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公开(公告)号：US08481540B2
公开(公告)日：2013-07-09
申请号：US13207481
申请日：2011-08-11
申请人： Steven Joseph Berthel , Roland Joseph Billedeau , Christine E. Brotherton-Pleiss , Fariborz Firooznia , Stephen Deems Gabriel , Xiaochun Han , Ramona Hilgenkamp , Saul Jaime-Figueroa , Buelent Kocer , Francisco Javier Lopez-Tapia , Yan Lou , Lucja Orzechowski , Timothy D. Owens , Jenny Tan , Peter Michael Wovkulich
发明人： Steven Joseph Berthel , Roland Joseph Billedeau , Christine E. Brotherton-Pleiss , Fariborz Firooznia , Stephen Deems Gabriel , Xiaochun Han , Ramona Hilgenkamp , Saul Jaime-Figueroa , Buelent Kocer , Francisco Javier Lopez-Tapia , Yan Lou , Lucja Orzechowski , Timothy D. Owens , Jenny Tan , Peter Michael Wovkulich
IPC分类号： A01N43/58 , A61K31/50 , C07D237/00
CPC分类号： C07D401/14 , C07D403/14 , C07D405/14 , C07D413/14 , C07D417/14 , C07D487/04 , C07D487/08 , C07D487/10 , C07D491/107
摘要： This application discloses 6-(2-Hydroxymethyl-phenyl)-2-methyl-2H-pyridazin-3-one derivatives according to generic Formula I: wherein, variables X, R, and Y4, 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 and at least one carrier, diluent or excipient.
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公开(公告)号：US20120040949A1
公开(公告)日：2012-02-16
申请号：US13207481
申请日：2011-08-11
申请人： Steven Joseph Berthel , Roland Joseph Billedeau , Christine E. Brotherton-Pleiss , Fariborz Firooznia , Stephen Deems Gabriel , Xiaochun Han , Ramona Hilgenkamp , Saul Jaime-Figueroa , Buelent Kocer , Francisco Javier Lopez-Tapia , Yan Lou , Lucja Orzechowski , Timothy D. Owens , Jenny Tan , Peter Michael Wovkulich
发明人： Steven Joseph Berthel , Roland Joseph Billedeau , Christine E. Brotherton-Pleiss , Fariborz Firooznia , Stephen Deems Gabriel , Xiaochun Han , Ramona Hilgenkamp , Saul Jaime-Figueroa , Buelent Kocer , Francisco Javier Lopez-Tapia , Yan Lou , Lucja Orzechowski , Timothy D. Owens , Jenny Tan , Peter Michael Wovkulich
IPC分类号： A61K31/502 , C07D413/14 , C07D403/14 , C07D487/10 , A61P37/00 , C07D491/107 , A61K31/5377 , A61K31/541 , A61K31/501 , A61P29/00 , C07D401/14 , C07D417/14
CPC分类号： C07D401/14 , C07D403/14 , C07D405/14 , C07D413/14 , C07D417/14 , C07D487/04 , C07D487/08 , C07D487/10 , C07D491/107
摘要： This application discloses 6-(2-Hydroxymethyl-phenyl)-2-methyl-2H-pyridazin-3-one derivatives according to generic Formula I: wherein, variables X, R, and Y4, 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 and at least one carrier, diluent or excipient.
摘要翻译： 本申请公开了根据通式I的6-（2-羟基甲基 - 苯基）-2-甲基-2H-哒嗪-3-酮衍生物：其中，变量X，R和Y4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细胞增殖相关的炎性和自身免疫疾病，例如类风湿性关节炎。 还公开了含有式I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：US08729078B2
公开(公告)日：2014-05-20
申请号：US13472541
申请日：2012-05-16
申请人： Roland Joseph Billedeau , Rama K. Kondru , Francisco Javier Lopez-Tapia , Yan Lou , Timothy D. Owens , Yimin Qian , Sung-Sau So , Kshitij C. Thakkar , Jutta Wanner , Omar Jose Morales
发明人： Roland Joseph Billedeau , Rama K. Kondru , Francisco Javier Lopez-Tapia , Yan Lou , Timothy D. Owens , Yimin Qian , Sung-Sau So , Kshitij C. Thakkar , Jutta Wanner , Omar Jose Morales
IPC分类号： A01N43/58 , A61K31/50 , C07D237/00
CPC分类号： C07D405/10 , C07D401/10 , C07D401/14 , C07D403/10 , C07D413/10 , C07D417/10 , C07D471/04
摘要： This application discloses compounds according to generic Formula I: wherein all variables 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 and at least one carrier, diluent or excipient.
摘要翻译： 本申请公开了根据通式I的化合物：其中所有变量如本文所述限定，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：US20120295885A1
公开(公告)日：2012-11-22
申请号：US13472541
申请日：2012-05-16
申请人： Roland Joseph Billedeau , Rama K. Kondru , Francisco Javier Lopez-Tapia , Yan Lou , Timothy D. Owens , Yimin Qian , Sung-Sau So , Kshitij C. Thakkar , Jutta Wanner
发明人： Roland Joseph Billedeau , Rama K. Kondru , Francisco Javier Lopez-Tapia , Yan Lou , Timothy D. Owens , Yimin Qian , Sung-Sau So , Kshitij C. Thakkar , Jutta Wanner
IPC分类号： A61K31/502 , A61P37/06 , A61P11/06 , C07D405/10 , C07D403/10 , C07D417/10 , C07D413/10 , C07D401/10 , A61K31/4725 , C07D413/14 , A61K31/5377 , C07D471/04 , C07D401/14 , C07D487/04 , A61K31/519 , A61K31/541 , A61P29/00
CPC分类号： C07D405/10 , C07D401/10 , C07D401/14 , C07D403/10 , C07D413/10 , C07D417/10 , C07D471/04
摘要： This application discloses compounds according to generic Formula I: wherein all variables 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 and at least one carrier, diluent or excipient.
摘要翻译： 本申请公开了根据通式I的化合物：其中所有变量如本文所述限定，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：US20110021425A1
公开(公告)日：2011-01-27
申请号：US12825390
申请日：2010-06-29
IPC分类号： A61K38/18 , C07D279/12 , A61K31/541 , C07D487/14 , A61K31/4985 , A61P11/06 , A61P19/02 , A61P29/00
CPC分类号： C07D487/14
摘要： The present invention relates to the use of novel compounds of Formulae I-II, wherein the variables R, X1, X2, X3, Y1, Y2, Y3, Z1, and Z2 are defined as described herein, which inhibit JAK and are useful for the treatment of auto-immune and inflammatory diseases.
摘要翻译： 本发明涉及式I-II的新化合物的用途，其中变量R，X1，X2，X3，Y1，Y2，Y3，Z1和Z2如本文所述定义，其抑制JAK并且可用于 治疗自身免疫和炎性疾病。
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公开(公告)号：US20230022922A1
公开(公告)日：2023-01-26
申请号：US17359990
申请日：2021-06-28
申请人： Lijing Chen , Roland Joseph Billedeau , Jim Li
发明人： Lijing Chen , Roland Joseph Billedeau , Jim Li
IPC分类号： C07H19/167 , C07H19/067 , C07H19/23
摘要： The invention relates to novel heterocyclic compounds and pharmaceutical preparations thereof. The invention further relates to methods of treating or preventing cancer using the novel heterocyclic compounds of the invention.
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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：US20100056535A1
公开(公告)日：2010-03-04
申请号：US12584436
申请日：2009-09-04
申请人： Nidhi Arora , Roland Joseph Billedeau , Joshua Kennedy-Smith , Weiling Liang , Ralf Roetz , Zachary Kevin Sweeney
发明人： Nidhi Arora , Roland Joseph Billedeau , Joshua Kennedy-Smith , Weiling Liang , Ralf Roetz , Zachary Kevin Sweeney
IPC分类号： A61K31/501 , C07D217/06 , C07D403/06 , A61K31/4709 , A61K31/4439 , A61P31/18
CPC分类号： C07D401/06 , C07D213/69 , C07D213/74 , C07D413/06
摘要： The present invention provides compounds for treating or preventing an HIV infection, or treating AIDS or ARC comprising administering a compound according to Formulae I and II wherein Q, R1, R2, and R3 are defined as described herein.
摘要翻译： 本发明提供了用于治疗或预防HIV感染或治疗AIDS或ARC的化合物，其包括给予根据式I和II的化合物，其中Q，R 1，R 2和R 3如本文所述定义。
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公开(公告)号：US08361962B2
公开(公告)日：2013-01-29
申请号：US12825390
申请日：2010-06-29
IPC分类号： A61K38/18 , A61K31/541 , A61K31/4985 , A61P19/02 , A61P29/00 , C07D279/12 , C07D487/14
CPC分类号： C07D487/14
摘要： The present invention relates to the use of novel compounds of Formulae I-II, wherein the variables R, X1, X2, X3, Y1, Y2, Y3, Z1, and Z2 are defined as described herein, which inhibit JAK and are useful for the treatment of auto-immune and inflammatory diseases.
摘要翻译： 本发明涉及式I-II的新化合物的用途，其中变量R，X1，X2，X3，Y1，Y2，Y3，Z1和Z2如本文所述定义，其抑制JAK并且可用于 治疗自身免疫和炎性疾病。
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公开(公告)号：US20080293664A1
公开(公告)日：2008-11-27
申请号：US12082069
申请日：2008-04-08
IPC分类号： A61K31/5025 , A61P31/18 , C07D471/04 , A61K31/7072 , A61K31/7068 , A61K31/551 , A61K31/513 , A61K31/496 , A61K31/538 , A61K31/708 , A61K31/437 , C07D487/04
CPC分类号： C07D487/04 , C07D471/04
摘要： Compounds of formula I, wherein R1, R2, R3, R4, Ra, X, X1, and Y 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，R2，R3，R4，Ra，X，X1和Y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的方法 感染和治疗艾滋病和/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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