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21. 发明授权

US08691806B2 Pyrazole derivatives as protein kinase modulators 失效
标题翻译：吡唑衍生物作为蛋白激酶调节剂
公开(公告)号：US08691806B2
公开(公告)日：2014-04-08
申请号：US13536174
申请日：2012-06-28
申请人： Valerio Berdini , Gordon Saxty , Marinus Leendert Verdonk , Steven John Woodhead , Paul Graham Wyatt , Robert George Boyle , Hannah Fiona Sore , David Winter Walker , Ian Collins , Robert Downham , Robin Arthur Ellis Carr
发明人： Valerio Berdini , Gordon Saxty , Marinus Leendert Verdonk , Steven John Woodhead , Paul Graham Wyatt , Robert George Boyle , Hannah Fiona Sore , David Winter Walker , Ian Collins , Robert Downham , Robin Arthur Ellis Carr
IPC分类号： A61K31/397 , C07D231/12
CPC分类号： A61K31/415 , A61K9/0019 , A61K9/20 , A61K9/48 , A61K31/4155 , A61K31/4178 , A61K31/4439 , A61K31/454 , A61K31/4545 , A61K31/496 , A61K31/497 , A61K31/5377 , A61K31/551 , A61K45/06 , C07D231/12 , C07D401/04 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/10 , C07D403/12 , C07D405/04 , C07D413/10
摘要： The invention provides compounds of the formula (I) having protein kinase B inhibiting activity: Also provided are pharmaceutical compositions containing the compounds, methods for preparing the compounds and their use as anticancer agents.
摘要翻译：本发明提供具有蛋白激酶B抑制活性的式（I）化合物：还提供含有化合物的药物组合物，制备化合物的方法及其作为抗癌剂的用途。

22. 发明授权

US08546407B2 Ortho-condensed pyridine and pyrimidine derivatives (e.g., purines) as protein kinases inhibitors 有权
标题翻译：正构缩合的吡啶和嘧啶衍生物（如嘌呤）作为蛋白激酶抑制剂
公开(公告)号：US08546407B2
公开(公告)日：2013-10-01
申请号：US11577963
申请日：2005-10-25
申请人： Valerio Berdini , Robert George Boyle , Gordon Saxty , David Winter Walker , Steven John Woodhead , Paul Graham Wyatt , Alastair Donald , John Caldwell , Ian Collins , Tatiana Faria Da Fonseca
发明人： Valerio Berdini , Robert George Boyle , Gordon Saxty , David Winter Walker , Steven John Woodhead , Paul Graham Wyatt , Alastair Donald , John Caldwell , Ian Collins , Tatiana Faria Da Fonseca
IPC分类号： C07D487/04 , A61K31/519 , A61P35/00
CPC分类号： C07D471/04 , A61K31/4545 , A61K31/519 , A61K31/52 , A61K31/522 , C07D473/34 , C07D487/04
摘要： The invention provides a compound for use as a protein kinase B inhibitor, the compound being a compound of the formula (Ic) or salts, tautomers or N-oxides thereof.
摘要翻译：本发明提供了用作蛋白激酶B抑制剂的化合物，该化合物是式（Ic）化合物或其盐，互变异构体或N-氧化物。

23. 发明授权

US08247576B2 Pyrazole derivatives as protein kinase modulators 有权
标题翻译：吡唑衍生物作为蛋白激酶调节剂
公开(公告)号：US08247576B2
公开(公告)日：2012-08-21
申请号：US10596788
申请日：2004-12-23
申请人： Valerio Berdini , Gordon Saxty , Marinus Leendert Verdonk , Steven John Woodhead , Paul Graham Wyatt , Robert George Boyle , Hannah Fiona Sore , David Winter Walker , Ian Collins , Robert Downham , Robin Arthur Ellis Carr
发明人： Valerio Berdini , Gordon Saxty , Marinus Leendert Verdonk , Steven John Woodhead , Paul Graham Wyatt , Robert George Boyle , Hannah Fiona Sore , David Winter Walker , Ian Collins , Robert Downham , Robin Arthur Ellis Carr
IPC分类号： C07D231/12
CPC分类号： A61K31/415 , A61K9/0019 , A61K9/20 , A61K9/48 , A61K31/4155 , A61K31/4178 , A61K31/4439 , A61K31/454 , A61K31/4545 , A61K31/496 , A61K31/497 , A61K31/5377 , A61K31/551 , A61K45/06 , C07D231/12 , C07D401/04 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/10 , C07D403/12 , C07D405/04 , C07D413/10
摘要： The invention provides compounds of the formula: (I) having protein kinase B inhibiting activity: wherein A is a saturated hydrocarbon linker group containing from 1 to 7 carbon atoms, the linker group having a maximum chain length of 5 atoms extending between R1 and NR2R3 and a maximum chain length of 4 atoms extending between E and NR2R3, wherein one of the carbon atoms in the linker group may optionally be replaced by an oxygen or nitrogen atom; and wherein the carbon atoms of the linker group A may optionally bear one or more substituents selected from oxo, fluorine and hydroxy, provided that the hydroxy group when present is not located at a carbon atom a with respect to the NR2R3 group and provided that the oxo group when present is located at a carbon atom a with respect to the NR2R3 group; E is a monocyclic or bicyclic carbocyclic or heterocyclic group; R1 is an aryl or heteroaryl group; and R2, R3, R4 and R5 are as defined in the claims. Also provided are pharmaceutical compositions containing the compounds, methods for preparing the compounds and their use as anticancer agents.
摘要翻译：本发明提供下式的化合物：（I）具有蛋白激酶B抑制活性：其中A是含有1至7个碳原子的饱和烃连接基团，连接基团在R1和NR2R3之间延伸的最大链长为5个原子并且在E和NR2R3之间延伸的4个原子的最大链长度，其中连接基团中的一个碳原子可以任选地被氧或氮原子替代; 并且其中连接基团A的碳原子可以任选地具有一个或多个选自氧代，氟和羟基的取代基，条件是当存在的羟基不相对于NR 2 R 3基团位于碳原子a时，存在时的氧代基相对于NR 2 R 3基团位于碳原子a; E是单环或双环碳环或杂环基; R1是芳基或杂芳基; 并且R 2，R 3，R 4和R 5如权利要求中所定义。还提供含有化合物的药物组合物，制备化合物的方法及其作为抗癌剂的用途。

24. 发明授权

US08110573B2 Pyrazole compounds that modulate the activity of CDK, GSK and aurora kinases 失效
标题翻译：调节CDK，GSK和极光激酶活性的吡唑化合物
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。

25. 发明申请

US20090247538A1 Ortho-Condensed Pyridine and Pyrimidine Derivatives (e.g., Purines) as Protein Kinases Inhibitors 有权
标题翻译：正电子缩合吡啶和嘧啶衍生物（如嘌呤）作为蛋白激酶抑制剂
公开(公告)号：US20090247538A1
公开(公告)日：2009-10-01
申请号：US11577963
申请日：2005-10-25
申请人： Valerio Berdini , Robert George Boyle , Gordon Saxty , David Winter Walker , Steven John Woodhead , Paul Graham Wyatt , Alastair Donald , John Caldwell , Ian Collins , Tatiana Faria Da Fonseca
发明人： Valerio Berdini , Robert George Boyle , Gordon Saxty , David Winter Walker , Steven John Woodhead , Paul Graham Wyatt , Alastair Donald , John Caldwell , Ian Collins , Tatiana Faria Da Fonseca
IPC分类号： A61K31/52 , C07D473/34 , C07D487/04 , A61K31/519 , C12N9/99 , C12Q1/48
CPC分类号： C07D471/04 , A61K31/4545 , A61K31/519 , A61K31/52 , A61K31/522 , C07D473/34 , C07D487/04
摘要： The invention provides a compound for use as a protein kinase B inhibitor, the compound being a compound of the formula (I) or salts, solvates, tautomers or N-oxides thereof, wherein T is N or CR5; J1-J2 is N═C(R6), (R7)C═N, (R8)N—C(O), (R8)2C—C(O), N═N or (R7)C═C(R6); E is a monocyclic carbocyclic or heterocyclic group of 5 or 6 ring members, the heterocyclic group containing up to 3 heteroatoms selected from O, N and S; Q1 is a bond or a saturated C1-3 hydrocarbon linker group, one of the carbon atoms in the linker group being optionally be replaced by an oxygen or nitrogen atom, or an adjacent pair of carbon atoms may be replaced by CONRq or NRqCO where Rq is hydrogen or methyl, or Rq is a C1-4 alkylene chain linked to R1 or a carbon atom of Q1 to form a cyclic moiety; and wherein the carbon atoms of the linker group Q1 may optionally bear one or more substituents selected from fluorine and hydroxy; Q2 is a bond or a saturated hydrocarbon linker group containing from 1 to 3 carbon atoms, wherein one of the carbon atoms in the linker group may optionally be replaced by an oxygen or nitrogen atom; and wherein the carbon atoms of the linker group may optionally bear one or more substituents selected from fluorine and hydroxy, provided that the hydroxy group when present is not located at a carbon atom a with respect to the G group; and provided that when E is aryl or heteroaryl, then Q2 is other than a bond; G is hydrogen, NR2R, OH or SH provided that when E is aryl or heteroaryl and Q2 is a bond, then G is hydrogen; R1 is hydrogen or an aryl or heteroaryl group, with the proviso that when R1 is hydrogen and G is NR2R3, then Q2 is a bond; and R2, R3, R4, R6 and R8 are as defined in the claims.
摘要翻译：本发明提供用作蛋白激酶B抑制剂的化合物，该化合物为式（I）化合物或其盐，溶剂合物，互变异构体或N-氧化物，其中T为N或CR 5; J1-J2是N-C（R6），（R7）C-N，（R8）N-C（O），（R8）2C-C（O），N-N或（R7）C-C（R6） E是5或6个环成员的单环碳环或杂环基，杂环基含有至多3个选自O，N和S的杂原子; Q1是键或饱和的C 1-3烃连接基团，连接基团中的一个碳原子任选被氧或氮原子代替，或者相邻的一对碳原子可被CONRq或NRqCO代替，其中Rq 是氢或甲基，或Rq是与R1或Q1的碳原子连接的C 1-4亚烷基链，形成环状部分; 并且其中所述连接基团Q1的碳原子可任选地具有一个或多个选自氟和羟基的取代基; Q2是含有1至3个碳原子的键或饱和烃连接基团，其中连接基团中的一个碳原子可任选被氧或氮原子取代; 并且其中所述连接基团的碳原子可以任选地具有一个或多个选自氟和羟基的取代基，条件是当存在的羟基不相对于G基团位于碳原子a时; 并且条件是当E是芳基或杂芳基时，则Q2不是键; G为氢，NR2R，OH或SH，条件是当E为芳基或杂芳基且Q2为键时，则G为氢; R 1是氢或芳基或杂芳基，条件是当R 1是氢且G是NR 2 R 3时，则Q2是一个键; 并且R 2，R 3，R 4，R 6和R 8如权利要求中所定义。

26. 发明申请

US20080275029A1 Compounds for Treating Protein-Kinase Mediated Disorders 审中-公开
公开(公告)号：US20080275029A1
公开(公告)日：2008-11-06
申请号：US11718943
申请日：2005-11-09
申请人： Valerio Berdini , Robert George Boyle , Gordon Saxty , Marinus Leendert Verdonk , Steven John Woodhead , Paul Graham Wyatt , Hannah Fiona Sore , David Winter Walker , John Caldwell , Ian Collins
发明人： Valerio Berdini , Robert George Boyle , Gordon Saxty , Marinus Leendert Verdonk , Steven John Woodhead , Paul Graham Wyatt , Hannah Fiona Sore , David Winter Walker , John Caldwell , Ian Collins
IPC分类号： A61K31/517 , C07D239/88 , C07D401/12 , C07D401/04 , A61K31/496 , A61K31/551 , A61P35/00 , C12N5/06 , A61K31/5377 , C07D401/06 , C07D403/12 , C07D413/14
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; J2-J1 is N═CR7 or R1aN—CO; G is OH or NR5R6; E is CONR7, NR7CO, C(R8)═C(R8) or (X)m(CR8R8a)n where X is O, S or NR7; provided that when J2-J1 is R1aN—CO, E is other than NR7CO; m and n are each 0 or 1, where m+n=1 or 2; A is a bond and R4 and R4a are absent or A is a saturated optionally substituted C1-7 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; R1, R1a, R2, and R3 are each H; halogen; C1-6 hydrocarbyl optionally substituted by halogen, OH or C1-2 alkoxy; CN; CONHR8; NH2; NHCOR10 or NHCONHR10; R4 is H or C1-4 alkyl; R4a is H, C1-4 alkyl or a group R9; R5 and R6 are each selected from H, R9 and C1-4 hydrocarbyl optionally substituted by halogen, C1-2 alkoxy or R9; or NR5R6 forms a saturated 4-7 membered monocyclic heterocyclic group; R7 is H or C1-4 alkyl; R8 and R8a each H or saturated C1-4 hydrocarbyl optionally substituted by fluorine; R9 is a monocyclic or bicyclic carbocyclic or heterocyclic group containing up to 3 ring heteroatoms selected from N, O and S; or R4, R4a and A together form a saturated monocyclic 4-7 membered heterocycle; or NR5R6, R4 and A form a saturated 4-7 membered monocyclic heterocycle; or R4, together with R7 or R8 and A and E form a 4-7 membered saturated monocyclic heterocycle; or NR5R6 and R7 or R8 together with A and E form a 4-7 membered saturated monocyclic heterocycle; and R10 is optionally substituted phenyl or benzyl.

27. 发明申请

US20080139620A1 Pyrazole Derivatives For The Inhibition Of Cdk's And Gsk's 审中-公开
标题翻译：吡唑衍生物抑制Cdk和Gsk的
公开(公告)号：US20080139620A1
公开(公告)日：2008-06-12
申请号：US11814449
申请日：2006-01-20
申请人： Paul Graham Wyatt , Valerio Berdini , Adrian Liam Gill , Gary Trewartha , Andrew James Woodhead
发明人： Paul Graham Wyatt , Valerio Berdini , Adrian Liam Gill , Gary Trewartha , Andrew James Woodhead
IPC分类号： C07D401/12 , A61K31/454 , C12N5/00 , A61P35/00
CPC分类号： C07D401/12
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。

28. 发明申请

US20080132495A1 Pyrazole Compounds that Modulate the Activity of Cdk, Gsk and Aurora Kinases 失效
标题翻译：调节Cdk，Gsk和Aurora激酶活性的吡唑化合物
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。

29. 发明授权

US09145394B2 Substituted quinoxalines as FGFR kinase inhibitors 有权
公开(公告)号：US09145394B2
公开(公告)日：2015-09-29
申请号：US13990193
申请日：2011-11-29
申请人： Gordon Saxty , Christopher William Murray , Valerio Berdini , Gilbert Ebai Besong , Christopher Charles Frederick Hamlett , Steven John Woodhead , Yannick Aime Eddy Ligny , Patrick René Angibaud
发明人： Gordon Saxty , Christopher William Murray , Valerio Berdini , Gilbert Ebai Besong , Christopher Charles Frederick Hamlett , Steven John Woodhead , Yannick Aime Eddy Ligny , Patrick René Angibaud
IPC分类号： A61K31/498 , C07D241/40 , C07D403/04 , C07D401/14 , C07D403/14
摘要： The invention relates to new quinoxaline derivative compounds of formula (I), 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.

30. 发明授权

US08481531B2 Bicyclic heterocyclyl derivatives as FGFR kinase inhibitors for therapeutic use 有权
标题翻译：双环杂环基衍生物作为治疗用途的FGFR激酶抑制剂
公开(公告)号：US08481531B2
公开(公告)日：2013-07-09
申请号：US13264593
申请日：2010-04-15
申请人： Gordon Saxty , Valerio Berdini , Eddy Jean Edgard Freyne , Alexandra Papanikos , Pascal Benderitter , Werner Constant Johan Embrechts , Berthold Wroblowski , Rhalid Akkari
发明人： Gordon Saxty , Valerio Berdini , Eddy Jean Edgard Freyne , Alexandra Papanikos , Pascal Benderitter , Werner Constant Johan Embrechts , Berthold Wroblowski , Rhalid Akkari
IPC分类号： A61K31/5377 , A61K31/437 , A61K31/496 , C07D413/02 , C07D471/04 , C07D401/02 , C07D239/20
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。

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