Menarini Ricerche S.p.a.

Laboratori Guidotti S.p.a.

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

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

Istituto Luso Farmaco D'italia

A. Menarini Industrie Farmaceutiche Riunite

Maria Altamura

Carlo Alberto Maggi

Enzo Perrotta

Danilo Giannotti

Federico Maria Arcamone

Alessandro Sisto

Vittorio Pestellini

Giuseppe Cascio

Alessandro Giolitti

Valerio Caciagli

Sandro Giuliani

Reinhard Schmitz

Valentina Fedi

Piero Sbraci

Claudia Lewerenz

Antonio Guidi

Nicholas Harmat

Rossano Nannicini

Alberto Aleotti

Franco Pasqui

Oral liquid pharmaceutical compositions containing as active ingredient Nepadutant, PGS as solubilizer and optionally a chelating agent. Such compositions are found to be very stable and suitable for paediatric use in the treatment of gastro-intestinal diseases.

Pediatric oral liquid compositions containing nepadutant

Pharmaceutical compositions containing NK2 antagonists are described, useful for the treatment of infantile colics.

Pharmaceutical compositions based on NK2 antagonists for pediatric use

Described herein are compounds of formula (I) useful as antagonists of tachykinins in general, and in particular of neurokinin A; and the pharmaceutical formulations comprising the compounds of formula (I) 

Linear basic compounds having NK-2 antagonist activity and formulations thereof

Basic monocyclic compounds having general formula (I) useful as NK-2 antagonists are described, processes for their preparation and pharmaceutical compositions containing them are also described.

Basic monocyclic compounds having Nk2 antagonist action, processes for their preparation, and formulations containing them

Process for the preparation of 2-halomethyl-penems (I) comprising (a) reacting an acetoxy-(protected hydroxyethyl)-2-azetidinone (III) with a 2-halothioacetic acid to form a 3-haloacetylthioazetidinone (V), (b) reacting (V) with oxalyl chloride to give an intermediate (VII), acylated on the beta-lactamic nitrogen, and (c) cyclizing (VII) in the presence of an organic phosphate or phosphonite to produce the corresponding 2-halomethyl-penem (I).

Process for the preparation of 2-halomethyl-penems and their use for the

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

Growing community of inventors

Florence, Italy

Maria Altamura