Sigma-tau Industrie Farmaceutiche Riunite S.p.a.

Chemi S.p.a.

Endura Spa

Italfarmaco Sud S.p.a.

Cambrex Profarmaco Milano S.r.l.

Centre National De La Recherche Scientifique

Université´ D'aix-marseille

Universite Dé Lorraine

Italfarmaco Spa

Universität De Barcelona

Oreste Piccolo Studio Di Consulenza Scientifica

Oreste Piccolo

Lorenzo De Ferra

Pietro Massardo

Valerio Borzatta

Paolo De Witt

Roberto Castagnani

Fausto Bonifacio

Giovanna Delogu

Elisa Capparella

Carlotta Gobbi

Cristina De Candia

Giovanna Di Blasi

Daniele Vigo

Alessandra Verrazzani

Maria Ornella Tinti

Sergio Penco

Paolo Mascagni

Giuseppe Bottoni

Mara Sada

Flavio Leoni

Tiziana Benincori

Giorgio Cignarella

Elio Ullucci

Stefano Servi

Cristina Crescenzi

Joan Bosch

Flavio Maina

Simona Rizzo

Rosanna Dono

Francesco Autuori

Daniele Passarella

Carlo Bianchini

Francesco Colombo

Valmen Monzani

Bernard Maigret

Sandra Rondinini

Guido Cifarelli

Michele Tragni

Francesco Caputo

Vincent Leroux

Patrizia R Mussini

Cristina Ciancimino

Francesco Sannicolo′

Simona Tollis

Disclosed are new intermediates for the synthesis of Linagliptin and of its salts and a process for its preparation involving said intermediates.

Intermediates and processes for the preparation of Linagliptin and its salts

Disclosed is a process for the preparation of Raltegravir and pharmaceutically acceptable salts thereof.

Process for the preparation of Raltegravir

The present invention provides a formulation characterised by the simultaneous presence in cyclodextrin based supramolecular complexes, of two components, one of which is a neonicotinoid selected from the group consisting of Thiacloprid and Thiamethoxam and the other possesses an activity synergistic with the first, enhancing its effectiveness. The synergistic component that is able to synergistically enhance the activity of the active principle is piperonyl butoxide, and. Processes for preparing said formulation and its use for the activities herein indicated are further aspects of the present invention.

Biologically active formulation

The present invention provides a formulation characterized by the simultaneous presence in cyclodextrin based supramolecular complexes, of two components, one of which possesses insecticidal, acaricidal, fungicidal, snailcidal or vermicidal activity and the other possesses an activity synergistic with the first, enhancing its effectiveness. The biologically active substance is chosen from the following classes of chemical products: carbamates, organophosphates, thioureas, pentatomic or hexatomic heterocycles in which 1, 2 or 3 nitrogen atoms are present. The synergistic substance can be chosen from components containing at least one aromatic or non aromatic carbocyclic ring, such as piperonyl butoxide, sesamol, verbutin or MGK 264. For the same dose, the activity of the present formulations is greater than that of the mixture of the two active components alone or separately complexed with cyclodextrin. The process for preparing said formulation and its use for the activities herein indicated are further aspects of the present invention.

Novel amino acids derivatives, in particular some amino acid amides derivatives, their process of preparation and their use for inhibiting Met-triggered disorders, in particular cancer.

Aminoacid derivatives, their process of preparation and their therapeutical uses as inhibitors of oncogenic signals by the Met family

The present invention provides a new insecticide formulation based on cyclodextrin characterized in that the active substance (insecticide and/or insect growth regulator), and a compound synergistic with the active substance, are complexed simultaneously with cyclodextrin. The formulation presents as a solid or as a solid/oil composition, and is soluble or completely emulsifiable in water or in aqueous mixtures of water miscible solvents. The activity of the present formulations was found to be greater than that of a mixture of the two active components each complexed separately with cyclodextrin, for the same dose. The preparation process of said formulation and its use as an insecticide in agriculture, for veterinary use or to eliminate household insects, are further aspects of the present invention.

Insecticide formulation

Metallic catalysts of the general formula (I) and their precursors, suitable for chemo- regio- and stereoselective reactions, derived from ortho-bis-(1-phospholanyl)-heteroarenes. The new catalysts are characterized by the presence of two homo-morphic phospholanic rings set in adjacent positions of an aromatic pentatomic heterocycle 

Metallic catalysts for chemo-, regio- and stereoselective reactions, and corresponding precursors

Stable, biologically compatible pharmaceutical compositions in the form of water-in-oil microemulsions (w/o), for the sustained release by parenteral administration of active ingredients which are hydrophilic or are made hydrophilic by suitable derivatization, a process for the preparation of said microemulsions and the use thereof.

Sustained release pharmaceutical compositions for the parenteral administration of hydrophilic compounds

A process for preparing an Rh-based catalytic system heterogenized on an organic or mineral support, characterized in that: a) a rhodium derivative with a valency state&#x3e;0 is reduced in an ether or aromatic solvent and in the presence of a compound chosen from the group consisting of lipophilic tertiary amines, lipophilic tertiary amides and lipophilic quaternary ammonium salts, and b) the mixture thus obtained is adsorbed onto a suitable organic or mineral support. Use of the abovementioned catalytic system to hydrogenate a C&#x2550;C double bond of an &#x3b1;,&#x3b2;-unsaturated carbonyl compound.

Preparation and use of a heterogeneous rhodium catalyst for the hydrogenation of a double bond of an &#x3b1;-&#x3b2;-unsaturated carbonyl compound

A new, more efficient and highly stereospecific process is described for the preparation of compounds with general formula (R)-(I) and of absolute configuration (R), where the groups M, W, Q and Q are as defined in the description, starting from compounds of absolute configuration (S) by hydrolysis, in the presence of acids, of the corresponding esterified derivatives. The (R)-(I) products obtained with the process described herein are chiral synthons useful for the production of enanthiomerically pure drugs. The preparation of (R)-carnitine is also provided.

Stereospecific hydrolysis of optically active esters

The present invention describes a process for the industrial production of L-carnitine, comprising the enantioselective reduction of an alkyl 4-chloro-3-oxobutyrate or 4-chloro-3-oxobutyramide. The optically active 3-hydroxy derivative thus obtained is reacted with trimethylamine, obtaining crude L-carnitine, which is then finally purified. The catalyst used for the reduction is a complex of ruthenium bound to a penta-atomic bis-heteroaromatic system. The reduction reaction, performed in controlled conditions of hydrogen pressure, substrate concentration, temperature, and substrate: catalyst molar ratio, enables 4-chloro-3-hydoxybutyrate or 4-chloro-hydroxybutyamide to be obtained in a high yield. The process described, which leads to L-carnitine being obtained, is easily applicable on an industrial scale.

Industrial process for the production of L-carnitine

Nitriloxy derivatives of (R) and (S)-carnitine

Process for the preparation of 3-substituted 4-phenyl-piperidine derivative

The invention relates to a process for the preparation of phosphatidylserines by reacting racemic or enantiomerically pure serine, preferably (L)-serine, with natural phosphatides, such as soybean or egg lecithin, or with synthetic phosphatides, in the presence of a phospholipase D, having transphosphatidylating activity, in an aqueous/organic diphasic system.

Process for the industrial preparation of phosphatidylserine

Growing community of inventors

Sirtori, Italy

Oreste Piccolo