US 4,728,649 AGranted

3-oxo-piperazin-1-yl-ergolines exhibiting antidopaminergic activity

AssigneeFarmitalia Carlo Erba S.p.A.

InventorsSergio Mantegani, Aldemio Temperilli, Gabriella Traquandi, Alessandro Rossi, Lorenzo Pegrassi

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Abstract

The invention relates to ergoline derivatives having the general formula (I): ##STR1## where R=H, CH.sub.3 ; R.sub.1 =H, halogen, CH.sub.3, phenylthio, C.sub.1 -C.sub.4 alkylthio; R.sub.2 =H, CH.sub.3 O, and R.sub.3 =H or R.sub.2 +R.sub.3 =chemical bond; R.sub.4 =C.sub.1 -C.sub.4 hydrocarbon; R.sub.5, R.sub.6, R.sub.8, R.sub.9 independently=H, C.sub.1 -C.sub.4 alkyl, or R.sub.5, R.sub.8 independently=H, C.sub.1 -C.sub.4 alkyl and R.sub.6 +R.sub.9 =CH.sub.2 CH.sub.2, CH.sub.2 CH.sub.2 CH.sub.2 ; R.sub.7 =H, C.sub.1 -C.sub.4 alkyl, phenyl, NR'R"; R',R" independently=H, C.sub.1 -C.sub.4 alkyl, acyl or NR'R"=heterocyclic ring; W=0, H.sub.2 ; n=0, 1, 2, and their pharmaceutically acceptable salts, these compounds exhibiting antihypertensive activity making them useful anxiolytic and antipsychotic agents. A process for their preparation and pharmaceutical compositions containing them are also described.

Claims16

Dependent claims

An ergoline compound of the formula I ##STR5## wherein R represents a hydrogen atom or a methyl group;

R.sub.1 represents a hydrogen or halogen atom, a methyl or phenylthio group or an alkylthio group having from 1 to 4 carbon atoms;
R.sub.2 represents a hydrogen atom or a methoxy group and R.sub.3 represents a hydrogen atom, or R.sub.2 and R.sub.3 together represent a chemical bond;
R.sub.4 represents a hydrocarbon group having from 1 to 4 carbon atoms selected from the group consisting of alkyl, cycloalkyl, and ethylenically or acetylenically unsaturated groups;
R.sub.5, R.sub.6, R.sub.8 and R.sub.9 each independently represents a hydrogen atom or an alkyl group having from 1 to 4 carbon atoms, or R.sub.5 and R.sub.8 are as above defined and R.sub.6 and R.sub.9 together represent an ethylene or trimethylene group;
R.sub.7 represents a hydrogen atom, an alkyl group having from 1 to 4 carbon atoms, a phenyl group or a group of the general formula NR'R" wherein either each of R' and R" independently represents a hydrogen atom, an alkyl group having from 1 to 4 carbon atoms or an acyl group selected from the group consisting of C.sub.1-5 alkanoyl and benzoyl groups, or R' and R" together with the nitrogen atom to which they are attached represent a heterocyclic ring selected from the group consisting of pyrrolidine, piperidine, morpholine, pyrazole, imidazole and pyrrole;
W represents an oxygen atom or two hydrogen atoms;
and
n is 0, 1 or 2;
and pharmaceutically acceptable salts of a compound of formula I.

6 more elements

Dependencies are inferred from the claim text.