| 摘要 |
<p>The invention comprises compounds of the general formula <FORM:1019468/C2/1> wherein R1 and R2 independently represent hydrogen, halogen, the trifluoromethyl group, the cyano group, or a C1- 6 alkyl or alkoxy radical, their pharmaceutically acceptable acid addition salts, their quaternary ammonium salts and their N-oxides. The compounds are prepared by reacting a compound of the general formula <FORM:1019468/C2/2> in which R3 represents hydrogen or a C1- 6 alkyl radical and R1 and R2 are as defined above, with a mineral acid, followed, if desired, by conversion to an acid addition salt, a quaternary ammonium compound or an N-oxide. The starting materials of Formula II above can be prepared by reacting a compound of the general formula <FORM:1019468/C2/3> in which Hal represents a halogen atom, in the presence of an acid binding agent with a compound of the general formula <FORM:1019468/C2/4> in which R31 has the meaning given for R3 with the exception of hydrogen, to give a compound of the general formula <FORM:1019468/C2/5> which is then reduced to give a compound of Formula II above in which R3 is C1- 6 alkyl; the product may be saponified to give a compound in which R3 is hydrogen. The invention also comprises medicaments containing at least one of the compounds of the invention together with at least one pharmaceutically acceptable carrier. The compounds of the invention have anti-convulsive and muscle-relaxing activity, have depressant action on the central nervous system, and influence the blood pressure. The compounds may be used as tranquillizers either per os or, in the form of aqueous solutions of their salts, quaternary ammonium compounds or of the N-oxides, also parenterally.</p> |
