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公开(公告)号：US20050261333A1
公开(公告)日：2005-11-24
申请号：US10524204
申请日：2003-08-13
IPC分类号： A61K31/437 , A61P11/06 , A61P37/08 , C07D471/04 , A61K31/4745 , C07D471/02
CPC分类号： C07D471/04 , A61K31/437
摘要： The use of compounds of formula (I) wherein R1, R3, R10, m and Ar are as defined in the Specification and pharmaceutically acceptable salts thereof in the manufacture of a medicament for the treatment or prophylaxis of diseases or conditions in which inhibition of kinase Itk activity is beneficial is disclosed. Certain novel compounds of formula (I), together with processes for their preparation, compositions containing them and their use in therapy are also disclosed.
摘要翻译： 使用其中R 1，R 3，R 10，m和Ar的式（I）化合物如本说明书和 其药学上可接受的盐在制备用于治疗或预防其中抑制激酶Itk活性有益的疾病或病症的药物中的用途。 还公开了某些新的式（I）化合物及其制备方法，含有它们的组合物及其在治疗中的用途。
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公开(公告)号：US07410966B2
公开(公告)日：2008-08-12
申请号：US10524204
申请日：2003-08-13
IPC分类号： C07D413/00 , C07D471/02 , C07D491/02 , C07D498/02 , A61K31/535 , A61K31/44 , A01N43/42
CPC分类号： C07D471/04 , A61K31/437
摘要： The use of compounds of formula (I) wherein R1, R3, R10, m and Ar are as defined in the Specification and pharmaceutically acceptable salts thereof in the manufacture of a medicament for the treatment or prophylaxis of diseases or conditions in which inhibition of kinase Itk activity is beneficial is disclosed. Certain novel compounds of formula (I), together with processes for their preparation, compositions containing them and their use in therapy are also disclosed
摘要翻译： 使用其中R 1，R 3，R 10，m和Ar的式（I）化合物如本说明书和 其药学上可接受的盐在制备用于治疗或预防其中抑制激酶Itk活性有益的疾病或病症的药物中的用途。 还公开了某些新的式（I）化合物及其制备方法，含有它们的组合物及其在治疗中的用途
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公开(公告)号：US20060035938A1
公开(公告)日：2006-02-16
申请号：US10534720
申请日：2003-11-11
申请人： Hakan Bladh , Tomas Klingstedt , Joakim Larsson , Karolina Lawitz , Matti Lepisto , Hans Lonn , Grigorios Nikitidis
发明人： Hakan Bladh , Tomas Klingstedt , Joakim Larsson , Karolina Lawitz , Matti Lepisto , Hans Lonn , Grigorios Nikitidis
IPC分类号： C07D211/72 , A61K31/4412
CPC分类号： C07D213/64 , C07D213/82 , C07D239/557 , C07D241/24 , C07D413/12
摘要： There are provided novel compounds of formula (I) wherein R1?, R4?. R5?, G1?, G2?, X, L, Y1?, Y2? and n are as defined in the Specification and optical isomers, racemates and tautomers thereof, and pharmaceutically acceptable salts thereof; together with processes for their preparation, compositions containing them and their use in therapy. The compounds are inhibitors or neutrophil elastase.
摘要翻译： 提供新的式（I）化合物，其中R
1？R
4？ 文件=“US20060035938A1-20060216-P00900.TIF”alt =“custom character”img-content =“character”img-id =“custom-character-00003”he =“2.46mm” 格式=“tif”/> 5 ?, G
1？G
2 ?, X，L，Y
1 ?, Y
2？ 和n如本说明书和光学异构体，外消旋体和互变异构体及其药学上可接受的盐所定义; 以及其制备方法，含有它们的组合物及其在治疗中的用途。 化合物是抑制剂或嗜中性粒细胞弹性蛋白酶。
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4.发明申请Pyridopyrimidine Derivatives as Pde4 Inhibitors for the Treatment of Inflammatory and Immune Diseases 审中-公开吡啶并嘧啶衍生物作为Pde4抑制剂治疗炎症和免疫疾病公开(公告)号：US20080227797A1
公开(公告)日：2008-09-18
申请号：US11994572
申请日：2006-07-03
申请人： Annea Lisius , Grigorios Nikitidis , Peter Sjo
发明人： Annea Lisius , Grigorios Nikitidis , Peter Sjo
IPC分类号： C07D487/04 , A61K31/519 , A61P37/00
CPC分类号： C07D471/04
摘要： The present invention provides a compound of a formula (I): [Chemical formula should be inserted here. Please see paper copy] wherein the variables are defined herein; to a process for preparing such a compound; and to the use of such a compound in the treatment of a PDE4 mediated disease state.
摘要翻译： 本发明提供式（I）的化合物：[化学式应该在此插入。 请参见纸质文件]其中变量在本文中定义; 涉及制备这种化合物的方法; 以及使用这种化合物治疗PDE4介导的疾病状态。
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公开(公告)号：US20080132502A1
公开(公告)日：2008-06-05
申请号：US11667064
申请日：2005-11-07
申请人： Malena Bengtsson , Joakim Larsson , Grigorios Nikitidis , Peter Storm , John Peter Bailey , Edward Jolyon Griffen , Jean-Claude Arnould , Thomas Geoffrey Colerick Bird
发明人： Malena Bengtsson , Joakim Larsson , Grigorios Nikitidis , Peter Storm , John Peter Bailey , Edward Jolyon Griffen , Jean-Claude Arnould , Thomas Geoffrey Colerick Bird
IPC分类号： A61K31/4439 , C07D417/04 , A61K31/506 , A61P35/00 , A61K31/5377 , C07D413/04
CPC分类号： C07D417/04 , C07D417/14
摘要： The invention provides thiazole derivatives of formula (I), or pharmaceutically acceptable salts thereof in which Ring A, R1, R2 and R3 are as defined in the specification; a processes for their preparation; pharmaceutical compositions containing them; and their use in therapy, for example in the treatment of disease mediated by a PI3K enzyme and/or a mTOR kinase.
摘要翻译： 本发明提供式（I）的噻唑衍生物或其药学上可接受的盐，其中环A，R 1，R 2和R 3， 如规范中所定义; 其准备过程; 含有它们的药物组合物; 以及它们在治疗中的用途，例如用于治疗由PI3K酶和/或mTOR激酶介导的疾病。
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公开(公告)号：US07868188B2
公开(公告)日：2011-01-11
申请号：US11667064
申请日：2005-11-07
申请人： Malena Bengtsson , Joakim Larsson , Grigorios Nikitidis , Peter Storm , John Peter Bailey , Edward Jolyon Griffen , Jean-Claude Arnould , Thomas Geoffrey Colerick Bird
发明人： Malena Bengtsson , Joakim Larsson , Grigorios Nikitidis , Peter Storm , John Peter Bailey , Edward Jolyon Griffen , Jean-Claude Arnould , Thomas Geoffrey Colerick Bird
IPC分类号： C07D207/00
CPC分类号： C07D417/04 , C07D417/14
摘要： The invention provides thiazole derivatives of formula (I), or pharmaceutically acceptable salts thereof in which Ring A, R1, R2 and R3 are as defined in the specification; a processes for their preparation; pharmaceutical compositions containing them; and their use in therapy, for example in the treatment of disease mediated by a PI3K enzyme and/or a mTOR kinase.
摘要翻译： 本发明提供式（I）的噻唑衍生物或其药学上可接受的盐，其中环A，R 1，R 2和R 3如说明书中所定义; 其准备过程; 含有它们的药物组合物; 以及它们在治疗中的用途，例如用于治疗由PI3K酶和/或mTOR激酶介导的疾病。
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公开(公告)号：US20090233907A1
公开(公告)日：2009-09-17
申请号：US12293480
申请日：2007-03-20
申请人： Rupert Austin , Roger Victor Bonnert , Simon Fraser Hunt , Grigorios Nikitidis , Hitesh Jayantilal Sanganee , Peter Olof Sjo , Dan Warner
发明人： Rupert Austin , Roger Victor Bonnert , Simon Fraser Hunt , Grigorios Nikitidis , Hitesh Jayantilal Sanganee , Peter Olof Sjo , Dan Warner
IPC分类号： A61K31/551 , A61K31/535 , A61K31/5377 , A61K31/519 , C07D243/00 , C07D413/14 , C07D471/04 , C07D487/00
CPC分类号： C07D471/04 , C07D519/00
摘要： The present invention provides a compound of a formula (I): wherein the variables are defined herein; to a process for preparing such a compound; and to the use of such a compound in the treatment of a PDE 4 mediated disease state.
摘要翻译： 本发明提供式（I）的化合物：其中变量在本文中定义; 涉及制备这种化合物的方法; 以及使用这种化合物治疗PDE4介导的疾病状态。
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8.发明授权Tetrahydroquinoline derivatives as stat6-modulators, preparation and use thereof 失效四氢喹啉衍生物作为stat6-调节剂，其制备和用途公开(公告)号：US07030246B2
公开(公告)日：2006-04-18
申请号：US10473056
申请日：2002-03-26
申请人： Håkan Bladh , Thomas Hansson , Grigorios Nikitidis , Carita Nordén , Lars Pettersson , Mikael Varga
发明人： Håkan Bladh , Thomas Hansson , Grigorios Nikitidis , Carita Nordén , Lars Pettersson , Mikael Varga
IPC分类号： C07D215/16 , C07D215/20 , A61K31/47
CPC分类号： C07D401/12 , A61K31/47 , C07D215/06 , C07D215/36 , C07D215/44 , C07D405/12
摘要： Compounds of formula (I) are modulators of STAT6 signal pathway activity, and can be used in the treatment of atopic dermatitis, urticaria, allergic asthma, allergic rhinitis, a food allergy, allergic conjunctivitis, hayfever, bullous pemphigoid, industrial sensitization, chronic rejection of transplants or COPD
摘要翻译： 式（I）化合物是STAT6信号通路活性的调节剂，可用于治疗特应性皮炎，荨麻疹，过敏性哮喘，过敏性鼻炎，食物过敏，过敏性结膜炎，高粱，大疱性类天疱疮，工业致敏，慢性排斥 的移植物或COPD
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