Newron Pharmaceuticals S.p.a.

Laura Faravelli

Patricia Salvati

Florian Thaler

Mauro Napoletano

Carla Caccia

Alessandra Restivo

Cibele Sabido-David

Elena Barbanti

Ermanno Moriggi

Renato Canevotti

Francesco Ponzini

Stefania Gagliardi

Emanuela Izzo

Elena Colombo

Cibele Maria Sabido David

A process for obtaining therapeutically active 2-[4-(3- and 2-(fluorobenzyloxy)benzylamino]propanamides, and their salts with pharmaceutically acceptable acids with high purity degree, in particular, with a content of dibenzyl derivatives impurities lower than 0.03%, preferably lower than 0.01% by weight. The process is carried out by submitting the Schiff bases intermediates 2-[4-(3- and 2-fluorobenzyloxy)benzylideneamino]propanamides to a reduction reaction with a reducing agent selected from sodium borohydride and potassium borohydride in an appropriate amount of an organic solvent selected from C-Clower alkanols, allowing the formation and presence during a substantial position of the reduction reaction course of a suspension of the Schiff base into the saturated solution of the Schiff base into the same organic solvent.

High purity 2-[4-(3- or 2-fluorobenzyloxy)benzylamino] propanamides and methods of use thereof

A process for obtaining therapeutically active 2-[4-(3- and 2-(fluorobenzyloxy)benzylamino]-propanamides and their salts with pharmaceutically acceptable acids with a high degree of purity, i.e. with a content of dibenzyl derivatives impurities lower than 0.03% by weight. The process is carried out by submitting a Schiff base intermediate to a reduction reaction with a reducing agent in an amount of organic solvent to allow the formation (and presence during a substantial portion of the reduction reaction) of a suspension of the Schiff base.

High purity 2-[4-(3- OR 2-fluorobenzyloxy)benzylamino]propanamides and methods of use thereof

2-Phenylethylamino substituted carboxamide derivatives and their use as sodium and/or calcium channel modulators useful in preventing, alleviating and curing a wide range of pathologies are presented.

2-phenylethylamino derivatives as calcium and/or sodium channel modulators

The disclosure relates to pharmacotherapy of a psychiatric disorder which is schizophrenia and/or anxiety, wherein schizophrenia includes schizophrenia related disorders such as brief psychotic disorders, delusional disorders, schizoaffective disorders, and schizophreniform disorders, and anxiety includes panic disorders, obsessive-compulsive disorders (OCD), post-traumatic stress disorders (PTSD), social phobia or social anxiety disorders, specific phobia, and generalized anxiety disorders (GAD). The compounds of the disclosure are useful for the treatment of the above psychiatric disorders alone or in combination with other therapeutical agents effective in the treatment of schizophrenia and/or anxiety disorders.

Alpha-aminoamide derivatives useful in the treatment of psychiatric disorders

2-Phenylethylamino substituted carboxamide derivatives of formula (I); wherein J, W, R, R, R, R, and Rhave the meanings as defined in the specification and pharmaceutically acceptable salts thereof, pharmaceutical compositions containing them as active ingredient and their use as sodium and/or calcium channel modulators useful in preventing alleviating and curing a wide range of pathologies, including neurological, psychiatric, cardiovascular, inflammatory, ophthalmic, urology, and gastrointestinal diseases where the above mechanisms have been described as playing a pathological role, are described. 

This invention is related to compounds and use of N-Acyl-N'-benzyl-alkylendiamino derivatives of the following general formula (I), wherein A is a straight or branched C-Calkyl chain; X is a methylene, oxygen, sulphur or a NRgroup; Ris a straight or branched C-Calkyl or C-Calkenylene or C-Calkynylene chain, optionally substituted with CF, phenyl, phenoxy or naphthyl, the aromatic rings optionally substituted by one or more C-Calkyl, halogens, trifluoromethyl, hydroxy or C-Calkoxy groups; R, Rare independently hydrogen, a C-Calkyl chain, halogen, trifluoromethyl, hydroxy or C-Calkoxy groups; R, Rare independently hydrogen or C-Calkyl; Ris a hydrogen or a straight or branched C-Calkyl or linked to Rcan form a five to seven membered lactam; Ris hydrogen or C-Calkyl; and the pharmaceutically acceptable salts thereof that are active as sodium and/or calcium channel modulators and therefore useful in preventing, alleviating and curing a wide range of pathologies, including, but not limited to, neurological, psychiatric, cardiovascular, inflammatory, ophthalmic, urologic, metabolic and gastrointestinal diseases, where the above mechanisms have been described as playing a pathological role 

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Garbagnate Milanese, Italy

Laura Faravelli