Farmitalia Carlo Erba S.r.l.

Farmitalia Carlo Erba

Pharmacia & Upjohn

Pharmacia Corporation

Carlo Erba

Pharmacia Italia S.p.a.

Pfizer Italia S.r.l.

Nerviano Medical Sciences S.r.l.

Nicola Mongelli

Giovanni Biasoli

Marina Ciomei

Enrico Pesenti

Federico Maria Arcamone

Antonino Suarato

Sergio Penco

Francesco Angelucci

Maria Grandi

Paolo Cozzi

Maria Menichincheri

Ermes Vanotti

Laura Capolongo

Ettore Lazzari

Maria A Verini

Alfredo Paio

Italo Beria

Andrea Lombardi Borgia

Alberto Bargiotti

Domenico Fusar Bassini

Walter Ceccarelli

Piero Melloni

Michele Caruso

Pier Giovanni Baraldi

Carmelo Gandolfi

Angelo Bedeschi

Gabriella Traquandi

Ilaria Candiani

Francesco Colotta

Anna Vulpetti

Alessandro Rossi

Francesco Lauria

Antonio Pillan

Francesco Casuscelli

Fabrizio Orzi

Angelo Crugnola

Maria Cristina Geroni

Pier P Lovisolo

Daniela Faiardi

Elena Casale

Raffaele Tommasini

Fabio Animati

Claudia Piutti

Claudio Dalvit

Maria Chiara Fagnola

Mariangela Mariani

Giuseppina Visentin

Cristina Geroni

Elena Ardini

Cesare Gennari

Gabriella Pezzoni

Rachele Alzani

Maria Bergamaschi

Maria Magdalena Flocco

Gianpaolo Fogliatto

Massimo Temponi

Elena Cozzi

Marina Veronesi

Francesco Sola

Nuccia Oneto

Patrizia Banfi

High-Throughput Screening (HTS) of large compound libraries is the method of drug-lead discovery. It is now well accepted that for a functional assay, quality is more important than quantity. A biochemical NMR method originally proposed by Percival and Withers (Biochemistry, 1992, 31, 498&#x2013;505) is extended to the screening of Ser/Thr kinases. The method requires the presence of a CF(or CF) moiety on the substrate and utilizesF NMR spectroscopy for the detection of the starting and enzymatically modified substrates. Experiments can be performed in real time or in an endpoint assay format using protein and substrate concentrations comparable to the ones used by other HTS techniques. Application of this technique to the phosphorylation of a substrate by the protein Ser/Thr kinase AKT1 is presented.

Fluorine NMR spectroscopy for biochemical screening

A process for preparing distamycin derivatives possessing antitumor activity, by starting from distamycin A itself, is described. The process involves the preparation of the novel intermediates of formula (III)

Process for preparing distamycin derivatives

Taxane derivatives modified at 13-position of the taxane derivative skeleton (taxol numbering) of formula (I), wherein R, R.sub.a, R.sub.b, R.sub.c, R.sub.1, R.sub.2, R.sub.3 are appropriate organic residues can be antitumor agents.

Taxane derivatives

Biologically active oreido derivatives useful in the treatment of

Combinatorial solid phase synthesis of a library of indole derivatives

Method for the preparation of taxol and its derivatives

Distamycin A analogues as antitumour or antiviral agents

A polymer conjugate consisting essentially of: from 90 to 99.9 mol % of units represented by the formula ##STR1## from 0.1 to 5 mol % of units represented by the formula ##STR2## wherein one of R.sub.1 and R.sub.2 is a copolymer residue of the formula ##STR3## and the other one is hydrogen atom; from 0 to 9.9 mol % of units represented by the formula ##STR4##

Polymer-bound paclitaxel derivatives

Ureido derivatives of naphthalenephosphonic acids

The invention relates to naphthalenesulfonic-pyrrolecarboxamido compounds of formula ##STR1## wherein n is zero or an integer of 1 to 3; R is a sulfonic acid residue; m is an integer of 1 to 3, or a pharmaceutically acceptable salt thereof, which are active as antiviral agents, in particular against Human Immunodeficiency Virus

Therapeutically active naphthalenesulfonic pyrrolecarboxamido derivatives

The invention relates to ureido derivatives of substituted pyrroles of formula ##STR1## wherein each of m and n, being the same, is an integer of 1 to 3; W is oxygen of sulphur;

New ureido derivatives of poly-4-amino-2-carboxy-1-methyl compounds

A polymer conjugate consisting essentially of: from 90 to 99.9 mol % of units represented by the formula ##STR1## from 0.1 to 5 mol % of units represented by the formula ##STR2## wherein one of R.sub.1 and R.sub.2 is a copolymer residue of the formula ##STR3## and the other one is hydrogen atom; from 0 to 9.9 mol % of units represented by the formula ##STR4## wherein R is a phenyl or t-butoxy group, R.sub.3 is H or an acetyl group, A and A.sub.1 which may be the same or different, represent a chemical single bond, an amino acid residue or peptide spacer selected from .beta. Ala, Gly, Phe-Gly, Phe-Phe-, Leu-Gly, Val-Ala, Phe-Ala, Leu-Phe, Leu-Ala, Phe-Leu-Gly, Phe-Phe-Leu, Leu-Leu-Gly, Phe-Tyr-Ala, Phe-Gly-Phe, Phe-Phe-Gly, Phe-Leu-Gly-Phe, Gly-Phe-Leu-Gly-Phe,Gly-.beta.Ala, Phe-Gly-.beta.Ala, Phe-Phe-.beta.Ala, Leu-Gly-.beta.Ala, Val-Ala-.beta.Ala, Phe-Ala-.beta.Ala, Leu-Phe-.beta.Ala, Leu-Gly-.beta.Ala, Phe-Leu-Gly-.beta.Ala, Phe-Phe-Leu .beta.Ala, Leu-Leu-Gly-.beta.Ala, Phe-Tyr-Ala-.beta.Ala, Phe-Gly-Phe-.beta., Phe-Phe-Gly .beta.Ala, Phe-Leu-Gly-Phe-.beta.Ala or Gly-Phe-Leu-Gly-Phe-.beta.Ala. The compounds are endowed with antitumor activity and show improved water solubility and decreased toxicity in comparison with paclitaxel or its known analogs. A method for their preparation and pharmaceutical compositions containing them are also described.

The invention relates to the use of compounds of formula (I) ##STR1## wherein each of m and n, being the same, is an integer of 1 to 3; and each of the R groups, which are the same, is a naphthyl group substituted by 1 to 3 sulfonic groups,or pharmaceutically acceptable salts thereof, in the preparation of a medicament for use in preventing and/or treating the metastatic spread of tumors.

Biologically active ureido derivatives useful as anit-metastic agenst

An anthracycline glycoside of general formula 1: ##STR1## wherein R.sub.1 is hydrogen or methoxy group; R.sub.2 is hydrogen or hydroxy group, A and B both represent hydrogen or one of A and B is hydrogen and the other is hydroxy or a group of formula --OSO.sub.2 R.sub.5 in which R.sub.5 is C1-C4 alkyl or aryl optionally substituted by C1-C4 alkyl, nitro, amino, methoxy or halogen; R.sub.3 is a hydrogen atom or a group of formula 2 and R.sub.4 is a group of formula 2

Mono and bis alkylamino-anthracyclines

Growing community of inventors

Milan, Italy

Nicola Mongelli