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公开(公告)号：US20120010222A1
公开(公告)日：2012-01-12
申请号：US13234634
申请日：2011-09-16
申请人： Paul Charifson , David Deininger , Anne-Laure Grillot , Yusheng Liao , Steven Ronkin , Dean Stamos , Emanuele Perola , Tiansheng Wang , Arnaud Le Tiran , Joseph Drumm
发明人： Paul Charifson , David Deininger , Anne-Laure Grillot , Yusheng Liao , Steven Ronkin , Dean Stamos , Emanuele Perola , Tiansheng Wang , Arnaud Le Tiran , Joseph Drumm
IPC分类号： A61K31/506 , A61K31/4184 , A61P31/04 , A61K31/4439
CPC分类号： C07D413/14 , A61K31/4439 , A61K31/506 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/04 , C07D405/14 , C07D417/14 , C07D471/04 , C07D487/04 , C07D491/04
摘要： The present invention relates to methods of treating, preventing, or lessening the severity of resistant bacterial infections in mammals, utilizing compounds of formula I or formula VII or pharmaceutically salts thereof. The present invention also relates to methods of using compounds of formula I or formula VII in combination with one or more additional antibacterial agents and/or one or more additional therapeutic agents that increase the susceptibility of bacterial organisms to antibiotics.
摘要翻译： 本发明涉及使用式I或式VII化合物或其药学上可接受的方法治疗，预防或减轻哺乳动物中抗性细菌感染的严重性。 本发明还涉及使用式I或式VII化合物与一种或多种另外的抗菌剂和/或一种或多种增加细菌生物体对抗生素敏感性的其它治疗剂的组合的方法。
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公开(公告)号：US08188095B2
公开(公告)日：2012-05-29
申请号：US12246778
申请日：2008-10-07
申请人： Paul Charifson , David Deininger , Anne-Laure Grillot , Yusheng Liao , Steven Ronkin , Dean Stamos , Emanuele Perola , Tiansheng Wang , Arnaud Le Tiran , Joseph Drumm
发明人： Paul Charifson , David Deininger , Anne-Laure Grillot , Yusheng Liao , Steven Ronkin , Dean Stamos , Emanuele Perola , Tiansheng Wang , Arnaud Le Tiran , Joseph Drumm
IPC分类号： A61K31/44 , C07D401/04 , C07D401/14
CPC分类号： C07D401/14 , C07D403/04 , C07D403/14 , C07D405/04 , C07D405/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D487/04 , C07D491/04
摘要： The present invention relates to compounds which inhibit bacterial gyrase and/or Topo IV and pharmaceutically acceptable compositions comprising said compounds. These compounds, and compositions thereof, are useful in treating bacterial infection. Accordingly, the present invention also relates to methods for treating bacterial infections in mammals.
摘要翻译： 本发明涉及抑制细菌促旋酶和/或Topo IV的化合物和包含所述化合物的药学上可接受的组合物。 这些化合物及其组合物可用于治疗细菌感染。 因此，本发明还涉及用于治疗哺乳动物细菌感染的方法。
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公开(公告)号：US20090325955A1
公开(公告)日：2009-12-31
申请号：US12483312
申请日：2009-06-12
申请人： PAUL Charifson , David Deininger , Anne-Laure Grillot , Yusheng Liao , Steven Ronkin , Dean Stamos , Emanuele Perola , Tiansheng Wang , Arnaud Le Tiran , Joseph Drumm
发明人： PAUL Charifson , David Deininger , Anne-Laure Grillot , Yusheng Liao , Steven Ronkin , Dean Stamos , Emanuele Perola , Tiansheng Wang , Arnaud Le Tiran , Joseph Drumm
IPC分类号： A61K31/506 , A61K31/5377 , A61P31/04 , A61K31/519 , A61K31/4439 , A61K31/4184
CPC分类号： A61K31/4439 , A61K31/506 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/04 , C07D405/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D487/04 , C07D491/04
摘要： The present invention relates to methods of treating, preventing, or lessening the severity of resistant bacterial infections in mammals, utilizing compounds of formula I or formula VII or pharmaceutically salts thereof. The present invention also relates to methods of using compounds of formula I or formula VII in combination with one or more additional antibacterial agents and/or one or more additional therapeutic agents that increase the susceptibility of bacterial organisms to antibiotics.
摘要翻译： 本发明涉及使用式I或式VII化合物或其药学上可接受的方法治疗，预防或减轻哺乳动物中抗性细菌感染的严重性。 本发明还涉及使用式I或式VII化合物与一种或多种另外的抗菌剂和/或一种或多种增加细菌生物体对抗生素敏感性的其它治疗剂的组合的方法。
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公开(公告)号：USRE40245E1
公开(公告)日：2008-04-15
申请号：US10833995
申请日：2004-04-28
申请人： Anne-Laure Grillot , Paul S. Charifson , Dean Stamos , Yusheng Liao , Michael C. Badia , Martin Trudeau
发明人： Anne-Laure Grillot , Paul S. Charifson , Dean Stamos , Yusheng Liao , Michael C. Badia , Martin Trudeau
IPC分类号： C07D403/04 , C07D413/04 , C07D235/30 , A61K31/55
CPC分类号： C07D403/12 , A61K31/00 , A61K31/4184 , A61K31/423 , A61K31/437 , A61K31/4439 , A61K31/4709 , A61K31/506 , A61K31/5377 , A61K31/55 , A61K45/06 , C07D231/12 , C07D233/56 , C07D235/30 , C07D249/08 , C07D263/58 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/04 , C07D405/14 , C07D409/04 , C07D413/04 , C07D471/04 , C07D471/14 , C07D491/04 , C07F9/65583 , C07F9/6561 , Y02A50/393 , Y02A50/473 , A61K2300/00
摘要： The present invention relates to compounds of the formula I: or a pharmaceutically acceptable derivative or prodrug thereof. The compounds are useful as inhibitors of bacterial gyrase activity. The present invention also relates to methods for treating bacterial infections in mammala. The present invention also relates to methods for decreasing bacterial quantity in a biological sample.
摘要翻译： 本发明涉及式I化合物或其药学上可接受的衍生物或前药。 这些化合物可用作细菌回旋酶活性的抑制剂。 本发明还涉及用于治疗哺乳动物细菌感染的方法。 本发明还涉及生物样品中细菌数量减少的方法。
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公开(公告)号：US08426426B2
公开(公告)日：2013-04-23
申请号：US12761576
申请日：2010-04-16
申请人： Paul Charifson , David Deininger , Joseph Drumm , Anne-Laure Grillot , Yusheng Liao , Patricia Oliver-Shaffer , Dean Stamos
发明人： Paul Charifson , David Deininger , Joseph Drumm , Anne-Laure Grillot , Yusheng Liao , Patricia Oliver-Shaffer , Dean Stamos
IPC分类号： C07D239/42 , C07D239/00 , C07D401/00 , A61K31/505 , A61K31/44
CPC分类号： C07D401/04 , A61K31/4439 , A61K31/444 , A61K31/506 , A61K45/06 , C07C275/06 , C07D401/14 , C07D403/04 , Y02A50/473 , Y02A50/478 , A61K2300/00
摘要： The present invention relates to compounds which inhibit bacterial gyrase and pharmaceutically acceptable compositions comprising said compounds. These compounds, and compositions thereof, are useful in treating bacterial infection. Accordingly, the present invention also relates to methods for treating bacterial infections in mammals. The present invention also relates to a method for preparing these compounds.
摘要翻译： 本发明涉及抑制细菌促旋酶的化合物和包含所述化合物的药学上可接受的组合物。 这些化合物及其组合物可用于治疗细菌感染。 因此，本发明还涉及用于治疗哺乳动物细菌感染的方法。 本发明还涉及一种制备这些化合物的方法。
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公开(公告)号：US20120184512A1
公开(公告)日：2012-07-19
申请号：US13349789
申请日：2012-01-13
申请人： Arnaud Le Tiran , Anne-Laure Grillot , Paul S. Charifson , Yousef Laafiret Bennani , Hardwin O'Dowd , Emanuele Perola
发明人： Arnaud Le Tiran , Anne-Laure Grillot , Paul S. Charifson , Yousef Laafiret Bennani , Hardwin O'Dowd , Emanuele Perola
IPC分类号： A61K31/506 , C07F9/09 , A61P31/04 , A01N43/54 , A01N57/16 , A01P1/00 , C07D405/14 , A61K31/675
CPC分类号： C07D405/14 , C07F9/65586
摘要： The present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof wherein X and R are as defined herein. The compounds of formula (I) are useful as gyrase and/or topoisomerase IV inhibitors for treating bacterial infections. The compounds of formula (I) either possess a broad range of anti-bacterial activity and advantageous toxicological properties or are prodrugs of compounds having said activity.
摘要翻译： 本发明涉及式（I）化合物或其药学上可接受的盐，其中X和R如本文所定义。 式（I）的化合物可用作用于治疗细菌感染的旋转酶和/或拓扑异构酶IV抑制剂。 式（I）化合物具有广泛的抗菌活性和有利的毒理特性，或具有所述活性的化合物的前药。
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公开(公告)号：US08481551B2
公开(公告)日：2013-07-09
申请号：US13349789
申请日：2012-01-13
申请人： Arnaud Le Tiran , Anne-Laure Grillot , Paul S. Charifson , Yousef Laafiret Bennani , Hardwin O'Dowd , Emanuele Perola
发明人： Arnaud Le Tiran , Anne-Laure Grillot , Paul S. Charifson , Yousef Laafiret Bennani , Hardwin O'Dowd , Emanuele Perola
IPC分类号： A01N43/54 , C07D239/42 , C07D471/04
CPC分类号： C07D405/14 , C07F9/65586
摘要： The present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof wherein X and R are as defined herein. The compounds of formula (I) are useful as gyrase and/or topoisomerase IV inhibitors for treating bacterial infections. The compounds of formula (I) either possess a broad range of anti-bacterial activity and advantageous toxicological properties or are prodrugs of compounds having said activity.
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公开(公告)号：US07414046B2
公开(公告)日：2008-08-19
申请号：US10444588
申请日：2003-05-23
申请人： Anne-Laure Grillot , Paul Charifson , Dean Stamos , Yusheng Liao , Michael Badia , Martin Trudeau
发明人： Anne-Laure Grillot , Paul Charifson , Dean Stamos , Yusheng Liao , Michael Badia , Martin Trudeau
IPC分类号： C07D403/04 , C07D413/04 , C07D235/30 , A61K31/55
CPC分类号： C07D403/12 , A61K31/00 , A61K31/4184 , A61K31/423 , A61K31/437 , A61K31/4439 , A61K31/4709 , A61K31/506 , A61K31/5377 , A61K31/55 , A61K45/06 , C07D231/12 , C07D233/56 , C07D235/30 , C07D249/08 , C07D263/58 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/04 , C07D405/14 , C07D409/04 , C07D413/04 , C07D471/04 , C07D471/14 , C07D491/04 , C07F9/65583 , C07F9/6561 , Y02A50/393 , Y02A50/473 , A61K2300/00
摘要： The present invention relates to compounds of the formula I: or a pharmaceutically acceptable derivative or prodrug thereof. The compounds are useful as inhibitors of bacterial gyrase activity. The present invention also relates to methods for treating bacterial infections in mammala. The present invention also relates to methods for decreasing bacterial quantity in a biological sample.
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公开(公告)号：US06632809B2
公开(公告)日：2003-10-14
申请号：US10015332
申请日：2001-12-12
申请人： Anne-Laure Grillot , Paul Charifson , Dean Stamos , Yusheng Liao , Michael Badia , Martin Trudeau
发明人： Anne-Laure Grillot , Paul Charifson , Dean Stamos , Yusheng Liao , Michael Badia , Martin Trudeau
IPC分类号： C07D40304
CPC分类号： C07D403/12 , A61K31/00 , A61K31/4184 , A61K31/423 , A61K31/437 , A61K31/4439 , A61K31/4709 , A61K31/506 , A61K31/5377 , A61K31/55 , A61K45/06 , C07D231/12 , C07D233/56 , C07D235/30 , C07D249/08 , C07D263/58 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/04 , C07D405/14 , C07D409/04 , C07D413/04 , C07D471/04 , C07D471/14 , C07D491/04 , C07F9/65583 , C07F9/6561 , Y02A50/393 , Y02A50/473 , A61K2300/00
摘要： The present invention relates to compounds of the formula I: or a pharmaceutically acceptable derivative or prodrug thereof. The compounds are useful as inhibitors of bacterial gyrase activity. The present invention also relates to methods for treating bacterial infections in mammala. The present invention also relates to methods for decreasing bacterial quantity in a biological sample.
摘要翻译： 本发明涉及式I化合物或其药学上可接受的衍生物或前药。 这些化合物可用作细菌回旋酶活性的抑制剂。 本发明还涉及用于治疗哺乳动物细菌感染的方法。 本发明还涉及用于降低生物样品中细菌数量的方法
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公开(公告)号：US08372873B2
公开(公告)日：2013-02-12
申请号：US13074772
申请日：2011-03-29
申请人： Kevin M. Cottrell , John Maxwell , Qing Tang , Anne-Laure Grillot , Arnaud Le Tiran , Emanuele Perola
发明人： Kevin M. Cottrell , John Maxwell , Qing Tang , Anne-Laure Grillot , Arnaud Le Tiran , Emanuele Perola
IPC分类号： A61K31/42 , A61K31/4245 , A61K31/4439 , A61K31/454 , A61K31/4725
CPC分类号： C07D498/10
摘要： The present invention relates to compounds of formula (I): or a pharmaceutically acceptable salt thereof. These compounds inhibit serine protease, particularly the hepatitis C virus NS3-NS4A protease.
摘要翻译： 本发明涉及式（I）化合物或其药学上可接受的盐。 这些化合物抑制丝氨酸蛋白酶，特别是丙型肝炎病毒NS3-NS4A蛋白酶。
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