Newron Pharmaceuticals S.p.a.

Pharmacia & Upjohn S.p.a.

Farmitalia Carlo Erba S.r.l.

Zambon S.p.a.

Vicuron Pharmaceuticals Inc.

Pharmacia S.p.a.

Carla Caccia

Patricia Salvati

Mario Varasi

Franco Heidempergher

Florian Thaler

Alessandra Restivo

Mauro Napoletano

Sergio Mantegani

Cibele Sabido-David

Ermanno Moriggi

Laura Faravelli

Tiziano Bandiera

Enzo Brambilla

Elena Barbanti

Francesco Velardi

Nicola Carfagna

Claudio Arrigoni

Luigi Bogogna

Tiziano Ruffilli

Piero Melloni

Enrico Selva

Ruggero Fariello

Daniele Losi

Cibele Maria Sabido David

Gloria Padoani

Maurizio Meroni

Petra Karin Kaltofen

Silvia Vailati

Elsa Melloni

Diana Conte

Sabata Pierno

Jean-François Desaphy

Stefania Vallese

Laura Girola

Stefania Nikem Vallese

The present invention relates to safmamide or a pharmaceutically acceptable salt thereof for use in the treatment of a condition caused by pathological sarcolemma hyperexcitability, and/or of any other condition in which the restoration of normal sarcolemma excitability may produce a therapeutic benefit or improvement, wherein said condition is preferably a myotonic disorder.

Safinamide for treating myotonia

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

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 catalytic hydrogenation in the presence of a heterogeneous catalyst in a protic organic solvent.

Process for the production of 2-[4-(3- and 2-fluorobenzyloxy) benzylamino] propanamides

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 hydroxylamino derivatives of the general formula (I) wherein n is 0, 1 or 2; Rand R, independently of each other, are H, OH or OCH; Ris H or CH; Ris H, C-Cstraight or branched alkyl or, together with R, forms a five to seven-membered carbocyclic ring; and Rand R, independently of each other, are H or C-Cstraight or branched alkyl and the pharmaceutically acceptable salts or prodrug thereof, for the preparation of medicaments useful for the prevention, treatment and diagnosis of CNS degenerative disorders related to protein misfolding and/or misaggregation. The invention also relates to novel compounds included in formula (I), to a method for preparing said compounds and to pharmaceutical compositions containing them. 

Hydroxylamine derivatives

This invention is related to compounds of general formula (I) wherein X is oxygen or sulphur or a NRgroup; Ris C-Calkyl, or C-Calkyl substituted by phenoxy or phenyl, both phenoxy or phenyl being optionally substituted by one or more fluoro, chloro, trifluoromethyl, C-Calkyl, hydroxyl, C-Calkoxy; R, Rare independently hydrogen, C-Calkyl, halogen, trifluoromethyl, hydroxy or C-Calkoxy; Ris hydrogen, C-Calkyl; R, Rare independently hydrogen, C-Calkyl, optionally substituted by hydroxy or phenyl; Ris hydrogen or straight or branched C-Calkyl; Het is a five to seven membered, saturated or unsaturated heteromonocyclic or an eight to ten membered, saturated or unsaturated heterobicyclic group, containing one or more heteroatoms chosen independently from nitrogen, oxygen and sulphur, said mono- or bicyclic groups being optionally substituted by C-Calkyl, halogen, hydroxyl or C-Calkoxy; and the pharmaceutically acceptable salts or prodrug thereof, that are active as sodium and/or calcium channel modulators and/or as selective MAO-B inhibitors 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. 

Substituted benzylaminoalkylene heterocycles

There are provided compounds of formula (I), wherein R,is a hydrogen, chlorine or bromine atom or a methyl, methylthio, hydroxy, cyano or carboxamido group; R,is C,-C,alkyl or an alkyl group; R,and R,are independently a hydrogen atom, a C,-C,alkyl group, a C,-C,alkenyl group, a C,-C,cycloalkyl C,-C,alkyl group, a phenyl-C,-C,alkenyl or phenyl group: which groups are optionally substituted by C,-C,alkyl, C,-C,alkoxy, triflouromethyl, hydroxy or amino group; or a group of formula (a), wherein R,is hydrogen atom or a C,-C,alkyl group and R,is a phenyl group, a substituted phenyl group as described above or a heterocyclic ring, R,is a hydrogen or bromine atom or an organic residue and R is H or an organic residue, or a pharmaceutically acceptable salt thereof. A process for their preparation and the pharmaceutical compositions comprising them are also provided.

Abeo-ergoline derivatives as 5HT1A ligands

Heterocyclyl-ergoline derivatives as 5-HT.sub.1A receptor ligands

Imidazolylalkyl derivatives of imidazo�1,5-a!indol-3-one

Imidazolylakyl derivatives of imidazo �5,1-c!�1,4!benzoxazin-1-one

Azabicycloalkyl derivatives of imidazo[1,5-a]indol-3-one and process for

The present invention provides compounds of the formula (I) ##STR1## wherein A, R.sub.1, R.sub.2 and R.sub.3 are defined as in the specification, or a pharmaceutically acceptable salt thereof. A process for their preparation and the pharmacetical compositions comprising them are also provided.

Serotoninergic ergoline derivatives

The invention relates to new derivatives of 1-imidazolylalkyl-3-phenyl-imidazolidin-2-ones of general formula (I) ##STR1## wherein n is 1, 2 or 3; each of R, R.sub.1 and R.sub.2, which may be the same or different, is hydrogen, halogen, hydroxy, cyano, C.sub.1 -C.sub.6 alkyl, CF.sub.3, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkylthio, formyl, C.sub.2 -C.sub.6 alkanoyl, carboxy, C.sub.1 -C.sub.6 alkoxy-carbonyl, nitro, --N(R.sub.4 R.sub.5) in which each of R.sub.4 and R.sub.5 independently is hydrogen C.sub.1 -C.sub.6 alkyl formyl or C.sub.2 -C.sub.6 alkanoyl; or a (R.sub.6 R.sub.7)N--SO.sub.2 group, in which each of R.sub.6 and R.sub.7 independently is hydrogen or C.sub.1 -C.sub.6 alkyl; R.sub.3 is an imidazolyl group of formula ##STR2## wherein each of R.sub.8 and R.sub.10 which may be the same or different is hydrogen or C.sub.1 -C.sub.6 alkyl, R.sub.9 is hydrogen, C.sub.1 -C.sub.6 alkyl or a nitrogen protecting group, or pharmaceutically acceptable salts thereof, which are useful in the treatment of CNS disorders, such as, e.g., anxiety and psychosis, and in the treatment of gut motility disorders, and/or emesis.

Phenyl-imidazolidinone derivatives

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Gallarate, Italy

Carla Caccia