-
1.发明公开ARYL-ALKYLAMINES AND HETEROARYL-ALKYLAMINES AS PROTEIN KINASE INHIBITORS 审中-公开芳基烷基和HETEROARYLALKYLAMINE ALS蛋白激酶抑制剂
公开(公告)号：EP1904451A1
公开(公告)日：2008-04-02
申请号：EP06755591.2
申请日：2006-06-21
申请人： Astex Therapeutics Limited , THE INSTITUTE OF CANCER RESEARCH: ROYAL CANCER HOSPITAL , Cancer Research Campaign Technology Limited , AstraZeneca AB
发明人： WOODHEAD, Steven, John , DOWNHAM, Robert , HAMLETT, Christopher , HOWARD, Steven , SORE, Hannah, Fiona , VERDONK, Marinus, Leendert , WALKER, David, Winter , LUKE, Richard, William, Arthur
IPC分类号： C07D231/12 , A61K31/415 , A61P37/02
CPC分类号： C07D231/12
摘要： The invention provides a compound of the formula (II): or a salt, solvate, tautomer or N-oxide thereof; wherein n is 0 or 1; one of Y1 and Y2 is CH and the other is selected from CH, CR8 and N; q is 0, 1 or 2 provided that q is 0 or 1 when Y1 or Y2 is CR8; R1 is an aryl or heteroaryl group of 5 to 10 ring members; R2a and R3a each are hydrogen, C1-4 hydrocarbyl or C1-4 acyl wherein the hydrocarbyl and acyl moieties are optionally substituted by fluorine, hydroxy, amino, methylamino, dimethylamino or methoxy; or NR2aR3a forms an imidazole group or a saturated monocyclic 4-7 membered heterocyclic group optionally containing a second heteroatom ring member selected from O and N; R18 is hydrogen or methyl; R19 is hydrogen or methyl; R24 is hydrogen or R24, R2a and the intervening nitrogen atom and carbon atoms together form an azetidine, pyrrolidine or piperidine ring; R25 is hydrogen or a C1-4 alkyl group wherein the C1-4 alkyl group is optionally substituted by hydroxy or amino provided that there are at least two carbon atoms between the hydroxy or amino group and the oxygen atom to which R25 is attached; and R4 and R5 each are hydrogen or a substituent as defined in the claims
-
公开(公告)号：EP1919875A2
公开(公告)日：2008-05-14
申请号：EP06755590.4
申请日：2006-06-21
申请人： Astex Therapeutics Limited , The Institute of Cancer Research : The Royal Cancer Hospital , AstraZeneca AB
发明人： SORE, Hannah, Fiona , BOYLE, Robert, George , HAMLETT, Christopher , SAXTY, Gordon , VERDONK, Marinus, Leendert , WALKER, David, Winter , WOODHEAD, Steven, John , HOWARD, Steven
IPC分类号： C07D231/12 , C07D401/10 , C07D401/12 , C07D401/14
CPC分类号： C07D231/12 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/14 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/14
摘要： The invention provides a compound of the formula (I) or a salt, solvate, tautomer or N-oxide thereof; wherein A is a saturated hydrocarbon linker group; E is a monocyclic or bicyclic carbocyclic or heterocyclic group; L1 is a bond or a linker selected from C1-C4 alkenylene, C1-C4 alkynylene, -CONR’, -NR’CO, -S-, -C(O)-, -C(NR11)-, -C(S)-, -N(R11)2, C(=CHR11), -SO- and -SO2-; or L1 together with t R16 forms an 8-12 membered fused bicyclic heteroaryl ring system; L3 is a bond or a linker selected from CONH and HNCO; provided that L1 and L3 cannot both be linkers simultaneously; and provided also that L1 and L3 cannot both be a bond simultaneously; R16 is an optionally substituted 5- to 12-membered monocyclic or bicyclic carbocyclic or heterocyclic ring; L2 is absent or is a linker selected from C]-C4 alkylene, Ci-C4 alkenylene, Ci-C4 alkynylene, -CONR’-, -NR’CO-, -O-, -S-, -C(O)-, C(=CHR11), C(S)-, -N(R11)2, C3-4 cycloalkanediyl, -SO- and -SO2-; R17 is absent or is C1-6 alkyl or an optionally substituted 5 to 12 membered carbocyclic or heterocyclic ring; provided that when R17 is absent, then L2 is also absent; and R2, R3, R4, R5, R11 and R’ are as defined in the claims. Compounds (I) modulate (PKA) and (PKB).
-
公开(公告)号：EP3371167A1
公开(公告)日：2018-09-12
申请号：EP16784575.9
申请日：2016-10-06
发明人： CALLAHAN, James Francis , KERNS, Jeffrey K. , LI, Tindy , MCCLELAND, Brent W. , NIE, Hong , PERO, Joseph E. , DAVIES, Thomas Glanmor , HEIGHTMAN, Thomas Daniel , GRIFFITHS-JONES, Charlotte Mary , HOWARD, Steven , NORTON, David , VERDONK, Marinus Leendert , WOOLFORD, Alison Jo-Anne
IPC分类号： C07D401/14 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/12 , A61K31/41 , A61K31/4196 , A61K31/445
CPC分类号： C07D231/14 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/08 , C07D403/10 , C07D403/14
摘要： methods of making them, pharmaceutical compositions containing them and their use as NRF2 regulators.
-
公开(公告)号：EP3356350A1
公开(公告)日：2018-08-08
申请号：EP16777770.5
申请日：2016-09-29
发明人： CHESSARI, Gianni , HOWARD, Steven , BUCK, Ildiko Maria , CONS, Benjamin David , JOHNSON, Christopher Norbert , HOLVEY, Rhian Sara , REES, David Charles , ST. DENIS, Jeffrey David , TAMANINI, Emiliano , GOLDING, Bernard Thomas , HARDCASTLE, Ian Robert , CANO, Celine Florence , MILLER, Duncan Charles , CULLY, Sarah , NOBLE, Martin Edward Mäntylä , OSBORNE, James Daniel , PEACH, Joanne , LEWIS, Arwel , HIRST, Kim Louise , WHITTAKER, Benjamin Paul , WATSON, David Wyn , MITCHELL, Dale Robert , GRIFFIN, Roger John
IPC分类号： C07D403/12 , C07D405/14 , C07F9/572 , C07B59/00 , C07D403/06 , C07D405/12 , C07D413/06 , C07D413/12 , C07D209/48 , A61K31/4035 , A61P35/00
CPC分类号： C07D209/48 , C07B2200/05 , C07D403/06 , C07D403/12 , C07D405/12 , C07D405/14 , C07D413/06 , C07D413/12 , C07F9/5728
摘要： The invention provides a compound of formula (I): (I) or tautomer or a solvate or a pharmaceutically acceptable salt thereof, wherein the various substituents are as defined in the claims. Also provided are pharmaceutical compositions containing the compounds of formula (I), processes for making the compounds and the medical uses of the compounds.
-
公开(公告)号：EP3083616A1
公开(公告)日：2016-10-26
申请号：EP14815838.9
申请日：2014-12-19
发明人： CHESSARI, Gianni , JOHNSON, Christopher Norbert , HOWARD, Steven , DAY, James Edward Harvey , BUCK, Ildiko Maria , GRIFFITHS-JONES, Charlotte Mary , SAXTY, Gordon , TAMANINI, Emiliano , WILSHER, Nicola Elisabeth
IPC分类号： C07D471/04 , A61K31/437 , A61P35/00
CPC分类号： C07D471/04 , A61K31/5377
摘要： The invention relates to new bicyclic heterocycle compounds, to pharmaceutical compositions comprising the compounds and to the use of the compounds in the treatment of diseases, e.g. cancer.
-
6.发明公开PYRAZOLE DERIVATIVES AS THAT MODULATE THE ACTIVITY OF CDK, GSK AND AURORA KINASES 审中-公开作者CDK，GSK和Aurora激酶MODULLIERENDE吡唑衍生物酶活性的影响
公开(公告)号：EP1836188A1
公开(公告)日：2007-09-26
申请号：EP05823522.7
申请日：2005-12-30
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 R1 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, NRg(C=O) or O(C=O) wherein Rg is hydrogen or C1-4 hydrocarbyl optionally substituted by hydroxy or C1-4 alkoxy; n is 0 or 1; Y is a bond or an alkylene chain of 1,2 or 3 carbon atoms in length; R2 is hydrogen; halogen; C1-4 alkoxy (e.g. methoxy); or a C1-4 hydrocarbyl group optionally substituted by halogen (e.g. fluorine), hydroxyl or C1-4 alkoxy (e.g. methoxy); R3 is selected from optionally substituted carbocyclic and heterocyclic groups having from 3 to 12 ring members or an optionally substituted C1-8 hydrocarbyl group; with the proviso that R1 is not formula (II): where X, R3’ and R4’ are defined in the claims.
-
公开(公告)号：EP3601272A1
公开(公告)日：2020-02-05
申请号：EP18715926.4
申请日：2018-03-28
发明人： HOWARD, Steven , CONS, Benjamin, David , ST. DENIS, Jeffrey, David , GRIFFITHS-JONES, Charlotte, Mary , HISCOCK, Steven, Douglas , HOLVEY, Rhian, Sara , BURNS, Alan, Richard , COUSIN, David , DEXTER, Hannah, Louise , PARRA, Guillaume, François , WATTS, John, Paul , JEWELL, Robert , STOCKWELL, Jennifer, Ann , HIRST, Kim, Louise , LEMASSON, Isabelle, Anne , NASH, David, John , OSBORNE, James, Daniel , PRIEDE, Jonas, Calleja , RICHARDS, Nicholas, Paul , DUMAS, Aaron, Michael , BISHOP, Brian, Christopher , PARRY-JONES, David , SCOTT, Jeremy, Peter , SHANMUGHAM, Meenakshi, Sundaram , MULLENS, Peter, Richard , LATHBURY, David, Charles , DIXON, Darren, James , GAUNT, Matthew, James
IPC分类号： C07D405/06
-
8.发明授权IMIDAZOLE DERIVATIVES AND THEIR USE AS MODULATORS OF CYCLIN DEPENDENT KINASES 有权咪唑衍生物及其作为细胞周期蛋白依赖性激酶的调节剂
公开(公告)号：EP2424843B1
公开(公告)日：2014-03-26
申请号：EP10719772.5
申请日：2010-04-30
发明人： HOWARD, Steven , MORTENSON, Paul Neil , HISCOCK, Steven Douglas , WOOLFORD, Alison Jo-Anne , WOODHEAD, Andrew James , CHESSARI, Gianni , O'REILLY, Marc , CONGREVE, Miles Stuart , DAGOSTIN, Claudio , CHO, Young Shin , YANG, Fan , CHEN, Christine Hiu-Tung , BRAIN, Christopher Thomas , LAGU, Bharat , WANG, Yaping , KIM, Sunkyu , GRIALDES, John , LUZZIO, Michael Joseph , PEREZ, Lawrence Blas , LU, Yipin
IPC分类号： C07D233/22 , C07D235/12 , C07D401/06 , C07D401/10 , C07D401/14 , C07D409/10 , C07D409/14 , C07D413/14 , C07D417/10 , A61K31/4164 , A61K31/4178 , A61P35/00
CPC分类号： C07D471/04 , C07D233/22 , C07D233/24 , C07D235/12 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/14 , C07D403/10 , C07D405/14 , C07D409/10 , C07D409/14 , C07D413/10 , C07D413/14 , C07D417/10 , C07D417/14 , C07D487/04 , C07D519/00
-
9.发明授权
公开(公告)号：EP1648426B1
公开(公告)日：2014-01-08
申请号：EP04743172.1
申请日：2004-07-05
发明人： BERDINI, Valerio 436 Cambridge Science Park , 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： A61K31/4184 , C07D403/04 , A61P35/00 , A61P31/10
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
-
10.发明公开IMIDAZOLE DERIVATIVES AND THEIR USE AS MODULATORS OF CYCLIN DEPENDENT KINASES 有权咪唑衍生物及其作为细胞周期蛋白依赖性激酶的调节剂
公开(公告)号：EP2424843A1
公开(公告)日：2012-03-07
申请号：EP10719772.5
申请日：2010-04-30
发明人： HOWARD, Steven , MORTENSON, Paul Neil , HISCOCK, Steven Douglas , WOOLFORD, Alison Jo-Anne , WOODHEAD, Andrew James , CHESSARI, Gianni , O'REILLY, Marc , CONGREVE, Miles Stuart , DAGOSTIN, Claudio , CHO, Young Shin , YANG, Fan , CHEN, Christine Hiu-Tung , BRAIN, Christopher Thomas , LAGU, Bharat , WANG, Yaping , KIM, Sunkyu , GRIALDES, John , LUZZIO, Michael Joseph , PEREZ, Lawrence Blas , LU, Yipin
IPC分类号： C07D233/22 , C07D235/12 , C07D401/06 , C07D401/10 , C07D401/14 , C07D409/10 , C07D409/14 , C07D413/14 , C07D417/10 , A61K31/4164 , A61K31/4178 , A61P35/00
CPC分类号： C07D471/04 , C07D233/22 , C07D233/24 , C07D235/12 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/14 , C07D403/10 , C07D405/14 , C07D409/10 , C07D409/14 , C07D413/10 , C07D413/14 , C07D417/10 , C07D417/14 , C07D487/04 , C07D519/00
摘要： The invention provides compounds of the formula (I): and salts, tautomers, solvates and N-oxides thereof; wherein Q is CH or N; X is N, N
+ -O
- or CR
3 ; Y is N, N
+ -O
- or CR
3a ; R
1 and R
2 are independently selected from hydrogen and various substituents as defined in the claims; or R
1 and R
2 together with the atoms to which they are attached, link to form an optionally substituted carbocyclic or heterocyclic aromatic or non-aromatic ring of 4 to 7 members; R
3 is selected from hydrogen and various substituents; and R
3a is selected from hydrogen and various substituents as defined in the claims. Also provided are pharmaceutical compositions containing the compounds of formula (I), processes for making the compounds and the medical uses of the compounds. The compounds of formula (I) have activity as inhibitors of CDK kinases and are useful in the treatment of
inter alia proliferative diseases such as cancers.
-
-
-
-
-
-
-
-
-
搜索结果
19 条记录 (耗时 0.048 秒)
