-
公开(公告)号:US08426409B2
公开(公告)日:2013-04-23
申请号:US12460387
申请日:2009-07-17
申请人: Rama K. Kondru , Yan Lou , Eric Brian Sjogren , Michael Soth
发明人: Rama K. Kondru , Yan Lou , Eric Brian Sjogren , Michael Soth
IPC分类号: A01N43/58 , A01N43/60 , A61K31/50 , A61K31/495 , C07D401/00 , C07D403/00 , C07D413/00 , C07D417/00 , C07D419/00
CPC分类号: C07D487/04
摘要: This application discloses 6-Phenyl-imidazo[1,2-a]pyrazine derivatives according to generic Formulae I-V: wherein, variables Q, R, 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]吡嗪衍生物:其中变量Q,R,Y 1,Y 2,Y 3,Y 4,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。
-
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.
-
公开(公告)号:US20110288067A1
公开(公告)日:2011-11-24
申请号:US13110062
申请日:2011-05-18
申请人: Robert Than Hendricks , Johannes Hermann , Saul Jaime-Figueroa , Rama Kondru , Yan Lou , Stephen Lynch , Timothy D. Owens , Michael Soth , Calvin Yee
发明人: Robert Than Hendricks , Johannes Hermann , Saul Jaime-Figueroa , Rama Kondru , Yan Lou , Stephen Lynch , Timothy D. Owens , Michael Soth , Calvin Yee
IPC分类号: A61K31/4985 , C07D295/155 , C07D491/107 , A61K31/541 , A61P29/00 , A61P37/00 , A61P35/00 , A61P25/00 , A61P9/00 , A61P3/10 , A61P37/04 , A61P11/06 , A61P19/04 , A61P17/06 , A61P37/06 , A61P17/00 , A61P5/14 , A61P1/04 , A61P1/00 , A61P25/28 , A61P35/02 , C07D487/04
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 Q and R, R2, and R3 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Q和R,R2和R3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 。
-
公开(公告)号:US08008298B2
公开(公告)日:2011-08-30
申请号:US12378977
申请日:2009-02-20
申请人: Joe Timothy Bamberg , Daisy Joe DuBois , Todd Richard Elworthy , Robert Than Hendricks , Johannes Cornelius Hermann , Alam Jahangir , Rama K. Kondru , Remy Lemoine , Yan Lou , Timothy D. Owens , David Bernard Smith , Michael Soth , Hanbiao Yang
发明人: Joe Timothy Bamberg , Daisy Joe DuBois , Todd Richard Elworthy , Robert Than Hendricks , Johannes Cornelius Hermann , Alam Jahangir , Rama K. Kondru , Remy Lemoine , Yan Lou , Timothy D. Owens , David Bernard Smith , Michael Soth , Hanbiao Yang
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 Q1, R, and X 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Q1,R和X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。
-
公开(公告)号:US07932254B2
公开(公告)日:2011-04-26
申请号:US12378869
申请日:2009-02-20
申请人: Daisy Joe DuBois , Robert Than Hendricks , Johannes Cornelius Hermann , Rama K. Kondru , Yan Lou , Timothy D. Owens , Calvin Wesley Yee
发明人: Daisy Joe DuBois , Robert Than Hendricks , Johannes Cornelius Hermann , Rama K. Kondru , Yan Lou , Timothy D. Owens , Calvin Wesley Yee
IPC分类号: A61K31/495
CPC分类号: C07D519/00 , C07D487/04
摘要: The present invention relates to the use of novel pyrrolopyrazine derivatives of Formula I, wherein the variables Q1 and R 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Q1和R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。
-
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。
-
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。
-
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。
-
公开(公告)号:US20090215788A1
公开(公告)日:2009-08-27
申请号:US12378971
申请日:2009-02-20
申请人: Todd Richard Elworthy , Robert Than Hendricks , Rama K. Kondru , Yan Lou , Timothy D. Owens , Michael Soth , Hanbiao Yang
发明人: Todd Richard Elworthy , Robert Than Hendricks , Rama K. Kondru , Yan Lou , Timothy D. Owens , Michael Soth , Hanbiao Yang
IPC分类号: A61K31/4985 , C07D487/04
CPC分类号: C07D487/04
摘要: The present invention relates to the use of novel pyrrolopyrazine derivatives of Formula I, wherein the variables Q and R are defined as described herein, which inhibit JAK and SYK and are useful for the treatment of auto-immune and inflammatory diseases.
-
公开(公告)号:US20090215785A1
公开(公告)日:2009-08-27
申请号:US12378837
申请日:2009-02-20
申请人: Daisy Joe DuBois , Todd Richard Elworthy , Robert Than Hendricks , Johannes Cornelius Hermann , Raman K. Kondru , Yan Lou , Timothy D. Owens , David Bernard Smith
发明人: Daisy Joe DuBois , Todd Richard Elworthy , Robert Than Hendricks , Johannes Cornelius Hermann , Raman K. Kondru , Yan Lou , Timothy D. Owens , David Bernard Smith
IPC分类号: A61K31/4985 , C07D487/04 , A61P35/00
CPC分类号: C07D487/04
摘要: The present invention relates to the use of novel pyrrolopyrazine derivatives of Formula I, wherein the variables Q and R 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Q和R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。
-
-
-
-
-
-
-
-
-