| 摘要 |
The invention comprises carbostyril compounds of the general formula <FORM:1002665/C2/1> wherein Y is -CH=CH- or -CH2-CH2-; X is oxygen or sulphur and R2 is lower alkyl, or, when Y is -CH2-CH2-, hydrogen. Compounds of the above general formula, may be prepared by the reaction schemes outlined below <FORM:1002665/C2/2> R represents trifluoromethyl, R1 is hydrogen, and X is an anion. The term "lower" refers to groups having 1 to 4 carbon atoms. The N-oxide of 6-trifluoromethylquinoline is prepared by action of hydrogen peroxide on quinoline and then treated with acetic anhydride before hydrogenation to give 3,4-dihydro-6-trifluoromethylcarbostyril.ALSO:Pharmaceutical compositions having muscle relaxant and analgesic activity comprise a pharmaceutical carrier in association with a carbostyril compound <FORM:1002665/A5-A6/1> wherein Y is -CH = CH- or -CH2-CH2-; X is O or S; R is hydrogen, halogen, hydroxy, nitro, amino, mono-lower alkyl amino, di-lower alkyl amino, acetamido, trifluoromethyl, lower alkyl, lower alkoxy or ethoxycarbonyl; R1 is hydrogen or, together with R, dihalogen, dihydroxy, diloweralkoxy or methylene-dioxy; and R2 is lower alkyl or, when R is -CH2-CH2-, hydrogen. "Lower" refers to groups having 1 to 4 carbon atoms and "halogen" denotes chlorine, bromine or fluorine. Conventional solid or liquid carriers may be used, together with a sustained release material. The compositions may be used in the forms of a tablet, capsule, troche or lozenge, and their administration may be effected parenterally or orally. |
