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1. 发明申请

WO2006077419A1 PYRAZOLE DERIVATIVES FOR THE INHIBITION OF CDK' S AND GSK' S 审中-公开
标题翻译：用于抑制CDK和GSK'S的吡唑衍生物
公开(公告)号：WO2006077419A1
公开(公告)日：2006-07-27
申请号：PCT/GB2006/000196
申请日：2006-01-20
申请人： ASTEX THERAPEUTICS LIMITED , WYATT, Paul, Graham , BERDINI, Valerio , GILL, Adrian, Liam , TREWARTHA, Gary , WOODHEAD, Andrew, James , NAVARRO, Eva, Figueroa , O'BRIEN, Michael, Alistair , PHILLIPS, Theresa, Rachel
发明人： WYATT, Paul, Graham , BERDINI, Valerio , GILL, Adrian, Liam , TREWARTHA, Gary , WOODHEAD, Andrew, James , NAVARRO, Eva, Figueroa , O'BRIEN, Michael, Alistair , PHILLIPS, Theresa, Rachel
IPC分类号： C07D453/02 , C07D401/14 , C07D401/12 , A61K31/44 , A61K31/4545 , A61K31/506 , A61P35/00 , A01N43/56
CPC分类号： C07D231/14 , C07D231/40 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/12 , C07D417/14
摘要： The invention provides compounds of the formula (I) or a salt, tautomer, solvate or N-oxides thereof; wherein: R 1 is selected from (a) 2,6-dichlorophenyl; (b) 2,6-difluorophenyl; (c) a 2,3,6-trisubstituted phenyl group wherein the substituents are fluorine, chlorine, methyl or methoxy; and (d) a group R 0 wherein R 0 is a 3-12 membered carbocyclic or heterocyclic group; or optionally substituted C 1-8 hydrocarbyl; R 2a and R 2b are each hydrogen or methyl; and R 3 is as defined in the claims. The compounds have activity as inhibitors of Cyclin Dependent Kinases (CDK) and Glycogen Synthase Kinases (GSK) kinases and are useful in the treatment or prophylaxis of disease states or conditions mediated by the kinases.
摘要翻译：本发明提供式（I）化合物或其盐，互变异构体，溶剂合物或N-氧化物; 其中：R 1选自（a）2,6-二氯苯基; （b）2,6-二氟苯基; （c）2,3,6-三取代的苯基，其中取代基是氟，氯，甲基或甲氧基; 和（d）R 0为0的基团，其中R 0为3-12元碳环或杂环基; 或任选取代的C 1-8烃基; R 2a和R 2b各自为氢或甲基; R 3和R 3如权利要求中所定义。该化合物具有作为细胞周期蛋白依赖性激酶（CDK）和糖原合酶激酶（GSK）激酶抑制剂的活性，可用于治疗或预防由激酶介导的疾病状态或病症。

2. 发明申请

WO2006077414A1 PYRAZOLE DERIVATIVES FOR THE INHIBITION OF CDK' S AND GSK' S 审中-公开
标题翻译：用于抑制CDK和GSK'S的吡唑衍生物
公开(公告)号：WO2006077414A1
公开(公告)日：2006-07-27
申请号：PCT/GB2006/000191
申请日：2006-01-20
申请人： ASTEX THERAPEUTICS LIMITED , WYATT, Paul, Graham , BERDINI, Valerio , GILL, Adrian, Liam , TREWARTHA, Gary , WOODHEAD, Andrew, James , NAVARRO, Eva, Figueroa , O'BRIEN, Michael, Alistair , PHILLIPS, Theresa, Rachel
发明人： WYATT, Paul, Graham , BERDINI, Valerio , GILL, Adrian, Liam , TREWARTHA, Gary , WOODHEAD, Andrew, James , NAVARRO, Eva, Figueroa , O'BRIEN, Michael, Alistair , PHILLIPS, Theresa, Rachel
IPC分类号： C07D401/14 , A61K31/44 , A61P35/00 , A01N43/56
CPC分类号： C07D231/14 , C07D231/40 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/12 , C07D417/14
摘要： The invention provides compounds of the formula (I), or salts, tautomers, N-oxides or solvates thereof wherein: R1 is selected from: (a) 2,6-dichlorophenyl; (b) 2,6-difluorophenyl; (c) a 2,3,6-trisubstituted phenyl group wherein the substituents for the phenyl group are selected from fluorine, chlorine, methyl and methoxy; (d) a group R0; (e) a group R a; (f) a group Rlb; (g) a group Rlc; (h) a group Rld; and 0) 2,6-difluorophenylamino ; wherein R )0υ, r R> llaa, T Rj I1bD, T R) I1cC, r R> Iidα, r R»2zaa, r R>22bD and RJ are as defined in the claims. The compounds have activity as inhibitors of cdk kinase (such as cdkl or cdk2) and glycogen synthase kinase-3 activity.
摘要翻译：本发明提供式（I）化合物或其盐，互变异构体，N-氧化物或溶剂合物，其中：R1选自：（a）2,6-二氯苯基; （b）2,6-二氟苯基; （c）2,3,6-三取代苯基，其中苯基的取代基选自氟，氯，甲基和甲氧基; （d）R0组; （e）基团R a; （f）组R1b; （g）R1c组; （h）一组Rld; 和0）2,6-二氟苯基氨基; 其中R 1，R 2，R 11a，R R 1，I R C，R R I，R R 2，R 2，R 22和R 22如权利要求中所定义。该化合物具有作为cdk激酶抑制剂（如cdk1或cdk2）和糖原合酶激酶-3活性的活性。

3. 发明申请

WO2006070198A1 PYRAZOLE DERIVATIVES AS THAT MODULATE THE ACTIVITY OF CDK, GSK AND AURORA KINASES 审中-公开
标题翻译：用于调节CDK，GSK和AURORA KINASES活性的吡唑衍生物
公开(公告)号：WO2006070198A1
公开(公告)日：2006-07-06
申请号：PCT/GB2005/005102
申请日：2005-12-30
申请人： ASTEX THERAPEUTICS LIMITED , BERDINI, Valerio , O'BRIEN, Michael, Alistair , CARR, Maria, Grazia , DAVIES, Nicholas, Gareth, Morse , GILL, Adrian, Liam , NAVARRO, Eva, Figueroa , HOWARD, Steven , TREWARTHA, Gary , WOODHEAD, Andrew, James , WOOLFORD, Alison, Jo-Anne , WYATT, Paul, Graham
发明人： BERDINI, Valerio , O'BRIEN, Michael, Alistair , CARR, Maria, Grazia , DAVIES, Nicholas, Gareth, Morse , GILL, Adrian, Liam , NAVARRO, Eva, Figueroa , HOWARD, Steven , TREWARTHA, Gary , WOODHEAD, Andrew, James , WOOLFORD, Alison, Jo-Anne , WYATT, Paul, Graham
IPC分类号： C07D401/04 , C07D401/14 , C07D403/04 , C07D417/04 , C07D413/04 , C07D471/04 , A61K31/4155 , A61K31/422 , A61K31/427 , A61P35/00
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 R 1 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, NR g (C=O) or O(C=O) wherein R g is hydrogen or C 1-4 hydrocarbyl optionally substituted by hydroxy or C 1-4 alkoxy; n is 0 or 1; Y is a bond or an alkylene chain of 1,2 or 3 carbon atoms in length; R 2 is hydrogen; halogen; C 1-4 alkoxy ( e.g . methoxy); or a C 1-4 hydrocarbyl group optionally substituted by halogen ( e.g. fluorine), hydroxyl or C 1-4 alkoxy (e.g. methoxy); R 3 is selected from optionally substituted carbocyclic and heterocyclic groups having from 3 to 12 ring members or an optionally substituted C 1-8 hydrocarbyl group; with the proviso that R 1 is not formula (II): where X, R 3’ and R 4’ 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R 1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是C = O，NR（C = O）或O（C = O），其中R g是氢或C 1-4 >任选被羟基或C 1-4烷氧基取代的烃基; 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; R 2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烷基; R 3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。

4. 发明申请

WO2005012256A1 3, 4-DISUBSTITUTED 1H-PYRAZOLE COMPOUNDS AND THEIR USE AS CYCLIN DEPENDENT KINASES (CDK) AND GLYCOGEN SYNTHASE KINASE-3 (GSK-3) MODULATORS 审中-公开
标题翻译： 3，4-取代的1H-吡唑化合物及其作为循环激酶（CDK）和GLYCOGEN SYNTHASE KINASE-3（GSK-3）调节剂的用途
公开(公告)号：WO2005012256A1
公开(公告)日：2005-02-10
申请号：PCT/GB2004/003179
申请日：2004-07-22
申请人： ASTEX TECHNOLOGY LIMITED , BERDINI, Valerio , O'BRIEN, Michael, Alistair , CARR, Maria, Grazia , EARLY, Theresa, Rachel , NAVARRO, Eva, Figueroa , GILL, Adrian, Liam , TREWARTHA, Gary , WOOLFORD, Alison, Jo-Anne , WOODHEAD, Andrew, James , WYATT, Paul, Graham
发明人： BERDINI, Valerio , O'BRIEN, Michael, Alistair , CARR, Maria, Grazia , EARLY, Theresa, Rachel , NAVARRO, Eva, Figueroa , GILL, Adrian, Liam , TREWARTHA, Gary , WOOLFORD, Alison, Jo-Anne , WOODHEAD, Andrew, James , WYATT, Paul, Graham
IPC分类号： C07D231/38
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. Formula (0). In formula (0): X is a group R 1 -A-NR 4 - or a 5- or 6-membered carbocyclic or heterocyclic ring; A is a bond, S0 2 , C=O, NR g (C=O) or O(C=O) wherein R g is hydrogen or C 1-4 hydrocarbyl optionally substituted by hydroxy or C 1-4 alkoxy; Y is a bond or an alkylene chain of 1, 2 or 3 carbon atoms in length; R 1 is hydrogen; a carbocyclic or heterocyclic group having from 3 to 12 ring members; or a C 1-8 hydrocarbyl group optionally substituted by one or more substituents selected from halogen (e.g. fluorine), hydroxy, C 1-4 hydrocarbyloxy, amino, mono- or di-C 1-4 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 0, S, NH, SO, S0 2 ; R 2 is hydrogen; halogen; C 1-4 alkoxy (e.g. methoxy); or a C 1-4 hydrocarbyl group optionally substituted by halogen (e.g. fluorine), hydroxyl or C 1-4 alkoxy (e.g. methoxy); R 3 is selected from hydrogen and carbocyclic and heterocyclic groups having from 3 to 12 ring members; and R 4 is hydrogen or a C 1-4 hydrocarbyl group optionally substituted by halogen (e.g. fluorine), hydroxyl or C 1-4 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。公式（0）。在式（0）中：X是基团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; R 1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，并且其中烃基中的1或2个碳原子可以任选地被选自0，S，NH，SO，SO 2的原子或基团取代; R 2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; 并且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。

5. 发明申请

WO2006070195A1 PYRAZOLE COMPOUNDS THAT MODULATE THE ACTIVITY OF CDK, GSK AND AURORA KINASIS 审中-公开
标题翻译：调节CDK，GSK和AURORA KINASIS的活性的吡咯化合物
公开(公告)号：WO2006070195A1
公开(公告)日：2006-07-06
申请号：PCT/GB2005/005097
申请日：2005-12-30
申请人： ASTEX THERAPEUTICS LIMITED , BERDINI, Valerio , CARR, Maria, Grazia , GILL, Adrian, Liam , HOWARD, Steven , NAVARRO, Eva, Figueroa , TREWARTHA, Gary , REES, David, Charles , VINKOVIC, Mladen , WYATT, Paul, Graham
发明人： BERDINI, Valerio , CARR, Maria, Grazia , GILL, Adrian, Liam , HOWARD, Steven , NAVARRO, Eva, Figueroa , TREWARTHA, Gary , REES, David, Charles , VINKOVIC, Mladen , WYATT, Paul, Graham
IPC分类号： C07D403/04 , C07D513/04 , C07D407/14 , A61K31/4184 , A61P35/00
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。

6. 发明申请

WO2006077416A1 PYRAZOLE DERIVATIVES FOR THE INHIBITION OF CDK' S AND GSK' S 审中-公开
标题翻译：用于抑制CDK和GSK'S的吡唑衍生物
公开(公告)号：WO2006077416A1
公开(公告)日：2006-07-27
申请号：PCT/GB2006/000193
申请日：2006-01-20
申请人： ASTEX THERAPEUTICS LIMITED , WYATT, Paul, Graham , BERDINI, Valerio , GILL, Adrian, Liam , TREWARTHA, Gary , WOODHEAD, Andrew, James
发明人： WYATT, Paul, Graham , BERDINI, Valerio , GILL, Adrian, Liam , TREWARTHA, Gary , WOODHEAD, Andrew, James
IPC分类号： C07D401/14 , A61K31/44 , A61P35/00 , A01N43/56
CPC分类号： C07D231/14 , C07D231/40 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/12 , C07D417/14
摘要： The invention provides a compound of the formula (I): or salts, tautomers, solvates and N-oxides thereof; wherein: R1 is 2,6-dichlorophenyl; R2a and R2 are both hydrogen; and R3 is a group: where R4 is C1-4 alkyl. The compounds have activity as inhibitors of CDK kinases and inhibit the proliferation of cancer cells.
摘要翻译：本发明提供式（I）的化合物或其盐，互变异构体，溶剂化物和N-氧化物; 其中：R1是2,6-二氯苯基; R2a和R2都是氢; 并且R 3是一个基团：其中R 4是C 1-4烷基。该化合物具有作为CDK激酶抑制剂的活性并抑制癌细胞的增殖。

7. 发明申请

WO2006070202A1 PYRAZOLE DERIVATIVES HAVING KINASE MODULATING ACTIVITY 审中-公开
标题翻译：具有激酶调节活性的吡唑衍生物
公开(公告)号：WO2006070202A1
公开(公告)日：2006-07-06
申请号：PCT/GB2005/005109
申请日：2005-12-30
申请人： ASTEX THERAPEUTICS LIMITED , BERDINI, Valerio , O'BRIEN, Michael, Alistair , NAVARRO, Eva, Figueroa , WYATT, Paul, Graham
发明人： BERDINI, Valerio , O'BRIEN, Michael, Alistair , NAVARRO, Eva, Figueroa , WYATT, Paul, Graham
IPC分类号： C07D413/14 , C07D403/04 , C07D407/14 , A01N43/56 , A61K31/4178 , A61K31/422 , A61P35/00
CPC分类号： C07D403/04 , C07D405/14 , C07D413/14
摘要： The invention provides a compound of the formula (I): or a salt, tautomer, N-oxide or solvate thereof; wherein A is selected from a bond, CH 2 and CH(CN); R l is selected from: (i) a cycloalkyl group of 3 to 6 ring members optionally substituted by one or more substituents selected from methyl, ethyl, hydroxy, methoxy, ethoxy, fluorine, amino and cyano; (ii) a phenyl group optionally substituted by up to three substituents selected from methyl, ethyl, fluorine, chlorine, methoxy, ethoxy and methylsulphonyl, but excluding 2,6-difluorophenyl, 2-fluoro-6-methoxy and 5-chloro-2-methoxyphenyl; (iii) a monocyclic heterocyclic group selected from furyl and isoxazolyl, the heterocyclic group being optionally substituted by one or two groups selected from methyl, ethyl, and a group CH 2 R 2 where R 2 is a five or six membered saturated heterocyclic ring containing one or two heteroatom ring members selected from O and N, the heterocyclic ring being optionally substituted by one or two methyl groups; and (iv) a bicyclic heterocyclic group selected from 2,3-dihydrobenzofuranyl and benzo[c]isoxazolyl, the bicyclic group being optionally substituted by one or two substituents selected from methyl, ethyl, hydroxy, methoxy, ethoxy, fluorine, amino, cyano and chlorine, the bicyclic heterocyclic group being other than a 2,2-dimethyl-2,3-dihydrobenzofuran-7-yl group.
摘要翻译：本发明提供式（I）化合物或其盐，互变异构体，N-氧化物或其溶剂合物; 其中A选自键，CH 2和CH（CN）; R 1选自：（i）任选被一个或多个选自甲基，乙基，羟基，甲氧基，乙氧基，氟，氨基和氰基的取代基取代的3至6个环成员的环烷基; （ii）任选被至多三个选自甲基，乙基，氟，氯，甲氧基，乙氧基和甲基磺酰基的取代基取代的苯基，但不包括2,6-二氟苯基，2-氟-6-甲氧基和5-氯-2 - 甲氧基; （iii）选自呋喃基和异恶唑基的单环杂环基，杂环基团任选被一个或两个选自甲基，乙基和CH 2 R 2 R 2 O 2基团取代其中R 2是含有一个或两个选自O和N的杂原子环成员的五或六元饱和杂环，杂环任选被一个或两个甲基取代; 和（iv）选自2,3-二氢苯并呋喃基和苯并[c]异恶唑基的双环杂环基，双环基团任选被一个或两个选自甲基，乙基，羟基，甲氧基，乙氧基，氟，氨基，氰基和氯，双环杂环基不同于2,2-二甲基-2,3-二氢苯并呋喃-7-基。

8. 发明申请

WO2005002576A2 PHARMACEUTICAL COMPOUNDS 审中-公开
标题翻译：药物化合物
公开(公告)号：WO2005002576A2
公开(公告)日：2005-01-13
申请号：PCT/GB2004/002913
申请日：2004-07-05
申请人： ASTEX TECHNOLOGY LIMITED , BERDINI, Valerio , WOODHEAD, Andrew, James , WYATT, Paul, Graham , O'BRIEN, Michael, Alistair , NAVARRO, Eva, Figueroa
发明人： BERDINI, Valerio , WOODHEAD, Andrew, James , WYATT, Paul, Graham , O'BRIEN, Michael, Alistair , NAVARRO, Eva, Figueroa
IPC分类号： A61K31/4184
CPC分类号： C07D401/14 , A61K31/00 , A61K31/4184 , C07D403/04 , C07D405/14 , C07D409/14 , C07D413/14
摘要： The invention provides a compound of the formula (I): or a salt, N-oxide or solvate thereof; wherein X is CR 5 or N; A is a bond or -(CH 2 ) m -(B) n -; B is C=O, NR g (C=O) or O(C=O) wherein R g is hydrogen or C I-4 hydrocarbyl optionally substituted by hydroxy or C I-4 alkoxy; m is 0, 1 or 2; n is 0 or 1; R 1 is hydrogen, a carbocyclic or heterocyclic group having from 3 to 12 ring members, or an optionally substituted C I-8 hydrocarbyl group; R 2 is hydrogen, halogen, methoxy, or a C I-4 hydrocarbyl group optionally substituted by halogen, hydroxyl or methoxy; R 3 and R 4 are the same or different and each is selected from hydrogen, CN, C(O)R 8 , optionally substituted C I-8 hydrocarbyl and carbocyclic or heterocyclic groups having from 3 to 12 ring members; and R 5 is hydrogen, a group R 2 or a group R 10 wherein R 10 is selected from halogen, hydroxy, trifluoromethyl, cyano, nitro, carboxy, amino, mono- or di-C I-4 hydrocarbyl amino, carbocyclic and heterocyclic groups having from 3 to 12 ring members; a group R a -R b wherein R a is a bond, 0, CO, X I C(X 2 ), C(X 2 )X I , X I C(X 2 )X I , S, SO, S0 2 , NR c , S0 2 NR c or NR c S0 2 ; and R b is selected from hydrogen, carbocyclic and heterocyclic groups having from 3 to 12 ring members, and a C 1-8 hydrocarbyl group optionally substituted by one or more substituents selected from hydroxy, oxo, halogen, cyano, nitro, carboxy, amino, mono- or di-C I-4 hydrocarbylamino, carbocyclic and heterocyclic groups having from 3 to 12 ring members and wherein one or more carbon atoms of the C 1-8 hydrocarbyl group may optionally be replaced by 0, S, SO, S0 2 , NR c , X 1 C(X 2 ), C(X 2 )X 1 or X 1 C(X 2 )X 1 ; R c is selected from hydrogen and C I-4 hydrocarbyl.; X 1 is 0, S or NR c and X 2 is =O, =S or =NR c ; and R 8 is selected from OR 11 , SR 11 and NR 12 R 13 ; R 11 is selected from optionally substituted C 1-8 hydrocarbyl and carbocyclic or heterocyclic groups having from 3 to 12 ring members; and one of R 12 and R 13 is a group R 11 and the otther of R 12 and R 13 is hydrogen or C 1-4 alkyl; or R 12 and R 13 and the nitrogen atom to which they are attached together form a saturated heterocyclic group having from 4 to 7 ring members and containing 1,2 or 3 heteroatom ring members selected from N, O and S. The compounds have activity against cyclin dependent kinases glycogen synthase kinase and Auroa kinases.
摘要翻译：本发明提供式（I）化合物或其盐，N-氧化物或其溶剂合物; 其中X是CR 5或N; A是键或 - （CH 2）m - （B）n-; B是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; m为0,1或2; n为0或1; R 1是氢，具有3至12个环成员的碳环或杂环基或任选取代的C 1-8烃基; R 2是氢，卤素，甲氧基或任选被卤素，羟基或甲氧基取代的C 1-4烃基; R 3和R 4相同或不同，各自选自氢，CN，C（O）R 8，任选取代的C 1-8烃基和具有3-12个环成员的碳环或杂环基 ; R 5为氢，R 2或R 10基团，其中R 10选自卤素，羟基，三氟甲基，氰基，硝基，羧基，氨基，单 - 或二 - 具有3-12个环成员的烃基氨基，碳环基和杂环基; 0，CO，XC（X 2），C（X 2）X，XC（X 2）X，X， S，SO，SO 2，NR c，SO 2 NR 3或NR c SO 2; 并且R b选自具有3至12个环成员的氢，碳环和杂环基，以及任选被一个或多个选自羟基，氧代，卤素，氰基，硝基，羧基，具有3至12个环成员的氨基，单或二-C 1-4烃基氨基，碳环基和杂环基，并且其中C 1-8烃基的一个或多个碳原子可任选地被0，S，SO，SO 2， X c，X 1 C（X 2），C（X 2）X 1或X 1 C（X 2）X 1; R c选自氢和C 1-4烃基。 X 1是0，S或NR c，X 2是= O，= S或= NR c; R 8选自OR 11，SR 11和NR 12 R 13; R 11选自具有3-12个环成员的任选取代的C 1-8烃基和碳环或杂环基; R 12和R 13之一是R 11基团，R 12和R 13的基团是氢或C 1-4烷基; 或R 12和R 13和它们所连接的氮原子一起形成具有4-7个环成员并含有1,2或3个选自N，O和S的杂原子环成员的饱和杂环基。该化合物具有抗细胞周期蛋白依赖性激酶糖原合酶激酶和Auroa激酶的活性。

9. 发明申请

WO2006070192A1 THIAZOLE AND ISOTHIAZOLE DERIVATIVES THAT MODULATE THE ACIVITY OF CDK, GSK AND AURORA KYNASES 审中-公开
标题翻译：调节CDK，GSK和AURORA KYNASES的活性的噻唑和异噻唑衍生物
公开(公告)号：WO2006070192A1
公开(公告)日：2006-07-06
申请号：PCT/GB2005/005089
申请日：2005-12-30
申请人： ASTEX THERAPEUTICS LIMITED , BERDINI, Valerio , O'BRIEN, Michael, Alistair , PHILLIPS, Theresa, Rachel , WYATT, Paul, Graham
发明人： BERDINI, Valerio , O'BRIEN, Michael, Alistair , PHILLIPS, Theresa, Rachel , WYATT, Paul, Graham
IPC分类号： C07D417/04 , C07D417/14 , A61K31/427 , A61P35/00
CPC分类号： C07D417/14 , C07D417/04
摘要： The invention provides a compound of the formula (I): or a salt, N-oxide, tautomer or solvate thereof, wherein X is CR 5 or N; each of Q 1 and Q 2 is a carbon atom; Q 3 is selected from S and CH; Q 4 is selected from CR 2 and S; provided that one of Q 3 and Q 4 is S and the other of Q 3 and Q 4 is not S; wherein when Q 3 is S, there is a double bond between Q 1 and Q 4 and a double bond between Q 2 and the adjacent ring nitrogen atom N; and when Q 4 is S, there is a double bond between Q 1 and Q 2 , and a double bond between Q 3 and the adjacent ring nitrogen atom N; A is a bond or -(CH 2 ) m -(B) n -; B is C=O, NR g (C=O) or O(C=O) wherein R 1 is hydrogen or C1_4 hydrocarbyl optionally substituted by hydroxy or C 1-4 alkoxy; m is 0, 1 or 2; n is 0 or 1; R ° is hydrogen or, together with NR g when present, forms a group -(CH 2 ) p - wherein p is 2 to 4; R 1 is hydrogen, a carbocyclic or heterocyclic group having from 3 to 12 ring members, or an optionally substituted C 1-8 hydrocarbyl group; R 2 is hydrogen, halogen, methoxy, or a C 1-4 hydrocarbyl group optionally substituted by halogen, hydroxyl or methoxy; R 3 and R 4 together with the carbon atoms to which they are attached form an optionally substituted fused carbocyclic or heterocyclic ring having from 5 to 7 ring members of which up to 3 can be heteroatoms selected from N, 0 and S; and R 5 is hydrogen, a group R 2 or a group R 10 wherein R 10 is as defined in the claims.The compounds have activity as inhibitors of cyclin dependent kinases, glycogen synthase kinases and Aurora kinases.
摘要翻译：本发明提供式（I）化合物或其盐，N-氧化物，互变异构体或溶剂合物，其中X为CR 5或N; Q 1和Q 2中的每一个是碳原子; Q 3和S 3选自S和CH; Q ^{4 选自CR 2和S; 只要Q 3和Q 4中的一个是S，Q 3和Q 4中的另一个不是 S; 其中当Q 3是S时，在Q 1和Q 2之间存在双键， / SUP>和相邻环氮原子N; 并且当Q 4是S时，Q 1和Q 2之间存在双键，并且Q 3 相邻环氮原子N; A是键或 - （CH 2）m - （B）n - B为C = O，NR（C = O）或O（C = O），其中R 1为氢或任选被羟基取代的C 1-4烃基或C}

10. 发明申请

WO2007129066A1 4- (2, E-DICHLORO-BENZOYLAMINO) -1H-PYRAZOLE-S-CARBOXYLIC ACID (1-METHANESULPH0NYL-PIPERIDIN-4-YL) -AMIDE FOR THE TREATMENT OF CANCER 审中-公开
标题翻译：用于治疗癌症的4-（2，E-二氯苯甲酰氨基）-1H-吡唑-S-羧酸（1-甲磺酰基 - 哌啶-4-基）酰胺
公开(公告)号：WO2007129066A1
公开(公告)日：2007-11-15
申请号：PCT/GB2007/001655
申请日：2007-05-04
申请人： ASTEX THERAPEUTICS LIMITED , TREWARTHA, Gary , NAVARRO, Eva, Figueroa , REES, David, Charles , VINKOVIC, Mladen , WOODHEAD, Andrew, James , WYATT, Paul, Graham
发明人： TREWARTHA, Gary , NAVARRO, Eva, Figueroa , REES, David, Charles , VINKOVIC, Mladen , WOODHEAD, Andrew, James , WYATT, Paul, Graham
IPC分类号： C07D401/12 , A61K31/4155 , A61P35/00
CPC分类号： C07D401/12
摘要： The invention provides the compound of formula (I) 4-(2,6-dichloro-benzoylamino)-1H-pyrazole- 3-carboxylic acid (l-methanesulphonyl-piperidin-4-yl)-amide in a substantially crystalline form, therapeutic uses thereof and pharmaceutical compositions containing the crystalline compound. The invention also provides novel pharmaceutical formulations containing 4-(2,6-dichloro-benzoylamino)-1H-pyrazole-3-carboxylic acid (1-methanesulphonyl-piperidin-4-yl)-amide and novel processes for preparing the compound.
摘要翻译：本发明提供基本上为结晶形式的式（I）4-（2,6-二氯 - 苯甲酰氨基）-1H-吡唑-3-羧酸（1-甲磺酰基 - 哌啶-4-基） - 酰胺的化合物，其为治疗其用途和含有结晶化合物的药物组合物。本发明还提供含有4-（2,6-二氯 - 苯甲酰基氨基）-1H-吡唑-3-羧酸（1-甲磺酰基 - 哌啶-4-基） - 酰胺的新型药物制剂及其制备方法。

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