5-O-Cyanobenzyl-4,5,6,7-tetrahydro-thieno\x9b3,2-c!pyridine maleate \n'
申请人:Centre d'Etudes Pour L'Industrie Pharmaceutique
公开号:US04097482A1
公开(公告)日:1978-06-27
The present invention relates to pyridine derivatives having the formula: ##STR1## in which: R is a radical selected from a phenyl radical mono- and polysubstituted with a group selected from the aryl, carboxy, alkoxycarbonyl, cyano, hydroxymethyl and ethylenedioxy groups; a styryl, thienyl and benzhydryl radical optionally mono- and polysubstituted with a group selected from halogen, lower alkyl, lower alkoxy, aryl, nitro, amino, sulfonylamino, carboxy, alkoxycarbonyl, cyano, hydroxymethyl and methylenedioxy; R.sub.1 and R.sub.2 represent each a group selected from hydrogen, halogen, hydroxy, lower alkyl, lower alkoxy, nitro and amino; R.sub.3 represents a group selected from hydrogen, halogen, hydroxy, lower alkyl, lower alkoxy, nitro and amino; and n is an integer from 1 to 15, And in which the symbols R.sub.3 may have different meanings in each radical CHR.sub.3 when n is greater than 1, And their inorganic and organic acid addition salts and quaternary ammonium derivatives, particularly 5-o-cyanobenzyl-4,5,6,7-tetrahydro-thieno\x9b3,2-c!pyridine maleate. \n' Said derivatives are therapeutically valuable in view of their anti-inflammatory and vasodilator activities and their inhibitor action on blood-platelet aggregation.
本发明涉及具有以下式的吡啶衍生物:##STR1## 其中:R是从苯基基团单选和多选而成的基团,所述基团被选择自芳基,羧基,烷氧羰基,氰基,羟甲基和乙二醚基的群;苯乙烯基,噻吩基和苯甲基基团,可选地单选和多选自卤素,低烷基,低烷氧基,芳基,硝基,氨基,磺酰氨基,羧基,烷氧羰基,氰基,羟甲基和亚甲二氧基的群;R.sub.1和R.sub.2分别表示从氢,卤素,羟基,低烷基,低烷氧基,硝基和氨基中选择的群;R.sub.3表示从氢,卤素,羟基,低烷基,低烷氧基,硝基和氨基中选择的群;n是1到15之间的整数,其中当n大于1时,符号R.sub.3在每个基团CHR.sub.3中可能具有不同的含义,并且它们的无机和有机酸加盐和季铵衍生物,特别是5-对氰基苄基-4,5,6,7-四氢噻吩\x9b3,2-c!吡啶马来酸盐。这些衍生物在抗炎和扩血管活性以及它们对血小板聚集的抑制作用方面具有治疗价值。