Egis Gyogyszergyar

Gyogyszerkutato Intezet Kft.

Egis Gyogyszergyar Rt.

Biogal Gyogyszergyar

Gyogyszerkutato Intezet

Cyogyszerkutato Intezet Kft

Gyogyszerkutato Intezet Kv.

Peter Botka

Tamas Hamori

Jeno Korosi

Imre Moravcsik

Ferenc Andrasi

Pal Berzsenyi

Katalin Goldschmidt

Sandor Farkas

Istvan Tarnawa

Istvan Elekes

Tibor Lang

Gabor Zolyomi

Gyula Horvath

Zsuzsanna Lang Nee Rihmer

Antal Simay

Tibor Balogh

Sandor Elek

Jozsef Borsi

Gyorgy Rabloczky

Istvan Ling

Gyorgy Somogyi

Andras Varro

Erno Orban

Maria Kuhar Nee Kurthy

Eva Tomori Nee Joszt

Katalin G Horvath

Zsuzsanna L Rihmer

Katalin Goldschmidt Nee Horvath

Marta Rusz Nee Patfalusi

Csilla Kiss

Maria Bidlo Nee Igloi

Nee Dievald Uskert

Roozsa Gyenge

Judit Sarossy Nee Kincsessy

The invention relates to novel N-acyl-2,3-benzodiezapine derivatives of the general formula (I), their stereoisomers and acid-addition salts, pharmaceutical compositions containing them and a process for their preparation. In the general formula (I)

N-acyl-2,3-benzodiazepine derivatives for treating acute and chronic

N-acyl-2,3-benzodiazepine derivatives pharmaceutical compositions

The invention relates to novel N-acyl-2,3-benzodiezapine derivatives and a method of treating spasms of the skeletal musculature therewith.

N-acyl-2,3-benzodiazepine derivatives and a method of treating spasms of

N-acyl-2,3-benzoidazepine derivatives, pharmaceutical compositions

The invention relates to novel N-acyl-2,3-benzodiezapine derivatives of the general formula (I), their stereoisomers and acid-addition salts, pharmaceutical compositions containing them and a process for their preparation. In the general formula (I), defined in the specification, a more complete description of the compounds may be found. The compounds of the general formula (I) possess valuable central nervous system effects, particularly muscle-relaxant, anticonvulsive and neuroprotective action. Thus, they may be useful for the treatment of various diseases of central nervous system origin.

N-acyl-2,3-benzodiazepine derivatives, pharmaceutical compositions

The invention relates to a process for the preparation of 1-(3-chlorophenyl)-4-methyl-7,8-dimethoxy-5 H-2,3-benzodiazepine of formula (I) ##STR1## in high purity and in a quality suitable for pharmaceutical purposes. According to the invention the reaction of 1 mole of 2-acetonyl-3'-chloro-4,5-dimethoxybenzophenone of formula (II) ##STR2## with 3-7 moles of hydrazine hydrate in an organic solvent or in a mixture of organic solvents at a temperature between 15.degree. C. and 85.degree. C. is carried out in the absence of air oxygen, optionally in the presence of water. The crude product is then recrystallized from an aliphatic alcohol containing 1 to 5 carbon atom(s).

Process for the preparation of high-purity

The invention relates to the new 1-(3-chlorophenyl)-4-hydroxymethyl-7,8-dimethoxy-5H-2,3-benzodiazepine of formula (I) ##STR1## and pharmaceutically acceptable acid addition salts thereof, furthermore to a process for preparing these compounds. The compounds according to the invention possess valuable anxiolytic, antiaggressive and antidepressant effects and have at the same time favorable acute toxicity values, so they can be used to advantage in therapy.

5H-benzodiazepin derivative

The invention relates to new 1-(4-aminophenyl)-4-methyl-7,8-methylenedioxy-3,4-dihydro-5H-2,3-benzodiaz epi ne of formula (1), optically active isomers and acid addition salts thereof as well as to pharmaceutical compositions containing these compounds. ##STR1## The new compounds of formula (I) can be prepared by reducing 1-(4-aminophenyl)-4-methyl-7,8-methylenedioxy-5H-2,3-benzodiazepine of formula (II) with an inorganic or organic-inorganic and/or complex metal hydride and, if desired, separating the optically active forms of the compound of formula (I) thus-obtained and, if desired, converting the base or bases into acid addition salts or converting the salts into the free bases(s). ##STR2## The new compound of formula (I) possesses significant central nervous effects and can advantageously be used in the therapy.

1-(4-Aminophenyl)-4-methyl-7,8-methylenedioxy-3,4-dihydro-5H-2,3-b

This invention relates to new 3-(hydroxymethyl)-isoquinoline derivatives of the general formula (I), their acid addition salts, and to a process for the preparation thereof, furthermore to pharmaceutical compositions containing the same, ##STR1## wherein R and R.sup.1 are identical or different and stand for a hydrogen or halogen atom, a nitro or a C.sub.1-4 alkoxy group,

3-(hydroxymethyl)-isoquinoline derivatives

The invention relates to new 5H-2,3-benzodiazepine derivatives and a process for the preparation thereof, furthermore to pharmaceutical compositions containing the same. The new 5H-2,3-benzodiazepine derivatives of the invention possess valuable central nervous effect and in particular exert antiaggressive, anxiolytic, narcosis potentiating and soporific properties.

5H-2,3-benzodiazepine derivatives and pharmaceutical compositions

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Budapest, Hungary

Peter Botka