Nerviano Medical Sciences S.r.l.

Danilo Mirizzi

Francesco Casuscelli

Matteo D'Anello

Gianluca Mariano Enrico Papeo

Ron Ferguson

Giovanni Cervi

Maria Gabriella Brasca

Tiziano Bandiera

Marcella Nesi

Achille Panzeri

Marina Caldarelli

Francesca Quartieri

Sten Christian Orrenius

Daniele Donati

Jay Aaron Bertrand

Paola Gnocchi

Paolo Trifiro'

Marco Silvagni

Paolo Trifirò

Matteo D'anello

The present invention relates to substituted pyrimidinyl-pyrrole compounds of formula (I) which modulate the activity of protein kinases and are therefore useful in treating diseases caused by dysregulated protein kinase activity, in particular Janus kinases. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing such compounds or the pharmaceutical compositions containing them. 

Substituted pyrimidinyl-pyrroles active as kinase inhibitors

Compounds which are 4,7-disubstituted derivatives of 3,4-dihydro-2H-pyrrolo[1,2-a]pyrazin-1-one compounds, or pharmaceutically acceptable salts thereof, their preparation process and pharmaceutical compositions comprising them are disclosed; these compounds are useful in the treatment of diseases caused by and/or associated with an altered protein kinase activity such as cancer, viral infection, prevention of AIDS development in HIV-infected individuals, cell proliferative disorders, autoimmune and neurodegenerative disorders; also disclosed is a process under Solid Phase Synthesis conditions for preparing the compounds of the invention and chemical libraries comprising a plurality of them.

Substituted 3,4-dihydro-2H-pyrrolo[1,2-a]pyrazin-1-ones as modulators of protein kinase activity

New substituted tricyclic compounds of formula (I) are described, wherein R1, R2, X, Y, Z are herein defined, having protein kinase inhibiting activity. The invention includes methods to prepare the compounds of formula (I), pharmaceutical compositions containing them, and their use in therapy, in particular for the treatment of diseases caused by and/or associated with dysregulated activity of protein kinase. 

Tricyclic derivatives, process for their preparation and their use as kinase inhibitors

There are provided 3,5-disubstituted derivatives of 6,7-dihydroimidazo[1,5-a]pyrazin-8(5H)-one compounds of formula (I) or a pharmaceutically acceptable salt thereof as defined in the present specification, which modulate the activity of protein kinases. The compounds are therefore useful in treating diseases caused by dysregulated protein kinase activity. In particular, such diseases to be treated with a compound of formula (I) of the present invention is one caused by and/or associated with disregulated protein kinase activity selected from the group consisting of cancer, viral infection, prevention of AIDS development in HIV-infected individuals, cell proliferative disorders, autoimmune and neurodegenerative disorders. The present invention also relates to processes for preparing the compounds of formula (I), combinatorial libraries thereof, pharmaceutical compositions comprising them, and methods of treating diseases utilizing pharmaceutical compositions comprising a compound of formula (I). 

6,7-dihydroimidazo[1,5-a]pyrazin-8(5H)-one derivatives as protein kinase modulators

Compounds which are 4,7-disubstituted derivatives of 3,4-dihydro-2H-pyrrolo[1,2-a]pyrazin-1-one compounds with the formula or pharmaceutically acceptable salts thereof, their preparation process and pharmaceutical compositions comprising them are disclosed; these compounds are useful in the treatment of diseases caused by and/or associated with an altered protein kinase activity such as cancer, viral infection, prevention of AIDS development in HIV-infected individuals, cell proliferative disorders, autoimmune and neurodegenerative disorders; also disclosed is a process under Solid Phase Synthesis conditions for preparing the compounds of the invention and chemical libraries comprising a plurality of them.

3,4-dihydro-2H-pyrrolo[1,2-a]pyrazin-1-one derivatives for the modulation of the activity of protein kinases

Growing community of inventors

Milan, Italy

Danilo Mirizzi