申请人:Machinaga Nobuo
公开号:US20090233901A1
公开(公告)日:2009-09-17
There is provided a VLA-4 inhibitory drug having good oral absorbability and exhibiting sufficient anti-inflammatory effects when administered orally.
A compound represented by the following formula (I):
wherein R
1
represents a hydrogen atom or a C1-8 alkyl group; R
2
represents a hydrogen atom, a halogen atom, a C1-8 alkoxy group, or a benzyloxy group which may be substituted; Q represents a monocyclic or bicyclic nitrogen-containing heterocyclic group which may be substituted, and has a nitrogen atom as the bonding site; Y represents an oxygen atom or CH
2
; W represents a bicyclic aromatic hydrocarbon ring group which may be substituted, or a bicyclic aromatic heterocyclic group which may be substituted; R
3a
, R
3b
and R
3c
each independently represent a hydrogen atom, a halogen atom, a C1-8 alkoxy group or a C1-8 alkyl group; and A
1
represents a nitrogen atom or C—R
3d
(wherein R
3d
represents a hydrogen atom, a halogen atom, a C1-8 alkoxy group or a C1-8 alkyl group),
or a salt thereof, or a VLA-4 inhibitory drug comprising the compound or the salt as an active ingredient.
提供了一种VLA-4抑制剂药物,具有良好的口服吸收性,并在口服给药时表现出足够的抗炎效果。其中,化合物的表示式如下(I):其中,R1表示氢原子或C1-8烷基;R2表示氢原子、卤素原子、C1-8烷氧基或可取代的苄氧基;Q表示可取代的单环或双环含氮杂环基团,并具有氮原子作为键合位点;Y表示氧原子或CH2;W表示可取代的双环芳香烃环基团或可取代的双环芳香杂环基团;R3a、R3b和R3c分别独立地表示氢原子、卤素原子、C1-8烷氧基或C1-8烷基;A1表示氮原子或C-R3d(其中,R3d表示氢原子、卤素原子、C1-8烷氧基或C1-8烷基),或其盐,或包含该化合物或其盐作为活性成分的VLA-4抑制剂药物。