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3. 发明授权

US08796244B2 Imidazopyridine derivatives as inhibitors of receptor tyrosine kinases 有权
标题翻译：咪唑并吡啶衍生物作为受体酪氨酸激酶的抑制剂
公开(公告)号：US08796244B2
公开(公告)日：2014-08-05
申请号：US12997754
申请日：2009-06-12
申请人： Valerio Berdini , Maria Grazia Carr , Miles Stuart Congreve , Martyn Frederickson , Charlotte Mary Griffiths-Jones , Christopher Charles Frederick Hamlett , Andrew Madin , Christopher William Murray , Rajdeep Kaur Benning , Gordon Saxty , Emma Vickerstaffe , Andrew James Woodhead , Steven John Woodhead , Eddy Jean Edgard Freyne , Tom Cornelis Hortense Govaerts , Patrick René Angibaud , Marian Williams
发明人： Valerio Berdini , Maria Grazia Carr , Miles Stuart Congreve , Martyn Frederickson , Charlotte Mary Griffiths-Jones , Christopher Charles Frederick Hamlett , Andrew Madin , Christopher William Murray , Rajdeep Kaur Benning , Gordon Saxty , Emma Vickerstaffe , Brian John Williams , Andrew James Woodhead , Steven John Woodhead , Eddy Jean Edgard Freyne , Tom Cornelis Hortense Govaerts , Patrick René Angibaud
IPC分类号： A61K31/5025 , C07D413/02
CPC分类号： C07D471/04 , C07D513/04
摘要： The invention relates to new bicyclic heterocyclic derivative compounds, to pharmaceutical compositions comprising the compounds and to the use of the 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，包含该化合物的药物组合物和该化合物在治疗疾病中的用途。癌症。

4. 发明申请

US20120208791A1 IMIDAZOPYRIDINE DERIVATIVES AS INHIBITORS OF RECEPTOR TYROSINE KINASES 有权
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：US20120208791A1
公开(公告)日：2012-08-16
申请号：US12997754
申请日：2009-06-12
申请人： Valerio Berdini , Maria Grazia Carr , Miles Stuart Congreve , Martyn Frederickson , Charlotte Mary Griffiths-Jones , Christopher Charles Frederick Hamlett , Andrew Madin , Christopher William Murray , Rajdeep Kaur Benning , Gordon Saxty , Emma Vickerstaffe , Brian John Williams , Marian Williams , Andrew James Woodhead , Steven John Woodhead , Eddy Jean Edgard Freyne , Tom Cornelis Hortense Govaerts , Patrick René Angibaud
发明人： Valerio Berdini , Maria Grazia Carr , Miles Stuart Congreve , Martyn Frederickson , Charlotte Mary Griffiths-Jones , Christopher Charles Frederick Hamlett , Andrew Madin , Christopher William Murray , Rajdeep Kaur Benning , Gordon Saxty , Emma Vickerstaffe , Brian John Williams , Marian Williams , Andrew James Woodhead , Steven John Woodhead , Eddy Jean Edgard Freyne , Tom Cornelis Hortense Govaerts , Patrick René Angibaud
IPC分类号： A61K31/437 , A61K31/501 , A61P35/00 , C07D513/04 , A61K31/53 , A61K31/506 , C07D471/04 , A61K31/5377
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。

5. 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.

6. 发明授权

US09290478B2 Substituted quinoxalines as FGFR kinase inhibitors 有权
标题翻译：取代的喹喔啉作为FGFR激酶抑制剂
公开(公告)号：US09290478B2
公开(公告)日：2016-03-22
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
CPC分类号： 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.
摘要翻译：本发明涉及式（I）的新的喹喔啉衍生物化合物，包含所述化合物的药物组合物，所述化合物的制备方法和所述化合物在治疗疾病中的用途。癌症。

7. 发明申请

US20130267525A1 SUBSTITUTED BENZOPYRAZIN DERIVATIVES AS FGFR KINASE INHIBITORS FOR THE TREATMENT OF CANCER DISEASES 有权
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：US20130267525A1
公开(公告)日：2013-10-10
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： C07D403/04 , C07D401/14 , C07D403/14
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

US20110144080A1 PYRAZOLE DERIVATIVES AS PROTEIN KINASE MODULATORS 有权
标题翻译：作为蛋白激酶调节剂的吡唑衍生物
公开(公告)号：US20110144080A1
公开(公告)日：2011-06-16
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 , Hanna 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 , Hanna Fiona Sore , David Winter Walker , Ian Collins , Robert Downham , Robin Arthur Ellis Carr
IPC分类号： A61K31/415 , C07D231/12 , C07D401/10 , A61K31/454 , A61K31/4439 , C07D413/10 , A61K31/5377 , C07D403/10 , A61K31/4155 , A61K31/496 , A61K31/497 , A61K31/551 , C07D401/04 , C07D401/14 , A61K31/4545 , A61P35/00
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。

9. 发明申请

US20130005702A1 PYRAZOLE DERIVATIVES AS PROTEIN KINASE MODULATORS 失效
标题翻译：作为蛋白激酶调节剂的吡唑衍生物
公开(公告)号：US20130005702A1
公开(公告)日：2013-01-03
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 , Hanna 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 , Hanna Fiona Sore , David Winter Walker , Ian Collins , Robert Downham , Robin Arthur Ellis Carr
IPC分类号： A61K31/415 , C07D401/10 , A61K31/451 , A61K31/4439 , C12N5/09 , A61K31/5377 , A61K31/4155 , C07D403/10 , A61K31/551 , A61P35/00 , C07D231/12 , C07D413/10
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。

10. 发明申请

US20090099213A1 Ortho-Condensed Pyridine and Pyrimidine Derivatives (e.g., Purines) as Protein Kinases Inhibitors 审中-公开
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：US20090099213A1
公开(公告)日：2009-04-16
申请号：US11577962
申请日：2005-10-25
申请人： Valerio Berdini , Robert George Boyle , Gordon Saxty , Marinus Leendert Verdonk , Steven John Woodhead , Paul Graham Wyatt , Hannah Fiona Sore , John Caldwell , Ian Collins , Tatiana Faria Da Fonseca , Alastair Donald
发明人： Valerio Berdini , Robert George Boyle , Gordon Saxty , Marinus Leendert Verdonk , Steven John Woodhead , Paul Graham Wyatt , Hannah Fiona Sore , John Caldwell , Ian Collins , Tatiana Faria Da Fonseca , Alastair Donald
IPC分类号： A61K31/52 , A61P35/00 , C07D473/34
CPC分类号： C07D471/04 , C07D473/00 , C07D473/34 , C07D487/04
摘要： The invention provides a compound for use in the prophylaxis or treatment of a disease state or condition mediated by protein kinase B, the compound having 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); A is an optionally substituted saturated C1-7 hydrocarbon 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, one of the carbon atoms in the linker group being optionally replaced by oxygen or nitrogen; E is a monocyclic or bicyclic carbocyclic or heterocyclic group or an acyclic group X-G wherein X is CH2, O, S or NH and G is a C1-4 alkylene chain wherein one of the carbon atoms is optionally replaced by O, S or NH; R1 is hydrogen or an aryl or heteroaryl group; R2 and R3 are each hydrogen, optionally substituted C1-4 hydrocarbyl or optionally substituted C1-4 acyl; or NR2R3 forms an imidazole group or a saturated monocyclic heterocyclic group having 4-7 ring members; or NR2R3 and A together form a saturated monocyclic heterocyclic group having 4-7 ring members which is optionally substituted by C1-4alkyl; or NR2R3 and the adjacent carbon atom of linker group A together form a cyano group; or R1, A and NR2R3 together form a cyano group; and R4, R5, R6, R7 and R8 are each independently selected from hydrogen and various substituents as defined in the claims.
摘要翻译：本发明提供了一种用于预防或治疗由蛋白激酶B介导的疾病状态或病症的化合物，其具有式（I）：或其盐，溶剂合物，互变异构体或N-氧化物，其中T为N或 CR5; J1-J2是N-C（R6），（R7）C-N，（R8）N-C（O），（R8）2C-C（O），N-N或（R7）C-C（R6） A是在R 1和NR 2 R 3之间延伸的最大链长度为5个原子并且在E和NR 2 R 3之间延伸的4个原子的最大链长度的任选取代的饱和C 1-7烃连接基团，连接基团中的一个碳原子是任选的用氧或氮代替; E是单环或双环碳环或杂环基或非环基X-G，其中X是CH 2，O，S或NH，G是C 1-4亚烷基链，其中一个碳原子任选被O，S或NH取代; R1是氢或芳基或杂芳基; R2和R3各自为氢，任选取代的C 1-4烃基或任选取代的C 1-4酰基; 或NR 2 R 3形成具有4-7个环成员的咪唑基或饱和单环杂环基; 或NR2R3和A一起形成具有4-7个环成员的饱和单环杂环基，其任选被C 1-4烷基取代; 或NR2R3和连接基团A的相邻碳原子一起形成氰基; 或R 1，A和NR 2 R 3一起形成氰基; 且R 4，R 5，R 6，R 7和R 8各自独立地选自氢和权利要求中所定义的各种取代基。

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