公开(公告)号：EP1706385A1

公开(公告)日：2006-10-04

申请号：EP04806258.2

申请日：2004-12-23

申请人： Astex Therapeutics Limited ,  Cancer Research Technology Limited ,  THE INSTITUTE OF CANCER RESEARCH: ROYAL CANCER HOSPITAL

发明人： BERDINI, Valerio ,  SAXTY, Gordon ,  VERDONK, Marinus, Leendert ,  WOODHEAD, Steven, John ,  WYATT, Paul, Graham ,  BOYLE, Robert, George ,  SORE, Hannah, Fiona ,  WALKER, David, Winter ,  COLLINS, Ian ,  DOWNHAM, Robert ,  CARR, Robin, Arthur, Ellis

IPC分类号： C07D231/12 ,  C07D413/10 ,  C07D401/10 ,  A61K31/415 ,  A61P37/02

CPC分类号： A61K31/415 ,  A61K9/0019 ,  A61K9/20 ,  A61K9/48 ,  A61K31/4155 ,  A61K31/4178 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/497 ,  A61K31/5377 ,  A61K31/551 ,  A61K45/06 ,  C07D231/12 ,  C07D401/04 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D403/10 ,  C07D403/12 ,  C07D405/04 ,  C07D413/10

摘要： The invention provides compounds of the formula: (I) having protein kinase B inhibiting activity: wherein A is a saturated hydrocarbon linker group containing from 1 to 7 carbon atoms, the linker group having a maximum chain length of 5 atoms extending between Rl and NR2R3 and a maximum chain length of 4 atoms extending between E and NR2R3, 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 inker group A may optionally bear one or more substituents selected from oxo, fluorine and hydroxy, provided that the hydroxy group when present is not located at a carbon atom a with respect to the NR2R3 group and provided that the oxo group when present is located at a carbon atom a with respect to the NR2R3 group; E is a monocyclic or bicyclic carbocyclic or heterocyclic group; Rl is an aryl or heteroaryl group; and R2, R3, R4 and R5 are as defined in the claims. Also provided are pharmaceutical compositions containing the compounds, methods for preparing the compounds and their use as anticancer agents.

公开(公告)号：EP1706385B1

公开(公告)日：2010-10-06

申请号：EP04806258.2

申请日：2004-12-23

申请人： Astex Therapeutics Limited ,  Cancer Research Technology Limited ,  The Institute of Cancer Research: Royal Cancer Hospital

发明人： BERDINI, Valerio ,  SAXTY, Gordon ,  VERDONK, Marinus, Leendert ,  WOODHEAD, Steven, John ,  WYATT, Paul, Graham ,  BOYLE, Robert, George ,  SORE, Hannah, Fiona ,  WALKER, David, Winter ,  COLLINS, Ian ,  DOWNHAM, Robert ,  CARR, Robin, Arthur, Ellis

IPC分类号： C07D231/12 ,  C07D413/10 ,  C07D401/10 ,  A61K31/415 ,  A61P37/02

CPC分类号： A61K31/415 ,  A61K9/0019 ,  A61K9/20 ,  A61K9/48 ,  A61K31/4155 ,  A61K31/4178 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/497 ,  A61K31/5377 ,  A61K31/551 ,  A61K45/06 ,  C07D231/12 ,  C07D401/04 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D403/10 ,  C07D403/12 ,  C07D405/04 ,  C07D413/10

公开(公告)号：EP1831170A1

公开(公告)日：2007-09-12

申请号：EP05815781.9

申请日：2005-12-12

申请人： AstraZeneca AB ,  Astex Therapeutics Limited

发明人： ALBERT, Jeffrey Scott AstraZeneca Wilmington ,  CALLAGHAN, Owen ,  CAMPBELL, James AstraZeneca Wilmington ,  CARR, Robin, Arthur, Ellis ,  CHESSARI, Gianni Astex Therapeutics ,  COWAN, Suzanna ,  CONGREVE, Miles Stuart Astex Therapeutics ,  EDWARDS, Phil AstraZeneca Wilmington ,  FREDERICKSON, Martyn Astex Therapeutics ,  MURRAY, Christopher William Astex Therapeutics ,  PATEL, Sahil Astex Therapeutics

IPC分类号： C07D213/73 ,  A61K31/44 ,  A61P25/16 ,  A61P25/28

CPC分类号： C07D213/73 ,  C07D213/74 ,  C07D213/81 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D405/10 ,  C07D409/14 ,  C07D413/12

摘要： This invention relates to novel compounds having the structural formula (I) and to their pharmaceutically acceptable salt, compositions and methods of use. These novel compounds provide a treatment or prophylaxis of cognitive impairment, Alzheimer Disease, neurodegeneration and dementia.