公开(公告)号：EP1881825A2

公开(公告)日：2008-01-30

申请号：EP06759135.4

申请日：2006-05-05

申请人： Merck & Co., Inc.

发明人： VACCA, Joseph, P. ,  WAI, John, S. ,  PAYNE, Linda, S. ,  ISAACS, Richard, C., A. ,  HAN, Wei ,  EGBERTSON, Melissa ,  PRACITTO, Richard

IPC分类号： A61K31/40 ,  A61K31/445

CPC分类号： C07D471/14 ,  A61K31/4353 ,  A61K31/4375 ,  C07D498/14

摘要： Tricyclic compounds of Formula (I) are inhibitors of HIV integrase and inhibitors of HIV replication: wherein bond a, ring A, Rl, R2 and R3 are defined herein. The compounds are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset 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）的三环化合物是HIV整合酶抑制剂和HIV复制抑制剂：其中键a，环A，R1，R2和R3如本文所定义。 这些化合物可用于预防或治疗HIV感染和预防，治疗或延缓AIDS发作。 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：EP1725556A1

公开(公告)日：2006-11-29

申请号：EP05725120.9

申请日：2005-03-09

申请人： Merck & Co., Inc.

发明人： HAN, Wei ,  EGBERTSON, Melissa ,  WAI, John, S. ,  ZHUANG, Linghang ,  RUZEK, Rowena, D. ,  PERLOW, Debra, S. ,  ISAACS, Richard, C., A. ,  CAMERON, Mark ,  FOSTER, Bruce, S. ,  DOLLING, Ulf, H. ,  HOERRNER, R., Scott ,  OBLIGADO, Vanessa, E. ,  NEILSON, Lou, Anne ,  KIM, Boyoung ,  PAYNE, Linda, S. ,  MORRISSETTE, Matthew, M. ,  WILLIAMS, Peter, D. ,  PYE, Philip, J. ,  ANGELAUD, Remy ,  ASKIN, David

IPC分类号： C07D471/04 ,  A61K31/4375 ,  A61P31/12 ,  A61P37/02

CPC分类号： C07D471/04

摘要： Hydroxy (tetra- or hexa-)hydronaphthyridine dione compounds of Formula I are inhibitors of HIV integrase and inhibitors of HIV replication: (I) wherein a, 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.

摘要翻译： 式I的羟基（四或六）氢化萘啶二酮化合物是HIV整合酶抑制剂和HIV复制抑制剂：（I）其中a，R1，R2，R3，R4和R5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：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).