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1. 发明专利

IL208405D0 SUBSTITUTED PYRIMIDIN-5-CARBOXAMIDES 281 未知
公开(公告)号：IL208405D0
公开(公告)日：2010-12-30
申请号：IL20840510
申请日：2010-10-03
申请人： ASTRAZENECA AB , WHITTAMORE PAUL ROBERT OWEN , PACKER MARTIN JOHN , LEACH ANDREW , GILL ADRIAN LIAM , SCOTT JAMES STEWART , SORME PERNILLA , SWALES JOHN GIBBIN
IPC分类号： C07D20060101
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 11betaHSD1, processes for making them and pharmaceutical compositions comprising them are also described.

2. 发明申请

WO2008078100A3 TRICYCLIC AMINE DERIVATIVES AS PROTEIN TYROSINE KINASE INHIBITORS 审中-公开
标题翻译：作为蛋白酪氨酸激酶抑制剂的三元胺衍生物
公开(公告)号：WO2008078100A3
公开(公告)日：2008-11-13
申请号：PCT/GB2007004960
申请日：2007-12-21
申请人： ASTEX THERAPEUTICS LTD , 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 , A61K31/437 , A61P35/00 , C07D487/04
CPC分类号： C07D471/04 , C07D487/04
摘要： The invention relates to new bicyclic heterocyclic derivative compounds of Formula (I), to pharmaceutical compositions comprising said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer. The compounds of Formula (I) are inhibitors of FGFR, VEGFR or PDGFR.
摘要翻译：本发明涉及式（I）的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以及所述化合物在治疗疾病中的用途。癌症。式（I）的化合物是FGFR，VEGFR或PDGFR的抑制剂。

3. 发明申请

WO2008078100A2 NEW COMPOUNDS 审中-公开
标题翻译：新化合物
公开(公告)号：WO2008078100A2
公开(公告)日：2008-07-03
申请号：PCT/GB2007/004960
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 , A61P35/00
CPC分类号： C07D471/04 , C07D487/04
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。

4. 发明申请

WO2006077414A1 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：WO2006077414A1
公开(公告)日：2006-07-27
申请号：PCT/GB2006/000191
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： 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 compounds of the formula (I), or salts, tautomers, N-oxides or solvates thereof wherein: R1 is selected from: (a) 2,6-dichlorophenyl; (b) 2,6-difluorophenyl; (c) a 2,3,6-trisubstituted phenyl group wherein the substituents for the phenyl group are selected from fluorine, chlorine, methyl and methoxy; (d) a group R0; (e) a group R a; (f) a group Rlb; (g) a group Rlc; (h) a group Rld; and 0) 2,6-difluorophenylamino ; wherein R )0υ, r R> llaa, T Rj I1bD, T R) I1cC, r R> Iidα, r R»2zaa, r R>22bD and RJ are as defined in the claims. The compounds have activity as inhibitors of cdk kinase (such as cdkl or cdk2) and glycogen synthase kinase-3 activity.
摘要翻译：本发明提供式（I）化合物或其盐，互变异构体，N-氧化物或溶剂合物，其中：R1选自：（a）2,6-二氯苯基; （b）2,6-二氟苯基; （c）2,3,6-三取代苯基，其中苯基的取代基选自氟，氯，甲基和甲氧基; （d）R0组; （e）基团R a; （f）组R1b; （g）R1c组; （h）一组Rld; 和0）2,6-二氟苯基氨基; 其中R 1，R 2，R 11a，R R 1，I R C，R R I，R R 2，R 2，R 22和R 22如权利要求中所定义。该化合物具有作为cdk激酶抑制剂（如cdk1或cdk2）和糖原合酶激酶-3活性的活性。

5. 发明申请

WO2006067466A2 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衍生物
公开(公告)号：WO2006067466A2
公开(公告)日：2006-06-29
申请号：PCT/GB2005/005011
申请日：2005-12-22
申请人： THE WELLCOME TRUST LIMITED , 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： C07D213/74 , C07D241/20 , 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。

6. 发明申请

WO2006043090A1 IMIDAZO[4,5-B]PYRIDIN-2-ONE AND OXAZOLO[4,5-B]PYRIDIN-2-ONE COMPOUNDS AND ANALOGS THEREOF AS THERAPEUTIC COMPOUNDS 审中-公开
标题翻译：咪唑并[4,5-B]吡啶-2-酮和氧杂唑[4,5-B]吡啶-2-酮化合物及其类似物作为治疗化合物
公开(公告)号：WO2006043090A1
公开(公告)日：2006-04-27
申请号：PCT/GB2005/004081
申请日：2005-10-21
申请人： CANCER RESEARCH TECHNOLOGY LIMITED , INSTITUTE OF CANCER RESEARCH: ROYAL CANCER HOSPITAL (THE) , ASTEX THERAPEUTICS LIMITED , NICULESCU-DUVAZ, Dan , SPRINGER, Caroline, Joy , GILL, Adrian, Liam , TAYLOR, Richard, David , MARAIS, Richard, Malcolm , DIJKSTRA, Harmen , GAULON, Catherine , MENARD, Delphine , ROMAN VELA, Esteban
发明人： NICULESCU-DUVAZ, Dan , SPRINGER, Caroline, Joy , GILL, Adrian, Liam , TAYLOR, Richard, David , MARAIS, Richard, Malcolm , DIJKSTRA, Harmen , GAULON, Catherine , MENARD, Delphine , ROMAN VELA, Esteban
IPC分类号： C07D471/04 , C07D498/04 , A61K31/4353 , A61P35/00
CPC分类号： C07D471/04
摘要： The present invention pertains to certain imidazo[4,5-b]pyridin-2-one and oxazolo[4,5-b]pyridin-2-one compounds and analogs thereof, which, inter alia , inhibit RAF (e.g., B-RAF) activity, inhibit cell proliferation, treat cancer, etc., and more particularly to compounds of the formula (I): wherein: J is independently -O- or -NR N1 -; R N1 , if present, is independently -H or a substituent; R N2 is independently -H or a substituent; Y is independently -CH= or -N=; Q is independently -(CH 2 ) j -M-(CH 2 ) k - wherein: j is independently 0, 1 or 2; k is independently 0, 1, or 2; j+k is 0, 1, or 2; M is independently -O-, -S-, -NH-, -NMe-, or -CH 2 -; each of R P1 , R P2 , R P3 , and R P4 is independently -H or a substituent; and additionally R P1 and R P2 taken together may be -CH=CH-CH=CH-; L is independently: a linker group formed by a chain of 2, 3, or 4 linker moieties; each linker moiety is independently -CH 2 -,-NR N -, -C(=X)-, or -S(=O) 2 -; exactly one linker moiety is -NR N -, or: exactly two linker moieties are -NR N -; exactly one linker moiety is -C(=X)-, and no linker moiety is -S(=O) 2 -; or: exactly one linker moiety is -S(=O) 2 -, and no linker moiety is -C(=X)-; no two adjacent linker moieties are -NR N -; X is independently =O or =S; each R N is independently -H or a substituent; A is independently: C 6-14 carboaryl, C 5-14 heteroaryl, C 3-12 carbocyclic, C 3-12 heterocyclic; and is independently unsubstituted or substituted; 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, 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：本发明涉及某些咪唑并[4,5-b]吡啶-2-酮和恶唑并[4,5-b]吡啶-2-酮化合物及其类似物，其中i

7. 发明申请

WO2006040569A1 THIOPHENE AMIDE COMPOUNDS FOR USE IN THE TREATMENT OR PROPHYLAXIS OF CANCERS 审中-公开
标题翻译：用于治疗或预防癌症的噻吩类化合物
公开(公告)号：WO2006040569A1
公开(公告)日：2006-04-20
申请号：PCT/GB2005/003957
申请日：2005-10-14
申请人： ASTEX THERAPEUTICS LIMITED , GILL, Adrian, Liam , LYONS, John, Francis , THOMPSON, Neil, Thomas
发明人： GILL, Adrian, Liam , LYONS, John, Francis , THOMPSON, Neil, Thomas
IPC分类号： A61K31/5386 , A61K31/4155 , A61K31/5377 , A61K31/496 , A61K31/4439 , A61P35/00
CPC分类号： A61K31/4155 , A61K31/4439 , A61K31/496 , A61K31/5377 , A61K31/5386
摘要： The invention provides the use of a compound for the manufacture of a medicament for the prophylaxis or treatment of a cancer or a para-neoplastic effect associated with a cancer, the para-neoplastic effect being other than cachexia, and the compound being a compound of the formula (I), or a salt, solvate or N-oxide thereof, 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 an aryl or heteroaryl group of 5 to 12 ring members optionally substituted by one or more substituent groups R 7 wherein R 7 is as defined in the claims; R 4 is a group YR 5 or a group R 6 ; Y is NH, O or S; R 5 is selected from (a) optionally substituted carbocyclic and heterocyclic groups having from 3 to 12 ring members; and (b) optionally substituted C 1-8 hydrocarbyl 20 groups; and R 6 is an optionally substituted 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.
摘要翻译：本发明提供化合物在制备用于预防或治疗与癌症相关的癌症或副肿瘤作用的药物中的用途，所述副肿瘤作用不是恶病质，所述化合物是化合物式（I）或其盐，溶剂合物或N-氧化物，其中：R

8. 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。

9. 发明申请

WO03087087A2 PHARMACEUTICAL COMPOUNDS 审中-公开
标题翻译：药物化合物
公开(公告)号：WO03087087A2
公开(公告)日：2003-10-23
申请号：PCT/GB0301507
申请日：2003-04-08
申请人： ASTEX TECHNOLOGY LTD , FREDERICKSON MARTYN , GILL ADRIAN LIAM , PADOVA ALESSANDRO , CONGREVE MILES STUART
发明人： FREDERICKSON MARTYN , GILL ADRIAN LIAM , PADOVA ALESSANDRO , CONGREVE MILES STUART
IPC分类号： 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
CPC分类号： C07D401/06 , A61K31/404 , C07D209/08 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/12
摘要： 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
摘要翻译：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

10. 发明申请

WO2006070198A1 PYRAZOLE DERIVATIVES AS THAT MODULATE THE ACTIVITY OF CDK, GSK AND AURORA KINASES 审中-公开
标题翻译：用于调节CDK，GSK和AURORA KINASES活性的吡唑衍生物
公开(公告)号：WO2006070198A1
公开(公告)日：2006-07-06
申请号：PCT/GB2005/005102
申请日：2005-12-30
申请人： ASTEX THERAPEUTICS LIMITED , BERDINI, Valerio , O'BRIEN, Michael, Alistair , CARR, Maria, Grazia , DAVIES, Nicholas, Gareth, Morse , GILL, Adrian, Liam , NAVARRO, Eva, Figueroa , HOWARD, Steven , TREWARTHA, Gary , WOODHEAD, Andrew, James , WOOLFORD, Alison, Jo-Anne , WYATT, Paul, Graham
发明人： BERDINI, Valerio , O'BRIEN, Michael, Alistair , CARR, Maria, Grazia , DAVIES, Nicholas, Gareth, Morse , GILL, Adrian, Liam , NAVARRO, Eva, Figueroa , HOWARD, Steven , TREWARTHA, Gary , WOODHEAD, Andrew, James , WOOLFORD, Alison, Jo-Anne , WYATT, Paul, Graham
IPC分类号： C07D401/04 , C07D401/14 , C07D403/04 , C07D417/04 , C07D413/04 , C07D471/04 , A61K31/4155 , A61K31/422 , A61K31/427 , A61P35/00
CPC分类号： C07D407/14 , C07D231/40 , C07D401/04 , C07D401/14 , C07D403/04 , C07D405/04 , C07D405/14 , C07D413/04 , C07D417/04 , C07D471/04
摘要： The invention provides a compound of the formula (I): for use in medicine: or salts or tautomers or N-oxides or solvates thereof; wherein R 1 is an optionally substituted heterocyclic group having from 3 to 12 ring members provided that the cyclic group joined to the pyrazole contains at least one heteroatom selected from N, O or S; A is a bond or -Y-(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; n is 0 or 1; Y is a bond or an alkylene chain of 1,2 or 3 carbon atoms in length; 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 optionally substituted carbocyclic and heterocyclic groups having from 3 to 12 ring members or an optionally substituted C 1-8 hydrocarbyl group; with the proviso that R 1 is not formula (II): where X, R 3’ and R 4’ are defined in the claims.
摘要翻译：本发明提供式（I）化合物：用于医药：或其盐或互变异构体或N-氧化物或溶剂合物; 其中R 1是具有3至12个环成员的任选取代的杂环基，条件是连接到吡唑的环状基团含有至少一个选自N，O或S的杂原子; A是键或-Y-（B）n - B是C = O，NR（C = O）或O（C = O），其中R g是氢或C 1-4 >任选被羟基或C 1-4烷氧基取代的烃基; n为0或1; Y是长度为1,2或3个碳原子的键或亚烷基链; 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烷基; R 3选自具有3至12个环成员或任选取代的C 1-8烃基的任选取代的碳环和杂环基; 条件是R 1不是式（II）：其中X，R 3'和R 4'在权利要求中限定。

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