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1. 发明申请

WO2006123165A2 PHARMACEUTICAL COMPOUNDS 审中-公开
标题翻译：药物化合物
公开(公告)号：WO2006123165A2
公开(公告)日：2006-11-23
申请号：PCT/GB2006/001851
申请日：2006-05-19
申请人： ASTEX THERAPEUTICS LIMITED , CHESSARI, Gianni , CONGREVE, Miles, Stuart , CALLAGHAN, Owen , COWAN, Suzanna, Ruth , MURRAY, Christopher, William , WOOLFORD, Alison, Jo-Anne , O'BRIEN, Michael, Alistair , WOODHEAD, Andrew, James
发明人： CHESSARI, Gianni , CONGREVE, Miles, Stuart , CALLAGHAN, Owen , COWAN, Suzanna, Ruth , MURRAY, Christopher, William , WOOLFORD, Alison, Jo-Anne , O'BRIEN, Michael, Alistair , WOODHEAD, Andrew, James
CPC分类号： C07D413/04 , C07D239/42 , C07D239/47 , C07D239/48 , C07D401/04 , C07D401/10 , C07D401/12 , C07D403/04 , C07D409/04
摘要： The invention provides a compound for use as an inhibitor of Hsp90, the compound having the formula (I): or salts, tautomers, solvates or N-oxides thereof; wherein: A is N or a group CR 3 ; R 1 is a monocyclic or bicyclic carbocyclic or heterocyclic ring of 5 to 10 ring members of which up to two ring members may be heteroatoms selected from N, O and S and the remainder are carbon atoms, the carbocyclic or heterocyclic ring being optionally substituted by one or more substituent groups independently selected from R 10 ; and R 2 , R 3 and R 10 are as defined in the claims.
摘要翻译：本发明提供了用作Hsp90抑制剂的化合物，具有式（I）的化合物：或其盐，互变异构体，溶剂合物或N-氧化物; 其中：A为N或基团CR 3; R 1是5至10个环成员的单环或双环碳环或杂环，其中多至两个环成员可以是选自N，O和S的杂原子，其余是碳原子，碳环或杂环任选被一个或多个独立地选自R 10的取代基取代; R 2，R 3和R 10如权利要求中所定义。

2. 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。

3. 发明申请

WO2006008545A3 THIAZOLE AND ISOTHIAZOLE DERIVATIVES AS PROTEIN KINASE INHIBITORS 审中-公开
标题翻译：作为蛋白激酶抑制剂的噻唑和异噻唑衍生物
公开(公告)号：WO2006008545A3
公开(公告)日：2006-03-30
申请号：PCT/GB2005002888
申请日：2005-07-22
申请人： ASTEX THERAPEUTICS LTD , BERDINI VALERIO , EARLY THERESA RACHAEL , O'BRIEN MICHAEL ALISTAIR , WOODHEAD ANDREW JAMES , WYATT PAUL GRAHAM
发明人： BERDINI VALERIO , EARLY THERESA RACHAEL , O'BRIEN MICHAEL ALISTAIR , WOODHEAD ANDREW JAMES , WYATT PAUL GRAHAM
IPC分类号： C07D417/12 , A61K31/425 , A61K31/426 , A61K31/427 , C07D275/02 , C07D277/56 , C07D417/14
CPC分类号： C07D275/03 , C07D277/56 , C07D417/12 , C07D417/14
摘要： The invention provides a compound for use in the prophylaxis or treatment of a disease state or condition mediated by a cyclin dependent kinase, the compound having the formula (I): (I) and salts, tautomers, N-oxides or solvates thereof; wherein A is a bond, C=O, NR
摘要翻译：本发明提供一种用于预防或治疗由细胞周期蛋白依赖性激酶介导的疾病状态或病症的化合物，具有式（I）：（I）的化合物及其盐，互变异构体，N-氧化物或溶剂合物; 其中A是键，C = O，NR

4. 发明申请

WO2005012256A8 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-吡唑类化合物及其作为依赖于细胞周期蛋白依赖性激酶（CDK）和糖原合成酶激酶-3（GSK-3）调节剂的用途
公开(公告)号：WO2005012256A8
公开(公告)日：2005-04-07
申请号：PCT/GB2004003179
申请日：2004-07-22
申请人： ASTEX TECHNOLOGY LTD , BERDINI VALERIO , O'BRIEN MICHAEL ALISTAIR , CARR MARIA GRAZIA , EARLY THERESA RACHEL , 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 , GILL ADRIAN LIAM , TREWARTHA GARY , WOOLFORD ALISON JO-ANNE , WOODHEAD ANDREW JAMES , WYATT PAUL GRAHAM
IPC分类号： A61P25/28 , A61P31/10 , A61P31/12 , A61P35/00 , A61P37/00 , C07D231/14 , C07D231/38 , 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 , A61K31/4155 , C07D231/42
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 -A-NR - or a 5- or 6-membered carbocyclic or heterocyclic ring; A is a bond, S02, C=O, NR (C=O) or O(C=O) wherein R 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; R 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 0, S, NH, SO, S02; R 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); R is selected from hydrogen and carbocyclic and heterocyclic groups having from 3 to 12 ring members; and R 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：本发明提供了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）的式（0）化合物或其盐或互变异构体或N-氧化物或溶剂化物。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烃基氨基和具有3至4个碳原子的杂环基团取代的取代基取代的C 1-8烃基 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的原子或基团替代; R 2是氢; 卤素; C 1-4烷氧基（例如甲氧基）; 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选自氢和具有3至12个环成员的碳环和杂环基团; 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

WO2008078091A1 BICYCLIC HETEROCYCLIC COMPOUNDS AS FGFR INHIBITORS 审中-公开
标题翻译：作为FGFR抑制剂的双相杂环化合物
公开(公告)号：WO2008078091A1
公开(公告)日：2008-07-03
申请号：PCT/GB2007/004934
申请日：2007-12-21
申请人： ASTEX THERAPEUTICS LIMITED , BERDINI, Valerio , BESONG, Gilbert, Ebai , CALLAGHAN, Owen , CARR, Maria, Grazia , CONGREVE, Miles, Stuart , GILL, Adrian, Liam , GRIFFITHS-JONES, Charlotte, Mary , MADIN, Andrew , MURRAY, Christopher, William , NIJJAR, Rajdeep, Kaur , O'BRIEN, Michael, Alistair , PIKE, Andrew , SAXTY, Gordon , TAYLOR, Richard, David , VICKERSTAFFE, Emma
发明人： BERDINI, Valerio , BESONG, Gilbert, Ebai , CALLAGHAN, Owen , CARR, Maria, Grazia , CONGREVE, Miles, Stuart , GILL, Adrian, Liam , GRIFFITHS-JONES, Charlotte, Mary , MADIN, Andrew , MURRAY, Christopher, William , NIJJAR, Rajdeep, Kaur , O'BRIEN, Michael, Alistair , PIKE, Andrew , SAXTY, Gordon , TAYLOR, Richard, David , VICKERSTAFFE, Emma
IPC分类号： C07D471/04 , C07D487/04 , A61K31/437 , A61K31/519 , A61P35/00
CPC分类号： C07D487/04 , A61K31/437 , C07D471/04
摘要： The invention relates to new bicyclic heterocyclic derivative compounds, to pharmaceutical compositions comprising said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.
摘要翻译：本发明涉及新的双环杂环衍生物化合物，包含所述化合物的药物组合物和所述化合物在治疗疾病中的用途。癌症。

6. 发明申请

WO2006008545A2 PHARMACEUTICAL COMPOUNDS 审中-公开
标题翻译：药物化合物
公开(公告)号：WO2006008545A2
公开(公告)日：2006-01-26
申请号：PCT/GB2005/002888
申请日：2005-07-22
申请人： ASTEX THERAPEUTICS LIMITED , BERDINI, Valerio , EARLY, Theresa, Rachael , O'BRIEN, Michael, Alistair , WOODHEAD, Andrew, James , WYATT, Paul, Graham
发明人： BERDINI, Valerio , EARLY, Theresa, Rachael , O'BRIEN, Michael, Alistair , WOODHEAD, Andrew, James , WYATT, Paul, Graham
IPC分类号： A61K31/00
CPC分类号： C07D275/03 , C07D277/56 , C07D417/12 , C07D417/14
摘要： The invention provides a compound for use in the prophylaxis or treatment of a disease state or condition mediated by a cyclin dependent kinase, the compound having the formula (I): (I) and salts, tautomers, N-oxides or solvates thereof; wherein A is a bond, 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; Q is S or CR 2 ; J is S or CH; provided that one of Q and J is S, and the other of Q and J is not S; when Q is S, there is a double bond between the ring carbon atoms “a” and “b” and a double bond between the ring nitrogen N and J; and when J is S, there is a double bond between Q and the ring carbon atom “a” and a double bond between the ring nitrogen N and the ring carbon atom “b”; and R 1 to R 4 are as defined in the claims.
摘要翻译：本发明提供一种用于预防或治疗由细胞周期蛋白依赖性激酶介导的疾病状态或病症的化合物，具有式（I）：（I）的化合物及其盐，互变异构体，N-氧化物或溶剂合物; 其中A是键，C = O，NR（C = O）或O（C = O），其中R g是氢或C 1〜任选被羟基或C 1-4烷氧基取代的烃基; Y是长度为1,2或3个碳原子的键或亚烷基链; Q是S或CR <2>; J为S或CH; 假设Q和J中的一个是S，Q和J中的另一个不是S; 当Q是S时，环碳原子“a”和“b”之间有双键，环氮N与J之间有双键; 当J为S时，Q与环碳原子“a”之间存在双键，环氮N与环碳原子“b”之间具有双键。和R 1至R 4如权利要求中所定义。

7. 发明申请

WO2005002576A3 BENZIMIDAZOLE DERIVATIVES AND THEIR USE AS ROTEIN KINASES INHIBITORS 审中-公开
标题翻译：苯并咪唑衍生物及其作为罗茨金杀伤剂的用途
公开(公告)号：WO2005002576A3
公开(公告)日：2005-06-16
申请号：PCT/GB2004002913
申请日：2004-07-05
申请人： ASTEX TECHNOLOGY LTD , 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： A61K31/00 , A61K31/4184 , A61P31/10 , A61P35/00 , C07D403/04
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. 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。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。

8. 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。

9. 发明申请

WO2008044027A2 PHARMACEUTICAL COMPOUNDS 审中-公开
标题翻译：药物化合物
公开(公告)号：WO2008044027A2
公开(公告)日：2008-04-17
申请号：PCT/GB2007/003860
申请日：2007-10-12
申请人： ASTEX THERAPEUTICS LIMITED , CONGREVE, Miles Stuart , FAZAL, Lyndsey Helen , FREDERICKSON, Martyn , MURRAY, Christopher William , O'BRIEN, Michael Alistair , WOODHEAD, Andrew James , LYONS, John, Francis , THOMPSON, Neil Thomas
发明人： CONGREVE, Miles Stuart , FAZAL, Lyndsey Helen , FREDERICKSON, Martyn , MURRAY, Christopher William , O'BRIEN, Michael Alistair , WOODHEAD, Andrew James , LYONS, John, Francis , THOMPSON, Neil Thomas
CPC分类号： C07D403/06 , C07D209/08 , C07D209/44 , C07D215/08 , C07D215/14 , C07D217/06 , C07D401/04 , C07D401/12 , C07D401/14 , C07D471/04 , C07D471/08 , C07D471/10 , C07D491/08 , C07D491/10 , C07D491/107 , C07D491/18
摘要： The invention provides a compound for use in medicine, the compound being a compound of the formula (Vl 0 ) or a salt, solvate, tautomer or N-oxide thereof: wherein the bicyclic group: is selected from the structures C1, C5 and C6: wherein n is 0, 1, 2 or 3; R 1 : is„ hydrogen, hydroxy, or O-R z; R 2a is hydroxy, methoxy or O-R z; provided that at least one of R 1 and R 2a is O-R z; R z is L p -R p1 ; SO 3 H; a glucuronide residue; a mono-, di- or tripeptide residue; or; L p is a bond, C=O, (C=O)O, (C=O)NR p1 or S(O) x NR p1 ; x is 1 or 2; R p1 is hydrogen or a an optionally substituted C 1-25 hydrocarbyl group containing 0, 1 or 2 carbocyclic rings and 0, 1, 2, 3, 4, 5 or 6 carbon-carbon multiple bonds, provided that R p1 is not hydrogen when L p is a bond, C=O or (C=O)O; and provided also that O-R z does not contain an 0-0 moiety; and excluding compounds wherein R1 is hydroxy and R2a is methoxy; Rp2 and Rp3 are the same or different and each is a group R p1; and R 3 , R 4a , R 8 and R 10 are defined in the claims. The compounds of formula (Vl0) are pro-drugs of parent compounds wherein R 1 and/or R 2a are hydroxy, wherein the parent compounds have Hsp90 inhibiting activity.
摘要翻译：本发明提供了一种用于医药的化合物，该化合物为下式化合物：其盐，溶剂化物，互变异构体或N-氧化物：其中双环基团选自：结构C1，C5和C6：其中n为0,1,2或3; R 1是氢，羟基或OR z; R 2是羟基，甲氧基或OR z; O / O >条件是R 1和R 2 2中的至少一个是OR z; R z是L SUP > p p> SO 3 H;葡糖苷酸残基;单 - ，二 - 或三肽残基;或●L < / SUP>是键，C = O，（C = O）O，（C = O）NR P1或S（O）x NR 6 x为1或2; R p1为氢或任选取代的含0,1或2个碳环的C 1-25烃基和0 ，1,2,3,4,5或6个碳 - 碳多重键，条件是当P = O时，R p2不是氢，C = O或（C = O）O;并且也提供OR 0不含0-0部分;并且不包括其中R 1是羟基并且R 2a是甲氧基的化合物; Rp2和Rp3相同或不同，每个是基团R p1; R 3和R 3，R 4a，R 8和R 10 是定义在权利要求中。式（V10）化合物是其中R 1和/或R 2a的羟基的母体化合物的前体药物，其中母体化合物具有Hsp90抑制活性。

10. 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}

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