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21. 发明申请

US20120035152A1 BICYCLIC HETEROCYCLIC COMPOUNDS AS PROTEIN TYROSINE KINASE INHIBITORS 有权
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：US20120035152A1
公开(公告)日：2012-02-09
申请号：US13275752
申请日：2011-10-18
申请人： Gordon SAXTY , Valerio BERDINI , Christopher William MURRAY , Charlotte Mary GRIFFITHS-JONES , Emma VICKERSTAFFE , Gilbert Ebai BESONG
发明人： Gordon SAXTY , Valerio BERDINI , Christopher William MURRAY , Charlotte Mary GRIFFITHS-JONES , Emma VICKERSTAFFE , Gilbert Ebai BESONG
IPC分类号： A61K31/437 , A61P35/00 , A61K31/519
CPC分类号： C07D471/04
摘要： The invention relates to new bicyclic heterocyclic derivative compounds of formula (I): wherein R1, q, A, B, X1, X2, X3, X4, X5 and R2 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。

22. 发明申请

US20110105501A1 PHARMACEUTICAL COMBINATIONS 有权
标题翻译：药物组合
公开(公告)号：US20110105501A1
公开(公告)日：2011-05-05
申请号：US12445136
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： A61K31/4035 , A61K31/438 , A61K31/5377 , A61K31/496 , A61P31/12 , A61P35/00
CPC分类号： C07D401/14 , A61K31/403 , A61K31/438 , A61K31/439 , A61K31/496 , A61K31/5375 , C07D209/08 , C07D209/44 , C07D215/08 , C07D401/04 , C07D471/04 , C07D471/10 , C07D491/08 , C07D491/10 , 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 and/or glycogen synthase kinase-3 and/or cyclin dependent kinase and/or aurora kinase 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和/或糖原合酶激酶-3和/或细胞周期蛋白依赖性激酶和/或极光激酶抑制剂的活性。

23. 发明申请

US20100331296A1 BICYCLIC HETEROCYCLIC COMPOUNDS AS PROTEIN TYROSINE KINASE INHIBITORS 有权
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：US20100331296A1
公开(公告)日：2010-12-30
申请号：US12682508
申请日：2008-10-10
申请人： Gordon Saxty , Valerio Berdini , Christopher William Murray , Charlotte Mary Griffiths-Jones , Emma Vickerstaffe , Gilbert Ebai Besong , Maria Grazia Carr
发明人： Gordon Saxty , Valerio Berdini , Christopher William Murray , Charlotte Mary Griffiths-Jones , Emma Vickerstaffe , Gilbert Ebai Besong , Maria Grazia Carr
IPC分类号： A61K31/437 , C07D471/04 , A61P35/00
CPC分类号： C07D471/04 , C07D487/04
摘要： The invention relates to new bicyclic heterocyclic derivative compounds of formula (I): wherein R1, A, X1, X2, X3, X4, X5 and R2 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。

24. 发明申请

US20100113551A1 COMPOSITIONS COMPRISING (S)-2-AMINO-1-(4-CHLOROPHENYL)-1-[4-(1H-PYRAZOL-4-YL)-PHENYL]-ETHANOL AS MODULATOR OF PROTEIN KINASES 审中-公开
标题翻译：包含（S）-2-氨基-1-（4-氯苯基）-1- [4-（1H-吡唑-4-基） - 苯基] - 乙醇的组合物作为蛋白激酶的调节剂
公开(公告)号：US20100113551A1
公开(公告)日：2010-05-06
申请号：US12531013
申请日：2008-03-14
申请人： Steven John Woodhead , David Charles Rees , Martyn Frederickson , Kyla Merriom Grimshaw
发明人： Steven John Woodhead , David Charles Rees , Martyn Frederickson , Kyla Merriom Grimshaw
IPC分类号： A61K31/415 , C07D231/12 , C07C211/00 , C07C245/00 , C07D303/00
CPC分类号： A61K31/415 , C07C215/32 , C07C247/10 , C07C309/30 , C07D231/12 , A61K2300/00
摘要： The invention provides a composition comprising (S) 2-amino-1-(4-chloro-phenyl)-1-[4-(1H-pyrazol-4-yl)-phenyl]-ethanol, wherein the composition is either substantially free of (R) 2-amino-1-(4-chloro-phenyl)-1-[4-(1H-pyrazol-4-yl)-phenyl]-ethanol or the composition contains a mixture of the (S) and (R) enantiomers in which the (S) enantiomer predominates. Also provided are processes for the preparation of the (S) 2-amino-1-(4-chloro-phenyl)-1-[4-(1H-pyrazol-4-yl)-phenyl]-ethanol, novel process intermediates and methods for making the novel process intermediates.
摘要翻译：本发明提供包含（S）2-氨基-1-（4-氯 - 苯基）-1- [4-（1H-吡唑-4-基） - 苯基] - 乙醇的组合物，其中组合物基本上不含的（R）2-氨基-1-（4-氯 - 苯基）-1- [4-（1H-吡唑-4-基） - 苯基] - 乙醇或该组合物含有（S）和（（S）对映异构体占优势。还提供了制备（S）2-氨基-1-（4-氯 - 苯基）-1- [4-（1H-吡唑-4-基） - 苯基] - 乙醇的方法，新工艺中间体和制备新工艺中间体的方法。

25. 发明申请

US20100004243A1 PHARMACEUTICAL COMPOUNDS 审中-公开
标题翻译：药物化合物
公开(公告)号：US20100004243A1
公开(公告)日：2010-01-07
申请号：US12373659
申请日：2007-07-13
申请人： Miles Stuart Congreve , Adrian Liam Gill , Steven Howard , Paul Neil Mortenson , Gillbert Ebai Besong
发明人： Miles Stuart Congreve , Adrian Liam Gill , Steven Howard , Paul Neil Mortenson , Gillbert Ebai Besong
IPC分类号： A61K31/5377 , C07D417/14 , C07D401/14 , C07D413/14 , A61K31/454 , A61K31/437 , A61K31/496 , A61K31/4375 , A61P35/00 , C12N9/99
CPC分类号： C07D417/12 , C07D401/12 , C07D401/14 , C07D513/04
摘要： The invention provides a cyclin dependent kinase (e.g. cdk-4 kinase) inhibitor of the formula (I) or a salt, tautomer, solvate or N-oxide thereof; wherein R1 is an optionally substituted monocyclic or bicyclic aryl or heteroaryl group containing 0-2 heteroatoms selected from O, N and S wherein the optional substituents are selected from halogen, C1-4 alkyl, C1-4 alkoxy, C3-4 cycloalkyl and cyano, and wherein the C1-4 alkyl and C1-4 alkoxy groups are each optionally further substituted by C1-2 alkoxy or one or more halogen atoms; and E is a group E1, E2, E3 or E4: formulae E1, E2, E3, E4 wherein n, q, A5 B, T, U, V, W, Z, R2, R5, R6 and R7 are as defined in the claims.
摘要翻译：本发明提供了式（I）的细胞周期蛋白依赖性激酶（例如cdk-4激酶）抑制剂或其盐，互变异构体，溶剂合物或N-氧化物; 其中R 1是含有0-2个选自O，N和S的杂原子的任选取代的单环或双环芳基或杂芳基，其中任选的取代基选自卤素，C 1-4烷基，C 1-4烷氧基，C 3-4环烷基和氰基并且其中所述C 1-4烷基和C 1-4烷氧基各自任选进一步被C 1-2烷氧基或一个或多个卤素原子取代; 并且E是E1，E2，E3或E4基团：式E1，E2，E3，E4其中n，q，A5B，T，U，V，W，Z，R2，R5，R6和R7如索赔。

26. 发明申请

US20090253718A1 Pharmaceutical Compounds 审中-公开
标题翻译：药物化合物
公开(公告)号：US20090253718A1
公开(公告)日：2009-10-08
申请号：US12298117
申请日：2007-04-25
申请人： Thomas Glanmor Davies , Michelle Dawn Garrett , Robert George Boyle , Ian Collins
发明人： Thomas Glanmor Davies , Michelle Dawn Garrett , Robert George Boyle , Ian Collins
IPC分类号： A61K31/522 , A61K31/52 , A61P35/04 , A61P35/00 , A61K31/519
CPC分类号： C07D473/34 , C07D471/04 , C07D473/00 , C07D487/04
摘要： The invention provides a 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 C1-4 alkyl; 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, wherein the compound is for use in: (a) the treatment or prophylaxis of a disease or condition in which the modulation (e.g. inhibition) of ROCK kinase or protein kinase p70S6K is indicated; and/or (b) the treatment of a subject or patient population in which the modulation (e.g. inhibition) of ROCK kinase or protein kinase p70S6K is indicated.
摘要翻译：本发明提供具有式（I）的化合物或其盐，溶剂化物，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） 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; 并且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定义的各种取代基，其中所述化合物用于：（a）治疗或预防其中调节表示ROCK激酶或蛋白激酶p70S6K的抑制作用）和/或（b）治疗其中指示ROCK激酶或蛋白激酶p70S6K的调节（例如抑制）的受试者或患者群体。

27. 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。

28. 发明申请

US20090233943A9 NEW COMPOUNDS 835 审中-公开
标题翻译：新化合物835
公开(公告)号：US20090233943A9
公开(公告)日：2009-09-17
申请号：US12120608
申请日：2008-05-14
申请人： Jeremy Nicholas Burrows , Sven Hellberg , Katharina Hogdin , Sofia Karlstrom , Karin Kolmodin , Johan Lindstrom , Can Slivo
发明人： Jeremy Nicholas Burrows , Sven Hellberg , Katharina Hogdin , Sofia Karlstrom , Karin Kolmodin , Johan Lindstrom , Can Slivo
IPC分类号： A61K31/497 , C07D233/90 , A61K31/4168 , C07D403/10 , A61K31/506 , C07D401/10 , A61K31/4439
CPC分类号： C07D401/10 , C07D233/86 , C07D233/88 , C07D403/10 , C07D417/10
摘要： This invention relates to novel compounds having the structural formula I below: and to their pharmaceutically acceptable salt, compositions and methods of use. These novel compounds provide a treatment or prophylaxis of cognitive impairment, Alzheimer Disease, neurodegeneration and dementia.
摘要翻译：本发明涉及具有以下结构式I的新化合物及其药学上可接受的盐，组合物和使用方法。这些新化合物提供了认知障碍，阿尔茨海默病，神经变性和痴呆症的治疗或预防。

29. 发明申请

US20090233930A9 Novel 2-Amino-Imidazole-4-One Compounds and Their Use in the Manufacture of a Medicament to Be Used in the Treatment of Cognitive Impairment, Alzheimer's Disease, Neurodegeneration and Dementia 审中-公开
标题翻译：新型2-氨基咪唑-4-酮化合物及其在制造用于治疗认知功能障碍，阿尔茨海默病，神经退行性和痴呆症药物中的应用
公开(公告)号：US20090233930A9
公开(公告)日：2009-09-17
申请号：US12094276
申请日：2006-11-20
申请人： Stefan Berg , Jeremy Burrows , Gianni Chessari , Miles Stuart Congreve , Johan Hedstrom , Sven Hellberg , Katharina Hogdin , Jacob Kihlstrom , Karin Kolmodin , Johan Lindstrom , Christopher Murray , Sahil Patel
发明人： Stefan Berg , Jeremy Burrows , Gianni Chessari , Miles Stuart Congreve , Johan Hedstrom , Sven Hellberg , Katharina Hogdin , Jacob Kihlstrom , Karin Kolmodin , Johan Lindstrom , Christopher Murray , Sahil Patel
IPC分类号： A61K31/5377 , C07D401/10 , A61K31/4725 , C07D339/08 , A61P25/28 , C07F7/08 , C12N9/99 , C07D413/12
CPC分类号： C07D233/88 , C07C25/22 , C07C25/24 , C07C39/373 , C07C43/1747 , C07C43/23 , C07C47/575 , C07C49/792 , C07C49/813 , C07C49/83 , C07C49/84 , C07D209/08 , C07D217/06 , C07D233/86 , C07D265/36 , C07D307/79 , C07D339/08 , C07D401/04 , C07D401/10 , C07D403/04 , C07D403/10 , C07D405/04 , C07D405/10 , C07D409/06 , C07D409/10 , C07D413/06 , C07D413/10 , C07D417/04 , C07F7/1804
摘要： This invention relates to novel compounds having the structural formula I below: and to their pharmaceutically acceptable salt, compositions and methods of use. These novel compounds provide a treatment or prophylaxis of cognitive impairment, Alzheimer Disease, neurodegeneration and dementia.
摘要翻译：本发明涉及具有以下结构式I的新化合物及其药学上可接受的盐，组合物和使用方法。这些新化合物提供了认知障碍，阿尔茨海默病，神经变性和痴呆症的治疗或预防。

30. 发明申请

US20080312223A1 Thiazole And Isothiazole Derivatives That Modulate The Activity Of CDK, GSK And Aurora Kinases 审中-公开
标题翻译：调节CDK，GSK和Aurora激酶活性的噻唑和异噻唑衍生物
公开(公告)号：US20080312223A1
公开(公告)日：2008-12-18
申请号：US11813173
申请日：2005-12-30
申请人： Valerio Berdini , Michael Alistair O'Brien , Theresa Rachel Phillips , Paul Graham Wyatt
发明人： Valerio Berdini , Michael Alistair O'Brien , Theresa Rachel Phillips , Paul Graham Wyatt
IPC分类号： A61K31/5377 , C07D277/38 , A61K31/426 , A61P35/02 , A61P35/00 , C07D417/14
CPC分类号： C07D417/14 , C07D417/04
摘要： The invention provides a compound of the formula (I): or a salt, N-oxide, tautomer or solvate thereof, wherein X is CR5 or N; each of Q1 and Q2 is a carbon atom; Q3 is selected from S and CH; Q4 is selected from CR2 and S; provided that one of Q3 and Q4 is S and the other of Q3 and Q4 is not S; wherein when Q3 is S, there is a double bond between Q1 and Q4 and a double bond between Q2 and the adjacent ring nitrogen atom N; and when Q4 is S, there is a double bond between Q1 and Q2, and a double bond between Q3 and the adjacent ring nitrogen atom N; A is a bond or —(CH2)m—(B)n—; B is C═O, NR8(C═O) or O(C═O) wherein R1 is hydrogen or C1_4 hydrocarbyl optionally substituted by hydroxy or C1-4 alkoxy; m is 0, 1 or 2; n is 0 or 1; Ro is hydrogen or, together with NRg when present, forms a group —(CH2)p— wherein p is 2 to 4; R1 is hydrogen, a carbocyclic or heterocyclic group having from 3 to 12 ring members, or an optionally substituted C1-8 hydrocarbyl group; R2 is hydrogen, halogen, methoxy, or a C1-4 hydrocarbyl group optionally substituted by halogen, hydroxyl or methoxy; R3 and R4 together with the carbon atoms to which they are attached form an optionally substituted fused carbocyclic or heterocyclic ring having from 5 to 7 ring members of which up to 3 can be heteroatoms selected from N, O and S; and R5 is hydrogen, a group R2 or a group R10 wherein R10 is as defined in the claims. The compounds have activity as inhibitors of cyclin dependent kinases, glycogen synthase kinases and Aurora kinases.
摘要翻译：本发明提供式（I）化合物或其盐，N-氧化物，互变异构体或其溶剂化物，其中X为CR 5或N; Q1和Q2中的每一个是碳原子; Q3选自S和CH; Q4选自CR2和S; 条件是Q3和Q4中的一个是S，Q3和Q4中的另一个不是S; 其中当Q3为S时，在Q1和Q4之间存在双键并且Q2和相邻的环氮原子之间存在双键; 当Q4为S时，Q1与Q2之间存在双键，Q3与相邻环氮原子之间的双键为N; A是键或 - （CH 2）m - （B）n-; B为C-O，NR8（C-O）或O（C-O），其中R 1为氢或任选被羟基或C 1-4烷氧基取代的C 1-4烃基; m为0,1或2; n为0或1; Ro是氢或与存在的NR g一起形成基团 - （CH 2）p - ，其中p是2至4; R 1是氢，具有3至12个环成员的碳环或杂环基或任选取代的C 1-8烃基; R2是氢，卤素，甲氧基或任选被卤素，羟基或甲氧基取代的C 1-4烃基; R3和R4与它们所连接的碳原子一起形成具有5至7个环成员的任选取代的稠合碳环或杂环，其中多达3个可以是选自N，O和S的杂原子; 并且R 5是氢，基团R 2或基团R 10，其中R 10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，糖原合成酶激酶和极光激酶抑制剂的活性。

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