[1,2]-Fused 1,4-benzodiazepine compounds, process for their prep

Details [1,2]-Fused 1,4-benzodiazepine compounds, process for their prep [1,2]-Fused 1,4-benzodiazepine compounds, process for their prep

1982-12-27

1985-04-02

Daus, Donald G.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Heterocyclic carbon compounds containing a hetero ring...

2602433, 2602393D, A61K 31495, C07D48704, C07D49804, C07D51304

Patent

active

045087164

ABSTRACT:
[1,2]-fused 1,4-benzodiazepine compounds are disclosed corresponding to the general formula I ##STR1## wherein X is an oxygen or sulfur atom or an optionally substituted imino group, R.sub.1 is a hydrogen or halogen atom, lower alkyl radical, a lower alkoxy radical or a nitro group and R.sub.2 is a hydrogen or halogen atom, a lower alkyl radical, a lower alkoxy radical or a nitro group, or if R.sub.1 is a hydrogen atom, R.sub.2 may also be a lower alkylthio radical, or, if R.sub.1 is a hydrogen atom and X is a sulfur atom or an imino group, R.sub.2 may be a trifluoromethyl radical; or R.sub.1 and R.sub.2 are bonded to adjacent carbon atoms and together denote a methylenedioxy or ethylenedioxy radical; R.sub.3 is an optionally substituted furyl, thienyl, pyrrolyl or pyridyl radical and n is zero or, if R.sub.3 is furyl or thienyl, n may be 0 or 1. The compounds may be in the form of their optical isomers or acid addition salts. The compounds exhibit neuroleptic properties. Processes for preparing the compounds and pharmaceutical compositions containing them are also disclosed.

REFERENCES:
patent: 3403161 (1968-09-01), Fryer et al.
patent: 3846443 (1974-11-01), Moffett
patent: 4073784 (1978-02-01), Moffett
patent: 4338314 (1982-07-01), Liepmann
Smith et al., J. Med. Chem. 1980, 23, (pp. 952-955), Synthesis and Anxiolytic Activity of a Series of Pyrazino[1,2-a][1,4]Benzodiazepine Derivatives.

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