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11. 发明申请

WO2006077419A1 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：WO2006077419A1
公开(公告)日：2006-07-27
申请号：PCT/GB2006/000196
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 , NAVARRO, Eva, Figueroa , O'BRIEN, Michael, Alistair , PHILLIPS, Theresa, Rachel
发明人： WYATT, Paul, Graham , BERDINI, Valerio , GILL, Adrian, Liam , TREWARTHA, Gary , WOODHEAD, Andrew, James , NAVARRO, Eva, Figueroa , O'BRIEN, Michael, Alistair , PHILLIPS, Theresa, Rachel
IPC分类号： C07D453/02 , C07D401/14 , C07D401/12 , A61K31/44 , A61K31/4545 , A61K31/506 , 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 compounds of the formula (I) or a salt, tautomer, solvate or N-oxides thereof; wherein: R 1 is selected from (a) 2,6-dichlorophenyl; (b) 2,6-difluorophenyl; (c) a 2,3,6-trisubstituted phenyl group wherein the substituents are fluorine, chlorine, methyl or methoxy; and (d) a group R 0 wherein R 0 is a 3-12 membered carbocyclic or heterocyclic group; or optionally substituted C 1-8 hydrocarbyl; R 2a and R 2b are each hydrogen or methyl; and R 3 is as defined in the claims. The compounds have activity as inhibitors of Cyclin Dependent Kinases (CDK) and Glycogen Synthase Kinases (GSK) kinases and are useful in the treatment or prophylaxis of disease states or conditions mediated by the kinases.
摘要翻译：本发明提供式（I）化合物或其盐，互变异构体，溶剂合物或N-氧化物; 其中：R 1选自（a）2,6-二氯苯基; （b）2,6-二氟苯基; （c）2,3,6-三取代的苯基，其中取代基是氟，氯，甲基或甲氧基; 和（d）R 0为0的基团，其中R 0为3-12元碳环或杂环基; 或任选取代的C 1-8烃基; R 2a和R 2b各自为氢或甲基; R 3和R 3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（CDK）和糖原合酶激酶（GSK）激酶抑制剂的活性，可用于治疗或预防由激酶介导的疾病状态或病症。

12. 发明申请

WO2005002576A8 IMIDAZOLE DERIVATIVES AND THEIR USE AS PROTEIN KINASES INHIBITORS 审中-公开
标题翻译：咪唑衍生物及其作为蛋白激酶抑制剂的用途
公开(公告)号：WO2005002576A8
公开(公告)日：2005-09-22
申请号：PCT/GB2004002913
申请日：2004-07-05
申请人： ASTEX THERAPEUTICS LTD , BERDINI VALERIO , WOODHEAD ANDREW JAMES , WYATT PAUL GRAHAM , O'BRIEN MICHAEL ALISTAIR , NAVARRO EVA FIGUEROA
发明人： BERDINI VALERIO , WOODHEAD ANDREW JAMES , WYATT PAUL GRAHAM , O'BRIEN MICHAEL ALISTAIR , NAVARRO EVA FIGUEROA
IPC分类号： A61K31/00 , A61K31/4184 , A61P31/10 , A61P35/00 , C07D403/04
CPC分类号： C07D401/14 , A61K31/00 , A61K31/4184 , C07D403/04 , C07D405/14 , C07D409/14 , C07D413/14
摘要： The invention provides a compound of the formula (I) or a salt, N-oxide or solvate thereof. The compounds have activity against cyclin dependent kinases, glycogen synthase kinase and Auroa kinases.
摘要翻译：本发明提供式（I）化合物或其盐，N-氧化物或其溶剂合物。该化合物具有针对细胞周期蛋白依赖性激酶，糖原合成酶激酶和Auroa激酶的活性。

13. 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。

14. 发明申请

WO2006008545A2 PHARMACEUTICAL COMPOUNDS 审中-公开
标题翻译：药物化合物
公开(公告)号：WO2006008545A2
公开(公告)日：2006-01-26
申请号：PCT/GB2005/002888
申请日：2005-07-22
申请人： ASTEX THERAPEUTICS LIMITED , BERDINI, Valerio , EARLY, Theresa, Rachael , O'BRIEN, Michael, Alistair , WOODHEAD, Andrew, James , WYATT, Paul, Graham
发明人： BERDINI, Valerio , EARLY, Theresa, Rachael , O'BRIEN, Michael, Alistair , WOODHEAD, Andrew, James , WYATT, Paul, Graham
IPC分类号： A61K31/00
CPC分类号： C07D275/03 , C07D277/56 , C07D417/12 , C07D417/14
摘要： The invention provides a compound for use in the prophylaxis or treatment of a disease state or condition mediated by a cyclin dependent kinase, the compound having the formula (I): (I) and salts, tautomers, N-oxides or solvates thereof; wherein A is a bond, 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; Q is S or CR 2 ; J is S or CH; provided that one of Q and J is S, and the other of Q and J is not S; when Q is S, there is a double bond between the ring carbon atoms “a” and “b” and a double bond between the ring nitrogen N and J; and when J is S, there is a double bond between Q and the ring carbon atom “a” and a double bond between the ring nitrogen N and the ring carbon atom “b”; and R 1 to R 4 are as defined in the claims.
摘要翻译：本发明提供一种用于预防或治疗由细胞周期蛋白依赖性激酶介导的疾病状态或病症的化合物，具有式（I）：（I）的化合物及其盐，互变异构体，N-氧化物或溶剂合物; 其中A是键，C = O，NR（C = O）或O（C = O），其中R g是氢或C 1〜任选被羟基或C 1-4烷氧基取代的烃基; Y是长度为1,2或3个碳原子的键或亚烷基链; Q是S或CR <2>; J为S或CH; 假设Q和J中的一个是S，Q和J中的另一个不是S; 当Q是S时，环碳原子“a”和“b”之间有双键，环氮N与J之间有双键; 当J为S时，Q与环碳原子“a”之间存在双键，环氮N与环碳原子“b”之间具有双键。和R 1至R 4如权利要求中所定义。

15. 发明申请

WO2005002576A3 BENZIMIDAZOLE DERIVATIVES AND THEIR USE AS ROTEIN KINASES INHIBITORS 审中-公开
标题翻译：苯并咪唑衍生物及其作为罗茨金杀伤剂的用途
公开(公告)号：WO2005002576A3
公开(公告)日：2005-06-16
申请号：PCT/GB2004002913
申请日：2004-07-05
申请人： ASTEX TECHNOLOGY LTD , BERDINI VALERIO , WOODHEAD ANDREW JAMES , WYATT PAUL GRAHAM , O'BRIEN MICHAEL ALISTAIR , NAVARRO EVA FIGUEROA
发明人： BERDINI VALERIO , WOODHEAD ANDREW JAMES , WYATT PAUL GRAHAM , O'BRIEN MICHAEL ALISTAIR , NAVARRO EVA FIGUEROA
IPC分类号： A61K31/00 , A61K31/4184 , A61P31/10 , A61P35/00 , C07D403/04
CPC分类号： C07D401/14 , A61K31/00 , A61K31/4184 , C07D403/04 , C07D405/14 , C07D409/14 , C07D413/14
摘要： The invention provides a compound of the formula (I) or a salt, N-oxide or solvate thereof. The compounds have activity against cyclin dependent kinases glycogen synthase kinase and Auroa kinases.
摘要翻译：本发明提供式（I）化合物或其盐，N-氧化物或其溶剂合物。该化合物具有抗细胞周期蛋白依赖性激酶糖原合酶激酶和Auroa激酶的活性。

16. 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。

17. 发明申请

WO2008044034A1 HYDROBENZAMIDE DERIVATIVES AS INHIBITORS OF HSP90 审中-公开
标题翻译：盐酸衍生物作为HSP90的抑制剂
公开(公告)号：WO2008044034A1
公开(公告)日：2008-04-17
申请号：PCT/GB2007/003871
申请日：2007-10-12
申请人： ASTEX THERAPEUTICS LIMITED , FREDERICKSON, Martyn , LYONS, John, Francis , THOMPSON, Neil, Thomas , VINKOVIC, Mladen , WILLIAMS, Brian , WOODHEAD, Andrew James , WOOLFORD, Alison, Jo-Anne
发明人： FREDERICKSON, Martyn , LYONS, John, Francis , THOMPSON, Neil, Thomas , VINKOVIC, Mladen , WILLIAMS, Brian , WOODHEAD, Andrew James , WOOLFORD, Alison, Jo-Anne
IPC分类号： C07D209/44 , C07C65/05 , C07C69/02 , A61P35/00 , A61K31/496
CPC分类号： C07C67/317 , C07C59/08 , C07C67/313 , C07C69/92 , C07C235/60 , C07D209/44
摘要： The invention provides an acid addition salt of a compound of the formula (1) Also provided by the invention are processes for preparing the compound of formula (1) and alkyl analogues thereof, novel intermediates for use in the process and methods for preparing the intermediates. The invention also provides new medical uses of compounds of the formula (1) and its ethyl analogue.
摘要翻译：本发明提供式（1）化合物的酸加成盐本发明还提供了制备式（1）化合物及其烷基类似物的方法，用于该方法的新中间体和制备中间体的方法。本发明还提供式（1）化合物及其乙基类似物的新的医学用途。

18. 发明申请

WO2008044027A2 PHARMACEUTICAL COMPOUNDS 审中-公开
标题翻译：药物化合物
公开(公告)号：WO2008044027A2
公开(公告)日：2008-04-17
申请号：PCT/GB2007/003860
申请日：2007-10-12
申请人： ASTEX THERAPEUTICS LIMITED , CONGREVE, Miles Stuart , FAZAL, Lyndsey Helen , FREDERICKSON, Martyn , MURRAY, Christopher William , O'BRIEN, Michael Alistair , WOODHEAD, Andrew James , LYONS, John, Francis , THOMPSON, Neil Thomas
发明人： CONGREVE, Miles Stuart , FAZAL, Lyndsey Helen , FREDERICKSON, Martyn , MURRAY, Christopher William , O'BRIEN, Michael Alistair , WOODHEAD, Andrew James , LYONS, John, Francis , THOMPSON, Neil Thomas
CPC分类号： C07D403/06 , C07D209/08 , C07D209/44 , C07D215/08 , C07D215/14 , C07D217/06 , C07D401/04 , C07D401/12 , C07D401/14 , C07D471/04 , C07D471/08 , C07D471/10 , C07D491/08 , C07D491/10 , C07D491/107 , C07D491/18
摘要： The invention provides a compound for use in medicine, the compound being a compound of the formula (Vl 0 ) or a salt, solvate, tautomer or N-oxide thereof: wherein the bicyclic group: is selected from the structures C1, C5 and C6: wherein n is 0, 1, 2 or 3; R 1 : is„ hydrogen, hydroxy, or O-R z; R 2a is hydroxy, methoxy or O-R z; provided that at least one of R 1 and R 2a is O-R z; R z is L p -R p1 ; SO 3 H; a glucuronide residue; a mono-, di- or tripeptide residue; or; L p is a bond, C=O, (C=O)O, (C=O)NR p1 or S(O) x NR p1 ; x is 1 or 2; R p1 is hydrogen or a an optionally substituted C 1-25 hydrocarbyl group containing 0, 1 or 2 carbocyclic rings and 0, 1, 2, 3, 4, 5 or 6 carbon-carbon multiple bonds, provided that R p1 is not hydrogen when L p is a bond, C=O or (C=O)O; and provided also that O-R z does not contain an 0-0 moiety; and excluding compounds wherein R1 is hydroxy and R2a is methoxy; Rp2 and Rp3 are the same or different and each is a group R p1; and R 3 , R 4a , R 8 and R 10 are defined in the claims. The compounds of formula (Vl0) are pro-drugs of parent compounds wherein R 1 and/or R 2a are hydroxy, wherein the parent compounds have Hsp90 inhibiting activity.
摘要翻译：本发明提供了一种用于医药的化合物，该化合物为下式化合物：其盐，溶剂化物，互变异构体或N-氧化物：其中双环基团选自：结构C1，C5和C6：其中n为0,1,2或3; R 1是氢，羟基或OR z; R 2是羟基，甲氧基或OR z; O / O >条件是R 1和R 2 2中的至少一个是OR z; R z是L SUP > p p> SO 3 H;葡糖苷酸残基;单 - ，二 - 或三肽残基;或●L < / SUP>是键，C = O，（C = O）O，（C = O）NR P1或S（O）x NR 6 x为1或2; R p1为氢或任选取代的含0,1或2个碳环的C 1-25烃基和0 ，1,2,3,4,5或6个碳 - 碳多重键，条件是当P = O时，R p2不是氢，C = O或（C = O）O;并且也提供OR 0不含0-0部分;并且不包括其中R 1是羟基并且R 2a是甲氧基的化合物; Rp2和Rp3相同或不同，每个是基团R p1; R 3和R 3，R 4a，R 8和R 10 是定义在权利要求中。式（V10）化合物是其中R 1和/或R 2a的羟基的母体化合物的前体药物，其中母体化合物具有Hsp90抑制活性。

19. 发明申请

WO2005002552A3 BENZIMIDAZOLE DERIVATIVES AND THEIR USE AS PROTEIN KINASES INHIBITORS 审中-公开
标题翻译：苯并咪唑衍生物及其作为蛋白激酶抑制剂的用途
公开(公告)号：WO2005002552A3
公开(公告)日：2005-06-16
申请号：PCT/GB2004002824
申请日：2004-07-05
申请人： ASTEX TECHNOLOGY LTD , BERDINI VALERIO , O'BRIEN MICHAEL ALISTAIR , CARR MARIA GRAZIA , EARLY THERESA RACHEL , NAVARRO EVA FIGUEROA , GILL ADRIAN LIAM , HOWARD STEVEN , TREWARTHA GARY , WOOLFORD ALISON JO-ANNE , WOODHEAD ANDREW JAMES , WYATT PAUL
发明人： BERDINI VALERIO , O'BRIEN MICHAEL ALISTAIR , CARR MARIA GRAZIA , EARLY THERESA RACHEL , NAVARRO EVA FIGUEROA , GILL ADRIAN LIAM , HOWARD STEVEN , TREWARTHA GARY , WOOLFORD ALISON JO-ANNE , WOODHEAD ANDREW JAMES , WYATT PAUL
IPC分类号： A61K31/00 , A61K31/4184 , A61P31/10 , A61P35/00 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D403/04
CPC分类号： A61K31/5377 , A61K31/00 , A61K31/4184 , A61K45/06 , C07D401/14 , C07D403/04 , C07D405/14 , C07D409/14 , C07D413/14 , C07D471/04 , C07D513/04
摘要： The invention provides compounds having activity as inhibitors of cyclin dependent kinases, glycogen synthase kinase-3 and Aurora kinases for use in the treatment of disease states and conditions such as cancer that are mediated by the kinases. The compounds have the general formula (I). Also included within formula (I) are the salts, solvates and N-oxides of the compounds.
摘要翻译：本发明提供具有作为细胞周期蛋白依赖性激酶抑制剂，糖原合成酶激酶-3和极光激酶的活性的化合物，其用于治疗由激酶介导的疾病状态和病症如癌症。化合物具有通式（I）。式（I）中还包括化合物的盐，溶剂合物和N-氧化物。

20. 发明申请

WO2005002673A1 RAF KINASE INHIBITORS 审中-公开
标题翻译： RAF激酶抑制剂
公开(公告)号：WO2005002673A1
公开(公告)日：2005-01-13
申请号：PCT/GB2004/002877
申请日：2004-07-02
申请人： ASTEX TECHNOLOGY LIMITED , GILL, Adrian, Liam , WOODHEAD, Steven, John , WOODHEAD, Andrew, James , FREDERICKSON, Martyn , PADOVA, Alessandro , APAYA, Robert, Patrick
发明人： GILL, Adrian, Liam , WOODHEAD, Steven, John , WOODHEAD, Andrew, James , FREDERICKSON, Martyn , PADOVA, Alessandro , APAYA, Robert, Patrick
IPC分类号： A61P35/00
CPC分类号： A61K31/4412 , A61K31/4965 , Y02A50/411
摘要： The use of a compound of the formula I or a pharmaceutically acceptable salt or solvate thereof, for the manufacture of a medicament for use in the treatment of a condition ameliorated by the inhibition of raf kinase, wherein: -X=Y- is selected from -CR 2 =CR 3 - and -CR 2 =N-; R 1 is selected from H, halo, NRR', NHC (=O)R, NHC (=O)NRR', NH 2 SO 2 R, and C (=O)NRR', where R and R' are independently selected from H and C 1-4 alkyl, and are optionally substituted by OH, NH 2 , SO 2 -NH 2 , C 5-20 carboaryl, C 5-20 heteroaryl and C 3-20 heterocyclyl, or may together form, with the nitrogen atom to which they are attached, an optionally substituted nitrogen containing C 5-7 heterocyclyl group; R 2 and R 3 (where present) are independently selected from H, optionally substituted C 1-7 alkyl, optionally substituted C 5-20 aryl, optionally substituted C 3-20 heterocyclyl, halo, amino, amido, hydroxy, ether, thio, thioether, acylamido, ureido and sulfonamino; R 4 an optionally substituted C 5-20 carboaryl or C 5-20 heteroaryl group; and R 5 is selected from R 5 ', halo, NHR 5' , C(=O)NHR 5' , OR 5 ', SR 5' , NHC (=O)R 5' , NHC (=O)NHR 5' , NHS (=O) 2 R 5' , wherein R 5' is H or C 1-3 alkyl (optionally substituted by halo, NH 2 , OH, SH).
摘要翻译：使用式I化合物或其药学上可接受的盐或溶剂合物，用于制备用于治疗通过抑制raf激酶改善的病症的药物，其中：-X = Y-选自 -CR 2 = CR 3 - 和-CR 2 = N-; R 1选自H，卤素，NRR'，NHC（= O）R，NHC（= O）NRR'，NH2SO2R和C（= O）NRR'，其中R和R'独立地选自H 和C 1-4烷基，并且任选地被OH，NH 2，SO 2 -NH 2，C 5-20碳酰基，C 5-20杂芳基和C 3-20杂环基取代，或者可以与它们所连接的氮原子一起形成一个任选取代的含有C 5-7杂环基的氮; R 2和R 3（如果存在）独立地选自H，任选取代的C 1-7烷基，任选取代的C 5-20芳基，任选取代的C 3-20杂环基，卤素，氨基，酰胺基，羟基，醚，硫代，硫醚，酰氨基，脲基和磺氨基; R 4是任选取代的C 5-20碳芳基或C 5-20杂芳基; R 5选自R 5，卤素，NHR 5，C（= O）NHR 5，OR 5，SR 5，NHC（= O） R 5，NHC（= O）NHR 5，NHS（= O）2 R 5，其中R 5'是H或C 1-3烷基（任选地被卤素，NH 2，OH ，SH）。

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