公开(公告)号：US20120295885A1

公开(公告)日：2012-11-22

申请号：US13472541

申请日：2012-05-16

申请人： Roland Joseph Billedeau ,  Rama K. Kondru ,  Francisco Javier Lopez-Tapia ,  Yan Lou ,  Timothy D. Owens ,  Yimin Qian ,  Sung-Sau So ,  Kshitij C. Thakkar ,  Jutta Wanner

发明人： Roland Joseph Billedeau ,  Rama K. Kondru ,  Francisco Javier Lopez-Tapia ,  Yan Lou ,  Timothy D. Owens ,  Yimin Qian ,  Sung-Sau So ,  Kshitij C. Thakkar ,  Jutta Wanner

IPC分类号： A61K31/502 ,  A61P37/06 ,  A61P11/06 ,  C07D405/10 ,  C07D403/10 ,  C07D417/10 ,  C07D413/10 ,  C07D401/10 ,  A61K31/4725 ,  C07D413/14 ,  A61K31/5377 ,  C07D471/04 ,  C07D401/14 ,  C07D487/04 ,  A61K31/519 ,  A61K31/541 ,  A61P29/00

CPC分类号： C07D405/10 ,  C07D401/10 ,  C07D401/14 ,  C07D403/10 ,  C07D413/10 ,  C07D417/10 ,  C07D471/04

摘要： This application discloses compounds according to generic Formula I: wherein all variables 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的化合物：其中所有变量如本文所述限定，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：US08729078B2

公开(公告)日：2014-05-20

申请号：US13472541

申请日：2012-05-16

申请人： Roland Joseph Billedeau ,  Rama K. Kondru ,  Francisco Javier Lopez-Tapia ,  Yan Lou ,  Timothy D. Owens ,  Yimin Qian ,  Sung-Sau So ,  Kshitij C. Thakkar ,  Jutta Wanner ,  Omar Jose Morales

发明人： Roland Joseph Billedeau ,  Rama K. Kondru ,  Francisco Javier Lopez-Tapia ,  Yan Lou ,  Timothy D. Owens ,  Yimin Qian ,  Sung-Sau So ,  Kshitij C. Thakkar ,  Jutta Wanner ,  Omar Jose Morales

IPC分类号： A01N43/58 ,  A61K31/50 ,  C07D237/00

CPC分类号： C07D405/10 ,  C07D401/10 ,  C07D401/14 ,  C07D403/10 ,  C07D413/10 ,  C07D417/10 ,  C07D471/04

摘要： This application discloses compounds according to generic Formula I: wherein all variables 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的化合物：其中所有变量如本文所述限定，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：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.

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：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：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：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。

公开(公告)号：US20100160389A1

公开(公告)日：2010-06-24

申请号：US12637923

申请日：2009-12-15

申请人： Jacob Berger ,  Joan Marie Caroon ,  Francisco Javier Lopez-Tapia ,  Dov Nitzan ,  Keith Adrian Murray Walker ,  Shu-Hai Zhao

发明人： Jacob Berger ,  Joan Marie Caroon ,  Francisco Javier Lopez-Tapia ,  Dov Nitzan ,  Keith Adrian Murray Walker ,  Shu-Hai Zhao

IPC分类号： A61K31/4412 ,  C07D213/78 ,  A61P19/02 ,  A61P37/06

CPC分类号： C07D211/86 ,  C07D405/12

摘要： Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, n, R1, R2, R3, R4, R5 and Ra 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，R1，R2，R3，R4，R5和Ra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。

公开(公告)号：US08288552B2

公开(公告)日：2012-10-16

申请号：US12637923

申请日：2009-12-15

申请人： Jacob Berger ,  Joan Marie Caroon ,  Francisco Javier Lopez-Tapia ,  Dov Nitzan ,  Keith Adrian Murray Walker ,  Shu-Hai Zhao

发明人： Jacob Berger ,  Joan Marie Caroon ,  Francisco Javier Lopez-Tapia ,  Dov Nitzan ,  Keith Adrian Murray Walker ,  Shu-Hai Zhao

IPC分类号： C07D211/00 ,  A61K31/44

CPC分类号： C07D211/86 ,  C07D405/12

摘要： Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, n, R1, R2, R3, R4, R5 and Ra 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，R1，R2，R3，R4，R5和Ra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。

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。