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公开(公告)号：US08026362B2
公开(公告)日：2011-09-27
申请号：US12156228
申请日：2008-05-30
IPC分类号： C07D239/02 , C07D233/00
CPC分类号： C07D239/22 , C07D233/72 , C07D233/78 , C07D239/54 , C07D239/545 , C07D239/553
摘要： Compounds of formula I, wherein R1, X1, X2 and A, are as defined herein or pharmaceutically acceptable salts thereof, inhibit HIV-1 reverse transcriptase and afford a method for prevention and treatment of HIV-1 infections and the treatment of AIDS and/or ARC. The present invention also relates to compositions containing compounds of formula I useful for the prevention and treatment of HIV-1 infections and the treatment of AIDS and/or ARC.
摘要翻译： 其中R 1，X 1，X 2和A如本文所定义的式I化合物或其药学上可接受的盐抑制HIV-1逆转录酶，并提供预防和治疗HIV-1感染的方法以及治疗AIDS和/ 或ARC。 本发明还涉及含有用于预防和治疗HIV-1感染和治疗AIDS和/或ARC的式I化合物的组合物。
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公开(公告)号：US20090076045A1
公开(公告)日：2009-03-19
申请号：US12156228
申请日：2008-05-30
IPC分类号： A61K31/513 , C07D239/54 , C07D233/74 , A61K31/4166 , A61P31/18
CPC分类号： C07D239/22 , C07D233/72 , C07D233/78 , C07D239/54 , C07D239/545 , C07D239/553
摘要： Compounds of formula I, wherein R1, X1, X2 and A, are as defined herein or pharmaceutically acceptable salts thereof, inhibit HIV-1 reverse transcriptase and afford a method for prevention and treatment of HIV-1 infections and the treatment of AIDS and/or ARC. The present invention also relates to compositions containing compounds of formula I useful for the prevention and treatment of HIV-1 infections and the treatment of AIDS and/or ARC.
摘要翻译： 其中R1，X1，X2和A如本文所定义的式I化合物或其药学上可接受的盐抑制HIV-1逆转录酶，并提供预防和治疗HIV-1感染的方法以及治疗AIDS和/ 或ARC。 本发明还涉及含有用于预防和治疗HIV-1感染和治疗AIDS和/或ARC的式I化合物的组合物。
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公开(公告)号：US07947709B2
公开(公告)日：2011-05-24
申请号：US12214651
申请日：2008-06-20
申请人： Todd Richard Elworthy , Joan Heather Hogg , Joshua Kennedy-Smith , Counde O'Yang , Mark Smith , Zachary Kevin Sweeney , Jeffrey Wu
发明人： Todd Richard Elworthy , Joan Heather Hogg , Joshua Kennedy-Smith , Counde O'Yang , Mark Smith , Zachary Kevin Sweeney , Jeffrey Wu
IPC分类号： A61K31/708 , A61K31/4184 , A61K31/437 , A61K31/5025 , A61P31/18 , C07D235/26 , C07D471/04 , C07D487/04
CPC分类号： C07D235/26 , C07D471/04 , C07D487/04
摘要： Compounds of formula I, wherein R1, R2, R3, X and Ar, are as defined herein or pharmaceutically acceptable salts thereof, inhibit HIV-1 reverse transcriptase and afford a method for prevention and treatment of HIV-1 infections and the treatment of AIDS and/or ARC. The present invention also relates to compositions containing compounds of formula I useful for the prevention and treatment of HIV-1 infections and the treatment of AIDS and/or ARC.
摘要翻译： 其中R 1，R 2，R 3，X和Ar如本文所定义的式I化合物或其药学上可接受的盐抑制HIV-1逆转录酶，并提供预防和治疗HIV-1感染和治疗AIDS的方法 和/或ARC。 本发明还涉及含有用于预防和治疗HIV-1感染和治疗AIDS和/或ARC的式I化合物的组合物。
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公开(公告)号：US20090012034A1
公开(公告)日：2009-01-08
申请号：US12214651
申请日：2008-06-20
申请人： Todd Richard Elworthy , Joan Heather Hogg , Joshua Kennedy-Smith , Counde O'Yang , Mark Smith , Zachary Kevin Sweeney , Jeffrey Wu
发明人： Todd Richard Elworthy , Joan Heather Hogg , Joshua Kennedy-Smith , Counde O'Yang , Mark Smith , Zachary Kevin Sweeney , Jeffrey Wu
IPC分类号： A61K31/708 , C07D235/26 , A61K31/4184 , C07D471/04 , A61P31/18 , A61K31/437 , A61K31/5025 , C07D487/04
CPC分类号： C07D235/26 , C07D471/04 , C07D487/04
摘要： Compounds of formula I, wherein R1, R2, R3, X and Ar, are as defined herein or pharmaceutically acceptable salts thereof, inhibit HIV-1 reverse transcriptase and afford a method for prevention and treatment of HIV-1 infections and the treatment of AIDS and/or ARC. The present invention also relates to compositions containing compounds of formula I useful for the prevention and treatment of HIV-1 infections and the treatment of AIDS and/or ARC.
摘要翻译： 其中R 1，R 2，R 3，X和Ar如本文所定义的式I化合物或其药学上可接受的盐抑制HIV-1逆转录酶，并提供预防和治疗HIV-1感染和治疗AIDS的方法 和/或ARC。 本发明还涉及含有用于预防和治疗HIV-1感染和治疗AIDS和/或ARC的式I化合物的组合物。
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公开(公告)号：US20090306041A1
公开(公告)日：2009-12-10
申请号：US12322870
申请日：2009-02-05
申请人： Nolan James Dewdney , Joshua Kennedy-Smith , Rama K. Kondru , Bradley E. Loc , Yan Lou , Joel McIntosh , Timothy D. Owens , Michael Soth , Zachary Kevin Sweeney , Joshua Paul Gergely Taygerly
发明人： Nolan James Dewdney , Joshua Kennedy-Smith , Rama K. Kondru , Bradley E. Loc , Yan Lou , Joel McIntosh , Timothy D. Owens , Michael Soth , Zachary Kevin Sweeney , Joshua Paul Gergely Taygerly
IPC分类号： A61K31/4725 , C07D413/14 , C07D401/14 , C07D417/14 , C07D491/107 , A61P29/00 , A61P37/00 , A61K31/496 , A61K31/5377 , A61K31/506 , A61K31/541 , A61P19/02 , A61P35/02
CPC分类号： A61K31/4725 , A61K31/496 , A61K31/506 , A61K31/5377 , A61K31/541 , C07D213/74
摘要： This application discloses 5-phenyl-1H-pyridin-2-one and 6-phenyl-2H-pyridazin-3-one derivatives according to generic Formulae I-III: wherein, variables R, X, Y1, Y2, Y3, Y4, n and m are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation such as rheumatoid arthritis. Also disclosed are compositions containing compounds of Formulae I-III and at least one carrier, diluent or excipient.
摘要翻译： 本申请公开了根据通式I-III的5-苯基-1H-吡啶-2-酮和6-苯基-2H-哒嗪-3-酮衍生物：其中，变量R，X，Y 1，Y 2，Y 3，Y 4， n和m定义如本文所述，其抑制Btk。 本文公开的化合物可用于调节Btk的活性并治疗与过量Btk活性相关的疾病。 该化合物还可用于治疗与异常B细胞增殖相关的炎症和自身免疫疾病，例如类风湿性关节炎。 还公开了含有式I-III化合物和至少一种载体，稀释剂或赋形剂的组合物。
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公开(公告)号：US20080045511A1
公开(公告)日：2008-02-21
申请号：US11893349
申请日：2007-08-15
IPC分类号： A61K31/415 , A61K31/341 , A61K31/416 , A61K31/427 , A61K31/437 , A61K31/472 , A61K31/4725 , A61K31/496 , A61K31/4985 , A61K31/50 , A61K31/5025 , A61K31/513 , A61K31/519 , A61K31/538 , A61K31/551 , A61K31/7068 , A61K31/7072 , A61K31/708 , A61P31/12 , A61P31/18 , C07D231/12 , C07D231/56 , C07D237/14 , C07D471/04 , C07D487/04
CPC分类号： C07D471/04 , C07D231/12 , C07D231/56 , C07D487/04
摘要： The present invention provides for compounds useful for treating an HIV infection, or preventing an HIV infection, or treating AIDS or ARC. The compounds of the invention are of formula I wherein A is A1, A2, A3 or A4 and R1, R2, R3, R4a, R4b, R5, R6, Ar, X1, X2, X4, X4 and X5 are as herein defined. Also disclosed in the present invention are methods of treating an HIV infection with compounds defined herein and pharmaceutical compositions containing said compounds.
摘要翻译： 本发明提供了可用于治疗HIV感染或预防HIV感染或治疗AIDS或ARC的化合物。 本发明的化合物具有式I的化合物，其中A为A 1，A 2，A 3或A 4，R 1，R 2，R 3， R 4a，R 4b，R 5，R 6，Ar，X 1，O 2， >，X 2，X 4，X 4和X 5如本文所定义。 本发明还公开了用本文定义的化合物治疗HIV感染的方法和含有所述化合物的药物组合物。
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公开(公告)号：US07906509B2
公开(公告)日：2011-03-15
申请号：US12635779
申请日：2009-12-11
申请人： Joshua Kennedy-Smith , Rama K. Kondru , Bradley E. Loe , Yan Lou , Joel McIntosh , Timothy D. Owens , Michael Soth , Zachary Kevin Sweeney , Joshua Paul Gergely Taygerly
发明人： Joshua Kennedy-Smith , Rama K. Kondru , Bradley E. Loe , Yan Lou , Joel McIntosh , Timothy D. Owens , Michael Soth , Zachary Kevin Sweeney , Joshua Paul Gergely Taygerly
IPC分类号： A61K31/4412 , A61K31/5355 , A61K31/496 , C07D413/14 , C07D401/14
CPC分类号： A61K31/4725 , A61K31/496 , A61K31/506 , A61K31/5377 , A61K31/541 , C07D213/74
摘要： This application discloses 5-phenyl-1H-pyridin-2-one and 6-phenyl-2H-pyridazin-3-one derivatives according to generic Formulae I-III: wherein, variables R, X, Y1, Y2, Y3, Y4, n and m are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation such as rheumatoid arthritis. Also disclosed are compositions containing compounds of Formulae I-III and at least one carrier, diluent or excipient.
摘要翻译： 本申请公开了根据通式I-III的5-苯基-1H-吡啶-2-酮和6-苯基-2H-哒嗪-3-酮衍生物：其中，变量R，X，Y 1，Y 2，Y 3，Y 4， n和m定义如本文所述，其抑制Btk。 本文公开的化合物可用于调节Btk的活性并治疗与过量Btk活性相关的疾病。 该化合物还可用于治疗与异常B细胞增殖相关的炎症和自身免疫疾病，例如类风湿性关节炎。 还公开了含有式I-III化合物和至少一种载体，稀释剂或赋形剂的组合物。
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公开(公告)号：US08063064B2
公开(公告)日：2011-11-22
申请号：US12708466
申请日：2010-02-18
IPC分类号： C07D471/04 , A61K31/437 , A61P31/18
CPC分类号： C07D471/04 , C07D231/12 , C07D231/56 , C07D487/04
摘要： The present invention provides for compounds useful for treating an HIV infection, or preventing an HIV infection, or treating AIDS or ARC. The compounds of the invention are of formula I wherein A is A2 and R1, R2, R3, R4a, R4b, R5, R6, Ar, X1, X2, X4, X4 and X5 are as herein defined. Also disclosed in the present invention are methods of treating an HIV infection with compounds defined herein and pharmaceutical compositions containing said compounds.
摘要翻译： 本发明提供了可用于治疗HIV感染或预防HIV感染或治疗AIDS或ARC的化合物。 本发明化合物是式Ⅰ化合物，其中A是A2，R 1，R 2，R 3，R 4a，R 4b，R 5，R 6，Ar，X 1，X 2，X 4，X 4和X 5如本文所定义。 本发明还公开了用本文定义的化合物治疗HIV感染的方法和含有所述化合物的药物组合物。
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公开(公告)号：US20110059975A1
公开(公告)日：2011-03-10
申请号：US12708466
申请日：2010-02-18
IPC分类号： A61K31/5025 , C07D231/12 , A61K31/415 , C07D231/56 , A61K31/416 , C07D471/04 , A61K31/437 , C07D487/04 , A61K31/519 , A61K31/4985 , C07D237/24 , A61K31/50 , A61P31/18
CPC分类号： C07D471/04 , C07D231/12 , C07D231/56 , C07D487/04
摘要： The present invention provides for compounds useful for treating an HIV infection, or preventing an HIV infection, or treating AIDS or ARC. The compounds of the invention are of formula I wherein A is A2 and R1, R2, R3, R4a, R4b, R5, R6, Ar, X1, X2, X4, X4 and X5 are as herein defined. Also disclosed in the present invention are methods of treating an HIV infection with compounds defined herein and pharmaceutical compositions containing said compounds.
摘要翻译： 本发明提供了可用于治疗HIV感染或预防HIV感染或治疗AIDS或ARC的化合物。 本发明化合物是式Ⅰ化合物，其中A是A2，R 1，R 2，R 3，R 4a，R 4b，R 5，R 6，Ar，X 1，X 2，X 4，X 4和X 5如本文所定义。 本发明还公开了用本文定义的化合物治疗HIV感染的方法和含有所述化合物的药物组合物。
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公开(公告)号：US07713974B2
公开(公告)日：2010-05-11
申请号：US11893349
申请日：2007-08-15
IPC分类号： C07D487/04 , A61K31/4985 , A61P31/18 , C07D231/20 , C07D231/12 , C07D231/56 , A61K31/415 , A61K31/407 , A61K31/519 , C07D471/04
CPC分类号： C07D471/04 , C07D231/12 , C07D231/56 , C07D487/04
摘要： The present invention provides for compounds useful for treating an HIV infection, or preventing an HIV infection, or treating AIDS or ARC. The compounds of the invention are of formula I wherein A is A1, A2, A3 or A4 and R1, R2, R3, R4a, R4b, R5, R6, Ar, X1, X2, X4, X4 and X5 are as herein defined. Also disclosed in the present invention are methods of treating an HIV infection with compounds defined herein and pharmaceutical compositions containing said compounds.
摘要翻译： 本发明提供了可用于治疗HIV感染或预防HIV感染或治疗AIDS或ARC的化合物。 本发明的化合物是式Ⅰ化合物，其中A是A 1，A 2，A 3或A 4，R 1，R 2，R 3，R 4a，R 4b，R 5，R 6，Ar，X 1，X 2，X 4，X 4和X 5如本文所定义。 本发明还公开了用本文定义的化合物治疗HIV感染的方法和含有所述化合物的药物组合物。
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