公开(公告)号：EP1153017B1

公开(公告)日：2006-05-03

申请号：EP00903864.7

申请日：2000-02-16

申请人： Aventis Pharma Limited

发明人： CLARK, David, Edward ,  EASTWOOD, Paul, Robert ,  HARRIS, Neil, Victor ,  MCCARTHY, Clive ,  MORLEY, Andrew, David ,  PICKETT, Stephen, Dennis

IPC分类号： C07D263/58 ,  C07D235/30 ,  C07D413/12 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  A61K31/423 ,  A61K31/4184 ,  A61P29/00 ,  A61P11/06

CPC分类号： C07D263/58 ,  C07D235/30

摘要： The invention is directed to physiologically active compounds of general formula (I): wherein Het is an optionally substituted, saturated, partially saturated or fully unsaturated 8 to 10 membered bicyclic ring; R1 is optionally substituted aryl or optionally substituted heteroaryl; R2 is hydrogen, halogen, lower alkyl or lower alkoxy; L1 is an -R3-R4- linkage where R3 is alkylene, alkenylene or alkynylene and R4 is a direct bond, cycloalkylene, heterocycloalkylene, arylene, heteroaryldiyl, -C(=Z?2)-NR5-, -NR5-C(=Z2)-, -Z2¿-, -C(=O)-, -C(=NOR?5)-, -NR5-, -NR5-C(=Z2)-NR5¿-, -SO¿2?-NR?5-, -NR5-SO¿2-, -O-C(=O)-, -C(=O)-O-, -NR5-C(=O)-O- or -O-C(=O)-NR5-; L2 is optionally substituted alkylene or alkenylene; Y is carboxy or an acid bioisostere; and Z?1 is NR5¿; and the corresponding N-oxides, and their prodrugs; and pharmaceutically acceptable salts and solvates (e.g. hydrates) of such compounds and their N-oxides and prodrugs. Such compounds have valuable pharmaceutical properties, in particular the ability to regulate the interaction of VCAM-1 and fibronectin with the integrin VLA-4 (α4β1).

公开(公告)号：EP1153017A1

公开(公告)日：2001-11-14

申请号：EP00903864.7

申请日：2000-02-16

申请人： Aventis Pharma Limited

发明人： CLARK, David, Edward ,  EASTWOOD, Paul, Robert ,  HARRIS, Neil, Victor ,  MCCARTHY, Clive ,  MORLEY, Andrew, David ,  PICKETT, Stephen, Dennis

IPC分类号： C07D263/58 ,  C07D235/30 ,  C07D413/12 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  A61K31/423 ,  A61K31/4184 ,  A61P29/00 ,  A61P11/06

CPC分类号： C07D263/58 ,  C07D235/30

摘要： The invention is directed to physiologically active compounds of general formula (I): wherein Het is an optionally substituted, saturated, partially saturated or fully unsaturated 8 to 10 membered bicyclic ring; R1 is optionally substituted aryl or optionally substituted heteroaryl; R2 is hydrogen, halogen, lower alkyl or lower alkoxy; L1 is an -R3-R4- linkage where R3 is alkylene, alkenylene or alkynylene and R4 is a direct bond, cycloalkylene, heterocycloalkylene, arylene, heteroaryldiyl, -C(=Z?2)-NR5-, -NR5-C(=Z2)-, -Z2¿-, -C(=O)-, -C(=NOR?5)-, -NR5-, -NR5-C(=Z2)-NR5¿-, -SO¿2?-NR?5-, -NR5-SO¿2-, -O-C(=O)-, -C(=O)-O-, -NR5-C(=O)-O- or -O-C(=O)-NR5-; L2 is optionally substituted alkylene or alkenylene; Y is carboxy or an acid bioisostere; and Z?1 is NR5¿; and the corresponding N-oxides, and their prodrugs; and pharmaceutically acceptable salts and solvates (e.g. hydrates) of such compounds and their N-oxides and prodrugs. Such compounds have valuable pharmaceutical properties, in particular the ability to regulate the interaction of VCAM-1 and fibronectin with the integrin VLA-4 (α4β1).