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。

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。

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：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。

公开(公告)号：US20100222325A1

公开(公告)日：2010-09-02

申请号：US12711312

申请日：2010-02-24

申请人： Steven Berthel ,  Fariborz Firooznia ,  Daniel Fishlock ,  Jun-Bae Hong ,  Yan Lou ,  Matthew Lucas ,  Timothy D. Owens ,  Keshab Sarma ,  Zachary Kevin Sweeney ,  Joshua Paul Gergely Taygerly

发明人： Steven Berthel ,  Fariborz Firooznia ,  Daniel Fishlock ,  Jun-Bae Hong ,  Yan Lou ,  Matthew Lucas ,  Timothy D. Owens ,  Keshab Sarma ,  Zachary Kevin Sweeney ,  Joshua Paul Gergely Taygerly

IPC分类号： A61K31/4725 ,  C07D413/14 ,  C07D401/14 ,  C07D401/10 ,  A61P29/00 ,  A61P37/00 ,  A61K31/5377 ,  A61K31/496 ,  A61K31/502

CPC分类号： C07D401/10 ,  C07D401/14 ,  C07D403/14 ,  C07D413/14

摘要： This application discloses 5-phenyl-1H-pyridin-2-one, 6-phenyl-2H-pyridazin-3-one, and 5-Phenyl-1H-pyrazin-2-one derivatives according to generic Formulae I-III: wherein, variables Q, R, X, X′, Y1, Y2, Y2′, Y3, Y4, Y5, m, and n 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，6-苯基-2H-哒嗪-3-酮和5-苯基-1H-吡嗪-2-酮衍生物：其中， 变量Q，R，X，X'，Y1，Y2，Y2'，Y3，Y4，Y5，m和n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。