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    • 10. 发明专利
    • DE1470110A1
    • 1969-11-20
    • DE1470110
    • 1964-12-05
    • MEAD JOHNSON & CO
    • WEBER ABRAHAME KREIGHBAUM WILLIAM
    • C07D285/36
    • The invention comprises dibenzo[1,2,5]thiadiazepine-5,5-dioxides of the general formula wherein R3 represents H or one or two substituents selected from halogen, Me, CF3 or C1- 4 alkoxy, alkylthio or alkylsulphonyl, R6 represents H, halogen, Me, CF3, -NMe2 or -SO2NME2, or alkoxycarbonyl, alkoxy, alkylthio, alkylsulphonyl or alkanoyl of up to 4C, Alk represents ethylene or trimethylene optionally having one Me or Et substituent, -NR1R2 represents amino, pyrrolidino, piperidino, morpholino, thiamorpholino, piperazino or 4-R4-piperazino (where R4 is C1- 4 alkyl or hydroxyalkyl, C2- 5 alkoxycarbonyl, or alkanoyloxyalkyl of up to 7C), R1 represents H or a group as defined for R4, and R2 represents C1- 4 alkyl or hydroxyalkyl, or an oxaalkylene, azaalkylene or thiaalkylene group the second valence of which is attached to Alk to form a heterocyclic ring, and their acid addition salts. Those compounds in which R1 is other than H are prepared by reacting the corresponding 11-unsubstituted compound with a compound of the general formula X-Alk-NR1R2 (where X is Cl, Br, I, p - C1H4SO3-, CH3SO3-, HSO4-, -OCO2- or C2H5OCO2-) in the presence of a strong base. Those compounds in which R1 is H are prepared by the foregoing process using a compound X-Alk-NR1R2 wherein R1 is a C2- 5 alkoxycarbonyl group which is subsequently removed by acid or alkaline hydrolysis, or (when R2 is C1- 4 alkyl) by reacting a compound in which R1 is Me with an alkyl chloroformate to form a compound in which R1 is a C2- 5 alkoxycarbonyl group, this being then removed as before. N - (3 - Chloropropyl) - N - methylcarbamic acid ethyl ester is prepared by reacting 3-dimethylaminopropyl - (1) chloride with ethyl chloroformate. Pharmaceutical compositions in dosage unit forms comprise the compounds of the invention and a pharmaceutical carrier. They act as psychotrophic agents and muscle relaxants.