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1. 发明专利

AT555112T 未知
公开(公告)号：AT555112T
公开(公告)日：2012-05-15
申请号：AT07732571
申请日：2007-04-26
申请人： CANCER REC TECH LTD , INST OF CANCER RES THE ROYAL CANCER HOSPITAL , ASTEX THERAPEUTICS LTD
发明人： NICULESCU-DUVAZ DAN , SPRINGER CAROLINE , MARAIS RICHARD , DIJKSTRA HARMEN , MENARD DELPHINE , NICULESCU-DUVAZ ION , DAVIES LAWRENCE , NOURRY ARNAUD
IPC分类号： C07D471/04 , A61K31/437 , A61K31/44 , A61K31/5377 , A61P35/00

2. 发明专利

ES2385103T3 Compuestos de imidazo[4,5-b]piridin-2-ona y análogos de los mismos como compuestos terapéuticos contra el cáncer 未知
公开(公告)号：ES2385103T3
公开(公告)日：2012-07-18
申请号：ES07732571
申请日：2007-04-26
申请人： CANCER REC TECH LTD , INST OF CANCER RES THE ROYAL CANCER HOSPITAL , ASTEX THERAPEUTICS LTD
发明人： NICULESCU-DUVAZ DAN , SPRINGER CAROLINE , MARAIS RICHARD , DIJKSTRA HARMEN , MENARD DELPHINE , NICULESCU-DUVAZ ION , DAVIES LAWRENCE , NOURRY ARNAUD
IPC分类号： C07D471/04 , A61K31/437 , A61K31/44 , A61K31/5377 , A61P35/00
摘要： Un compuesto seleccionado de compuestos de la siguiente fórmula, y sales farmacéuticamente aceptables y solvatos de los mismos: en la que: J es independientemente -NRN1-; RN1 es independientemente -H o -Me; RN2 es independientemente -H o -Me; Y es independientemente -CH >= ; Q es independientemente -O-; cada uno de RP1, RP2, RP5 y RP4 es independientemente -H, -Me, -CF3, -F o -Cl; el grupo A-L- es independientemente A-NH-C( >= O)-NH-, A-C( >= O)-NH- o A-N H-C( >= O)-; A es independientemente fenilo o pirazolilo, y está independientemente sin sustituir o sustituido con uno o más grupos seleccionados de: -(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, -F, -Cl, -Br, -I, -CN, -OH, -OMe, -OEt, -O(iPr), -O(tBu), -OPh, -OCH2Ph, -OCF3, -OCH2CF3, -OCF2CF2H, -OCH2CH2OH, -OCH2CH2OMe -OCH2CH2OEt, -OCH2CH2NH2, -20 OCH2CH2NMe2, -OCH2CH2N(iPr)2, -OCH2CH2-morfolino, -OCH2CH2-piperazino, -OCH2CH2-pirrolidino, -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, -NH(C >= O)Me, -NH(C >= O)Et, -NH(C >= O)nPr, -NH(C >= O)Ph, -NHC( >= O)CH2Ph, -NMe(C >= O)Me, -NMe(C >= O)Et, -NMe(C >= O)Ph, -NMeC( >= O)CH2Ph, -SO2Me, -SO2CF3, -SO2Et, -SO2Ph, -SO2PhMe, -SO2CH2Ph, -SO2NH2, O2NHMe, -SO2NHEt, -SO2NMe2 -SO2NEt2 -SO2-25 morfolino, -SO2NHPh, -SO2NHCH2Ph, -CH2Ph, -CH2Ph-Me, -CH2Ph-OH, -CH2Ph-F, -CH2Ph-Cl, -Ph, -Ph-Me, -Ph-OH, -Ph-OMe, -Ph-NH2, -Ph-F, -Ph-Cl, -Ph-Br, -Ph-I, piridilo, pirazinilo, pirimidinilo, piridazinilo, furanilo, tiofenilo, pirrolilo, imidazolilo, pirazolilo, oxazolilo, tiazolilo, tiadiazolilo, pirrolidinilo, imidazolidinilo, pirazolidinilo, piperidinilo, piperazinilo, azepinilo, tetrahidrofuranilo, tetrahidropiranilo, morfolinilo, azetidinilo, -Me, -Et, -nPr, -iPr, -nBu, -iBu, -sBu, -tBu, -nPe, -iPe, ter-Pe, neo-Pe, -cPr, -cHex, -CH >= CH2, -CH2-CH >= CH2, -CF3, -CHF2, -CH2F, -CCl3, -CBr3, -30 CH2CH2F, -CH2CHF2, H2CF3, -CH2OH, -CH2OMe, -CH2OEt, -CH2NH2, -CH2NMe2, -CH2CH2OH, -CH2CH2OMe -CH2CH2OEt, -CH2CH2CH2NH2, -CH2CH2NMe2, -CH2CH2-morfolino, -CH2CH2-piperazino, -CH2CH2-pirrolidino, y >= O; o: A es un grupo pirazolilo seleccionado de grupos de las siguientes fórmulas: en las que: RPY es independientemente alquilo C1-7 saturado; y RN3 es independientemente fenilo, y está independientemente sin sustituir o sustituido con uno o más sustituyentes seleccionados de -F, -Cl, -Br, -I, -OMe, -OCF3, -Me y -CF3.

3. 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-;

4. 发明专利

NZ572246A IMIDAZO[4,5-B]PYRIDIN-2-ONE AND OXAZOLO[4,5-B]PYRIDIN-2-ONE COMPOUNDS AND ANALOGS THEREOF AS CANCER THERAPEUTIC COMPOUNDS 未知
公开(公告)号：NZ572246A
公开(公告)日：2011-12-22
申请号：NZ57224607
申请日：2007-04-26
申请人： CANCER REC TECH LTD , CANCER RES INST ROYAL , ASTEX THERAPEUTICS LTD
发明人： NICULESCU-DUVAZ DAN , SPRINGER CAROLINE JOY , MARAIS RICHARD MALCOLM , DIJKSTRA HARMEN , MENARD DELPHINE , NICULESCU-DUVAZ ION , DAVIES LAWRENCE , NOURRY ARNAUD
IPC分类号： C07D471/04 , A61K31/437 , A61K31/44 , A61K31/5377 , A61P35/00
摘要： Disclosed are imidazo[4,5-b]pyridine-2-one compounds represented by general formula (I), such as 3-fluoro-5-morpholino-N-(3-(2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin-7-yloxy)phenyl)benzamide. Also disclosed is the use of the compounds of formula (I) for treating cancer.

5. 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.

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.

10. 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.

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