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公开(公告)号：US20090170856A1
公开(公告)日：2009-07-02
申请号：US12341594
申请日：2008-12-22
IPC分类号： A61K31/437 , C07D471/04 , C07D487/04 , A61K31/5025 , A61P31/18
CPC分类号： C07D471/04 , C07D487/04
摘要： Compounds of formula I, wherein R1, R2, R3, X1, X2 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 1，X 2和Ar如本文所定义或其药学上可接受的盐的式I化合物抑制HIV-1逆转录酶，并提供预防和治疗HIV-1感染和治疗的方法 的艾滋病和/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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33.发明申请公开(公告)号：US20150232501A1
公开(公告)日：2015-08-20
申请号：US14421249
申请日：2013-08-27
申请人： Sampath-Kumar ANADAN , Virender Singh AULAKH , Martijn FENAUX , Xiaodong LIN , Liang MAO , Oliver SAUNDERS , Zachary Kevin SWEENEY , Fumiaki YOKOKAWA , Weidong ZHONG
发明人： Sampath-Kumar Anandan , Virender Singh Aulakh , Martijn Fenaux , Xiaodong Lin , Liang Mao , Oliver Saunders , Zachary Kevin Sweeney , Fumiaki Yokokawa , Weidong Zhong
IPC分类号： C07H19/10 , A61K31/7068 , A61K45/06 , A61K31/7072
CPC分类号： A61K31/7072 , A61K31/7068 , A61K45/06 , A61K47/22 , C07H19/06 , C07H19/067 , C07H19/10
摘要： The present invention provides a compound of formula A: or a pharmaceutically acceptable salt thereof, wherein B, Q, R1, R5, R6, R7, R8 and Z are as defined herein, which is a 2′-branched nucleoside useful for the treatment or prevention of viral infections, particularly dengue fever, yellow fever, West Nile virus, Japanese encephalitis virus, tick-borne encephalitis virus, Kunjin virus, Murray Valley encephalitis, St Louis encephalitis, Omsk hemorrhagic fever virus, bovine viral diarrhea virus, Zika virus and Hepatitis C virus.
摘要翻译： 本发明提供式A化合物或其药学上可接受的盐，其中B，Q，R 1，R 5，R 6，R 7，R 8和Z如本文所定义，其为可用于治疗的2'-支链核苷 或预防病毒感染，特别是登革热，黄热病，西尼罗病毒，日本脑炎病毒，蜱传脑炎病毒，昆金病毒，墨累谷脑炎，圣路易脑炎，鄂木斯克出血热病毒，牛病毒性腹泻病毒，Zika病毒 和丙型肝炎病毒。
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公开(公告)号：US08536166B2
公开(公告)日：2013-09-17
申请号：US12459595
申请日：2009-07-01
IPC分类号： A61K31/496 , A61K31/497 , A61K31/517 , A61K31/5377 , A61K31/541 , C07D401/10 , C07D401/14 , C07D407/14 , C07D413/14 , C07D417/14 , A61K31/502
CPC分类号： C07D403/10 , C07D401/14 , C07D403/14 , C07D413/14 , C07D417/14
摘要： This application discloses 5-phenyl-1H-pyrazin-2-one derivatives according to generic Formulae I-V: wherein, variables Q, R, Y1, Y2, 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 comprising compounds of Formulae I-V and at least one carrier, diluent or excipient.
摘要翻译： 本申请公开了根据通式IV的5-苯基-1H-吡嗪-2-酮衍生物：其中，变量Q，R，Y1，Y2，Y2'，Y3，Y4，n和m如本文所述定义，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。 还公开了包含式I-V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：US08329755B2
公开(公告)日：2012-12-11
申请号：US12606320
申请日：2009-10-27
IPC分类号： A61K31/16 , A61K31/165 , A61K31/18
CPC分类号： A61K31/277
摘要： The present invention provides compositions for treating an HIV infection comprising administering a compound according to formula I where Ar, R1-R5, R11c and X1 are as defined herein with at least one carrier, excipient or diluent.
摘要翻译： 本发明提供用于治疗HIV感染的组合物，包括给予式I化合物，其中Ar，R 1 -R 5，R 11c和X 1如本文所定义与至少一种载体，赋形剂或稀释剂。
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公开(公告)号：US08299077B2
公开(公告)日：2012-10-30
申请号：US12711312
申请日：2010-02-24
申请人： Steven Berthel , Fariborz Firooznia , Daniel Fishlock , Jun-Bae Hong , Yan Lou , Matthew Lucas , Timothy D. Owens , Keshab Sarma , Zachary Kevin Sweeney , Joshua Paul Gergely Taygerly
发明人： Steven Berthel , Fariborz Firooznia , Daniel Fishlock , Jun-Bae Hong , Yan Lou , Matthew Lucas , Timothy D. Owens , Keshab Sarma , Zachary Kevin Sweeney , Joshua Paul Gergely Taygerly
IPC分类号： A61K31/502 , C07D237/32
CPC分类号： C07D401/10 , C07D401/14 , C07D403/14 , C07D413/14
摘要： This application discloses 5-phenyl-1H-pyridin-2-one, 6-phenyl-2H-pyridazin-3-one, and 5-Phenyl-1H-pyrazin-2-one derivatives according to generic Formula I-III: wherein, variables Q, R, X, X′, Y1, Y2, Y2′, Y3, Y4, Y5, m, and n 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 Formula I-III and at least one carrier, diluent or excipient.
摘要翻译： 该申请公开了根据通式I-III的5-苯基-1H-吡啶-2-酮，6-苯基-2H-哒嗪-3-酮和5-苯基-1H-吡嗪-2-酮衍生物：其中， 变量Q，R，X，X'，Y1，Y2，Y2'，Y3，Y4，Y5，m和n如本文所述限定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：US08293778B2
公开(公告)日：2012-10-23
申请号：US12709473
申请日：2010-02-20
IPC分类号： A61K31/44 , A61K31/427 , A61K31/4725 , A61K31/496 , A61K31/513 , A61K31/536 , A61K31/7068 , A61K31/7072 , A61K31/708
CPC分类号： A61K31/41 , A61K31/427 , A61K31/4725 , A61K31/496 , A61K31/513 , A61K31/536 , A61K31/551 , A61K31/7068 , A61K31/7072 , A61K31/708
摘要： The present invention relates to a method of treating an HIV-I infection with a compound according to formula I where R1, R2, R3, R4, R5, are as defined herein.
摘要翻译： 本发明涉及用式I化合物治疗HIV-1感染的方法，其中R1，R2，R3，R4，R5如本文所定义。
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公开(公告)号：US08063028B2
公开(公告)日：2011-11-22
申请号：US12341594
申请日：2008-12-22
IPC分类号： C07D487/04 , A61K31/4965 , A61K31/675 , C07F9/09 , A61P31/18
CPC分类号： C07D471/04 , C07D487/04
摘要： Compounds of formula I, wherein R1, R2, R3, X1, X2 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 1，X 2和Ar如本文所定义或其药学上可接受的盐的式I化合物抑制HIV-1逆转录酶，并提供预防和治疗HIV-1感染和治疗的方法 的艾滋病和/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：US20110207688A1
公开(公告)日：2011-08-25
申请号：US12709473
申请日：2010-02-20
IPC分类号： A61K31/41 , A61P31/18 , A61K31/7072 , A61K31/513 , A61K31/708 , A61K31/7068 , A61K31/536 , A61K31/551 , A61K31/4725 , A61K31/427 , A61K31/496
CPC分类号： A61K31/41 , A61K31/427 , A61K31/4725 , A61K31/496 , A61K31/513 , A61K31/536 , A61K31/551 , A61K31/7068 , A61K31/7072 , A61K31/708
摘要： The present invention relates to a method of treating an HIV-I infection with a compound according to formula I where R1, R2, R3, R4, R5, are as defined herein.
摘要翻译： 本发明涉及用式Ⅰ化合物治疗HIV-1感染的方法，其中R1，R2，R3，R4，R5如本文所定义。
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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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