Pyrrolo-diazepine derivatives and their pharmaceutical compositions
AssigneeGruppo Lepetit S.p.A.
InventorsLuigi Mariani, Giorgio Tarzia
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Abstract
A new class of pyrrolo-diazepines with anticonvulsant and anti-anxiety activity of the general formula ##STR1## wherein R is (C.sub.1 -C.sub.4)alkyl, R.sub.1 is chloro, bromo or nitro, R.sub.2 is hydrogen or (C.sub.1 -C.sub.4)alkyl and R.sub.3 is hydrogen, chloro, bromo, fluoro, trifluoromethyl or methoxy. The new compounds are prepared starting from the corresponding compounds wherein R.sub.1 is hydrogen through halogenation or nitration. Pharmaceutical preparations containing the new compounds of formula I are also described.
Claims6
A pyrrolo[ 3,4-e][1,4]diazepin-2(1H)-one of the formula ##STR4## wherein R represents methyl, ethyl, propyl, 1-methylethyl, butyl, 1-methylpropyl, 2-methylpropyl, or 1,1-dimethylethyl, R.sub.1 designates a chlorine or bromine atom or a nitro group, R.sub.2 represents hydrogen, methyl, ethyl, propyl, 1-methylethyl, butyl, 1-methylpropyl, 2-methylpropyl, or 1,1-dimethylethyl, and R.sub.3 is hydrogen, chloro, bromo, fluoro, trifluoromethyl or methoxy.
A process for preparing a compound of formula ##STR5## wherein R represents methyl, ethyl, propyl, 1-methylethyl, butyl, 1-methylpropyl, 2-methylpropyl, or 1,1-dimethylethyl, R.sub.1 designates a chlorine or bromine atom or a nitro group, R.sub.2 represents hydrogen, methyl, ethyl, propyl, 1-methylethyl, butyl, 1-methylpropyl, 2-methylpropyl, or 1,1-dimethylethyl, and R.sub.3 is hydrogen, chloro, bromo, fluoro, trifluoromethyl or methoxy, which comprises nitrating or halogenating a compound of formula II ##STR6## wherein R, R.sub.2 and R.sub.3 are as defined above.
Dependencies are inferred from the claim text.