发明公开
- 专利标题： Pyridine compounds, process for the preparation thereof and pharmaceutical composition containing the same
- 专利标题（中）： 吡啶化合物，它们的制备方法和含有它们的药物组合物。
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申请号： EP86305421.9申请日： 1986-07-15
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公开(公告)号： EP0210782A2公开(公告)日： 1987-02-04
- 发明人: Uno, Hitoshi , Nishikawa, Yoshinori , Shindo, Tokuhiko , Nakamura, Hideo , Ishii, Katsumi
- 申请人： Dainippon Pharmaceutical Co., Ltd.
- 申请人地址： 25, Doshomachi 3-chome Higashi-ku Osaka-shi, Osaka 541 JP
- 专利权人： Dainippon Pharmaceutical Co., Ltd.
- 当前专利权人： Dainippon Pharmaceutical Co., Ltd.
- 当前专利权人地址： 25, Doshomachi 3-chome Higashi-ku Osaka-shi, Osaka 541 JP
- 代理机构： Paget, Hugh Charles Edward
- 优先权： JP160783/85 19850719
- 主分类号： C07D213/56
- IPC分类号： C07D213/56 ; C07D213/61 ; C07D401/12 ; C07D213/65 ; C07D213/72 ; C07D213/89 ; C07D213/80 ; C07D213/64 ; C07D213/70 ; C07D213/57 ; A61K31/44
摘要：
Compounds of the formula:
wherein X is alkylene or-(CR 6 -CR 7 ) r - wherein R 6 is H, alkyl or phenyl, R 7 is H, alkyl, cyano or phenyl, and r is 1 or 2; A is alkylene or alkylene interrupted by at least one double bond;
R 1 is H, halogen, alkyl, alkoxy, alkylthio, cycloalkyloxy, cycloa-Ikylthio, alkoxycarbonyl, carboxy, phenyl, phenoxy, phenylthio, 3-pyridyloxy or 3-pyridylthio; R 2 is H, hydroxy, alkanoyloxy or alkoxycarbonyloxy, or adjacent R, and R 2 may combine to form tetramethylene or-CH 2 OCR 8 R 9 O-(R 8 and Rg are alkyl); R 3 is H, alkyl or hydroxyalkyl; R 4 is H or alkyl; R 5 is phenyl, heteroaryl or-(CH 2 ) m -CHR 10 R 11 (R 10 is H or phenyl, R 11
is phenyl or pyridyl and m is 0 to 2); p is 0 or 1; and q is 2 or 3; the phenyl group or moiety being optionally substituted, and salts thereof show excellent antiallergic activity mainly through 5-lipoxygenase inhibiting activity, antihistamine activity and/or inhibitory activity against chemical mediator release and are useful for treatment of allergic diseases. Processes for their preparation and pharmaceutical compositions containing them are also described.
wherein X is alkylene or-(CR 6 -CR 7 ) r - wherein R 6 is H, alkyl or phenyl, R 7 is H, alkyl, cyano or phenyl, and r is 1 or 2; A is alkylene or alkylene interrupted by at least one double bond;
R 1 is H, halogen, alkyl, alkoxy, alkylthio, cycloalkyloxy, cycloa-Ikylthio, alkoxycarbonyl, carboxy, phenyl, phenoxy, phenylthio, 3-pyridyloxy or 3-pyridylthio; R 2 is H, hydroxy, alkanoyloxy or alkoxycarbonyloxy, or adjacent R, and R 2 may combine to form tetramethylene or-CH 2 OCR 8 R 9 O-(R 8 and Rg are alkyl); R 3 is H, alkyl or hydroxyalkyl; R 4 is H or alkyl; R 5 is phenyl, heteroaryl or-(CH 2 ) m -CHR 10 R 11 (R 10 is H or phenyl, R 11
is phenyl or pyridyl and m is 0 to 2); p is 0 or 1; and q is 2 or 3; the phenyl group or moiety being optionally substituted, and salts thereof show excellent antiallergic activity mainly through 5-lipoxygenase inhibiting activity, antihistamine activity and/or inhibitory activity against chemical mediator release and are useful for treatment of allergic diseases. Processes for their preparation and pharmaceutical compositions containing them are also described.
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