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公开(公告)号：US08309571B2
公开(公告)日：2012-11-13
申请号：US13084622
申请日：2011-04-12
IPC分类号： A01N43/42 , A61K31/44 , C07D413/00
CPC分类号： C07D487/04
摘要： A compound of Formula (I) and enantiomers, diastereomers and pharmaceutically-acceptable salts thereof. Also disclosed are pharmaceutical compositions containing compounds of Formula I, and methods of treating conditions associated with the activity of p38 kinase.
摘要翻译： 式（I）的化合物及其对映异构体，非对映异构体和药学上可接受的盐。 还公开了含有式I化合物的药物组合物，以及治疗与p38激酶活性相关的病症的方法。
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公开(公告)号：US07943658B2
公开(公告)日：2011-05-17
申请号：US12177319
申请日：2008-07-22
申请人： Chunjian Liu , Stephen T. Wrobleski , Katerina Leftheris , Gang Wu , Philip M. Sher , Bruce A. Ellsworth
发明人： Chunjian Liu , Stephen T. Wrobleski , Katerina Leftheris , Gang Wu , Philip M. Sher , Bruce A. Ellsworth
IPC分类号： A61K31/404 , C07D209/04
CPC分类号： C07D209/42 , C07D413/06
摘要： Indole indane amides which are CB2 agonists are provided which have the structure wherein R1, R2, R3, R4 and R5 are as defined herein, which compounds are useful in treating autoimmune diseases, inflammation, pain, cardiovascular disorders and other diseases mediated by CB2 receptors. A method for preventing or treating such diseases employing the compounds of the invention is also provided.
摘要翻译： 提供了CB2激动剂的吲哚二氢化茚酰胺，其具有其中R 1，R 2，R 3，R 4和R 5如本文所定义的结构，该化合物可用于治疗由CB2受体介导的自身免疫疾病，炎症，疼痛，心血管疾病和其它疾病 。 还提供了使用本发明化合物预防或治疗这些疾病的方法。
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43.发明授权公开(公告)号：US07605273B2
公开(公告)日：2009-10-20
申请号：US12118794
申请日：2008-05-12
申请人： Alaric J. Dyckman , Jagabandhu Das , Katerina Leftheris , Chunjian Liu , Rulin Zhao , Bang-Chi Chen , Stephen T. Wrobleski
发明人： Alaric J. Dyckman , Jagabandhu Das , Katerina Leftheris , Chunjian Liu , Rulin Zhao , Bang-Chi Chen , Stephen T. Wrobleski
IPC分类号： C07D231/14
CPC分类号： C07D231/14 , C07D231/12 , C07D231/40 , C07D401/12 , C07D413/12
摘要： The present invention relates to compounds having the formula, and pharmaceutically-acceptable salts, prodrugs, solvates, isomers, and/or hydrates thereof, wherein Q is an optionally-substituted phenyl, pyridyl, pyridazinyl, pyrimidinyl, or pyrazinyl ring; R2 is alkyl or an amino group as defined herein; and Z is optionally-substituted oxadiazolyl or —C(═O)NR6, wherein R6 is lower alkyl or cyclopropyl. The compounds are surprisingly advantageous in preparing pharmaceutical compositions for treating p38 kinase related conditions and/or in methods of treating conditions associated with the activity of p38 kinase in a patient.
摘要翻译： 本发明涉及具有下式的化合物及其药学上可接受的盐，前体药物，溶剂合物，异构体和/或其水合物，其中Q是任选取代的苯基，吡啶基，哒嗪基，嘧啶基或吡嗪基; R2是如本文所定义的烷基或氨基; 和Z是任选取代的恶二唑基或-C（-O）NR 6，其中R 6是低级烷基或环丙基。 该化合物在制备用于治疗p38激酶相关病症的药物组合物和/或治疗与患者中p38激酶活性相关的病症的方法中令人惊奇地有利。
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公开(公告)号：US20090041722A1
公开(公告)日：2009-02-12
申请号：US12177319
申请日：2008-07-22
申请人： Chunjian Liu , Stephen T. Wrobleski , Katerina Leftheris , Gang Wu , Philip M. Sher , Bruce A. Ellsworth
发明人： Chunjian Liu , Stephen T. Wrobleski , Katerina Leftheris , Gang Wu , Philip M. Sher , Bruce A. Ellsworth
IPC分类号： A61K31/404 , C07D209/42 , A61K31/5377 , A61P11/00 , A61P25/00 , A61K38/21 , C07D413/06
CPC分类号： C07D209/42 , C07D413/06
摘要： Indole indane amides which are CB2 agonists are provided which have the structure wherein R1, R2, R3, R4 and R5 are as defined herein, which compounds are useful in treating autoimmune diseases, inflammation, pain, cardiovascular disorders and other diseases mediated by CB2 receptors. A method for preventing or treating such diseases employing the compounds of the invention is also provided.
摘要翻译： 提供了CB2激动剂的吲哚二氢化茚酰胺，其具有其中R 1，R 2，R 3，R 4和R 5如本文所定义的结构，该化合物可用于治疗由CB2受体介导的自身免疫疾病，炎症，疼痛，心血管疾病和其它疾病 。 还提供了使用本发明化合物预防或治疗这些疾病的方法。
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公开(公告)号：US07479495B2
公开(公告)日：2009-01-20
申请号：US11143430
申请日：2005-06-02
申请人： Kevin Joseph Moriarty , Yvonne Shimshock , Gulzar Ahmed , Junjun Wu , James Wen , Wei Li , Shawn David Erickson , Jeffrey John Letourneau , Edward McDonald , Katerina Leftheris , Stephen T. Wrobleski , Zahid Hussain , Ian Henderson , Axel Metzger , John J. Baldwin , Alaric J. Dyckman
发明人： Kevin Joseph Moriarty , Yvonne Shimshock , Gulzar Ahmed , Junjun Wu , James Wen , Wei Li , Shawn David Erickson , Jeffrey John Letourneau , Edward McDonald , Katerina Leftheris , Stephen T. Wrobleski , Zahid Hussain , Ian Henderson , Axel Metzger , John J. Baldwin , Alaric J. Dyckman
IPC分类号： C07D239/32 , C07D239/48 , C07D239/50 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/12 , A61K31/505 , A61K31/506 , A61P19/02 , A61P35/00
CPC分类号： C07D251/52 , C07D231/12 , C07D233/56 , C07D249/08 , C07D251/48 , C07D251/54 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14
摘要： N-heterocyclic compounds that block cytokine production via inhibition of p38 kinase are disclosed. In one embodiment, compounds of the present invention are represented by Formula I: Methods of production, pharmaceutical compositions and methods of treating conditions associated with inappropriate p38 kinase activity or TNF-α expression utilizing compounds of the present invention are also disclosed.
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公开(公告)号：US20080275052A1
公开(公告)日：2008-11-06
申请号：US11940382
申请日：2007-11-15
IPC分类号： A61K31/4985 , C07D471/04 , A61K31/437 , C07D487/04 , A61K31/519 , A61P11/06 , A61P9/00 , A61P3/10 , A61P1/00 , A61P17/06 , A61P9/10
CPC分类号： C07D487/04
摘要： A compound of Formula (I) and enantiomers, diastereomers and pharmaceutically-acceptable salts thereof. Also disclosed are pharmaceutical compositions containing compounds of Formula I, and methods of treating conditions associated with the activity of p38 kinase.
摘要翻译： 式（I）的化合物及其对映异构体，非对映异构体和药学上可接受的盐。 还公开了含有式I化合物的药物组合物，以及治疗与p38激酶活性相关的病症的方法。
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公开(公告)号：US07390810B2
公开(公告)日：2008-06-24
申请号：US11931309
申请日：2007-10-31
申请人： Alaric J. Dyckman , Jagabandhu Das , Katerina Leftheris , Chunjian Liu , Robert V. Moquin , Stephen T. Wrobleski
发明人： Alaric J. Dyckman , Jagabandhu Das , Katerina Leftheris , Chunjian Liu , Robert V. Moquin , Stephen T. Wrobleski
IPC分类号： A61K31/501 , C07F9/02 , C07D401/12 , C07D271/06 , C07D277/84
CPC分类号： C07D231/14 , C07D231/12 , C07D231/40 , C07D401/12 , C07D413/12
摘要： The present invention provides pyrazole derived compounds of formula (I) useful for treating p38 kinase-associated conditions, where G, X, R1, R2, R3, R4, R5, R6 and m are as defined herein. The invention further pertains to pharmaceutical compositions containing at least one compound according to the invention useful for treating p38 kinase-associated conditions, and methods of inhibiting the activity of p38 kinase in a mammal.
摘要翻译： 本发明提供了可用于治疗p38激酶相关病症的式（I）的吡唑衍生化合物，其中G，X，R 1，R 2，R 2， R 3，R 4，R 5，R 6和m如本文所定义。 本发明还涉及含有至少一种可用于治疗p38激酶相关病症的本发明化合物的药物组合物，以及抑制哺乳动物中p38激酶活性的方法。
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公开(公告)号：US20080015185A1
公开(公告)日：2008-01-17
申请号：US11778219
申请日：2007-07-16
申请人： Gulzar Ahmed , Axel Metzger , Ian Henderson , David J. Diller , Jun Wen , Stephen T. Wrobleski , Katerina Leftheris , Chunjian Liu
发明人： Gulzar Ahmed , Axel Metzger , Ian Henderson , David J. Diller , Jun Wen , Stephen T. Wrobleski , Katerina Leftheris , Chunjian Liu
IPC分类号： A61K31/513 , A61K31/55 , A61P29/00 , C07D239/50
CPC分类号： C07D239/48 , C07D213/85 , C07D239/47 , C07D239/50 , C07D401/12 , C07D403/12
摘要： N-heterocyclic compounds that block cytokine production via inhibition of p38 kinase are disclosed. In one embodiment, compounds of the present invention are represented by Formula (I): Methods of production, pharmaceutical compositions and methods of treating conditions associated with inappropriate p38 kinase activity or TNF-α expression utilizing compounds of the present invention are also disclosed.
摘要翻译： 公开了通过抑制p38激酶阻断细胞因子产生的N-杂环化合物。 在一个实施方案中，本发明的化合物由式（I）表示：还公开了使用本发明的化合物来治疗与不适当p38激酶活性或TNF-α表达相关的病症的生产方法，药物组合物和方法。
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公开(公告)号：US07253174B2
公开(公告)日：2007-08-07
申请号：US11485075
申请日：2006-07-12
申请人： Gulzar Ahmed , Axel Metzger , Ian Henderson , David J. Diller , Jun Wen , Stephen T. Wrobleski , Katerina Leftheris , Chunjian Liu
发明人： Gulzar Ahmed , Axel Metzger , Ian Henderson , David J. Diller , Jun Wen , Stephen T. Wrobleski , Katerina Leftheris , Chunjian Liu
IPC分类号： C07D239/48 , A61K31/505
CPC分类号： C07D239/48 , C07D213/85 , C07D239/47 , C07D239/50 , C07D401/12 , C07D403/12
摘要： N-heterocyclic compounds that block cytokine production via inhibition of p38 kinase are disclosed. In one embodiment, compounds of the present invention are represented by Formula (I): Methods of production, pharmaceutical compositions and methods of treating conditions associated with inappropriate p38 kinase activity or TNF-α expression utilizing compounds of the present invention are also disclosed.
摘要翻译： 公开了通过抑制p38激酶阻断细胞因子产生的N-杂环化合物。 在一个实施方案中，本发明的化合物由式（I）表示：还公开了使用本发明的化合物来治疗与不适当p38激酶活性或TNF-α表达相关的病症的生产方法，药物组合物和方法。
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公开(公告)号：US07253170B2
公开(公告)日：2007-08-07
申请号：US11477010
申请日：2006-06-28
申请人： Alaric J. Dyckman , Jagabandhu Das , Katerina Leftheris , Chunjian Liu , Robert V. Moquin , Stephen T. Wrobleski
发明人： Alaric J. Dyckman , Jagabandhu Das , Katerina Leftheris , Chunjian Liu , Robert V. Moquin , Stephen T. Wrobleski
IPC分类号： A61K31/501 , A61K31/4709 , A61K31/454 , A61K31/4439 , A61K31/4152 , C07D403/02
CPC分类号： C07D231/14 , C07D231/12 , C07D231/40 , C07D401/12 , C07D413/12
摘要： The present invention provides pyrazole derived compounds of formula (I) useful for treating p38 kinase-associated conditions, where W, X, R1, R2, R3, R4, R5, R6 and m are as defined herein. The invention further pertains to pharmaceutical compositions containing at least one compound according to the invention useful for treating p38 kinase-associated conditions, and methods of inhibiting the activity of p38 kinase in a mammal.
摘要翻译： 本发明提供了可用于治疗p38激酶相关病症的式（I）的吡唑衍生化合物，其中W，X，R 1，R 2，R 2， R 3，R 4，R 5，R 6和m如本文所定义。 本发明还涉及含有至少一种可用于治疗p38激酶相关病症的本发明化合物的药物组合物，以及抑制哺乳动物中p38激酶活性的方法。
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