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1. 发明专利

TW200602046A 醫藥化合物 PHARMACEUTICAL COMPOUNDS 失效
简体标题：医药化合物 PHARMACEUTICAL COMPOUNDS
公开(公告)号：TW200602046A
公开(公告)日：2006-01-16
申请号：TW094118996
申请日：2005-06-08
申请人：亞士德科技股份有限公司 ASTEX TECHNOLOGY LIMITED , 癌症研究科技股份有限公司 CANCER RESEARCH TECHNOLOGY LIMITED , 癌症研究機構:皇家癌症醫院 THE INSTITUTE OF CANCER RESEARCH:ROYAL CANCER HOSPITAL
发明人：法利瑞歐柏帝尼 BERDINI, VALERIO , 高登撒西提 SAXTY, GORDON , 瑪琳納斯林德特韋當克 VERDONK, MARINUS LEENDERT , 史帝芬約翰伍荷 WOODHEAD, STEVEN JOHN , 保羅葛拉罕懷特 WYATT, PAUL GRAHAM , 羅勃特喬治伯利 BOYLE, ROBERT GEORGE , 漢娜費歐娜索莉 SORE, HANNAH FIONA , 大衛溫特瓦特 WALKER, DAVID WINTER , 羅勃特當罕 DOWNHAM, ROBERT , 羅賓亞瑟艾力斯卡爾 CARR, ROBIN ARTHUR ELLIS , 伊恩考林斯 COLLINS, IAN
IPC分类号： A61K
摘要：本發明係提供具有蛋白質激B抑制活性之式(I)化合物：094118996-p01.bmp其中A為含有1至7個碳原子之飽和烴連結基，此連結基具有一個最大鏈長為5個原子，延伸於R^1與NR^2R^3之間，與一個最大鏈長為4個原子，延伸於E與NR^2R^3之間，其中連結基中碳原子之一可視情況被氧或氮原子置換；且其中連結基A之碳原子可視情況帶有一或多個取代基，選自酮基、氟及羥基，其條件是羥基當存在時係不位在相對於NR^2R^3基團α位之碳原子處，且其條件是酮基當存在時係位在相對於NR^2R^3基團α位之碳原子處；E為單環狀或雙環狀碳環族或雜環族基團；R^1為芳基或雜芳基；且R^2,R^3,R^4及R^5均如請求項中之定義。亦提供含有此等化合物之醫藥組合物，製備此等化合物之方法，及其作為抗癌劑之用途。094118996-p01.bmp
简体摘要：本发明系提供具有蛋白质激B抑制活性之式(I)化合物：094118996-p01.bmp其中A为含有1至7个碳原子之饱和烃链接基，此链接基具有一个最大链长为5个原子，延伸于R^1与NR^2R^3之间，与一个最大链长为4个原子，延伸于E与NR^2R^3之间，其中链接基中碳原子之一可视情况被氧或氮原子置换；且其中链接基A之碳原子可视情况带有一或多个取代基，选自酮基、氟及羟基，其条件是羟基当存在时系不位在相对于NR^2R^3基团α位之碳原子处，且其条件是酮基当存在时系位在相对于NR^2R^3基团α位之碳原子处；E为单环状或双环状碳环族或杂环族基团；R^1为芳基或杂芳基；且R^2,R^3,R^4及R^5均如请求项中之定义。亦提供含有此等化合物之医药组合物，制备此等化合物之方法，及其作为抗癌剂之用途。094118996-p01.bmp

2. 发明专利

TW200524598A 藥用化合物 PHARMACEUTICAL COMPOUNDS 失效
简体标题：药用化合物 PHARMACEUTICAL COMPOUNDS
公开(公告)号：TW200524598A
公开(公告)日：2005-08-01
申请号：TW093120042
申请日：2004-07-02
申请人：亞斯泰克斯科技有限公司 ASTEX TECHNOLOGY LIMITED
发明人：維里歐伯狄尼 BERDINI, VALERIO , 麥可歐布萊恩 O'BRIEN, MICHAEL ALISTAIR , 瑪莉亞卡爾 CARR, MARIA GRAZIA , 勒瑞莎爾利 EARLY, THERESA RACHEL , 伊娃納瓦洛 NAVARRO, EVA FIGUEROA , 艾德瑞安吉爾 GILL, ADRIAN LIAM , 史蒂芬霍華德 HOWARD, STEVEN , 蓋瑞翠瓦沙 TREWARTHA, GARY , 艾莉森伍爾弗 WOOLFORD, ALISON JO-ANNE , 安德魯伍海德 WOODHEAD, ANDREW JAMES , 保羅瓦特 WYATT, PAUL GRAHAM
IPC分类号： A61K , C07D , A61P
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：本發明係提供用以作為週期素依賴性激，肝醣合成激–3及極光(Aurora)激之抑制劑，及供用以治療癌症之已知且新穎之化合物。化合物具有通式(I)：093120042-p01.bmp及其鹽，N–氧化物及溶劑化物；其中X為CR^5或N；A為一個鍵或–(CH2)m–(B)n–；B為C＝O，NR^g(C＝O)或O(C＝O)且其中R^g為氫或任經羥基或C1–4烷氧基取代之C1–4烴基；m為0，1或2；n為0或1；R^0為氫，或者當NR^g存在時，則與NR^g共同形成–(CH2)p–基團，其中p為2至4；R^1為氫，具有3至12個環節之碳環型或雜環型基團，或任經取代之C1–8烴基團；R^2為氫，鹵素，甲氧基，或任經鹵素，羥基或甲氧基取代之C1–4烴基團；R^3及R^4與彼等所接合之碳原子共同形成具5至7個環節且其中至多有3個環節可為擇自N，O及S中之雜原子之任經取代稠合碳環型或雜環型環，且R^5為氫，R^2基團或R^10基團且其中R^10乃擇自鹵素，羥基，三氟甲基，氰基，硝基，羧基，胺基，單–或二–C1–4烴胺基，具3至12個環節之碳環型及雜環型基團；R^a–R^b基團其中R^a為一個鍵，O，CO，X^1C(X^2)，C(X^2)X^1，X^1C(X^2)X^1，S，SO，SO2，NR^c，SO2NR^c或NR^cSO2；且R^b乃擇自氫，具3至12個環節之碳環型或雜環型基團，及任經一或更多個由羥基，合氧基，鹵素，氰基，硝基，羧基，胺基，單–或二–C1–4烴胺基，具3至12個環節之碳環型及雜環型基團中所擇定之取代基所取代之C1–8烴基團且其中C1–8烴基團中之一或更多個碳原子可任經O，S，SO，SO2，NR^c，X^1C(X^2)，C(X^2)X^1或X^1C(X^2)X^1所替代；R^c乃擇自氫及C1–4烴基；且X^1為O，S或NR^c且X^2為＝O，＝S或＝NR^c。093120042-p01.bmp
简体摘要：本发明系提供用以作为周期素依赖性激，肝糖合成激–3及极光(Aurora)激之抑制剂，及供用以治疗癌症之已知且新颖之化合物。化合物具有通式(I)：093120042-p01.bmp及其盐，N–氧化物及溶剂化物；其中X为CR^5或N；A为一个键或–(CH2)m–(B)n–；B为C＝O，NR^g(C＝O)或O(C＝O)且其中R^g为氢或任经羟基或C1–4烷氧基取代之C1–4烃基；m为0，1或2；n为0或1；R^0为氢，或者当NR^g存在时，则与NR^g共同形成–(CH2)p–基团，其中p为2至4；R^1为氢，具有3至12个环节之碳环型或杂环型基团，或任经取代之C1–8烃基团；R^2为氢，卤素，甲氧基，或任经卤素，羟基或甲氧基取代之C1–4烃基团；R^3及R^4与彼等所接合之碳原子共同形成具5至7个环节且其中至多有3个环节可为择自N，O及S中之杂原子之任经取代稠合碳环型或杂环型环，且R^5为氢，R^2基团或R^10基团且其中R^10乃择自卤素，羟基，三氟甲基，氰基，硝基，羧基，胺基，单–或二–C1–4烃胺基，具3至12个环节之碳环型及杂环型基团；R^a–R^b基团其中R^a为一个键，O，CO，X^1C(X^2)，C(X^2)X^1，X^1C(X^2)X^1，S，SO，SO2，NR^c，SO2NR^c或NR^cSO2；且R^b乃择自氢，具3至12个环节之碳环型或杂环型基团，及任经一或更多个由羟基，合氧基，卤素，氰基，硝基，羧基，胺基，单–或二–C1–4烃胺基，具3至12个环节之碳环型及杂环型基团中所择定之取代基所取代之C1–8烃基团且其中C1–8烃基团中之一或更多个碳原子可任经O，S，SO，SO2，NR^c，X^1C(X^2)，C(X^2)X^1或X^1C(X^2)X^1所替代；R^c乃择自氢及C1–4烃基；且X^1为O，S或NR^c且X^2为＝O，＝S或＝NR^c。093120042-p01.bmp

3. 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

4. 发明申请

WO2005011697A2 PHARMACEUTICAL COMPOUNDS 审中-公开
标题翻译：药物化合物
公开(公告)号：WO2005011697A2
公开(公告)日：2005-02-10
申请号：PCT/GB2004/003196
申请日：2004-07-23
申请人： ASTEX TECHNOLOGY LIMITED , CANCER RESEARCH TECHNOLOGY LIMITED , THE INSTITUTE OF CANCER RESEARCH: ROYAL CANCER HOSPITAL , MCDONALD, Edward , DE FONSECA, Tatiana, Faria , BAVETSIAS, Vassilios , CALDWELL, John , WYATT, Paul, Graham , BERDINI, Valerio
发明人： MCDONALD, Edward , DE FONSECA, Tatiana, Faria , BAVETSIAS, Vassilios , CALDWELL, John , WYATT, Paul, Graham , BERDINI, Valerio
IPC分类号： A61K31/472
CPC分类号： C04B35/632 , A61K31/472 , C07D217/02 , C07D401/12
摘要： The invention provides compounds for the prophylaxis or treatment of a disease state or condition mediated by protein kinase A or protein kinase B, the compounds having the formula (I°), or being salts or solvates thereof. In formula (I°), n is 0 or 1; A and E are alkylene 2-3 carbon atoms in length optionally substituted by R 11 and -X-CH(R 6 )(R 7 ); G is hydrogen when n is 0 and, when n is 1, G is hydrogen or -X-CH(R 6 )(R 7 ); R 1 is an aryl or heteroaryl group having 5-12 ring members; R 2 and R 4 are selected from hydrogen, R 7 , R 11 and CH(R 6 )(R 7 ); R 3 , R 3a and R 5 are selected from hydrogen, R 11 and -X-CH(R 6 )(R 7 ); or any one pair or any two non-overlapping pairs selected from R 2 and R 3 ; R 3 and R 4 ; R 2 and R 5 ; R 3 and R 5 ; R 4 and R 5 ; R 3 and R 8 ; and R 4 and R 8 are linked together in a ring and together form an alkylene chain of 1-5 carbon atoms in length which may be optionally substituted by R 11 and -X-CH(R 6 )(R 7 ); or the pair R 2 and R 4 are linked together in a ring and together form an alkylene chain of 2-5 carbon atoms in length which may be optionally substituted by R 11 and -X-CH(R 6 )(R 7 ); and optionally R 3 and R 3a may be linked together in a ring and together form an alkylene chain of 1-6 carbon atoms in length which may be optionally substituted by R 11 and -X-CH(R 6 )(R 7 ); or R 6 and R 7 together with the carbon atom to which they are attached form a cyclic group having 5-12 ring members; X, R 6 , R 7 , R 8 , R 9 , R 10 and R 11 are each as defined in claim 1; and wherein the definitions of, A, E, G, X, n and R 1 to R 11 are subject to the provisos set ou in claim 1.
摘要翻译：本发明提供了用于预防或治疗由蛋白激酶A或蛋白激酶B，具有式（I°）的化合物或其盐或溶剂合物介导的疾病状态或病症的化合物。在式（I°）中，n为0或1; A和E是长度任选被R 11和-X-CH（R 6）（R 7）取代的2-3个碳原子的亚烷基; 当n为0时，G为氢，当n为1时，G为氢或-X-CH（R 6）（R 7）; R 1是具有5-12个环成员的芳基或杂芳基; R 2和R 4选自氢，R 7，R 7和CH（R 6）（R 7）; R 3，R 3a和R 5选自氢，R 11和-X-CH（R 6）（R 7）; 或选自R 2和R 3中的任何一对或任何两个非重叠对; R 3和R 4; R 2和R 5; R 3和R 5; R 4和R 5; R 3和R 8; 并且R 4和R 8以环连接在一起并且一起形成长度为1-5个碳原子的亚烷基链，其可任选地被R 11和-X-CH（R 6）取代，）（R <7>）; 或者R 2和R 4在环中连接在一起并且一起形成长度为2-5个碳原子的亚烷基链，其可以任选地被R 11和-X-CH（R' 6>）（R <7>）; 并且任选地R 3和R 3a可以以环连接在一起并且一起形成长度为1-6个碳原子的亚烷基链，其可任选地被R 11和-X-CH（R' 6>）（R <7>）; 或R 6和R 7与它们所连接的碳原子一起形成具有5-12个环成员的环状基团; X，R 6，R 7，R 8，R 9，R 10和R 11各自如权利要求1所定义; 并且其中A，E，G，X，n和R 1至R 11的定义符合权利要求1所述的限制条件。

5. 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）。

6. 发明申请

WO2004089929A1 5-AMINO-2-CARBONYLTHIOPHENE DERIVATIVES FOR USE AS P38 MAP KINASE INHIBITORS IN THE TREATMENT OF INFLAMMATORY DISEASES 审中-公开
标题翻译：用于治疗炎症性疾病的P38 MAP激酶抑制剂的5-氨基-2-碳二苯醚衍生物
公开(公告)号：WO2004089929A1
公开(公告)日：2004-10-21
申请号：PCT/GB2004/001589
申请日：2004-04-13
申请人： ASTEX TECHNOLOGY LIMITED , GILL, Adrian, Liam , WOODHEAD, Steven , CARR, Maria
发明人： GILL, Adrian, Liam , WOODHEAD, Steven , CARR, Maria
IPC分类号： C07D333/38
CPC分类号： C07D409/12 , C07D333/38 , C07D409/14 , C07D417/12 , C07D417/14
摘要： The invention provides the use of a compound for the manufacture of a medicament for the prophylaxis or treatment of a disease state or condition mediated by a p38 MAP kinase; the compound being defined by formula (I): wherein: R 1 and R 2 are the same or different and each is selected from hydrogen, C 1-4 hydrocarbyl, halogen and cyano; X is selected from C=O, C=S, C(=O)NH, C(=S)NH, C(=O)O, C(=O)S, C(=S)O and C(=S)S; R 3 is selected from aryl and heteroaryl groups each having from 5 to 12 ring members, the aryl and heteroaryl groups each being unsubstituted or substituted by one or more substituent groups R 7 selected from halogen, hydroxy, trifluoromethyl, cyano, nitro, carboxy, amino, carbocyclic and heterocyclic groups having from 3 to 12 ring members; a group R a -R b wherein R a is a bond, 0, CO, X 1 C(X 2 ), C(X 2 )X 1 , X 1 C(X 2 )X 1 , S, SO, SO 2 , NR c , SO 2 NR c or NR c SO 2; and R b is selected from hydrogen, carbocyclic and heterocyclic groups having from 3 to 7 ring members, and a C 1-8 hydrocarbyl group optionally substituted by one or more substituents selected from hydroxy, oxo, halogen, cyano, nitro, amino, mono- or di-C 1-4 hydrocarbylamino, carbocyclic and heterocyclic groups having from 3 to 12 ring members and wherein one or more carbon atoms of the C 1-8 hydrocarbyl group may optionally be replaced by 0, S, SO, SO 2 , NR c , X 1 C(X 2 ), C(X 2 )X 1 or X 1 C(X 2 )X 1 ; X 1 is 0, S or NR c and X 2 is =0, =S or =NR c ; R c is hydrogen or C 1-4 hydrocarbyl; R 4 is a group YR 5 or a group R 6 ; Y is is NH, 0 or S; R 5 is selected from (a) carbocyclic and heterocyclic groups having from 3 to 12 ring members; and (b) C 1-8 hydrocarbyl groups optionally substituted by one or more substituents selected from hydroxy, oxo, halogen, cyano, amino, mono- or di- C 1-4 hydrocarbylamino, and carbocyclic and heterocyclic groups having from 3 to 12 ring members, wherein one or more carbon atoms of the C 1-8 hydrocarbyl group may optionally be replaced by 0, S, SO, SO 2 , NR c , X 1 C(X 2 ), C(X 2 )X 1 or X 1 C(X 2 )X 1 , provided that when Y is 0, a carbon atom adjacent to the group Y is not replaced by 0; and R 6 is a heterocyclic group having from 4 to 12 ring members and containing at least one ring nitrogen atom through which R 6 is linked to the adjacent carbonyl group; wherein the carbocyclic and heterocyclic groups of substituents R 5 and R 6 are each unsubstituted or substituted by one or more substituent groups R 7 as hereinbefore defined. Also provided are novel compounds, pharmaceutical compositions containing the compounds and methods for their preparation.
摘要翻译：本发明提供了化合物在制备用于预防或治疗由p38MAP激酶介导的疾病状态或病症的药物中的用途; 该化合物由式（I）定义：其中：R 1和R 2相同或不同，各自选自氢，C 1-4烃基，卤素和氰基; X选自C = O，C = S，C（= O）NH，C（= S）NH，C（= O）O，C（= O）S，C（= S）O和C（= S）S; R 3选自具有5至12个环成员的芳基和杂芳基，芳基和杂芳基各自未被取代或被一个或多个选自卤素，羟基，三氟甲基，氰基，具有3-12个环成员的硝基，羧基，氨基，碳环和杂环基; 其中R a是键，0，CO，X 1 C（X 2），C（X 2）X 1，X 1， C（X 2）X 1，S，SO，SO 2，NR c，SO 2 NR c或NR c SO 2; 并且R b选自具有3至7个环成员的氢，碳环和杂环基，以及任选被一个或多个选自羟基，氧代，卤素，氰基，硝基，氨基，具有3-12个环成员的单 - 或二-C 1-4烃基氨基，碳环和杂环基，其中C 1-8烃基的一个或多个碳原子可任选地被0，S，SO，SO 2，（X 2），C（X 2）X 1或X 1 C（X 2）X 1; X 1是0，S或NR c，X 2是= O，= S或= NR c; R c是氢或C 1-4烃基; R 4是基团YR 5或基团R 6; Y为NH，O或S; R 5选自（a）具有3-12个环成员的碳环和杂环基; 任选被一个或多个选自羟基，氧代，卤素，氰基，氨基，一或二-C 1-4烃基氨基的取代基取代的C 1-8烃基，以及具有3-12个环成员的碳环和杂环基，其中C 1-8烃基的一个或多个碳原子可以任选地被0，S，SO，SO 2，NR c，X 1 C（X 2），C（X 2））X 1或X 1 C（X 2）X 1，条件是当Y为0时，与Y相邻的碳原子不被0取代; 并且R 6是具有4至12个环成员并且含有至少一个环氮原子的杂环基，R 6通过其与相邻的羰基连接; 其中取代基R 5和R 6的碳环和杂环基团各自是未取代的或被如上文所定义的一个或多个取代基R 7取代。还提供了新化合物，含有这些化合物的药物组合物及其制备方法。

7. 发明申请

WO2004014864A1 1H-INDAZOLE-3-CARBOXAMIDE COMPOUNDS AS CYCLIN DEPENDENT KINASES (CDK) INHIBITORS 审中-公开
标题翻译： 1H-吲唑-3-羧酰胺化合物作为循环激酶（CDK）抑制剂
公开(公告)号：WO2004014864A1
公开(公告)日：2004-02-19
申请号：PCT/GB2003/003491
申请日：2003-08-08
申请人： ASTEX TECHNOLOGY LIMITED , BERDINI, Valerio , PADOVA, Alessandro , SAXTY, Gordon , WOOLFORD, Alison, Jo-Anne , WYATT, Paul, Graham
发明人： BERDINI, Valerio , PADOVA, Alessandro , SAXTY, Gordon , WOOLFORD, Alison, Jo-Anne , WYATT, Paul, Graham
IPC分类号： C07D231/56
CPC分类号： C07D231/56 , C07D401/12 , C07D403/12 , C07D405/04 , C07D405/12 , C07D409/04 , C07D413/04 , C07D413/12 , C07D417/04 , C07D417/12 , C07D417/14
摘要： The invention provides a compound of the formula (I) for use in the prophylaxis or treatment of a disease state or condition mediated by a cyclin dependent kinase: wherein A is a group R 2 or CH 2 -R 2 where R 2 is a carbocyclic or heterocyclic group having from 3 to 12 ring members; B is a bond or an acyclic linker group having a linking chain length of up to 3 atoms selected from C, N, S and O; R 1 is hydrogen or a group selected from SO 2 R b ,SO 2 NR 7 R 8 ,CONR 7 R 8 ,NR 7 R 9 and carbocyclic and heterocyclic groups having from 3 to 7 ring members; R 3 , to R 9 are defined in the description but excluding the compounds N-[(morpholin-4-yl)phenyl-1H-indazole-3-carboxamide and N-[4-(acetylaminosulphonyl)phenyl-1H-indazole-3-carboxamide.
摘要翻译：本发明提供了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式（I）化合物：其中A是基团R 2或CH 2 -R 2，其中R 1， 2>是具有3至12个环成员的碳环或杂环基; B是具有至多3个选自C，N，S和O的原子的连接链长度的键或无环连接基团; R 1是氢或选自SO 2 R b，SO 2 NR 7 R 8，CONR 7 R 8，NR 7 R 9和具有3个碳原子的碳环和杂环基团的基团至7名成员; R 3至R 9在描述中定义，但不包括化合物N - [（吗啉-4-基）苯基-1H-吲唑-3-甲酰胺和N- [4-（乙酰氨基磺酰基）苯基-1H- - 吲唑-3-甲酰胺。

8. 发明申请

WO2005061463A1 PYRAZOLE DERIVATIVES AS PROTEIN KINASE MODULATORS 审中-公开
标题翻译：作为蛋白激酶调节剂的吡唑衍生物
公开(公告)号：WO2005061463A1
公开(公告)日：2005-07-07
申请号：PCT/GB2004/005464
申请日：2004-12-23
申请人： ASTEX TECHNOLOGY LIMITED , CANCER RESEARCH TECHNOLOGY LIMITED , THE INSTITUTE OF CANCER RESEARCH: ROYAL CANCER HOSPITAL , BERDINI, Valerio , SAXTY, Gordon , VERDONK, Marinus, Leendert , WOODHEAD, Steven, John , WYATT, Paul, Graham , BOYLE, Robert, George , SORE, Hannah, Fiona , WALKER, David, Winter , COLLINS, Ian , DOWNHAM, Robert , CARR, Robin, Arthur, Ellis
发明人： BERDINI, Valerio , SAXTY, Gordon , VERDONK, Marinus, Leendert , WOODHEAD, Steven, John , WYATT, Paul, Graham , BOYLE, Robert, George , SORE, Hannah, Fiona , WALKER, David, Winter , COLLINS, Ian , DOWNHAM, Robert , CARR, Robin, Arthur, Ellis
IPC分类号： C07D231/12
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 R l and NR 2 R 3 and a maximum chain length of 4 atoms extending between E and NR 2 R 3 , 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 inker 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 NR 2 R 3 group and provided that the oxo group when present is located at a carbon atom a with respect to the NR 2 R 3 group; E is a monocyclic or bicyclic carbocyclic or heterocyclic group; R l is an aryl or heteroaryl group; and R 2 , R 3 , R 4 and R 5 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，该连接基团的最大链长度在R 1之间延伸 >和NR 2 R 3，并且在E和NR 2 R 3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代替原子; 并且其中，墨水基团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'位于碳原子a时，并且条件是当存在的氧代基位于相对于NR 2 R 3基团的碳原子a时; E是单环或双环碳环或杂环基; R 1是芳基或杂芳基; 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

WO2005002576A2 PHARMACEUTICAL COMPOUNDS 审中-公开
标题翻译：药物化合物
公开(公告)号：WO2005002576A2
公开(公告)日：2005-01-13
申请号：PCT/GB2004/002913
申请日：2004-07-05
申请人： ASTEX TECHNOLOGY LIMITED , 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： A61K31/4184
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; wherein X is CR 5 or N; 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 I-4 hydrocarbyl optionally substituted by hydroxy or C I-4 alkoxy; m is 0, 1 or 2; n is 0 or 1; R 1 is hydrogen, a carbocyclic or heterocyclic group having from 3 to 12 ring members, or an optionally substituted C I-8 hydrocarbyl group; R 2 is hydrogen, halogen, methoxy, or a C I-4 hydrocarbyl group optionally substituted by halogen, hydroxyl or methoxy; R 3 and R 4 are the same or different and each is selected from hydrogen, CN, C(O)R 8 , optionally substituted C I-8 hydrocarbyl and carbocyclic or heterocyclic groups having from 3 to 12 ring members; and R 5 is hydrogen, a group R 2 or a group R 10 wherein R 10 is selected from halogen, hydroxy, trifluoromethyl, cyano, nitro, carboxy, amino, mono- or di-C I-4 hydrocarbyl amino, carbocyclic and heterocyclic groups having from 3 to 12 ring members; a group R a -R b wherein R a is a bond, 0, CO, X I C(X 2 ), C(X 2 )X I , X I C(X 2 )X I , S, SO, S0 2 , NR c , S0 2 NR c or NR c S0 2 ; and R b is selected from hydrogen, carbocyclic and heterocyclic groups having from 3 to 12 ring members, and a C 1-8 hydrocarbyl group optionally substituted by one or more substituents selected from hydroxy, oxo, halogen, cyano, nitro, carboxy, amino, mono- or di-C I-4 hydrocarbylamino, carbocyclic and heterocyclic groups having from 3 to 12 ring members and wherein one or more carbon atoms of the C 1-8 hydrocarbyl group may optionally be replaced by 0, S, SO, S0 2 , NR c , X 1 C(X 2 ), C(X 2 )X 1 or X 1 C(X 2 )X 1 ; R c is selected from hydrogen and C I-4 hydrocarbyl.; X 1 is 0, S or NR c and X 2 is =O, =S or =NR c ; and R 8 is selected from OR 11 , SR 11 and NR 12 R 13 ; R 11 is selected from optionally substituted C 1-8 hydrocarbyl and carbocyclic or heterocyclic groups having from 3 to 12 ring members; and one of R 12 and R 13 is a group R 11 and the otther of R 12 and R 13 is hydrogen or C 1-4 alkyl; or R 12 and R 13 and the nitrogen atom to which they are attached together form a saturated heterocyclic group having from 4 to 7 ring members and containing 1,2 or 3 heteroatom ring members selected from N, O and S. 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; 其中X是CR 5或N; A是键或 - （CH 2）m - （B）n-; B是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; m为0,1或2; n为0或1; 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; R 2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; R 3和R 4相同或不同，各自选自氢，CN，C（O）R 8，任选取代的C 1-8烃基和具有3-12个环成员的碳环或杂环基 ; R 5为氢，R 2或R 10基团，其中R 10选自卤素，羟基，三氟甲基，氰基，硝基，羧基，氨基，单 - 或二 - 具有3-12个环成员的烃基氨基，碳环基和杂环基; 0，CO，XC（X 2），C（X 2）X，XC（X 2）X，X， S，SO，SO 2，NR c，SO 2 NR 3或NR c SO 2; 并且R b选自具有3至12个环成员的氢，碳环和杂环基，以及任选被一个或多个选自羟基，氧代，卤素，氰基，硝基，羧基，具有3至12个环成员的氨基，单或二-C 1-4烃基氨基，碳环基和杂环基，并且其中C 1-8烃基的一个或多个碳原子可任选地被0，S，SO，SO 2， X c，X 1 C（X 2），C（X 2）X 1或X 1 C（X 2）X 1; R c选自氢和C 1-4烃基。 X 1是0，S或NR c，X 2是= O，= S或= NR c; R 8选自OR 11，SR 11和NR 12 R 13; R 11选自具有3-12个环成员的任选取代的C 1-8烃基和碳环或杂环基; R 12和R 13之一是R 11基团，R 12和R 13的基团是氢或C 1-4烷基; 或R 12和R 13和它们所连接的氮原子一起形成具有4-7个环成员并含有1,2或3个选自N，O和S的杂原子环成员的饱和杂环基。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。

10. 发明申请

WO2005002552A2 PHARMACEUTICAL COMPOUNDS 审中-公开
标题翻译：药物化合物
公开(公告)号：WO2005002552A2
公开(公告)日：2005-01-13
申请号：PCT/GB2004/002824
申请日：2004-07-05
申请人： ASTEX TECHNOLOGY LIMITED , 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
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); wherein X is CR 5 or N; 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; R 1 is hydrogen, a carbocyclic or heterocyclic group having from 3 to 12 ring members, or an optionally substituted C 1-8 hydrocarbyl group; R 2 is hydrogen, halogen, methoxy, or a C 1-4 hydrocarbyl group optionally substituted by halogen, hydroxyl or methoxy; R 3 and R 4 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 R 5 is hydrogen, a group R 2 or a group R 10 wherein R 10 is selected from halogen, hydroxy, trifluoromethyl, cyano, nitro, carboxy, amino, mono- or di-C 1-4 hydrocarbylamino, carbocyclic and heterocyclic groups having from 3 to 12 ring members; a group R a -R b wherein R a is a bond, O, CO, X 1 C(X 2 ), C(X 2 )X 1 , X 1 C(X 2 )X 1 , S, SO, SO 2 , NR c , SO 2 NR c or NR c SO 2 ; and R b is selected from hydrogen, carbocyclic and heterocyclic groups having from 3 to 12 ring members, and a C 1-8 hydrocarbyl group optionally substituted by one or more substituents selected from hydroxy, oxo, halogen, cyano, nitro, carboxy, amino, mono- or di-C 1 - 4 hydrocarbylamino, carbocyclic and heterocyclic groups having from 3 to 12 ring members and wherein one or more carbon atoms of the C 1-8 hydrocarbyl group may optionally be replaced by O, S, SO, SO 2 , NR c , X 1 C(X 2 ), C(X 2 )X I or X 1 C(X 2 )X 1 ; R c is selected from hydrogen and C 1-4 hydrocarbyl; and X 1 is O, S or NR c and X 2 is =O, =S or =NR c . 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。所述化合物具有通式（I）; 其中X是CR 5或N; A是键或 - （CH 2）m - （B）n-; B是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; m为0,1或2; n为0或1; 当R 0为氢时，或与NR g一起形成基团 - （CH 2）p - ，其中p为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; R 2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; R 3和R 4与它们所连接的碳原子一起形成任选取代的稠合碳环或杂环，其具有5至7个环成员，其中多达3个可以是选自N，O和S的杂原子 ; R 5是氢，R 2或R 10基团，其中R 10选自卤素，羟基，三氟甲基，氰基，硝基，羧基，氨基，单或二-C1 具有3-12个环成员的烃基氨基，碳环和杂环基; 其中R a是键的基团R a -R b，O，CO，X C（X 2），C（X 2）X 1， C（X 2）X 1，S，SO，SO 2，NR c，SO 2 NR c或NR c SO 2; 并且R b选自具有3至12个环成员的氢，碳环和杂环基，以及任选被一个或多个选自羟基，氧代，卤素，氰基，硝基，羧基，具有3至12个环成员的氨基，单或二-C 1-4烃基氨基，碳环和杂环基，并且其中C 1-8烃基的一个或多个碳原子可以任选地被O，S，SO，SO 2， X c，X 1 C（X 2），C（X 2）X或X 1 X（X 2）X 1; R c选自氢和C 1-4烃基; 且X 1为O，S或NR c且X 2为= O，= S或= NR c。式（I）中还包括化合物的盐，溶剂合物和N-氧化物。

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