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1. 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。

2. 发明申请

WO2008078100A2 NEW COMPOUNDS 审中-公开
标题翻译：新化合物
公开(公告)号：WO2008078100A2
公开(公告)日：2008-07-03
申请号：PCT/GB2007/004960
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 , A61P35/00
CPC分类号： C07D471/04 , C07D487/04
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。

3. 发明申请

WO2009047506A1 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：WO2009047506A1
公开(公告)日：2009-04-16
申请号：PCT/GB2008/003418
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 , CARR, Maria, Grazia
发明人： SAXTY, Gordon , BERDINI, Valerio , MURRAY, Christopher, William , GRIFFITHS-JONES, Charlotte, Mary , VICKERSTAFFE, Emma , BESONG, Gilbert, Ebai , CARR, Maria, Grazia
IPC分类号： C07D471/04 , C07D487/04 , A61P35/00 , A61K31/437
CPC分类号： C07D471/04 , C07D487/04
摘要： The invention relates to new bicyclic heterocyclic derivative compounds of formula (I): wherein R 1 , A, 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，A，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所述化合物在疾病的治疗，例如癌症。

4. 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。

5. 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。

6. 发明申请

WO2012073017A1 SUBSTITUTED BENZOPYRAZIN DERIVATIVES AS FGFR KINASE INHIBITORS FOR THE TREATMENT OF CANCER DISEASES 审中-公开
标题翻译：作为FGFR激酶抑制剂治疗癌症疾病的替代苯并噻嗪衍生物
公开(公告)号：WO2012073017A1
公开(公告)日：2012-06-07
申请号：PCT/GB2011/052356
申请日：2011-11-29
申请人： ASTEX THERAPEUTICS LIMITED , SAXTY, Gordon , MURRAY, Christopher William , BERDINI, Valerio , BESONG, Gilbert Ebai , HAMLETT, Christopher Charles Frederick , WOODHEAD, Steven John , LIGNY, Yannick Aimé Eddy , ANGIBAUD, Patrick René
发明人： SAXTY, Gordon , MURRAY, Christopher William , BERDINI, Valerio , BESONG, Gilbert Ebai , HAMLETT, Christopher Charles Frederick , WOODHEAD, Steven John , LIGNY, Yannick Aimé Eddy , ANGIBAUD, Patrick René
IPC分类号： C07D403/04 , A61K31/502 , A61P35/00
CPC分类号： C07D403/04 , C07D401/14 , C07D403/14
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。

8. 发明申请

WO2010119285A1 IMIDAZO [1,2-A]PYRIDINE DERIVATIVES AS FGFR KINASE INHIBITORS FOR USE IN THERAPY 审中-公开
标题翻译：作为用于治疗的FGFR激酶抑制剂的咪唑并[1,2-A]吡啶衍生物
公开(公告)号：WO2010119285A1
公开(公告)日：2010-10-21
申请号：PCT/GB2010/050618
申请日：2010-04-15
申请人： ASTEX THERAPEUTICS LIMITED , SAXTY, Gordon , BERDINI, Valerio , MURRAY, Christopher William , FREYNE, Eddy Jean Edgard , LIGNY, Yannick Aimé Eddy , BONNET, Pascal Ghislain André , WROBLOWSKI, Berthold , PAPANIKOS, Alexandra
发明人： SAXTY, Gordon , BERDINI, Valerio , MURRAY, Christopher William , FREYNE, Eddy Jean Edgard , LIGNY, Yannick Aimé Eddy , BONNET, Pascal Ghislain André , WROBLOWSKI, Berthold , PAPANIKOS, Alexandra
IPC分类号： C07D471/04 , A61K31/437 , A61P35/00
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。

9. 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。

10. 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。}}

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