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：EP1819683A2

公开(公告)日：2007-08-22

申请号：EP05852866.2

申请日：2005-12-02

申请人： Merck & Co., Inc. ,  ISTITUTO DI RICERCHE DI BIOLOGIA MOLECOLARE P. ANGELETTI S.P.A. ,  MERCK SHARP & DOHME LTD.

发明人： BELYK, Kevin, M. ,  MORRISON, Henry, G. ,  JONES, Philip ,  SUMMA, Vincenzo ,  COOPER, V., Brett ,  MAHAJAN, Amar, J. ,  KUMKE, Daniel, J. ,  TUNG, Hsien-Hsin ,  WAI, Lawrence ,  PRUZINSKY, Vanessa ,  PYE, Philip ,  ANGELAUD, Remy ,  MANCHENO, Danny

IPC分类号： C07D239/557 ,  C07D413/12 ,  A61K31/513 ,  A61P31/18

CPC分类号： C07D239/557 ,  C07D313/12 ,  C07D413/12

摘要： Potassium salts of Coompound A and methods for their preparation are disclosed, wherein Compound A is of formula: (Compound A). Compound A is an HIV integrase inhibitor useful for treating or prophylaxis of HIV infection, for delaying the onset of AIDS, and for treating or prophylaxis of AIDS.