Hoffmann-la Roche Inc.

Joseph Hellerbach

Armin Walser

Dieter Binder

Andre Szente

Otto Hromatka

Paul Zeller

Guido Zanetti

Hermann Bretschneider

Henri Hoffmann

Werner Rudolph

Novel thienotriazolodiazepine derivatives and processes for their preparation are described. These compounds are useful as anticonvulsants, muscle-relaxants and sedatives.

Thienotriazolodiazepine derivatives

Benzophenone derivatives are produced which have the formula ##STR1## wherein R.sub.1 signifies hydrogen, nitro, halogen or trifluoromethyl; R.sub.2 represents hydrogen or halogen; R.sub.3, R.sub.4 and R.sub.5 are the same or different and signify hydrogen or lower alkyl; R.sub.6 and R.sub.7 each represent lower alkyl or together with the nitrogen atom form a morpholino, 4-(lower alkyl)-1-piperazinyl, 1-pyrrolidinyl or piperidino group, A signifies an alkylene group with 2 to 8 C atoms and Y represents oxygen or a group ##STR2## R.sub.8 and R.sub.9 each signifying lower alkyl or together signifying lower alkylene. The benzophenone derivatives and their pharmaceutically acceptable salts exhibit sedative, anti-convulsant, muscle relaxant and anxiolytic activities. Also provided are methods for the preparation of these compounds.

Benzophenone derivatives

Novel 1,4-benzodiazepin-2-ones bearing a polyhydroxyalkyl group in the 1-position are disclosed. These 1-substituted benzodiazepins are useful as muscle relaxant, anti-convulsant and sedative agents.

1-Polyhydroxy alkyl-1,4-benzodiazepin-2-ones

1,4-Benzodiazepin-2-ones bearing an acylamidoalkyl-substituent in the 1-position and methods for the preparation thereof are disclosed. These 1,4-benzodiazepin-2-ones exhibit sedative, anti-convulsant and muscle relaxant activity.

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Basel, Switzerland

Joseph Hellerbach