Euticals Spa

Saitec S.r.l.

Amri Italy S.r.l.

Almirall, LLC

Curia IP Holdings, LLC

Giuseppe Motta

Maria Argese

Paride Grisenti

Maria Donata Grilli

Emanuela Fumagalli

Daniele Pengo

Giorgio Bertolini

Domenico Vergani

Lorenzo Rodriguez

Cristina Cavallari

Maurizio Cini

Sean M Johnston

Farzaneh Seyedi

Meinrad Brenner

Maurizio Gallina

Giovanni Palombi

Eugenio Castelli

Ruiliang Lu

Shaozhi Huang

William Paul Armstrong

Gajanan Joshi

Nicola Landoni

The described invention relates to sarecycline, related compounds, intermediates and salts thereof and processes for preparing the same.

Process for making sarecycline hydrochloride

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 preparing fexofenadine is described, which provides for the hydrolysis of 4-[4-[4-(hydroxydiphenylmethyl)-1-piperidyl]-1-oxobutyl]-&#x3b1;,&#x3b1;-dimethylbenzeneacetic acid-alkyl ester, in a mixture of water and optionally an organic solvent, in the presence of a base; the carboxylate salt of 4-[4-[4-(hydroxydiphenylmethyl)-1-piperidyl]-1-oxobutyl]-&#x3b1;,&#x3b1;-dimethylbenzeneacetic acid is thus obtained, which is then directly reduced as carboxylate in a basic environment with hydrogen in the presence of a suitable hydrogenation catalyst to give the carboxylate of fexofenadine, which is precipitated by neutralization of the solution.

Process for preparing fexofenadine

The object of the present invention is a new process for the synthesis of tapentadol, both as free base and in hydrochloride form, which comprises the step of alkylation of the ketone (VII) to yield the compound (VIII), as reported in Diagram 1, with high stereoselectivity due to the presence of the benzyl group as substituent of the amino group. It was surprisingly found that this substitution shifts the keto-enol equilibrium towards the desired enantiomer and amplifies the capacity of the stereocenter present in the compound (VII) to orient the nucleophilic addition of the organometallic compound at the carbonyl towards the desired stereoisomer. This substitution thus allows obtaining a considerable increase of the yields in this step, and consequently allows significantly increasing the overall yield of the entire tapentadol synthesis process. A further object of the present invention is constituted by the tapentadol free base in solid form, obtainable by means of the process of the invention. Still another object of the invention is represented by the crystalline forms I and II of the tapentadol free base. A further object of the present invention is the mixture of the crystalline forms I and II of the tapentadol free base. 

Process for the synthesis of tapentadol and intermediates thereof

The present invention refers to a new process for the synthesis of tapentadol comprising the quantitative resolution of the racemic mixture (V) to obtain the stereoisomer of (S)-3-(dimethylamino)-2-methyl-1-(3-nitrophenyl)-propan-1-one (VII) according to the Scheme 2 below using the (2R,3R)&#x2014;O,O'-dibenzoyltartaric chiral acid wherein said resolution is quantitative. The present invention also refers to some intermediate compounds of the new synthesis process of tapentadol.

Process for the preparation of tapentadol and intermediates thereof

Process for pressing materials

Apparatus and method for preparing solid forms with controlled release

Process for preparing controlled release pharmaceutical forms and the

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Rescaldina, Italy

Giuseppe Motta