Benzamide derivatives, process for their preparation and pharmaceutical compositions containing them
申请人:BEECHAM GROUP PLC
公开号:EP0041817A1
公开(公告)日:1981-12-16
Compounds of formula (1) and pharmaceutically acceptable salts thereof:
wherein: X is oxygen or sulphur;
R1 is alkoxy or alkylthio
R2 and R3 are hydrogen, halogen, CF3, acyl, acylamino or amino, aminocarbonyl or aminosulphonyl optionally substituted by one or two alkyl groups, alkylsulphonyl, alkylsulphinyl, alkoxy, alkylthio, hydroxy or nitro or R1 and R2 taken together are methylenedioxy or ethylenedioxy in which case R3 is any one of the groups given for R2 and R3 above;
R4 is alkyl or a group -(CH2)sR5 in which s is 0 to 2 and Rs is a cycloalkyl group, or a group -(CH2)sR6 in which t is 1 or 2 and R6 is a phenyl group optionally substituted by one or two substituents selected from alkyl, alkoxy, trifluoromethyl and halogen, or a thienyl group;
n is 0 to 2; there at least being two carbon atoms between the benzamide and heterogranatane ring nitrogen atoms;
The compounds having a useful pharmacological activity; pharmaceutical compositions containing them; process for their preparation.
式(1)化合物及其药学上可接受的盐类:
其中X 是氧或硫;
R1 是烷氧基或烷硫基
R2 和 R3 是氢、卤素、CF3、酰基、酰氨基或可选择被一个或两个烷基、烷基磺酰基、 烷基亚磺酰基、烷氧基、烷硫基、羟基或硝基取代的氨基、氨基羰基或氨基磺酰基;
R4 是烷基或基团-(CH2)sR5(其中 s 为 0 至 2,Rs 为环烷基),或基团-(CH2)sR6(其中 t 为 1 或 2,R6 为苯基,任选被一个或两个选自烷基、烷氧基、三氟甲基和卤素的取代基取代)或噻吩基;
n 为 0 至 2;苯甲酰胺和杂环氮原子之间至少有两个碳原子;
具有有用药理活性的化合物;含有这些化合物的药物组合物;其制备工艺。