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Generated: December 15, 2017

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Title: Imidazodiazepines and processes therefor
Abstract:Novel immidazobenzodiazepines and their analogs are useful as anticonvulsants, muscle relaxant, anxiolytic and sedative agents. Preferred compounds of this class belong to the imidazo[1,5-a][1,4]diazepine series which may have a very wide variety of organic substituents. An especially preferred genus included with the purview of the invention encompasses a compound of the formula ##STR1## wherein R.sub.1 is hydrogen and lower alkyl, preferably methyl; R.sub.3 and R.sub.5 are hydrogen; R.sub.4 is hydrogen, nitro or halogen, most preferably, chlorine, and in a most preferred embodiment when positioned on the fused benzo portion of the imidazobenzodiazepine is in the 8-position thereof; R.sub.6 is phenyl or halo, nitro, or lower alkyl-substituted phenyl, preferably, halo, with fluorine being the preferred halogen, the substituted fluoro being positioned in the 2-position of the phenyl moiety; and R.sub.2 is hydrogen and lower alkyl.
Inventor(s): Walser; Armin (West Caldwell, NJ), Fryer; Rodney I. (North Caldwell, NJ)
Assignee: Hoffmann-La Roche Inc. (Nutley, NJ)
Filing Date:Mar 12, 1981
Application Number:06/242,852
Claims:1. A compound of the formula ##STR85## wherein R is lower alkyl; A is ##STR86## R.sub.3 is selected from the group consisting of hydrogen and lower alkyl; R.sub.6 is selected from the group consisting of phenyl, mono-halo or mono-nitro substituted phenyl, dihalo or halo/nitro substituted phenyl, pyridyl and mono-halo or mono-nitro substituted pyridyl; R.sub.4 is selected from the group consisting of hydrogen, halogen, nitro, cyano, trifluoromethyl, lower alkyl, mono- or di-C.sub.1 to C.sub.7 alkyl or phenyl or chlorophenyl or tolyl substituted amino, amino, hydroxy lower alkyl and lower alkanoyl; R.sub.1 is selected from the group consisting of hydrogen, lower alkyl, hydroxy lower alkyl, C.sub.1 to C.sub.7 acyloxy lower alkyl, phenyl, C.sub.1 to C.sub.7 alkoxy lower alkyl, halo lower alkyl, amino lower alkyl, mono- or di-C.sub.1 to C.sub.7 alkyl or phenyl or chlorophenyl or tolyl substituted amino lower alkyl, pyridyl, benzyl and the groups ##STR87## wherein R is hydrogen or lower alkyl and COOR wherein R is lower alkyl; and ##STR88## is selected from the group consisting of ##STR89##
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