Kali-chemie Pharma Gmbh

Stephen J Magda

Gerd Buschmann

Heinrich-Wilhelm Ohlendorf

Wilhelm Kaupmann

Ulrich G Kuehl

Ulrich G Kuhl

New 1-phenyl-2-aminocarbonylindole compounds are described which have the general formula I ##STR1## where R.sub.1 is a hydrogen atom, or a lower alkyl, alkenyl, cycloalkyl or cycloalkylalkyl radical, R.sub.2 is a hydrogen atom or a lower alkyl radical, R.sub.3 is a hydrogen or halogen atom, or a lower alkyl, hydroxyl or lower alkoxy radical, R.sub.4 is a hydrogen or halogen atom, or a lower alkyl, hydroxyl or lower alkoxy radical, or, if R.sub.3 is a hydrogen atom, R.sub.4 may be a nitro or trifluoromethyl radical, or R.sub.3 and R.sub.4 together denote a methylenedioxy or ethylenedioxy radical, R.sub.5 has the meanings given for R.sub.3, R.sub.6 has the meanings given for R.sub.4, R.sub.7 is a hydrogen atom or, if R.sub.5 and R.sub.6 are lower alkoxy radicals, R.sub.7 may also be a lower alkoxy radical, R.sub.8 and R.sub.9 are each a hydrogen atom or a lower alkyl radical or, together with the nitrogen atom, form a heterocyclic group, and Z is a alkylene chain which is optionally substituted by hydroxyl. The compounds have pharmacological properties, in particular antiarrhythmic properties. The compounds may be in the form of the free base or acid addition salts. Pharmaceutical compositions containing these compounds are described as is a method of preparing them. Valuable intermediates for the production of these compounds and methods of preparing the intermediates are also described.

1-phenyl-2-aminocarbonylindole compounds, preparation thereof and

Novel 1-phenyl-2-aminocarbonylindole compounds are disclosed having the general formula I ##STR1## wherein R.sub.1 is an aliphatic or aromatic acyl group or an optionally substituted benzyl group; R.sub.2 is hydrogen or a lower alkyl radical; R.sub.3 is a hydrogen, a halogen, a lower alkyl radical, or a lower alkoxy radical; R.sub.4 is hydrogen, a halogen, a lower alkyl radical, or a lower alkoxy radical; R.sub.5 has the significance given R.sub.3 ; R.sub.6 has the significance given for R.sub.4, or R.sub.6 is nitro or trifluoromethyl; R.sub.7 and R.sub.8 each represent hydrogen or a lower alkyl radical, or together with a nitrogen atom form a heterocyclic group; and Z signifies an alkylene chain optionally substituted by hydroxy or acyloxy. The compounds have pharmacological, in particular antiarrhythmic, properties.

New 1-phenyl-2-aminocarbonylindole compounds are described which have the general formula I ##STR1## where R.sub.1 is a hydrogen atom, or a lower alkyl, alkenyl, cycloalkylalkyl radical, R.sub.2 is a hydrogen atom or a lower alkyl radical, R.sub.3 is a hydrogen or halogen atom, or a lower alkyl, hydroxyl or lower alkoxy radical, R.sub.4 is a hydrogen or halogen atom, or a lower alkyl, hydroxyl or lower alkoxy radical, or, if R.sub.3 is a hydrogen atom, R.sub.4 may be a nitro or trifluoromethyl radical, or R.sub.3 and R.sub.4 together denote a methylenedioxy or ethylenedioxy radical, R.sub.5 has the meanings given for R.sub.3, R.sub.6 has the meanings given for R.sub.4, R.sub.7 is a hydrogen atom or, if R.sub.5 and R.sub.6 are lower alkoxy radicals, R.sub.7 may also be a lower alkoxy radical, R.sub.8 and R.sub.9 are each a hydrogen atom or a lower alkyl radical or, together with the nitrogen atom, form a heterocyclic group, and Z is an alkylene chain which is optionally substituted by hydroxyl. The compounds have pharmaceutical properties, in particular antiarrhythmic properties. The compounds may be in the form of the free bases or acid addition salts. Pharmaceutical compositions containing these compounds are described as is a method of preparing them. Valuable intermediates for the production of these compounds and methods of preparing the intermediates are also described.

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Hanover, Germany

Stephen J Magda