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公开(公告)号:US20090170920A1
公开(公告)日:2009-07-02
申请号:US12331538
申请日:2008-12-10
IPC分类号: A61K31/4166 , C07D403/06 , A61P35/00
CPC分类号: C07D233/74 , C07D233/78 , C07D417/14
摘要: The present invention relates to compounds of the formula methods for the preparation thereof, and methods for their use. The compounds are useful in treating diseases characterized by the hyperactivity of MEK. Accordingly the compounds are useful in the treatment of diseases, such as cancer, cognitive and CNS disorders, and inflammatory/autoimmune diseases.
摘要翻译: 本发明涉及其制备方法的化合物及其使用方法。 该化合物可用于治疗以MEK多动症为特征的疾病。 因此,该化合物可用于治疗诸如癌症,认知和CNS疾病以及炎性/自身免疫性疾病的疾病。
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公开(公告)号:US20090048452A1
公开(公告)日:2009-02-19
申请号:US12186648
申请日:2008-08-06
IPC分类号: C07D403/06 , C07D409/14
CPC分类号: C07D403/06
摘要: This invention relates to compounds of formula I: or pharmaceutically acceptable salts thereof,wherein R1, R2, R3, R4, R5, and R6 are described in this application. These compounds inhibit the enzymes MEK 1 and MEK2, protein kinases that are components of the MAP kinase signal transduction pathway and as such the compounds will have anti-hyperproliferative cellular activity.
摘要翻译: 本发明涉及式I化合物或其药学上可接受的盐,其中本申请中描述了R1,R2,R3,R4,R5和R6。 这些化合物抑制作为MAP激酶信号转导途径成分的蛋白激酶MEK1和MEK2,因此这些化合物将具有抗过度增殖的细胞活性。
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公开(公告)号:US08063085B2
公开(公告)日:2011-11-22
申请号:US12331538
申请日:2008-12-10
IPC分类号: A01N43/50 , A61K31/415 , C07D407/00
CPC分类号: C07D233/74 , C07D233/78 , C07D417/14
摘要: The present invention relates to compounds of the formula methods for the preparation thereof, and methods for their use. The compounds are useful in treating diseases characterized by the hyperactivity of MEK. Accordingly the compounds are useful in the treatment of diseases, such as cancer, cognitive and CNS disorders, and inflammatory/autoimmune diseases.
摘要翻译: 本发明涉及其制备方法的化合物及其使用方法。 该化合物可用于治疗以MEK多动症为特征的疾病。 因此,该化合物可用于治疗诸如癌症,认知和CNS疾病以及炎性/自身免疫性疾病的疾病。
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公开(公告)号:US07557221B2
公开(公告)日:2009-07-07
申请号:US12186648
申请日:2008-08-06
IPC分类号: A61K31/4184 , C07D403/06
CPC分类号: C07D403/06
摘要: This invention relates to compounds of formula I: or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, and R6 are described in this application. These compounds inhibit the enzymes MEK 1 and MEK2, protein kinases that are components of the MAP kinase signal transduction pathway and as such the compounds will have anti-hyperproliferative cellular activity.
摘要翻译: 本发明涉及式I化合物或其药学上可接受的盐,其中本申请中描述了R1,R2,R3,R4,R5和R6。 这些化合物抑制作为MAP激酶信号转导途径成分的蛋白激酶MEK1和MEK2,因此这些化合物将具有抗过度增殖的细胞活性。
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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。
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