A. Menarini S.a.s.

A. Menarini Industrie Farmaceutiche Riunite

Istituto Luso Farmaco D'italia

A. Menarini Industrie Farmaceutiche Riunite S.r.l.

A. Menarini Industrie Farmaceutiche Riunite S.t.l.

Vittorio Pestellini

Alberto Meli

Mario Ghelardoni

Carlo Alberto Maggi

Giovanna Volterra

Danilo Giannotti

Alessandro Giolitti

Piero Del Soldato

Claudio Bianchini

Gabrio Roncucci

Federico Maria Arcamone

Giuseppe Cascio

Stefano Manzini

Maria Altamura

Sandro Giuliani

Enzo Perrotta

Paolo Rovero

Piero Sbraci

Franco Barsini

Nicola Pisanti

Martino Furio

Guglielmo Grimaldi

Adriano Barzanti

Carlo Ortolani

Riccardo Patacchini

Rossella Ciappi

Paolo Santicioli

Giovanni Viti

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

A synthetic peptide corresponding to the following formula:

Synthetic peptide antagonists of neurokinin A, salts thereof and

Use of a 10-amino-5,6-dihydro-11H-dibenzo(b,e)azepine-6,11-dione of formula I ##STR1## where R represents an atom of hydrogen or a lower alkyl group, especially containing from 1 to 5 carbon atoms, as well as of a therapeutically acceptable salt of said compound, to prepare a drug for use in the treatment of urinary incontinence.

Therapy of 10-amino-5,6-dihydro-11H-dibenzo(b,e)azepine-6,11-dione and

Novel derivatives of 11-carbonyl-6,11-dihydrodibenzo[c,f][1,2,5]thiadiazepine 5,5-dioxide of the general formula ##STR1## wherein R and R.sub.1, which can be different, represent a hydrogen atom or a (C.sub.1 -C.sub.5) alkyl or (C.sub.1 -C.sub.4)hydroxyalkyl group, or R and R.sub.1 together can form a 5-membered and/or 6-membered heterocyclic ring which may contain a further heteroatom,

Novel derivatives of 6,11-dihydro-dibenzo(C,F)(1,2,5)-thiadiazepine

Compounds corresponding to the general formula ##STR1## wherein: R and R1, that may be different, represent a hydrogen atom, a halogen, an alkyl group, an alkoxy radical in which the alkyl group contains one to four carbon atoms, a nitro group, a cyano group, an amino group, an acetamino group, a sulfamidic or N-substituted sulfamidic group; R2 represents a hydrogen atom, a halogen, an alkoxy radical, an alkyl group, a phenyl group, a phenylalkyl group, a phenylalkylene or phenylalkenyl group in which the alkylene or alkenyl radical contains two to four carbon atoms, a nitro group, a cyano group, an amino group, an acetamino group, an N-substituted suylfamidic group; and R3 represents a hydrogen atom, an alkyl group, preferably containing one to three carbon atoms or a cyano group.

(Benzofuran-2-yl)imidazoles having pharmaceutical activity, their salts

A 2-substituted benzofuran derivative of general formula I or II ##STR1## in which R.sub.1 and R.sub.2, can be the same or different, and are a hydrogen atom, a halogen atom, an alkyl group containing 1 to 4 carbon atoms, an arylalkyl group, an aryl group, a hydroxyl group, an alkoxy group, or an NH.sub.2, NH-alkyl, N(alkyl).sub.2, NH(CO-alkyl), NH(CO-aryl) or NO.sub.2 group, or R.sub.1 and R.sub.2 can together form a ring of 5-8 carbon atoms; R.sub.3 is a hydrogen atom, an alkyl group containing 1 to 4 carbon atoms or an aryl group; R.sub.4 is a hydrogen atom, an alkyl group, an aryl or an arylalkyl group, R.sub.5 is a hydroxyl group, an alkoxy group, an OCO-alkyl, an OCO-aryl, OCOHN-alkyl or OCONH-aryl group, ##STR2## where n is a number between 1 and 4, R.sub.7 is a hydrogen atom or an alkyl group containing 1 to 4 carbon atoms, and R.sub.8 and R.sub.9, which can be the same or different, represent a hydrogen atom, an alkyl group, an aryl group, an alkoyl group, arylalkoyl group or an aroyl group, or can together form a heterocyclic ring which can contain supplementary heteratoms, and R.sub.6 is a hydrogen or halogen atom, an alkyl group, an arylalkyl group, an aryl group, a hydroxyl group, an alkoxy group, or an NH.sub.2, NH-alkyl, (N(alkyl).sub.2, NHCO-alkyl, NHCO-aryl or NO.sub.2 group. The compounds are useful for treating cardiac arrhythmic, histaminic and tussive conditions.

2-substituted benzofuran derivatives useful in treating cardiac

A pharmacologically active compound has the general formula ##STR1## in which R is a hydrogen atom or an alkyl group containing from 1 to 4 carbon atoms; R.sub.1 and R.sub.2, which can be different, represent a hydrogen atom, a hydroxyl group, an alkyl group, an alkoxy group, an arylalkyl group, or an arylalkoxy group, or can jointly represent an oxygen atom or a CHCOOR.sub.1 ' group where R.sub.1 ' is a hydrogen atom or an alkyl group; and R.sub.3 represents a hydrogen or halogen atom or an alkyl, NH.sub.2, NO.sub.2, NHCO-alkyl, NHCO-aryl, NHCONH-alkyl or NHCOHN-aryl group. These compounds act on the central nervous system and have an anti-convulsant sedative activity.

Tricyclic derivatives of 5,6-dihydro-11H-dibenzo (b,e) azepin-6-one

The invention comprises: a derivative of 1-alkylamine-3-[4(p-alkyloxy-benzamide)phenoxy]-2-propanol of general formula I: ##STR1## where R.sub.1 is a linear or branched alkyl chain with 1 to 8 carbon atoms included, an alkenyl chain with 2 to 8 carbon atoms included, or an arylalkyl chain with 7 to 10 carbon atoms included, and R is a linear or branched alkyl group with 1 to 8 carbon atoms included;

Derivatives of

A 2-substituted benzofuran derivative of general formula I or II ##STR1## in which R.sub.1 and R.sub.2, can be the same or different, and are a hydrogen atom, a halogen atom, an alkyl group containing 1 to 4 carbon atoms, an arylalkyl group, an aryl group, a hydroxyl group, an alkoxy group, or an NH.sub.2, NH-alkyl, N(alkyl).sub.2, NH(CO-alkyl), NH(CO-aryl) or NO.sub.2 group, or R.sub.1 and R.sub.2 can together form a ring of 5-8 carbon atoms; R.sub.3 is a hydrogen atom, an alkyl group containing 1 to 4 carbon atoms or an aryl group; R.sub.4 is a hydrogen atom, an alkyl group, an aryl or an arylalkyl group, R.sub.5 is a hydroxyl group, an alkoxy group, an OCO-aryl an OCO-alkyl, OCONH-alkyl or OCONH-aryl group, ##STR2## where n is a number between 1 and 4, R.sub.7 is a hydrogen atom or an alkyl group containing 1 to 4 carbon atoms, and R.sub.8 and R.sub.9, which can be the same or different, represent a hydrogen atom, an alkyl group, an aryl group, an alkoyl group, arylalkoyl group or an aroyl group, or can together form a heterocyclic ring which can contain supplementary heteratoms, and R.sub.6 is a hydrogen or halogen atom, an alkyl group, an arylalkyl group, an aryl group, a hydroxyl group, an alkoxy group, or an NH.sub.2, NH-alkyl, N(alkyl).sub.2, NHCO-alkyl, NHCO-aryl or NO.sub.2 group. The compounds are useful for treating arrhythmic, histaminic and tussive conditions.

N-[(Benzofuran-2-yl)(phenyl)methyl]-alkylene diamines useful in treating

A new compound 3(4-phenyl-1-piperazinio-1-yl)-1,2-propanediol 3(theophyllin-7-yl)-1-propanesulphonate, possesses antitussive action and is therefore usable in therapy. The compound is obtained by treating 3(theophyllin-7-yl)-1-propanesulphonic acid with 3(4-phenylpiperazin-1-yl)-1,2-propanediol in a suitable solvent.

Compound having antitussive activity

A compound for use as a normolipidemizer and/or a platelet anti-binder in therapy, and pharmaceutical compositions containing the compound. The compound comprises (2-benzofuryl)-(p-chlorophenyl)-carbinol (Chloridarol, DCI) of formula: ##STR1##

Pharmaceutical methods

A compound having pharmacological properties comprising the structural formula ##STR1## wherein R is selected from the isopropyl, n-octyl, n-butyl or isobutyl groups; R.sub.1 is selected from the 1-naphthyloxymethyl, (2-allylphenoxy)-methyl, 4-nitrophenyl, {2-[(tetrahydrofurfuryl)oxy-]-phenoxy}-methyl, [4-(2-methoxyethyl)phenoxy]methyl, 4-isopropylthiophenyl, 4-acetaminophenoxymethyl groups; and R.sub.2 represents a hydrogen atom or a methyl group. A method for synthetizing the compound is also disclosed comprising the cyclization of aminoalcohol or halogenurethane.

Derivatives of 2-oxazolydone and methods for preparing the same

New compounds useful as spasmolytic agents are provided with the following formula: ##STR1## wherein n is either 2 or 3. In addition, salts of these new compounds are provided and are suitable for oral as well as parenteral administration to animals and man as spasmolytic agents. In compositions for oral and parenteral or rectal administration, from about 5 to about 40 mg of active ingredient per dosage unit is used. The bromide and iodide salts of these new compounds are especially useful.

2-(4-Biphenylyl)-N-(2-diethylamino alkyl)propionamide and salts thereof

This invention relates to the use of 2-(1-chloro-2-yloxy) propionic acid and its derivatives having physiological activity, notably as antiphlogistics, analgesics, analgesics and anti-pyretics. The physiologically active compounds include esters and amides of the substituted propionic acid. The compounds can be presented in conventional pharmaceutical form, including the non-toxic, pharmaceutically acceptable salts thereof.

Growing community of inventors

Florence, Italy

Vittorio Pestellini