Pharmacia & Upjohn S.p.a.

Farmitalia Carlo Erba

Farmitalia Carlo Erba S.p.a.

Farmitalia Carlo Erba S.r.l.

Nerviano Medical Sciences S.r.l.

Carlo Battistini

Sergio Vioglio

Giovanni Franceschi

Dario Ballinari

Antonella Ermoli

Domenico Ungheri

Franco Buzzetti

Maurizio Foglio

Marina Ciomei

Antonio Guerriero

Michele D'Ambrosio

Francesco Pietra

Federico Maria Arcamone

Sergio Penco

Maria Gabriella Brasca

Marco Alpegiani

Angelo Bedeschi

Paolo Carminati

Ermes Vanotti

Giuseppe Cassinelli

Franco Zarini

Matteo D'Anello

Alberto Bardelli

Paolo Comoglio

Cosimo Scarafile

Patrizia Giordano

Maria Gioia Fornaretto

Maria A Verini

Silvia Fustinoni

Luisa Garofano

Fabio Corradi

Roberto Bianchini

Pierluigi Griggi

Guy Mazue

Rosanna Mazzoleni

Sabrina De Rosa

Stefano Del Nero

Matteo D'anello

The present invention relates to a process for the preparation of 5-(2-amino-pyrimidin-4-yl)-2-aryl-1H-pyrrole-3-carboxamides and to the useful intermediate compounds of such process. 5-(2-Amino-pyrimidin-4-yl)-2-aryl-1H-pyrrole-3-carboxamides are described and claimed in WO2007110344, which also discloses processes for their preparation. These compounds can be advantageously prepared through a process which allows to obtain the desired products in high yields and purity and with a limited number of steps. The synthesis is starting from a cyano pyrrole derivative, and is characterized from the final hydrolysis of 5-(2-amino-pyrimidin-4-yl)-2-aryl-1H-pyrrole-3-carbonitrile. The compounds prepared according to the process of the present invention are endowed with protein kinase inhibiting activity and, more particularly, Cdc7 or Cdc7/Cdks inhibiting activity. The compounds are therefore useful in the treatment of a variety of cancers, cell proliferative disorders and diseases associated with protein kinases.

Process for the preparation of 5-(2-amino-pyrimidin-4-yl)-2-aryl-1H-pyrrole-3-carboxamides

The present invention relates to peptides and peptidomimetic compounds and pharmaceutical compositions containing them as useful pharmacological agents in the control or treatment of proliferative diseases such as cancer, against tumor growing and/or tumoral metastasis, and psoriasis and in the control or treatment of inflammatory, allergic, autoimmune, viral, and cardiovascular diseases. These new compounds have the unique property to inhibit the recognition of several phosphotyrosine containing motifs within all the cellular receptors and cytosolic transducers by a wide spectrum of SH2 domains contained in cytosolic transducers and other effector proteins laying along different pathways of the signal transduction process and with a particularly high affinity for the SH2 domain of the adaptor transducer Grb2, a key element along the pathway to mitogenesis and motogenesis, this last activity leading to invasiveness and to metastasis. The invention also relates to methods for production of the compounds and methods of treatment employing the compounds.

Peptide antagonists of cellular mitogenesis and motogenesis and their therapeutic use

Substituted tetralymethylen-Oxindoles analogues as tyrosine kinase

The present invention relates to terpenoidic derivatives, known in the art as Sarcodictyins, for use as therapeutic agents, and to pharmaceutical compositions containing them. In particular, Sarcodictyins can be useful as therapeutic antineoplastic agents in the treatment of cancers in human or animal beings.

Terpenoidic derivatives useful as antitumor agents

Substituted quinolymethylen-oxindole analogues as tyrosine kinase

Substituted indolylmethylene-oxindole analogues as tyrosine kinase

There are provided compounds of formula (I) ##STR1## wherein each group B is, independently, a naturally occurring or modified heterocyclic base linked through a nitrogen or a carbon atom of the ring to the sugar moiety;

Cyclic dinucleoside diphosphorothioates, related compounds and

The present invention relates to the use as antivirals of compounds of formula: ##STR1## wherein B is a purinic or pyrimidinic heterocycle; X is oxygen or sulphur; R.sup.1 is a hydroxyl group or a hydrogen atom; R.sup.2 is a linear, branched or cyclic, alkyl group of up to twenty carbon atoms; R.sup.3 is as specified for R.sup.2 above or a hydrogen atom, a cation or a polyhydroxy group.

5'-alkylphosphonylnucleosides as antivirals

A crystalline form of (5R,6S)-2-carbamoyloxymethyl-6-[(1R)-hydroxyethyl]-2-penem-3-carboxylic acid incorporates two molecules of water per molecule of the acid and is useful as an antibacterial agent.

Crystalline

A pharmaceutcial composition is provided for use in the prevention or treatment of viral infections caused by enveloped viruses. The composition comprises a fibroblast growth factor, a sulfated polysaccharide with antiviral activity, and one or more pharmaceutically acceptable carriers. The fibroblast growth factor may be a basic fibroblast growth factor or an analogue thereof, and the polysaccharide may be a carrageenan, heparin, dextran sulfate, pentosan polysulfate or a sulfated polysaccharides produced by marine algae belonging to the class of Rhodophyceae.

Synergistic composition comprising a fibroblast growth factor and a

A process for preparing 2-methyl substituted penems useful as antibiotics agent and/or as intermediates thereof, by reacting an appropriate 1-imido-3,4-disubstituted azetidinone derivative with a trivalent organophosphorus compound in an inert solvent at a temperature of from 110.degree. to 150.degree. C. for a period of from 2 hours to a few days.

Process for the preparation of penems

Processes for the preparation of a penem derivative of formula I ##STR1## wherein n=0 or 1; R is a carboxy protecting group or H;

Process for preparing optically active penems

Compounds are disclosed of the formula ##STR1## wherein R.sub.1 represents a hydrogen or chlorine atom, as well as intermediates. These include 4'-deoxy-paromomycin; 4'-deoxy-4'-epi-chloro-paromomycin; 4'-deoxy-4'-epi-chloro-penta-N-benzyloxycarbonylparomomycin; 4'-deoxy-penta-N-benzyloxycarbonylparomomycin; 6,3',2',5',3'',4''-hexa-O-acetyl-6'-O-benzoyl-4'-deoxy-penta-N-benzyloxyca rbonylparomomycin; 6,3',2',5',3'',4''-hexa-O-acetyl-6'-O-benzoyl-4'-epi-chloro-4'-deoxy-penta -N-benzyloxycarbonylparomomycin; 6,3',2',5',3'',4''-hexa-O-acetyl-6'-O-benzyl-penta-N-benzyloxycarbonylparo momycin; 6,3',2',5',3'',4''-hexa-O-acetyl-6'-O-benzoyl-4'-O-[(methylthio)-thiocarbo nyl]-penta-N-benzyloxycarbonylparomomycin; and 6,3',2',5',3'',4''-hexa-O-acetyl-6'-O-benzoyl-4'-O-[(phenylthio)-thiocarbo nyl]-penta-N-benzyloxycarbonylparomomycin. The compounds illustrated by the structural formula are useful in treating amoebic dysentery in man and animals.

Paromomycin containing compounds and method of use

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Novate Milanese, Italy

Carlo Battistini