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1. 发明授权

US09283226B2 Pyrazole derivatives as protein kinase modulators 有权
标题翻译：吡唑衍生物作为蛋白激酶调节剂
公开(公告)号：US09283226B2
公开(公告)日：2016-03-15
申请号：US14180440
申请日：2014-02-14
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 , C07D231/12 , A61K31/5377 , C07D401/04 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/10 , C07D403/12 , C07D405/04 , C07D413/10 , A61K31/4155 , A61K31/4178 , A61K31/454 , A61K31/496 , A61K31/497 , A61K45/06
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。

2. 发明授权

US08809336B2 Ortho-condensed pyridine and pyrimidine derivatives (e.g., purines) as protein kinases inhibitors 有权
标题翻译：正构缩合的吡啶和嘧啶衍生物（如嘌呤）作为蛋白激酶抑制剂
公开(公告)号：US08809336B2
公开(公告)日：2014-08-19
申请号：US14017814
申请日：2013-09-04
申请人： Astex Therapeutics Limited , The Institute of Cancer Research: Royal Cancer Hospital , Cancer Research Technology Limited
发明人： Valerio Berdini , Robert George Boyle , Gordon Saxty , David Winter Walker , Steven John Woodhead , Paul Graham Wyatt , Alastair Donald , John Caldwell , Ian Collins , Tatiana Faria Da Fonseca
IPC分类号： A61K31/497 , A61K31/52 , A61K31/519
CPC分类号： C07D471/04 , A61K31/4545 , A61K31/519 , A61K31/52 , A61K31/522 , C07D473/34 , C07D487/04
摘要： The invention provides a compound for use as a protein kinase B inhibitor, the compound being a compound of the formula (I) or salts, solvates, tautomers or N-oxides thereof, wherein T is N or CR5; J1-J2 is N═C(R6), (R7)C═N, (R8)N—C(O), (R8)2C—C(O), N═N or (R7)C═C(R6); E is a monocyclic carbocyclic or heterocyclic group of 5 or 6 ring members, the heterocyclic group containing up to 3 heteroatoms selected from O, N and S; Q1 is a bond or a saturated C1-3 hydrocarbon linker group, one of the carbon atoms in the linker group being optionally be replaced by an oxygen or nitrogen atom, or an adjacent pair of carbon atoms may be replaced by CONRq or NRqCO where Rq is hydrogen or methyl, or Rq is a C1-4 alkylene chain linked to R1 or a carbon atom of Q1 to form a cyclic moiety; and wherein the carbon atoms of the linker group Q1 may optionally bear one or more substituents selected from fluorine and hydroxy; Q2 is a bond or a saturated hydrocarbon linker group containing from 1 to 3 carbon atoms, 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 may optionally bear one or more substituents selected from fluorine and hydroxy, provided that the hydroxy group when present is not located at a carbon atom a with respect to the G group; and provided that when E is aryl or heteroaryl, then Q2 is other than a bond; G is hydrogen, NR2R3, OH or SH provided that when E is aryl or heteroaryl and Q2 is a bond, then G is hydrogen; R1 is hydrogen or an aryl or heteroaryl group, with the proviso that when R1 is hydrogen and G is NR2R3, then Q2 is a bond; and R2, R3, R4, R6 and R8 are as defined in the claims.
摘要翻译：本发明提供用作蛋白激酶B抑制剂的化合物，该化合物为式（I）化合物或其盐，溶剂合物，互变异构体或N-氧化物，其中T为N或CR 5; J1-J2是N = C（R6），（R7）C = N，（R8）N-C（O），（R8）2C-C（O），N = N或（R7）C = C ）; E是5或6个环成员的单环碳环或杂环基，杂环基含有至多3个选自O，N和S的杂原子; Q1是键或饱和的C 1-3烃连接基团，连接基团中的一个碳原子任选被氧或氮原子代替，或者相邻的一对碳原子可被CONRq或NRqCO代替，其中Rq 是氢或甲基，或Rq是与R1或Q1的碳原子连接的C 1-4亚烷基链，形成环状部分; 并且其中所述连接基团Q1的碳原子可任选地具有一个或多个选自氟和羟基的取代基; Q2是含有1至3个碳原子的键或饱和烃连接基团，其中连接基团中的一个碳原子可任选被氧或氮原子取代; 并且其中所述连接基团的碳原子可以任选地具有一个或多个选自氟和羟基的取代基，条件是当存在的羟基不相对于G基团位于碳原子a时; 并且条件是当E是芳基或杂芳基时，则Q2不是键; G为氢，NR2R3，OH或SH，条件是当E为芳基或杂芳基且Q2为键时，则G为氢; R 1是氢或芳基或杂芳基，条件是当R 1是氢且G是NR 2 R 3时，则Q2是一个键; 并且R 2，R 3，R 4，R 6和R 8如权利要求中所定义。

3. 发明授权

US09006430B2 Ortho-condensed pyridine and pyrimidine derivatives (e.g., purines) as protein 有权
标题翻译：正构缩合的吡啶和嘧啶衍生物（如嘌呤）作为蛋白激酶抑制剂
公开(公告)号：US09006430B2
公开(公告)日：2015-04-14
申请号：US14310475
申请日：2014-06-20
申请人： Astex Therapeutics Limited , The Institute of Cancer Research: Royal Cancer Hospital , Cancer Research Technology Limited
发明人： Valerio Berdini , Robert George Boyle , Gordon Saxty , David Winter Walker , Steven John Woodhead , Paul Graham Wyatt , Alastair Donald , John Caldwell , Ian Collins , Tatiana Faria Da Fonseca
IPC分类号： C07D487/04 , C07D471/02 , C07D471/04 , C07D473/34 , A61K31/4545 , A61K31/519 , A61K31/52 , A61K31/522
CPC分类号： C07D471/04 , A61K31/4545 , A61K31/519 , A61K31/52 , A61K31/522 , C07D473/34 , C07D487/04
摘要： The invention provides a compound for use as a protein kinase B inhibitor, the compound being a compound of the formula (I) or salts, solvates, tautomers or N-oxides thereof, wherein T is N or CR5; J1-J2 is N═C(R6), (R7)C═N, (R8)N—C(O), (R8)2C—C(O), N═N or (R7)C═C(R6); E is a monocyclic carbocyclic or heterocyclic group of 5 or 6 ring members, the heterocyclic group containing up to 3 heteroatoms selected from O, N and S; Q1 is a bond or a saturated C1-3 hydrocarbon linker group, one of the carbon atoms in the linker group being optionally be replaced by an oxygen or nitrogen atom, or an adjacent pair of carbon atoms may be replaced by CONRq or NRqCO where Rq is hydrogen or methyl, or Rq is a C1-4 alkylene chain linked to R or a carbon atom of Q1 to form a cyclic moiety; and wherein the carbon atoms of the linker group Q1 may optionally bear one or more substituents selected from fluorine and hydroxy; Q2 is a bond or a saturated hydrocarbon linker group containing from 1 to 3 carbon atoms, 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 may optionally bear one or more substituents selected from fluorine and hydroxy, provided that the hydroxy group when present is not located at a carbon atom a with respect to the G group; and provided that when E is aryl or heteroaryl, then Q2 is other than a bond; G is hydrogen, NR2R3, OH or SH provided that when E is aryl or heteroaryl and Q2 is a bond, then G is hydrogen; R1 is hydrogen or an aryl or heteroaryl group, with the proviso that when R1 is hydrogen and G is NR2R3, then Q is a bond; and R2, R3, R4, R6 and R8 are as defined in the claims.
摘要翻译：本发明提供用作蛋白激酶B抑制剂的化合物，该化合物为式（I）化合物或其盐，溶剂合物，互变异构体或N-氧化物，其中T为N或CR 5; J1-J2是N = C（R6），（R7）C = N，（R8）N-C（O），（R8）2C-C（O），N = N或（R7）C = C ）; E是5或6个环成员的单环碳环或杂环基，杂环基含有至多3个选自O，N和S的杂原子; Q1是键或饱和的C 1-3烃连接基团，连接基团中的一个碳原子任选被氧或氮原子代替，或者相邻的一对碳原子可被CONRq或NRqCO代替，其中Rq 是氢或甲基，或Rq是与R或Q1的碳原子连接的C 1-4亚烷基链，以形成环状部分; 并且其中所述连接基团Q1的碳原子可任选地具有一个或多个选自氟和羟基的取代基; Q2是含有1至3个碳原子的键或饱和烃连接基团，其中连接基团中的一个碳原子可任选被氧或氮原子取代; 并且其中所述连接基团的碳原子可以任选地具有一个或多个选自氟和羟基的取代基，条件是当存在的羟基不相对于G基团位于碳原子a时; 并且条件是当E是芳基或杂芳基时，则Q2不是键; G为氢，NR2R3，OH或SH，条件是当E为芳基或杂芳基且Q2为键时，则G为氢; R 1是氢或芳基或杂芳基，条件是当R 1是氢并且G是NR 2 R 3时，则Q是一个键; 并且R 2，R 3，R 4，R 6和R 8如权利要求中所定义。

5. 发明授权

US09856236B2 Substituted quinoxalines as FGFR kinase inhibitors 有权
公开(公告)号：US09856236B2
公开(公告)日：2018-01-02
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： C07D241/40 , 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 of formula (I), 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.

7. 发明授权

US10519137B2 Pyrazolyl quinoxaline kinase inhibitors 有权
公开(公告)号：US10519137B2
公开(公告)日：2019-12-31
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 , Steven John Woodhead , Michael Reader , Laurence Anne Mevellec , Patrick René Angibaud , Eddy Jean Edgard Freyne , Timothy Pietro Suren Perera , Berthold Wroblowski , Alexandra Papanikos , Olivier Alexis Georges Querolle , Isabelle Noëlle Constance Pilatte , Pascal Ghislain André Bonnet , Werner Constant Johan Embrechts , Rhalid Akkari , Lieven Meerpoel
IPC分类号： C07D231/10 , C07D231/12 , A61K31/415 , C07D403/04 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D487/08 , A61K31/498 , A61K31/5377 , A61K45/06 , C07D491/113 , C07D401/14 , C07F9/6524
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.

8. 发明授权

US09464071B2 Pyrazolyl quinoxaline kinase inhibitors 有权
标题翻译：吡唑基喹喔啉激酶抑制剂
公开(公告)号：US09464071B2
公开(公告)日：2016-10-11
申请号：US14505020
申请日：2014-10-02
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： A61K31/415 , C07D231/10 , C07D231/12 , C07D403/04 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D487/08 , A61K31/498 , A61K31/5377 , A61K45/06 , C07D491/113
CPC分类号： C07D403/04 , A61K31/498 , A61K31/5377 , A61K45/06 , C07D401/14 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D487/08 , C07D491/113 , C07F9/6524
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。

9. 发明授权

US09051278B2 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： 3,4-二取代的1H-吡唑化合物及其作为细胞周期蛋白依赖性激酶和糖原合成酶激酶-3调节剂的用途
公开(公告)号：US09051278B2
公开(公告)日：2015-06-09
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： A61K31/4439 , C07D401/12 , C07D231/38 , A61K31/4152 , A61K31/416 , A61K31/454 , C04B35/632 , C07D231/14 , C07D231/40 , C07D401/14 , C07D403/04 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D453/02 , C07D471/04 , A61K31/415 , A61K31/4155 , A61K31/4178 , A61K31/4196 , A61K31/496 , A61K31/5377 , A61K31/541 , A61K45/06
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至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。

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