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    • 4. 发明授权
    • 2-Amino-5-phenyl-1,3-benzodiazepines
    • 2-氨基-5-苯基-1,3-苯并二氮杂卓
    • US4554273A
    • 1985-11-19
    • US578046
    • 1984-02-07
    • Michel BayssatGerard FerrandJean-Claude Depin
    • Michel BayssatGerard FerrandJean-Claude Depin
    • A61K31/55A61P25/24A61P25/26C07D243/04C07D401/12C07D403/12C07D405/12C07D403/04
    • C07D401/12C07D243/04C07D403/12C07D405/12
    • Disclosed are 2-amino-5-phenyl-1,3-benzodiazepines of the formula ##STR1## wherein R.sub.1 and R.sub.2 are hydrogen, halogen, alkyl, or alkoxy; R.sub.2 being able to occupy any of the possible positions on the aromatic ring; R.sub.3 is hydrogen or alkyl; and R.sub.4 is hydrogen, alkyl, cycloalkyl, arylalkyl, heteroarylalkyl, dialkylaminoethyl, dialkylaminopropyl, (1-ethyl-2-pyrrolidino) methyl, dialkylamino, alkoxycarbonyl or cyano; or R.sub.3 and R.sub.4 form, with the adjacent nitrogen atom, a heterocycle having 5 to 7 side chains, optionally containing another heteroatom selected from oxygen, sulfur or nitrogen, this latter being able to be substituted by an alkyl group. The majority of the compounds are obtained by condensation of the corresponding 2-methylthio benzodiazepine hydroiodide with an appropriate amine. The compounds are useful as antidepressants.
    • 公开了下式的2-氨基-5-苯基-1,3-苯并二氮杂其中R 1和R 2是氢,卤素,烷基或烷氧基; R2能够占据芳香环上任何可能的位置; R3是氢或烷基; 并且R 4是氢,烷基,环烷基,芳基烷基,杂芳基烷基,二烷基氨基乙基,二烷基氨基丙基,(1-乙基-2-吡咯烷子基)甲基,二烷基氨基,烷氧基羰基或氰基; 或R3和R4与相邻的氮原子形成具有5至7个侧链的杂环,任选地含有选自氧,硫或氮的另外的杂原子,后者可被烷基取代。 大部分化合物通过相应的2-甲硫基苯并二氮杂环丁烷与合适的胺的缩合得到。 这些化合物可用作抗抑郁药。