Farmitalia Carlo Erba

Farmitalia Carlo Erba S.r.l.

Pharmacia & Upjohn

Farmitalia Carlo Erba S.r.l. an Italian Body Corporate

Enzo Brambilla

Sergio Mantegani

Aldemio Temperilli

Nicola Carfagna

Patricia Salvati

Tiziano Bandiera

Mauro Gobbini

Alessandro Rossi

Carla Caccia

Daniela Ruggieri

Lorenzo Pegrassi

Maria A Cervini

Mario Varasi

Luigi Bernardi

Gabriella Traquandi

Enrico Di Salle

Laura Chiodini

Metilde Buonamici

Osvaldo Sapini

Rosanna Eccel

Roberto Maj

There are provided compounds of formula (I), wherein R,is a hydrogen, chlorine or bromine atom or a methyl, methylthio, hydroxy, cyano or carboxamido group; R,is C,-C,alkyl or an alkyl group; R,and R,are independently a hydrogen atom, a C,-C,alkyl group, a C,-C,alkenyl group, a C,-C,cycloalkyl C,-C,alkyl group, a phenyl-C,-C,alkenyl or phenyl group: which groups are optionally substituted by C,-C,alkyl, C,-C,alkoxy, triflouromethyl, hydroxy or amino group; or a group of formula (a), wherein R,is hydrogen atom or a C,-C,alkyl group and R,is a phenyl group, a substituted phenyl group as described above or a heterocyclic ring, R,is a hydrogen or bromine atom or an organic residue and R is H or an organic residue, or a pharmaceutically acceptable salt thereof. A process for their preparation and the pharmaceutical compositions comprising them are also provided.

Abeo-ergoline derivatives as 5HT1A ligands

Antineurodegenerative ergoline derivatives

The present invention provides compounds of the formula (I) ##STR1## wherein A, R.sub.1, R.sub.2 and R.sub.3 are defined as in the specification, or a pharmaceutically acceptable salt thereof. A process for their preparation and the pharmacetical compositions comprising them are also provided.

Serotoninergic ergoline derivatives

Process for preparing ergoline derivatives

Use of ergoline derivatives in treating emesis

t-alkyl eroline derivatives of formula I are produced ##STR1## wherein (R.sub.1 =H, OCH.sub.3 and R.sub.2 H) or (R.sub.1 +R.sub.2 =a ring bond and R.sub.3 =H, optionally substituted nicotinynoyl or 1-oxo-2-cyclopenten-3-yl); and their pharmaceutically acceptable salts. A process for the preparation of these derivatives from lysergol and a t-alkyl alcohol is also described, as are pharmaceutical compositions containing them.

t-alkyl ergoline derivatives

An ergoline derivative of the formula I: ##STR1## wherein R.sub.1 represents hydrogen or a methyl group; R.sub.2 represents hydrogen or a halogen atom, a methyl, cyano or phenyl group or an alkylthio group having from 1 to about 4 carbon atoms; R.sub.3 represents a hydrocarbon group having from 1 to about 4 carbon atoms; R.sub.4 represents hydrogen, a phenyl group or a hydrocarbon group having from 1 to about 4 carbon atoms; wherein either (a) R.sub.6 and R.sub.7 represent a valence bond or hydrogen atoms and R.sub.8 represents a hydrogen atom or a methoxy group, or (b) R.sub.6 represents a hydrogen atom and R.sub.7 and R.sub.8 taken together represent a valence bond; W represents an oxygen atom or an imino group; A represents a group of the formula CHR.sub.5, CH.dbd.CR.sub.5 or CH.sub.2 CHR.sub.5 wherein R.sub.5 represents a hydrogen atom or an alkyl group having from 1 to about 4 carbon atoms; X represents an oxygen or sulphur atom or an imino group; and n is 0, 1 or 2; or a pharmaceutically acceptable salt thereof.

N-oxide ergolines as antihypertensive agents

t-Alkyl ergoline derivatives of formula I are produced ##STR1## wherein (R.sub.1 =H, OCH.sub.3 and R.sub.2 =H) or (R.sub.1 +R.sub.2 =a ring bond and R.sub.3 =H, optionally substituted nicotinoyl or 1-oxo-2-cyclopenten-3-yl); and their pharmaceutically acceptable salts. A process for the preparation of these derivatives from lysergol and a t-alkyl alcohol is also described, as are pharmaceutical compositions containing them.

1-t-butyl ergolines useful in the treatment of cerebral insufficiency

Ergoline derivatives of the 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;

Ergolinyl heterocycles for the treatment of Parkinson's disease and

Compounds of the formula I: ##STR1## wherein R.sub.1 =H, CH.sub.3 ; m=0,1; R.sub.2 =R.sub.3 =H or R.sub.2, R.sub.3 =bond, R.sub.4 =C.sub.1 -C.sub.4 hydrocarbon, n=1 or 2 and their pharmaceutically acceptable salts are antihypertensive agents. Their preparation and pharmaceutical compositions containing them are also described.

Tetracyclic indole derivatives for treating hypertension

Ergoline Esters having the formula (I) ##STR1## in which R.sub.1 =H or CH.sub.3 ; R.sub.2 =C.sub.1 -C.sub.4 hydrocarbon; R.sub.3 =H or OCH.sub.3 ; R.sub.4 =H or halogen; R.sub.5 =C.sub.1 -C.sub.4 alkyl and their pharmaceutically acceptable salts are active at the central nervous system level. A process for their preparation is described.

Ergoline esters

There are provided ergoline derivatives of the formula: ##STR1## wherein R.sub.1 represents a hydrogen atom or a methyl group, R.sub.2 represents a hydrogen or halogen atom or a methyl group, R.sub.3 represents a hydrogen atom or a methoxy group, R.sub.4 represents a hydrocarbon group having from 1 to 4 carbon atoms; each of X and W independently represents a hydrogen atom, a methyl group, a chlorine atom or a methoxy group, and n is 0, 1 or 2. A method for their preparation is also provided. The compounds have strong antiprolactin activity.

Ergoline carboxamides

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Mariano Comense, Italy

Enzo Brambilla