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公开(公告)号:US09353096B2
公开(公告)日:2016-05-31
申请号:US14683452
申请日:2015-04-10
发明人: Christine E. Brotherton-Pleiss , Zhi Chen , Shawn David Erickson , Kyungjin Kim , Hongju Li , Yimin Qian , Sung-Sau So , Peter Michael Wovkulich , Lin Yi
IPC分类号: C07D241/04 , C07D265/30 , C07D279/12 , C07D413/04 , C07D413/06 , C07D413/12
CPC分类号: C07D413/12 , C07D241/04 , C07D265/30 , C07D279/12 , C07D413/04 , C07D413/06
摘要: The invention is concerned with the compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein Y, R1, R2 and R3 are defined in the detailed description and claims. In addition, the present invention relates to methods of manufacturing and using the compounds of formula (I) as well as pharmaceutical compositions containing such compounds. The compounds of formula (I) are antagonists of the TRPA1 channel and may be useful in treating inflammatory diseases and disorders associated with that channel.
摘要翻译: 本发明涉及式(I)化合物及其药学上可接受的盐,其中Y,R 1,R 2和R 3在详细描述和权利要求书中定义。 此外,本发明涉及制备和使用式(I)化合物的方法以及含有这些化合物的药物组合物。 式(I)化合物是TRPA1通道的拮抗剂,可用于治疗与该通道相关的炎性疾病和病症。
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公开(公告)号:US09580411B2
公开(公告)日:2017-02-28
申请号:US14671643
申请日:2015-03-27
发明人: Christine E. Brotherton-Pleiss , Huifen Chen , Shaoqing Chen , Zhi Chen , Shawn David Erickson , Anthony Estrada , Kyungjin Kim , Hongju Li , Allen John Lovey , Joseph P. Lyssikatos , Yimin Qian , Sung-Sau So , Peter Michael Wovkulich , Lin Yi
IPC分类号: C07D305/08 , C07D409/12 , C07D231/18 , C07D401/04 , C07D401/12 , C07D403/04 , C07D237/08 , C07D239/42 , C07D409/14 , C07D241/12 , C07D213/26 , C07D213/40 , C07C311/19 , C07C311/16 , C07C311/17 , C07C311/20 , C07D239/26 , C07D305/06 , C07D403/12
CPC分类号: C07D409/12 , C07C311/16 , C07C311/17 , C07C311/19 , C07C311/20 , C07C2601/02 , C07D213/26 , C07D213/40 , C07D231/18 , C07D237/08 , C07D239/26 , C07D239/42 , C07D241/12 , C07D305/06 , C07D305/08 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/12 , C07D409/14
摘要: The invention is concerned with the compounds of formula (I): and salts thereof, wherein X, Y, Z, R1, R2, R3, R3′, R4, R5 and R6 are defined in the detailed description and claims. In addition, the present invention relates to methods of manufacturing and using the compounds of Formula (I) as well as pharmaceutical compositions containing such compounds. The compounds may be useful in treating diseases and conditions mediated by TRPA1, such as pain.
摘要翻译: 本发明涉及式(I)化合物及其盐,其中X,Y,Z,R 1,R 2,R 3,R 3,R 4,R 5和R 6在详细说明书和权利要求书中定义。 此外,本发明涉及制备和使用式(I)化合物的方法以及含有这些化合物的药物组合物。 该化合物可用于治疗TRPA1介导的疾病和病症,例如疼痛。
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公开(公告)号:US09556147B2
公开(公告)日:2017-01-31
申请号:US14768488
申请日:2014-03-03
IPC分类号: A61K31/50 , A61K31/501 , C07D237/30 , C07D401/14 , C07D237/32 , A61K31/502
CPC分类号: C07D401/14 , A61K31/502 , C07D237/32
摘要: This application discloses compounds according to generic Formula I: (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:(I)其中所有变量如本文所述限定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:US09499548B2
公开(公告)日:2016-11-22
申请号:US14427501
申请日:2013-09-10
发明人: Christine E. Brotherton-Pleiss , Ramona Hilgenkamp , Rama K. Kondru , Francisco Javier Lopez-Tapia , Yan Lou
IPC分类号: C07D487/04 , C07D401/14 , C07D413/14 , C07D403/14 , C07D405/14
CPC分类号: C07D487/04 , C07D401/14 , C07D403/14 , C07D405/14 , C07D413/14
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.
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公开(公告)号:US09359337B2
公开(公告)日:2016-06-07
申请号:US14712655
申请日:2015-05-14
IPC分类号: C07D211/26 , C07D413/04 , C07D265/30 , C07D207/09
CPC分类号: C07D413/04 , C07D207/09 , C07D211/26 , C07D265/30
摘要: The invention is concerned with a compound of formula (I) and pharmaceutically acceptable salts thereof wherein R1 to R3, X and Y are as defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.
摘要翻译: 本发明涉及式(I)化合物及其药学上可接受的盐,其中R1至R3,X和Y如说明书和权利要求中所定义。 式(I)化合物可以用作药物。
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公开(公告)号:US08742098B2
公开(公告)日:2014-06-03
申请号:US13706399
申请日:2012-12-06
IPC分类号: C07D413/14 , A61K31/5377
CPC分类号: C07D413/14 , A61K31/5377 , C07D471/04 , 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。
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公开(公告)号:US20150210704A1
公开(公告)日:2015-07-30
申请号:US14427501
申请日:2013-09-10
发明人: Christine E. Brotherton-Pleiss , Ramona Hilgenkamp , Rama K. Kondru , Francisco Javier Lopez-Tapia , Yan Lou
IPC分类号: C07D487/04 , C07D405/14 , C07D401/14
CPC分类号: C07D487/04 , C07D401/14 , C07D403/14 , C07D405/14 , C07D413/14
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。
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公开(公告)号:US20130178461A1
公开(公告)日:2013-07-11
申请号:US13781815
申请日:2013-03-01
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: C07D401/14 , C07D405/14 , C07D487/04
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。
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公开(公告)号:US09388172B2
公开(公告)日:2016-07-12
申请号:US14707524
申请日:2015-05-08
IPC分类号: C07D413/14 , C07D413/06 , C07D403/06 , C07D401/06 , C07D271/107
CPC分类号: C07D413/06 , C07D271/107 , C07D401/06 , C07D403/06 , C07D413/14
摘要: The invention is concerned with the compounds of formula (I): and pharmaceutically acceptable salts thereof. In addition, the present invention relates to methods of manufacturing and using the compounds of formula (I) as well as pharmaceutical compositions containing such compounds. The compounds of formula (I) are antagonists of the TRPA1 channel and may be useful in treating inflammatory diseases and disorders associated with that channel.
摘要翻译: 本发明涉及式(I)化合物及其药学上可接受的盐。 此外,本发明涉及制备和使用式(I)化合物的方法以及含有这些化合物的药物组合物。 式(I)化合物是TRPA1通道的拮抗剂,可用于治疗与该通道相关的炎性疾病和病症。
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公开(公告)号:US20160002206A1
公开(公告)日:2016-01-07
申请号:US14768488
申请日:2014-03-03
IPC分类号: C07D401/14
CPC分类号: C07D401/14 , A61K31/502 , C07D237/32
摘要: This application discloses compounds according to generic Formula I: (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:(I)其中所有变量如本文所述限定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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