Bresso, Italy

Newron Pharmaceuticals

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Bresso, Italy
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The invention relates to a new process for the production and/or purification of the salt of the compound (S)-2-[4-(2-fluorobenzyloxy) benzylamino]propanamide, i.e. ralfinamide, or the respective R-enantiomer, with methane sulfonic acid in high yields and very high enantiomeric and chemical purity in the form of the crystalline anhydrous polymorph identified as form A, wherein said salt is substantially free from impurities having genotoxic effect, such as (C_(1)-C_(5))alkanylmethanesulfonates, and residual solvents known as potential precursors thereof, such as (C_(1)-C_(5))alkanols or esters thereof with lower alkanoic acids.


Patent
Newron Pharmaceuticals | Date: 2016-07-27

Fluorinated arylalkylaminocarboxamide derivatives of formula (I) are described wherein W, J, n, R^(1), R^(2), R^(2), R^(3), R^(4), R^(5 )and R^(6 )have the meanings as defined in the specification and pharmaceutically salts thereof, pharmaceutical compositions containing them as active ingredients 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, urolological, and gastrointestinal diseases, where the above mechanisms have been described as playing a pathological role.


Patent
Newron Pharmaceuticals | Date: 2016-01-27

The present invention is in the field of pharmacotherapy of cognitive deficits in learning and memory by administering an -aminoamide, particularly safin-amide. Examples of disturbances in cognition that can be treated with compounds of the invention are the ones associated with disorders such as autism, dyslexia, attention deficit hyperactivity disorder, schizophrenia, obsessive compulsive disorders, psychosis, bipolar disorders, depression, Tourettes syndrome, Mild Cognitive Impairment (MCI) and disorders of learning in children, adolescents and adults, Age Associated Memory Impairment, Age Associated Cognitive Decline, Alzheimers Disease, Parkinsons Disease, Downs Syndrome, traumatic brain injury Huntingtons Disease, Progressive Supranuclear Palsy (PSP), HIV, stroke, vascular diseases, Picks or Creutzfeldt-Jacob diseases, multiple sclerosis (MS), other white matter disorders and drug-induced cognitive worsening.


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_(1)-C_(5 )lower 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.


Substituted 2-[2-(phenyl)ethylamino]alkaneamide derivatives of formula (I) wherein X, Y, Z, R, R_(1), R_(2), R_(3), R_(3 )R_(4), R_(5), R_(6), R_(7 )have the meanings 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, but not limited to, neurological, cognitive, psychiatric, inflammatory, urogenital and gastrointestinal diseases, where the above mechanisms have been described as playing a pathological role.


Substituted 2-[2-(phenyl)ethylamino]alkaneamide derivatives of formula (I) wherein X, Y, Z, R, R_(1), R_(2), R_(3), R_(3 )R_(4), R_(5), R_(6), R_(7 )have the meanings 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, but not limited to, neurological, cognitive, psychiatric, inflammatory, urogenital and gastrointestinal diseases, where the above mechanisms have been described as playing a pathological role.


Substituted 2-[2-(phenyl)ethylamino]alkaneamide derivatives of formula (I) wherein


Substituted 2-[2-(phenyl)ethylamino]alkaneamide derivatives of formula (I)


Substituted 2-[2-(phenyl)ethylamino]alkaneamide derivatives of formula (I) wherein X, Y, Z, R, R_(1), R_(2), R_(3), R_(3 )R_(4), R_(5), R_(6), R_(7 )have the meanings 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, but not limited to, neurological, cognitive, psychiatric, inflammatory, urogenital and gastrointestinal diseases, where the above mechanisms have been described as playing a pathological role.


Patent
Newron Pharmaceuticals | Date: 2014-11-04

New uses of safinamide, safinamide derivatives and MAO-B inhibitors in novel types of treatment for Parkinsons Disease are described. More specifically, the invention relates to methods for treating Parkinsons Disease through the administration of safinamide, a safinamide derivative, or a MAO-B inhibitor, in combination with other Parkinsons Disease agents or treatments, such as levodopa/PDI or dopamine agonists.

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