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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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公开(公告)号:US20060167247A1
公开(公告)日:2006-07-27
申请号:US11295638
申请日:2005-12-07
申请人: Enrique Michelotti , Eric Springman , Duyan Nguyen , Rupa Shetty , Younghee Lee , Kristofer Moffett , Jennifer Ludington , Ted Fujimoto , Zenon Konteatis , Bin Liu , Frank Hollinger , Bruce Dorsey
发明人: Enrique Michelotti , Eric Springman , Duyan Nguyen , Rupa Shetty , Younghee Lee , Kristofer Moffett , Jennifer Ludington , Ted Fujimoto , Zenon Konteatis , Bin Liu , Frank Hollinger , Bruce Dorsey
IPC分类号: C07D417/02 , C07D413/02 , C07D409/02
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R 1,R 2,G和Q在本文中定义。 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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公开(公告)号:US20100041642A1
公开(公告)日:2010-02-18
申请号:US12541922
申请日:2009-08-15
IPC分类号: A61K31/496 , C07D409/14 , C07D413/14 , A61K31/5377 , A61K31/551 , A61P43/00
CPC分类号: C07D417/14 , C07D401/12 , C07D405/14 , C07D409/06 , C07D409/12 , C07D409/14 , C07D413/14 , C07D495/04
摘要: Urea containing compounds that inhibit MAP kinases, pharmaceutical compositions including such compounds and methods for using these compounds to treat inflammatory diseases and cancer are described herein.
摘要翻译: 本文描述了抑制MAP激酶的含尿素化合物,包含这些化合物的药物组合物和使用这些化合物治疗炎性疾病和癌症的方法。
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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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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:US20080280891A1
公开(公告)日:2008-11-13
申请号:US11819494
申请日:2007-06-27
申请人: Martha Kelly , Younghee Lee , Bin Liu , Ted Fujimoto , Joel Freundlich , Bruce D. Dorsey , Gary A. Flynn , Arifa Husain , William R. Moore, Jr.
发明人: Martha Kelly , Younghee Lee , Bin Liu , Ted Fujimoto , Joel Freundlich , Bruce D. Dorsey , Gary A. Flynn , Arifa Husain , William R. Moore, Jr.
IPC分类号: A61K31/541 , A61K31/404 , C07D209/42 , C07D401/02 , C07D417/14 , A61K31/44 , A61P35/00 , A61K31/4439 , A61K31/5377 , C07D413/14
CPC分类号: A61K31/404 , A61K31/44 , A61K31/4439 , A61K31/5377 , A61K31/541 , C07D213/74 , C07D231/56 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D409/10 , C07D413/12 , C07D498/04
摘要: The present invention is in the area of novel compounds and salts thereof, their syntheses, and their use as anti-cancer agents. The compounds include compounds of Formula I: and solvates, hydrates and pharmaceutically-acceptable salts thereof, wherein A1 is N or CR1; A3 is N or CR3; A5 is N or CR5; R1, R3-R6 and L are defined in the specification; n is 0 or 1; and X is an optionally-substituted aryl group having 6-10 carbons in the ring portion, an optionally-substituted 6-membered heteroaryl group having 1-3 nitrogen atoms in the ring portion, an optionally-substituted 5-membered heteroaryl group having 0-4 nitrogen atoms in the ring portion and optionally having 1 sulfur atom or 1 oxygen atom in the ring portion, or an optionally-substituted heteroaryl group in which a 6-membered ring is fused either to a 5-membered ring or to a 6-membered ring, wherein in each case 1, 2, 3 or 4 ring atoms are heteroatoms independently selected from nitrogen, oxygen and sulfur. They are effective against a broad range of cancers, especially leukemia, prostate, non-small cell lung and colon. They are additionally useful in the treatment of proliferative retinopathies such as diabetic neuropathy and macular degeneration.
摘要翻译: 本发明涉及新型化合物及其盐,其合成及其作为抗癌剂的用途。 化合物包括式I化合物及其溶剂合物,水合物及其药学上可接受的盐,其中A 1是N或CR 1; N 3或N 3是N或CR 3; A <5>为N或CR 5; 在说明书中定义了R 1,R 3,R 6和L 6; n为0或1; 并且X是在环部分中具有6-10个碳的任选取代的芳基,在环部分中具有1-3个氮原子的任选取代的6元杂芳基,任选取代的5元杂芳基具有0 -4个氮原子,并且在环部分中任选具有1个硫原子或1个氧原子,或任选取代的杂芳基,其中6元环稠合到5元环或6元环 其中在每种情况下,1,2,3或4个环原子是独立地选自氮,氧和硫的杂原子。 它们对广泛的癌症尤其是白血病,前列腺,非小细胞肺和结肠有效。 它们还可用于治疗增殖性视网膜病变,例如糖尿病性神经病变和黄斑变性。
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公开(公告)号:US20060270686A1
公开(公告)日:2006-11-30
申请号:US10928401
申请日:2004-08-30
申请人: Martha Kelly , Younghee Lee , Bin Liu , Ted Fujimoto , Joel Freundlich , Bruce Dorsey , Gary Flynn , Arifa Husain
发明人: Martha Kelly , Younghee Lee , Bin Liu , Ted Fujimoto , Joel Freundlich , Bruce Dorsey , Gary Flynn , Arifa Husain
IPC分类号: A61K31/497 , A61K31/44 , C07D403/02
CPC分类号: C07D209/08 , C07D213/74 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/10 , C07D403/12 , C07D405/10 , C07D405/12 , C07D409/12 , C07D409/14 , C07D417/10
摘要: The present invention is in the area of novel compounds and salts thereof, their syntheses, and their use as anti-cancer agents. The compounds include compounds of Formula I: and solvates, hydrates and pharmaceutically-acceptable salts thereof, wherein A1 is N or CR1; A3 is N or CR3; A5 is N or CR5; R1, R3—R6 and L are defined in the specification; n is 0 or 1; and X is an optionally-substituted aryl group having 6-10 carbons in the ring portion, an optionally-substituted 6-membered heteroaryl group having 1-3 nitrogen atoms in the ring portion, an optionally-substituted 5-membered heteroaryl group having 0-4 nitrogen atoms in the ring portion and optionally having 1 sulfur atom or 1 oxygen atom in the ring portion, or an optionally-substituted heteroaryl group in which a 6-membered ring is fused either to a 5-membered ring or to a 6-membered ring, wherein in each case 1, 2, 3 or 4 ring atoms are heteroatoms independently selected from nitrogen, oxygen and sulfur. They are effective against a broad range of cancers, especially leukemia, non-small cell lung and colon.
摘要翻译: 本发明涉及新型化合物及其盐,其合成及其作为抗癌剂的用途。 化合物包括式I化合物及其溶剂合物,水合物及其药学上可接受的盐,其中A 1是N或CR 1; N 3或N 3是N或CR 3; A <5>为N或CR 5; 在说明书中定义了R 1,R 3,R 6和L 6; n为0或1; 并且X是在环部分中具有6-10个碳的任选取代的芳基,在环部分中具有1-3个氮原子的任选取代的6元杂芳基,任选取代的5元杂芳基具有0 -4个氮原子,并且在环部分中任选具有1个硫原子或1个氧原子,或任选取代的杂芳基,其中6元环稠合到5元环或6元环 其中在每种情况下,1,2,3或4个环原子是独立地选自氮,氧和硫的杂原子。 它们对广泛的癌症尤其是白血病,非小细胞肺和结肠有效。
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