Sigma-tau Industrie Farmaceutiche Riunite S.p.a.

Maria Assunta Di Cesare

Patrizia Minetti

Maria Ornella Tinti

Paolo Carminati

Giorgio Tarzia

Orlando Ghirardi

Vito Nacci

Giuseppe Campiani

Gilberto Spadoni

Derivatives of pyrrolo[2,1-b]benzothiazepines with formula (I) where A is CH&#x2014;CHC&#x2550;CH; R is hydrogen, halogen, C-Calkoxy, C-Calkylthio, C-Calkyl, C-Ccycloalkyl; Ris 1-peperazinyl, 1-homopiperazinyl and 1-piperidinyl; Ris hydrogen, C-Calkoxy, C-Calkylthio, C-Calkyl, CHO, CH&#x2550;NOH,CHOH. The formula (I) compounds are endowed with characteristic atypical anti-psychotic activity, and are therefore useful as medicaments, in particular for the treatment and prevention of schizophrenia, paranoid states, manic-depressive states, disorders of the affective sphere, social regression, personality regression, and hallucinations. Said compounds also present advantageous pharmacokinetic properties.

Dealkylated derivatives of pyrrolo[2,1-b]benzothiazepines with atypical antipsychotic activity

Compounds of Formula (I): (I); wherein: Rand Reither the same or different, are H or linear or branched C&#x2013;Calkyl; R=linear or branched C&#x2013;Calkyl; R=halogen, and pharmaceutically acceptable salts thereof are useful as active ingredients in the preparation of medicaments used as ligands of the 5-HTand/or 5-HTserotoninergic receptors.

[object Object]

Pyrrolo &lsqb;2,1-b&rsqb;&lsqb;1,3&rsqb;benzothiazepines with atypical antipsychotic activity

Growing community of inventors

Rome, Italy

Maria Assunta Di Cesare