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

Menarini Ricerche S.p.a.

Cristina Rossi

Carlo Alberto Maggi

Alessandro Giolitti

Laura Quartara

Christopher Ingo Fincham

Patrizia Felicetti

Rosa Terracciano

Federico Calvani

Fernando Catrambone

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

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Pomezia, Italy

Cristina Rossi