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1. 发明授权

US07067522B2 2,4,DI (hetero-) arylamino (-oxy)-5-substituted pyrimidines as antineoplastic agents 有权
标题翻译： 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
申请人： Elizabeth Janet Pease , Emma Jane Williams , Robert Hugh Bradbury , Stuart Eric Pearson
发明人： Elizabeth Janet Pease , Emma Jane Williams , Robert Hugh Bradbury , Stuart Eric Pearson
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。

2. 发明授权

US06838464B2 2,4-Di(hetero-)arylamino(-oxy)-5-substituted pyrimidines as antineaoplastic agents 有权
标题翻译： 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
申请人： Elizabeth Janet Pease , Emma Jane Williams , Robert Hugh Bradbury , Stuart Eric Pearson
发明人： Elizabeth Janet Pease , Emma Jane Williams , Robert Hugh Bradbury , Stuart Eric Pearson
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。

3. 发明授权

US06649608B2 2,4-di(hetero-)arylamino (oxy)-5-substituted pyrimidines as antineoplastic agents 失效
标题翻译： 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。

4. 发明授权

US06710052B2 Pyrimidine compounds 失效
标题翻译：嘧啶化合物
公开(公告)号：US06710052B2
公开(公告)日：2004-03-23
申请号：US10203549
申请日：2002-08-08
申请人： Elizabeth Janet Pease , Gloria Anne Breault , Robert Hugh Bradbury
发明人： Elizabeth Janet Pease , Gloria Anne Breault , Robert Hugh Bradbury
IPC分类号： C07D23948
CPC分类号： C07D239/47 , C07D417/12
摘要： Pyrimidine derivatives of the formula (I) wherein: one of Q1 and Q2 or both of Q1 and Q2 is substituted on a ring carbon by one substituent of the formula (Ia) [provided that when present in Q1 the substituent of formula (Ia) is not adjacent to the —NH— link]; wherein Q1, Q2, G, R1, X, Y1, Y2, Z, n and m are as described within; and pharmaceutically acceptable salts and in vivo hydrolyzable 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：Q1和Q2中的一个或Q1和Q2两者在环碳上被式（Ia）的一个取代基取代[条件是当在Q1中存在式（Ia）的取代基时，不与-NH-链接相邻]; 其中Q 1，Q 2，G，R 1，X，Y 1，Y 2，Z，n和m如上所述; 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。

5. 发明授权

US07153964B2 Pyrimidine compounds 有权
标题翻译：嘧啶化合物
公开(公告)号：US07153964B2
公开(公告)日：2006-12-26
申请号：US10220139
申请日：2001-02-26
申请人： Elizabeth Janet Pease , Gloria Anne Breault , Jeffrey James Morris
发明人： Elizabeth Janet Pease , Gloria Anne Breault , Jeffrey James Morris
IPC分类号： C07D239/47 , C07D239/48 , C07D471/04 , C07D471/14 , A61K31/437 , A61P35/00
CPC分类号： C07D239/47 , C07D239/48 , C07D401/12 , C07D413/12 , C07D417/12
摘要： Pyrimidine derivatives of formula (I) wherein: Qh1 and Q2 are independently selected from aryl or carbon linked heteroaryl optionally substituted as defined within; and one of Q1 and Q2 or both Q1 and Q2 is substituted on a ring carbon by one group selected from sulphamoyl, N—(C1-4alkyl)sulphamoyl (optionally substituted by halo or hydroxy), N,N-di-(C1-4alkyl)sulphamoyl (optionally substituted by halo or hydroxy), C1-4alkylsulphonyl (optionally substituted by halo or hydroxy) or a substituent of the formula (Ia) or (Ia′): wherein Q1, Q2, G, R1, Y, Z, Q3, n and m 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) inhibitors are also described
摘要翻译：式（I）的嘧啶衍生物其中：Q 1'和Q 2个独立地选自如上所定义的任选取代的芳基或碳连接的杂芳基; 且Q 1和Q 2中的一个或Q 1和Q 2 2中的一个在环碳上被一个选自氨磺酰基，N-（C 1-4烷基）氨磺酰基（任选被卤素或羟基取代）的基团，N，N-二 - （C 1-4 - 烷基）氨磺酰基（任选被卤素或羟基取代），C 1-4烷基磺酰基（任选被卤素或羟基取代）或式（Ia）或（Ia'）的取代基：其中Q < Q 1，Q 2，G，R 1，Y，Z，Q 3，n和m如上定义中; 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）抑制剂的用途

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