Pharmacia & Upjohn

Nerviano Medical Sciences S.r.l.

Pharmacia Italia S.p.a.

Istituto Europeo Di Oncologia S.r.l.

Congenia Slr

Cogenia Srl

Pharmacia & Tubjohn Spa

Congenia S.r.l.

Manuela Villa

Mario Varasi

Paolo Pevarello

Raffaella Amici

Anna Vulpetti

Anna Cappa

Tiziano Bandiera

Gabriella Traquandi

Antonella Isacchi

Marcella Nesi

Daniele Fancelli

Paola Vianello

Andrea Lombardi Borgia

Paolo Polucci

Carmela Speciale

Saverio Minucci

Ciro Mercurio

Mauro Angiolini

Barbara Salom

Giacomo Carenzi

Marco Ballarini

Gilles Pain

Giuseppe Meroni

Simon Plyte

Maria Gabriella Brasca

Paolo Orsini

Antonio Giordani

Sergio Mantegani

Antonio Longo

Antonello Mai

Claudia Piutti

Luca Sartori

Alessia Romussi

Loris Moretti

Elisa Zagarri

Sergio Valente

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

Acrylamido derivatives useful as therapeutic agents, particularly for the prevention and/or treatment of diseases and conditions associated with the activity of the mitochondrial permeability transition pore (MPTP), such as the diseases characterized by ischemia/reperfusion, oxidative or degenerative tissue damage, are herein described. These compounds belong to the structural formula (I) wherein R, R', R&#x2033;, W and a are as defined in the specification. The invention also relates to the preparation of these compounds, as well as to pharmaceutical compositions comprising them. 

Acrylomido derivatives useful as inhibitors of the mitochondrial permeability transition

Acrylamido derivatives useful as inhibitors of the mitochondrial permeability transition

Substituted pyrazolo[4,3-c]pyridine derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification, 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 dysregulated protein kinase activity, like cancer.

Substituted pyrazolo[4,3-C]pyridine derivatives active as kinase inhibitors

Substituted pyrazolo[4,3-c]pyridine derivatives active as kinase inhibitors

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

Compounds which are 4,5,6,7-tetrahydroindazole derivative formula (1), wherein the dotted line (x) represents a single or double bond; n is 0 or 1; R , R and R have the meanings reported in the description; Ra, R&prime;a, Rb, R&prime;b, Rc, R&prime;c have the meanings reported in the description, also comprising that Ra and Rb together and/or Ra and Rc together form a N-alkylpiperydinyl ring with 1 to 6 carbon atoms in the alkyl chain or a phenyl ring; or pharmaceutically acceptable salts thereof, are useful for treating cell proliferative disorders and Alzheimer's disease.

4,5,6,7-tetrahydroindazole derivatives as antitumor agents

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

5-(3-Phenyl-3-oxo-propyl)-1H-tetrazole derivatives

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

Disubstituted piperidine derivatives as neuroprotective agents

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Lurago d'Erba, Italy

Manuela Villa