公开(公告)号：EP1809639B1

公开(公告)日：2009-10-14

申请号：EP05857829.5

申请日：2005-11-10

申请人： Achillion Pharmaceuticals, Inc.

发明人： BRADBURY, Barton, James ,  DESHPANDE, Milind ,  PUCCI, Michael, John ,  WANG, Qiuping ,  WILES, Jason, Allan ,  SONG, Yongsheng ,  HASHIMOTO, Akihiro ,  LUCIEN, Edlaine

IPC分类号： C07D513/04 ,  A61K31/437 ,  A61P31/04 ,  A61P33/02

CPC分类号： C07D513/04 ,  C07D513/14

摘要： The invention provides compounds and salts of Formula I and Formula II which possess antimicrobial activity. The invention also provides novel synthetic intermediates useful in making compounds of Formula I and Formula II. The variables n, m, p, RA, RB, A1, R2, R3, R5, R6, R7, A8 and R9 are defined herein. Certain compounds of Formula I and Formula II disclosed herein are potent and /or selective inhibitors of bacterial replication. The invention also provides antimicrobial compositions, including pharmaceutical compositions, containing one or more compounds of Formula I or Formula II and one or more carriers, excipients, or diluents. Such compositions may contain a compound of Formula I or Formula II as the only active agent or may contain a combination of a compound of Formula I or Formula II and one or more other active agents. The invention also provides methods for treating microbial infections in eukaryotes.

公开(公告)号：EP1848723A1

公开(公告)日：2007-10-31

申请号：EP06735273.2

申请日：2006-02-15

申请人： Achillion Pharmaceuticals, Inc.

发明人： BRADBURY, Barton, James ,  PAIS, Godwin ,  WANG, Qiuping ,  DESHPANDE, Milind ,  PUCCI, Michael, John ,  SONG, Yongsheng ,  LUCIEN, Edlaine ,  WILES, Jason ,  HASHIMOTO, Akihiro

IPC分类号： C07D513/04 ,  A61K31/437 ,  A61K31/4365 ,  A61P31/00 ,  C07D513/14

CPC分类号： C07D513/04 ,  C07D513/14

摘要： The invention provides certain compounds and salts of Formula I and Formula II:which possess antimicrobial activity. The invention also provides novel synthetic intermediatesuseful in making compounds of Formula I and Formula II. The variables A1, R2, R3, R5, R6, R7, A8, and Rg are defined herein. Certain compounds of Formula I and Formula II disclosed herein are potent and selective inhibitors of bacterial DNA synthesis and bacterial replication. The invention also provides antimicrobial compositions, including pharmaceutical compositions, containing one or more compounds of Formula I or Formula II and one or more carriers, excipients, or diluents. Such compositions may contain a compound of Formula I or Formula II as the only active agent or may contain a combination of a compound of Formula I or Formula II and one or more other active agents. The invention also provides methods for treating microbial infections in animals.

公开(公告)号：EP1664062B1

公开(公告)日：2013-03-13

申请号：EP04780234.3

申请日：2004-08-04

申请人： Achillion Pharmaceuticals, Inc.

发明人： BRADBURY, Barton, James ,  DESHPANDE, Milind ,  PUCCI, Michael, John ,  WANG, Quiping ,  WILES, Jason, Allan ,  SONG, Yongsheng ,  HASHIMOTO, Akihiro ,  LUCIEN, Edlaine

IPC分类号： C07D513/04 ,  A61K31/435

CPC分类号： C07D513/04

公开(公告)号：EP1809639A2

公开(公告)日：2007-07-25

申请号：EP05857829.5

申请日：2005-11-10

申请人： Achillion Pharmaceuticals, Inc.

发明人： BRADBURY, Barton, James ,  DESHPANDE, Milind ,  PUCCI, Michael, John ,  WANG, Qiuping ,  WILES, Jason, Allan ,  SONG, Yongsheng ,  HASHIMOTO, Akihiro ,  LUCIEN, Edlaine

IPC分类号： C07D513/04 ,  A61K31/437 ,  A61P31/04 ,  A61P33/02

CPC分类号： C07D513/04 ,  C07D513/14

摘要： The invention provides compounds and salts of Formula I and Formula II which possess antimicrobial activity. The invention also provides novel synthetic intermediates useful in making compounds of Formula I and Formula II. The variables n, m, p, RA, RB, A1, R2, R3, R5, R6, R7, A8 and R9 are defined herein. Certain compounds of Formula I and Formula II disclosed herein are potent and /or selective inhibitors of bacterial replication. The invention also provides antimicrobial compositions, including pharmaceutical compositions, containing one or more compounds of Formula I or Formula II and one or more carriers, excipients, or diluents. Such compositions may contain a compound of Formula I or Formula II as the only active agent or may contain a combination of a compound of Formula I or Formula II and one or more other active agents. The invention also provides methods for treating microbial infections in eukaryotes.

公开(公告)号：EP1664062A1

公开(公告)日：2006-06-07

申请号：EP04780234.3

申请日：2004-08-04

申请人： Achillion Pharmaceuticals, Inc.

发明人： BRADBURY, Barton, James ,  DESHPANDE, Milind ,  PUCCI, Michael, John ,  WANG, Quiping ,  WILES, Jason, Allan ,  SONG, Yongsheng ,  HASHIMOTO, Akihiro ,  LUCIEN, Edlaine

IPC分类号： C07D513/04 ,  A61K31/435

CPC分类号： C07D513/04

摘要： The invention provides compounds and salts of Formula (I) and Formula (II): which possess antimicrobial activity. The invention also provides novel synthetic intermediates useful in making compounds of Formula (I) and Formula (II). The variables A1, R2, R3, R5, R6, R7, A8 and R9 are defined herein. Certain compounds of Formula (I) and Formula (II) disclosed herein are potent and selective inhibitors of bacterial DNA synthesis and bacterial replication. The invention also provides antimicrobial compositions, including pharmaceutical compositions, containing one or more compounds of Formula (I) or Formula (II) and one or more carriers, excipients, or diluents. Such compositions may contain a compound of Formula (I) or Formula (II) as the only active agent or may contain a combination of a compound of Formula (I) or Formula (II) and one or more other active agents. The invention also provides methods for treating microbial infections in animals.

公开(公告)号：EP1848723B1

公开(公告)日：2010-12-15

申请号：EP06735273.2

申请日：2006-02-15

申请人： Achillion Pharmaceuticals, Inc.

发明人： BRADBURY, Barton, James ,  PAIS, Godwin ,  WANG, Qiuping ,  DESHPANDE, Milind ,  PUCCI, Michael, John ,  SONG, Yongsheng ,  LUCIEN, Edlaine ,  WILES, Jason ,  HASHIMOTO, Akihiro

IPC分类号： C07D513/04 ,  A61K31/437 ,  A61K31/4365 ,  A61P31/00 ,  C07D513/14

CPC分类号： C07D513/04 ,  C07D513/14

摘要： The invention provides certain compounds and salts of Formula I and Formula II:which possess antimicrobial activity. The invention also provides novel synthetic intermediatesuseful in making compounds of Formula I and Formula II. The variables A1, R2, R3, R5, R6, R7, A8, and Rg are defined herein. Certain compounds of Formula I and Formula II disclosed herein are potent and selective inhibitors of bacterial DNA synthesis and bacterial replication. The invention also provides antimicrobial compositions, including pharmaceutical compositions, containing one or more compounds of Formula I or Formula II and one or more carriers, excipients, or diluents. Such compositions may contain a compound of Formula I or Formula II as the only active agent or may contain a combination of a compound of Formula I or Formula II and one or more other active agents. The invention also provides methods for treating microbial infections in animals.

公开(公告)号：EP1986654A2

公开(公告)日：2008-11-05

申请号：EP07751388.5

申请日：2007-02-20

申请人： Achillion Pharmaceuticals, Inc.

发明人： BRADBURY, Barton, James ,  HUANG, Mingjun

IPC分类号： A61K31/56 ,  C07J63/00 ,  A61P31/18

CPC分类号： C07J63/008 ,  C07C62/32

摘要： Substituted taraxastanes useful for treating viral infections, are provided herein. Thus, in a first aspect, the invention provides compounds of Formula I and the pharmaceutically acceptable salts thereof, wherein the variables Ri, R2, and X are defined herein. The compounds described herein are thought to act by inhibiting retroviral maturation, including maturation of encapsulated retroviruses viruses, such as the HIV viruses, HIV-I and HIV-2. Pharmaceutical compositions comprising such compounds of Formula I are included herein. Methods of using such compounds to treat human patients infected with an HIV virus and reducing the mortality of AIDS are also provided herein.