专利检索 ap:("ASTEX THERAPEUTICS LTD") AND inv:"Valerio BERDINI" 第 1 页

1.

发明申请
SUBSTITUTED QUINOXALINES AS FGFR KINASE INHIBITORS 有权
标题翻译：作为FGFR激酶抑制剂的替代喹喔啉

公开(公告)号：US20160031856A1

公开(公告)日：2016-02-04

申请号：US14816565

申请日：2015-08-03

申请人： ASTEX THERAPEUTICS LTD

发明人： Gordon SAXTY , Christopher William MURRAY , Valerio BERDINI , Gilbert Ebai BESONG , Christopher Charles Frederick HAMLETT , Steven John WOODHEAD , Yannick Aime Eddy LIGNY , Patrick René ANGIBAUD

IPC分类号： C07D403/04 , C07D401/14 , C07D403/14

CPC分类号： C07D403/04 , C07D401/14 , C07D403/14

摘要： The invention relates to new quinoxaline derivative compounds, to pharmaceutical compositions comprising said compounds, to processes for the preparation of said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.

摘要翻译： 本发明涉及新的喹喔啉衍生物化合物，包含所述化合物的药物组合物，用于制备所述化合物的方法和所述化合物在治疗疾病中的用途。癌症。

2.

发明申请
PYRAZOLYL QUINOXALINE KINASE INHIBITORS 审中-公开

公开(公告)号：US20180127397A1

公开(公告)日：2018-05-10

申请号：US15810521

申请日：2017-11-13

申请人： ASTEX THERAPEUTICS LTD

发明人： Gordon SAXTY , Christopher William MURRAY , Valerio BERDINI , Gilbert Ebai BESONG , Christopher Charles Frederick HAMLETT , Christopher Norbert JOHNSON , Steven John WOODHEAD , Michael READER , David Charles REES , Laurence Anne MEVELLEC , Patrick René ANGIBAUD , Eddy Jean Edgard FREYNE , Tom Cornelis Hortense GOVAERTS , Johan Erwin Edmond WEERTS , Timothy Pietro Suren PERERA , Ronaldus Arnodus Hendrika Joseph GILISSEN , Berthold WROBLOWSKI , Jean Fernand Armand LACRAMPE , Alexandra PAPANIKOS , Olivier Alexis Georges QUEROLLE , Elisabeth Thérèse Jeanne PASQUIER , Isabelle Noëlle Constance PILATTE , Pascal Ghislain André BONNET , Werner Constant Johan EMBRECHTS , Rhalid AKKARI , Lieven MEERPOEL

IPC分类号： C07D403/04 , C07D491/113 , A61K45/06 , A61K31/5377 , A61K31/498 , C07F9/6524 , C07D487/08 , C07D413/14 , C07D409/14 , C07D405/14 , C07D403/14 , C07D401/14

摘要： The invention relates to new quinoxaline derivative compounds, to pharmaceutical compositions comprising said compounds, to processes for the preparation of said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.

3.

发明申请
3,4-DISUBSTITUTED 1H-PYRAZOLE COMPOUNDS AND THEIR USE AS CYCLIN DEPENDENT KINASE AND GLYCOGEN SYNTHASE KINASE-3 MODULATORS 有权
标题翻译： 3,4-取代的1H-吡唑化合物及其作为循环依赖性激酶和GLYCOGEN SYNTHASE激酶3调节剂的用途

公开(公告)号：US20140371213A1

公开(公告)日：2014-12-18

申请号：US14281360

申请日：2014-05-19

申请人： ASTEX THERAPEUTICS, LTD.

发明人： Valerio BERDINI , Michael Alistair O'BRIEN , Maria Grazia CARR , Theresa Rachel EARLY , Adrian Liam GILL , Gary TREWARTHA , Alison Jo-Anne WOOLFORD , Andrew James WOODHEAD , Paul Graham WYATT

IPC分类号： C07D231/38 , A61K31/415 , C07D231/40 , C07D403/12 , A61K31/4155 , A61K31/541 , A61K31/4439 , A61K31/4196 , A61K31/454 , A61K31/496 , A61K31/4178 , A61K31/5377 , A61K45/06 , C07D401/12

CPC分类号： C07D231/38 , A61K31/415 , A61K31/4152 , A61K31/4155 , A61K31/416 , A61K31/4178 , A61K31/4196 , A61K31/4439 , A61K31/454 , A61K31/496 , A61K31/5377 , A61K31/541 , A61K45/06 , C04B35/632 , C07D231/14 , C07D231/40 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D453/02 , C07D471/04

摘要： The invention provides compounds of the formula (0) or salts or tautomers or N-oxides or solvates thereof for use in the prophylaxis or treatment of disease states and conditions such as cancers mediated by cyclin-dependent kinase and glycogen synthase kinase-3. In formula (0): X is a group R1-A-NR4— or a 5- or 6-membered carbocyclic or heterocyclic ring; A is a bond, SO2, C═O, NRg(C═O) or O(C═O) wherein Rg is hydrogen or C1-4 hydrocarbyl optionally substituted by hydroxy or C1-4 alkoxy; Y is a bond or an alkylene chain of 1, 2 or 3 carbon atoms in length; R1 is hydrogen; a carbocyclic or heterocyclic group having from 3 to 12 ring members; or a C1-8 hydrocarbyl group optionally substituted by one or more substituents selected from halogen (e.g. fluorine), hydroxy, C1-4 hydrocarbyloxy, amino, mono- or di-C1-4 hydrocarbylamino, and carbocyclic or heterocyclic groups having from 3 to 12 ring members, and wherein 1 or 2 of the carbon atoms of the hydrocarbyl group may optionally be replaced by an atom or group selected from O, S, NH, SO, SO2; R2 is hydrogen; halogen; C1-4 alkoxy (e.g. methoxy); or a C1-4 hydrocarbyl group optionally substituted by halogen (e.g. fluorine), hydroxyl or C1-4 alkoxy (e.g. methoxy); R3 is selected from hydrogen and carbocyclic and heterocyclic groups having from 3 to 12 ring members; and R4 is hydrogen or a C1-4 hydrocarbyl group optionally substituted by halogen (e.g. fluorine), hydroxyl or C1-4 alkoxy (e.g. methoxy).

摘要翻译： 本发明提供式（O）的化合物或其盐或互变异构体或N-氧化物或溶剂合物，用于预防或治疗疾病状态和病症，例如由细胞周期蛋白依赖性激酶和糖原合酶激酶-3介导的癌症。在式（0）中：X为基团R 1 -A-NR 4 - 或5或6元碳环或杂环; A是键，SO 2，C = O，NR g（C = O）或O（C = O），其中R g是氢或任选被羟基或C 1-4烷氧基取代的C 1-4烃基; Y是长度为1,2或3个碳原子的键或亚烷基链; R1是氢; 具有3-12个环成员的碳环或杂环基; 或任选被一个或多个选自卤素（例如氟），羟基，C 1-4烃氧基，氨基，单或二-C 1-4烃基氨基的取代基取代的C 1-8烃基，以及具有3至 12个环成员，并且其中烃基的1或2个碳原子可以任选地被选自O，S，NH，SO，SO 2的原子或基团取代; R2是氢; 卤素; C 1-4烷氧基（如甲氧基）; 或任选被卤素（例如氟），羟基或C 1-4烷氧基（例如甲氧基）取代的C 1-4烃基; R 3选自具有3至12个环成员的氢和碳环和杂环基; 和R 4是氢或任选被卤素（例如氟），羟基或C 1-4烷氧基（例如甲氧基）取代的C 1-4烃基。

4.

发明申请
PYRAZOLE DERIVATIVES AS PROTEIN KINASE MODULATORS 有权
标题翻译：作为蛋白激酶调节剂的吡唑衍生物

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。

5.

发明申请
PYRAZOLE DERIVATIVES AS PROTEIN KINASE MODULATORS 审中-公开
标题翻译：作为蛋白激酶调节剂的吡唑衍生物

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。