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31. 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。

32. 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）。

33. 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。

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