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1. 发明申请

WO2010119284A1 BICYCLIC HETEROCYCLYL DERIVATIVES AS FGFR KINASE INHIBITORS FOR THERAPEUTIC USE 审中-公开
标题翻译：作为用于治疗用途的FGFR激酶抑制剂的双相间苯二酚衍生物
公开(公告)号：WO2010119284A1
公开(公告)日：2010-10-21
申请号：PCT/GB2010/050617
申请日：2010-04-15
申请人： ASTEX THERAPEUTICS LIMITED , SAXTY, Gordon , BERDINI, Valerio , FREYNE, Eddy Jean Edgard , PAPANIKOS, Alexandra , BENDERITTER, Pascal , EMBRECHTS, Werner Constant Johan , WROBLOWSKI, Berthold , AKKARI, Rhalid
发明人： SAXTY, Gordon , BERDINI, Valerio , FREYNE, Eddy Jean Edgard , PAPANIKOS, Alexandra , BENDERITTER, Pascal , EMBRECHTS, Werner Constant Johan , WROBLOWSKI, Berthold , AKKARI, Rhalid
IPC分类号： C07D471/04 , A61P35/00 , A61K31/437
CPC分类号： C07D471/04
摘要： The invention relates to new bicyclic heterocyclyl derivatives of formula (I), 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：本发明涉及式（I）的新的双环杂环基衍生物，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，例如，癌症。

2. 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。

3. 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。

4. 发明申请

WO2006051290A2 PHARMACEUTICAL COMPOUNDS 审中-公开
标题翻译：药物化合物
公开(公告)号：WO2006051290A2
公开(公告)日：2006-05-18
申请号：PCT/GB2005/004323
申请日：2005-11-09
申请人： ASTEX THERAPEUTICS LIMITED , THE INSTITUTE OF CANCER RESEARCH:ROYAL CANCER HOSPITAL , CANCER RESEARCH TECHNOLOGY LIMITED , BERDINI, Valerio , BOYLE, Robert, George , SAXTY, Gordon , VERDONK, Marinus, Leendert , WOODHEAD, Steven, John , WYATT, Paul, Graham , SORE, Hannah, Fiona , WALKER, David, Winter , CALDWELL, John , COLLINS, Ian
发明人： BERDINI, Valerio , BOYLE, Robert, George , SAXTY, Gordon , VERDONK, Marinus, Leendert , WOODHEAD, Steven, John , WYATT, Paul, Graham , SORE, Hannah, Fiona , WALKER, David, Winter , CALDWELL, John , COLLINS, Ian
IPC分类号： A61K31/505 , A61P35/00 , C07D239/88 , C07D401/12 , C07D401/04 , C07D401/06 , C07D403/12
CPC分类号： C07D403/12 , A61K31/505 , C07D239/88 , C07D239/91 , C07D239/96 , C07D401/04 , C07D401/06 , C07D401/12 , C07D403/04
摘要： The invention provides a compound of the formula (I) or a salt, solvate, tautomer or N-oxide thereof for use in the treatment or prophylaxis of a disease state or condition mediated by protein kinase A and/or protein kinase B, wherein the ring Q is a benzene ring; J 2 -J 1 is N=CR 7 or R 1a N-CO; G is OH or NR 5 R 6 ; E is CONR 7 , NR 7 CO, C(R 8 )=C(R 8 ) or (X) m (CR 8 R 8a ) n where X is O, S or NR 7 ; provided that when J 2 -J 1 is R 1a N-CO, E is other than NR 7 CO; m and n are each 0 or 1, where m + n = 1 or 2; A is a bond and R 4 and R 4a are absent, or A is a saturated optionally substituted C 1-7 hydrocarbon linker group having a maximum chain length of 5 atoms extending between E and G, one carbon atom in the linker group A being optionally replaced by O or N; R 1 , R la , R 2 , and R 3 are each H; halogen; C 1-6 hydrocarbyl optionally substituted by halogen, OH or C 1-2 alkoxy; CN; CONHR 8 ; NH 2 ; NHCOR 10 or NHCONHR 10 ; R 4 is H or C 1-4 alkyl; R 4a is H, C 1-4 alkyl or a group R 9 ; R 5 and R 6 are each selected from H, R 9 and C 1-4 hydrocarbyl optionally substituted by halogen, C 1-2 alkoxy or R 9 ;or NR 5 R 6 forms a saturated 4-7 membered monocyclic heterocyclic group; R 7 is H or C 1-4 alkyl; R 8 and R 8a each H or saturated C 1-4 hydrocarbyl optionally substituted by fluorine; R 9 is a monocyclic or bicyclic carbocyclic or heterocyclic group containing up to 3 ring heteroatoms selected from N, O and S; or R 4 , R 4a and A together form a saturated monocyclic 4-7 membered heterocycle; or NR 5 R 6 , R 4 and A form a saturated 4-7 membered monocyclic heterocycle; or R 4 , together with R 7 or R 8 and A and E form a 4-7 membered saturated monocyclic heterocycle; or NR 5 R 6 and R 7 or R 8 together with A and E form a 4-7 membered saturated monocyclic heterocycle; and R 10 is optionally substituted phenyl or benzyl.
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，用于治疗或预防由蛋白激酶A和/或蛋白激酶B介导的疾病状态或病症，其中环Q是苯环; N 2是N = CR 7或R 1a N-CO; G是OH或NR 5 R 6; E是CONR 7，NR 7 CO，C（R 8）= C（R 8）或（R 8）其中X是O，S或NR 7（其中X是O，S或NR 7）其中X是O，S或NR 7 ; 条件是当J 2是-J 1，R 1是N-CO时，E不是NR 7 CO ; m和n各自为0或1，其中m + n = 1或2; A是键，R 4和R 4a不存在，或A是饱和的任选取代的C 1-7烃连接基团，其具有在E和G之间延伸的5个原子的最大链长度，连接基团A中的一个碳原子任选地被O或N取代; R 1，R 2，R 2，R 3和R 3各自为H; 卤素; 任选被卤素，OH或C 1-12烷氧基取代的C 1-6烷基; CN; CONHR ^{8 ; NH _{2 ; NHCOR 10或NHCONHR 10; R 4是H或C 1-4烷基; R 4a是H，C 1-4烷基或基团R 9; R 5和R 6各自选自H，R 9和C 1-4烃基，任选被卤素，C 1-2烷氧基或R 9或NR 5 R 6形成饱和的4-7 元环杂环基; R 7是H或C 1-4烷基; 每个H或任选被氟取代的饱和C 1-4烃基的R 8和R 8 8a; R 9是含有至多3个选自N，O和S的环杂原子的单环或双环碳环或杂环基; 或R 4，R 4a和A一起形成饱和单环4-7元杂环; 或NR 5 R 6，R 4和A形成饱和的4-7元单环杂环; 或R 4，...，以及R 7或R 8，A和E形成4-7元饱和单环杂环; 或NR 5 R 6和R 7或R 8与A和E一起形成4-7元环饱和单环杂环; R 10是任选取代的苯基或苄基。}}

5. 发明申请

WO2005002576A8 IMIDAZOLE DERIVATIVES AND THEIR USE AS PROTEIN KINASES INHIBITORS 审中-公开
标题翻译：咪唑衍生物及其作为蛋白激酶抑制剂的用途
公开(公告)号：WO2005002576A8
公开(公告)日：2005-09-22
申请号：PCT/GB2004002913
申请日：2004-07-05
申请人： ASTEX THERAPEUTICS 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。该化合物具有针对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。

6. 发明申请

WO2009150240A1 IMIDAZOPYRIDINE DERIVATIVES AS INHIBITORS OF RECEPTOR TYROSINE KINASES 审中-公开
标题翻译：作为受体酪氨酸激酶抑制剂的咪唑吡啶衍生物
公开(公告)号：WO2009150240A1
公开(公告)日：2009-12-17
申请号：PCT/EP2009/057318
申请日：2009-06-12
申请人： ASTEX THERAPEUTICS LIMITED , BERDINI, Valerio , CARR, Maria, Grazia , CONGREVE, Miles, Stuart , FREDERICKSON, Martyn , GRIFFITHS-JONES, Charlotte, Mary , HAMLETT, Christopher, Charles, Frederick , MADIN, Andrew , MURRAY, Christopher, William , BENNING, Rajdeep Kaur , SAXTY, Gordon , VICKERSTAFFE, Emma , WOODHEAD, Andrew, James , WOODHEAD, Steven, John , FREYNE, Eddy, Jean, Edgard , GOVAERTS, Tom, Cornelis, Hortense , ANGIBAUD, Patrick, René , ASTEX THERAPEUTICS LIMITED
发明人： BERDINI, Valerio , CARR, Maria, Grazia , CONGREVE, Miles, Stuart , FREDERICKSON, Martyn , GRIFFITHS-JONES, Charlotte, Mary , HAMLETT, Christopher, Charles, Frederick , MADIN, Andrew , MURRAY, Christopher, William , BENNING, Rajdeep Kaur , SAXTY, Gordon , VICKERSTAFFE, Emma , WOODHEAD, Andrew, James , WOODHEAD, Steven, John , FREYNE, Eddy, Jean, Edgard , GOVAERTS, Tom, Cornelis, Hortense , ANGIBAUD, Patrick, René
IPC分类号： C07D471/04 , C07D513/04 , A61P35/00 , A61K31/437 , A61K31/506 , A61K31/501 , A61K31/53 , A61K31/444 , A61K31/497 , A61K31/496 , A61K31/4545
CPC分类号： C07D471/04 , C07D513/04
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。

7. 发明申请

WO2009047522A1 BICYCLIC HETEROCYCLIC COMPOUNDS AS PROTEIN TYROSINE KINASE INHIBITORS 审中-公开
标题翻译：作为蛋白酪氨酸激酶抑制剂的双相杂环化合物
公开(公告)号：WO2009047522A1
公开(公告)日：2009-04-16
申请号：PCT/GB2008/003439
申请日：2008-10-10
申请人： ASTEX THERAPEUTICS LIMITED , SAXTY, Gordon , BERDINI, Valerio , MURRAY, Christopher, William , GRIFFITHS-JONES, Charlotte, Mary , VICKERSTAFFE, Emma , BESONG, Gilbert, Ebai
发明人： SAXTY, Gordon , BERDINI, Valerio , MURRAY, Christopher, William , GRIFFITHS-JONES, Charlotte, Mary , VICKERSTAFFE, Emma , BESONG, Gilbert, Ebai
IPC分类号： C07D471/04 , C07D487/04 , A61P35/00 , A61K31/437
CPC分类号： C07D471/04
摘要： The invention relates to new bicyclic heterocyclic derivative compounds of formula (I): wherein R 1 , q, A, B, X 1 , X 2 , X 3 , X 4 , X 5 and R 2 are as defined herein, 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：本发明涉及式（I）的新的双环杂环衍生物化合物：其中R1，q，A，B，X1，X2，X3，X4，X5和R2如本文所定义，包含所述化合物的药物组合物和使用的所述化合物治疗疾病，例如癌症。

8. 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。

9. 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

10. 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。

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