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公开(公告)号:US20100004231A1
公开(公告)日:2010-01-07
申请号:US12459595
申请日:2009-07-01
IPC分类号: A61K31/5415 , A61K31/5377 , A61K31/502 , A61K31/497 , C07D417/08 , C07D413/14 , C07D403/10 , C07D403/14 , C07D401/08 , A61P35/00
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:US20090318448A1
公开(公告)日:2009-12-24
申请号:US12456911
申请日:2009-06-24
申请人: Nolan James Dewdney , Rama K. Kondru , Bradley E. Loe , Yan Lou , Joel McIntosh , Timothy D. Owens , Michael Soth
发明人: Nolan James Dewdney , Rama K. Kondru , Bradley E. Loe , Yan Lou , Joel McIntosh , Timothy D. Owens , Michael Soth
IPC分类号: A61K31/5377 , C07D413/04 , C07D401/14 , C07D403/12 , A61K31/497 , A61K31/501 , A61P37/06
CPC分类号: C07D417/14 , C07D401/10 , C07D401/14 , C07D413/14
摘要: This application discloses 5-phenyl-1H-pyridin-2-one and 6-phenyl-2H-pyridazin-3-one derivatives according to generic Formulae I-IV: wherein, variables R, X, 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-IV and at least one carrier, diluent or excipient.
摘要翻译: 本申请公开了根据通式I-IV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 2,Y 3, Y4,n和m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。 还公开了包含式I-IV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: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: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:US08426441B2
公开(公告)日:2013-04-23
申请号:US12316343
申请日:2008-12-11
申请人: Nolan James Dewdney , Yan Lou , Michael Soth
发明人: Nolan James Dewdney , Yan Lou , Michael Soth
IPC分类号: C07D471/04 , A61K31/437 , A61P19/02
CPC分类号: A61K31/5025 , C07D487/04
摘要: This application discloses novel imidazo[1,2-a]pyridine and imidazo[1,2-b]pyridazine derivatives according to Formulae I-VI: wherein R, R′, R″, Q, X, and Y 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-VI and at least one carrier, diluent or excipient.
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公开(公告)号:US08124604B2
公开(公告)日:2012-02-28
申请号:US12987187
申请日:2011-01-10
申请人: Nolan James Dewdney , Rama K. Kondru , Bradley E. Loe , Yan Lou , Joel McIntosh , Timothy D. Owens , Michael Soth
发明人: Nolan James Dewdney , Rama K. Kondru , Bradley E. Loe , Yan Lou , Joel McIntosh , Timothy D. Owens , Michael Soth
IPC分类号: C07D401/14 , C07D413/14 , A61K31/5355 , A61K31/513
CPC分类号: C07D417/14 , C07D401/10 , C07D401/14 , C07D413/14
摘要: This application discloses 5-phenyl-1H-pyridin-2-one and 6-phenyl-2H-pyridazin-3-one derivatives according to generic Formulae I-IV: wherein, variables R, X, 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-IV and at least one carrier, diluent or excipient.
摘要翻译: 本申请公开了根据通式I-IV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 2',Y 3 ,Y4,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。 还公开了包含式I-IV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:US08324211B2
公开(公告)日:2012-12-04
申请号:US12460226
申请日:2009-07-15
申请人: Nolan James Dewdney , Yan Lou , Eric Brian Sjogren , Michael Soth
发明人: Nolan James Dewdney , Yan Lou , Eric Brian Sjogren , Michael Soth
IPC分类号: A61K31/50 , C07D237/00
CPC分类号: C07D487/04 , C07D471/04
摘要: This application discloses 6-Phenyl-imidazo[1,2-a]pyridine and 6-Phenyl-imidazo[1,2-b]pyridazine derivatives according to generic Formulae I-V: wherein, variables Q, 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 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6-苯基 - 咪唑并[1,2-a]吡啶和6-苯基 - 咪唑并[1,2-b]哒嗪衍生物:其中,变量Q,R,X,Y 1, Y3,Y4,n和m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:US20110105479A1
公开(公告)日:2011-05-05
申请号:US12987187
申请日:2011-01-10
申请人: Nolan James Dewdney , Rama K. Kondru , Bradley E. Loe , Yan Lou , Joel McIntosh , Timothy D. Owens , Michael Soth
发明人: Nolan James Dewdney , Rama K. Kondru , Bradley E. Loe , Yan Lou , Joel McIntosh , Timothy D. Owens , Michael Soth
IPC分类号: A61K31/5415 , C07D417/14 , C07D413/14 , A61K31/5377 , A61P29/00 , A61P37/06 , A61P11/06
CPC分类号: C07D417/14 , C07D401/10 , C07D401/14 , C07D413/14
摘要: This application discloses 5-phenyl-1H-pyridin-2-one and 6-phenyl-2H-pyridazin-3-one derivatives according to generic Formulae I-IV: wherein, variables R, X, 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-IV and at least one carrier, diluent or excipient.
摘要翻译: 本申请公开了根据通式I-IV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 2',Y 3 ,Y4,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。 还公开了包含式I-IV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:US07902194B2
公开(公告)日:2011-03-08
申请号:US12456911
申请日:2009-06-24
申请人: Nolan James Dewdney , Rama K. Kondru , Bradley E. Loe , Yan Lou , Joel McIntosh , Timothy D. Owens , Michael Soth
发明人: Nolan James Dewdney , Rama K. Kondru , Bradley E. Loe , Yan Lou , Joel McIntosh , Timothy D. Owens , Michael Soth
IPC分类号: A61K31/502 , C07D237/32
CPC分类号: C07D417/14 , C07D401/10 , C07D401/14 , C07D413/14
摘要: This application discloses 5-phenyl-1H-pyridin-2-one and 6-phenyl-2H-pyridazin-3-one derivatives according to generic Formulae I-IV: wherein, variables R, X, 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-IV and at least one carrier, diluent or excipient.
摘要翻译: 本申请公开了根据通式I-IV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 2,Y 3, Y4,n和m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。 还公开了包含式I-IV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:US20090105209A1
公开(公告)日:2009-04-23
申请号:US12288730
申请日:2008-10-23
申请人: Nolan James Dewdney , Rama K. Kondru , Yan Lou , Michael Soth , Tobias Gabriel
发明人: Nolan James Dewdney , Rama K. Kondru , Yan Lou , Michael Soth , Tobias Gabriel
IPC分类号: A61K31/5377 , C07D403/14 , C07D417/14 , A61K31/501
CPC分类号: C07D213/63 , C07D401/12 , C07D401/14 , C07D403/14 , C07D409/12 , C07D413/12 , C07D413/14
摘要: This application discloses pyridine and pyrimidine compounds according to formula I wherein R1, R2, R3, R4, R5, X1 and A are 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: 本申请公开了根据式I的吡啶和嘧啶化合物,其中R 1,R 2,R 3,R 4,R 5,X 1和A如本文所述抑制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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