,  C07K5

CPC分类号： C07K5/06191 ,  A61K38/00 ,  C07K5/0222 ,  C07K5/06078 ,  C07K5/06139

摘要： A compound which inhibits human thrombin and has the structure (I) such as (II).

公开(公告)号：EP0729467A1

公开(公告)日：1996-09-04

申请号：EP95901884.0

申请日：1994-11-14

申请人： Merck & Co., Inc.

发明人： ALEXANDER, Jose ,  BINDRA, Dilbir ,  DORSEY, Bruce, D. ,  REPTA, Arnold, J. ,  VACCA, Joseph, P.

IPC分类号： C07D401 ,  A61K31 ,  A61P31 ,  A61P37 ,  C07D213

CPC分类号： C07D213/38

摘要： Prodrugs of formula (I) are useful in the inhibition of HIV protease, 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：EP1259506A1

公开(公告)日：2002-11-27

申请号：EP00983727.9

申请日：2000-11-20

申请人： Merck & Co., Inc.

发明人： BURGEY, Christopher ,  ISAACS, Richard, C. ,  DORSEY, Bruce, D. ,  ROBINSON, Kyle, A. ,  STAAS, Donnette ,  SANDERSON, Philip, E. ,  BARROW, James

IPC分类号： C07D401/12 ,  C07D401/14 ,  A61K31/50

CPC分类号： C07D401/12 ,  C07D401/14

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 A is (a), (b), (c) or (d).

公开(公告)号：EP0734387B1

公开(公告)日：2002-04-10

申请号：EP95905886.8

申请日：1994-12-12

申请人： Merck & Co., Inc.

发明人： HUFF, Joel, R. ,  VACCA, Joseph, P. ,  DORSEY, Bruce, D.

IPC分类号： C07D473/00 ,  C07D487/04 ,  C07D491/04 ,  C07D495/04 ,  C07D498/04 ,  A61K31/52 ,  A61K31/495 ,  C07D307/79 ,  C07D307/81 ,  C07D333/54 ,  C07D333/58

CPC分类号： C07D491/04 ,  C07D241/04 ,  C07D307/81 ,  C07D405/06 ,  C07D495/04

摘要： Compounds of formula (I) 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.

公开(公告)号：EP0969840A1

公开(公告)日：2000-01-12

申请号：EP98911875.7

申请日：1998-03-20

申请人： MERCK & CO., INC.

发明人： ISAACS, Richard, C., A. ,  NAYLOR-OLSEN, Adel, M. ,  DORSEY, Bruce, D. ,  NEWTON, Christina, L.

IPC分类号： A61K31/495 ,  A61K31/535 ,  C07D401/14 ,  C07D403/12 ,  C07D413/06

CPC分类号： C07D401/12 ,  A61K38/00 ,  C07D401/14 ,  C07D403/12 ,  C07K5/0207 ,  C07K5/06139

摘要： A compound which inhibits human thrombin and has structure (I) or (II) or (III) and pharmaceutically acceptable salts thereof, wherein compounds such as (IV) are useful for inhibiting formation of blood platelet aggregates in blood in a mammal.

公开(公告)号：EP0835109A1

公开(公告)日：1998-04-15

申请号：EP96923399.0

申请日：1996-06-24

申请人： MERCK & CO., INC.

发明人： SANDERSON, Philip, E. ,  NAYLOR-OLSEN, Adel, M. ,  DYER, Dona, L. ,  VACCA, Joseph, P. ,  ISAACS, Richard, C., A. ,  DORSEY, Bruce, D. ,  FRALEY, Mark, E.

IPC分类号： A61K31 ,  A61P7 ,  A61P43 ,  C07D213 ,  C07D401 ,  C07K5

CPC分类号： C07D213/64 ,  C07D213/74 ,  C07D213/75 ,  C07D213/76 ,  C07D401/12 ,  C07K5/06139

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

公开(公告)号：EP1267876A1

公开(公告)日：2003-01-02

申请号：EP01918822.6

申请日：2001-03-19

申请人： Merck & Co., Inc.

发明人： BARROW, James, C. ,  DORSEY, Bruce, D. ,  SELNICK, Harold, G. ,  NGO, Phung, L.

IPC分类号： A61K31/495 ,  A61K31/50 ,  A61K31/535 ,  A61P7/02 ,  C07D401/00 ,  C07D498/00

CPC分类号： C07D401/12 ,  C07D401/14 ,  C07D471/04

摘要： Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions and are selected from the group (I) or a pharmaceutically acceptable salt thereof, wherein T is selected from the group (II) and (III), and ;D, E, F, G, H, I, and J are independently N or C Y1, provided that the number of such variables D, E, F, G, H, I, and J representing N is 0, 1, or 2; K, L, M and Q are independently NH or C Y1Y2, provided that the number of such variables D, E, F, K, L, M, and Q representing N is 0, 1, or 2;Y?1 and Y2¿ are independently selected from the group consisting of hydrogen, C¿1-4? alkyl, halogen, amino, or hydroxy; A is (IV), (V), (VI), or (VII).