公开(公告)号：US20070135477A1

公开(公告)日：2007-06-14

申请号：US10564166

申请日：2004-07-05

申请人： Valerio Berdini ,  Michael O'Brien ,  Maria Carr ,  Theresa Early ,  Eva Navarro ,  Adrian Gill ,  Steven Howard ,  Gary Trewartha ,  Alison Woolford ,  Andrew Woodhead ,  Paul Wyatt

发明人： Valerio Berdini ,  Michael O'Brien ,  Maria Carr ,  Theresa Early ,  Eva Navarro ,  Adrian Gill ,  Steven Howard ,  Gary Trewartha ,  Alison Woolford ,  Andrew Woodhead ,  Paul Wyatt

IPC分类号： A61K31/4745 ,  A61K31/4184 ,  C07D403/04

CPC分类号： A61K31/5377 ,  A61K31/00 ,  A61K31/4184 ,  A61K45/06 ,  C07D401/14 ,  C07D403/04 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D471/04 ,  C07D513/04

摘要： The invention provides compounds of the formula (1): The compounds have activity against cyclin depdenent kinases, glycogen synthase kinase and Auroa kinases and are therefore useful to treat cancer and viral diseases.

摘要翻译： 本发明提供式（1）化合物：该化合物对细胞周期蛋白依赖性激酶，糖原合酶激酶和Auroa激酶具有活性，因此可用于治疗癌症和病毒性疾病。

公开(公告)号：US20060194843A1

公开(公告)日：2006-08-31

申请号：US11336599

申请日：2006-01-20

申请人： Valerio Berdini ,  Michael O'Brien ,  Maria Carr ,  Theresa Early ,  Adrian Gill ,  Gary Trewartha ,  Alison Woolford ,  Andrew Woodhead ,  Paul Wyatt

发明人： Valerio Berdini ,  Michael O'Brien ,  Maria Carr ,  Theresa Early ,  Adrian Gill ,  Gary Trewartha ,  Alison Woolford ,  Andrew Woodhead ,  Paul Wyatt

IPC分类号： A61K31/454 ,  A61K31/416 ,  A61K31/4152 ,  C07D403/02

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).

公开(公告)号：US07977477B2

公开(公告)日：2011-07-12

申请号：US10564166

申请日：2004-07-05

申请人： Valerio Berdini ,  Michael Alistair O'Brien ,  Maria Grazia Carr ,  Theresa Rachel Early ,  Eva Figueroa Navarro ,  Adrian Liam Gill ,  Steven Howard ,  Gary Trewartha ,  Alison Jo-Anne Woolford ,  Andrew James Woodhead ,  Paul Wyatt

发明人： Valerio Berdini ,  Michael Alistair O'Brien ,  Maria Grazia Carr ,  Theresa Rachel Early ,  Eva Figueroa Navarro ,  Adrian Liam Gill ,  Steven Howard ,  Gary Trewartha ,  Alison Jo-Anne Woolford ,  Andrew James Woodhead ,  Paul Wyatt

IPC分类号： A61K31/5377 ,  A61K31/4184 ,  C07D413/14

CPC分类号： A61K31/5377 ,  A61K31/00 ,  A61K31/4184 ,  A61K45/06 ,  C07D401/14 ,  C07D403/04 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D471/04 ,  C07D513/04

摘要： The invention provides compounds of the formula (I): The compounds have activity against cyclin dependent kinases, glycogen synthase kinase and Auroa kinases and are therefore useful to treat cancer and viral diseases.

摘要翻译： 本发明提供式（I）化合物：该化合物具有抗细胞周期蛋白依赖性激酶，糖原合成酶激酶和Auroa激酶的活性，因此可用于治疗癌症和病毒性疾病。

公开(公告)号：US08778936B2

公开(公告)日：2014-07-15

申请号：US13329952

申请日：2011-12-19

申请人： Valerio Berdini ,  Maria Grazia Carr ,  Adrian Liam Gill ,  Steven Howard ,  Eva Figueroa Navarro ,  Gary Trewartha ,  David Charles Rees ,  Mladen Vinkovic ,  Paul Graham Wyatt

发明人： Valerio Berdini ,  Maria Grazia Carr ,  Adrian Liam Gill ,  Steven Howard ,  Eva Figueroa Navarro ,  Gary Trewartha ,  David Charles Rees ,  Mladen Vinkovic ,  Paul Graham Wyatt

IPC分类号： A61K31/535

CPC分类号： C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D407/14 ,  C07D413/14 ,  C07D487/04 ,  C07D513/04

摘要： The invention provides a compound of the formula (I): or a salt, solvate, tautomer or N-oxide thereof, wherein M is selected from a group D1 and a group D2: and R′, E, A and X are as defined in the claims. Also provided are pharmaceutical compositions containing the compounds, processes for making the compounds and the use of the compounds in the prophylaxis or treatment of a disease state mediated by a CDK kinase, GSK-3 kinase or Aurora kinase.

摘要翻译： 本发明提供式（I）化合物或其盐，溶剂化物，互变异构体或N-氧化物，其中M选自D1和D2组：R'，E，A和X如上所定义 在权利要求中。 还提供了含有化合物的药物组合物，制备该化合物的方法以及该化合物在预防或治疗由CDK激酶，GSK-3激酶或极光激酶介导的疾病状态中的用途。

公开(公告)号：US20100160324A1

公开(公告)日：2010-06-24

申请号：US11813167

申请日：2005-12-30

申请人： Valerio Berdini ,  Michael Alistair O'Brien ,  Maria Grazia Carr ,  Nicholas Gareth Morse Davies ,  Adrian Liam Gill ,  Eva Figueroa Navarro ,  Steven Howard ,  Gary Trewartha ,  Andrew James Woodhead ,  Alison Jo-Anne Woolford ,  Paul Graham Wyatt

发明人： Valerio Berdini ,  Michael Alistair O'Brien ,  Maria Grazia Carr ,  Nicholas Gareth Morse Davies ,  Adrian Liam Gill ,  Eva Figueroa Navarro ,  Steven Howard ,  Gary Trewartha ,  Andrew James Woodhead ,  Alison Jo-Anne Woolford ,  Paul Graham Wyatt

IPC分类号： C07D403/04 ,  A61P25/28 ,  C07D413/04 ,  A61K31/497 ,  A61K31/4353 ,  A61K31/4439 ,  A61K31/4245 ,  A61K31/427 ,  A61K31/422 ,  A61K31/4196 ,  A61K31/415 ,  A61K31/5377 ,  C07D471/04 ,  C07D401/04 ,  C07D417/04 ,  C07D249/12 ,  A61K31/4155 ,  A61K31/496 ,  C07D231/10 ,  A61P35/04

CPC分类号： C07D407/14 ,  C07D231/40 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D405/04 ,  C07D405/14 ,  C07D413/04 ,  C07D417/04 ,  C07D471/04

摘要： The invention provides a compound of the formula (I): for use in medicine: or salts or tautomers or N-oxides or solvates thereof; wherein R1 is an optionally substituted heterocyclic group having from 3 to 12 ring members provided that the cyclic group joined to the pyrazole contains at least one heteroatom selected from N, O or S; A is a bond or —Y—(B)n—; B is 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; n is 0 or 1; Y is a bond or an alkylene chain of 1,2 or 3 carbon atoms in length; 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 optionally substituted carbocyclic and heterocyclic groups having from 3 to 12 ring members or an optionally substituted C1-8 hydrocarbyl group; with the proviso that R1 is not formula (II): where X, R3′ and R4′ are defined in the claims.

摘要翻译： 本发明提供式（I）化合物：用于医药：或其盐或互变异构体或N-氧化物或溶剂合物; 其中R1是具有3至12个环成员的任选取代的杂环基，条件是连接到吡唑的环状基团含有至少一个选自N，O或S的杂原子; A是键或-Y-（B）n-; B为C = O，NR g（C = O）或O（C = O），其中R g为氢或任选被羟基或C 1-4烷氧基取代的C 1-4烃基; n为0或1; Y是长度为1,2或3个碳原子的键或亚烷基链; 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; R3选自具有3至12个环成员或任选取代的C 1-8烃基的任选取代的碳环和杂环基; 条件是R 1不是式（II）：其中X，R 3'和R 4'在权利要求中限定。

公开(公告)号：US08110573B2

公开(公告)日：2012-02-07

申请号：US11813031

申请日：2005-12-30

申请人： Valerio Berdini ,  Maria Grazia Carr ,  Adrian Liam Gill ,  Steven Howard ,  Eva Figueroa Navarro ,  Gary Trewartha ,  David Charles Rees ,  Mladen Vinkovic ,  Paul Graham Wyatt

发明人： Valerio Berdini ,  Maria Grazia Carr ,  Adrian Liam Gill ,  Steven Howard ,  Eva Figueroa Navarro ,  Gary Trewartha ,  David Charles Rees ,  Mladen Vinkovic ,  Paul Graham Wyatt

IPC分类号： A61K31/535 ,  C07D413/14

CPC分类号： C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D407/14 ,  C07D413/14 ,  C07D487/04 ,  C07D513/04

摘要： The invention provides a compound of the formula (I): or a salt, solvate, tautomer or N-oxide thereof, wherein M is selected from a group D1 and a group D2: and R′, E, A and X are as defined in the claims. Also provided are pharmaceutical compositions containing the compounds, processes for making the compounds and the use of the compounds in the prophylaxis or treatment of a disease state mediated by a CDK kinase, GSK-3 kinase or Aurora kinase.

摘要翻译： 本发明提供式（I）化合物或其盐，溶剂化物，互变异构体或N-氧化物，其中M选自D1和D2组：R'，E，A和X如上所定义 在权利要求中。 还提供了含有化合物的药物组合物，制备该化合物的方法以及该化合物在预防或治疗由CDK激酶，GSK-3激酶或极光激酶介导的疾病状态中的用途。

公开(公告)号：US20080132495A1

公开(公告)日：2008-06-05

申请号：US11813031

申请日：2005-12-30

申请人： Valerio Berdini ,  Maria Grazia Carr ,  Adrian Liam Gill ,  Steven Howard ,  Eva Figueroa Navarro ,  Gary Trewartha ,  David Charles Rees ,  Mladen Vinkovic ,  Paul Graham Wyatt

发明人： Valerio Berdini ,  Maria Grazia Carr ,  Adrian Liam Gill ,  Steven Howard ,  Eva Figueroa Navarro ,  Gary Trewartha ,  David Charles Rees ,  Mladen Vinkovic ,  Paul Graham Wyatt

IPC分类号： A61K31/4184 ,  A61K31/454 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/541 ,  A61P35/00 ,  A61P35/02 ,  C07D231/38 ,  C07D401/14 ,  C07D403/14 ,  C07D413/02 ,  C07D413/14 ,  C07D417/14 ,  C07D487/14

CPC分类号： C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D407/14 ,  C07D413/14 ,  C07D487/04 ,  C07D513/04

摘要： The invention provides a compound of the formula (I): or a salt, solvate, tautomer or N-oxide thereof, wherein M is selected from a group D1 and a group D2: and R′, E, A and X are as defined in the claims. Also provided are pharmaceutical compositions containing the compounds, processes for making the compounds and the use of the compounds in the prophylaxis or treatment of a disease state mediated by a CDK kinase, GSK-3 kinase or Aurora kinase.

摘要翻译： 本发明提供式（I）化合物或其盐，溶剂化物，互变异构体或N-氧化物，其中M选自D1和D2组：R'，E，A和X如上所定义 在权利要求中。 还提供了含有化合物的药物组合物，制备该化合物的方法以及该化合物在预防或治疗由CDK激酶，GSK-3激酶或极光激酶介导的疾病状态中的用途。

公开(公告)号：US20080200509A1

公开(公告)日：2008-08-21

申请号：US11875482

申请日：2007-10-19

申请人： 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

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： A61K31/454 ,  A61P35/00 ,  A61P35/02

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).

公开(公告)号：US08080666B2

公开(公告)日：2011-12-20

申请号：US12877499

申请日：2010-09-08

申请人： 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

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： C07D401/02

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。

公开(公告)号：US07825140B2

公开(公告)日：2010-11-02

申请号：US11875482

申请日：2007-10-19

申请人： 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

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： A61K31/4465 ,  C07D211/56

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。