Nerviano Medical Sciences S.r.l.

Pharmacia & Upjohn S.p.a.

Pharmacia Italia S.p.a.

Jurgen Moll

Mario Varasi

Tiziano Bandiera

Daniele Fancelli

Maria Menichincheri

Paola Vianello

Dario Ballinari

Maurizio Pulici

Francesca Quartieri

Mauro Angiolini

Barbara Forte

Antonella Isacchi

Michele Modugno

Arturo Galvani

Rosita Lupi

Domenico Fusar Bassini

Luisa Rusconi

Chiara Soncini

Mats Dahlberg

Tizizno Bandiera

Luisella Bonomini

Markus Gude

Jean-Yves Trosset

Fabrina Bologna

There are provided thieno[2,3-c]pyrazole derivatives of formula (I), wherein A is an aryl or heteroaryl ring, on which the substituent-NHZRis at the ortho position to the CONH linker; Rand Rare the same or different and, independently from each other, represent a hydrogen atom or an organic group; Ris a hydrogen or halogen atom or an organic group; Z is direct bond, &#x3e;C&#x2550;O, or &#x2014;C(&#x2550;O)NH&#x2014;; Ris hydrogen or an organic group; or isomers, tautomers, carriers, metabolites, prodrugs, and pharamaceutically acceptable salts thereof. A process for their preparation and pharamaceutical compositions comprising them are also disclosed; the compounds of the invention may be useful, in theraphy, in the treatment of diseases associated with a disregulated protein kinase activity, like cancer.

1H-thieno[2,3-c]pyrazole compounds useful as kinase inhibitors

The invention provides low molecular weight compounds, namely 1H-thieno[2,3-c]pyrazoles, showing a high affinity for the ATP pocket of ABL tyrosine kinase. These compounds are thus ATP-competitive tyrosine kinase inhibitors displaying a significant inhibitory potency also, and in particular, towards BCR-ABL inhibitor-resistant T315I ABL mutants. The compounds of the invention find a useful application in the treatment of BCR-ABL inhibitor-resistant ABL-mediated diseases, such as Imatinib-resistant chronic myelogenous leukemia. Moreover, the invention provides a screening method for the identification of compounds capable of binding the ATP pocket of a kinase protein, in particular of the T315I mutant ABL kinase.

Use of a kinase inhibitor for the treatment of particular resistant tumors

The invention provides pyrido[2,3-d]pyrimidin-7(8H)-one telomerase inhibitors of the formulawhere R1, R2 are as defined herein. The invention also provides methods for preparing the compounds of formula I, methods of using the compounds to treat diseases such as cancer, and pharmaceutical compositions comprising the compounds.

Pyridopyrimidinones derivatives as telomerase inhibitors

The present invention provides a human polypeptide homolog of P-activated kinase (PAK) polynucleotides which identify and encode PAKserine/threonine kinase. In addition, the invention provides expression vectors, host cells and methods for its production. The invention also provides methods for the identification of PAKagonists/antagonists, useful for the treatment of human diseases and conditions.

Human p21-activated kinase 5 polypeptide

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Appiano Gentile, Italy

Jurgen Moll