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公开(公告)号：US08569298B2
公开(公告)日：2013-10-29
申请号：US12999025
申请日：2009-06-15
IPC分类号： C07D217/24 , C07D401/12 , A61K31/4709
CPC分类号： C07D401/12 , C07D401/14 , C07D405/14 , C07D413/14
摘要： The present invention relates to compounds that inhibit of focal adhesion kinase function, processes for their preparation, pharmaceutical compositions containing them as the active ingredient, to their use as medicaments and to their use in the manufacture of medicaments for use in the treatment in warm-blooded animals such as humans of diseases such as cancer.
摘要翻译： 本发明涉及抑制粘着斑激酶功能的化合物，其制备方法，含有它们作为活性成分的药物组合物，作为药物的用途，以及它们在制备用于温热治疗的药物中的用途， 血液动物如人类的疾病如癌症。
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公开(公告)号：US20110166139A1
公开(公告)日：2011-07-07
申请号：US12999025
申请日：2009-06-15
IPC分类号： A61K31/5377 , C07D401/12 , C07D217/24 , C07D409/14 , C07D401/14 , C07D413/14 , A61K31/4439 , A61K31/4709 , A61K31/497 , A61K31/4545 , A61P35/00 , A61P35/02
CPC分类号： C07D401/12 , C07D401/14 , C07D405/14 , C07D413/14
摘要： The present invention relates to compounds that inhibit of focal adhesion kinase function, processes for their preparation, pharmaceutical compositions containing them as the active ingredient, to their use as medicaments and to their use in the manufacture of medicaments for use in the treatment in warm-blooded animals such as humans of diseases such as cancer.
摘要翻译： 本发明涉及抑制粘着斑激酶功能的化合物，其制备方法，含有它们作为活性成分的药物组合物，作为药物的用途，以及它们在制备用于温热治疗的药物中的用途， 血液动物如人类的疾病如癌症。
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公开(公告)号：US08530470B2
公开(公告)日：2013-09-10
申请号：US13444221
申请日：2012-04-11
申请人： Bernard Christophe Barlaam , Sebastien Louis Degorce , Christine Marie Paul Lambert-Van Der Brempt , Jean-Jacques Marcel Lohmann , Patrick Ple
发明人： Bernard Christophe Barlaam , Sebastien Louis Degorce , Christine Marie Paul Lambert-Van Der Brempt , Jean-Jacques Marcel Lohmann , Patrick Ple
IPC分类号： A61K31/535 , C07D413/14
CPC分类号： C07D413/14 , A61K31/5377 , A61K31/715 , C07D417/14
摘要： The invention concerns chromenone compounds of Formula I; or pharmaceutically-acceptable salts thereof, wherein each of R1, R2, R3, R4, R5, n and R6 has any of the meanings defined hereinbefore in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use in the treatment of cell proliferative disorders.
摘要翻译： 本发明涉及式I的色烯酮化合物; 或其药学上可接受的盐，其中R 1，R 2，R 3，R 4，R 5，n和R 6中的每一个在本说明书中具有上文定义的任何含义; 其制备方法，含有它们的药物组合物及其在制备用于治疗细胞增殖性疾病的药物中的用途。
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4.发明申请4-ANILINO-SUBSTITUTED QUINAZOLINE DERIVATIVES AS TYROSINE KINASE INHIBITORS 审中-公开作为酪氨酸激酶抑制剂的4-苯胺替代喹啉酮衍生物公开(公告)号：US20100222344A1
公开(公告)日：2010-09-02
申请号：US12095665
申请日：2006-11-29
IPC分类号： A61K31/5377 , C07D413/14 , C07D413/02 , C07D239/94 , A61K31/517 , A61P35/00
CPC分类号： C07D239/94 , C07D405/12
摘要： A quinazoline derivative of the Formula (I): wherein the substituents are as defined in the text for use in the production of an anti-proliferative effect which effect is produced alone or in part by inhibiting erbB2 receptor tyrosine kinase in a warm-blooded animal such as man.
摘要翻译： 式（I）的喹唑啉衍生物：其中取代基如用于产生抗增殖作用的文本中所定义，其作用单独或部分通过在温血动物中抑制erbB2受体酪氨酸激酶产生 如男人。
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公开(公告)号：US20080242663A1
公开(公告)日：2008-10-02
申请号：US12039030
申请日：2008-02-28
申请人： Susan Elizabeth Ashton , Darren Anthony Edward Cross , Simon John East , Jason Grant Kettle , Mark Andrew Pearson , Stephen Robert Wedge , Bernard Christophe Barlaam , Richard Ducray , Stuart Charles Purkiss
发明人： Susan Elizabeth Ashton , Darren Anthony Edward Cross , Simon John East , Jason Grant Kettle , Mark Andrew Pearson , Stephen Robert Wedge , Bernard Christophe Barlaam , Richard Ducray , Stuart Charles Purkiss
IPC分类号： A61K31/5377 , C07D413/14 , A61P35/04
CPC分类号： C07D239/48 , C07D401/12 , C07D403/12 , C07D405/12 , C07D413/12
摘要： The invention concerns compounds of Formula I, or a pharmaceutically acceptable salt thereof, where R1, n, R2, R3, and R4 are as defined in the description. The present invention also relates to processes for the preparation of such compounds, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use as an antiproliferative agent in the prevention or treatment of tumours or other proliferative conditions which are sensitive to the inhibition of EphB4 kinases.
摘要翻译： 本发明涉及式I化合物或其药学上可接受的盐，其中R 1，R 2，R 3，R 3和R 3， 4 如说明书中所定义的。 本发明还涉及制备这些化合物的方法，含有它们的药物组合物及其在制备用于预防或治疗对抑制敏感的肿瘤或其它增殖性病症中的抗增殖剂的药物中的用途 的EphB4激酶。
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公开(公告)号：US20120329795A1
公开(公告)日：2012-12-27
申请号：US13607999
申请日：2012-09-10
IPC分类号： A61K31/517 , A61P35/00 , A61K31/5377
CPC分类号： C04B35/632 , C07D401/12
摘要： The invention concerns quinazoline derivatives of Formula I: wherein each of R1, X1, R2, R3, R5, n and m have any of the meanings defined in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use as an antiproliferative agent in the prevention or treatment of tumours which are sensitive to inhibition of EGF and erbB receptor tyrosine kinases.
摘要翻译： 本发明涉及式I的喹唑啉衍生物：其中R1，X1，R2，R3，R5，n和m各自具有本说明书中定义的任何含义; 其制备方法，含有它们的药物组合物及其在制备用于预防或治疗对EGF和erbB受体酪氨酸激酶的抑制敏感的肿瘤中作为抗增殖剂的药物中的用途。
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公开(公告)号：US20110237610A1
公开(公告)日：2011-09-29
申请号：US12902543
申请日：2010-10-12
IPC分类号： A61K31/517 , C07D409/14 , C07D413/14 , C07D401/12 , C07D401/14 , A61P35/00
CPC分类号： C07D413/14 , C07D401/12 , C07D401/14 , C07D405/14 , C07D409/14
摘要： The invention concerns quinazoline derivatives of Formula I wherein each of R1a, R1b, R2, R3 and a have any of the meanings defined in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use as an antiproliferative agent in the prevention or treatment of tumours which are sensitive to inhibition of erbB receptor tyrosine kinases.
摘要翻译： 本发明涉及式I的喹唑啉衍生物，其中R1a，R1b，R2，R3和a各自具有本说明书中定义的任何含义; 其制备方法，含有它们的药物组合物及其在制备用于预防或治疗对erbB受体酪氨酸激酶抑制敏感的肿瘤中的抗增殖剂的药物中的用途。
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公开(公告)号：US08017611B2
公开(公告)日：2011-09-13
申请号：US12256739
申请日：2008-10-23
申请人： Bernard Christophe Barlaam , Craig Steven Harris , Christine Marie Paul Lambert , Gilles Ouvry , Justin Fairfield Bower , Benedicte Delouvrie , Gary Fairley , Jon James Gordon Winter
发明人： Bernard Christophe Barlaam , Craig Steven Harris , Christine Marie Paul Lambert , Gilles Ouvry , Justin Fairfield Bower , Benedicte Delouvrie , Gary Fairley , Jon James Gordon Winter
IPC分类号： A61K31/497 , C07D413/14
CPC分类号： C07D413/04 , C07D413/14 , C07D417/14 , C07D498/04
摘要： The invention concerns pyridine and pyrazine derivatives of Formula I or a pharmaceutically-acceptable salt thereof, wherein each of W, G1, G2, G3, G4, J, Ring A, n and R3 has any of the meanings defined hereinbefore in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use in the treatment of cell proliferative disorders.
摘要翻译： 本发明涉及式I的吡啶和吡嗪衍生物或其药学上可接受的盐，其中W，G 1，G 2，G 3，G 4，J，环A，n和R 3中的每一个具有上文在描述中定义的任何含义; 其制备方法，含有它们的药物组合物及其在制备用于治疗细胞增殖性疾病的药物中的用途。
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公开(公告)号：US20080096881A1
公开(公告)日：2008-04-24
申请号：US10571991
申请日：2004-09-15
IPC分类号： A61K31/517 , A61K31/496 , A61K31/5377 , A61P35/00 , C07D401/12 , C07D401/14 , C07D413/14
CPC分类号： C04B35/632 , C07D401/12
摘要： The invention concerns quinazoline derivatives of Formula (I): wherein each of R1, X1, R2, R3, R5, n and m have any of the meanings defined in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use as an antiproliferative agent in the prevention or treatment of tumours which are sensitive to inhibition of EGF and erbB receptor tyrosine kinases.
摘要翻译： 本发明涉及式（I）的喹唑啉衍生物：其中R 1，X 1，R 2，R 3， R 5，n和m具有本说明书中定义的任何含义; 其制备方法，含有它们的药物组合物及其在制备用于预防或治疗对EGF和erbB受体酪氨酸激酶的抑制敏感的肿瘤中作为抗增殖剂的药物中的用途。
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公开(公告)号：US06518301B1
公开(公告)日：2003-02-11
申请号：US09959032
申请日：2002-01-07
IPC分类号： A61K3138
CPC分类号： A61K31/37 , A61K31/00 , A61K31/122 , A61K31/352
摘要： A method for treating a disease associated with the estrogen receptor-&bgr;, comprising the step of administering a therapeutically-effective amount of a compound that satisfies the equation: (Ki&agr;A/Ki&bgr;A)/(Ki&agr;E/Ki&bgr;E)>1, optionally having the general structure (I).
摘要翻译： 一种用于治疗与雌激素受体-β相关的疾病的方法，包括施用治疗有效量的满足以下等式的化合物的步骤：（KialphaA / KibetaA）/（KialphaE / KibetaE）> 1，任选地具有一般 结构（I）。
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