Dac S.r.l.

Centre National De La Recherche Scientifique

Emory University

Pierre Fabre Medicament

Università Degli Studi Di Roma "la Sapienza"

Universita′ Degli Studi Di Milano

Istituto Superiore Di Sanita

Istituto Europeo Di Oncologia S.r.l.

Universitá Degli Studi Di Pavia

Sapienza Universitá Di Roma

Fondazione Ieo

Repla Chemical Ltd.

Epi-c S.r.l.

Antonello Mai

Saverio Minucci

Silvio Massa

Marco Ballarini

Gaetano Gargiulo

Pier Giuseppe Pelicci

Mario Varasi

Paola Vianello

Florian Thaler

Stefania Gagliardi

Manuela Villa

Enrico Garaci

Ciro Mercurio

Young-Sup Yoon

Anna Cappa

Marino Artico

Paola Barbara Arimondo

Gilles Pain

Ludovic Halby

Giuseppe Meroni

Andrea Savarino

Federico Corelli

Andrea Mattevi

Andrea Colombo

Anna Teresa Palamara

Ji Woong Han

Lucia Altucci

Xiaodong Cheng

Sergio Valente

Dante Rotili

Enzo Tramontano

Paola Arimondo

Joost Hendrik Adriaan Martens

Marina Lusic

Barbara Di Rienzo

The present invention relates to compounds of the following formula (I) and pharmaceutically acceptable salts and solvates thereof, their methods of preparation, their use as a drug, notably in the treatment of cancer, and pharmaceutical compositions containing such compounds. 

Substituted quinazoline derivatives as DNA methyltransferase inhibitors

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

This disclosure relates to compounds, compositions and methods of epigenetically transforming cells. In certain embodiments, the disclosure relates to methods of generating epigenetically altered cells comprising mixing isolated cells with compositions disclosed herein under conditions such that epigenetically altered cells are formed. In certain embodiments, the disclosure contemplates inducing cells, such as adult somatic cells or cells that are not naturally pluripotent, into cells with chemically induce pluripotency. In certain embodiments, the disclosure contemplates certain compounds disclosed herein, compounds disclosed herein optionally substituted with one or more substituents, derivatives, or salts thereof, for these purposes.

Compounds and compositions used to epigenetically transform cells and methods related thereto

Activation of HIV-1 replication causes oxidative stress, which in turn potentiates HIV-1 replication. The common basis for the compounds of the present invention is: A) the capacity of reactivating HIV-1 from latency, and B) the ability to counteract the cellular machinery which activates in order to limit the effects of oxidative stress. In this way, oxidative stress can be potentiated and a 'chain reaction' is sparked. This 'chain reaction' induces a more efficient reactivation of HIV-1 from latency and, in some cases, induces selective killing of the infected cells. Actions A) and B) can either be carried out by one drug exerting both effects, or obtained by the combined use of distinct drugs. There are two main cellular machineries counteracting oxidative stress, i.e. the thioredoxin (Trx) thioredoxin reductase (TrxR) system and glutathione. Herein, we present drug strategies capable of exerting action B) by blocking either of the two machineries.

Treatment of retroviral reservoirs exploiting oxidative stress

Tranylcypromine derivatives useful as therapeutic agents, particularly for the prevention and/or treatment of diseases and conditions associated with the activity of histone demethylases LSD1 and LSD2, such as the diseases characterized by deregulation of gene transcription, cell differentiation and proliferation, e.g. tumors, viral infections, are herein described. These compounds belong to the structural formula (I) wherein A and Rare as defined in the specification. The invention also relates to the preparation of these compounds, as well as to compositions containing them and to therapeutic use thereof. 

Tranylcypromine derivatives as inhibitors of histone demethylases LSD1 and/or LSD2

New histone deacetylase inhibitors according to the general formula (I) wherein: Q is a bond, CH, CH&#x2014;NRR, NRor oxygen, X is CH or nitrogen, Y is a bond, CH, oxygen or NR, Z is CH or nitrogen, R, Rare, independently, hydrogen, halogen, C-Calkyl or C-Chaloalkyl, R, Rare, independently, hydrogen or C-Calkyl, and R, R, Rand Rare as further defined in the specification.

Class of histone deacetylase inhibitors

New inhibitors of histone deacetylases having antitumor activity, and the process of preparation thereof are herein described. These compounds belong to the structural formula (I) where Ris a linear or branched chain containing at least two conjugated double bonds, A is an optionally substituted phenyl or pyridyl ring, Ar is an aryl or heteroaryl group, and Ris hydrogen or alkoxyalkyl. The application also describes the use of said compounds in the treatment of diseases associated to the deregulation of histone deacetylases activity, such as tumors, as well as the relevant pharmaceutical compositions for administration to patients requiring said treatment.

Histone deacetylases inhibitors

Antirhinoviral compounds having the formula ##STR1## wherein R is hetrocyclic, particularly pyrrole or pyrrolidine, X is H.sub.2 or O, n IS 3 to 7, and R.sub.1 is substituted phenyl are disclosed.

Synthetic derivatives of pyrrole and pyrrolidine suitable for the

Growing community of inventors

Rome, Italy

Antonello Mai