Nerviano Medical Sciences S.r.l.

Alessandra Badari

Chiara Marchionni

Maurizio Pulici

Fabio Zuccotto

Gabriella Traquandi

Marina Caldarelli

Mauro Angiolini

Giovanni Cervi

Davide Carenzi

Stefano Nuvoloni

Michele Modugno

Sonia Biondaro

Marcella Nesi

Francesca Quartieri

Francesco Casuscelli

Sten Christian Orrenius

Elena Casale

Teresa Disingrini

Claudia Piutti

Paolo Trifiro'

Paolo Trifiro′

The present invention relates to substituted pyrazolo-quinazoline derivatives which modulate the activity of Choline Kinase (ChoK). The compounds of this invention are therefore useful in treating diseases caused by an altered choline metabolism, such as cancer, cell proliferative disorders, infectious diseases of different origin, immune-related disorders and neurodegenerative disorders. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing pharmaceutical compositions comprising these compounds. The compounds of this disclosure include those of formula (I): 

Substituted pyrazolo[4,3-h]quinazolines as choline kinase inhibitors

The present invention relates to 4-alkyl substituted 3,4-dihydropyrrolo[1,2-a]pyrazin-1(2H)-one derivatives, of formula (I) which modulate the activity of protein kinases and are therefore useful in treating diseases caused by dysregulated protein kinase activity. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing such these compounds or the pharmaceutical compositions containing them.

Substituted 3,4-dihydropyrrolo[1,2-a]pyrazin-1(2H)-ones as protein kinase inhibitors

Pyrimidinylpyrrolopyridinone derivatives of formula (I) as defined in the specification, and pharmaceutically acceptable salts thereof, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful, in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, like cancer.

Substituted pyrimidinylpyrrolopyridinone derivatives, process for their preparation and their use as kinase inhibitors

3,4-diarylpyrazole derivatives of formula (I) as defined in the specification, and pharmaceutically acceptable salts thereof, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful, in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, like cancer. 

3,4-diarylpyrazoles as protein kinase inhibitors

Pyrimidinylpyrrolopyridinone derivatives of formula (I) as defined in the specification, and pharmaceutically acceptable salts thereof, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful, in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, like cancer. 

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Vedano al Lambro, Italy

Alessandra Badari