Nerviano Medical Sciences S.r.l.

Les Laboratoires Servier

Helena Posteri

Maria Gabriella Brasca

Michele Caruso

Italo Beria

Ron Ferguson

Gianluca Mariano Enrico Papeo

Paolo Orsini

Alessandra Scolaro

Fabio Zuccotto

Marina Caldarelli

Barbara Forte

Giovanni Cervi

Elena Casale

Jay Aaron Bertrand

Mikhail Yurievitch Krasavin

Barbara Valsasina

Alessia Montagnoli

Rosita Lupi

Sergio Mantegani

Francesco Casuscelli

Matteo Salsa

Mauro Angiolini

Teresa Disingrini

Stefano Nuvoloni

Alexander Khvat

Walter Ceccarelli

Marco Silvagni

Alina Anatolievna Busel

Daniela Borghi

Riccardo Colombo

Gabriele Fachin

Carlo Visco

Gianluca Mariano Papeo

There are provided 3-oxo-2,3-dihydro-1H-indazole-4-carboxamide derivatives which selectively inhibit the activity of poly (ADP-ribose) polymerase PARP-1 with respect to poly (ADP-ribose) polymerase PARP-2. The compounds of this invention are therefore useful in treating diseases such as cancer, cardiovascular diseases, central nervous system injury and different forms of inflammation. 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.

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There are provided substituted isoquinolin-1(2H)-one derivatives which selectively inhibit the activity of poly (ADP-ribose) polymerase PARP-1 with respect to poly (ADP-ribose) polymerase PARP-2. The compounds of the present invention are therefore useful in treating diseases such as cancer, cardiovascular diseases, central nervous system injury and different forms of inflammation. 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. A screening method for the identification of compounds capable of binding several PARP proteins, as well the probes used in such method, are further objects of the invention.

Isoquinolin-1(2H)-one derivatives as PARP-1 inhibitors

The present invention relates to pyrazolo-quinazolines, characterized by an ortho-substituted-arylamino, heterocyclylamino- or C-Ccycloalkylamino residue at 8 position and an aryl, heterocyclyl or C-Ccycloalkyl as substituent of a carboxamide at 3 position of the molecule framework. The compounds of this invention modulate the activity of protein kinases and are therefore useful in treating diseases caused by dysregulated protein kinase activity, in particular MPS1/TTK. 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.

Pyrazolo-quinazolines

There are provided substituted 3-oxo-2,3-dihydro-1H-isoindole-4-carboxamide derivatives (I) which selectively inhibit the activity of poly (ADP-ribose) polymerase PARP-1 with respect to poly (ADP-ribose) polymerase PARP-2. The compounds of this invention are therefore useful in treating diseases such as cancer, cardiovascular diseases, central nervous system injury and different forms of inflammation. 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. 

Substituted pyrrolo-pyrazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification, 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 dysregulated protein kinase activity, like cancer.

Substituted pyrrolo-pyrazole derivatives as kinase inhibitors

Pyrazolo-quinazoline 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 pyrazolo-quinazoline derivatives, process for their preparation and their use as kinase inhibitors

Dihydropteridin-6-one 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 dihydropteridin-6-one derivatives, process for their preparation and their use as kinase inhibitors

Isoquinolin-1 (2H)-one derivatives as PARP-1 inhibitors

Substituted pyrrolo-pyrimidine derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification, 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 dysregulated protein kinase activity, like cancer. 

Substituted pyrrolo-pyrimidine derivatives, process for their preparation and their use as kinase inhibitors

Bicyclic pyrazole and isoxazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification, 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 mediated by HSP90 protein, like cancer and neurodegenerative disorders.

Bicyclic pyrazole and isoxazole derivatives as antitumor and antineurodegenerative agents

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Travedona Monate, Italy

Helena Posteri