专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明专利

ES2550050T3 Compuestos de imidazo[4,5-b]piridin-2-ona y oxazolo[4,5-b]piridin-2-ona y análogos de los mismos como compuestos terapéuticos 未知
公开(公告)号：ES2550050T3
公开(公告)日：2015-11-04
申请号：ES05796691
申请日：2005-10-21
申请人： CANCER REC TECH LTD , CANCER RES INST ROYAL , ASTEX THERAPEUTICS LTD
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 , A61K31/4353 , A61P35/00 , C07D498/04
摘要： Un compuesto seleccionado entre compuestos de la siguiente fórmula, y sales y solvatos farmacéuticamente aceptables de los mismos:**Fórmula** en la que: J es independientemente -O- o -NRN1-; RN1 es independientemente -H o un grupo seleccionado entre: alquilo C1-5 alifático saturado; alquenilo C2-5 alifático; alquinilo C2-5 alifático; cicloalquilo C3-6 saturado; cicloalquenilo C3-6; carboarilo C6; heteroarilo C5-6; y heterocíclico C5-6; y está independientemente sin sustituir o sustituido con uno o más sustituyentes seleccionados entre -(C>=O)NH2, - (C>=O)NMe2, -(C>=O)NEt2, -(C>=O)N(iPr)2, -(C>=)N(CH2CH2OH)2, -(C>=O)-morfolino, -(C>=O)NHPh, -(C>=O)NHCH2Ph, - C(>=O)H, -(C>=O)Me, -(C>=O)Et, -(C>=O)(tBu), -(C>=O)-cHex, -(C>=O)Ph, -(C>=O)CH2Ph, -OH, -OMe, -OEt, -O(iPr), - O(tBu), -OPh, -OCH2Ph, -OCF3, -OCH2CF3, -OCH2CH2OH, -OCH2CH2OMe, -OCH2CH2OEt, -OCH2CH2NH2, - OCH2CH2NMe2, -OCH2CH2N(iPr)2, -OPh-Me, -OPh-OH, -OPh-OMe, -OPh-F, -OPh-Cl, -OPh-Br, -OPh-I, -NH2, - NHMe, -NHEt, -NH(iPr), -NMe2, -NEt2, -N(iPr)2, -N(CH2CH2OH)2, -NHPh, -NHCH2Ph, piperidino, piperazino, morfolino, -SO2Me, -SO2CF3, -SO2Et, -SO2Ph, -SO2PhMe, -SO2CH2Ph, -Ph, -Ph-Me, -Ph-OH, -Ph-OMe, -Ph-NH2, - Ph-F, -Ph-Cl, -Ph-Br, -Ph-I, piridinilo, pirazinilo, pirimidinilo, piridazinilo, furanilo, tiofenilo, pirrolilo, imidazolilo, pirazolilo, oxazolilo, tiazolilo, tiadiazolilo, pirrolidinilo, imidazolidinilo, pirazolidinilo, piperidinilo, piperazinilo, azepinilo, tetrahidrofuranoílo, tetrahidropiranilo, morfolinilo y azetidinilo; RN2 es independientemente -H o un grupo seleccionado entre: alquilo C1-5 alifático saturado; alquenilo C2-5 alifático; alquinilo C2-5 alifático; cicloalquilo C3-6 saturado; cicloalquenilo C3-6; carboarilo C6; heteroarilo C5-6; y heterocíclico C5-6; y está independientemente sin sustituir o sustituido con uno o más sustituyentes seleccionados entre -(C>=O)NH2, - (C>=O)NMe2, -(C>=O)NEt2, -(C>=O)N(iPr)2, -(C>=O)N(CH2CH2OH)2, -(C>=O)-morfolino, -(C>=O)NHPh, -(C>=O)NHCH2Ph, - C(>=O)H, -(C>=O)Me, -(C>=O)Et, -(C>=O)(tBu), -(C>=O)-cHex, -(C>=O)Ph, -(C>=O)CH2Ph, -OH, -OMe, -OEt, -O(iPr), - O(tBu), -OPh, -OCH2Ph, -OCF3, -OCH2CF3, -OCH2CH2OH, -OCH2CH2OMe, -OCH2CH2OEt, -OCH2CH2NH2, - OCH2CH2NMe2, -OCH2CH2N(iPr)2, -OPh-Me, -OPh-OH, -OPh-OMe, -OPh-F, -OPh-Cl, -OPh-Br, -OPh-I, -NH2, - NHMe, -NHEt, -NH(iPr), -NMe2, -NEt2, -N(iPr)2, -N(CH2CH2OH)2, -NHPh, -NHCH2Ph, piperidino, piperazino, morfolino, -SO2Me, -SO2CF3, -SO2Et, -SO2Ph, -SO2PhMe, -SO2CH2Ph, -Ph, -Ph-Me, -Ph-OH, -Ph-OMe, -Ph-NH2, - Ph-F, -Ph-Cl, -Ph-Br, -Ph-I, piridinilo, pirazinilo, pirimidinilo, piridazinilo, furanilo, tiofenilo, pirrolilo, imidazolilo, pirazolilo, oxazolilo, tiazolilo, tiadiazolilo, pirrolidinilo, imidazolidinilo, pirazolidinilo, piperidinilo, piperazinilo, azepinilo, tetrahidrofuranoílo, tetrahidropiranilo, morfolinilo y azetidinilo; Y es independientemente -CH>= o -N>=; Q es independientemente -(CH2)j-M-(CH2)k- en la que: j es independientemente 0, 1 o 2; k es independientemente 0, 1 o 2; j+k es 0, 1 o 2; M es independientemente -O-, -S-, -NH-, -NMe- o -CH2-; cada uno de RP1, RP2, RP3 y RP4 es independientemente -H o un grupo seleccionado entre: -Me, -Et, -nPr, -iPr, -nBu, -iBu, -sBu, -tBu, -CH>=CH2, -CH2-CH>=CH2, -C≡CH, -CH2-C≡CH, ciclopropilo, ciclobutilo, ciclopentilo, ciclohexilo, ciclopropenilo, ciclobutenilo, ciclopentenilo, ciclohexenilo, -CF3, -CH2CF3, -CF2CF3, -C(>=O)OH, -C(>=O)OMe, - C(>=O)OEt, -OH, -OMe, -OEt, -SH, -SMe, -SEt, -C(>=O)NH2, -C(>=O)NHMe, -C(>=O)NHEt, -C(>=O)NMe2, - C(>=O)morfolino, -C(>=O)piperidino, -C(>=O)piperizino, -NH2, -NHMe, -NMe2, -NHEt, -NEt2, morfolino, piperidino, piperazino, -NHC(>=O)Me, -NMeC(>=O)Me, -NHC(>=O)Et, -NMeC(>=O)Et, -F, -Cl, -Br, -I y -CN; y adicionalmente RP1 y RP2 tomados juntos pueden ser -CH>=CH-CH>=CH-;

2. 发明专利

AU2005297089A1 Imidazo[4,5-b]pyridin-2-one and oxazolo[4,5-b]pyridin-2-one compounds and analogs thereof as therapeutic compounds 未知
公开(公告)号：AU2005297089A1
公开(公告)日：2006-04-27
申请号：AU2005297089
申请日：2005-10-21
申请人： ASTEX THERAPEUTICS LTD , CANCER REC TECH LTD , CANCER RES INST ROYAL
发明人： NICULESCU-DUVAZ DAN , GILL ADRIAN LIAM , VELA ESTEBAN ROMAN , DIJKSTRA HARMEN , MENARD DELPHINE , TAYLOR RICHARD DAVID , GAULON CATHERINE , MARAIS RICHARD MALCOLM , SPRINGER CAROLINE JOY
IPC分类号： C07D471/04 , A61K31/4353 , A61P35/00 , C07D498/04
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 -NRN1-; RN1, if present, is independently -H or a substituent; RN2 is independently -H or a substituent; Y is independently -CH- or -N-; Q is independently -(CH2)j-M-(CH2)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 -CH2-; each of RP1, RP2, RP3, and RP4 is independently -H or a substituent; and additionally RP1 and RP2 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 -CH2-, -NRN-, -C(-X)-, or -S(-O)2-; exactly one linker moiety is -NRN-, or: exactly two linker moieties are -NRN-; 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 -NRN-; X is independently -O or -S; each RN is independently -H or a substituent; A is independently: C6-14carboaryl, C5-14heteroaryl, C3-12carbocyclic, C3-12heterocyclic; 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.

4. 发明专利

NZ555005A Imidazo[4,5-B]pyridin-2-one and oxazolo[4,5-B]pyridin-2-one compounds and analogs thereof as therapeutic compounds 未知
公开(公告)号：NZ555005A
公开(公告)日：2010-10-29
申请号：NZ55500505
申请日：2005-10-21
申请人： CANCER REC TECH LTD , ASTEX THERAPEUTICS LTD , CANCER RES INST ROYAL
发明人： NICULESCU-DUVAZ DAN , DIJKSTRA HARMEN , GAULON CATHERINE , MENARD DELPHINE , SPRINGER CAROLINE JOY , GILL ADRIAN LIAM , TAYLOR RICHARD DAVID , MARAIS RICHARD MALCOLM , ROMAN VELA ESTEBAN
IPC分类号： C07D471/04 , A61K31/4353 , A61P35/00 , C07D498/04
摘要： Disclosed are imidazo[4,5-B]pyridine-2-one and oxazolo[4,5-B]pyridine-2-one compounds of the formula as depicted, pharmaceutically acceptable salts and solvates thereof, pharmaceutical compositions thereof and their use in treating cell proliferation, cancer and disease of conditions that are ameliorated by the inhibition of RAF.

5. 发明专利

CA2584651A1 IMIDAZO[4,5-B]PYRIDIN-2-ONE AND OXAZOLO[4,5-B]PYRIDIN-2-ONE COMPOUNDS AND ANALOGS THEREOF AS THERAPEUTIC COMPOUNDS 未知
公开(公告)号：CA2584651A1
公开(公告)日：2006-04-27
申请号：CA2584651
申请日：2005-10-21
申请人： CANCER REC TECH LTD , CANCER RES INST ROYAL , ASTEX THERAPEUTICS LTD
发明人： TAYLOR RICHARD DAVID , DIJKSTRA HARMEN , MARAIS RICHARD MALCOLM , ROMAN VELA ESTEBAN , NICULESCU-DUVAZ DAN , GILL ADRIAN LIAM , GAULON CATHERINE , SPRINGER CAROLINE JOY , MENARD DELPHINE
IPC分类号： C07D471/04 , A61K31/4353 , A61P35/00 , C07D498/04
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 -NRN1-; RN1, if present, is independently -H or a substituent; RN2 is independently -H or a substituent; Y is independently -CH- or -N-; Q is independently -(CH2)j-M-(CH2)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 -CH2-; each of RP1, RP2, RP3, and RP4 is independently -H or a substituent; and additionally RP1 and RP2 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 -CH2-, -NRN-, -C(-X)-, or -S(-O)2-; exactly one linker moiety is -NRN-, or: exactly two linker moieties are -NRN-; 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 -NRN-; X is independently -O or -S; each RN is independently -H or a substituent; A is independently: C6-14carboaryl, C5-14heteroaryl, C3-12carbocyclic, C3-12heterocyclic; 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.

7. 发明专利

CA2584651C IMIDAZO[4,5-B]PYRIDIN-2-ONE AND OXAZOLO[4,5-B]PYRIDIN-2-ONE COMPOUNDS AND ANALOGS THEREOF AS THERAPEUTIC COMPOUNDS 未知
公开(公告)号：CA2584651C
公开(公告)日：2013-05-28
申请号：CA2584651
申请日：2005-10-21
申请人： CANCER REC TECH LTD , CANCER RES INST ROYAL , ASTEX THERAPEUTICS LTD
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 , A61K31/4353 , A61P35/00 , C07D498/04
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 -NRN1-; RN1, if present, is independently -H or a substituent; RN2 is independently -H or a substituent; Y is independently -CH= or -N=; Q is independently -(CH2)j-M-(CH2)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 -CH2-; each of RP1, RP2, RP3, and RP4 is independently -H or a substituent; and additionally RP1 and RP2 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 -CH2-,-NRN-, -C(=X)-, or -S(=O)2-; exactly one linker moiety is -NRN-, or: exactly two linker moieties are -NRN-; 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 -NRN-; X is independently =O or =S; each RN is independently -H or a substituent; A is independently: C6-14carboaryl, C5-14heteroaryl, C3-12carbocyclic, C3-12heterocyclic; 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.

8. 发明申请

WO2006070195A8 PYRAZOLE COMPOUNDS THAT MODULATE THE ACTIVITY OF CDK, GSK AND AURORA KINASES 审中-公开
标题翻译：调节CDK，GSK和AURORA KINASES活性的吡咯化合物
公开(公告)号：WO2006070195A8
公开(公告)日：2006-08-24
申请号：PCT/GB2005005097
申请日：2005-12-30
申请人： ASTEX THERAPEUTICS LTD , BERDINI VALERIO , CARR MARIA GRAZIA , GILL ADRIAN LIAM , HOWARD STEVEN , NAVARRO EVA FIGUEROA , TREWARTHA GARY , REES DAVID CHARLES , VINKOVIC MLADEN , WYATT PAUL GRAHAM
发明人： BERDINI VALERIO , CARR MARIA GRAZIA , GILL ADRIAN LIAM , HOWARD STEVEN , NAVARRO EVA FIGUEROA , TREWARTHA GARY , REES DAVID CHARLES , VINKOVIC MLADEN , WYATT PAUL GRAHAM
IPC分类号： C07D403/04 , A61K31/4184 , A61P35/00 , C07D407/14 , C07D513/04
CPC分类号： C07D401/14 , C07D403/04 , C07D403/14 , C07D405/14 , C07D407/14 , C07D413/14 , C07D487/04 , C07D513/04
摘要： The invention provides a compound of the formula (I): or a salt, solvate, tautomer or N-oxide thereof, wherein M is selected from a group D1 and a group D2: and R', E, A and X are as defined in the claims. Also provided are pharmaceutical compositions containing the compounds, processes for making the compounds and the use of the compounds in the prophylaxis or treatment of a disease state mediated by a CDK kinase, GSK-3 kinase or Aurora kinase.
摘要翻译：本发明提供式（I）化合物或其盐，溶剂化物，互变异构体或N-氧化物，其中M选自D1和D2组：R'，E，A和X如上所定义在权利要求中。还提供了含有化合物的药物组合物，制备该化合物的方法以及该化合物在预防或治疗由CDK激酶，GSK-3激酶或极光激酶介导的疾病状态中的用途。

9. 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。

10. 发明申请

WO2008007123A3 PHARMACEUTICAL COMPOUNDS 审中-公开
标题翻译：药物化合物
公开(公告)号：WO2008007123A3
公开(公告)日：2008-02-28
申请号：PCT/GB2007002655
申请日：2007-07-13
申请人： ASTEX THERAPEUTICS LTD , NOVARTIS AG , CONGREVE MILES STUART , GILL ADRIAN LIAM , HOWARD STEVEN , MORTENSON PAUL NEIL , BESONG GILBERT EBAI
发明人： CONGREVE MILES STUART , GILL ADRIAN LIAM , HOWARD STEVEN , MORTENSON PAUL NEIL , BESONG GILBERT EBAI
IPC分类号： C07D401/12 , A61K31/4155 , A61P25/28 , A61P31/10 , A61P31/12 , A61P35/00 , A61P37/00 , C07D401/14 , C07D417/12 , C07D497/04
CPC分类号： C07D417/12 , C07D401/12 , C07D401/14 , C07D513/04
摘要： The invention provides a cyclin dependent kinase (e.g. cdk-4 kinase) inhibitor of the formula (I) or a salt, tautomer, solvate or N-oxide thereof; wherein R 1 is an optionally substituted monocyclic or bicyclic aryl or heteroaryl group containing 0-2 heteroatoms selected from O, N and S wherein the optional substituents are selected from halogen, C 1-4 alkyl, C 1-4 alkoxy, C 3-4 cycloalkyl and cyano, and wherein the C 1-4 alkyl and C 1-4 alkoxy groups are each optionally further substituted by C 1-2 alkoxy or one or more halogen atoms; and E is a group E1, E2, E3 or E4: formulae E1, E2, E3, E4 wherein n, q, A5 B, T, U, V, W, Z, R 2 , R 5 , R 6 and R 7 are as defined in the claims.
摘要翻译：本发明提供式（I）的细胞周期蛋白依赖性激酶（例如cdk-4激酶）抑制剂或其盐，互变异构体，溶剂化物或N-氧化物; 其中R 1是任选取代的含有0-2个选自O，N和S的杂原子的单环或双环芳基或杂芳基，其中任选的取代基选自卤素，C 1-4烷基，烷基，C 1-4烷氧基，C 3-4环烷基和氰基，并且其中C 1-4烷基和C 1-4烷基 1-4烷氧基各自任选进一步被C 1-2烷氧基或一个或多个卤素原子取代; 和E是基团E1，E2，E3或E4：式E1，E2，E3，E4其中n，q，A5 B，T，U，V，W，Z，R 2，R R5，R6和R7如权利要求中所定义。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式