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公开(公告)号：US20160250187A1
公开(公告)日：2016-09-01
申请号：US15010831
申请日：2016-01-29
申请人： Astex Therapeutics Ltd , The Institute of Cancer Research: Royal Cancer Hospital , Cancer Research Technology Limited
发明人： Valerio BERDINI , Gordon SAXTY , Marinus Leendert VERDONK , Steven John WOODHEAD , Paul Graham WYATT , Robert George BOYLE , Hannah Fiona SORE , David Winter WALKER , Ian COLLINS , Robert DOWNHAM , Robin Arthur Ellis CARR
IPC分类号： A61K31/415 , A61K31/454 , A61K31/4439 , A61K31/5377 , A61K31/4155 , A61K9/20 , A61K31/4178 , A61K31/497 , A61K31/551 , A61K31/4545 , A61K9/00 , A61K9/48 , A61K45/06 , A61K31/496
CPC分类号： A61K31/415 , A61K9/0019 , A61K9/20 , A61K9/48 , A61K31/4155 , A61K31/4178 , A61K31/4439 , A61K31/454 , A61K31/4545 , A61K31/496 , A61K31/497 , A61K31/5377 , A61K31/551 , A61K45/06 , C07D231/12 , C07D401/04 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/10 , C07D403/12 , C07D405/04 , C07D413/10
摘要： The invention provides compounds of the formula (I) having protein kinase B inhibiting activity: wherein A is a saturated hydrocarbon linker group containing from 1 to 7 carbon atoms, the linker group having a maximum chain length of 5 atoms extending between R1 and NR2R3 and a maximum chain length of 4 atoms extending between E and NR2R3, wherein one of the carbon atoms in the linker group may optionally be replaced by an oxygen or nitrogen atom; and wherein the carbon atoms of the linker group A may optionally bear one or more substituents selected from oxo, fluorine and hydroxy, provided that the hydroxy group when present is not located at a carbon atom α with respect to the NR2R3 group and provided that the oxo group when present is located at a carbon atom α with respect to the NR2R3 group; E is a monocyclic or bicyclic carbocyclic or heterocyclic group; R1 is an aryl or heteroaryl group; and R2, R3, R4 and R5 are as defined in the claims. Also provided are pharmaceutical compositions containing the compounds, methods for preparing the compounds and their use as anticancer agents.
摘要翻译： 本发明提供了具有蛋白激酶B抑制活性的式（I）化合物：其中A是含有1至7个碳原子的饱和烃连接基团，该连接基团具有在R1和NR2R3之间延伸的最大链长度为5个原子，以及 在E和NR2R3之间延伸的4个原子的最大链长度，其中连接基团中的一个碳原子可以任选地被氧或氮原子取代; 并且其中连接基团A的碳原子可以任选地具有一个或多个选自氧代，氟和羟基的取代基，条件是存在的羟基相对于NR 2 R 3基团不位于碳原子α，条件是 存在时的氧代基相对于NR2R3基团位于碳原子α; E是单环或双环碳环或杂环基; R1是芳基或杂芳基; 并且R 2，R 3，R 4和R 5如权利要求中所定义。 还提供含有化合物的药物组合物，制备化合物的方法及其作为抗癌剂的用途。
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公开(公告)号：US20140271662A1
公开(公告)日：2014-09-18
申请号：US14180440
申请日：2014-02-14
申请人： Astex Therapeutics Ltd , Cancer Research Technology Limited , The Institute of Cancer Research: Royal Cancer Hospital
发明人： Valerio BERDINI , Gordon SAXTY , Marinus Leendert VERDONK , Steven John WOODHEAD , Paul Graham WYATT , Robert George BOYLE , Hannah Fiona SORE , David Winter WALKER , Ian COLLINS , Robert DOWNHAM , Robin Arthur Ellis CARR
IPC分类号： A61K31/5377 , A61K45/06 , A61K31/415 , C07D401/10 , A61K31/497 , A61K31/4155 , A61K31/496 , C07D403/10 , A61K31/4178 , C07D231/12 , A61K31/454
CPC分类号： A61K31/415 , A61K9/0019 , A61K9/20 , A61K9/48 , A61K31/4155 , A61K31/4178 , A61K31/4439 , A61K31/454 , A61K31/4545 , A61K31/496 , A61K31/497 , A61K31/5377 , A61K31/551 , A61K45/06 , C07D231/12 , C07D401/04 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/10 , C07D403/12 , C07D405/04 , C07D413/10
摘要： The invention provides compounds of the formula (I) having protein kinase B inhibiting activity: wherein A is a saturated hydrocarbon linker group containing from 1 to 7 carbon atoms, the linker group having a maximum chain length of 5 atoms extending between R1 and NR2R3 and a maximum chain length of 4 atoms extending between E and NR2R3, wherein one of the carbon atoms in the linker group may optionally be replaced by an oxygen or nitrogen atom; and wherein the carbon atoms of the linker group A may optionally bear one or more substituents selected from oxo, fluorine and hydroxy, provided that the hydroxy group when present is not located at a carbon atom α with respect to the NR2R3 group and provided that the oxo group when present is located at a carbon atom α with respect to the NR2R3 group; E is a monocyclic or bicyclic carbocyclic or heterocyclic group; R1 is an aryl or heteroaryl group; and R2, R3, R4 and R5 are as defined in the claims. Also provided are pharmaceutical compositions containing the compounds, methods for preparing the compounds and their use as anticancer agents.
摘要翻译： 本发明提供了具有蛋白激酶B抑制活性的式（I）化合物：其中A是含有1至7个碳原子的饱和烃连接基团，该连接基团具有在R1和NR2R3之间延伸的最大链长度为5个原子，以及 在E和NR2R3之间延伸的4个原子的最大链长度，其中连接基团中的一个碳原子可以任选地被氧或氮原子取代; 并且其中连接基团A的碳原子可以任选地具有一个或多个选自氧代，氟和羟基的取代基，条件是存在的羟基相对于NR 2 R 3基团不位于碳原子α，条件是 存在时的氧代基相对于NR2R3基团位于碳原子α; E是单环或双环碳环或杂环基; R1是芳基或杂芳基; 并且R 2，R 3，R 4和R 5如权利要求中所定义。 还提供含有化合物的药物组合物，制备化合物的方法及其作为抗癌剂的用途。
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