公开(公告)号：US07485633B2

公开(公告)日：2009-02-03

申请号：US11684710

申请日：2007-03-12

申请人： Nicholas A. Meanwell ,  Robert G. Gentles ,  Min Ding ,  John A. Bender ,  John F. Kadow ,  Piyasena Hewawasam ,  Thomas W. Hudyma ,  Xiaofan Zheng

发明人： Nicholas A. Meanwell ,  Robert G. Gentles ,  Min Ding ,  John A. Bender ,  John F. Kadow ,  Piyasena Hewawasam ,  Thomas W. Hudyma ,  Xiaofan Zheng

IPC分类号： A61K31/55 ,  A61P31/00 ,  C07D223/14

CPC分类号： C07D487/04

摘要： The invention encompasses compounds of Formula I, pharmaceutically acceptable salts thereof, compositions, and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and are useful in treating those infected with HCV.

摘要翻译： 本发明包括式I的化合物，其药学上可接受的盐，组合物和使用该化合物的方法。 该化合物具有抗丙型肝炎病毒（HCV）的活性，可用于治疗HCV感染者。

公开(公告)号：US20110020275A1

公开(公告)日：2011-01-27

申请号：US12922722

申请日：2009-03-25

申请人： Kap-Sun Yeung ,  Ying Han ,  John F. Kadow

发明人： Kap-Sun Yeung ,  Ying Han ,  John F. Kadow

IPC分类号： A61K38/20 ,  C07D487/04 ,  A61K31/55 ,  A61K38/21 ,  A61K38/13 ,  A61P31/14

CPC分类号： C07D487/04

摘要： The disclosure provides compounds of formula (I), including their salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV.

摘要翻译： 本公开提供式（I）化合物，包括其盐，以及使用该化合物的组合物和方法。 该化合物具有抗丙型肝炎病毒（HCV）的活性，可用于治疗HCV感染者。

公开(公告)号：US08178523B2

公开(公告)日：2012-05-15

申请号：US12922722

申请日：2009-03-25

申请人： Kap-Sun Yeung ,  Ying Han ,  John F. Kadow

发明人： Kap-Sun Yeung ,  Ying Han ,  John F. Kadow

IPC分类号： A61P31/12 ,  A61K31/55 ,  C07D487/04

CPC分类号： C07D487/04

摘要： The disclosure provides compounds of formula (I), including their salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV.

摘要翻译： 本公开提供式（I）化合物，包括其盐，以及使用该化合物的组合物和方法。 该化合物具有抗丙型肝炎病毒（HCV）的活性，可用于治疗HCV感染者。

公开(公告)号：US20080132516A1

公开(公告)日：2008-06-05

申请号：US12028189

申请日：2008-02-08

申请人： Kap-Sun Yeung ,  Michelle E. Farkas ,  John F. Kadow ,  Nicholas A. Meanwell ,  Malcolm Taylor ,  David Johnston ,  Thomas Stephen Coulter ,  J.J Kim Wright

发明人： Kap-Sun Yeung ,  Michelle E. Farkas ,  John F. Kadow ,  Nicholas A. Meanwell ,  Malcolm Taylor ,  David Johnston ,  Thomas Stephen Coulter ,  J.J Kim Wright

IPC分类号： A61K31/496 ,  C07D401/14 ,  A61P31/18

CPC分类号： C07D413/14 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D471/04 ,  C07D491/04

摘要： This invention provides compounds of Formula I, including pharmaceutically acceptable salts thereof, having drug and bio-affecting properties, their pharmaceutical compositions and method of use. These compounds possess unique antiviral activity, whether used alone or in combination with other antivirals, antiinfectives, immunomodulators or HIV entry inhibitors. More particularly, the present invention relates to the treatment of HIV and AIDS. The compounds of Formula I have the formula wherein: Z is Q is selected from the group consisting of m is 2; A is selected from the group consisting of cinnolinyl, napthyridinyl, quinoxalinyl, pyridinyl, pyrimidinyl, quinolinyl, isoquinolinyl, quinazolinyl, azabenzofuryl, and phthalazinyl each of which may be optionally substituted with one or two groups independently selected from methyl, methoxy, hydroxy, amino and halogen; and —W— is

摘要翻译： 本发明提供具有药物和生物影响性质的式I化合物，包括其药学上可接受的盐，其药物组合物和使用方法。 这些化合物具有独特的抗病毒活性，无论是单独使用还是与其他抗病毒药，抗感染剂，免疫调节剂或HIV进入抑制剂组合使用。 更具体地说，本发明涉及艾滋病毒和艾滋病的治疗。 式I的化合物具有下式：其中：Z为Q选自m为2; A选自噌啉基，萘啶基，喹喔啉基，吡啶基，嘧啶基，喹啉基，异喹啉基，喹唑啉基，氮杂苯并呋喃基和酞嗪基，其各自可以任选被一个或两个独立地选自甲基，甲氧基，羟基，氨基 和卤素; 和-W-是

公开(公告)号：US08507683B2

公开(公告)日：2013-08-13

申请号：US13310863

申请日：2011-12-05

申请人： Kap-Sun Yeung ,  John F. Kadow ,  Rajesh Onkardas Bora ,  Kumaravel Selvakumar

发明人： Kap-Sun Yeung ,  John F. Kadow ,  Rajesh Onkardas Bora ,  Kumaravel Selvakumar

IPC分类号： C07D471/04 ,  A61K31/437

CPC分类号： C07D405/14 ,  C07D407/12

摘要： The disclosure provides compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV.

公开(公告)号：US08168615B2

公开(公告)日：2012-05-01

申请号：US12767222

申请日：2010-04-26

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： A01N57/00 ,  A61K31/675 ,  C07D401/00

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。

公开(公告)号：US08039486B2

公开(公告)日：2011-10-18

申请号：US12028189

申请日：2008-02-08

申请人： Kap-Sun Yeung ,  Michelle E. Farkas ,  John F. Kadow ,  Nicholas A. Meanwell ,  Malcolm Taylor ,  David Johnston ,  Thomas Stephen Coulter ,  J. J. Kim Wright

发明人： Kap-Sun Yeung ,  Michelle E. Farkas ,  John F. Kadow ,  Nicholas A. Meanwell ,  Malcolm Taylor ,  David Johnston ,  Thomas Stephen Coulter ,  J. J. Kim Wright

IPC分类号： A61K31/04 ,  C07D215/38

CPC分类号： C07D413/14 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D471/04 ,  C07D491/04

摘要： This invention provides compounds of Formula I, including pharmaceutically acceptable salts thereof, having drug and bio-affecting properties, their pharmaceutical compositions and method of use. These compounds possess unique antiviral activity, whether used alone or in combination with other antivirals, antiinfectives, immunomodulators or HIV entry inhibitors. More particularly, the present invention relates to the treatment of HIV and AIDS. The compounds of Formula I have the formula wherein: Z is Q is selected from the group consisting of m is 2; A is selected from the group consisting of cinnolinyl, napthyridinyl, quinoxalinyl, pyridinyl, pyrimidinyl, quinolinyl, isoquinolinyl, quinazolinyl, azabenzofuryl, and phthalazinyl each of which may be optionally substituted with one or two groups independently selected from methyl, methoxy, hydroxy, amino and halogen; and —W— is

摘要翻译： 本发明提供具有药物和生物影响性质的式I化合物，包括其药学上可接受的盐，其药物组合物和使用方法。 这些化合物具有独特的抗病毒活性，无论是单独使用还是与其他抗病毒药，抗感染剂，免疫调节剂或HIV进入抑制剂组合使用。 更具体地说，本发明涉及艾滋病毒和艾滋病的治疗。 式I的化合物具有下式：其中：Z为Q选自m为2; A选自噌啉基，萘啶基，喹喔啉基，吡啶基，嘧啶基，喹啉基，异喹啉基，喹唑啉基，氮杂苯并呋喃基和酞嗪基，其各自可以任选被一个或两个独立地选自甲基，甲氧基，羟基，氨基 和卤素; 和-W-是

公开(公告)号：US20080188458A1

公开(公告)日：2008-08-07

申请号：US12022541

申请日：2008-01-30

申请人： Kap-Sun Yeung ,  John F. Kadow ,  Katharine A. Grant-Young

发明人： Kap-Sun Yeung ,  John F. Kadow ,  Katharine A. Grant-Young

IPC分类号： A61K31/55 ,  C07D223/32 ,  A61P31/12

CPC分类号： C07D487/04 ,  C07D519/00

摘要： The invention encompasses compounds of formula I as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and are useful in treating those infected with HCV.

公开(公告)号：US08461333B2

公开(公告)日：2013-06-11

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： C07F9/02

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。

公开(公告)号：US20120059019A1

公开(公告)日：2012-03-08

申请号：US13043747

申请日：2011-03-09

申请人： Kap-Sun Yeung ,  Katharine A. Grant-Young ,  John F. Kadow

发明人： Kap-Sun Yeung ,  Katharine A. Grant-Young ,  John F. Kadow

IPC分类号： A61K31/519 ,  A61P31/14 ,  C07D498/04 ,  C07D471/04 ,  A61K31/4375 ,  A61K31/437

CPC分类号： C07D471/04 ,  C07D498/04

摘要： The disclosure provides compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV.