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1. 发明公开

EP3782996A1 NRF2 REGULATORS 审中-公开
公开(公告)号：EP3782996A1
公开(公告)日：2021-02-24
申请号：EP20200207.7
申请日：2016-06-15
申请人： GlaxoSmithKline Intellectual Property Development Limited , Astex Therapeutics Limited
发明人： KERNS, Jeffrey K , CALLAHAN, James Francis , YAN, Hongxing , HEIGHTMAN, Thomas Daniel , GRIFFITHS-JONES, Charlotte Mary , WOOLFORD, Alison Jo-Anne , LI, Tindy , LAKDAWALA SHAH, Ami , DAVIS, Roderick S. , NORTON, David , GOODWIN, Nicole Cathleen , JIN, Yun , HAMILTON, Paris L. , BOEHM, Jeffrey Charles
IPC分类号： C07D417/10 , C07D403/10 , C07D249/04 , C07D249/18 , C07C15/16 , A61P25/00 , A61P11/00 , A61P27/00 , A61P9/00 , A61P35/00 , A61P37/00 , A61K31/5365
摘要： The present invention relates to compositions comprising the compounds of formula (I) for their use as NRF2 regulators

2. 发明授权

EP2861584B1 Pyridopyrazine and naphthyridine derivatives for the treatment of cancer 有权
公开(公告)号：EP2861584B1
公开(公告)日：2020-02-19
申请号：EP13731851.5
申请日：2013-05-30
申请人： Astex Therapeutics Limited
发明人： ANGIBAUD, Patrick René , PILATTE, Isabelle Noëlle Constance , QUEROLLE, Olivier Alexis Georges
IPC分类号： C07D403/04 , A61K31/4985 , A61P35/00 , A61K31/4375

4. 发明公开

EP3421471A1 PURINE AND DEAZAPURINE DERIVATIVES AS PHARMACEUTICAL COMPOUNDS 有权转让
公开(公告)号：EP3421471A1
公开(公告)日：2019-01-02
申请号：EP18182786.6
申请日：2007-04-25
申请人： Astex Therapeutics Limited , The Institute of Cancer Research: Royal Cancer Hospital , Cancer Research Technology Limited
发明人： DAVIES, Thomas, Glanmor , BOYLE, Robert, George , COLLINS, Ian
IPC分类号： C07D471/04 , C07D473/34 , C07D487/04 , A61K31/4523 , A61K31/519 , A61K31/52 , A61K31/522 , A61P35/00
摘要： The invention provides a compound of the formula (I):

or salts, solvates, tautomers or N-oxides thereof, wherein T is N or CR 5 ; J 1 -J 2 is N=C(R 6 ), (R 7 )C=N, (R 8 )N-C(O), (R 8 ) 2 C-C(O), N=N or (R 7 )C=C(R 6 ); E is a monocyclic carbocyclic or heterocyclic group of 5 or 6 ring members, the heterocyclic group containing up to 3 heteroatoms selected from O, N and S; Q 1 is a bond or a saturated C 1-3 hydrocarbon linker group, one of the carbon atoms in the linker group being optionally be replaced by an oxygen or nitrogen atom, or an adjacent pair of carbon atoms may be replaced by CONR q or NR q CO where R q is hydrogen or methyl, or R q is a C 1-4 alkylene chain linked to R 1 or a carbon atom of Q 1 to form a cyclic moiety; and wherein the carbon atoms of the linker group Q 1 may optionally bear one or more substituents selected from fluorine and hydroxy; Q 2 is a bond or a saturated hydrocarbon linker group containing from 1 to 3 carbon atoms, wherein one of the carbon atoms in the linker group may optionally be replaced by an oxygen or nitrogen atom; and wherein the carbon atoms of the linker group may optionally bear one or more substituents selected from fluorine and hydroxy, provided that the hydroxy group when present is not located at a carbon atom α with respect to the G group; and provided that when E is aryl or heteroaryl, then Q 2 is other than a bond; G is hydrogen, NR 2 R 3 , OH or SH provided that when E is aryl or heteroaryl and Q 2 is a bond, then G is hydrogen;
R 1 is hydrogen or an aryl or heteroaryl group, with the proviso that when R 1 is hydrogen and G is NR 2 R 3 , then Q 2 is a bond; and R 2 , R 3 , R 4 , R 6 and R 8 are as defined in the claims, wherein the compound is for use in: (a) the treatment or prophylaxis of a disease or condition in which the modulation (e.g. inhibition) of ROCK kinase or protein kinase P70S6K is indicated; and/or (b) the treatment of a subject or patient population in which the modulation (e.g. inhibition) of ROCK kinase or protein kinase P70S6K is indicated.

5. 发明授权

EP2073803B1 PHARMACEUTICAL COMBINATIONS 有权
公开(公告)号：EP2073803B1
公开(公告)日：2018-09-19
申请号：EP07824133.8
申请日：2007-10-12
申请人： Astex Therapeutics Limited
发明人： GALLAGHER, Neil, James , LYONS, John, Francis , THOMPSON, Neil, Thomas , YULE, Stephen, Murray , MURRAY, Christopher, William
IPC分类号： A61K31/403
CPC分类号： A61K31/403 , A61K31/4035 , A61K45/06 , A61K2300/00
摘要： The invention provides combinations comprising (or consisting essentially of) one or more ancillary compound(s) and a compound of the formula (I): or salts, tautomers, solvates and N-oxides thereof; wherein R1 is hydroxy or hydrogen; R2 is hydroxy; methoxy or hydrogen; provided that at least one of R1 and R2 is hydroxy; R3 is selected from hydrogen; halogen; cyano; optionally substituted C1-5 hydrocarbyl and optionally substituted C1-5 hydrocarbyloxy; R4 is selected from hydrogen; a group —(O)n—R7 where n is 0 or 1 and R7 is an optionally substituted acyclic C1-5 hydrocarbyl group or a monocyclic carbocyclic or heterocyclic group having 3 to 7 ring members; halogen; cyano; hydroxy; amino; and optionally substituted mono- or di-C1-5 hydrocarbyl-amino; or R3 and R4 together form a monocyclic carbocyclic or heterocyclic ring of 5 to 7 ring members; and NR5R6 forms an optionally substituted bicyclic heterocyclic group having 8 to 12 ring members of which up to 5 ring members are heteroatoms selected from oxygen, nitrogen and sulphur. The combinations have activity as Hsp90 and/or glycogen synthase kinase-3 and/or cyclin dependent kinase inhibitors.

6. 发明公开

EP3371167A1 ARYLCYCLOHEXYL PYRAZOLES AS NRF2 REGULATORS 审中-公开
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
申请人： GlaxoSmithKline Intellectual Property Development Limited , Astex Therapeutics Limited
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.

7. 发明公开

EP3356350A1 ISOINDOLINONE INHIBITORS OF THE MDM2-P53 INTERACTION HAVING ANTICANCER ACTIVITY 有权转让
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
申请人： Astex Therapeutics Limited , Cancer Research Technology Limited
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.

8. 发明授权

EP2546233B1 HYDROBENZAMIDE DERIVATIVES AS INHIBITORS OF HSP90 有权
标题翻译：氢化苯甲酰胺衍生物作为HSP90的抑制剂
公开(公告)号：EP2546233B1
公开(公告)日：2018-02-21
申请号：EP12187611.4
申请日：2007-10-12
申请人： Astex Therapeutics Limited
发明人： Frederickson, Martyn , Lyons, John, Francis , Thompson, Neil, Thomas , Vinkovic, Mladen , Williams, Brian , Woodhead, Andrew, James , Woolford, Alison, Jo-Anne
IPC分类号： C07D209/44 , C07C65/05 , C07C69/02 , A61P35/00 , A61K31/496
CPC分类号： C07C67/317 , C07C59/08 , C07C67/313 , C07C69/92 , C07C235/60 , C07D209/44
摘要： The invention provides an acid addition salt of a compound of the formula (1) which is a salt fomred with L-lactic acid. Also provided by the invention are combinations comprising said salt. The invention also provides medical uses of said salt or combinations thereof.

9. 发明公开

EP3083616A1 BICYCLIC HETEROCYCLE COMPOUNDS AND THEIR USES IN THERAPY 有权转让
标题翻译：双环杂环化合物及其用途在治疗中
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
申请人： Astex Therapeutics Limited
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.

10. 发明授权

EP2121687B1 TRICYCLIC AMINE DERIVATIVES AS PROTEIN TYROSINE KINASE INHIBITORS 有权
标题翻译：三环AMIN衍生物作为蛋白酪氨酸激酶抑制剂
公开(公告)号：EP2121687B1
公开(公告)日：2015-10-14
申请号：EP07848681.8
申请日：2007-12-21
申请人： Astex Therapeutics Limited
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

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