Pharmacia & Upjohn

Nerviano Medical Sciences S.r.l.

Pharmacia Italia S.p.a.

Pfizer Italia S.r.l.

Dac S.r.l.

Ifom Fondazione Istituto Firc Di Oncologia Molecolare

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

Raffaella Amici

Paolo Pevarello

Anna Vulpetti

Mario Varasi

Maria Gabriella Brasca

Paolo Orsini

Marcella Nesi

Daniele Fancelli

Patrick Roussel

Manuela Villa

Fabrizio Orzi

Gabriella Traquandi

Barbara Salom

Patricia Salvati

Ciro Mercurio

Antonella Isacchi

Antonio Longo

Florian Thaler

Matteo D'Anello

Saverio Minucci

Alberto Bonsignori

Roberto Maj

Katia Martina

Claudia Piutti

Simona Polo

Agnese Abate

Maria Carmela Fulco

Sebastiano Pasqualato

Maurizio Pasi

Luca Sartori

Giovanni Faga'

Elena Maspero

Matteo D'anello

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

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. 

Spirocyclic derivatives as histone deacetylase inhibitors

Compounds represented by formula (Ia) or (Ib) and wherein R and Rare as defined in the description, and pharmaceutically acceptable salts thereof, are disclosed; the said compounds are useful in the treatment of cell cycle proliferative disorders, e.g. cancer, associated with an altered cell cycle dependent kinase activity.

Substituted pyrrolo-pyrazole derivatives as kinase inhibitors

Compounds which are 3-aminoindazole derivatives or pharmaceutically acceptable salts thereof, together with pharmaceutical compositions comprising them are disclosed; these compounds or compositions are useful in the treatment of diseases caused by and/or associated with an altered protein kinase activity such as cancer, cell proliferative disorders, Alzheimer's disease, viral infections, auto-immune diseases and neurodegenerative disorders.

Aminoindazole derivatives active as kinase inhibitors

A new class of pyrazolo derivative compounds having the formula where R and Rhave the meanings given herein. The pyrazolo derivative compounds are useful in treating cell proliferative disorders caused by and/or associated with an altered cell cycle dependent kinase activity in mammals. The compounds may be provided in pharmaceutical compositions or in a kit.

Compounds which are 2-amino-1,3-thiazole derivatives of formula (I)wherein R is a halogen atom, a nitro group, an optionally substituted amino group or it is a group, optionally further substituted, selected from i) straight or branched C&#x2013;Calkyl, C&#x2013;Calkenyl or C&#x2013;Calkynyl; ii) C&#x2013;Ccycloalkyl; iii) aryl or arylalkyl with from 1 to 8 carbon atoms within the straight or branched alkyl chain; Ris an optionally further substituted group selected from: i) straight or branched C&#x2013;Calkyl or C&#x2013;Calkenyl; ii) 3 to 6 membered carbocycle or 5 to 7 membered heterocycle ring; iii) aryl or arylcarbonyl; iv) arylalkyl with from 1 to 8 carbon atoms within the straight or branched alkyl chain; v) arylalkenyl with from 2 to 6 carbon atoms within the straight or branched alkenyl chain; vi) an optionally protected amino acid residue; or a pharmaceutically acceptable salt thereof; are useful for treating cell proliferative disorders associated with an altered cell dependent kinase activity.

2-amino-thiazole derivatives, process for their preparation, and their use as antitumor agents

Compounds which are 2-ureido-1,3-thiazole derivatives of formula (I) wherein R is a halogen atom, a nitro group, an optionally substituted amino group or it is a group optionally further substituted, selected from: i) straight or branched C-Calkyl; ii) C-Ccycloalkyl; iii) aryl or arylalkyl with from 1 to 6 carbon atoms within the straight or branched alkyl chain; Ris an optionally substituted group selected from: i) straight or branched C-Calkyl; ii) 3 to 6 membered carbocycle or 5 to 7 membered heterocycle ring; iii) aryl or arylcarbonyl; iv) arylalkyl with from 1 to 6 carbon atoms within the straight or branched alkyl chain; Ris hydrogen, a straight or branched C-Calkyl or C-Calkenyl or alkynyl group; or, taken together with the nitrogen atom so which they are bonded, Rand Rform a substituted or unsubstituted group selected from: i) an optionally benzocondensed or bridged 5 to 7 membered heterocycle; or ii) a 9 to 11 membered spiro-heterocyclic compound; or a pharmaceutically acceptable salt thereof; are useful for treating cell proliferative disorders associated with an altered cell dependent kinase activity.

2-Ureido-thiazole derivatives, process for their preparation, and their use as antitumor agents

2-amino-1,3-thiazole derivatives represented by formula (I) or (II): where R, R , R and R are defined herein, or pharmaceutically acceptable salts thereof are useful as, for example, the treatment of cancer, cell proliferative disorders, Alzheimer's disease, viral infections, auto-immune diseases or neurodegenerative diseases.

Arylmethyl-carbonylamino-thiazole derivatives and their use as antitumor agents

Phenylacetamido-pyrazole derivatives, process for their preparation and their use as antitumor agents

2-amino-1,3-thiazole derivatives represented by formula (I) or (II): ##STR1## where R, R.sub.1, R.sub.2 and R.sub.3 are as defined herein, or pharmaceutically acceptable salts thereof, are useful in, for example, the treatment of cancer, cell proliferative disorders, Alzheimer's disease, viral infections, auto-immune diseases or neurodegenerative diseases.

Arylmethyl-carbonylamino-thiazole derivatives, process for their

2-(4-substituted)-benzylamino-2-methyl-propanamide derivatives

N-(4-substituted-benzyl)-2-aminolactam derivatives

Growing community of inventors

Codogno, Italy

Raffaella Amici