Farmitalia Carlo Erba

Carlo Erba

Farmitalia Carlo Erba S.r.l.

Alessandro Rossi

Piero Melloni

Sergio Mantegani

Aldemio Temperilli

Lorenzo Pegrassi

Luigi Bernardi

Francesco Lauria

Raffaele Tommasini

Arturo Della Torre

Gabriella Traquandi

Norina Passerini

Metilde Buonamici

Enzo Brambilla

Germano Bosisio

Giovanni C Carniel

Gerhard Zetler

Chiara De Paolis

Patricia Salvati

Nicola Mongelli

Lucio Merlini

Ettore Lazzari

Arturo D Torre

Giuseppe Mazzini

Rosanna Eccel

Maria L Malnati

Use of ergoline derivatives in treating emesis

Compounds of the formula I ##STR1## wherein R.sub.1 represents a hydrogen atom or a methyl group, either R.sub.2 and R.sub.3 represent hydrogen atoms or together represent a chemical bond, R.sub.4 represents a hydrogen atom or a C.sub.1 -C.sub.4 alkyl group, R.sub.5 represents a C.sub.1 -C.sub.4 alkyl group or an allyl group and R.sub.6 represents a hydrogen or halogen atom, and pharmaceutically acceptable salts thereof, are disclosed as being useful for the treatment of extrapyramidal syndromes such as Parkinson's disease.

Antiparkinson ergoline derivatives

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

Ergoline derivatives of the formula I ##STR1## wherein R.sub.1 =H,CH.sub.3 ; R.sub.2 =H, halogen, CH.sub.3, CN, C.sub.1 -C.sub.4 alkylthio or phenylthio; R.sub.3 =C.sub.1 -C.sub.4 hydrocarbon; R.sub.4 =H, OCH.sub.3 ; R.sub.5 =H and R.sub.6 =--CH.dbd.CH--CONHR.sub.7 or R.sub.5 and R.sub.6 =.dbd.CH--CONHR.sub.7 ; R.sub.7 =2-thiazolyl, 3-pyridazinyl, 1,3,4-thiadiazol-2-yl or 4-pyrimidinyl group optionally substituted, and pharmaceutically acceptable salts thereof, display activity on the Central Nervous System and are useful as antiprolactinic agents. Their preparation and pharmaceutical compositions containing them are also described.

Ergoline compounds useful as antiparkinson agents

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.

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

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

There are provided compounds of formula 1: ##STR1## wherein R=halogen atom or CN, NH.sub.2 and NO.sub.2 group, and pharmaceutically acceptable salts thereof. The compounds are antipsycotic agents.

Antipsycotic benzoxazines

Substituted imino derivatives of 4 H-2, 3-dihydrobenzopyran and 4 H-2, 3-dihydrobenzothiopyran, and pharmaceutical compositions containing them. The compounds are active on the central nervous system, in particular as central nervous system depressants, i.e., sedatives, anticonvulsive agents, tranquilizers and sleep-inducing agents.

Substituted iminoderivatives of dihydrobenzopyran and

A method of treating pain of whatever origin and nature in human and animal which comprises administering to the patient in need an effective amount of a polypeptide of structure: ##STR1## wherein X is selected from the group consisting of hydrogen, t-butyloxycarbonyl(Boc), Asp, Pyr-Glu, Pyr-Gln-Asp, Pyr-Asn-Asp; Y is selected from the group consisting of Thr, Met, Leu, Nle, Val; W is selected from the group consisting of Met, Nle, Leu.

Use of polypeptides as analgesic drugs

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

A method of treating pain of whatever origin and nature in human and animal which comprises administering to the patient in need an effective amount of a polypeptide of structure: ##STR1## wherein X is selected from the group consisting of hydrogen, t-butyloxycarbonyl(Boc), Asp, Pyr--Glu, Pyr--Gln--Asp, Pyr--Asn--Asp;

Substituted morpholine derivatives, such as, for instance the compound 2-[.alpha.-(3,4-methylendioxy-phenoxy)-benzyl]-morpholine are disclosed. The claimed compounds are active on the central nervous system, and may be used as antidepressant agents.

Substituted morpholine derivatives and pharmaceutical compositions

Substituted morpholine derivatives, such as, for instance, the compound 2-[.alpha.-(2-methoxy-phenoxy)-benzyl]-morpholine are disclosed. The claimed compounds are active on the central nervous system, and may be used as antidepressant agents.

Substituted morpholine derivatives and compositions

Cyclic derivatives of 1,4-benzoxazine and 1,4-benzothiazine are disclosd, such as, for instance, 1H,2,3,3a,4-tetrahydro-2-carbamoylmethyl-imidazo[5,1-c][1,4]benzoxazin-1-o ne and 1H,2,3,3a,4-tetrahydro-2-carbamoylmethyl-8-chloro-imidazo[5,1-c][1,4]benzo xazin-1-one. These compounds are active on the central nervous system, and function as antidepressant agents.

Imidazo[5,1-c][1,4]benzoxazin-1-one

Novel N-tricyclic derivatives of azetidine are disclosed of the general formula ##STR1## where A is a C.sub.1 -C.sub.3 alkylene group, a C.sub.2 -C.sub.3 alkenylene group or a cyclopropylene group, the remaining substituents being defined in the specification. Such compounds are useful for their anti-depressant, anti-convulsant and anxiolytic activities. The compound 1-[5-(10, 11-dihydro-5H-dibenzo [a,d]cyclopheptenyl)]-3-methyl-amino-azetidine is illustrative.

Growing community of inventors

Milan, Italy

Alessandro Rossi