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    • 5. 发明申请
      WO2006067466A2 PYRAZINES AND PYRIDINES AND DERIVATIVES THEREOF AS THERAPEUTIC COMPOUNDS 审中-公开
    • PYRAZINES AND PYRIDINES AND DERIVATIVES THEREOF AS THERAPEUTIC COMPOUNDS
    • 作为治疗化合物的吡咯并吡啶及衍生物
    • WO2006067466A2
    • 2006-06-29
    • PCT/GB2005/005011
    • 2005-12-22
    • THE WELLCOME TRUST LIMITED , SPRINGER, Caroline, Joy , NICULESCU-DUVAZ, Ion , ROMAN VELA, Esteban , GILL, Adrian, Liam , TAYLOR, Richard, David , MARAIS, Richard, Malcolm
    • SPRINGER, Caroline, Joy , NICULESCU-DUVAZ, Ion , ROMAN VELA, Esteban , GILL, Adrian, Liam , TAYLOR, Richard, David , MARAIS, Richard, Malcolm
    • C07D213/74 , C07D241/20 , C07D317/46 , C07D319/18 , C07D321/10 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/12 , C07D409/12 , C07D413/12 , C07D417/12
    • C07D213/74 , C07D241/20 , C07D317/46 , C07D319/18 , C07D321/10 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/12 , C07D409/12 , C07D413/12 , C07D417/12
    • 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.
    • 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。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
    • 8. 发明申请
      WO2005002552A2 PHARMACEUTICAL COMPOUNDS 审中-公开
    • PHARMACEUTICAL COMPOUNDS
    • 药物化合物
    • WO2005002552A2
    • 2005-01-13
    • PCT/GB2004/002824
    • 2004-07-05
    • 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
    • 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
    • A61K31/00
    • A61K31/5377 , A61K31/00 , A61K31/4184 , A61K45/06 , C07D401/14 , C07D403/04 , C07D405/14 , C07D409/14 , C07D413/14 , C07D471/04 , C07D513/04
    • 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.
    • 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。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
    • 9. 发明申请
      WO03087087A2 PHARMACEUTICAL COMPOUNDS 审中-公开
    • PHARMACEUTICAL COMPOUNDS
    • 药物化合物
    • WO03087087A2
    • 2003-10-23
    • PCT/GB0301507
    • 2003-04-08
    • ASTEX TECHNOLOGY LTD , FREDERICKSON MARTYN , GILL ADRIAN LIAM , PADOVA ALESSANDRO , CONGREVE MILES STUART
    • FREDERICKSON MARTYN , GILL ADRIAN LIAM , PADOVA ALESSANDRO , CONGREVE MILES STUART
    • A61K31/404 , A61K31/437 , A61K31/4439 , A61K31/506 , A61K31/5377 , A61P1/04 , A61P9/10 , A61P11/00 , A61P11/06 , A61P17/14 , A61P19/02 , A61P19/06 , A61P19/08 , A61P21/00 , A61P25/28 , A61P29/00 , A61P31/00 , A61P31/04 , A61P31/06 , A61P31/18 , A61P33/06 , A61P35/00 , A61P37/06 , A61P43/00 , C07D209/08 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/12 , C07D471/04
    • C07D401/06 , A61K31/404 , C07D209/08 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/12
    • The invention provides a compound for use in the prophylaxis or treatment of a disease state or condition mediated by a p38 MAP kinase such as rheumatoid arthritis and osteoarthritis; the compound being of the general formula (I): wherein U, T, V and W are each a nitrogen atom or a group CR provided that no more than three of U, T, V and W are nitrogen atoms; R is hydrogen, C1-4 hydrocarbyl, halogen or a group -A-R ; R is hydrogen, C1-4 hydrocarbyl or a group -A-R ; provided that only one of R and R is a group -A-R ; R is hydrogen, C1-4 hydrocarbyl or halogen; A is a carbon- or heteroatom-containing linker group having a linking chain length of one or two atoms; R is a monocyclic or bicyclic heteroaryl group containing from five to twelve ring members; each group R is independently selected from hydrogen, hydroxy, halogen, nitro, cyano, a monocyclic heterocyclic group having up to seven ring members, a group N(R )2, a group C(O)N(R )2, a group S02N(R )2, a group R -R and a group Y; provided that no more than one group Y is present; R is a bond, O, S, SO, S02, NH or N-C1-4 hydrocarbyl; R is C1-8 hydrocarbyl optionally interrupted by O, S, SO, SO2, NH or N-C1- 4 hydrocarbyl and optionally substituted by one or more substitutents selected from hydroxy, amino, mono- or di-C1-4 hydrocarbylamino, C1 -4 hydrocarbyloxy, oxo, C1 -4 hydrocarbylthio and halogen; each group R is independently selected from hydrogen, C1-4 alkyl, C1-4 acyl and C 1-4 alkylsulphonyl; each group R is independently selected from hydrogen and C1-4 hydrocarbyl; Y is a group -N(R )-C(O)-R or -N(R )_SO2-R ; R is hydrogen, C1-4 hydrocarbyl or a group C(O)-R or S02-R ; R is selected from C1-l0 hydrocarbyl, CI-10 hydrocarbylamino, CI-10 hydrocarbylthio, C1-l0 hydrocarbyloxy, and aryl, arylamino, arylthio and aryloxy groups, the aryl moieties of which are carbocyclic or heterocyclic and have from five to twelve ring members, each substituent group R being optionally substituted by one or more groups R other than Y; or R and R together with the nitrogen and carbon or sulphur atoms to which they are attached are linked to form a ring structure of 4 to 7 ring members; wherein R is other than a 2-(2,4-diamino-6-triazinyl)ethyl group when, in combination, U, T, V and W are all CH, and R and R are both hydrogen; and provided that when the group -A-R contains an acidic substitituent group selected from carboxylic, phosphonic and sulphonic acids and tetrazoles, or contains a -C(O)NSO2- group, or when -A- is -C(O)N- and the nitrogen atom of the group A is linked directly to a furan or thiophene ring, then either R is -A-R and both R
    • 本发明提供了一种用于预防或治疗p38 MAP激酶介导的疾病状态或病症的化合物，例如类风湿性关节炎和骨关节炎; 所述化合物为通式（I）：其中U，T，V和W各自为氮原子或基团CR 4，条件是U，T，V和W中不超过三个为氮原子; R 0是氢，C 1-4烃基，卤素或基团-A-R 3; R 1是氢，C 1-4烃基或基团-A-R 3; 条件是R 0和R 1中仅有一个为-A-R 3基团; R 2是氢，C 1-4烃基或卤素; A是具有一个或两个原子的连接链长度的含碳或杂原子的连接基团; R 3是含有5至12个环成员的单环或双环杂芳基; 每个基团R 4独立地选自氢，羟基，卤素，硝基，氰基，具有至多七个环成员的单环杂环基，基团N（R 5）2，基团C（O）N（ R 6）2，SO 2 N（R 6）2，基团R a -R b和基团Y; 只要不存在不止一个Y组; R a是键，O，S，SO，SO 2，NH或N-C 1-4烃基; R b是任选地被O，S，SO，SO 2，NH或N-C 1-4烃基中断的C 1-8烃基，并任选被一个或多个选自羟基，氨基，单或二-C 1-4的取代基取代 烃基氨基，C 1-4烃氧基，氧代，C 1-4烃基硫基和卤素; 每个基团R 5独立地选自氢，C 1-4烷基，C 1-4酰基和C 1-4烷基磺酰基; 每个基团R 6独立地选自氢和C 1-4烃基; Y是基团-N（R 7）-C（O）-R 8或-N（R 7）SO 2 -R 8; R 7是氢，C 1-4烃基或C（O）-R 8或SO 2 -R 8; R 8选自C 1-10烃基，C 1-10烃基氨基，C 1-10烃基硫代，C 1-10烃氧基和芳基，芳基氨基，芳硫基和芳氧基，其芳基部分是碳环或杂环的并具有五 至12个环成员，每个取代基R 8任选被一个或多个除Y以外的R 4基团取代; 或R 7和R 8与它们所连接的氮原子和碳原子一起连接形成4至7个环成员的环结构; 当组合U，T，V和W均为CH时，R 0不是2-（2,4-二氨基-6-三嗪基）乙基，R 1和R 2均为 都是氢; 并且条件是当基团-AR 3含有选自羧酸，膦酸和磺酸和四唑的酸性取代基时，或含有-C（O）NSO 2 - 基团，或当-A-是-C（O） N-和氮原子的基团A直接连接到呋喃或噻吩环，那么R 1是-AR 3，并且两个R
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
    • 10. 发明申请
      WO2009024821A3 OXADIAZOLE DERIVATIVES AS DGAT INHIBITORS 审中-公开
    • OXADIAZOLE DERIVATIVES AS DGAT INHIBITORS
    • 氧化氮衍生物作为DGAT抑制剂
    • WO2009024821A3
    • 2009-04-09
    • PCT/GB2008050716
    • 2008-08-15
    • ASTRAZENECA AB , ASTRAZENECA UK LTD , BIRCH ALAN MARTIN , BUTLIN ROGER JOHN , GILL ADRIAN LIAM , GROOMBRIDGE SAMUEL DAVID , PLOWRIGHT ALLEYN , WARING MICHAEL JAMES
    • BIRCH ALAN MARTIN , BUTLIN ROGER JOHN , GILL ADRIAN LIAM , GROOMBRIDGE SAMUEL DAVID , PLOWRIGHT ALLEYN , WARING MICHAEL JAMES
    • C07D413/12 , A61K31/4245 , A61P3/00
    • C07D413/12
    • 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; R1and R2are, 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; RA1 and RA2 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.
    • 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。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
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