100449

100449



4,125,726


1

IMIDAZOI 1,5-all MJBENZODIAZEPINES

DESCRJPTION OF THE INVENTION

The prescnt invention rclates to cotnpounds of the 5 formula

2

wherein Rj is hydrogen, halogen or trifluoromethyl; R2 is sclected from the group consisting of lower alkylthio together with the sulfoxide and sulfone thercof, halo, lower alkylamino or lower alkoxy; Y U 0x0 or thio; R3 is sclected from the group consist-ing of hydrogen, —COOR4 wherein R4 is hydrogen or lower alkyl; — CONR4R5 wherein R5 and R6 are hydrogen or lower alkyl; X is hydrogen or halogen; and R? is lower alkyl or hydrogen and the pharmaceutically acccptable salts and N-oxides thereof.

As used in this disclosure, the term “lower alkyl" or "alkyl” comprchends both straight and branched chain (Cj to C7) carbon-hydrogen radicals, preferably Cj to C4 carbon-hydrogen radicals such as methyl, ethyl, propyl, isopropyl, butyl and the like.

The term “halogen” is used to include all four forms thereof, i.c., chłonne, bromine, fluorinc and iodine,

The cotnpounds of the present invcntion exhibit phar-macological activity as sedatives, muscle relasants, anx-iolytics and anticonvulsants.

The following reaction scheme sets forth the pro-cesses utilized to produce the novel corapounds of the present invention.




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