公开(公告)号：EP1694678A2

公开(公告)日：2006-08-30

申请号：EP04813437.3

申请日：2004-12-08

申请人： Merck & Co., Inc. ,  BANYU PHARMACEUTICAL CO., LTD.

发明人： ASKIN, David ,  CONLON, David ,  LEE, Jaemoon ,  PIPIK, Brenda ,  ZHONG, Yong-Li ,  KOHMURA, Yoshinori

IPC分类号： C07D487/00

CPC分类号： C07F9/6561 ,  C07C251/60 ,  C07C255/26 ,  C07C259/14 ,  C07D239/557 ,  C07D487/04

摘要： Processes for preparing 10-amino-3-hydroxy-4-oxo-4,6,7,8,9,10-hexahydropyrimido[1,2-a]azepine-2-carboxylates and related compounds are disclosed. The preparation of carboxamide derivatives from these carboxylates is also disclosed. The carboxamides are HIV integrase inhibitors and are useful for treating HIV infection and AIDS.

公开(公告)号：EP0931066B1

公开(公告)日：2002-05-15

申请号：EP97942446.2

申请日：1997-09-12

申请人： MERCK & CO., INC.

发明人： DORZIOTIS, Ilias, K. ,  HOUPIS, Ioannis, N. ,  LEE, Jaemoon ,  VOLANTE, Ralph, P.

IPC分类号： C07D213/30 ,  C07D213/16 ,  A61K31/44

CPC分类号： C07D213/16 ,  C07D213/30

摘要： This invention is concerned with a novel process for the preparation of a compound of structural formula (I) wherein R?1 and R2¿ independently are aryl, C¿2-15? alkenyl or C1-15 alkyl, either unsubstituted or substituted with one or three substituents, which can be the same or different, selected from the group consisting of Ra, wherein Ra belongs to a group consisting of C1-6 alkyl, aryl, halo, -N(R?3)¿2, -NO2, -CN, -OR3, -C¿3-6? cycloalkoxy, -CO(R?3¿), -COOR3, SO2R3 and -SR3; wherein R3 is selected from the group consisting of hydrogen, C¿1-6? alkyl, C2-6 alkenyl and aryl, said alkyl, alkenyl or aryl optionally substituted with 1 to 3 groups of R?a¿, which is an important antiasthmatic agent.

公开(公告)号：EP1007511A1

公开(公告)日：2000-06-14

申请号：EP98943349.5

申请日：1998-08-24

申请人： MERCK & CO., INC.

发明人： CHOI, Woo-Baeg ,  LEE, Jaemoon ,  LYNCH, Joseph, E. ,  REIDER, Paul, J. ,  VOLANTE, Ralph, P.

IPC分类号： C07D205/08 ,  C07F7/18

CPC分类号： C07D205/08 ,  C07F7/186 ,  Y02P20/55

摘要： The instant invention relates to a compound of formula (I) wherein Ra and P are: (a) hydrogen, (b) methyl, or (c) a hydroxy protecting group and an efficient process for its synthesis.

公开(公告)号：EP1007511B1

公开(公告)日：2003-07-02

申请号：EP98943349.5

申请日：1998-08-24

申请人： MERCK & CO., INC.

发明人： CHOI, Woo-Baeg ,  LEE, Jaemoon ,  LYNCH, Joseph, E. ,  REIDER, Paul, J. ,  VOLANTE, Ralph, P.

IPC分类号： C07D205/08 ,  C07F7/18

CPC分类号： C07D205/08 ,  C07F7/186 ,  Y02P20/55

摘要： The instant invention relates to a compound of formula (I) wherein Ra and P are: (a) hydrogen, (b) methyl, or (c) a hydroxy protecting group and an efficient process for its synthesis.

公开(公告)号：EP0931066A1

公开(公告)日：1999-07-28

申请号：EP97942446.0

申请日：1997-09-12

申请人： MERCK & CO., INC.

发明人： DORZIOTIS, Ilias, K. ,  HOUPIS, Ioannis, N. ,  LEE, Jaemoon ,  VOLANTE, Ralph, P.

IPC分类号： B01J31 ,  C07B61 ,  C07D213

CPC分类号： C07D213/16 ,  C07D213/30

摘要： This invention is concerned with a novel process for the preparation of a compound of structural formula (I) wherein R?1 and R2¿ independently are aryl, C¿2-15? alkenyl or C1-15 alkyl, either unsubstituted or substituted with one or three substituents, which can be the same or different, selected from the group consisting of Ra, wherein Ra belongs to a group consisting of C1-6 alkyl, aryl, halo, -N(R?3)¿2, -NO2, -CN, -OR3, -C¿3-6? cycloalkoxy, -CO(R?3¿), -COOR3, SO2R3 and -SR3; wherein R3 is selected from the group consisting of hydrogen, C¿1-6? alkyl, C2-6 alkenyl and aryl, said alkyl, alkenyl or aryl optionally substituted with 1 to 3 groups of R?a¿, which is an important antiasthmatic agent.