Nerviano Medical Sciences S.r.l.

Pharmacia & Upjohn S.p.a.

Paola Gnocchi

Marcella Nesi

Maria Gabriella Brasca

Achille Panzeri

Jay Aaron Bertrand

Tiziano Bandiera

Francesco Colotta

Paola Vianello

Francesca Quartieri

Mario Ferrari

Anna Maria Isetta

Sten Christian Orrenius

Elena Casale

Ilaria Motto

Maria C Fornasiero

Danilo Mirizzi

Federico Riccardi Sirtori

Roberto D&prime;Alessio

Emiliana Corti

Emliana Corti

There are provided substituted purine and 3-deazapurine analogues, 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.

Purine and 3-deazapurine analogues as choline kinase inhibitors

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

The present invention relates to alkynyl substituted pyrimidinyl-pyrrole compounds which modulate the activity of protein kinases and are therefore useful in treating diseases caused by dysregulated protein kinase activity, in particular Jak and/or Src family 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.

Alkynyl substituted pyrimidinyl-pyrroles active as kinases inhibitors

A product containing: (a) an immunosuppressant agent (A) and (b) at least one immunosuppressant 2,2&prime;-bi-1H-pyrrole compound (B) having formula (I) wherein R,is hydrogen, phenyl, C,-C,alkyl or C,-C,alkenyl, wherein the alkyl and alkenyl groups are unsubstituted or substituted by 1 to 3 substituents, which are the same or different, chosen independently from halogen, C,-C,alkoxy, hydroxy, aryl and aryloxy; R,is hydrogen, C,-C,alkyl, cyano, carboxy or (C,-C,alkoxy)carbonyl; R,is halogen, hydroxy or C,-C,alkoxy unsubstitued or substituted by phenyl; R,is hydrogen, C,-C,alkyl or phenyl; each of R,and R,, which are the same or different, is independently hydrogen, C,-C,alkanoyl, C,-C,alkenoyl, phenyl, C,-C,alkyl or C,-C,alkenyl; or two of R,, R,and R,, taken together, form a C,-C,polymethylene chain, which is unsubstituted or substituted by a C,-C,alkyl, by a C,-C,alkenyl or by a C,-C,alkylidene group; or a pharmaceutically acceptable salt thereof; as a combined preparation for simultaneous, separate or sequential use in immunosuppressant therapy, said preparation having a potentiated immunosuppressive activity with respect to products containing either the immunosuppressive agent (A) or the 2,2&prime;-bi-1H-pyrrole immunosuppressive compound (B).

Synergistic immunosuppressant composition containing a 2,2'-bi-1H-pyrrole compound

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Stresa, Italy

Paola Gnocchi