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21. 发明申请

WO2009130496A1 SUBSTITUTED PYRIMIDIN-5-CARBOXAMIDES 281 审中-公开
标题翻译：取代的吡咯烷-5-羧酰胺281
公开(公告)号：WO2009130496A1
公开(公告)日：2009-10-29
申请号：PCT/GB2009/050392
申请日：2009-04-20
申请人： ASTRAZENECA AB , ASTRAZENECA UK LIMITED , GILL, Adrian, Liam , LEACH, Andrew , PACKER, Martin , SCOTT, James, Stewart , SÖRME, Pernilla , SWALES, John, Gibbin , WHITTAMORE, Paul, Robert, Owen
发明人： GILL, Adrian, Liam , LEACH, Andrew , PACKER, Martin , SCOTT, James, Stewart , SÖRME, Pernilla , SWALES, John, Gibbin , WHITTAMORE, Paul, Robert, Owen
IPC分类号： C07D239/28 , C07D239/38 , C07D239/42 , C07D239/47 , C07D239/48 , C07D239/58 , C07D401/14 , C07D403/04 , C07D405/12 , C07D405/14 , C07D413/04 , C07D417/04 , C07D239/557 , A61K31/506 , A61P3/10
CPC分类号： C07D239/42 , C07D239/28 , C07D239/38 , C07D239/47 , C07D239/48 , C07D239/557 , C07D239/58 , C07D401/14 , C07D403/04 , C07D405/12 , C07D405/14 , C07D413/04 , C07D417/04
摘要： A compound of formula (I) and pharmaceutically-acceptable salts thereof wherein the variable groups are defined within; their use in the inhibition of 11βHSD1, processes for making them and pharmaceutical compositions comprising them are also described.
摘要翻译：式（I）化合物及其药学上可接受的盐，其中可变基团定义在其内; 还描述了其在抑制11βHSD1中的用途，其制备方法和包含它们的药物组合物。

22. 发明申请

WO2009024821A2 CHEMICAL COMPOUNDS 979 审中-公开
标题翻译：化学化合物979
公开(公告)号：WO2009024821A2
公开(公告)日：2009-02-26
申请号：PCT/GB2008/050716
申请日：2008-08-15
申请人： ASTRAZENECA AB , ASTRAZENECA UK LIMITED , BIRCH, Alan, Martin , BUTLIN, Roger, John , GILL, Adrian, Liam , GROOMBRIDGE, Samuel, David , PLOWRIGHT, Alleyn , WARING, Michael, James
发明人： BIRCH, Alan, Martin , BUTLIN, Roger, John , GILL, Adrian, Liam , GROOMBRIDGE, Samuel, David , PLOWRIGHT, Alleyn , WARING, Michael, James
IPC分类号： C07D413/12 , A61K31/4245 , A61P3/00
CPC分类号： C07D413/12
摘要： Compounds of formula (I), or pharmaceutically-acceptable salts and/or pro-drugs thereof, which inhibit acetyl CoA(acetyl coenzyme A):diacylglycerol acyltransferase (DGAT1) activity are provided, wherein n is 0 to 3; p is 0 or 1; q is 0 to 2; R 1 and R 2 are, for example, independently fluoro, chloro, bromo, cyano or (1-4C)alkyl; X is -O-, -S- or -NRa- wherein Ra is hydrogen or (1-4C)alkyl; R A1 and R A2 are, for example, independently hydrogen or (1-4C)alkyl; Ring A is a di-linked ring or ring system chosen from (4-6C)cycloalkane, (7- 10C)bicycloalkane and (8-12C)tricycloalkane each optionally substituted, for example, by one substituent selected from (1-4C)alkyl, (1-4C)alkoxy and (1-4C)alkoxy(1-4C)alkyl; or Ring A is phenylene optionally substituted, for example, by up to four substituents selected from fluoro, chloro, bromo, cyano, (1-4C)alkyl, (1-4C)alkoxy and (1- 4C)alkoxy(1-4C)alkyl; togetherwith processes for their preparation, pharmaceutical compositions containing them and their use as medicaments.
摘要翻译：提供了抑制乙酰CoA（乙酰辅酶A）：二酰基甘油酰基转移酶（DGAT1）活性的式（I）化合物或其药学上可接受的盐和/或前药，其中n为0-3; p为0或1; q为0〜2; R 1和R 2例如独立地为氟，氯，溴，氰基或（1-4C）烷基; X是-O - ， - S-或-NRa-，其中R a是氢或（1-4C）烷基; RA1和RA2例如独立地为氢或（1-4C）烷基; 环A是选自（4-6C）环烷烃，（7-10C）双环烷烃和（8-12C）三环烷烃的二联环或环系，其各自任选被例如选自（1-4C）的一个取代基取代，烷基，（1-4C）烷氧基和（1-4C）烷氧基（1-4C）烷基; 或环A是任选取代的亚苯基，例如至多四个选自氟，氯，溴，氰基，（1-4C）烷基，（1-4C）烷氧基和（1-4C）烷氧基（1-4C））烷基; 以及其制备方法，含有它们的药物组合物及其作为药物的用途。

23. 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。

24. 发明申请

WO2007077435A1 PHARMACEUTICAL COMPOUNDS 审中-公开
标题翻译：药物化合物
公开(公告)号：WO2007077435A1
公开(公告)日：2007-07-12
申请号：PCT/GB2006/004954
申请日：2006-12-29
申请人： ASTEX THERAPEUTICS LIMITED , BERDINI, Valerio , CURRY, Jayne, Elizabeth , GALLAGHER, Neil, James , GILL, Adrian, Liam , LYONS, John, Francis
发明人： BERDINI, Valerio , CURRY, Jayne, Elizabeth , GALLAGHER, Neil, James , GILL, Adrian, Liam , LYONS, John, Francis
IPC分类号： A61K31/4155 , A61K31/4184 , C07D403/04 , A61P35/00
CPC分类号： C07D403/04 , A61K31/4155 , A61K31/4184 , C07D401/14 , C07D403/14 , C07D405/14 , C07D413/14 , C07D487/04 , C07D491/056 , C07D513/04
摘要： The use of a compound for the manufacture of a medicament for the prophylaxis or treatment of: A. a disease state or condition mediated by a kinase which is BCR-abl, VEGFR, PDGFR, EGFR, Flt3, JAK (e.g. JAK2 or JAK3), C-abl, PDKl , Chk (e.g. Cbkl or Chk2), FGFR (e.g. FGFR3), Ret, Eph (e.g. EphB2 or EphB4), or Src (e.g. cSrc); or B. a cancer in which the cancer cells thereof contain a drug resistant kinase mutation which is: (a) a threonine gatekeeper mutation; or (b) a drug-resistant gatekeeper mutation; or (c)an imatinib resistant mutation; or (d) a nilotinib resistant mutation; or (e) a dasatinib resistant mutation; or (f) a T670I mutation in KIT; or (g) a T674I mutation in PDGFR; or (h) T790M mutation in EGFR; or (i) a T315I mutation in abl; or C. a cancer which expresses a mutated molecular target which is a mutated form of BCRabl, c-kit, PDGF, EGF receptor or ErbB2; or D. a disease mediated by a kinase containing a mutation in a region of the protein that binds to or interacts with other cancer agents but does not bind to or interact with the compounds of formula (I) or (I’), for example a mutated kinase selected from c-abl, c-kit, PDGFR including PDGFR-beta and PDGFR-alpha, and ErbB family members such as EGFR (ErbBl), HER2 (ErbB2), ErbB3, and ErbB4, members of the Ephrin receptor family including EphA1, EphA2, EphA3, EphA4, EphA5, EphA8, EphA10, EphB1, EphB2, EphB3, EphB5, EphB6, c-Src and kinases of the JAK family such as TYK2; wherein the compound is a compound of the formula (I or I’) : or a salt, solvate, tautomer or N-oxide thereof; wherein R 0’ , R 1 , R 1’ , R 2’ , R 3’ , R 4’ , A’, X’, E, A and M are as defined in the claims.
摘要翻译：化合物用于制备用于预防或治疗以下药物的用途：A.由BCR-abl，VEGFR，PDGFR，EGFR，Flt3，JAK（例如JAK2或JAK3）的激酶介导的疾病状态或病症，，C-abl，PDK1，Chk（例如Cbk1或Chk2），FGFR（例如FGFR3），Ret，Eph（例如EphB2或EphB4）或Src（例如cSrc）; 或B.一种其癌细胞含有耐药性激酶突变的癌症，其为：（a）苏氨酸关守突变; 或（b）耐药性守门人突变; 或（c）伊马替尼耐药突变; 或（d）尼洛替尼耐药突变; 或（e）达沙替尼抗性突变; 或（f）KIT中的T670I突变; 或（g）PDGFR中的T674I突变; 或（h）EGFR中的T790M突变; 或（i）abl中的T315I突变; 或C.表达突变形式的BCRab1，c-kit，PDGF，EGF受体或ErbB2的突变分子靶的癌症; 或D.由包含与其它癌症药物结合或与其它癌症药剂相互作用而不与式（I）或（I'）化合物结合或相互作用的蛋白质区域中的突变的激酶介导的疾病，例如选自c-abl，c-kit，PDGFR（包括PDGFR-β和PDGFR-α）的突变激酶和ErbB家族成员如EGFR（ErbB1），HER2（ErbB2），ErbB3和ErbB4，Ephrin受体家族的成员包括EK1A1，EphA2，EphA3，EphA4，EphA5，EphA8，EphA10，EphB1，EphB2，EphB3，EphB5，EphB6，c-Src和JAK家族的激酶如TYK2; 其中所述化合物是式（I或I'）的化合物：或其盐，溶剂合物，互变异构体或N-氧化物; 其中R 0'，R'1，R 1'，R 2'，R 3'， R 4，S 4，A'，X'，E，A和M如权利要求中所定义。

25. 发明申请

WO2006070195A8 PYRAZOLE COMPOUNDS THAT MODULATE THE ACTIVITY OF CDK, GSK AND AURORA KINASES 审中-公开
标题翻译：调节CDK，GSK和AURORA KINASES活性的吡咯化合物
公开(公告)号：WO2006070195A8
公开(公告)日：2006-08-24
申请号：PCT/GB2005005097
申请日：2005-12-30
申请人： ASTEX THERAPEUTICS LTD , BERDINI VALERIO , CARR MARIA GRAZIA , GILL ADRIAN LIAM , HOWARD STEVEN , NAVARRO EVA FIGUEROA , TREWARTHA GARY , REES DAVID CHARLES , VINKOVIC MLADEN , WYATT PAUL GRAHAM
发明人： BERDINI VALERIO , CARR MARIA GRAZIA , GILL ADRIAN LIAM , HOWARD STEVEN , NAVARRO EVA FIGUEROA , TREWARTHA GARY , REES DAVID CHARLES , VINKOVIC MLADEN , WYATT PAUL GRAHAM
IPC分类号： C07D403/04 , A61K31/4184 , A61P35/00 , C07D407/14 , C07D513/04
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。

26. 发明申请

WO2006077416A1 PYRAZOLE DERIVATIVES FOR THE INHIBITION OF CDK' S AND GSK' S 审中-公开
标题翻译：用于抑制CDK和GSK'S的吡唑衍生物
公开(公告)号：WO2006077416A1
公开(公告)日：2006-07-27
申请号：PCT/GB2006/000193
申请日：2006-01-20
申请人： ASTEX THERAPEUTICS LIMITED , WYATT, Paul, Graham , BERDINI, Valerio , GILL, Adrian, Liam , TREWARTHA, Gary , WOODHEAD, Andrew, James
发明人： WYATT, Paul, Graham , BERDINI, Valerio , GILL, Adrian, Liam , TREWARTHA, Gary , WOODHEAD, Andrew, James
IPC分类号： C07D401/14 , A61K31/44 , A61P35/00 , A01N43/56
CPC分类号： C07D231/14 , C07D231/40 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/12 , C07D417/14
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。

27. 发明申请

WO2006070195A1 PYRAZOLE COMPOUNDS THAT MODULATE THE ACTIVITY OF CDK, GSK AND AURORA KINASIS 审中-公开
标题翻译：调节CDK，GSK和AURORA KINASIS的活性的吡咯化合物
公开(公告)号：WO2006070195A1
公开(公告)日：2006-07-06
申请号：PCT/GB2005/005097
申请日：2005-12-30
申请人： ASTEX THERAPEUTICS LIMITED , BERDINI, Valerio , CARR, Maria, Grazia , GILL, Adrian, Liam , HOWARD, Steven , NAVARRO, Eva, Figueroa , TREWARTHA, Gary , REES, David, Charles , VINKOVIC, Mladen , WYATT, Paul, Graham
发明人： BERDINI, Valerio , CARR, Maria, Grazia , GILL, Adrian, Liam , HOWARD, Steven , NAVARRO, Eva, Figueroa , TREWARTHA, Gary , REES, David, Charles , VINKOVIC, Mladen , WYATT, Paul, Graham
IPC分类号： C07D403/04 , C07D513/04 , C07D407/14 , A61K31/4184 , A61P35/00
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。

28. 发明申请

WO2005012256A1 3, 4-DISUBSTITUTED 1H-PYRAZOLE COMPOUNDS AND THEIR USE AS CYCLIN DEPENDENT KINASES (CDK) AND GLYCOGEN SYNTHASE KINASE-3 (GSK-3) MODULATORS 审中-公开
标题翻译： 3，4-取代的1H-吡唑化合物及其作为循环激酶（CDK）和GLYCOGEN SYNTHASE KINASE-3（GSK-3）调节剂的用途
公开(公告)号：WO2005012256A1
公开(公告)日：2005-02-10
申请号：PCT/GB2004/003179
申请日：2004-07-22
申请人： ASTEX TECHNOLOGY LIMITED , BERDINI, Valerio , O'BRIEN, Michael, Alistair , CARR, Maria, Grazia , EARLY, Theresa, Rachel , NAVARRO, Eva, Figueroa , GILL, Adrian, Liam , TREWARTHA, Gary , WOOLFORD, Alison, Jo-Anne , WOODHEAD, Andrew, James , WYATT, Paul, Graham
发明人： BERDINI, Valerio , O'BRIEN, Michael, Alistair , CARR, Maria, Grazia , EARLY, Theresa, Rachel , NAVARRO, Eva, Figueroa , GILL, Adrian, Liam , TREWARTHA, Gary , WOOLFORD, Alison, Jo-Anne , WOODHEAD, Andrew, James , WYATT, Paul, Graham
IPC分类号： C07D231/38
CPC分类号： C07D231/38 , A61K31/415 , A61K31/4152 , A61K31/4155 , A61K31/416 , A61K31/4178 , A61K31/4196 , A61K31/4439 , A61K31/454 , A61K31/496 , A61K31/5377 , A61K31/541 , A61K45/06 , C04B35/632 , C07D231/14 , C07D231/40 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D453/02 , C07D471/04
摘要： The invention provides compounds of the formula (0) or salts or tautomers or N-oxides or solvates thereof for use in the prophylaxis or treatment of disease states and conditions such as cancers mediated by cyclin-dependent kinase and glycogen synthase kinase-3. Formula (0). In formula (0): X is a group R 1 -A-NR 4 - or a 5- or 6-membered carbocyclic or heterocyclic ring; A is a bond, S0 2 , C=O, NR g (C=O) or O(C=O) wherein R g is hydrogen or C 1-4 hydrocarbyl optionally substituted by hydroxy or C 1-4 alkoxy; Y is a bond or an alkylene chain of 1, 2 or 3 carbon atoms in length; R 1 is hydrogen; a carbocyclic or heterocyclic group having from 3 to 12 ring members; or a C 1-8 hydrocarbyl group optionally substituted by one or more substituents selected from halogen (e.g. fluorine), hydroxy, C 1-4 hydrocarbyloxy, amino, mono- or di-C 1-4 hydrocarbylamino, and carbocyclic or heterocyclic groups having from 3 to 12 ring members, and wherein 1 or 2 of the carbon atoms of the hydrocarbyl group may optionally be replaced by an atom or group selected from 0, S, NH, SO, S0 2 ; R 2 is hydrogen; halogen; C 1-4 alkoxy (e.g. methoxy); or a C 1-4 hydrocarbyl group optionally substituted by halogen (e.g. fluorine), hydroxyl or C 1-4 alkoxy (e.g. methoxy); R 3 is selected from hydrogen and carbocyclic and heterocyclic groups having from 3 to 12 ring members; and R 4 is hydrogen or a C 1-4 hydrocarbyl group optionally substituted by halogen (e.g. fluorine), hydroxyl or C 1-4 alkoxy (e.g. methoxy).
摘要翻译：本发明提供式（O）的化合物或其盐或互变异构体或N-氧化物或溶剂合物，用于预防或治疗疾病状态和病症，例如由细胞周期蛋白依赖性激酶和糖原合酶激酶-3介导的癌症。公式（0）。在式（0）中：X是基团R 1 -A-NR 4 - 或5或6元碳环或杂环; A是键，SO 2，C = O，NR g（C = O）或O（C = O），其中R g是氢或任选被羟基或C 1-4烷氧基取代的C 1-4烃基; Y是长度为1,2或3个碳原子的键或亚烷基链; R 1是氢; 具有3-12个环成员的碳环或杂环基; 或任选被一个或多个选自卤素（例如氟），羟基，C 1-4烃氧基，氨基，单 - 或二-C 1-4烃基氨基的取代基取代的C 1-8烃基，以及具有3至 12个环成员，并且其中烃基中的1或2个碳原子可以任选地被选自0，S，NH，SO，SO 2的原子或基团取代; R 2是氢; 卤素; C 1-4烷氧基（如甲氧基）; 或任选被卤素（例如氟），羟基或C 1-4烷氧基（例如甲氧基）取代的C 1-4烃基; R 3选自具有3至12个环成员的氢和碳环和杂环基; 并且R 4是氢或任选被卤素（例如氟），羟基或C 1-4烷氧基（例如甲氧基）取代的C 1-4烃基。

29. 发明申请

WO2006067466A3 PYRAZINES AND PYRIDINES AND DERIVATIVES THEREOF AS THERAPEUTIC COMPOUNDS 审中-公开
标题翻译：作为治疗化合物的吡咯并吡啶及其衍生物
公开(公告)号：WO2006067466A3
公开(公告)日：2007-07-05
申请号：PCT/GB2005005011
申请日：2005-12-22
申请人： WELLCOME TRUST LTD , SPRINGER CAROLINE JOY , NICULESCU-DUVAZ ION , ROMAN VELA ESTEBAN , GILL ADRIAN LIAM , TAYLOR RICHARD DAVID , MARAIS RICHARD MALCOLM
发明人： SPRINGER CAROLINE JOY , NICULESCU-DUVAZ ION , ROMAN VELA ESTEBAN , GILL ADRIAN LIAM , TAYLOR RICHARD DAVID , MARAIS RICHARD MALCOLM
IPC分类号： C07D241/20 , A61K31/444 , A61K31/497 , A61P35/00 , C07D213/74 , C07D317/46 , C07D319/18 , C07D321/10 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/12 , C07D409/12 , C07D413/12 , C07D417/12
CPC分类号： C07D213/74 , C07D241/20 , C07D317/46 , C07D319/18 , C07D321/10 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/12 , C07D409/12 , C07D413/12 , C07D417/12
摘要： The present invention pertains to certain pyrazines and pyridines, and dervatives thereof, which, inter alia, inhibit RAF (e.g., B RAF) activity, inhibit cell proliferation, treat cancer, etc., and more particularly to compounds of the formulae: (I) wherein: Q is independently -N= or -CH=; one of R P2 and R P3 is independently a group of the formula -J 1 -L 1 -Z; wherein: if Q is -N=, then -J 1 -L 1 -Z is independently: -NH-Z; -O-Z; or S-Z; if Q is -CH=, then -J 1 -L 1 -Z is independently: -NH-(CH 2 ) n -Z, wherein n is independently 0 or 1; -O-Z; or -S-Z; Z is independently: C 6-14 carboaryl, C 5-14 heteroaryl, C 3-12 carbocyclic, C 3-12 heterocyclic; and is independently unsubstituted or substituted; the other of R P2 and R P3 is independently -H, -NHR N1 , or -NHC(=O)R N2 ; wherein: R N1 , if present, is independently -H or aliphatic saturated C 1-4 alkyl; R N2 , if present, is independently -H or aliphatic saturated C 1-4 alkyl; one of R P5 and R P6 is independently a group of the formula -W-Y; wherein: W is independently: a covalent bond; -NR N4 -, -O-, -S-, -C(=O)-, -CH 2 -; -NR N4 -CH 2 -, -O-CH 2 -, -S-CH 2 -, -C(=O)-CH 2 -, -(CH 2 ) 2 -; -CH 2 -NR N4 -, -CH 2 -O-, -CH 2 -S-, or -CH 2 -C(=O)-; wherein R N4 , if present, is independently -H or aliphatic saturated C 1-4 alkyl; Y is independently: C 6-14 carboaryl, C 5-14 heteroaryl, C 3-12 carbocyclic, C 3-12 heterocyclic; and is independently unsubstituted or substituted; the other of R P5 and R P6 is independently -H; and pharmaceutically acceptable salts, solvates, amides, esters, ethers, N-oxides, chemically protected forms, and prodrugs thereof. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, e.g., both in vitro and in vivo, to inhibit RAF (e.g., B-RAF) activity, to inhibit receptor tyrosine kinase (RTK) activity, to inhibit cell proliferation, and in the treatment of diseases and conditions that are ameliorated by the inhibition of RAF, RTK, etc., proliferative conditions such as cancer (e.g., colorectal cancer, melanoma), etc.
摘要翻译：本发明涉及某些吡嗪和吡啶及其衍生物，其特别是抑制RAF（例如，B RAF）活性，抑制细胞增殖，治疗癌症等，更具体地涉及下式的化合物：（I ）其中：Q独立地为-N =或-CH =; R“P2”和“R”中的一个独立地是式-I-1-L-1-Z的基团 ; 其中：如果Q是-N =，则-J 1 -L 1 -Z独立地是：-NH-Z; -O-Z; 或S-Z; 如果Q是-CH =，则-J 1 -L 1 -Z独立地是：-NH-（CH 2 CH 2） n -Z，其中n独立地为0或1; -O-Z; 或-S-Z; Z独立地为：C 6-14芳烷基，C 5-14杂芳基，C 3-12碳环，C 3-12 杂环; 并且独立地是未取代的或取代的; R 2 P2和R 3 P 2中的另一个独立地为-H，-NHR 1 N 1或-NHC（= O）R N 2 ; 其中：如果存在，R“独立地为-H或脂族饱和C 1-4烷基; 如果存在，则R 2独立地为-H或脂族饱和C 1-4烷基; R 5 P 5和R 6 P 6中的一个独立地是式-W-Y的基团; 其中：W独立地为：共价键; -NR N - ， - O - ， - S - ， - C（= O） - ， - CH 2 - 。 -NR N4 - CH 2 - ， - O-CH 2 - ， - S-CH 2 - ， - -C（= O）-CH 2 - ， - （CH 2）2 - ; - （CH 2）2 - -CH 2，-NR N 4 - ， - CH 2 -O - ， - CH 2 -S-，或-CH 2 -C（= O） - ; 其中R“N4”（如果存在）独立地是-H或脂族饱和C 1-4烷基; Y独立地为：C 6-14碳芳基，C 5-14杂芳基，C 3-12碳环，C 3-12 杂环基; 并且独立地是未取代的或取代的; R“P5”和“R”P6中的另一个独立地是-H; 酰胺，酯，醚，N-氧化物，化学保护形式及其前体药物。本发明还涉及包含这些化合物的药物组合物，以及这些化合物和组合物在体外和体内两者抑制RAF（例如B-RAF）活性抑制受体酪氨酸激酶（RTK）的用途，活性，抑制细胞增殖，以及通过抑制RAF，RTK等改善增殖条件如癌症（例如结肠直肠癌，黑素瘤）等的疾病和病症的治疗。

30. 发明申请

WO2006003440A1 3,4-DISUBSTITUTED PYRAZOLES AS CYCLIN DEPENDENT KINASES (CDK) OR AURORA KINASE OR GLYCOGEN SYNTHASE 3 (GSK-3) INHIBITORS 审中-公开
标题翻译：作为循环激素（CDK）或者AURORA KINASE或GLYCOGEN SYNTHASE 3（GSK-3）抑制剂的3,4-取代的吡咯烷
公开(公告)号：WO2006003440A1
公开(公告)日：2006-01-12
申请号：PCT/GB2005/002629
申请日：2005-07-05
申请人： ASTEX TECHNOLOGY LIMITED , GILL, Adrian, Liam , CARR, Maria, Grazia , O'BRIEN, Michael, Alistair , WYATT, Paul, Graham , BERDINI, Valerio
发明人： GILL, Adrian, Liam , CARR, Maria, Grazia , O'BRIEN, Michael, Alistair , WYATT, Paul, Graham , BERDINI, Valerio
IPC分类号： C07D471/04
CPC分类号： C07D471/04 , C07D487/04 , C07D495/04
摘要： The invention provides compounds of the formula (I); or salts or solvates or N-oxides thereof; wherein: R q is selected from groups (a), (b) and (c); the asterisk denoting the point of attachment to the pyrazole ring; X is N or CR 5 ; X" is NR 4 ', O, S or S(O); A is a bond or -(CH 2 ) m -(B) n -; B is C=O, NR g (C=O) or O(C=O) wherein R g is hydrogen or C 1-4 hydrocarbyl optionally substituted by hydroxy or C 1-4 alkoxy; m is 0, 1 or 2; n is 0 or 1; R 0 is hydrogen or, together with NR g when present, forms a group -(CH 2 ) p - wherein p is 2 to 4; and R 1 to R 6b are as defined in the description. Compounds of the formula (I) have activity as inhibitors of CDK, aurora and GSK-3 kinases are useful in treating or preventing diseases such as cancers that are mediated by the said kinases.
摘要翻译：本发明提供式（I）化合物; 或其盐或溶剂合物或N-氧化物; 其中：R

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