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11.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：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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公开(公告)号：US07625908B2
公开(公告)日：2009-12-01
申请号：US10578663
申请日：2004-11-11
IPC分类号： A61K31/517 , A61P35/02 , C07D239/84 , A61K31/4965
CPC分类号： C07D401/14 , C04B35/632 , C07D239/94 , C07D401/12 , C07D403/12 , C07D405/14 , C07D409/12 , C07D413/12 , C07D417/12
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受体酪氨酸激酶而产生， 作为人
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公开(公告)号：US20080269487A1
公开(公告)日：2008-10-30
申请号：US12147250
申请日：2008-06-26
IPC分类号： C07D401/02
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Q 1，Z，R 1和Q 2 2中的每一个具有定义的任何含义 在说明中; 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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15.发明授权2,4,DI (hetero-) arylamino (-oxy)-5-substituted pyrimidines as antineoplastic agents 有权2,4，DI（杂）芳基氨基（ - 氧基）-5-取代的嘧啶作为抗肿瘤剂公开(公告)号：US07067522B2
公开(公告)日：2006-06-27
申请号：US10995931
申请日：2004-11-24
IPC分类号： C07D239/48 , C07D403/04 , C07D401/12 , A61K31/506 , A61K35/00
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的式（I）的嘧啶衍生物如本文所定义; 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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16.发明授权Substituted pyrazin-2-yl-sulphonamide-(3-pyridyl) compounds and uses thereof 有权取代的吡嗪-2-基 - 磺酰胺 - （3-吡啶基）化合物及其用途
公开(公告)号：US6060475A
公开(公告)日：2000-05-09
申请号：US211483
申请日：1998-12-14
IPC分类号： A61K31/495 , A61K31/497 , A61K31/505 , A61K31/506 , A61K31/535 , A61K31/5377 , A61P1/00 , A61P3/00 , A61P9/00 , A61P9/10 , A61P9/12 , A61P11/00 , A61P13/02 , A61P15/00 , A61P19/00 , A61P35/00 , A61P43/00 , C07D401/12 , C07D401/14 , C07D405/14 , C07D413/14 , C07D417/14 , A01N43/60 , A61K31/445 , C07D241/04 , C07D401/00 , C07D413/00
CPC分类号： C07D401/12 , C07D401/14 , C07D413/14
摘要： The invention concerns pharmaceutically useful compounds of the formula I, in which A.sup.1, A.sup.2, A.sup.3, A.sup.4, B.sup.1, m, Ar, W, X, Y, Z and R.sup.1 have any of the meanings defined herein, and their pharmaceutically acceptable salts, and pharmaceutical compositions containing them. The novel compounds possess endothelin receptor antagonist activity and are useful, for example, in the treatment of diseases or medical conditions in which elevated or abnormal levels of endothelin play a significant causative role. The invention further concerns processes for the manufacture of the novel compounds and the use of the compounds in medical treatment.
摘要翻译： 本发明涉及药学上有用的式I化合物，其中A1，A2，A3，A4，B1，m，Ar，W，X，Y，Z和R1具有本文定义的任何含义及其药学上可接受的盐， 和含有它们的药物组合物。 新型化合物具有内皮素受体拮抗剂活性，并且可用于例如治疗疾病或医学病症，其中升高或异常水平的内皮素起重要作用。 本发明还涉及制备新化合物的方法和该化合物在医疗中的用途。
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17.发明授权4-(1H-indazol-5-yl-amino)-quinazoline compounds as erbB receptor tyrosine kinase inhibitors for the treatment of cancer 失效4-（1H-吲唑-5-基氨基） - 喹唑啉化合物作为治疗癌症的erbB受体酪氨酸激酶抑制剂公开(公告)号：US07820683B2
公开(公告)日：2010-10-26
申请号：US12067416
申请日：2006-09-14
IPC分类号： A61K31/517
CPC分类号： C07D403/12 , 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中抑制erbB2受体酪氨酸激酶产生，例如 人。
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公开(公告)号：US20090137615A1
公开(公告)日：2009-05-28
申请号：US11817393
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 , C07D403/14
CPC分类号： C07D417/14 , C07D401/14 , C07D403/14
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中抑制erbB2受体酪氨酸激酶产生 如男人。
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19.发明申请Quinazoline Derivatives as Inhibitors of EGF and/or erbB2 Receptor Tyrosine Kinase 审中-公开喹唑啉衍生物作为EGF和/或erbB2受体酪氨酸激酶的抑制剂公开(公告)号：US20090023759A1
公开(公告)日：2009-01-22
申请号：US11912794
申请日：2006-04-27
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
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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20.发明授权2,4-di(hetero-)arylamino (oxy)-5-substituted pyrimidines as antineoplastic agents 失效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：US06649608B2
公开(公告)日：2003-11-18
申请号：US10203154
申请日：2002-08-06
申请人： Elizabeth Janet Pease , Gloria Anne Breault , Emma Jane Williams , Robert Hugh Bradbury , Jeffrey James Morris
发明人： Elizabeth Janet Pease , Gloria Anne Breault , Emma Jane Williams , Robert Hugh Bradbury , Jeffrey James Morris
IPC分类号： C07D23948
CPC分类号： C07D239/47 , C07D231/12 , C07D233/56 , C07D239/48 , C07D249/08 , C07D401/12 , C07D401/14 , C07D403/12 , C07D409/12 , C07D471/04
摘要： Pyrimidine derivatives of the formula (I), wherein: Q1 and Q2 are independently selected from aryl or carbon linked heteroaryl optionally substituted as defined within; and one or both Q1 and Q2 are substituted on a ring carbon by one substituent of the formula (Ia) or (Ia′), wherein: Y, Z, n, m Q3, G, R1, are as defined within; and pharmaceutically acceptable salts and in 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： 式（I）的嘧啶衍生物，其中：Q 1和Q 2独立地选自如上定义的任选取代的芳基或碳连接的杂芳基; 并且Q1和Q2中的一个或两个在环碳上由式（Ia）或（Ia'）的一个取代基取代，其中：Y，Z，n，m Q3，G，R 1如 ; 和其药学上可接受的盐及其体内可水解的酯。 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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