公开(公告)号：EP2051981B1

公开(公告)日：2010-08-25

申请号：EP07729539.2

申请日：2007-05-25

申请人： NERVIANO MEDICAL SCIENCES S.R.L.

发明人： FANCELLI, Daniele ,  PULICI, Maurizio ,  MOLL, Jurgen ,  BANDIERA, Tiziano

IPC分类号： C07D491/04 ,  A61K31/4162 ,  A61P35/00

CPC分类号： C07D491/048

摘要： Furo[3,2-c]pyrazole derivatives of formula (I) as defined in the description, and pharmaceutically acceptable salts thereof, wherein A is an aryl or heteroaryl ring, - NHZR5 is at the ortho position to the CONH linker; - R1 and R2 are the same or different and, independently from each other, represent a hydrogen atom, or an organic residue; R3 is a hydrogen or halogen atom or an organic group; R4 is a hydrogen or halogen atom or an organic group; Z is direct bond, >C=O, or -C(=O)NH-; - R5 is hydrogen or an optionally substituted organic group or isomers, tautomers, carriers, metabolites, prodrugs, and pharmaceutically acceptable salts thereof. A 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, in particular Aurora kinases activity or IGF-1R activity, like cancer.

公开(公告)号：EP2007380A2

公开(公告)日：2008-12-31

申请号：EP07727485.0

申请日：2007-03-29

申请人： Nerviano Medical Sciences S.r.l.

发明人： FANCELLI, Daniele ,  ISACCHI, Antonella ,  MODUGNO, Michele ,  MOLL, Jurgen ,  RUSCONI, Luisa ,  SONCINI, Chiara ,  LUPI, Rosita

IPC分类号： A61K31/4162 ,  A61K31/44 ,  A61P35/02

CPC分类号： A61K31/4162 ,  A61K31/44

摘要： 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.

公开(公告)号：EP1999131A2

公开(公告)日：2008-12-10

申请号：EP07726618.7

申请日：2007-03-02

申请人： Nerviano Medical Sciences S.r.l.

发明人： BANDIERA, Tiziano ,  BERTRAND, Jay Aaron ,  PEVARELLO, Paolo ,  PERRONE, Ettore ,  LOMBARDI BORGIA, Andrea ,  ORRENIUS, Sten Christian ,  ANGIOLINI, Mauro ,  FANCELLI, Daniele

IPC分类号： C07D487/04 ,  A61K31/4162 ,  A61P35/00

CPC分类号： C07D487/04 ,  A61K31/4162 ,  A61K31/496 ,  A61K31/5377

摘要： A compound having formula (I): wherein: R, A, R1 and R2, are as defined in the specification, and pharmaceutical formulas thereof, and methods of use thereof, as Kinase inhibitors.