A. Menarini S.a.s.

Menarini Ricerche S.p.a.

Istituto Luso Farmaco D'italia

Alessandro Giolitti

Carlo Alberto Maggi

Vittorio Pestellini

Mario Ghelardoni

Danilo Giannotti

Alberto Meli

Laura Quartara

Christopher Ingo Fincham

Cristina Rossi

Patrizia Felicetti

Alessandro Sisto

Stefano Manzini

Giovanna Volterra

Maria Altamura

Valerio Caciagli

Valentina Fedi

Nicholas Harmat

Rossano Nannicini

Franco Pasqui

Federico Calvani

Fernando Catrambone

Martino Furio

Guglielmo Grimaldi

Rosa Terracciano

Adriano Barzanti

Carlo Ortolani

Rossella Ciappi

Antonio Guidi

Non-peptide compounds having activity as selective antagonists of bradykinin (BK) B2 receptor are disclosed. The compounds have the general formula (I) in which R is hydrogen or methyl; W is a single bond or an oxygen atom; n=3; X is hydrogen or a &#x2014;NRRamino group in which Rand Rcan be independently hydrogen or a group which is methyl, ethyl, n-propyl, or isopropyl; Y is a &#x2014;NRRRquaternary ammonium group in which RRRcan be independently a group which is methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl, or n-pentyl; and the enantiomers and enantiomeric mixtures thereof. Pharmaceutical compositions containing these compounds and methods of using the compounds to treat patients having conditions, disorders or diseases involving activation of bradykinin B2 receptors are also disclosed.

Non-peptide bradykinin antagonists and pharmaceutical compositions therefrom

Non-peptide compounds of formula (I) having activity as specific antagonists of bradykinin (BK) B2 receptor. The compounds are chemically characterized by the presence of an alpha, alpha-disubstituted amino acid at least one amino group, free or salified, or the corresponding ammonium quaternary salt. These BK receptor antagonists are a novel class of medicaments which can be used in all the disorders in which the receptors are involved.

Basic non-peptide bradykinin antagonists and pharmaceutical compositions therefrom

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

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 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;

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Florence, Italy

Alessandro Giolitti