公开(公告)号：EP1737861A1

公开(公告)日：2007-01-03

申请号：EP05732864.3

申请日：2005-04-05

申请人： Merck & Co., Inc.

发明人： BILODEAU, Mark, T. ,  CHEN, Chixu ,  COSFORD, Nicholas, D., P. ,  EASTMAN, Brian, W. ,  HARTNETT, John, C. ,  HU, Essa, H. ,  MANLEY, Peter, J. ,  NEILSON, Lou, Anne ,  TEHRANI, Lida, R. ,  WU, Zhicai

IPC分类号： C07D471/04 ,  C07D487/04 ,  A61K31/4375 ,  A61K31/519 ,  A61P35/00

CPC分类号： C07D471/04 ,  C07D519/00

摘要： The present invention is directed to compounds which contain substituted napthyridines which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for treating cancer comprising administration of the compounds of the invention.

摘要翻译： 本发明涉及含有取代的萘啶的化合物，其抑制丝氨酸/苏氨酸蛋白激酶Akt的活性。 本发明还涉及含有本发明化合物的化学治疗组合物和用于治疗癌症的方法，其包括施用本发明的化合物。

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：EP1784175A2

公开(公告)日：2007-05-16

申请号：EP05807835.3

申请日：2005-08-19

申请人： Merck & Co., Inc.

发明人： BILODEAU, Mark, T. ,  COSFORD, Nicholas, D., P. ,  HARTNETT, John, C. ,  LIANG, Jun ,  MANLEY, Peter, J. ,  NEILSON, Lou, Anne ,  SIU, Tony ,  WU, Zhicai ,  LI, Yiwei

IPC分类号： A61K31/395

CPC分类号： C07D471/04

摘要： The present invention is directed to compounds which contain substituted 5-deazapteridine moieties which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for treating cancer comprising administration of the compounds of the invention.

摘要翻译： 本发明涉及含有抑制Akt（一种丝氨酸/苏氨酸蛋白激酶）活性的取代的5-脱氮喋啶结构部分的化合物。 本发明还涉及含有本发明化合物的化学治疗组合物和用于治疗癌症的方法，其包括施用本发明的化合物。

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。