Rottapharm Spa

Other

Fondazione Cariplo

Fondazione Istituto Insubrico Di Ricerca Per La Vita

Milanese, Alberto

Alberto Milanese

Riccardo Stradi

Marino Nebuloni

Lucia Carrano

Derio Desideri

Desiderio Desideri

Disclosed is a process for the preparation of partricin alkyl esters which involves reacting partricin in a solvent with primary alkyl alcohols in the quantity of 5 to 1000 moles per mole of partricin in the presence of carbodiimides, and optionally in the presence of acylation catalysts and/or nitrogen bases or anhydrous acids.

Method of esterification of carboxyl groups present on multihydroxyl cyclic polyene molecular structures carrying basic nitrogen groups

A stable complex of tomoxiprole with 2-hydroxypropyl-beta-cyclodextrin with fast dissolution rate and rapid absorption wherein amorphous tomoxiprole forms a complex with 2-hydroxypropyl-beta-cyclodextrin in about equimolecular ratio. The complex shows a remarkably faster dissolution rate and absorption with respect to crystalline tomoxiprole and is particularly suitable for the production of pharmaceutical oral dosage forms, such as tablets and capsules, where rapid onset of therapeutical action is required. A method of manufacture of the complex is also described and claimed.

Complex of amorphous tomoxiprole and cyclodextrin with fast dissolution rate and process for the preparation thereof

Compounds of formula I ##STR1## wherein: X is N or &gt;C--F;

7-(4-amino-piperazinyl)- or 7-(4-chloro-piperazinyl)quinolinone and

Compounds of formula I ##STR1## wherein R is a phenyl group; a phenyl group mono- or di-substituted by halogen atoms, methyl, methoxy, nitro, or trifluoromethyl group; or a 2-, 3- or 4-pyridyl group; and pharmaceutically acceptable acid addition salts thereof. Compounds I are prepared by reacting N-substituted piperazines with 1-(2',4'-dichloro-benzoylmetyl)-imidazole, optionally reducing thereafter the resulting enamines. Compounds I have antimycotic and antibacterial activities, higher than those of known comparison drugs.

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Monza, Italy

Alberto Milanese