Poli Industria Chimica Spa

Euticals Spa

Amri Italy S.r.l.

Other

Polichem S.a.

Curia IP Holdings, LLC

Paride Grisenti

Maria Argese

Ambrogio Magni

Giuseppe Motta

Daniele Pengo

Maria Donata Grilli

Emanuela Fumagalli

Elisa Verza

Giuseppe Guazzi

Alberto Mangia

Shahrzad Reza Elahi

Stefano Poli

Massimo Leoni

Roberto Scrocchi

Laura Bossi

Vincenzo Olgiati

Alessandro Livieri

Roberto Girardello

Elahi Shahrzad Reza

Riccardo Monti

Paolo Prestileo

Fabio Pecora

Sharzad Reza Helai

A Rifaximin polymorphic mixture of &#x3b1;/&#x3b2; form in a relative ratio of 85/15&#xb1;3 and a process for its preparation. The polymorphic mixture of Rifaximin is for use as a medicament, in particular in the treatment of traveler's diarrhea and hepatic encephalopathy. A pharmaceutical composition comprises the polymorphic mixture of Rifaximin as active ingredient, in particular, a solid formulation, more in particular, a film coated tablet. A polymorphic form of crude wet rifaximin and of purified wet rifaximin their use are used as intermediates in a process for the preparation of Rifaximin polymorphic mixture of &#x3b1;/&#x3b2; form in a relative ratio of 85/15&#xb1;3.

Polymorphic mixture of Rifaximin and its use for the preparation of solid formulations

Polymorphic mixture of rifaximin and its use for the preparation of solid formulations

A process for the preparation of the amorphous form of Regadenoson of formula is disclosed together with new crystalline polymorphic forms E, F and G and methods for their preparation. Regadenoson amorphous form can be prepared in mild reaction conditions with high chemical purity (&#x3e;99.6%) and high stability to the heating. A particularly thermodynamically stable anhydrous crystalline form of Regadenoson (form G) is also disclosed, provided with high stability not when exposed to 90% RH at 25&#xb0; C. for 96 hour, but also to the heating up to 200&#xb0; C.

Stable solid forms of regadenoson

A cocrystal of tiotropium bromide and lactose monohydrate is herein disclosed. In the cocrystal the components tiotropium bromide and lactose are preferably present in an almost stoichiometric ratio. Said cocrystal has a single endothermic event at about 191-193&#xb0; C. determined by DSC. A process for the preparation of the cocrystal is also disclosed. Preferably, the cocrystal has a particle size distribution of D90&#x3c;10 &#x3bc;m. The cocrystal is also disclosed for use as medicament, in particular for the treatment of a respiratory complaint, such as chronic obstructive pulmonary disease (COPD), bronchitis, emphysema and asthma. A pharmaceutical composition comprising the cocrystal as active ingredient is also disclosed, in particular for administration by inhalation. In the latter case, said cocrystal has a mean particle size of 0.5 to 10 &#x3bc;m, preferably 1 to 6 &#x3bc;m, more preferably 1.5 to 5 &#x3bc;m.

Crystalline form of tiotropium bromide with lactose

The present invention relates to the biocatalyzed synthesis of enantiomerically pure (3R) and (3S)-methyl-1,2,3,4-tetrahydroquinoline. Said enantiomerically pure compounds are useful as chiral synthons in organic synthesis and, in particular, for the preparation of diastereomerically pure (21R) and (21S)-agratroban and its analogs. New compounds used as intermediates in the process of the invention are also disclosed.

Biocatalyzed synthesis of the optically pure (R) and (S) 3-methyl-1,2,3,4-tetrahydroquinoline and their use as chiral synthons for the preparation of the antithrombic (21R)- and (21S)-argatroban

This invention relates to new water-soluble solid pharmaceutical inclusion complexes and their aqueous solutions for oral, ophthalmic, topical or parenteral use containing a macrolide and certain cyclodextrins. More particularly the invention relates to new water-soluble solid pharmaceutical inclusion complexes and their solutions in aqueous solvents, said compositions containing

Water-soluble solid pharmaceutical inclusion complexes and their aqueous solutions for oral, ophthalmic, topical or parenteral use containing a macrolide and certain cyclodextrins

Processes for preparing pimecrolimus starting from ascomycin, exploiting the selectivity characteristics of the purified enzymatic systems particularly regarding the selective functionalization of the hydroxyl groups present in position 24 and 33 of ascomycin. Such method represents the first example of chemoenzymatic synthesis for preparing pimecrolimus.

Chemo-enzymatic approach to the synthesis of pimecrolimus

The present invention relates to a process for the preparation of mycophenolate mofetil (MMF) in which an ester of mycophenolic acid (MPA) with a low-molecular-weight aliphatic alcohol is transesterified with N-(2-hydroxyethyl)morpholine in the presence oflipase, and in which the MPA esterification reaction is carried out in the presence oflipase using the corresponding alcohol as the solvent.

Method for the preparation of mycophenolate mofetil by enzyme tranesterification

The present invention relates to a new process of synthesis and to some new intermediates for the preparation of steroids with progestogen activity, more particularly, for the preparation of Desogestrel of formula (I). Said process is characterized by the regioselective reduction of the compound of formula (II) to give the intermediate of formula (III). 

Process and new intermediates for the preparation of steroids with a progestogen activity

Process for the preparation of compounds active in the treatment of Parkinson's disease, and such compounds, having general formula (VI) wherein R may be, independently, a linear, branched or cyclic, saturated or unsaturated C alkyl radical, such as, for example, the radicals methyl, ethyl, propyl, butyl, isobutyl, tert-butyl, pentyl, cyclopentyl, hexyl, cyclohexyl and octyl. The process utilizes as starting materials the compound of formula (I) wherein R represents a linear, branched or cyclic, saturated or unsaturated C alkyl residue.

Process for the preparation of alkyl mercapto methyl ergoline derivatives

Diastereomerically pure 3-oxo and 3-thioxo-4-aza-androstan derivatives

The present invention provides new process of preparing neuromuscular blocking agents. The process include preparing neuromuscular blocking agents using the compounds of formula I: ##STR1## wherein R.sub.1 is=O and X is halo; and formula II: ##STR2## wherein R, and X are as defined above.

Process for preparing neuromuscular blocking agents and intermediates

The present invention provides new process of preparing neuromuscular blocking agents. The process include preparing neuromuscular blocking agents using the compounds of formula I: ##STR1## wherein R.sub.1 is .dbd.O and X is halo; and formula II: ##STR2## wherein R.sub.1 and X are as defined above.

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Milan, Italy

Paride Grisenti