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公开(公告)号：US20100160384A1
公开(公告)日：2010-06-24
申请号：US12637940
申请日：2009-12-15
申请人： Jacob Berger , Christine E. Brotherton-Pleiss , Francisco Javier Lopez-Tapia , Keith Adrian Murray Walker , Shu-Hai Zhao
发明人： Jacob Berger , Christine E. Brotherton-Pleiss , Francisco Javier Lopez-Tapia , Keith Adrian Murray Walker , Shu-Hai Zhao
IPC分类号： A61K31/4439 , C07D401/12
CPC分类号： C07D401/12 , C07D211/90 , C07D413/12 , C07D417/12
摘要： Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, n, p, q, R1, R2, R3, R4, R5 and R6 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of diseases associated with the P2X7 purinergic receptor.
摘要翻译： 式I化合物或其药学上可接受的盐，其中m，n，p，q，R 1，R 2，R 3，R 4，R 5和R 6如本文所定义。 还公开了制备化合物和使用该化合物治疗与P2X7嘌呤能受体有关的疾病的方法。
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公开(公告)号：US20080146595A1
公开(公告)日：2008-06-19
申请号：US12001947
申请日：2007-12-13
IPC分类号： A61K31/506 , C07D401/12 , A61P31/18 , A61P31/12
CPC分类号： C07D401/14 , C07D403/12 , C07D403/14 , C07D471/10
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 R1, R2, R3, R4, R5a, R5b, R6a, R6b and X 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的化合物，其中R 1，R 2，R 3，R 4， R 5a，R 5b，R 6a，R 6b和X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：US08889682B2
公开(公告)日：2014-11-18
申请号：US13586958
申请日：2012-08-16
申请人： Christine E. Brotherton-Pleiss , Saul Jaime-Figueroa , Francisco Javier Lopez-Tapia , Yan Lou , Timothy D. Owens
发明人： Christine E. Brotherton-Pleiss , Saul Jaime-Figueroa , Francisco Javier Lopez-Tapia , Yan Lou , Timothy D. Owens
IPC分类号： A61K31/501 , A61K31/502 , C07D237/02 , C07D413/14
CPC分类号： C07D401/14 , C07D487/04
摘要： This application discloses compounds according to generic Formula I: wherein the variables are defined as described herein, and 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：其中变量如本文所述定义并且抑制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：US08153809B2
公开(公告)日：2012-04-10
申请号：US12637903
申请日：2009-12-15
申请人： Christine E. Brotherton-Pleiss , Joan Marie Caroon , Francisco Javier Lopez-Tapia , Dov Nitzan , Keith Adrian Murray Walker
发明人： Christine E. Brotherton-Pleiss , Joan Marie Caroon , Francisco Javier Lopez-Tapia , Dov Nitzan , Keith Adrian Murray Walker
IPC分类号： C07D213/62 , A61K31/44
CPC分类号： C07D211/86 , C07D401/12 , C07D405/12 , C07D409/12 , C07D417/12
摘要： Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, n, R1, R2, R3, R4 and R5 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of diseases associated with the P2X7 purinergic receptor.
摘要翻译： 式I化合物或其药学上可接受的盐，其中m，n，R 1，R 2，R 3，R 4和R 5如本文所定义。 还公开了制备化合物和使用该化合物治疗与P2X7嘌呤能受体有关的疾病的方法。
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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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6.发明授权公开(公告)号：US06627644B2
公开(公告)日：2003-09-30
申请号：US10308081
申请日：2002-12-02
IPC分类号： A61K31445
CPC分类号： C07D401/06 , C07D211/26 , C07D211/92 , C07D401/12 , C07D409/06 , C07D409/12 , C07D413/06
摘要： This invention relates to compounds which are generally muscarinic receptor antagonists and which are represented by Formula I: wherein p, R1, R2, R3 and A are as defined in the specification, or individual isomers, racemic or non-racemic mixtures of isomers, or acceptable salts or solvates thereof. The invention further relates to pharmaceutical compositions containing such compounds and methods for their use and preparation as therapeutic drugs.
摘要翻译： 本发明涉及通常为毒蕈碱受体拮抗剂并由式I表示的化合物：其中p，R 1，R 2，R 3和A如说明书中所定义，或单个异构体，外消旋 或异构体的非外消旋混合物，或其可接受的盐或溶剂合物。 本发明还涉及含有这些化合物的药物组合物及其用作治疗药物的方法。
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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：US20110071143A1
公开(公告)日：2011-03-24
申请号：US12882514
申请日：2010-09-15
申请人： Christine E. Brotherton-Pleiss , Ralph New Harris, III , Bradley E. Loe , Francisco Javier Lopez-Tapia , Pankaj D. Rege , David Bruce Repke , Russell Stephen Stabler , Keith Adrian Murray Walker
发明人： Christine E. Brotherton-Pleiss , Ralph New Harris, III , Bradley E. Loe , Francisco Javier Lopez-Tapia , Pankaj D. Rege , David Bruce Repke , Russell Stephen Stabler , Keith Adrian Murray Walker
IPC分类号： A61K31/542 , C07D487/04 , A61K31/4985 , C07D471/04 , A61K31/437 , C07D513/04 , C07D498/04 , A61K31/5383 , A61P19/02 , A61P29/00 , A61P31/12 , A61P17/06 , A61P31/04 , A61P33/00 , A61P11/00 , A61P3/10
CPC分类号： C07D487/04 , C07D471/04 , C07D491/20 , C07D498/04 , C07D513/04
摘要： Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein X, Y, R1, R2, and R3 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of diseases associated with the P2X7 purinergic receptor.
摘要翻译： 式I化合物或其药学上可接受的盐，其中X，Y，R 1，R 2和R 3如本文所定义。 还公开了制备化合物和使用该化合物治疗与P2X7嘌呤能受体有关的疾病的方法。
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9.发明授权公开(公告)号：US06864266B2
公开(公告)日：2005-03-08
申请号：US10611193
申请日：2003-07-01
IPC分类号： A61K31/445 , A61K31/4525 , A61K31/4535 , A61K31/454 , A61K31/4545 , A61K31/496 , A61K31/5377 , A61P1/00 , A61P1/06 , A61P1/12 , A61P11/00 , A61P11/06 , A61P13/02 , A61P13/10 , A61P21/00 , A61P25/02 , A61P25/28 , A61P43/00 , C07D211/26 , C07D211/92 , C07D401/06 , C07D401/12 , C07D405/06 , C07D409/06 , C07D409/12 , C07D413/06 , C07D413/14 , C07D211/06
CPC分类号： C07D401/06 , C07D211/26 , C07D211/92 , C07D401/12 , C07D409/06 , C07D409/12 , C07D413/06
摘要： This invention relates to the (R)-isomers of compounds which are generally muscarinic receptor antagonists and which are represented by Formula I: wherein p, R1, R2, R3 and A are as defined in the specification, or individual isomers, racemic or non-racemic mixtures of isomers, or acceptable salts or solvates thereof. The invention further relates to pharmaceutical compositions containing such compounds and methods for their use and preparation as therapeutic drugs.
摘要翻译： 本发明涉及通常是毒蕈碱受体拮抗剂并由式I表示的化合物的（R） - 异构体：其中p，R 1，R 2，R 3和A如 规格或各异构体，异构体的外消旋或非外消旋混合物，或其可接受的盐或溶剂合物。 本发明还涉及含有这些化合物的药物组合物及其用作治疗药物的方法。
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公开(公告)号：US20130045965A1
公开(公告)日：2013-02-21
申请号：US13586958
申请日：2012-08-16
申请人： Christine E. Brotherton-Pleiss , Saul Jaime-Figueroa , Francisco Javier Lopez-Tapia , Yan Lou , Timothy D. Owens
发明人： Christine E. Brotherton-Pleiss , Saul Jaime-Figueroa , Francisco Javier Lopez-Tapia , Yan Lou , Timothy D. Owens
IPC分类号： A61K31/501 , A61K31/502 , C07D413/14 , A61P11/06 , C07D401/14 , C07D405/14 , A61P29/00 , A61P19/02 , A61K31/5377 , C07D487/04
CPC分类号： C07D401/14 , C07D487/04
摘要： This application discloses compounds according to generic Formula I: wherein the variables are defined as described herein, and 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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