Farmitalia Carlo Erba

Societa' Farmaceutici Italia

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

Farmitalia Carlo Erba S.r.l.

Other

Bristol-Myers Squibb

Consiglio Nazionale Delle Ricerche

Istituto Luso Farmaco D'italia

Malesci Istituto Farmacobiologico S.p.a.

A. Menarini Industrie Farmaceutiche Riunite

Bristol-Meyers Squibb

Societa Farmaceutici Italia (Farmitalia Carlo Erba S.p.a.)

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

A. Menarini Industrie Farmaceutice Reunite S.r.l.

Federico Maria Arcamone

Sergio Penco

Luigi Bernardi

Antonino Suarato

Francesco Angelucci

Aurelio Di Marco

Giuseppe Cassinelli

Paolo Lombardi

Paolo Masi

Giovanni Franceschi

Maurizio Foglio

Bianca Patelli

Alberto Bargiotti

Nicola Mongelli

Fabio Animati

Alessandro Sisto

Stefano Manzini

Pietro Giardino

Ettore Lazzari

Cosimo Scarafile

Edoardo Potier

Ermes Vanotti

Giuseppe Giannini

Aurora Sanfilippo

Giuliano Franchi

Maria A Verini

Christopher Fincham

Fausto Gozzi

Annamaria Casazza

Michele Caruso

Franco Zarini

Giorgio Palamidessi

Anna M Casazza

Aurelio DIMarco

Carlo Alberto Maggi

Vittorio Pestellini

Carlo Battistini

Daniela Ruggieri

Danilo Giannotti

Giuseppe Cascio

Maria Altamura

Ugo Scarponi

Cristina Rossi

Laura Quartara

Enzo Perrotta

Edith Monteagudo

Piero Sbraci

Massimo Luigi Capobianco

Stefania Zanella

Gianfranco Cainelli

Stefania Bonazzi

Aurelia Di Marco

Anna Maria Garbesi

Giovanna Schioppacassi

Gian P Vicario

Antonio Suarato

Rosanna Mazzoleni

Giueseppe Cassinelli

Oligonucleotide-anthracycline and oligonucleotide-anthracyclinone

This invention relates to novel compounds of general formula (I): ##STR1## and to pharmaceutical compositions containing them.

Bicyclic tachykinins antagonists, preparation thereof and their use in

The present invention refers to tachykinins antagonists of general formula (I) ##STR1## their preparation and pharmaceutical compositions containing them.

Tachykinins antagonists

S-fluoro-anthracyclines, processes for their preparation and

New 8-fluoroanthracycline derivatives of formula I possessing antitumoral properties are described, together with their preparation and pharmaceutical compositions containing them.

3'-Deamino-4'-deoxy-4'-amino-8-fluoroanthracyclines

A description is given of tachykinin receptor antagonists having general formula (I) ##STR1## their preparation and use in pharmaceutical formulations.

Tachykinin antagonists

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

Distamycin a derivatives as anti-malarial agents

Tachyquinine antagonists, their preparation and use in pharmaceutical

This invention relates to polyaminopyrrolecarboxyamide derivatives of general formula (I) and their pharmaceutically acceptable salts, in which A represents a chemical bond or an aromatic or heteroaromatic radical, and: if A is a chemical bond, R is hydrogen, alkyl, dialkylaminoalkyl, alkenyl, cycloalkyl, arylalkyl, arylalkenyl, haloalkyl, or an aromatic or heteroaromatic radical; whereas if A is an aromatic or heteroaromatic radical, R is nitro, amino or formylamino; n is 0 or a whole number between 1 and 4; Z is an alkylene or aromatic radical. ##STR1##

Poly 4-aminopyrrole-2-carboxyamide derivatives, and pharmaceutical

The invention relates to distamycin A analogs of the following formula ##STR1## wherein n is 2, 3 or 4; A is an optionally substituted divalent radical chosen from ##STR2## and --Het-- wherein Het is a pentatomic or hexatomic heteromonocyclic ring, except pyrrole; and wherein either one of R.sub.1 and R.sub.2 is hydrogen and the other is an acylating moiety or R.sub.1 and R.sub.2 are both hydrogen or both alkyl groups optionally substituted, including the pharmaceutically acceptable salts of the said compounds. The compounds of the invention can be useful antitumor and antiviral agents.

Site specific alkylating agents

Anthracycline glycosides useful as antitumor agents of formula XV: ##STR1## wherein R.sub.1 represents a hydrogen atom or a hydroxy group, one of R.sub.2 and R.sub.3 represents a hydrogen atom, the other of R.sub.2 and R.sub.3 represents a hydrogen atom or a hydroxy group and X is a hydrogen atom or a trifluoro acetyl group.

6-deoxyanthracyclines

The invention relates to distamycin A analogs of the following formula ##STR1## wherein n is 2, 3 or 4; A is an optionally substituted divalent radical chosen from ##STR2## and -Het- wherein Het is a pentatomic or hexatomic heteromonocyclic ring, except pyrrole; and wherein either one of R.sub.1 and R.sub.2 is hydrogen and the other is an acylating moiety or R.sub.1 and R.sub.2 are both hydrogen or both alkyl groups optionally substituted, including the pharmaceutically acceptable salts of the said compounds. The compounds of the invention can be useful antitumor and antiviral agents.

A compound of the formula ##STR1## wherein R.sub.1 represents a hydrogen atom or a hydroxy group, one of R.sub.2 and R.sub.3 represents a hydrogen atom, the other of R.sub.2 and R.sub.3 represents a hydrogen atom or a hydroxy group and X is a hydrogen atom or a trifluoro acetyl group. The N-trifluoroacetyl 7S:9S and 7R:9R derivatives of the .alpha.-glycosides of formula XV can be separated by chromatography on silica gel to obtain, after mild alkaline hydrolysis the wanted 7S:9S .alpha.-glycosides (R.sub.1 =H) as free bases and can eventually be transformed into their corresponding doxorubicin derivatives (R.sub.1 =OH) by known procedures.

Growing community of inventors

Nerviano, Italy

Federico Maria Arcamone