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|Title:||Intermediates to produce imidazodiazepines|
|Abstract:||Novel imidazobenzodiazepines 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. As especially preferred genus included within 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 and 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|
|Claims:||1. A compound of the formula ##STR82## wherein R is lower alkyl; A is ##STR83## R.sup.3 is selected from the group consisting of hydrogen and lower alkyl; R.sup.6 is selected from the group consisting of phenyl, mono-halo or mono-nitro substituted phenyl, di-halo or halo and nitro substituted phenyl, pyridyl and mono-halo or mono-nitro substituted pyridyl; R.sup.4 is selected from the group consisting of hydrogen, halogen, nitro, cyano, trifluoromethyl, lower alkyl, mono-or di-lower alkyl substituted amino, amino, hydroxy lower alkyl and lower alkanoyl; R.sub.1 is selected from the group consisting of hydrogen, lower alkyl, phenyl, alkoxy lower alkyl, mono-halo or mono-nitro substituted phenyl, pyridyl, aralkyl; and ##STR84## is selected from the group consisting of ##STR85## .|
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