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

Patrizia Minetti

Maria Ornella Tinti

Mauro Marzi

Fabio Giannessi

Francesco De Angelis

Arduino Arduini

Piero Chiodi

Maria Assunta Di Cesare

Piero Foresta

Giorgio Tarzia

Vito Nacci

Giuseppe Campiani

Sergio Penco

Walter Cabri

Claudio Pisano

Paolo Carminati

Giuseppe Giannini

Orlando Ghirardi

Gian Piero Moretti

Domenico Mastroianni

Gilberto Spadoni

Enrico Garattini

Domenico Mastrojanno

Assunta Di Cesare

Giovanni Piersanti

Fabio Giannesi

The present invention relates to new triazolyl purine derivatives of formula (I), processes for their preparation, and to pharmaceutical compositions containing them for the treatment of neurological disorders or cerebral ischaemia for which inhibition of adenosine A2A receptor will result at improving the health state of a patient.

Oxidated derivatives of triazolylpurines useful as ligands of the adenosine A2A receptor and their use as medicaments

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 having reversible inhibiting activity of carnitine palmitoyl-transferase

Compounds of formula (I)wherein the groups are as defined in the description are disclosed. The compounds of formula (I) are endowed with reversible inhibiting activity of carnitine palmitoyl-transferase and are useful in the preparation of medicaments useful in the pathologies related to a hyperactivity of carnitine palmitoyl-transferase, such as hyperglycemia, diabetes and pathologies related thereto, heart failure, ischemia.

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]

Bis-heterocyclic compounds of general formula (I) are described which are useful as antitumour and cheomsensitising agents.

Bis-heterocyclic compounds with antitumour and chemosensitising activity

A process is described for the preparation of compounds with the following formula where the groups are as defined below; in particular, Ris a substituted amine; said process includes essentially the reaction of pyrrolobenzothiazepin-9-one with amine RH to give the corresponding enamine, which is subsequently transformed into the final compound 

Process for the preparation of 9-amino substituted 9,10-dihydropyrrolo[2,1-b][1,3]benzotiazepines

Pyrrolo&lsqb;2,1-B&rsqb;&lsqb;3,1&rsqb; benzothiazepines and their use for the preparation of medicaments with antipsychotic activity

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

Ipoxantine derivatives of general formula (I): ##STR1## both as racemate and chiral forms and the salts thereof with pharmacologically acceptable cations, wherein n is an integer comprised between 2 and 6, and A is the residue of a dipeptide, tripeptide, tetrapeptide and pentapeptide selected, respectively, from the groups consisting of:

Oligopeptide derivatives of ipoxantine endowed with immunomodulating

The present invention concerns aminoacyl and oligopeptidyl derivatives of allopurinol (1,5-dihydro-4H-pyrazolo-[3,4-d]-pyrimidin-4-one) of general formula (I), and related salts with ##STR1## pharmacologically-acceptable cations, in which n is an integer between 2 and 6, preferably 5, Y is H or CO--A, in which A is a racemic or chiral amino acid, dipeptide, tripeptide, tetrapeptide, or pentapeptide chosen, respectively, from the groups consisting of:

Aminoacyl and oligopeptidyl derivatives of allopurinol exhibiting

Growing community of inventors

Rome, Italy

Patrizia Minetti