2-(aminoalkyl)-pyrrole derivatives, to treat disorders caused by restriction in cerebral function
AssigneeCassella Aktiengesellschaft
InventorsGerhard Zoller, Rudi Beyerle, Ursula Schindler, Rolf-Eberhard Nitz, Piero A. Martorana
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Abstract
2-(Aminoalkyl)-pyrrole derivatives of the formula ##STR1## wherein R denotes hydrogen, alkyl or phenyl, R.sup.1 denotes, for example, hydrogen, alkyl, alkoxy-carbonyl, aryl, substituted aryl or heteroaryl, R.sup.2 and R.sup.3 denote, for example, hydrogen, alkyl, alkanoyl, arylcarbonyl, heteroarylcarbonyl or arylenedicarbonyl and n denotes 1, 2 or 3, and their acid addition salts, are used as pharmacological active compounds for combating cerebral aging processes.
Claims12
Method for the treatment of humans for combating and preventing disorders which are caused by a restriction in cerebral function, and for the treatment of cerebral aging processes, which comprises administering to a human subject to or afflicted with such disorders and for aging processes an effective dose of 2-(aminoalkyl)-pyrrole derivative of the formula I ##STR8## wherein R denotes hydrogen, alkyl(C.sub.1 -C.sub.5) or phenyl;
- R.sup.1 denotes hydrogen, alkyl(C.sub.1 -C.sub.5), cyano-alkyl(C.sub.1 -C.sub.4), alkoxy(C.sub.1 -C.sub.4)-carbonyl, alkoxy(C.sub.1 -C.sub.4)-carbonyl-alkyl(C.sub.1 -C.sub.4);
- R.sup.7 (R.sup.8)N-carbonylalkyl(C.sub.1 -C.sub.4), acetyl-amino-ethyl, phenyl or phenyl-alkyl(C.sub.1 -C.sub.4), it being possible for the phenyl or the phenyl of the phenyl-alkyl also to be monosubstituted or polysubstituted by halogen, alkoxy(C.sub.1 -C.sub.4), alkyl(C.sub.1 -C.sub.4), R.sup.4 (R.sup.5)N-, hydroxyl, mercapto, alkylmercapto(C.sub.1 -C.sub.4), nitro, cyano, alkoxy(C.sub.1 -C.sub.4)-carbonyl or alkoxy(C.sub.1 -C.sub.4)-carbonyl-alkyl(C.sub.1 -C.sub.4) or R.sup.1 denotes R.sup.4 (R.sup.5)N-R.sup.6 -, hydroxy-carbonyl-alkyl(C.sub.1 -C.sub.4), 1-(alkoxy(C.sub.1 -C.sub.4)-carbonyl)-2-mercapto-ethyl, 1-(alkoxy(C.sub.1 -C.sub.4)-carbonyl)-2-hydroxy-ethyl, 1-(alkoxy(C.sub.1 -C.sub.4)-carbonyl)-2-alkoxy(C.sub.1 -C.sub.4)-ethyl, 1-(alkoxy(C.sub.1 -C.sub.4)-carbonyl-2-alkylthio(C.sub.1 -C.sub.4)-ethyl, 1-(alkoxy(C.sub.1 -C.sub.4)-carbonyl)-2-(alkyl(C.sub.1 -C.sub.4)-carbonyl-thio)-ethyl, 1-(alkoxy(C.sub.1 -C.sub.4)-carbonyl)-2-(alkyl(C.sub.1 -C.sub.4)-carbonyl-oxy)-ethyl, or 1-(alkoxy(C.sub.1 -C.sub.4)-carbonyl)-2-phenyl-ethyl;
- R.sup.2 und R.sup.3 independently of one another denote hydrogen, alkyl(C.sub.1 -C.sub.5), alkanoyl(C.sub.1 -C.sub.5), alkanoyl(C.sub.2 -C.sub.5) which is mono-, di- or tri-substituted by amino, alkoxy(C.sub.1 -C.sub.4), hydroxyl, alkanoyloxy(C.sub.1 -C.sub.4), phenyl or halogen, phenylcarbonyl, phenylcarbonyl which is mono- or polysubstituted by halogen, alkoxy(C.sub.1 -C.sub.4), alkyl(C.sub.1 -C.sub.4), amino, R.sup.4 (R.sup.5)N-, hydroxy, alkanoyloxy(C.sub.1 -C.sub.4), mercapto, alkylmercapto(C.sub.1 -C.sub.4), nitro, cyano, alkoxy(C.sub.1 -C.sub.4)-carbonyl or aminosulphonyl, or R.sup.2 and/or R.sup.3 denote cycloalkylcarbonyl with 5 to 7 C atoms in the cycloalkyl radical or (4-chlorophenoxy)-acetyl;
- R.sup.4 and R.sup.5 denote hydrogen or alkyl(C.sub.1 -C.sub.4);
- R.sup.6 denotes alkylene(C.sub.1 -C.sub.4);
- R.sup.7 and R.sup.8 independently of one another denote hydrogen or alkyl(C.sub.1 -C.sub.4);
- and n denotes 1, 2 or 3, or a pharmacologically acceptable acid addition salt thereof.
Pharmaceutical product useful for the treatment of humans for combating and preventing disorders which are caused by a restriction in cerebral function, and for the treatment of cerebral aging processes, said product comprising an effective amount of a pharmacologically-active compound and a physiologically-acceptable, pharmacologically-inert excipient, said active compound comprising a 2-(aminoalkyl)-pyrrole derivative of the formula I ##STR9## wherein R denotes hydrogen, alkyl(C.sub.1 -C.sub.5) or phenyl;
- R.sup.1 denotes hydrogen, alkyl(C.sub.1 -C.sub.5), cyano-alkyl(C.sub.1 -C.sub.4), alkoxy(C.sub.1 -C.sub.4)-carbonyl, alkoxy(C.sub.1 -C.sub.4)-carbonyl-alkyl(C.sub.1 -C.sub.4);
- R.sup.7 (R.sup.8)N-carbonylalkyl(C.sub.1 -C.sub.4), acetyl-amino-ethyl, phenyl or phenyl-alkyl(C.sub.1 -C.sub.4), it being possible for the phenyl or the phenyl of the phenyl-alkyl also to be monosubstituted or polysubstituted by halogen, alkoxy(C.sub.1 -C.sub.4), alkyl(C.sub.1 -C.sub.4), R.sup.4 (R.sup.5)N-, hydroxyl, mercapto, alkylmercapto(C.sub.1 -C.sub.4), nitro, cyano, alkoxy(C.sub.1 -C.sub.4)-carbonyl or alkoxy(C.sub.1 -C.sub.4)-carbonyl-alkyl(C.sub.1 -C.sub.4) or R.sup.1 denotes R.sup.4 (R.sup.5)N-R.sup.6 -, hydroxy-carbonyl-alkyl(C.sub.1 -C.sub.4), 1-(alkoxy(C.sub.1 -C.sub.4)-carbonyl)-2-mercapto-ethyl, 1-(alkoxy(C.sub.1 -C.sub.4)-carbonyl)-2-hydroxy-ethyl, 1-(alkoxy(C.sub.1 -C.sub.4)-carbonyl)-2-alkoxy(C.sub.1 -C.sub.4)-ethyl, 1(alkoxy(C.sub.1 -C.sub.4)-carbony-2-alkylthio(C.sub.1 -C.sub.4)-ethyl, 1-(alkoxy(C.sub.1 -C.sub.4)-carbonyl)-2-(alkyl(C.sub.1 -C.sub.4 )-carbonyl-thio)-ethyl, 1(alkoxy(C.sub.1 -C.sub.4)-carbonyl)-2-(alkyl(C.sub.1 -C.sub.4)-carbonyl-oxy)-ethyl, or 1-(alkoxy(C.sub.1 -C.sub.4)-carbonyl)-2-phenyl-ethyl;
- R.sup.2 und R.sup.3 independently of one another denote hydrogen, alkyl(C.sub.1 -C.sub.5), alkanoyl(C.sub.1 -C.sub.5), alkanoyl(C.sub.2 -C.sub.5) which is mono-, di- or tri-substituted by amino, alkoxy(C.sub.1 -C.sub.4), hydroxyl, alkanoyloxy(C.sub.1 -C.sub.4), phenyl or halogen, phenylcarbonyl, phenylcarbonyl which is mono- or polysubstituted by halogen, alkoxy(C.sub.1 -C.sub.4), alkyl(C.sub.1 -C.sub.4), amino, R.sup.4 (R.sup.5)N-, hydroxy, alkanoyloxy(C.sub.1 -C.sub.4), mercapto, alkylmercapto(C.sub.1 -C.sub.4), nitro, cyano, alkoxy(C.sub.1 -C.sub.4)-carbonyl or aminosulphonyl, or R.sup.2 and/or R.sup.3 denote cycloalkylcarbonyl with 5 to 7 C atoms in the cycloalkyl radical or (4-chlorophenoxy)-acetyl;
- R.sup.4 and R.sup.5 denote hydrogen or alkyl(C.sub.1 -C.sub.4);
- R.sup.6 denotes alkylene(C.sub.1 -C.sub.4);
- R.sup.7 and R.sup.8 independently of one another denote hydrogen or alkyl(C.sub.1 -C.sub.4);
- and n denotes 1, 2 or 3, or a pharmaceutically acceptable acid addition salt thereof.
Dependencies are inferred from the claim text.