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公开(公告)号:US20100099659A1
公开(公告)日:2010-04-22
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 Mclntosh , 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 Mclntosh , Timothy D. Owens , Michael Soth , Zachary Kevin Sweeney , Joshua Paul Gergely Taygerly
IPC分类号: A61K31/4725 , C07D413/14 , C07D401/14 , A61K31/541 , A61P29/00 , A61P37/00 , A61K31/5377 , A61K31/496 , A61P19/02
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:US07683064B2
公开(公告)日:2010-03-23
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: A61K31/501 , A61K31/4725 , C07D401/10 , C07D217/24
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:US20100016301A1
公开(公告)日:2010-01-21
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: A61K31/5377 , C07D487/04 , A61K31/437 , C07D471/04
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:US20090186898A1
公开(公告)日:2009-07-23
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: A61K31/5025 , C07D487/04 , A61P29/00 , 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.
摘要翻译: 本申请公开了根据式I-VI的新的咪唑并[1,2-a]吡啶和咪唑并[1,2-b]哒嗪衍生物:其中R,R',R“,Q,X和Y定义为 这抑制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-VI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:US07432283B2
公开(公告)日:2008-10-07
申请号:US11061000
申请日:2005-02-18
IPC分类号: A01N43/40 , A61K31/445 , C07D295/00 , C07D211/00
CPC分类号: A61K31/437 , A61K31/5383 , C07D471/04 , C07D487/04
摘要: This invention relates to a method for modulating α2 subtype GABAA receptors with heterocyclic compounds of formula I, and salts, solvates and prodrugs thereof. The invention further relates to novel heteocyclic compounds and pharmaceutical compositions containing said compounds. In addition the invention relates to the treatment of depression, an anxiety disorder, a psychiatric disorder, a learning or cognitive disorder, a sleep disorder, a convulsive or seizure disorder or pain
摘要翻译: 本发明涉及用式I杂环化合物调节α2亚型GABA A A受体的方法及其盐,溶剂合物和前药。 本发明还涉及含有所述化合物的新颖的杂环化合物和药物组合物。 此外,本发明涉及抑郁症,焦虑障碍,精神障碍,学习或认知障碍,睡眠障碍,惊厥或发作性疾病或疼痛的治疗
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公开(公告)号:US08618103B2
公开(公告)日:2013-12-31
申请号:US12878048
申请日:2010-09-09
申请人: Javier de Vicente Fidalgo , Johannes Cornelius Hermann , Remy Lemoine , Hongju Li , Allen John Lovey , Eric Brian Sjogren , Michael Soth
发明人: Javier de Vicente Fidalgo , Johannes Cornelius Hermann , Remy Lemoine , Hongju Li , Allen John Lovey , Eric Brian Sjogren , Michael Soth
IPC分类号: C07D487/04 , A61K31/4985 , C07D239/04 , A61K31/506 , A61P29/00 , A61P35/00
CPC分类号: C07D487/04 , C07D513/04
摘要: The present invention relates to the use of novel compounds of Formula I, wherein the variables m, n, p, q, Q, r, R, R′, X, X′, Y, Z1, Z2, and Z3 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的新化合物的用途,其中变量m,n,p,q,Q,r,R,R',X,X',Y,Z 1,Z 2和Z 3定义为 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:US08618098B2
公开(公告)日:2013-12-31
申请号:US13358557
申请日:2012-01-26
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 , A61K31/517
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:US08518945B2
公开(公告)日:2013-08-27
申请号:US13040310
申请日:2011-03-04
申请人: Robert Than Hendricks , Johannes Hermann , Rama Kondru , Yan Lou , Stephen M. Lynch , Timothy D. Owens , Michael Soth
发明人: Robert Than Hendricks , Johannes Hermann , Rama Kondru , Yan Lou , Stephen M. Lynch , Timothy D. Owens , Michael Soth
IPC分类号: A61K31/495
CPC分类号: C07D487/04 , C07D519/00
摘要: The present invention relates to the use of novel pyrrolopyrazine derivatives of Formula I, wherein the variables n, p, q, Q, X, X′ and Y are defined as described herein, which inhibit JAK and SYK and are useful for the treatment of auto-immune and inflammatory diseases.
摘要翻译: 本发明涉及式I的新型吡咯并吡嗪衍生物的用途,其中变量n,p,q,Q,X,X'和Y如本文所述定义,其抑制JAK和SYK,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:US20120129845A1
公开(公告)日:2012-05-24
申请号:US13358557
申请日:2012-01-26
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 , A61K31/517 , C07D413/14 , A61P11/06 , C07D417/14 , A61P29/00 , A61P37/06 , C07D401/10 , A61K31/5377
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:US20110230462A1
公开(公告)日:2011-09-22
申请号:US13040310
申请日:2011-03-04
申请人: Robert Than Hendricks , Johannes Hermann , Rama Kondru , Yan Lou , Stephen M. Lynch , Timothy D. Owens , Michael Soth
发明人: Robert Than Hendricks , Johannes Hermann , Rama Kondru , Yan Lou , Stephen M. Lynch , Timothy D. Owens , Michael Soth
IPC分类号: A61K31/4985 , C07D487/04 , A61P29/00 , A61P35/00 , A61P37/00 , A61P9/00 , A61P3/10 , A61P11/06 , A61P17/06 , A61P25/28 , A61K31/5377 , A61K31/541
CPC分类号: C07D487/04 , C07D519/00
摘要: The present invention relates to the use of novel pyrrolopyrazine derivatives of Formula I, wherein the variables n, p, q, Q, X, X′ and Y are defined as described herein, which inhibit JAK and SYK and are useful for the treatment of auto-immune and inflammatory diseases.
摘要翻译: 本发明涉及式I的新型吡咯并吡嗪衍生物的用途,其中变量n,p,q,Q,X,X'和Y如本文所述定义,其抑制JAK和SYK,并且可用于治疗 自身免疫和炎性疾病。
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