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1. 发明申请

US20060235041A1 New isothiazoloquinolones and related compounds as anti-infective agents 失效
标题翻译：新异噻唑并喹啉酮和相关化合物作为抗感染剂
公开(公告)号：US20060235041A1
公开(公告)日：2006-10-19
申请号：US11354521
申请日：2006-02-15
申请人： Barton Bradbury , Godwin Pais , Qiuping Wang , Milind Deshpande , Michael Pucci , Yongsheng Song , Edlaine Lucien , Jason Wiles , Akihiro Hashimoto
发明人： Barton Bradbury , Godwin Pais , Qiuping Wang , Milind Deshpande , Michael Pucci , Yongsheng Song , Edlaine Lucien , Jason Wiles , Akihiro Hashimoto
IPC分类号： C07D498/02 , A61K31/4745
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 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.
摘要翻译：本发明提供某些具有抗微生物活性的式I和式II化合物和盐。本发明还提供了可用于制备式I和式II化合物的新型合成中间体。变量A 1，R 2，R 3，R 5，R 6，/或 >，R 7，A 8和R 9在本文中定义。本文公开的某些式I和式II化合物是细菌DNA合成和细菌复制的有效和选择性抑制剂。本发明还提供包含一种或多种式I或式II化合物和一种或多种载体，赋形剂或稀释剂的抗微生物组合物，包括药物组合物。这样的组合物可以含有式I或式II的化合物作为唯一的活性剂或可以含有式I或式II的化合物与一种或多种其它活性剂的组合。本发明还提供了治疗动物微生物感染的方法。

2. 发明申请

US20060100215A1 8A,9-dihydro-4aH-isothiazolo[5,4-b]quinoline-3,4-diones and related compounds as anti-infective agents 审中-公开
标题翻译： 8A，9-二氢-4a-异噻唑并[5,4-b]喹啉-3,4-二酮和相关化合物作为抗感染剂
公开(公告)号：US20060100215A1
公开(公告)日：2006-05-11
申请号：US11271556
申请日：2005-11-10
申请人： Barton Bradbury , Milind Deshpande , Michael Pucci , Qiuping Wang , Jason Wiles , Yongsheng Song , Akihiro Hashimoto , Edlaine Lucien
发明人： Barton Bradbury , Milind Deshpande , Michael Pucci , Qiuping Wang , Jason Wiles , Yongsheng Song , Akihiro Hashimoto , Edlaine Lucien
IPC分类号： A61K31/496 , A61K31/4745 , C07D498/02
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 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.
摘要翻译：本发明提供具有抗微生物活性的式I和式II化合物和盐。本发明还提供了可用于制备式I和式II化合物的新型合成中间体。变量n，m，p，R a，R B，A 1，R 2，R 2， R 3，R 5，R 6，R 7，A 8和R 8，本文定义了SUB> 9 。本文公开的某些式I和式II化合物是细菌DNA合成和细菌复制的有效和/或选择性抑制剂。本发明还提供包含一种或多种式I或式II化合物和一种或多种载体，赋形剂或稀释剂的抗微生物组合物，包括药物组合物。这样的组合物可以含有式I或式II的化合物作为唯一的活性剂或可以含有式I或式II的化合物与一种或多种其它活性剂的组合。本发明还提供了用于治疗真核生物中的微生物感染的方法。

3. 发明授权

US08114888B2 Isothiazoloquinolones and related compounds as anti-infective agents 失效
标题翻译：异噻唑并喹啉酮和相关化合物作为抗感染剂
公开(公告)号：US08114888B2
公开(公告)日：2012-02-14
申请号：US11354521
申请日：2006-02-15
申请人： Barton James Bradbury , Godwin Pais , Qiuping Wang , Milind Deshpande , Michael Pucci , Yongsheng Song , Edlaine Lucien , Jason Allan Wiles , Akihiro Hashimoto
发明人： Barton James Bradbury , Godwin Pais , Qiuping Wang , Milind Deshpande , Michael Pucci , Yongsheng Song , Edlaine Lucien , Jason Allan Wiles , Akihiro Hashimoto
IPC分类号： A61K31/4365 , A61K31/4375 , C07D491/14
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 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.
摘要翻译：本发明提供某些具有抗微生物活性的式I和式II化合物和盐。本发明还提供了可用于制备式I和式II化合物的新型合成中间体。变量A1，R2，R3，R5，R6，R7，A8和R9在本文中定义。

4. 发明申请

US20080071086A1 METHOD FOR SYNTHESIS OF 8-ALKOXY-9H-ISOTHIAZOLO[5,4-B]QUINOLINE-3,4-DIONES 有权
标题翻译：合成8-羟基-9-异亮氨酸[5,4-B]喹啉-3,4-二酮的方法
公开(公告)号：US20080071086A1
公开(公告)日：2008-03-20
申请号：US11840006
申请日：2007-08-16
申请人： Barton Bradbury , Jason Wiles , Akihiro Hashimoto , Qiuping Wang , Edlaine Lucien , Godwin Pais , Ha Young Kim
发明人： Barton Bradbury , Jason Wiles , Akihiro Hashimoto , Qiuping Wang , Edlaine Lucien , Godwin Pais , Ha Young Kim
IPC分类号： C07D491/00
CPC分类号： C07D215/28 , C07D401/04 , C07D513/04
摘要： The present invention provides process for synthesis of 8-methoxy-9H-isothiazolo[5,4-b]quinoline-3,4-diones and 8A,9-dihydro-4aH-isothiazolo[5,4-b]quinoline-3,4-diones of the Formula A. The substituents R, R5, R6, R7, R8 and R9 are defined herein. The invention also provides novel synthetic intermediates useful in the synthesis of 8-methoxy-9H-isothiazolo[5,4-b]quinoline-3,4-diones and 8A,9-dihydro-4aH-isothiazolo[5,4-b]quinoline-3,4-diones.
摘要翻译：本发明提供8-甲氧基-9H-异噻唑并[5,4-b]喹啉-3,4-二酮和8A,9-二氢-4a-异噻唑并[5,4-b]喹啉-3的合成方法，取代基R 1，R 5，R 6，R 7，R 8，R 8， >和R 9'在本文中定义。本发明还提供了用于合成8-甲氧基-9H-异噻唑并[5,4-b]喹啉-3,4-二酮和8A,9-二氢-4a-异噻唑并[5,4-b] 喹啉-3,4-二酮。

5. 发明授权

US08173636B2 Hydroxylthienoquinolones and related compounds as anti-infective agents 失效
标题翻译：羟基噻吩并喹啉酮和相关化合物作为抗感染剂
公开(公告)号：US08173636B2
公开(公告)日：2012-05-08
申请号：US12754057
申请日：2010-04-05
申请人： Barton James Bradbury , Milind Deshpande , Akihiro Hashimoto , Ha Young Kim , Edlaine Lucien , Godwin Pais , Michael Pucci , Qiuping Wang , Jason Allan Wiles , Avinash Phadke
发明人： Barton James Bradbury , Milind Deshpande , Akihiro Hashimoto , Ha Young Kim , Edlaine Lucien , Godwin Pais , Michael Pucci , Qiuping Wang , Jason Allan Wiles , Avinash Phadke
IPC分类号： C07D495/04 , A61K31/4743 , A61K31/496
CPC分类号： A61K31/4743 , A61K31/496 , C07D495/04 , C07D498/16 , C07D519/00
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.
摘要翻译：本文公开的是羟基噻吩并喹啉酮和相关化合物及其药学上可接受的盐，其可用作抗病毒剂并具有通式，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。

6. 发明申请

US20070049586A1 8-methoxy-9H-isothiazolo[5,4-b]quinoline-3,4-diones and related compounds as anti-infective agents 有权
标题翻译： 8-甲氧基-9H-异噻唑并[5,4-b]喹啉-3,4-二酮和相关化合物作为抗感染剂
公开(公告)号：US20070049586A1
公开(公告)日：2007-03-01
申请号：US11494205
申请日：2006-07-27
申请人： Barton Bradbury , Jason Wiles , Qiuping Wang , Akhiro Hashimoto , Edlaine Lucien , Godwin Clarence Pais , Milind Deshpande , Michael Pucci , Ha Kim
发明人： Barton Bradbury , Jason Wiles , Qiuping Wang , Akhiro Hashimoto , Edlaine Lucien , Godwin Clarence Pais , Milind Deshpande , Michael Pucci , Ha Kim
IPC分类号： A61K31/541 , A61K31/5377 , A61K31/496 , A61K31/4745 , C07D498/02
CPC分类号： C07D495/04 , C07D498/04 , C07D513/04 , C07D513/14
摘要： The invention provides compound and salts of Formula I and II, disclosed herein, which includes compounds of Formula A and Formula B: Such compounds possess useful antimicrobial activity. The variables R2, R3, R5, R6, R7, and R9 shown in Formula A and B 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 animals.
摘要翻译：本发明提供本文公开的式I和II的化合物和盐，其包括式A和式B的化合物：这些化合物具有有效的抗微生物活性。变量R 2，R 3，R 5，R 6，R 7和/或N >，并且式A和B中所示的R 9是本文定义的。本文公开的某些式I和式II化合物是细菌DNA合成和细菌复制的有效和/或选择性抑制剂。本发明还提供包含一种或多种式I或式II化合物和一种或多种载体，赋形剂或稀释剂的抗微生物组合物，包括药物组合物。这样的组合物可以含有式I或式II的化合物作为唯一的活性剂或可以含有式I或式II的化合物与一种或多种其它活性剂的组合。本发明还提供了治疗动物微生物感染的方法。

7. 发明申请

US20050075363A1 Isothiazoloquinolones and related compounds as anti-infective agents 审中-公开
标题翻译：异噻唑并喹啉酮和相关化合物作为抗感染剂
公开(公告)号：US20050075363A1
公开(公告)日：2005-04-07
申请号：US10911406
申请日：2004-08-04
申请人： Barton Bradbury , Milind Deshphande , Michael Pucci , Qiuping Wang , Jason Wiles , Monishing Song , Akihiro Hashimoto , Edlaine Lucien
发明人： Barton Bradbury , Milind Deshphande , Michael Pucci , Qiuping Wang , Jason Wiles , Monishing Song , Akihiro Hashimoto , Edlaine Lucien
IPC分类号： C07D498/04 , C07D513/04 , C07D498/14 , A61K31/4745
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.
摘要翻译：本发明提供具有抗微生物活性的式I和式II化合物和盐。本发明还提供了可用于制备式I和式II化合物的新型合成中间体。变量A1，R2，R3，R5，R6，R7，A8和R9在本文中定义。本文公开的某些式I和式II化合物是细菌DNA合成和细菌复制的有效和选择性抑制剂。本发明还提供包含一种或多种式I或式II化合物和一种或多种载体，赋形剂或稀释剂的抗微生物组合物，包括药物组合物。这样的组合物可以含有式I或式II的化合物作为唯一的活性剂或可以含有式I或式II的化合物与一种或多种其它活性剂的组合。本发明还提供了治疗动物微生物感染的方法。

8. 发明申请

US20090012071A1 4-SUBSTITUTED-1H-ISOTHIAZOLO[5,4-B][1,4]OXAZINO[2,3,4-IJ]QUINOLINE-7,8(2H,9H)-DIONES AND RELATED COMPOUNDS AS ANTI-INFECTIVE AGENTS 审中-公开
标题翻译： 4-取代的1H-异亮氨酸[5,4-B] [1,4]氧杂嗪[2,3,4-I]喹啉-7,8（2H，9H） - 和相关化合物作为抗感染剂
公开(公告)号：US20090012071A1
公开(公告)日：2009-01-08
申请号：US12108106
申请日：2008-04-23
申请人： Barton James Bradbury , Milind Deshpande , Akihiro Hashimoto , Ha Young Kim , Edlaine Lucien , Godwin Pais , Michael John Pucci , Qiuping Wang , Jason Allan Wiles
发明人： Barton James Bradbury , Milind Deshpande , Akihiro Hashimoto , Ha Young Kim , Edlaine Lucien , Godwin Pais , Michael John Pucci , Qiuping Wang , Jason Allan Wiles
IPC分类号： A61K31/5383 , C07D498/06 , A61P33/02 , A61P31/04
CPC分类号： C07D513/16
摘要： The present invention provides compounds of the formula that possess antimicrobial activity. Certain compounds provided herein possess potent antibacterial, antiprotozoal, or antifungal activity. Particular compounds provided herein are also potent and/or selective inhibitors of microbial DNA synthesis and reproduction. The invention provides anti-microbial compositions, including pharmaceutical compositions, containing a compound of the invention and one or more or more carriers. The invention provides pharmaceutical compositions containing a 4-substituted-1H-isothiazolo[5,4-b][1,4]oxazino[2,3,4-ij]quinoline-7,8(2H,9H)-dione or related compound as the only active agent or in combination with one or more other active agents. The invention provides methods for treating or preventing microbial infections, preferably animals, by administering an effective amount of a 4-substituted-1H-isothiazolo[5,4-b][1,4]oxazino[2,3,4-ij]quinoline-7,8(2H,9H)-dione or related compound to an organism suffering from or susceptible to microbial infection. The invention also provides methods of inhibiting microbial growth and survival by applying an effective amount of a 4-substituted-1H-isothiazolo[5,4-b][1,4]oxazino[2,3,4-ij]quinoline-7,8(2H,9H)-dione or related compound.
摘要翻译：本发明提供具有抗微生物活性的具有下式的化合物。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。本文提供的具体化合物也是微生物DNA合成和繁殖的有效和/或选择性抑制剂。本发明提供包含本发明化合物和一种或多种或多种载体的抗微生物组合物，包括药物组合物。本发明提供含有4-取代-1H-异噻唑并[5,4-b] [1,4]恶嗪并[2,3,4-ij]喹啉-7,8（2H，9H） - 二酮或相关化合物作为唯一的活性剂或与一种或多种其它活性剂组合。本发明通过施用有效量的4-取代的1H-异噻唑并[5,4-b] [1,4]恶嗪并[2,3,4-ij]，提供了治疗或预防微生物感染，优选动物的方法。喹啉-7,8（2H，9H） - 二酮或相关化合物与患有或易感微生物感染的生物体接触。本发明还提供了通过应用有效量的4-取代的1H-异噻唑并[5,4-b] [1,4]恶嗪并[2,3,4-ij]喹啉-7 ，8（2H，9H） - 二酮或相关化合物。

9. 发明申请

US20110213152A1 METHOD FOR SYNTHESIS OF 8-ALKOXY-9H-ISOTHIAZOLO[5,4-B]QUINOLINE-3,4-DIONES 有权
标题翻译：合成8-羟基-9-异亮氨酸[5,4-B]喹啉-3,4-二酮的方法
公开(公告)号：US20110213152A1
公开(公告)日：2011-09-01
申请号：US13040369
申请日：2011-03-04
申请人： Barton James Bradbury , Jason Allan Wiles , Akihiro Hashimoto , Qiuping Wang , Edlaine Lucien , Godwin Pais , Ha Young Kim
发明人： Barton James Bradbury , Jason Allan Wiles , Akihiro Hashimoto , Qiuping Wang , Edlaine Lucien , Godwin Pais , Ha Young Kim
IPC分类号： C07D401/04 , C07D417/14 , C07D413/14 , C07D498/04
CPC分类号： C07D215/28 , C07D401/04 , C07D513/04
摘要： The present invention provides process for synthesis of 8-methoxy-9H-isothiazolo[5,4-b]quinoline-3,4-diones and 8A,9-dihydro-4aH-isothiazolo[5,4-b]quinoline-3,4-diones of the Formula A. The substituents R, R5, R6, R7, R8 and R9 are defined herein. The invention also provides novel synthetic intermediates useful in the synthesis of 8-methoxy-9H-isothiazolo[5,4-b]quinoline-3,4-diones and 8A,9-dihydro-4aH-isothiazolo[5,4-b]quinoline-3,4-diones.
摘要翻译：本发明提供8-甲氧基-9H-异噻唑并[5,4-b]喹啉-3,4-二酮和8A,9-二氢-4a-异噻唑并[5,4-b]喹啉-3的合成方法，取代基R，R 5，R 6，R 7，R 8和R 9在本文中定义。本发明还提供了用于合成8-甲氧基-9H-异噻唑并[5,4-b]喹啉-3,4-二酮和8A,9-二氢-4a-异噻唑并[5,4-b] 喹啉-3,4-二酮。

10. 发明授权

US08138346B2 Method for synthesis of 8-alkoxy-9H-isothiazolo[5,4-B]quinoline-3,4-diones 有权
标题翻译： 8-烷氧基-9H-异噻唑并[5,4-B]喹啉-3,4-二酮的合成方法
公开(公告)号：US08138346B2
公开(公告)日：2012-03-20
申请号：US13040369
申请日：2011-03-04
申请人： Barton James Bradbury , Jason Allan Wiles , Akihiro Hashimoto , Qiuping Wang , Edlaine Lucien , Godwin Pais , Ha Young Kim
发明人： Barton James Bradbury , Jason Allan Wiles , Akihiro Hashimoto , Qiuping Wang , Edlaine Lucien , Godwin Pais , Ha Young Kim
IPC分类号： C07D215/38
CPC分类号： C07D215/28 , C07D401/04 , C07D513/04
摘要： The present invention provides process for synthesis of 8-methoxy-9H-isothiazolo[5,4-b]quinoline-3,4-diones and 8A,9-dihydro-4aH-isothiazolo[5,4-b]quinoline-3,4-diones of the Formula A. The substituents R, R5, R6, R7, R8 and R9 are defined herein. The invention also provides novel synthetic intermediates useful in the synthesis of 8-methoxy-9H-isothiazolo[5,4-b]quinoline-3,4-diones and 8A,9-dihydro-4aH-isothiazolo[5,4-b]quinoline-3,4-diones.
摘要翻译：本发明提供8-甲氧基-9H-异噻唑并[5,4-b]喹啉-3,4-二酮和8A,9-二氢-4a-异噻唑并[5,4-b]喹啉-3的合成方法，取代基R，R 5，R 6，R 7，R 8和R 9在本文中定义。本发明还提供了用于合成8-甲氧基-9H-异噻唑并[5,4-b]喹啉-3,4-二酮和8A,9-二氢-4a-异噻唑并[5,4-b] 喹啉-3,4-二酮。

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