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11. 发明申请

US20160075666A1 QUINAZOLINONE DERIVATIVES USEFUL AS FGFR KINASE MODULATORS 有权
标题翻译：喹诺酮酮衍生物作为FGFR激酶调节剂有用
公开(公告)号：US20160075666A1
公开(公告)日：2016-03-17
申请号：US14787089
申请日：2014-04-25
申请人： ASTEX THERAPEUTICS LIMITED
发明人： Patrick René ANGIBAUD , Olivier Alexis Georges QUEROLLE , Isabelle Noëlle Constance PILATTE , Lieven MEERPOEL , Virginie Sophie PONCELET
IPC分类号： C07D239/91 , A61K45/06 , C07D403/12 , C07D405/14 , C07D403/14 , C07D401/04 , C07D405/04 , A61K31/517 , C07D403/04
CPC分类号： C07D239/91 , A61K31/517 , A61K45/06 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/12 , C07D403/14 , C07D405/04 , C07D405/14
摘要： The invention relates to new quinazolinone 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：本发明涉及新的喹唑啉酮衍生物化合物，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以及所述化合物在治疗疾病中的用途。癌症。

12. 发明授权

US09155743B2 Bicyclic heterocycle compounds and their uses in therapy 有权
标题翻译：双环杂环化合物及其在治疗中的应用
公开(公告)号：US09155743B2
公开(公告)日：2015-10-13
申请号：US14112581
申请日：2012-04-20
申请人： Ildiko Maria Buck , Gianni Chessari , Steven Howard , David Charles Rees , Alison Jo-Anne Woolford
发明人： Ildiko Maria Buck , Gianni Chessari , Steven Howard , David Charles Rees , Alison Jo-Anne Woolford
IPC分类号： C07D498/10 , A61K31/5365 , A61K31/5386 , C07D471/04 , C07D498/04 , A61K45/06 , A61K31/519 , A61K31/437 , A61K31/4985 , A61K31/5383
CPC分类号： C07D471/04 , A61K31/437 , A61K31/4985 , A61K31/519 , A61K31/5383 , A61K31/5386 , A61K45/06 , C07D498/04 , C07D498/10 , A61K2300/00
摘要： The invention relates to bicyclic heterocycle compounds of formula (I): or tautomeric or stereochemically isomeric forms, N-oxides, pharmaceutically acceptable salts or the solvates thereof; wherein R1, R2, R3, A, W, U and V 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）的双环杂环化合物：或互变异构体或立体化学异构形式，N-氧化物，药学上可接受的盐或其溶剂合物; 其中R1，R2，R3，A，W，U和V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治疗疾病中的用途。癌症。

13. 发明授权

US09006430B2 Ortho-condensed pyridine and pyrimidine derivatives (e.g., purines) as protein 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：US09006430B2
公开(公告)日：2015-04-14
申请号：US14310475
申请日：2014-06-20
申请人： Astex Therapeutics Limited , The Institute of Cancer Research: Royal Cancer Hospital , Cancer Research Technology Limited
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 , C07D471/02 , C07D471/04 , C07D473/34 , A61K31/4545 , A61K31/519 , A61K31/52 , A61K31/522
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 R 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, NR2R3, 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 Q 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 ）; 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R或Q1的碳原子连接的C 1-4亚烷基链，以形成环状部分; 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，NR2R3，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是氢并且G是NR 2 R 3时，则Q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。

14. 发明申请

US20150057293A1 NEW COMPOUNDS 有权
标题翻译：新化合物
公开(公告)号：US20150057293A1
公开(公告)日：2015-02-26
申请号：US14354793
申请日：2012-10-26
申请人： ASTEX THERAPEUTICS LIMITED
发明人： Patrick Rene Angibaud , Michel Obringer , Julien Jeremie Joseph Marin , Matthieu Jeanty
IPC分类号： C07D471/04 , A61K31/506 , A61K45/06 , A61K31/4375
CPC分类号： A61K31/4375 , A61K31/444 , A61K31/4545 , A61K31/506 , A61K45/06 , C07D471/04
摘要： The invention relates to new naphthyridine 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：本发明涉及新的萘啶衍生物化合物，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以及所述化合物在治疗疾病中的用途。癌症。

15. 发明申请

US20140296236A1 QUINOLINES AS FGFR KINASE MODULATORS 有权
标题翻译：喹诺酮作为FGFR激酶调节剂
公开(公告)号：US20140296236A1
公开(公告)日：2014-10-02
申请号：US14354773
申请日：2012-10-26
申请人： ASTEX THERAPEUTICS LIMITED
发明人： Valerio Berdini , Patrick Rene Angibaud , Steven John Woodhead , Gordon Saxty
IPC分类号： C07D413/14 , A61K31/4709 , A61K45/06 , A61K31/5377 , A61K31/506 , C07D405/14 , C07D215/38 , A61K31/47 , C07D401/04 , C07D401/14
CPC分类号： A61K31/4709 , A61K31/47 , A61K31/506 , A61K31/5377 , A61K45/06 , C07D215/38 , C07D401/04 , C07D401/14 , C07D405/14 , C07D407/14 , C07D413/14
摘要： The invention relates to new quinoline 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. Formula (I)
摘要翻译：本发明涉及式（I）的新的喹啉衍生物化合物，包含所述化合物的药物组合物，所述化合物的制备方法以及所述化合物在治疗疾病中的用途。癌症。式（I）

16. 发明申请

US20140179666A1 BICYCLIC HETEROCYCLE COMPOUNDS AND THEIR USES IN THERAPY 有权
标题翻译：双相异构体化合物及其在治疗中的用途
公开(公告)号：US20140179666A1
公开(公告)日：2014-06-26
申请号：US14112597
申请日：2012-04-20
申请人： Alison Jo-Anne Woolford , Steven Howard , Ildiko Maria Buck , Gianni Chessari , Christopher Norbert Johnson , Emiliano Tamanini , James Edward Harvey Day , Elisabetta Chiarparin , Thomas Daniel Heightman , Martyn Frederickson , Charlotte Mary Griffiths-Jones
发明人： Alison Jo-Anne Woolford , Steven Howard , Ildiko Maria Buck , Gianni Chessari , Christopher Norbert Johnson , Emiliano Tamanini , James Edward Harvey Day , Elisabetta Chiarparin , Thomas Daniel Heightman , Martyn Frederickson , Charlotte Mary Griffiths-Jones
IPC分类号： C07D471/04 , C07D403/14 , C07D487/10 , C07D403/06 , C07D471/10
CPC分类号： C07D471/04 , A61K31/496 , A61K31/497 , A61K31/501 , A61K31/5025 , A61K31/506 , A61K31/5377 , C07D401/06 , C07D403/06 , C07D403/14 , C07D413/14 , C07D471/10 , C07D487/04 , C07D487/10 , C07D519/00
摘要： The invention relates to bicyclic heterocycle compounds of formula (I): or tautomeric or stereochemically isomeric forms, N-oxides, pharmaceutically acceptable salts or the solvates thereof; wherein R1, R2a, R2b, R3a, R3b, R5, R6, R7, R8, R9, p and E 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）的双环杂环化合物：或互变异构体或立体化学异构形式，N-氧化物，药学上可接受的盐或其溶剂合物; 其中R1，R2a，R2b，R3a，R3b，R5，R6，R7，R8，R9，p和E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治疗疾病中的用途。癌症。

17. 发明申请

US20130210820A1 Pharmaceutical Compounds 有权
标题翻译：药物化合物
公开(公告)号：US20130210820A1
公开(公告)日：2013-08-15
申请号：US13753904
申请日：2013-01-30
申请人： ASTEX THERAPEUTICS LIMITED
发明人： Brian John Williams , Martyn Frederickson
IPC分类号： C07D295/155
CPC分类号： C07D295/155 , C07D209/44
摘要： The invention provides a compound of the formula (1): or a salt, solvate, N-oxide or tautomer thereof.
摘要翻译：本发明提供式（1）化合物或其盐，溶剂化物，N-氧化物或其互变异构体。

19. 发明授权

US08277807B2 Pharmaceutical combinations 有权
标题翻译：药物组合
公开(公告)号：US08277807B2
公开(公告)日：2012-10-02
申请号：US12445141
申请日：2007-10-12
申请人： Neil James Gallagher , John Francis Lyons , Neil Thomas Thompson , Stephen Murray Yule , Christopher William Murray
发明人： Neil James Gallagher , John Francis Lyons , Neil Thomas Thompson , Stephen Murray Yule , Christopher William Murray
IPC分类号： A61K31/404 , A61K31/4035 , A61K31/47 , A61K31/472 , A61K31/438 , A61K31/5377 , A61K39/395 , A61K31/4745
CPC分类号： A61K45/06 , A61K31/403 , A61K31/4035 , A61K2300/00
摘要： The invention provides combinations comprising (or consisting essentially of) one or more ancillary compound(s) and a compound of the formula (I): or salts, tautomers, solvates and N-oxides thereof; wherein R1 is hydroxy or hydrogen; R2 is hydroxy; methoxy or hydrogen; provided that at least one of R1 and R2 is hydroxy; R3 is selected from hydrogen; halogen; cyano; optionally substituted C1-5 hydrocarbyl and optionally substituted C1-5 hydrocarbyloxy; R4 is selected from hydrogen; a group —(O)n—R7 where n is 0 or 1 and R7 is an optionally substituted acyclic C1-5 hydrocarbyl group or a monocyclic carbocyclic or heterocyclic group having 3 to 7 ring members; halogen; cyano; hydroxy; amino; and optionally substituted mono- or di-C1-5 hydrocarbyl-amino; or R3 and R4 together form a monocyclic carbocyclic or heterocyclic ring of 5 to 7 ring members; and NR5R6 forms an optionally substituted bicyclic heterocyclic group having 8 to 12 ring members of which up to 5 ring members are heteroatoms selected from oxygen, nitrogen and sulphur. The combinations have activity as Hsp90 inhibitors.
摘要翻译：本发明提供包含（或基本上由）一种或多种辅助化合物和式（I）化合物或其盐，互变异构体，溶剂合物和N-氧化物的组合; 其中R1是羟基或氢; R2是羟基; 甲氧基或氢; 条件是R 1和R 2中的至少一个是羟基; R3选自氢; 卤素; 氰基; 任选取代的C 1-5烃基和任选取代的C 1-5烃氧基; R4选自氢; 其中n为0或1，R7为任选取代的无环C 1-5烃基或具有3至7个环成员的单环碳环或杂环基团 - （O）n -R 7基团; 卤素; 氰基; 羟基; 氨基; 和任选取代的单或二-C 1-5烃基 - 氨基; 或R 3和R 4一起形成5至7个环成员的单环碳环或杂环; 并且NR 5 R 6形成具有8至12个环成员的任选取代的双环杂环基，其中多达5个环成员是选自氧，氮和硫的杂原子。这些组合具有作为Hsp90抑制剂的活性。

20. 发明申请

US20120035171A1 BICYCLIC HETEROCYCLYL DERIVATIVES AS FGFR KINASE INHIBITORS FOR THERAPEUTIC USE 有权
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：US20120035171A1
公开(公告)日：2012-02-09
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 , A61P35/00 , A61K31/496 , A61K31/513 , C07D471/04 , 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。

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