Flamma S.p.a.

Newron Pharmaceuticals S.p.a.

Novozymes A/s

Universita′ Degli Studi Di Milano

Renato Canevotti

Gianpaolo Negrisoli

Francesco Ponzini

Patricia Salvati

Elena Barbanti

Laura Faravelli

Lise Munch Mikkelsen

Carlo Alberto Bignozzi

Massimo Previtali

Federico Della Negra

Alessandro Dondoni

Anna Rencurosi

Marco De Amici

Clelia Dallanoce

Almin Silnovic

Stefania Gagliardi

Giulio Vistoli

Marica Orioli

Marina Carini

Giancarlo Aldini

Roberto Bisaccia

Francesco Mormile

Alberto Marra

Valeria Dissette

Gian Paolo Negrisoli

Disclosed are peptide or pseudopeptide derivatives containing a nitrogenous heterocyclic residue with blocking activity against the by-products of lipid oxidative stress, and in particular of unsaturated aldehydes such as malondialdehyde and 4-hydroxy-trans-2-nonenal (HNE).

Peptide derivatives and therapeutic activity thereof

The present invention relates to a process for preparation of triazolo[4,5-d] pyrimidine cyclopentane compounds of formula (I), and pharmaceutically acceptable salts thereof. The invention also provides novel compounds that can be used as intermediates in the process for preparing triazolo[4,5-d] pyrimidine cyclopentane compounds. The process and the intermediates are particularly useful for the preparation of ticagrelor and pharmaceutically acceptable salts thereof.

Process for the preparation of triazolo[4,5-D] pyrimidine cyclopentane compounds

The conversion of a peptide aldehyde to a hydrosulfite adduct can be used to increase the aqueous solubility in the purification of the peptide aldehydes. Advantageously, this hydrosulfite adduct is itself effective as a subtilisin inhibitor and stabilizer and it can also stabilize a second enzyme if present. The hydrosulfite adduct is effective as a subtilisin inhibitor, and it maintains its inhibitory and stabilizing effect in a liquid detergent during storage. Thus, use of the hydrosulfite adduct can avoid the cost and time of converting it back to the peptide aldehyde and subsequent drying of the peptide aldehyde can be saved, and this can avoid the inconvenience of handling the peptide aldehyde in powder form or as a highly diluted aqueous solution.

Stabilized subtilisin composition

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

Dipeptide compounds containing a histidine residue proved to have interesting blocking activity on secondary products from lipid oxidative stress, in particular on unsaturated aldehydes such as malondialdehyde and hydroxynonenal, which are known to contribute to the inset of quite a number of chronic pathologies such as neurodegenerative, inflammatory chronic, cardiovascular diseases, diabetes complications and cataract.

Peptide derivatives with therapeutic activity

The present invention relates to amino alcohol derivatives of general formula I:  These derivatives possess an interesting activity in that they block the secondary products of lipid oxidative stress, and are consequently suitable for therapeutic use in all disorders related with the presence of reactive carbonyl compounds.

Amino alcohol derivatives and their therapeutic activities

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

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Chignolo d'Isola, Italy

Renato Canevotti