Benzodiazepine derivatives

Details Benzodiazepine derivatives Benzodiazepine derivatives

C - Chemistry, Metallurgy

07

D

260/239.1

C07D 487/04 (2006.01) A61H 23/02 (2006.01) A61K 31/55 (2006.01) C07D 498/04 (2006.01)

Patent

CA 1041498

ABSTRACT Tricyclic benzodiazepines of formula: Image I wherein A represents the group -CH2- or -?-; Z is -O- or -?-, where R6 is hydrogen, lower alkyl or acyl; R1 is hydrogen, halogen, or trifluoromethyl, R2 is hydrogen or lower alkyl; R3 is hydrogen; Y is a di- or trimethylene group which may be substituted by R4, R4 being lower alkyl or -CH2X where X is chlorine, bromine, lower alkoxy-lower alkyl or di-lower alkylamino; and R5 is phenyl or phenyl substituted with halogen or trifluoromethyl are prepared by cyclization of the corresponding open compounds. Compounds of formula I wherein Z is -O- and Y is a dimethylene group which may be substituted by R4 may also be prepared by treating the corresponding 4,5-unsaturated benzodiaze- pines with an epoxide compound in the presence of an acid catalyst. The com- pounds of formula I are useful as sedative, muscle relaxant and anti-convulsant agents.

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