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公开(公告)号：US20060247247A1
公开(公告)日：2006-11-02
申请号：US11477010
申请日：2006-06-28
申请人： Alaric Dyckman , Jagabandhu Das , Katerina Leftheris , Chunjian Liu , Robert Moquin , Stephen Wrobleski
发明人： Alaric Dyckman , Jagabandhu Das , Katerina Leftheris , Chunjian Liu , Robert Moquin , Stephen 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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公开(公告)号：US20050004176A1
公开(公告)日：2005-01-06
申请号：US10837778
申请日：2004-05-03
申请人： Alaric Dyckman , Jagabandhu Das , Katerina Leftheris , Chunjian Liu , Robert Moquin , Stephen Wrobleski
发明人： Alaric Dyckman , Jagabandhu Das , Katerina Leftheris , Chunjian Liu , Robert Moquin , Stephen Wrobleski
IPC分类号： A61K20060101 , A61K31/415 , A61K31/4152 , A61K31/4155 , A61K31/416 , A61K31/4439 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/535 , A61K31/675 , C07D20060101 , C07D231/04 , C07D231/14 , C07D231/18 , C07D401/04 , C07D401/12 , C07D403/04 , C07D405/12 , C07D413/12 , C07D413/14 , C07
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 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：US20080004278A1
公开(公告)日：2008-01-03
申请号：US11832924
申请日：2007-08-02
申请人： Alaric Dyckman , Jagabandhu Das , Katerina Leftheris , Chunjian Liu , Robert Moquin , Stephen Wrobleski
发明人： Alaric Dyckman , Jagabandhu Das , Katerina Leftheris , Chunjian Liu , Robert Moquin , Stephen Wrobleski
IPC分类号： C07D231/10 , A61K31/4155 , A61K31/5377 , C07D403/02 , C07D413/02 , C07D231/56 , A61P29/00
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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4.发明申请公开(公告)号：US20050159424A1
公开(公告)日：2005-07-21
申请号：US10838129
申请日：2004-05-03
申请人： Alaric Dyckman , Jagabandhu Das , Katerina Leftheris , Chunjian Liu , Rulin Zhao , Bang-Chi Chen , Stephen Wrobleski
发明人： Alaric Dyckman , Jagabandhu Das , Katerina Leftheris , Chunjian Liu , Rulin Zhao , Bang-Chi Chen , Stephen Wrobleski
IPC分类号： A61K20060101 , A61K31/415 , A61K31/4152 , A61K31/4155 , A61K31/416 , A61K31/4439 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/535 , A61K31/675 , C07D20060101 , C07D231/04 , C07D231/14 , C07D231/18 , C07D401/04 , C07D401/12 , C07D403/04 , C07D405/12 , C07D413/12 , C07D413/14 , C07D43/04
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; R 2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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5.发明申请Methods for the preparation of pyrrolotriazine compounds useful as kinase inhibitors 有权制备用作激酶抑制剂的吡咯并三嗪化合物的方法公开(公告)号：US20050107462A1
公开(公告)日：2005-05-19
申请号：US11019788
申请日：2004-12-22
申请人： Jollie Godfrey , John Hynes , Alaric Dyckman , Katerina Leftheris , Zhongping Shi , Stephen Wrobleski , Wendel William Doubleday , John Grosso
发明人： Jollie Godfrey , John Hynes , Alaric Dyckman , Katerina Leftheris , Zhongping Shi , Stephen Wrobleski , Wendel William Doubleday , John Grosso
IPC分类号： A61P11/06 , A61P19/02 , A61P19/10 , C07D207/50 , C07D487/04 , C07D519/00 , A61K31/4015 , A61K31/401 , A61K31/4025
CPC分类号： C07D487/04 , C07D207/50
摘要： Methods of preparing kinase inhibiting pharmaceutical compounds having the formula (I): or a pharmaceutically acceptable salt or solvate thereof, wherein R1 through R6 and Z are as described in the specification. The methods according to the invention utilize an amination process, in which a pyrrole is reacted with a haloamine, preferably chloramine. This step is followed by cyclization to form the pyrrolotriazine core.
摘要翻译： 制备具有式（I）的激酶抑制药物化合物或其药学上可接受的盐或溶剂化物的方法，其中R 1至R 6和Z如 规范。 根据本发明的方法利用胺化方法，其中吡咯与卤胺，优选氯胺反应。 该步骤之后环化形成吡咯并三嗪核心。
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6.发明申请Heteroaryl-substituted pyrrolo-triazine compounds useful as kinase inhibitors 有权可用作激酶抑制剂的杂芳基取代的吡咯并 - 三嗪化合物公开(公告)号：US20050043306A1
公开(公告)日：2005-02-24
申请号：US10678388
申请日：2003-10-03
IPC分类号： C07D487/04 , A61K31/53
CPC分类号： C07D487/04
摘要： Compounds having the formula (I), and pharmaceutically acceptable salts, prodrugs, and solvates thereof, are useful as kinase inhibitors, wherein R1, R2, R3, R4, R5, R6, X and Z are as described in the specification.
摘要翻译： 具有式（I）的化合物及其药学上可接受的盐，前药和溶剂合物可用作激酶抑制剂，其中R1，R2，R3，R4，R5，R6，X和Z如说明书中所述。
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公开(公告)号：US20080108626A1
公开(公告)日：2008-05-08
申请号：US11931309
申请日：2007-10-31
申请人： Alaric Dyckman , Jagabandhu Das , Katerina Leftheris , Chunjian Liu , Robert Moquin , Stephen Wrobleski
发明人： Alaric Dyckman , Jagabandhu Das , Katerina Leftheris , Chunjian Liu , Robert Moquin , Stephen Wrobleski
IPC分类号： A61K31/501 , C07D231/12 , A61K31/415 , C07D413/12 , A61K31/42 , C07D413/14 , A61K31/4439 , C07D401/04
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：US20070043053A1
公开(公告)日：2007-02-22
申请号：US11585598
申请日：2006-10-24
IPC分类号： A61K31/53 , C07D487/04
CPC分类号： C07D487/04
摘要： Compounds having the formula (I), and pharmaceutically acceptable salts, prodrugs, and solvates thereof, are useful as kinase inhibitors, wherein R1, R2, R3, R4, R5, R6, X and Z are as described in the specification.
摘要翻译： 具有式（I）的化合物及其药学上可接受的盐，前药和溶剂合物可用作激酶抑制剂，其中R 1，R 2，R 2， 3，R 4，R 5，R 6，X和Z如说明书中所述。
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公开(公告)号：US20050239770A1
公开(公告)日：2005-10-27
申请号：US11143430
申请日：2005-06-02
申请人： Kevin Moriarty , Yvonne Shimshock , Gulzar Ahmed , Junjun Wu , James Wen , Wei Li , Shawn Erickson , Jeffrey Letourneau , Edward McDonald , Katerina Leftheris , Stephen Wrobleski , Zahid Hussain , Ian Henderson , Axel Metzger , John Baldwin , Alaric Dyckman
发明人： Kevin Moriarty , Yvonne Shimshock , Gulzar Ahmed , Junjun Wu , James Wen , Wei Li , Shawn Erickson , Jeffrey Letourneau , Edward McDonald , Katerina Leftheris , Stephen Wrobleski , Zahid Hussain , Ian Henderson , Axel Metzger , John Baldwin , Alaric Dyckman
IPC分类号： A61K31/40 , A61K31/551 , C07D251/52 , C07D251/54 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D403/14 , C07D405/14 , C07D521/00
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.
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化合物的生产方法，药物组合物和治疗与不适当的p38激酶活性或TNF-α表达相关的病症的方法。
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公开(公告)号：US07160883B2
公开(公告)日：2007-01-09
申请号：US10420399
申请日：2003-04-22
IPC分类号： C07D487/04 , C07D413/08 , A61K31/53 , A61K31/5377 , A61P19/02 , A61P19/04 , A61P9/10
CPC分类号： C07D487/04
摘要： Compounds having the formula (I), and pharmaceutically acceptable salts, prodrugs, and solvates thereof, are useful as kinase inhibitors, wherein R1, R2, R3, R4, R5, R6, X and Z are as described in the specification.
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