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1. 发明专利

CA2756701A1 HYDROXYTHIENOQUINOLONES AND RELATED COMPOUNDS AS ANTI-INFECTIVE AGENTS 未知
公开(公告)号：CA2756701A1
公开(公告)日：2010-10-07
申请号：CA2756701
申请日：2010-04-05
申请人： ACHILLION PHARMACEUTICALS INC
发明人： BRADBURY BARTON JAMES , DESHPANDE MILIND , HASHIMOTO AKIHIRO , KIM HA YOUNG , LUCIEN EDLAINE , PAIS GODWIN , PUCCI MICHAEL , WANG QIUPING , WILES JASON ALLAN , PHADKE AVINASH
IPC分类号： C07D495/04 , A61P29/00 , C07D495/14 , C07D495/16
摘要： Disclosed herein are hydroxythienoquinolones and related compounds and their pharmaceutically acceptable salts useful as antiviral agents and having the general formula (I) in which the variables R2, R6, and R7 are defined herein. Certain compounds provided herein possess potent antibacterial, antiprotozoal, or antifungal activity and are particularly efficacious for the treatment of MRSA infections. The invention also provides pharmaceutical compositions, pharmaceutical compositions containing a hydroxythienoquinolone in combination with one or more other active agent, and methods of treating microbial infections in animals by administering an effective amount of a hydroxythienoquinolone or related compound to an animal suffering from a microbial infection.

2. 发明专利

SG174498A1 HYDROXYTHIENOQUINOLONES AND RELATED COMPOUNDS AS ANTI-INFECTIVE AGENTS 未知
公开(公告)号：SG174498A1
公开(公告)日：2011-10-28
申请号：SG2011068236
申请日：2010-04-05
申请人： ACHILLION PHARMACEUTICALS INC
发明人： BRADBURY BARTON JAMES , DESHPANDE MILIND , HASHIMOTO AKIHIRO , KIM HA YOUNG , LUCIEN EDLAINE , PAIS GODWIN , PUCCI MICHAEL , WANG QIUPING , WILES JASON ALLAN , PHADKE AVINASH
摘要： Disclosed herein are hydroxythienoquinolones and related compounds and their pharmaceutically acceptable salts useful as antiviral agents and having the general formula (I) in which the variables R2, R6, and R7 are defined herein. Certain compounds provided herein possess potent antibacterial, antiprotozoal, or antifungal activity and are particularly efficacious for the treatment of MRSA infections. The invention also provides pharmaceutical compositions, pharmaceutical compositions containing a hydroxythienoquinolone in combination with one or more other active agent, and methods of treating microbial infections in animals by administering an effective amount of a hydroxythienoquinolone or related compound to an animal suffering from a microbial infection.

3. 发明申请

WO2010115184A3 HYDROXYTHIENOQUINOLONES AND RELATED COMPOUNDS AS ANTI-INFECTIVE AGENTS 审中-公开
标题翻译：羟肟酸和相关化合物作为抗感染剂
公开(公告)号：WO2010115184A3
公开(公告)日：2011-03-24
申请号：PCT/US2010029938
申请日：2010-04-05
申请人： ACHILLION PHARMACEUTICALS INC , BRADBURY BARTON JAMES , DESHPANDE MILIND , HASHIMOTO AKIHIRO , KIM HA YOUNG , LUCIEN EDLAINE , PAIS GODWIN , PUCCI MICHAEL , WANG QIUPING , WILES JASON ALLAN , PHADKE AVINASH
发明人： BRADBURY BARTON JAMES , DESHPANDE MILIND , HASHIMOTO AKIHIRO , KIM HA YOUNG , LUCIEN EDLAINE , PAIS GODWIN , PUCCI MICHAEL , WANG QIUPING , WILES JASON ALLAN , PHADKE AVINASH
IPC分类号： C07D495/04 , A61P29/00 , C07D495/14 , C07D495/16
CPC分类号： A61K31/4743 , A61K31/496 , C07D495/04 , C07D498/16 , C07D519/00
摘要： Disclosed herein are hydroxythienoquinolones and related compounds and their pharmaceutically acceptable salts useful as antiviral agents and having the general formula (I) in which the variables R2, R6, and R7 are defined herein. Certain compounds provided herein possess potent antibacterial, antiprotozoal, or antifungal activity and are particularly efficacious for the treatment of MRSA infections. The invention also provides pharmaceutical compositions, pharmaceutical compositions containing a hydroxythienoquinolone in combination with one or more other active agent, and methods of treating microbial infections in animals by administering an effective amount of a hydroxythienoquinolone or related compound to an animal suffering from a microbial infection.
摘要翻译：本文公开了羟基噻吩并喹啉酮及其可药用盐，其可用作抗病毒剂并具有通式（I），其中变量R2，R6和R7在本文中定义。本文提供的某些化合物具有有效的抗细菌，抗原生动物或抗真菌活性，并且对于治疗MRSA感染特别有效。本发明还提供药物组合物，含有羟基噻吩并喹啉酮与一种或多种其它活性剂的药物组合物，以及通过向有微生物感染的动物施用有效量的羟基噻吩并喹啉酮或相关化合物来治疗动物微生物感染的方法。

4. 发明专利

HK1160855A1 HYDROXYTHIENOQUINOLONES AND RELATED COMPOUNDS AS ANTI-INFECTIVE AGENTS HYDROXYTHIENOQUINOLONES 未知
公开(公告)号：HK1160855A1
公开(公告)日：2012-08-17
申请号：HK12101285
申请日：2012-02-09
申请人： ACHILLION PHARMACEUTICALS INC
发明人： BRADBURY BARTON JAMES , DESHPANDE MILIND , HASHIMOTO AKIHIRO , KIM HA YOUNG , LUCIEN EDLAINE , PAIS GODWIN , PUCCI MICHAEL , WANG QIUPING , WILES JASON ALLAN , PHADKE AVINASH
IPC分类号： C07D20060101 , A61P20060101
摘要： Disclosed herein are hydroxylthienoquinolones and related compounds and their pharmaceutically acceptable salts useful as antiviral agents and having the general formula in which the variables R2, R6, and R7 are defined herein. Certain compounds provided herein possess potent antibacterial, antiprotozoal, or antifungal activity and are particularly efficacious for the treatment of MRSA infections. The invention also provides pharmaceutical compositions, pharmaceutical compositions containing a hydroxylthienoquinolone in combination with one or more other active agent, and methods of treating microbial infections in animals by administering an effective amount of a hydroxylthienoquinolone or related compound to an animal suffering from a microbial infection.

5. 发明专利

MX2011010434A HIDROXITIENOQUINOLONAS Y COMPUESTOS RELACIONADOS COMO AGENTES ANTIINFECCIOSOS. 未知
公开(公告)号：MX2011010434A
公开(公告)日：2012-01-20
申请号：MX2011010434
申请日：2010-04-05
申请人： ACHILLION PHARMACEUTICALS INC
发明人： DESHPANDE MILIND , PHADKE AVINASH , BRADBURY BARTON JAMES , HASHIMOTO AKIHIRO , LUCIEN EDLAINE , KIM HA YOUNG , WANG QIUPING , PAIS GODWIN , PUCCI MICHAEL , WILES JASON ALLAN
IPC分类号： C07D495/04 , A61P29/00 , C07D495/14 , C07D495/16
摘要： Se describen en la presente las hidroxitienoquinolonas y compuestos relacionados y sus sales farmacéuticamente aceptables útiles como agentes antivirus y que tienen la fórmula general (I) en la cual las variables R2, R6, y R7 se definen en la presente. Ciertos compuestos proporcionados en la presente poseen una actividad potente antibacteriana, antiprotozoaria, o antihongos y son particularmente eficaces para el tratamiento de las infecciones por MRSA. La invención también proporciona las composiciones farmacéuticas, composiciones farmacéuticas que contienen una hidroxitienoquinolona en combinación con uno o más de otros agentes activos, y los métodos para tratar las infecciones microbianas en animales administrando una cantidad efectiva de una hidroxitienoquinolona o compuesto relacionado a un animal que sufre de una infección microbiana.

6. 发明专利

AT445623T 未知
公开(公告)号：AT445623T
公开(公告)日：2009-10-15
申请号：AT05857829
申请日：2005-11-10
申请人： ACHILLION PHARMACEUTICALS INC
发明人： BRADBURY BARTON , DESHPANDE MILIND , PUCCI MICHAEL , WANG QIUPING , WILES JASON , SONG YONGSHENG , HASHIMOTO AKIHIRO , LUCIEN EDLAINE
IPC分类号： C07D513/04 , A61K31/437 , A61P31/04 , A61P33/02
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, R A , R B , A 1 , R 2 , R 3 , R 5 , R 6 , R 7 , A 8 and R 9 are defined herein. Certain compounds of Formula I and Formula II disclosed herein are potent and/or 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 eukaryotes.

7. 发明专利

BRPI1015079A2 Hidroxitienoquinolonas e compostos relacionados como agentes anti-infecciosos 未知
公开(公告)号：BRPI1015079A2
公开(公告)日：2015-09-01
申请号：BRPI1015079
申请日：2010-04-05
申请人： ACHILLION PHARMACEUTICALS INC
发明人： BRADBURY BARTON JAMES , DESHPANDE MILIND , HASHIMOTO AKIHIRO , KIM HA YOUNG , LUCIEN EDLAINE , PAIS GODWIN , PUCCI MICHAEL , WANG QIUPING , WILES JASON ALLAN , PHADKE AVINASH
IPC分类号： C07D495/04 , A61P29/00 , C07D495/14 , C07D495/16

8. 发明专利

ES2358048T3 NUEVAS ISOTIAZOLOQUINOLONAS Y COMPUESTOS RELACIONADOS COMO AGENTES ANTIINFECCIOSOS. 未知
公开(公告)号：ES2358048T3
公开(公告)日：2011-05-05
申请号：ES06735273
申请日：2006-02-15
申请人： ACHILLION PHARMACEUTICALS INC
发明人： BRADBURY BARTON , PAIS GODWIN , WANG QIUPING , DESHPANDE MILIND , PUCCI MICHAEL , SONG YONGSHENG , LUCIEN EDLAINE , WILES JASON , HASHIMOTO AKIHIRO
IPC分类号： C07D513/04 , A61K31/4365 , A61K31/437 , A61P31/00 , C07D513/14
摘要： Un compuesto o sal farmacéuticamente aceptable del mismo, en el que el compuesto es: 9-ciclopropil-8-metoxi-7-(4-(piperidin-1-ilmetil)fenil)isotiazolo[5,4-b]quinolin-3,4(2H,9H)-diona; 9-ciclopropil-6-fluoro-8-metoxi-7-(2-metilpiridin-4-il)isotiazolo[5,4-b]quinolin-3,4(2H,9H)-diona; 9-ciclopropil-8-metoxi-7-(1,2,3,4-tetrahidroisoquinolin-6-il)isotiazolo[5,4-b]quinolin-3,4(2H,9H)-diona; 9-ciclopropil-6-fluoro-8-metoxi-7-(6-metilpiridin-3-il)isotiazolo[5,4-b]quinolin-3,4(2H,9H)-diona; 9-ciclopropil-6-fluoro-8-metoxi-7-((R)-1-metilisoindolin-5-il)isotiazolo[5,4-b]quinolin-3,4(2H,9H)-diona; 9-ciclopropil-6-fluoro-7-(isoindolin-5-il)-8-metoxiisotiazolo[5,4-b]quinolin-3,4(2H,9H)-diona; 9-ciclopropil-6-fluoro-8-metoxi-7-(1,2,3,4-tetrahidroisoquinolin-6-il)isotiazolo[5,4-b]quinolin-3,4(2H,9H)-diona; 9-ciclopropil-8-metoxi-7-(2-metil-1,2,3,4-tetrahidroisoquinolin-6-il)isotiazolo[5,4-b]quinolin-3,4(2H,9H)-diona; 9-ciclopropil-6-fluoro-8-metoxi-7-(2-metil-1,2,3,4-tetrahidroisoquinolin-6-il)isotiazolo[5,4-b]quinolin-3,4(2H, 9H)-diona; 7-(3-amino-4-fluorofenil)-9-ciclopropil-8-metoxiisotiazolo[5,4-b]quinolin-3,4(2H,9H)-diona; 9-ciclopropil-8-metoxi-7-(2-metilpiridin-4-il)isotiazolo[5,4b]quinolin-3,4(2H,9H)-diona; O-metil oxima del (E)-4-(9-ciclopropil-6-fluoro-3,4-dioxo-2,3,4,9-tetrahidroisotiazolo[5,4-b]quinolin-7-il)picolinaldehído; 9-ciclopropil-6-fluoro-7-(2-(hidroximetil)piridin-4-il)isotiazolo[5,4-b]quinolin-3,4(2H,9H)-diona, 9-ciclopropil-6-fluoro-7-(6-fluoropiridin-3-il)-8-metoxiisotiazolo[5,4-b]quinolin-3,4(2H,9H)-diona; 9-ciclopropil-6-fluoro-7-(2-fluoropiridin-3-il)-8-metoxiisotiazolo[5,4-b]quinolin-3,4(2H,9H)-diona; 9-ciclopropil-6-fluoro-7-(2-fluoropiridin-4-il)-8-metoxiisotiazolo[5,4-b]quinolin-3,4(2H,9H)-diona; 9-ciclopropil-7-(4-(hidroximetil)fenil)-8-metoxiisotiazolo[5,4-b]quinolin-3,4(2H,9H)-diona; 9-ciclopropil-7-(3-hidroxifenil)-8-metoxiisotiazolo[5,4-b]quinolin-3,4(2H,9H)-diona; 7-(4-aminofenil)-9-ciclopropil-8-metoxiisotiazolo[5,4-b]quinolin-3,4(2H,9H)-diona; 7-(4-amino-3,5-dimetilfenil)-9-ciclopropil-6-fluoro-8-metoxiisotiazolo[5,4-b]quinolin-3,4(2H,9H)-diona; 7-(4-amino-3,5-dimetilfenil)-9-ciclopropil-6-fluoroisotiazolo[5,4-b]quinolin-3,4(2H,9H)-diona; 9-ciclopropil-6-fluoro-7-(4-hidroximetil)fenil)-8-metoxiisotiazolo[5,4-b]quinolin-3,4(2H,9H)-diona; 9-ciclopropil-7-(2-fluoropiridin-4-il)-8-metoxiisotiazolo[5,4-b]quinolin-3,4(2H,9H)-diona; 9-ciclopropil-6-fluoro-7-(2-metilpiridin-4-il)isotiazolo[5,4-b][1,8]naftiridin-3,4(2H,9H)-diona; 9-ciclopropil-7-(2,6-dimetilpiridin-4-il)-6-fluoroisotiazolo[5,4-b][1,8]naftiridin-3,4(2H,9H)-diona; 9-ciclopropil-8-metoxi-7-(piridin-3-il)isotiazolo[5,4-b]quinolin-3,4(2H,9H)-diona; 9-ciclopropil-7-(isoquinolin-6-il)-8-metoxiisotiazolo[5,4-b]quinolin-3,4(2H,9H)-diona; 5-(9-ciclopropil-6-fluoro-3,4-dioxo-2,3,4,9-tetrahidroisotiazolo[5,4-b]quinolin-7-il)nicotinonitrilo; 5-(9-ciclopropil-8-metoxi-3,4-dioxo-2,3,4,9-tetrahidroisotiazolo[5,4-b]quinolin-7-il)nicotinonitrilo; 5-(9-ciclopropil-6-fluoro-8-metoxi-3,4-dioxo-2,3,4,9-tetrahidroisotiazolo[5,4-b]quinolin-7-il)nicotinonitrilo; 9-ciclopropil-7-(6-fluoro-2-metilpiridin-3-il)-8-metoxiisotiazolo[5,4-b]quinolin-3,4(2H,9H)-diona; 9-ciclopropil-6-fluoro-7-(6-fluoro-2-metilpiridin-3-il)isotiazolo[5,4-b]quinolin-3,4(2H,9H)-diona; 9-ciclopropil-7-(2,6-dimetilpiridin-3-il)-8-metoxiisotiazolo[5,4-b]quinolin-3,4(2H,9H)-diona; 9-ciclopropil-6-fluoro-7-(piridin-4-il)isotiazolo[5,4-b][1,8]naftiridin-3,4(2H,9H)-diona; 9-ciclopropil-6-fluoro-7-(6-metilpiridin-3-il)isotiazolo[5,4-b][1,8]naftiridin-3,4(2H,9H)-diona; 9-ciclopropil-6-fluoro-7-(piridin-3-il)isotiazolo[5,4-b][1,8]naftiridin-3,4(2H,9H)-diona; 7-(4-(aminometil)fenil)-9-ciclopropil-6-fluoroisotiazolo[5,4,b][1,8]naftiridin-3,4(2H,9H)-diona; 9-cilopropil-7-(2,6-difluoropiridin-3-il)-8-metoxisotiazolo[5,4-b]quinolin-3,4(2H,9H)-diona; 9-ciclopropil-6-fluoro-7-(3-hidroxifenil)-8-metoxiisotiazolo[5,4b]quinolin-3,4(2H,9H)-diona; 7-(4-aminofenil)-9-ciclopropil-6-fluoro-8-metoxiisotiazolo[5,4-b]quinolin-3,4(2H,9H)-diona; o 9-ciclopropil-6-fluoro-8-metoxi-7-(piridin-3-il)isotiazolo[5,4-b]quinolin-3,4(2H,9H)-diona.

9. 发明专利

NZ595448A HYDROXYTHIENOQUINOLONES AND RELATED COMPOUNDS AS ANTI-INFECTIVE AGENTS 未知
公开(公告)号：NZ595448A
公开(公告)日：2013-01-25
申请号：NZ59544810
申请日：2010-04-05
申请人： ACHILLION PHARMACEUTICALS INC
发明人： BRADBURY BARTON JAMES , DESHPANDE MILIND , HASHIMOTO AKIHIRO , KIM HA YOUNG , LUCIEN EDLAINE , PAIS GODWIN , PUCCI MICHAEL , WANG QIUPING , WILES JASON ALLAN , PHADKE AVINASH
IPC分类号： C07D495/04 , A61P29/00 , C07D495/14 , C07D495/16
摘要： Disclosed herein are hydroxythienoquinolones and related compounds and their pharmaceutically acceptable salts useful as antiviral agents and having the general formula (I) in which the variables R2, R6, and R7 are defined herein. Certain compounds provided herein possess potent antibacterial, antiprotozoal, or antifungal activity and are particularly efficacious for the treatment of MRSA infections. The disclosure also provides pharmaceutical compositions, pharmaceutical compositions containing a hydroxythienoquinolone in combination with one or more other active agent, and methods of treating microbial infections in animals by administering an effective amount of a hydroxythienoquinolone or related compound to an animal suffering from a microbial infection.

10. 发明专利

AT491713T 未知
公开(公告)号：AT491713T
公开(公告)日：2011-01-15
申请号：AT06735273
申请日：2006-02-15
申请人： ACHILLION PHARMACEUTICALS INC
发明人： BRADBURY BARTON , PAIS GODWIN , WANG QIUPING , DESHPANDE MILIND , PUCCI MICHAEL , SONG YONGSHENG , LUCIEN EDLAINE , WILES JASON , HASHIMOTO AKIHIRO
IPC分类号： C07D513/04 , A61K31/4365 , A61K31/437 , A61P31/00 , 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 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.

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