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公开(公告)号:US07592338B2
公开(公告)日:2009-09-22
申请号:US11832924
申请日:2007-08-02
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: A61K31/4155 , A61K31/5377 , C07D403/02 , C07D413/02 , C07D231/56
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 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:US07414056B2
公开(公告)日:2008-08-19
申请号:US10837778
申请日:2004-05-03
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:US07151113B2
公开(公告)日:2006-12-19
申请号:US10838006
申请日:2004-05-03
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: C07D271/113 , A61K31/4155
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: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: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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6.
公开(公告)号:US06962915B2
公开(公告)日:2005-11-08
申请号:US10440864
申请日:2003-05-19
IPC分类号: A61K31/519 , A61K31/5377 , A61K31/551 , A61P1/00 , A61P1/04 , A61P1/16 , A61P1/18 , A61P3/10 , A61P5/14 , A61P7/00 , A61P7/04 , A61P7/06 , A61P9/00 , A61P9/10 , A61P11/00 , A61P11/06 , A61P11/16 , A61P13/12 , A61P17/00 , A61P17/04 , A61P17/06 , A61P19/00 , A61P19/02 , A61P19/06 , A61P19/08 , A61P19/10 , A61P21/00 , A61P21/04 , A61P25/00 , A61P25/16 , A61P25/28 , A61P29/00 , A61P31/00 , A61P31/04 , A61P31/12 , A61P31/18 , A61P33/06 , A61P35/00 , A61P35/02 , A61P35/04 , A61P37/02 , A61P37/06 , A61P37/08 , A61P43/00 , C07D487/04
CPC分类号: C07D487/04
摘要: Compounds having the formula (I), and pharmaceutically acceptable salts or prodrugs thereof, are useful as kinase inhibitors, wherein Y is —C(═O)NR1—, —NR1C(═O)—, —NR1C(═O)NR1—, —NR1SO2—, —SO2NR1—, —C(═O)—, —OC(═O)—, or —CO2—; B is alkyl, substituted alkyl, alkenyl, substituted alkenyl, hydroxy, alkoxy, aryl, cycloalkyl, heteroaryl, and heterocyclo; or when Y is —C(═O)NR1—, B also may be selected from —C(═O)R8, —C(═O)NR8R9, and —CO2R8; R1 is hydrogen, C1-4alkyl, or substituted C1-4alkyl; R2 is hydrogen or C1-4alkyl; R3 is hydrogen, methyl, perfluoromethyl, hydroxy, methoxy, halogen, cyano, NH2, or NH(CH3); and R4, R5, R6, R7, R8, and R9 are as defined 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或前药可用作激酶抑制剂,其中Y是-C(-O)NR 1 - , - NR 1 - C(-O) - , - NR 1 C(-O)NR 1 - , - NR 1 SO 2 - , - SO 2 - , - C( - ) - , - OC(-O) - 或-CO 2 SUB> - ; B是烷基,取代的烷基,烯基,取代的烯基,羟基,烷氧基,芳基,环烷基,杂芳基和杂环; 或当Y为-C(-O)NR 1 - )时,B也可以选自-C(-O)R 8,-C(-O)NR 8个R 9和-CO 2 R 8;以及-CO 2 R 8。 R 1是氢,C 1-4烷基或取代的C 1-4烷基; R 2是氢或C 1-4烷基; R 3是氢,甲基,全氟甲基,羟基,甲氧基,卤素,氰基,NH 2或NH(CH 3)。 和R 4,R 5,R 6,R 7,R 8, 和R 9是如说明书中所定义的。
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公开(公告)号:US07169771B2
公开(公告)日:2007-01-30
申请号:US10773790
申请日:2004-02-06
申请人: John Hynes , Hong Wu , Katerina Leftheris , Chunjian Liu , Jagabandhu Das , Robert V. Moquin
发明人: John Hynes , Hong Wu , Katerina Leftheris , Chunjian Liu , Jagabandhu Das , Robert V. Moquin
IPC分类号: A61K31/425 , C07D277/20
CPC分类号: C07D277/56 , C07D417/12
摘要: The present invention provides thiazolyl-based compounds of formula (I), useful for treating p38 kinase-associated conditions, wherein ring A is phenyl or pyridyl, and X, Y, B, R2, R3, Z1 m and n 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.
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公开(公告)号:US07323482B2
公开(公告)日:2008-01-29
申请号:US11633337
申请日:2006-12-04
申请人: John Hynes , Hong Wu , Katerina Leftheris , Chunjian Liu , Jagabandhu Das , Robert V. Moquin
发明人: John Hynes , Hong Wu , Katerina Leftheris , Chunjian Liu , Jagabandhu Das , Robert V. Moquin
IPC分类号: A61K31/426 , C07D277/20
CPC分类号: C07D277/56 , C07D417/12
摘要: The present invention provides thiazolyl-based compounds of formula (I), useful for treating p38 kinase-associated conditions, wherein ring A is phenyl or pyridyl, and X, Y, B, R2, R3, Z1 m and n 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)的噻唑基类化合物,其中环A是苯基或吡啶基,X,Y,B,R 2, Z 3,Z 1和Z 3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:US08822510B2
公开(公告)日:2014-09-02
申请号:US13811032
申请日:2011-07-20
IPC分类号: C07D413/10 , C07D413/14 , C07D413/08 , C07D413/06 , C07D271/06 , A61K31/454 , A61K31/4439 , A61K31/4245 , C07D487/10
CPC分类号: C07D413/10 , A61K31/4245 , A61K31/4439 , A61K31/454 , C07D271/06 , C07D413/06 , C07D413/08 , C07D413/14 , C07D487/10
摘要: Disclosed are compounds of Formula (I): (I) or stereoisomers, salts, or prodrugs thereof, wherein: (i) R1 and R2 are independently C1-C4 alkyl, or (ii) R1 and R2 together with the carbon atom to which they are attached, form a cyclic group; and Q is H, C1-6alkyl, phenyl or 5- to 6-membered heteroaryl substituted with zero to 3 substituents, and G is defined herein. Also disclosed are method of using such compounds as selective agonists for G protein-coupled receptor S1P1, and pharmaceutical compositions comprising such compounds. There compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and chronic inflammatory disease.
摘要翻译: 公开了式(I)的化合物:(I)或其立体异构体,盐或前药,其中:(i)R 1和R 2独立地为C 1 -C 4烷基,或(ii)R 1和R 2与其中 它们相连,形成一个环状基团; 并且Q是H,C 1-6烷基,苯基或被0至3个取代基取代的5至6元杂芳基,并且G在本文中定义。 还公开了使用这些化合物作为G蛋白偶联受体S1P1的选择性激动剂的方法,以及包含这些化合物的药物组合物。 其中化合物可用于治疗,预防或减缓各种治疗领域(例如自身免疫性疾病和慢性炎症性疾病)中的疾病或病症的进展。
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公开(公告)号:US20130158001A1
公开(公告)日:2013-06-20
申请号:US13811032
申请日:2011-07-20
IPC分类号: C07D413/10 , C07D413/08 , C07D413/06 , C07D487/10 , C07D271/06 , C07D413/14
CPC分类号: C07D413/10 , A61K31/4245 , A61K31/4439 , A61K31/454 , C07D271/06 , C07D413/06 , C07D413/08 , C07D413/14 , C07D487/10
摘要: Disclosed are compounds of Formula (I): (I) or stereoisomers, salts, or prodrugs thereof, wherein: (i) R1 and R2 are independently C1-C4 alkyl, or (ii) R1 and R2 together with the carbon atom to which they are attached, form a cyclic group; and Q is H, C1-6alkyl, phenyl or 5- to 6-membered heteroaryl substituted with zero to 3 substituents, and G is defined herein. Also disclosed are method of using such compounds as selective agonists for G protein-coupled receptor S1P1, and pharmaceutical compositions comprising such compounds. There compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and chronic inflammatory disease.
摘要翻译: 公开了式(I)的化合物:(I)或其立体异构体,盐或前药,其中:(i)R 1和R 2独立地为C 1 -C 4烷基,或(ii)R 1和R 2与其中 它们相连,形成一个环状基团; 并且Q是H,C 1-6烷基,苯基或被0至3个取代基取代的5至6元杂芳基,并且G在本文中定义。 还公开了使用这些化合物作为G蛋白偶联受体S1P1的选择性激动剂的方法,以及包含这些化合物的药物组合物。 其中化合物可用于治疗,预防或减缓各种治疗领域(例如自身免疫性疾病和慢性炎症性疾病)中的疾病或病症的进展。
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