Istituto Europeo Di Oncologia S.r.l.

Dac S.r.l.

Nerviano Medical Sciences S.r.l.

Ifom Fondazione Istituto Firc Di Oncologia Molecolare

Ieo - Istituto Europeo Di Oncologia S.r.l.

Ifom - Istituto Fondazione Di Oncologia Molecolare Ets

Ciro Mercurio

Mario Varasi

Paola Vianello

Anna Cappa

Florian Thaler

Luca Sartori

Saverio Minucci

Alessia Romussi

Agnese Abate

Raffaella Amici

Loris Moretti

Paolo Pevarello

Stefania Gagliardi

Giuseppe Meroni

Manuela Villa

Giacomo Carenzi

Paolo Trifiro′

Enrico Pesenti

Antonello Mai

Simona Polo

Paolo Trifiro'

Andrea Colombo

Maurizio Pasi

Maria Carmela Fulco

Sebastiano Pasqualato

Giovanni Faga'

Elena Maspero

Maria Grazia Porro

Elisa Zagarri

Sergio Valente

The present invention relates to tricyclic derivatives of formula (I), which are useful as inhibitors of HECT-domain-containing E3 ligases, in particular NEDD4. The present invention also refers to pharmaceutical compositions comprising compounds of formula (I), to their medical use and to their process of preparation.

HECT E3 ligase inhibitors and uses thereof

The present application relates to compounds of formula (I), wherein A, R, R, and Rare as defined in the specification, pharmaceutical compositions containing such compounds and to their use in therapy. 

Indole derivatives as histone demethylase inhibitors

The present invention relates to imidazole derivatives, wherein A, R, R, and Rare as defined in the specification, pharmaceutical compositions containing such compounds and to their use in therapy. 

Imidazoles as histone demethylase inhibitors

The present invention relates to imidazole derivatives of Formula (I), wherein A, R, R, and Rare as defined in the specification, pharmaceutical compositions containing such compounds and to their use in therapy. 

The present disclosure relates to cyclopropyl compounds of general formula (I), wherein R, and Rare as defined in the specification. The present application also relates to pharmaceutical compositions containing such compounds and to their use in therapy. 

Cyclopropylamine compounds as histone demethylase inhibitors

The present application relates to thienopyrrole derivatives, compounds of Formulas (I) and (Ia), wherein R, R, Rand Rare as defined in the specification, pharmaceutical compositions containing such compounds and to their use in therapy. The compounds of the application can be useful for inhibiting KDM1 and the prevention and/or treatment of cancer, infectious disease, or a disease characterized by aberration of cellular energy metabolism, e.g., obesity. 

Thienopyrroles as histone demethylase inhibitors

The present invention relates to cyclopropyl derivatives of general formula (I), wherein A, R, and Rare as defined in the specification. The present application also relates to pharmaceutical compositions containing such compounds and to their use in therapy. 

Cycloproplyamine derivatives useful as inhibitors of histone demethylases KDM1A

This invention is related to new histone deacetylase inhibitors according to the general formula (I) wherein: the dotted line is an optional additional bond; n is zero or an integer from 1 to 4; Ris hydrogen; C-Calkyl, optionally substituted by cycloalkyl, aryl or by heteroaryl; (CO)R; (SO)R; cycloalkyl; aryl; or heteroaryl; Ris C-Calkyl, optionally substituted by aryl or by heteroaryl; aryl; heteroaryl; or (CO)R; X is CH, oxygen or NR; Y is a bond, CHRor NR; Z is oxygen, CRRor C&#x2550;R; and R, R, R, R, R, R, R, Rand Rare as further defined in the specification; and pharmaceutical acceptable salts thereof. 

Spirocyclic derivatives as histone deacetylase inhibitors

This invention is related to new histone deacetylase inhibitors according to the general formula (I), wherein: m and n are independently zero or an integer from 1 to 4; p is zero or an integer from 1 to 3, with the proviso that when p is zero, n and m cannot be both 1; R is hydrogen; C-Calkyl, optionally substituted by C-Ccycloalkyl, C-Caryl or hetero(C-C)aryl; (CO)R; (SO)R; C-Ccycloalkyl; C-Caryl; or hetero(C-C)aryl; Ris halogen, C-Calkyl, C-Chaloalkyl, C-Calkoxy, C-Chaloalkoxy; Y is CHor NR; Z is C&#x2550;R; and R, R, R, and Rare as further defined in the specification; and pharmaceutical acceptable salts thereof. 

The present invention provides a combination comprising a compound A of formula (I) as set forth in the specification or a pharmaceutically acceptable salt thereof, and an antibody inhibiting a growth factor or its receptor and/or an antimitotic agent or a derivative or prodrug thereof, useful in the treatment of tumors. The chemical name of compound A is 8-[4-(4-methyl-piperazin-1-yl)-phenylamino]-1,4,4-trimethyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxylic acid methylamide.

Combinations comprising a CDK inhibitor and a growth factor antibody or anti-mitotic

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Legnano, Italy

Ciro Mercurio