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公开(公告)号:US20120157437A1
公开(公告)日:2012-06-21
申请号:US13363990
申请日:2012-02-01
申请人: Nobuo MACHINAGA , Shin Ilmura , Yoshiyuki Yoneda , Jun Chiba , Fumihito Muro , Hideko Hoh , Atsushi Nakayama
发明人: Nobuo MACHINAGA , Shin Ilmura , Yoshiyuki Yoneda , Jun Chiba , Fumihito Muro , Hideko Hoh , Atsushi Nakayama
IPC分类号: A61K31/404 , C07D401/14 , C07D413/14 , A61K31/5377 , C07D417/14 , A61K31/541 , A61K31/553 , A61P29/00 , A61P37/00 , A61P35/04 , A61P11/06 , A61P11/02 , A61P3/10 , A61P19/02 , A61P17/06 , A61P25/00 , A61P1/00 , A61P37/06 , A61P35/02 , A61P37/08 , A61P9/10 , A61P27/02 , A61P1/16 , A61P35/00 , C07D403/14
CPC分类号: C07D409/12 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/12 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D487/08 , C07D491/048 , C07D491/056 , C07D491/08 , C07D495/04
摘要: This invention relates to a VLA-4 inhibitory drug, having good oral absorbability and exhibiting sufficient anti-inflammatory effects when administered orally, wherein an active ingredient is represented by formula (I), or a salt thereof: Q represents an optionally-substituted monocyclic or bicyclic nitrogen-containing heterocyclic group having a nitrogen atom as the bonding site; Y represents an oxygen atom or CH2; W represents an optionally-substituted bicyclic aromatic hydrocarbon ring group or an optionally-substituted bicyclic aromatic heterocyclic group; A1 represents a nitrogen atom or C—R3d wherein R3d represents a hydrogen atom, a halogen atom, a C1-8 alkoxy group or a C1-8 alkyl group; R1 represents H or a C1-8 alkyl group; R2 represents H, a halogen, a C1-8 alkoxy group, or an optionally-substituted benzyloxy group; and R3a, R3b and R3c independently represent H, a halogen atom, a C1-8 alkoxy group or a C1-8 alkyl group.
摘要翻译: 本发明涉及具有良好口服吸收性且口服给药时具有足够抗炎作用的VLA-4抑制药物,其中活性成分由式(I)表示,或其盐:Q表示任选取代的单环 或具有氮原子的双环含氮杂环基作为键合位置; Y表示氧原子或CH2; W表示任选取代的双环芳烃环基或任选取代的双环芳族杂环基; 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; R1表示H或C1-8烷基; R 2表示H,卤素,C 1-8烷氧基或任选取代的苄氧基; R3a,R3b和R3c独立地表示H,卤素原子,C1-8烷氧基或C1-8烷基。