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公开(公告)号：US08962623B2
公开(公告)日：2015-02-24
申请号：US14001936
申请日：2012-02-29
申请人： Rupa S. Shetty , Martha J. Kelly , Bin Liu , Jinming Zou , Kristofer K. Moffett , Younghee Lee , Dora Do-York Wong
发明人： Rupa S. Shetty , Kevin J. Moriarity , Martha J. Kelly , Bin Liu , Jinming Zou , Kristofer K. Moffett , Younghee Lee
IPC分类号： A61K31/5377 , C07D487/04 , C07D491/056 , C07D401/12 , C07D413/14 , C07D403/12 , C07D401/14 , C07D407/14 , C07D409/14 , C07D417/14
CPC分类号： C07D413/14 , C07D401/12 , C07D401/14 , C07D403/12 , C07D407/14 , C07D409/14 , C07D417/14 , C07D487/04 , C07D491/056
摘要： A compound of formula (I): wherein all symbols have the same meanings as defined in the specification; a salt thereof, a solvate thereof, an N-oxide thereof, or a prodrug thereof, has an Itk inhibitory activity, and is useful as a method for preventing and/or treating atopic dermatitis, and the like.
摘要翻译： 式（I）的化合物：其中所有符号具有与说明书中定义的相同的含义; 其盐，其溶剂合物，N-氧化物或其前药具有Itk抑制活性，可用作预防和/或治疗特应性皮炎等的方法。
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2.发明授权17.beta.-nitro-11.beta.-arylsteroids and their derivatives having agonist or antagonist hormonal properties 失效17β-硝基-11β-芳族甾族化合物及其衍生物具有激动剂或拮抗剂激素特性
公开(公告)号：US5962444A
公开(公告)日：1999-10-05
申请号：US86674
申请日：1998-05-29
IPC分类号： A61K31/56 , A61K31/58 , A61K45/06 , A61P15/00 , A61P35/00 , A61P43/00 , C07J41/00 , C07J43/00
摘要： The invention is directed to 17.beta.-nitro-11.beta.-arylsteroids of formula I: ##STR1## wherein R.sup.1, R.sup.6, R.sup.7, R.sup.12 and X are as defined by the specification. The compounds exhibit potent antiprogestational activity and are useful in the treatment of fibroids, endometriosis, cervical ripening prior to delivery, hormone replacement therapy and in the control of fertility.
摘要翻译： 本发明涉及17种式I的β-硝基-11β-芳基甾族化合物：其中R1，R6，R7，R12和X如本说明书所定义。 这些化合物显示出有力的抗雌激素活性，并且可用于治疗子宫肌瘤，子宫内膜异位症，分娩前的子宫颈成熟，激素替代疗法和控制生育力。
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公开(公告)号：US07741479B2
公开(公告)日：2010-06-22
申请号：US11295638
申请日：2005-12-07
申请人： Enrique Luis Michelotti , Eric Bruce Springman , Duyan Nguyen , Rupa S. Shetty , Younghee Lee , Kristofer Kent Moffett , Jennifer Lee Ludington , Ted Tsutomis Fujimoto , Zenon D. Konteatis , Bin Liu , Frank Hollinger , Bruce D. Dorsey
发明人： Enrique Luis Michelotti , Eric Bruce Springman , Duyan Nguyen , Rupa S. Shetty , Younghee Lee , Kristofer Kent Moffett , Jennifer Lee Ludington , Ted Tsutomis Fujimoto , Zenon D. Konteatis , Bin Liu , Frank Hollinger , Bruce D. Dorsey
IPC分类号： C07D273/06
CPC分类号： C07D333/38 , C07D231/40 , C07D243/08 , C07D277/48 , C07D277/56 , C07D295/192 , C07D333/36 , C07D403/06 , C07D405/06 , C07D409/04 , C07D409/06 , C07D409/12 , C07D413/12 , C07D413/14 , C07D417/06 , C07D417/14 , C07D495/04
摘要： The present invention is directed to a compound having the formula wherein R1, R2, G, and Q are defined herein. The compounds of the present invention are useful as inhibitors of protein kinases such as MAP kinases, in particular p38 kinases. The present invention is also directed to compositions comprising a compound according to the above formula. The compounds and compositions described herein are useful for treating and preventing an inflammatory condition or disease. The present invention is also directed to a method of treating or preventing a protein kinase-mediated condition.
摘要翻译： 本发明涉及具有下式的化合物：其中R1，R2，G和Q如本文所定义。 本发明的化合物可用作蛋白激酶如MAP激酶，特别是p38激酶的抑制剂。 本发明还涉及包含根据上式的化合物的组合物。 本文所述的化合物和组合物可用于治疗和预防炎性疾病或疾病。 本发明还涉及治疗或预防蛋白激酶介导的病症的方法。
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4.发明授权17β-amino and hydroxylamino-11 β-arylsteroids and their derivatives having agonist or antagonist hormonal properties 有权17β-氨基和羟氨基-11β-芳基甾族化合物及其衍生物具有激动剂或拮抗剂激素特性公开(公告)号：US07018991B2
公开(公告)日：2006-03-28
申请号：US10611785
申请日：2003-07-02
申请人： C. Edgar Cook , John A. Kepler , Gary S. Bartley , Rupa S. Shetty
发明人： C. Edgar Cook , John A. Kepler , Gary S. Bartley , Rupa S. Shetty
摘要： The invention is directed to a novel class of steroids which exhibit potent antiprogestational activity.
摘要翻译： 本发明涉及一种新型的类固醇，其表现出有力的抗雌激素活性。
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公开(公告)号：US6043235A
公开(公告)日：2000-03-28
申请号：US357923
申请日：1999-07-21
申请人： C. Edgar Cook , Rupa S. Shetty , John A. Kepler , David Y.-W. Lee
发明人： C. Edgar Cook , Rupa S. Shetty , John A. Kepler , David Y.-W. Lee
CPC分类号： C07J33/00
摘要： The invention is directed to 11.beta.-aryl-17,17-spirothiolane substituted steroid compounds of formula (I) exhibiting binding to the progestin receptor. ##STR1## Also disclosed are methods of using and process of making the compounds.
摘要翻译： 本发明涉及表现出与孕激素受体结合的式（I）的11α-芳基-17,17-螺噻唑烷取代的类固醇化合物。 还公开了使用和制备化合物的方法。
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6.发明授权17.beta.-nitro-11.beta.-arylsteroids and their derivatives having agonist or antagonist hormonal properties 有权17β-硝基-11β-芳族甾族化合物及其衍生物具有激动剂或拮抗剂激素特性
公开(公告)号：US6093707A
公开(公告)日：2000-07-25
申请号：US434473
申请日：1999-11-05
IPC分类号： A61K31/56 , A61K31/58 , A61K45/06 , A61P15/00 , A61P35/00 , A61P43/00 , C07J41/00 , C07J43/00
摘要： The invention is directed to a novel class of steroids which exhibit potent antiprogestational activity.
摘要翻译： 本发明涉及一种新型的类固醇，其表现出有力的抗雌激素活性。
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公开(公告)号：US20140187529A1
公开(公告)日：2014-07-03
申请号：US14001936
申请日：2012-02-29
申请人： Rupa S. Shetty , Martha J. Kelly , Bin Liu , Jinming Zou , Kristopher K. Moffett , Younghee Lee
发明人： Rupa S. Shetty , Kevin J. Moriarity , Martha J. Kelly , Bin Liu , Jinming Zou , Kristopher K. Moffett , Younghee Lee
IPC分类号： C07D413/14 , C07D401/12 , C07D401/14
CPC分类号： C07D413/14 , C07D401/12 , C07D401/14 , C07D403/12 , C07D407/14 , C07D409/14 , C07D417/14 , C07D487/04 , C07D491/056
摘要： A compound of formula (I): wherein all symbols have the same meanings as defined in the specification; a salt thereof, a solvate thereof, an N-oxide thereof, or a prodrug thereof, has an Itk inhibitory activity, and is useful as a method for preventing and/or treating atopic dermatitis, and the like.
摘要翻译： 式（I）的化合物：其中所有符号具有与说明书中定义的相同的含义; 其盐，其溶剂合物，N-氧化物或其前药具有Itk抑制活性，可用作预防和/或治疗特应性皮炎等的方法。
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公开(公告)号：US06620801B2
公开(公告)日：2003-09-16
申请号：US09895395
申请日：2001-07-02
申请人： C. Edgar Cook , John A. Kepler , Gary S. Bartley , Rupa S. Shetty
发明人： C. Edgar Cook , John A. Kepler , Gary S. Bartley , Rupa S. Shetty
IPC分类号： A61K3158
摘要： The invention is directed to a novel class of steroids which exhibit potent antiprogestational activity.
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9.发明授权17.beta.-nitro-11.beta.-arylisteroids and their derivatives having agonist or antagonist hormonal properties 有权17β-硝基-11β-芳醚甾族化合物及其衍生物具有激动剂或拮抗剂的激素特性
公开(公告)号：US6015805A
公开(公告)日：2000-01-18
申请号：US317945
申请日：1999-05-25
IPC分类号： A61K31/56 , A61K31/58 , A61K45/06 , A61P15/00 , A61P35/00 , A61P43/00 , C07J41/00 , C07J43/00
摘要： The invention is directed to 11.beta.-arylsteroids of formula II: ##STR1## wherein R.sup.1, R.sup.6, R.sup.8, R.sup.12 and X are as defined by the specification. The compounds exhibit potent antiprogestational activity and are useful in the treatment of fibroids, endometriosis, cervical ripening prior to delivery, hormone replacement therapy and in the control of fertility.
摘要翻译： 本发明涉及式II的11β-芳基甾族化合物：其中R1，R6，R8，R12和X如本说明书所定义。 这些化合物显示出有力的抗雌激素活性，并且可用于治疗子宫肌瘤，子宫内膜异位症，分娩前的子宫颈成熟，激素替代疗法和控制生育力。
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