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![Imidazo-fused oxazolo [4,5-b]pyridine and imidazo-fused thiazolo[4,5-b]pyridine based tricyclic compounds and pharmaceutical compositions comprising same](/abs-image/US/2008/11/25/US07456194B2/abs.jpg.150x150.jpg)
1.发明授权Imidazo-fused oxazolo [4,5-b]pyridine and imidazo-fused thiazolo[4,5-b]pyridine based tricyclic compounds and pharmaceutical compositions comprising same 有权咪唑并恶唑并[4,5-b]吡啶和咪唑并稠合的噻唑并[4,5-b]吡啶三环化合物和包含它们的药物组合物公开(公告)号：US07456194B2
公开(公告)日：2008-11-25
申请号：US11272401
申请日：2005-11-10
申请人： Alaric Dyckman , William J. Pitts , Makonen Belema , Patrice Gill , James Kempson , Yuping Qiu , Claude Quesnelle , Steven H. Spergel , F. Christopher Zusi
发明人： Alaric Dyckman , William J. Pitts , Makonen Belema , Patrice Gill , James Kempson , Yuping Qiu , Claude Quesnelle , Steven H. Spergel , F. Christopher Zusi
IPC分类号： A61K31/4365 , A61K31/437 , C07D471/14 , C07D471/16
CPC分类号： C07D513/14
摘要： The present invention provides for pyrazolopurine-based tricyclic compounds having the formula (I), wherein R1, R2, R3, and R6 are as described herein. The present invention further provides pharmaceutical compositions comprising such compounds, as well as the use of such compounds for treating inflammatory and immune diseases.
摘要翻译： 本发明提供具有式（I）的吡唑并嘌呤类三环化合物，其中R 1，R 2，R 3和R 3，R 如本文所述。 本发明还提供包含这些化合物的药物组合物，以及这些化合物用于治疗炎症和免疫疾病的用途。
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![Imidazo-fused oxazolo[4,5-b]pyridine and imidazo-fused thiazolo[4,5-b]pyridine based tricyclic compounds and pharmaceutical compositions comprising same](/abs-image/US/2006/05/18/US20060106051A1/abs.jpg.150x150.jpg)
2.发明申请Imidazo-fused oxazolo[4,5-b]pyridine and imidazo-fused thiazolo[4,5-b]pyridine based tricyclic compounds and pharmaceutical compositions comprising same 有权咪唑并恶唑并[4,5-b]吡啶和咪唑并稠合的噻唑并[4,5-b]吡啶三环化合物和包含它们的药物组合物公开(公告)号：US20060106051A1
公开(公告)日：2006-05-18
申请号：US11272401
申请日：2005-11-10
申请人： Alaric Dyckman , William Pitts , Makonen Belema , Patrice Gill , James Kempson , Yuping Qiu , Claude Quesnelle , Steven Spergel , F. Zusi
发明人： Alaric Dyckman , William Pitts , Makonen Belema , Patrice Gill , James Kempson , Yuping Qiu , Claude Quesnelle , Steven Spergel , F. Zusi
IPC分类号： A61K31/4745 , C07D498/14
CPC分类号： C07D513/14
摘要： The present invention provides for pyrazolopurine-based tricyclic compounds having the formula (I), wherein R1, R2, R3, and R6 are as described herein. The present invention further provides pharmaceutical compositions comprising such compounds, as well as the use of such compounds for treating inflammatory and immune diseases.
摘要翻译： 本发明提供具有式（I）的吡唑并嘌呤类三环化合物，其中R 1，R 2，R 3和R 3，R 如本文所述。 本发明还提供包含这些化合物的药物组合物，以及这些化合物用于治疗炎症和免疫疾病的用途。
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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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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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公开(公告)号：US20110098467A1
公开(公告)日：2011-04-28
申请号：US12983048
申请日：2010-12-31
IPC分类号： 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：US07759343B2
公开(公告)日：2010-07-20
申请号：US12259483
申请日：2008-10-28
IPC分类号： C07D487/04 , C07D403/12 , C07D413/08 , A61K31/53 , A61P9/10 , A61P19/02 , A61P19/04 , A61P35/00
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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9.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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10.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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