Farmitalia Carlo Erba

Societa' Farmaceutici Italia

Germano Bosisio

Luigi Bernardi

Aldemio Temperilli

Giuliana Arcari

Sergio Mantegani

Anna M Caravaggi

Alfredo Glasser

Patricia Salvati

Alessandro Rossi

Gabriella Traquandi

Enrico Di Salle

Maurizio Foglio

Rosanna Eccel

Osvaldo Sapini

Innocenzio Sinatra

Gian Carlo Fregnan

Guiliana Arcari

Ergoline derivatives of formula: ##STR1## wherein n=0,1,2; R.sub.1 =H, CH.sub.3 ; R.sub.2 =H, CH.sub.3, halogen; R.sub.3 =H, OCH.sub.3 ; R.sub.4 =hydrocarbon group and R.sub.5 is a residue of general formula II, III, IV, V, VI, VII: ##STR2## wherein R.sub.6 =H, Cl, OCH.sub.3, NR.sub.11 R.sub.12, wherein R.sub.11 and R.sub.12 =H, lower alkyl; phenyl or are bonded together to form a heterocyclic ring, R.sub.7, R.sub.8 and R.sub.9 and R.sub.10 =H or C.sub.1 -C.sub.3 alkyl, with the proviso that if R.sub.5 is of formula II and R.sub.2 =R.sub.7 =R.sub.8 =H, then R.sub.4 is not methyl or n is not 0. Pharmaceutically acceptable acid addition salts are also provided. A method for their preparation is also provided. The compounds have anti-depressive, anti-hypertensive and antiprolactin activity.

8-pyridazinylcarbamoyl ergolines

Novel ergoline derivatives formed by reaction of an 8-carboxy ergoline with a carbodiimide and having hypotensive and antiprolatinic activity.

Dimethylaminoalkyl-3-(ergoline-8'.beta.carbonyl)-ureas

Compounds are disclosed of formula (I) ##STR1## wherein R.sub.1 represents a hydrogen atom or a methyl group; R.sub.2 represents a hydrogen atom or a methoxy group;

Ercoline derivatives and therapeutic compositions having CNS affecting

Compounds and process for making same are disclosed, the compounds having the formula (I): ##STR1## wherein R.sub.1 represents methyl, phenyl, piperidino, 1-pyrrolidinyl, morpholino or 4-methyl-1-piperazinyl, alkyl or alkoxy having from 1 to 4 carbon atoms, amino, substituted amino of the formula NHR' (wherein R' is alkyl having from 1 to 4 carbon atoms, cycloalkyl, a benzyl, or phenyl) or substituted amino of the formula NR' R'' (wherein R' and R'' both represent alkyl having from 1 to 4 carbon atoms);

Ergot derivatives

Compounds and process for making same are disclosed, the compounds having the formula (I): ##STR1## wherein R.sub.1 represents a methyl, phenyl, piperidino, 1-pyrrolidinyl, morpholino or 4-methyl-1-piperazinyl group, an alkyl or alkoxy group having from 1 to 4 carbon atoms, an amino group, a substituted amino group of the formula NHR' (wherein R' represents an alkyl group having from 1 to 4 carbon atoms, a cycloalkyl group, a benzyl group, or a phenyl group) or a substituted amino group of the formula NR' R'' (wherein R' and R'' both represent alkyl groups having from 1 to 4 carbon atoms);

Pyrimidinoaminoethyl ergoline derivatives of the formula: ##STR1## wherein R is hydrogen or methyl; R.sub.1 and R.sub.2 are independently selected from the group consisting of hydrogen, alkyl having 1 to 3 carbon atoms, methoxy and phenyl; R.sub.3 is hydrogen, halogen, alkyl and alkoxy each having 1 to 3 carbon atoms, phenyl, nitro, amino, cyano, acylamino, carboxamido and carbalkoxy each having 1 to 3 carbon atoms, trifluoromethyl or --SO.sub.2 --Y wherein Y is hydroxyl, amino or methyl and R.sub.4 is hydrogen or methoxy are prepared by reacting an ergoline derivative of formula III and a 2-aminopyrimidine anion of formula II ##STR2##

Pyrimidinoaminoethyl ergoline derivatives

Ergoline derivatives are disclosed having the general formula ##SPC1## Wherein R is selected from the group consisting of a lower alkyl radical having from 1 to 4 carbon atoms; an --NH-lower alkyl radical having from 1 to 4 carbon atoms; a free or substituted phenyl- or 2-furanoyl radical; the --O--CH.sub.2 --C.sub.6 H.sub.5 radical; a (3)- or (4)-pyridine radical free or substituted by a methyl radical or a chlorine or bromine atom; a pyrrole radical of formula ##SPC2## Wherein

1,6-Dimethyl-8.beta.-[2' or 3'-pyrroyloxyethyl or substituted

Esters of 1-methyl-lumilysergol-10-methylether having the formula: ##SPC1## Wherein R is selected from the group consisting of 2-furanoyl and the pyrrole group of the formula: ##SPC2## Wherein Y is selected from the group consisting of hydrogen, lower alkyl having from 1 to 6 carbon atoms and phenyl; R.sub.1 is selected from the group consisting of hydrogen, methyl and carbonyl; R.sub.2 is selected from the group consisting of hydrogen, methyl, halogen and carbonyl, provided that only one of R.sub.1 and R.sub.2 can be carbonyl; R.sub.3 and R.sub.4 are selected from the group consisting of hydrogen, halogen, alkyl, alkoxy having from 1 to 6 carbon atoms and carboethoxy; the pharmaceutically acceptable addition salts thereof with an organic acid and a process for the preparation thereof. The compounds possess adrenolytic, hypotensive, sedative and antiserotoninic activities.

Pyrrole-carboxylic acids lumilysergol esters

Novel 8.beta.-pyrimidino-aminomethyl-10.alpha.-ergoline and 10.alpha.-methoxyergoline derivatives which possess a high and prolonged adrenolytic activity and a low toxicity, and some of which also possess hypotensive and analgesic activity are prepared by reacting a pyrimidine anion with an ergoline derivative in an aprotic solvent.

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Milan, Italy

Germano Bosisio