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公开(公告)号：US20090215817A1
公开(公告)日：2009-08-27
申请号：US11573928
申请日：2005-08-08
申请人： Paul V. Rucker , Kevin D. Jerome , Shaun R. Selness , John E. Baldus , Li Xing
发明人： Paul V. Rucker , Kevin D. Jerome , Shaun R. Selness , John E. Baldus , Li Xing
IPC分类号： A61K31/437 , C07D471/04 , A61P29/00
CPC分类号： C07D471/04
摘要： This invention is directed generally to triazolopyridine compounds that generally inhibit p38 kinase, TNF, and/or cyclooxygenase activity. Such triazolopyridine include compounds generally corresponding in structure to the following formula: wherein R1, R2, R3, R4, and R5 are as defined in this specification. This invention also is directed to compositions of such triazolopyridines (particularly pharmaceutical compositions), intermediates for the syntheses of such triazolopyridines, methods for making such triazolopyridines, and methods for treating (including preventing) conditions (typically pathological conditions) associated with p38 kinase activity, TNF activity, and/or cyclooxygenase-2 activity.
摘要翻译： 本发明一般涉及通常抑制p38激酶，TNF和/或环氧合酶活性的三唑并吡啶化合物。 这样的三唑并吡啶包括通常在结构上对应于下式的化合物：其中R 1，R 2，R 3，R 4和R 5如本说明书中所定义。 本发明还涉及这种三唑并吡啶（特别是药物组合物）的组合物，用于合成这种三唑并吡啶的中间体，制备这种三唑并吡啶的方法，以及用于治疗（包括预防）与p38激酶活性相关的病症（通常是病理状态）的方法， TNF活性和/或环氧合酶-2活性。
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公开(公告)号：US20090270350A1
公开(公告)日：2009-10-29
申请号：US12162048
申请日：2007-02-05
申请人： Balekudru Devadas , Susan J. Hartmann , Richard F. Heier , Kevin D. Jerome , Steve A. Kolodziej , John Mathias , Monica B. Norton , Michele A. Promo , Paul V. Rucker , Shaun Selness
发明人： Balekudru Devadas , Susan J. Hartmann , Richard F. Heier , Kevin D. Jerome , Steve A. Kolodziej , John Mathias , Monica B. Norton , Michele A. Promo , Paul V. Rucker , Shaun Selness
IPC分类号： A61K31/695 , C07F7/18 , A61K31/4439 , C07D401/12
CPC分类号： C07D401/12 , C07D403/12
摘要： This invention is directed generally to substituted pyridinone and pyrimidinone compounds that generally inhibit p38 kinase, TNF, and/or cyclooxygeπase activity. Such substituted pyridinone and pyrimidinone compounds include compounds generally corresponding in structure to the following formula: wherein Z, n, R1, R2a, R2b, R2c, R2d, R2e, R3a, R3b, R3c, R3d, R4, R5, R6, R7a, R7b, R7c, R7d and R7e are as defined in this specification. This invention also is directed to compositions of such substituted pyridinones and pyrimidinones (particularly pharmaceutical compositions), and methods for treating disorders (typically pathological disorders) associated with p38 kinase activity, TNF activity, and/or cyclooxygenase-2 activity.
摘要翻译： 本发明通常涉及通常抑制p38激酶，TNF和/或环氧糖蛋白酶活性的取代的吡啶酮和嘧啶酮化合物。 这种取代的吡啶酮和嘧啶酮化合物包括通式在下列结构相应的化合物：其中Z，n，R1，R2a，R2b，R2c，R2d，R2e，R3a，R3b，R3c，R3d，R4，R5，R6，R7a， R7b，R7c，R7d和R7e如本说明书中所定义。 本发明还涉及这种取代的吡啶酮和嘧啶酮（特别是药物组合物）的组合物，以及用于治疗与p38激酶活性，TNF活性和/或环氧合酶-2活性相关的疾病（通常为病理学障碍）的方法。
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公开(公告)号：US20090209577A1
公开(公告)日：2009-08-20
申请号：US11573764
申请日：2005-08-08
申请人： Paul V. Rucker , Kevin D. Jerome , Shaun R. Selness , John E. Baldus , Li Xing
发明人： Paul V. Rucker , Kevin D. Jerome , Shaun R. Selness , John E. Baldus , Li Xing
IPC分类号： A61K31/437 , C07D471/04 , A61P19/02
CPC分类号： C07D471/04
摘要： This invention is directed generally to triazolopyridine compounds that generally inhibit p38 kinase, TNF, and/or cyclooxygenase activity. Such triazolopyridine include compounds generally corresponding in structure to the following formula: wherein R1, R2 and R3, are as defined in this specification. This invention also is directed to compositions of such triazolopyridines (particularly pharmaceutical compositions), intermediates for the syntheses of such triazolopyridines, methods for making such triazolopyridines, and methods for treating (including preventing) conditions (typically pathological conditions) associated with p38 kinase activity, TNF activity, and/or cyclooxygenase-2 activity.
摘要翻译： 本发明一般涉及通常抑制p38激酶，TNF和/或环氧合酶活性的三唑并吡啶化合物。 这样的三唑并吡啶包括通常在结构上对应于下式的化合物：其中R1，R2和R3如本说明书中所定义。 本发明还涉及这种三唑并吡啶（特别是药物组合物）的组合物，用于合成这种三唑并吡啶的中间体，制备这种三唑并吡啶的方法，以及用于治疗（包括预防）与p38激酶活性相关的病症（通常是病理状态）的方法， TNF活性和/或环氧合酶-2活性。
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公开(公告)号：US08552035B2
公开(公告)日：2013-10-08
申请号：US13406446
申请日：2012-02-27
申请人： Paul V. Rucker
发明人： Paul V. Rucker
IPC分类号： C07D213/75 , A61K31/44
CPC分类号： C07D213/75
摘要： The present invention is directed to compounds of Formula I: or salt thereof, which are modulators of the glucocorticoid receptor. The compounds and salts of the invention are useful in the treatment of conditions mediated by glucocorticoid receptor activity.
摘要翻译： 本发明涉及式I化合物或其盐，它们是糖皮质激素受体的调节剂。 本发明的化合物和盐可用于治疗由糖皮质激素受体活性介导的病症。
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公开(公告)号：US08148409B2
公开(公告)日：2012-04-03
申请号：US12505932
申请日：2009-07-20
申请人： Paul V. Rucker
发明人： Paul V. Rucker
IPC分类号： C07D213/72 , A61K31/44
CPC分类号： C07D213/75
摘要： The present invention is directed to compounds of Formula I: or salt thereof, which are modulators of the glucocorticoid receptor. The compounds and salts of the invention are useful in the treatment of conditions mediated by glucocorticoid receptor activity.
摘要翻译： 本发明涉及式I化合物或其盐，它们是糖皮质激素受体的调节剂。 本发明的化合物和盐可用于治疗由糖皮质激素受体活性介导的病症。
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公开(公告)号：US20100069444A1
公开(公告)日：2010-03-18
申请号：US12505932
申请日：2009-07-20
申请人： Paul V. Rucker
发明人： Paul V. Rucker
CPC分类号： C07D213/75
摘要： The present invention is directed to compounds of Formula I: or salt thereof, which are modulators of the glucocorticoid receptor. The compounds and salts of the invention are useful in the treatment of conditions mediated by glucocorticoid receptor activity.
摘要翻译： 本发明涉及式I化合物或其盐，它们是糖皮质激素受体的调节剂。 本发明的化合物和盐可用于治疗由糖皮质激素受体活性介导的病症。
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17.发明授权Compounds which mimic the chemical and biological properties of discodermolide 有权模仿discodermolide的化学和生物学性质的化合物公开(公告)号：US07652031B2
公开(公告)日：2010-01-26
申请号：US10296138
申请日：2002-08-06
IPC分类号： A61K31/43 , C07D607/00
CPC分类号： C07D407/06 , C07C49/248 , C07D303/30 , C07D309/10 , C07D309/32 , C07D319/06 , C07D413/06 , C07F9/6552 , C07H15/04 , C07H15/203
摘要： Compounds which mimic the chemical and/or biological activity of discodermolide are provided.
摘要翻译： 提供了模仿盘菊酯的化学和/或生物活性的化合物。
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