Benzodiazepine derivatives and pharmaceutical compositions conta

Drug – bio-affecting and body treating compositions – Antigen – epitope – or other immunospecific immunoeffector – Fungus – except allergen – or component thereof or substance...

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26032647, 2603265SF, 2603265J, 2603265FM, 2603473, 260556AR, 260557R, 260558R, 260561R, 2603265B, 2603269, 544372, 548253, 548217, 548236, 548180, 548200, 548262, 2602457, 260326R, 260326A, 260326C, 260326N, 26032614R, 26032635, 26032636, 26032637, A61K 3155, C07D48704

Patent

active

041691504

ABSTRACT:
Novel 4H-pyrrolo[1,2-a][1,4]benzodiazepine derivatives of the formula ##STR1## wherein at least one of R.sub.1, R.sub.2 and R.sub.3 represent lower alkyl and the remainder hydrogen, R.sub.4 represents hydrogen or lower alkyl, ring A optionally contains at least one substituent selected from halogen, nitro and trifluoromethyl, and ring B optionally contains at least one substituent selected from halogen, nitro, trifluoromethyl, lower alkyl and lower alkoxy; and novel intermediates thereof expressed by the formula ##STR2## wherein Z represents protected amino. Compounds of formula (I) are prepared by subjecting compounds of formula (II) to protective group-elimination and cyclization. The compounds of formula (I) and acid addition salts thereof have useful anti-anxietic, sedative, anti-convulsant, muscle relaxant and hypnotic, and their toxicity is low.

REFERENCES:
patent: 3642820 (1972-02-01), Hester
patent: 3917627 (1975-11-01), Hester et al.
patent: 3987052 (1976-10-01), Hester
Garcia et al., J. Org. Chem., vol. 33, pp. 1359-1363, (1968).

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