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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：US20100292222A1
公开(公告)日：2010-11-18
申请号：US12776970
申请日：2010-05-10
IPC分类号： A61K31/551 , C07D487/04 , A61K31/5025 , C07D243/08 , A61P35/00
CPC分类号： C07D487/04
摘要： The invention concerns bicyclic compounds of Formula (I) wherein, R1, R2, R3, R4, R5, X1, X2, Y, k, m, n and p 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 treatment of androgen-receptor associated conditions, particularly prostate cancer.
摘要翻译： 本发明涉及式（I）的双环化合物，其中R1，R2，R3，R4，R5，X1，X2，Y，k，m，n和p如说明书中所定义。 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治疗雄激素受体相关病症，特别是前列腺癌中的用途。
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公开(公告)号：US20100267699A1
公开(公告)日：2010-10-21
申请号：US12702603
申请日：2010-02-09
申请人： Robert Hugh Bradbury , Gregory Richard Carr , Alfred Arthur Rabow , Srinivasa Rao Korupoju , Harikrishna Tumma
发明人： Robert Hugh Bradbury , Gregory Richard Carr , Alfred Arthur Rabow , Srinivasa Rao Korupoju , Harikrishna Tumma
IPC分类号： A61K31/551 , C07D487/04 , A61K31/5025 , C07D243/08 , A61P35/00
CPC分类号： A61K31/5025 , A61K31/551 , A61K31/58 , C07D471/04 , C07D487/04
摘要： The invention concerns bicyclic compounds of Formula I wherein , R1, R2, L1, L2, J, Y, k, n, p and r 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 treatment of androgen-receptor associated conditions, particularly prostate cancer.
摘要翻译： 本发明涉及式I的双环化合物，其中R1，R2，L1，L2，J，Y，k，n，p和r如说明书中所定义。 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治疗雄激素受体相关病症，特别是前列腺癌中的用途。
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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：US20100029696A1
公开(公告)日：2010-02-04
申请号：US11817391
申请日：2006-02-28
申请人： Robert Hugh Bradbury
发明人： Robert Hugh Bradbury
IPC分类号： A61K31/517 , C07D401/14 , A61P35/00
CPC分类号： C07D401/14 , C07D417/14
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例如人中抑制erbB2受体酪氨酸激酶产生 。
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6.发明申请公开(公告)号：US20090029968A1
公开(公告)日：2009-01-29
申请号：US12095659
申请日：2006-11-29
IPC分类号： A61K31/517 , C07D455/02 , A61P35/00 , A61K31/55
CPC分类号： C07D239/94
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，例如 人。
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7.发明授权2,4-Di(hetero-)arylamino(-oxy)-5-substituted pyrimidines as antineaoplastic agents 有权2,4-二（异）芳基氨基（ - 氧基）-5-取代的嘧啶作为抗肿瘤剂公开(公告)号：US06838464B2
公开(公告)日：2005-01-04
申请号：US10203025
申请日：2001-02-26
IPC分类号： A61K31/505 , A61K31/506 , A61K31/5377 , A61P35/00 , A61P43/00 , C07D239/48 , C07D401/12 , C07D403/12 , C07D413/12 , C07D453/02 , C07D521/00 , C07D403/04
CPC分类号： C07D239/48 , C04B35/632 , C07D231/12 , C07D233/56 , C07D249/08 , C07D401/12 , C07D403/12
摘要： Pyrimidine derivatives of formula (I) wherein Q1, Q2, G and R1 are as defined within; and pharmaceutically acceptable salts and in vivo hydrolysable esters thereof are described. Processes for their manufacture, pharmaceutical compositions and their use as cyclin-dependent serine/threonine kinase (CDK) and focal adhesion kinase (FAK) inhibitors are also described.
摘要翻译： 其中Q 1，Q 2，G和R 1如在其中所定义的式（I）的嘧啶衍生物; 和其药学上可接受的盐和体内可水解的酯。 还描述了其制备方法，药物组合物及其作为细胞周期蛋白依赖性丝氨酸/苏氨酸激酶（CDK）和粘着斑激酶（FAK）抑制剂的用途。
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公开(公告)号：US20130203714A1
公开(公告)日：2013-08-08
申请号：US13564029
申请日：2012-08-01
申请人： Robert Hugh Bradbury , Gregory Richard Carr , Alfred Arthur Rabow , Srinivasa Rao Korupoju , Harikrishna Tumma
发明人： Robert Hugh Bradbury , Gregory Richard Carr , Alfred Arthur Rabow , Srinivasa Rao Korupoju , Harikrishna Tumma
IPC分类号： A61K31/5025 , A61K31/58 , A61K31/551 , C07D487/04 , C07D471/04
CPC分类号： A61K31/5025 , A61K31/551 , A61K31/58 , C07D471/04 , C07D487/04
摘要： The invention concerns bicyclic compounds of Formula I wherein R1, R2, L1, L2, J, Y, k, n, p and r 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 treatment of androgen-receptor associated conditions, particularly prostate cancer.
摘要翻译： 本发明涉及式I的双环化合物，其中R 1，R 2，L 1，L 2，J，Y，k，n，p和r如说明书中所定义。 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治疗雄激素受体相关病症，特别是前列腺癌中的用途。
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公开(公告)号：US08399667B2
公开(公告)日：2013-03-19
申请号：US12706675
申请日：2010-02-16
IPC分类号： C07D239/72
CPC分类号： C07D401/12 , C07D403/12
摘要： The invention concerns quinazoline derivatives of Formula (I) wherein each of Q1, Z, R1 and Q2 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Q1，Z，R1和Q2各自具有在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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10.发明授权Bicyclic derivatives for use in the treatment of androgen receptor associated conditions-155 失效用于治疗雄激素受体相关病症的双环衍生物155公开(公告)号：US08003649B2
公开(公告)日：2011-08-23
申请号：US12338405
申请日：2008-12-18
IPC分类号： A61N31/50 , A61K31/501 , A61K31/41 , A01N43/64 , C07D487/00 , C07D249/00
CPC分类号： C07D487/04 , C07D471/04 , C07D519/00
摘要： The invention concerns bicyclic compounds of Formula I wherein the integers X1, X2, X3, Ring A, R4, R5 and m 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 in the prevention or treatment of androgen-receptor associated conditions.
摘要翻译： 本发明涉及式I的双环化合物，其中整数X1，X2，X3，环A，R4，R5和m如说明书中所定义。 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雄激素受体相关病症的药物中的用途。
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