Istituto Luso Farmaco D'italia S.p.a.

Istituto Luso Farmaco D'italia S.r.l.

Instituto Luso Farmaco D'italia S.p.a.

Instituto Luso Farmaco D'italia S.r.l.

Istituto Luso Farmaco D'italia

A. Menarini Industrie Farmaceutiche Riunite

Giuseppe Cascio

Elso Manghisi

Giancarlo B Fregnan

Federico Maria Arcamone

Aldo Salimbeni

Vittorio Pestellini

Roberto Porta

Maria Altamura

Enzo Perrotta

Giovanni Ferni

Liliana Bastianini

Piero Sbraci

Penem derivatives of general formula (I), below, and pharmaceutically acceptable salts thereof are disclosed. ##STR1## wherein: R.sub.1 is H, C.sub.1 -C.sub.6 alkoxy, C.sub.3 -C.sub.7 cycloalkyl, or an optionally protected C.sub.1 -C.sub.6 hydroxyalkyl; R.sub.2 is a free or esterified carboxyl group or a carboxylate anion; R.sub.3 is H or C.sub.1 -C.sub.6 alkyl; R.sub.4 is H, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 hydroxyalkyl, C.sub.1 -C.sub.6 mercaptoalkyl, C.sub.1 -C.sub.6 aminoalkyl, C.sub.1 -C.sub.6 alkyl substituted by a quaternary ammonium group, C.sub.1 -C.sub.6 carboxyalkyl, cycloalkyl, aryl, arylalkyl, heterocyclyl-alkyl optionally substituted, saturated or unsaturated heterocycle, or R.sub.3 and R.sub.4 are linked together to form a heterocyclic ring having 3-7 atoms; R.sub.5 and R.sub.6 independently are H, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 hydroxyalkyl, C.sub.1 -C.sub.6 mercaptoalkyl, C.sub. -C.sub.6 aminoalkyl, alkenyl, cycloalkyl, aryl, arylalkyl, alkylaryl, heterocyclyl-alkyl, C.sub.1 -C.sub.6 alkyl carboxyamide, or R.sub.5 and R.sub.6 are taken together to form a heterocyclic ring having 3-7 atoms, and n is an intiger from 1 to 3.

Penem derivatives, their preparation and pharmaceutical compositions

Invention concerns 4,5-bisubstituted-2-imidazolone derivatives of formula I ##STR1## and pharmaceutically acceptable salts thereof, having high affinity in vitro for D.sub.2, 5-HT.sub.2, .sub.1 receptors and in vivo activity on central nervous system and antihypertensive activity with negligible secondary effects; methods for the preparation thereof; pharmaceutical formulations containing them.

Imidazolone derivatives with activity on central nervous system and

A pharmaceutical compound characterized by a delayed release of the therapeutically active component, comprising a sulfonic type ion exchange resin and cis(.+-.)-3-acetyloxy-5-[2-(dimethylamino)ethyl]-2,3-dihydro-2-(4-methoxyp henyl)-1,5-benzothiazepin-4(5H)one, or cis(.+-.)-3-hydroxy-5-[2-(dimethylamino)ethyl]-2,3-dihydro-2-(4-methoxyphe nyl)-1,5-benzothiazepin-4(5H)one as a therapeutically active compound. A process for the preparation of the active compound. A pharmaceutical composition including said active compound, and use of said composition for the prophylaxis and therapy of acute and chronical coronary insufficiency and of arterial hypertension.

Sulfonic resins having a therapeutical activity, preparation thereof and

The dl-.alpha.-2-hydroxy-3-(4-methoxyphenyl)-3-(2-aminophenylthio)propionic acid, which is a useful intermediate for the synthesis of pharmacologically active compounds, is separated in its enantiomers through salification with L-lysine with high yields and optical purities.

Process for the optical resolution of the

The invention provides novel substituted 2-phenylamino-imidazolines-(2) having hypotensive, bradycardizing and diuretic activities.

Substituted 2-phenylamino-imidazolines-(2) and pharmaceutical

The invention provides novel 4-aryl-5-aminoalkyl-1,3-dioxol-2-ones having hypocholesterolemic, hypolipemic, antiulcer, antihistaminic and antiserotoninic activities.

4-Aryl-5-piperazinoalkyl-1,3-dioxol-2-ones, and compositions

The invention provides novel 4-aryl-5-aminoalkyl-4-thiazolin-2-ones and their salts and complexes which have activity on the central nervous system, the cardio-vascular system, and anti-inflammatory, adrenolytic and anti-ulcer activity.

Certain 4-aryl-5-(4-phenylpiperazino)alkyl-4-thiazolin-2-ones

1,3-Disubstituted-3-aroylpropanes of the formula: ##EQU1## and their salts, in which Ar represents an aryl residue unsubstituted or substituted by halogen, polyhalogeno alkyl or lower alkoxy; R.sup.1 represents an hydroxy, acyloxy, carbamoyloxy, alkylcarbamoyloxy, dialkylcarbamoyloxy, aroyloxy, alkoxy, aryloxy, or cyano group or an amino group of the formula: ##EQU2## which can be the residue of a secondary amine, a tertiary amine, or of a heterocyclic amine; and ##EQU3## represents the residue of a secondary amine, a tertiary amine, or of a heterocyclic amine, have interesting properties as analgesic agents, anti-arrhythmic agents, and central nervous depressants.

1,3-Disubstituted 3-aroylpropanes and process for the preparation thereof

The invention relates to compounds of the formula: ##EQU1## wherein Ar is a substituted or unsubstituted aryl group, --N(R.sub.1 R.sub.2) is a generic primary or secondary amine, X is O or a functional derivative of the C = O group, and R.sub.3 is a generic hydrocarbyl radical. These compounds are endowed with anti-bacterial, anti-mitotic and anti-mycotic activity.

Growing community of inventors

Monza, Italy

Giuseppe Cascio