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公开(公告)号：US08383639B2
公开(公告)日：2013-02-26
申请号：US12901147
申请日：2010-10-08
申请人： B. Narasimhulu Naidu , Kevin Peese , Ira B. Dicker , Chen Li , Manoj Patel , Nicholas A. Meanwell , Michael A. Walker
发明人： B. Narasimhulu Naidu , Kevin Peese , Ira B. Dicker , Chen Li , Manoj Patel , Nicholas A. Meanwell , Michael A. Walker
IPC分类号： A01N43/54 , A61K31/505
CPC分类号： C07D498/04 , C07D413/04
摘要： The disclosure generally relates to the novel compounds of formula I, including their salts, which inhibit HIV integrase and prevent viral integration into human DNA. This action makes the compounds useful for treating HIV infection and AIDS. The invention also encompasses pharmaceutical compositions and methods for treating those infected with HIV.
摘要翻译： 本公开一般涉及式I的新化合物，包括其盐，其抑制HIV整合酶并防止病毒整合入人DNA。 这种作用使这些化合物可用于治疗艾滋病毒和艾滋病。 本发明还包括用于治疗感染HIV的那些的药物组合物和方法。
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公开(公告)号：US20110245241A1
公开(公告)日：2011-10-06
申请号：US12901147
申请日：2010-10-08
申请人： B. Narasimhulu Naidu , Kevin Peese , Ira B. Dicker , Chen Li , Manoj Patel , Nicholas A. Meanwell , Michael A. Walker
发明人： B. Narasimhulu Naidu , Kevin Peese , Ira B. Dicker , Chen Li , Manoj Patel , Nicholas A. Meanwell , Michael A. Walker
IPC分类号： A61K31/5383 , C07D498/04 , C07D413/04 , A61K31/506 , C07D413/14 , A61K31/5377 , A61P31/18
CPC分类号： C07D498/04 , C07D413/04
摘要： The disclosure generally relates to the novel compounds of formula I, including their salts, which inhibit HIV integrase and prevent viral integration into human DNA. This action makes the compounds useful for treating HIV infection and AIDS. The invention also encompasses pharmaceutical compositions and methods for treating those infected with HIV.
摘要翻译： 本公开一般涉及式I的新化合物，包括其盐，其抑制HIV整合酶并防止病毒整合入人DNA。 这种作用使这些化合物可用于治疗艾滋病毒和艾滋病。 本发明还包括用于治疗感染HIV的那些的药物组合物和方法。
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公开(公告)号：US08129398B2
公开(公告)日：2012-03-06
申请号：US12406268
申请日：2009-03-18
申请人： Francis Beaulieu , Carl Ouellet , B. Narasimhulu Naidu , Manoj Patel , Yasutsugu Ueda , Timothy P. Connolly , Jonathan R. Weiss , Michael A. Walker , Nicholas A. Meanwell , Kevin M. Peese , Margaret E. Sorenson , Chen Li
发明人： Francis Beaulieu , Carl Ouellet , B. Narasimhulu Naidu , Manoj Patel , Yasutsugu Ueda , Timothy P. Connolly , Jonathan R. Weiss , Michael A. Walker , Nicholas A. Meanwell , Kevin M. Peese , Margaret E. Sorenson , Chen Li
IPC分类号： A61K31/505 , C07D487/12
CPC分类号： C07D498/18 , C07D471/08 , C07D471/18 , C07D487/08 , C07D493/18
摘要： The disclosure generally relates to the novel compounds of formula I, including their salts, which inhibit HIV integrase and prevent viral integration into human DNA. This action makes the compounds useful for treating HIV infection and AIDS. The invention also encompasses pharmaceutical compositions and methods for treating those infected with HIV.
摘要翻译： 本公开一般涉及式I的新化合物，包括其盐，其抑制HIV整合酶并防止病毒整合入人DNA。 这种作用使这些化合物可用于治疗艾滋病毒和艾滋病。 本发明还包括用于治疗感染HIV的那些的药物组合物和方法。
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公开(公告)号：US20090253677A1
公开(公告)日：2009-10-08
申请号：US12406268
申请日：2009-03-18
申请人： Francis Beaulieu , Carl Ouellet , B. Narasimhulu Naidu , Manoj Patel , Yasutsugu Ueda , Timothy P. Connolly , Jonathan R. Weiss , Michael A. Walker , Nicholas A. Meanwell , Kevin M. Peese , Margaret E. Sorenson
发明人： Francis Beaulieu , Carl Ouellet , B. Narasimhulu Naidu , Manoj Patel , Yasutsugu Ueda , Timothy P. Connolly , Jonathan R. Weiss , Michael A. Walker , Nicholas A. Meanwell , Kevin M. Peese , Margaret E. Sorenson
IPC分类号： A61K31/551 , A61K31/55 , A61K31/537 , A61K31/529 , C07D487/14 , C07D487/04 , C07D498/18 , C07D471/04
CPC分类号： C07D498/18 , C07D471/08 , C07D471/18 , C07D487/08 , C07D493/18
摘要： The disclosure generally relates to the novel compounds of formula I, including their salts, which inhibit HIV integrase and prevent viral integration into human DNA. This action makes the compounds useful for treating HIV infection and AIDS. The invention also encompasses pharmaceutical compositions and methods for treating those infected with HIV.
摘要翻译： 本公开一般涉及式I的新化合物，包括其盐，其抑制HIV整合酶并防止病毒整合入人DNA。 这种作用使这些化合物可用于治疗艾滋病毒和艾滋病。 本发明还包括用于治疗感染HIV的那些的药物组合物和方法。
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公开(公告)号：US06803378B2
公开(公告)日：2004-10-12
申请号：US10254365
申请日：2002-09-25
IPC分类号： C07D31700
CPC分类号： C07D213/30 , C07C59/90 , C07C235/28 , C07C235/74 , C07C237/42 , C07C311/51 , C07C2601/02 , C07D213/38 , C07D213/40 , C07D307/52 , C07D317/34 , C07D317/40 , C07D317/46 , C07D317/58 , C07D333/20 , C07D405/12 , C07D407/12
摘要： Novel diketoacid compounds of Formula I are provided which are useful as HIV integrase inhibitors and for the treatment of AIDS or ARC.
摘要翻译： 提供式I的新型二酮酸化合物，其可用作HIV整合酶抑制剂和用于治疗AIDS或ARC。
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公开(公告)号：US08691757B2
公开(公告)日：2014-04-08
申请号：US13492982
申请日：2012-06-11
申请人： Ramkumar Rajamani , Kishore V. Renduchintala , Kandhasamy Sarkunam , Pulicharla Nagalakshmi , Nicholas A. Meanwell , Paul Michael Scola
发明人： Ramkumar Rajamani , Kishore V. Renduchintala , Kandhasamy Sarkunam , Pulicharla Nagalakshmi , Nicholas A. Meanwell , Paul Michael Scola
CPC分类号： A61K38/06 , A61K38/2013 , A61K38/204 , A61K38/208 , A61K38/21 , A61K38/212 , C07D401/12 , C07D487/04 , C07K5/02 , C07K5/0804
摘要： Hepatitis C virus inhibitors having the general formula (I) are disclosed. Compositions comprising the compounds and methods for using the compounds to inhibit HCV are also disclosed.
摘要翻译： 公开了具有通式（I）的丙型肝炎病毒抑制剂。 还公开了包含化合物的组合物和使用该化合物抑制HCV的方法。
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公开(公告)号：US08664213B2
公开(公告)日：2014-03-04
申请号：US13596211
申请日：2012-08-28
IPC分类号： A01N43/00 , A61K31/00 , A01N43/38 , A61K31/40 , C07D209/96 , C07D487/00 , C07D491/00 , C07D495/00 , C07D205/00
CPC分类号： C07D471/04 , C07D519/00
摘要： Compounds of Formula I, including pharmaceutically acceptable salts thereof: wherein A is selected from the group consisting of: are useful as HIV attachment inhibitors.
摘要翻译： 式I化合物，包括其药学上可接受的盐：其中A选自：可用作HIV附着抑制剂。
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公开(公告)号：US20130252968A1
公开(公告)日：2013-09-26
申请号：US13990815
申请日：2011-12-01
申请人： Tao Wang , Zhongxing Zhang , Zhiwei Yin , John F. Kadow , Nicholas A. Meanwell
发明人： Tao Wang , Zhongxing Zhang , Zhiwei Yin , John F. Kadow , Nicholas A. Meanwell
IPC分类号： C07D471/04
CPC分类号： C07D471/04
摘要： Compounds of Formula (I), including pharmaceutically acceptable salts thereof, wherein A is selected from the group (II), are useful as HIV attachment inhibitors.
摘要翻译： 式（I）化合物，包括其药学上可接受的盐，其中A选自（II）组，可用作HIV附着抑制剂。
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9.发明授权公开(公告)号：US08450361B2
公开(公告)日：2013-05-28
申请号：US13198197
申请日：2011-08-04
申请人： Tao Wang , Zhongxing Zhang , Zhiwei Yin , John F. Kadow , Nicholas A. Meanwell
发明人： Tao Wang , Zhongxing Zhang , Zhiwei Yin , John F. Kadow , Nicholas A. Meanwell
IPC分类号： A61K31/4025 , A61K31/498 , A61K31/4439 , C07D209/40 , C07D403/06 , C07D401/06
CPC分类号： C07D401/06 , A61K31/437 , C07D209/40 , C07D471/04 , C07F5/025
摘要： Compounds having drug and bio-affecting properties are described herein, including their properties, pharmaceutical compositions and methods of use. In particular, tricyclic aryl or heteroaryl piperazine diamide derivatives that possess unique antiviral activity are set forth. These compounds are useful for the treatment of HIV and AIDS. The compounds herein have the general Formula I: wherein: Y is selected from the group of indole or azaindole systems: and Z is selected from the group of:
摘要翻译： 本文描述了具有药物和生物影响特性的化合物，包括其性质，药物组合物和使用方法。 特别地，阐述了具有独特抗病毒活性的三环芳基或杂芳基哌嗪二酰胺衍生物。 这些化合物可用于治疗艾滋病毒和艾滋病。 本文的化合物具有通式I：其中：Y选自吲哚或氮杂醇体系：Z选自：
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10.发明申请公开(公告)号：US20120238755A1
公开(公告)日：2012-09-20
申请号：US13429838
申请日：2012-03-26
申请人： YASUTSUGU UEDA , Timothy P. Connolly , John F. Kadow , Nicholas A. Meanwell , Tao Wang , Chung-Pin H. Chen , Kap-Sun Yeung , Zhongxing Zhang , David Kenneth Leahy , Shawn K. Pack , Nachimuthu Soundararajan , Pierre Sirard , Kathia Levesque , Dominique Thoraval
发明人： YASUTSUGU UEDA , Timothy P. Connolly , John F. Kadow , Nicholas A. Meanwell , Tao Wang , Chung-Pin H. Chen , Kap-Sun Yeung , Zhongxing Zhang , David Kenneth Leahy , Shawn K. Pack , Nachimuthu Soundararajan , Pierre Sirard , Kathia Levesque , Dominique Thoraval
IPC分类号： C07F9/6561
CPC分类号： A61K31/675 , A61K31/497 , A61K45/06 , C07D471/04 , C07F9/062 , C07F9/5728 , C07F9/65515 , C07F9/65586 , C07F9/6561
摘要： This invention provides for prodrug Compounds I, pharmaceutical compositions thereof, and their use in treating HIV infection. wherein: X is C or N with the proviso that when X is N, R1 does not exist; W is C or N with the proviso that when W is N, R2 does not exist; V is C; E is hydrogen or a pharmaceutically acceptable salt thereof; and Y is selected from the group consisting of Also, this invention provides for intermediate Compounds II useful in making prodrug Compounds I. wherein: L and M are independently selected from the group consisting of C1-C6 alkyl, phenyl, benzyl, trialkylsilyl, -2,2,2-trichloroethoxy and 2-trimethylsilylethoxy.
摘要翻译： 本发明提供前药化合物I，其药物组合物及其在治疗HIV感染中的用途。 其中：X为C或N，条件是当X为N时，R1不存在; W为C或N，条件是当W为N时，R2不存在; V是C; E是氢或其药学上可接受的盐; 并且Y选自本发明另外，本发明提供了可用于制备前药化合物I的中间体化合物II。其中：L和M独立地选自C 1 -C 6烷基，苯基，苄基，三烷基甲硅烷基， 2,2,2-三氯乙氧基和2-三甲基甲硅烷基乙氧基。
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