Montedison S.p.a.

Consiglio Nazionale Delle Ricerche

Farmitalia Carlo Erba S.p.a.

Alfa Wassermann S.p.a.

Biochimica Opos Spa

Farmabios S.r.l.

Biochimica Ops Spa

Gianfranco Cainelli

Marco Da Col

Michele Contento

Mauro Panunzio

Leone Dall'Asta

Sergio Sandri

Achille Umani Ronchi

Enrico Di Salle

Egidio Marchi

Aldo Roda

Marco Foa'

Andrea Gardano

Silvano Piani

Giuliano Nannini

Maria R Milani

Irene Resta

Achille Umani-Ronchi

Achille U Ronchi

Giuseppe Spunta

Giorgio Martelli

Described herein is the isomerisation process of 6&bgr;-fluorosteroids into the corresponding pharmacologically active 6&agr;-fluoro derivatives, comprising the reaction of 6&bgr;-fluorosteroids, or 6&agr;/6&bgr; isomeric mixtures, with an organic base containing a diazoimino group in a suitable organic solvent.

Isomerisation of 6&bgr;-fluorosteroids into the corresponding 6&agr;-fluoro derivatives

The present invention refers to process for the preparation of a tiazoline-azetidinone of formula I ##STR1## which comprises N-protecting in position 1 of (3S,4S)-3-phenylace tamido-4-acetoxy-azetidin-2-one, converting the product thus obtained into the corresponding thioamide and subsequently ciclyzing and deprotecting.

Process for the preparation of a thiazoline-azetidinone

An amide of formula ##STR1## and its pharmacologically acceptable organic or inorganic salt shows a metabolic stability, both enteric and hepatic, greater than that of the corresponding bile acids conjugated with glycine or taurine physiologically present in the enterohepatic circulation. The pharmacological activity of the compounds of formula I or their pharmacologically acceptable organic or inorganic salt makes the use effective for the therapy of biliary calculosis from cholesterol and in every pathology caused by cholestasis like chronic hepatitis from cholestasis, primitive biliary cirrhosis and juvenile hepatopathy associated with cystic fibrosis.

Bile acids derivatives useful in the therapy of the biliary calculosis

There is described the preparation of halogenated .beta.-lactam derivatives by introduction of a chlorine atom in the 3-position of the cephem nucleus starting from a 3-sulfonyloxycephem. Such starting materials are reacted with a chlorine ions donor in a basic medium.

Process for the preparation of halogenated .beta.-lactam compounds

The present invention relates to new 4-aza-17.beta.-substituted 5.alpha.-androstan-3-ones, to a process for their preparation, to pharmacological compostions containing them, and to the use of said compounds as inhibitors of androgen action by means of testosterone 5-reductase inhibition.

Steroidic 5.alpha.-reductase inhibitors

A process is herein described for preparing carboxylated organic compounds (acids, esters, alkaline salts) of formula ##STR1## wherein R is a hydrocarbyl group having up to 11 carbon atoms (an aliphatic, alicyclic, aryl- or heteroarylalkyl group), also substituted, in its turn, by groups inert under the reaction conditions (alkyl, aryl, etheric, thioetheric, halogen, nitrile, ester, amide, ketonic groups), and R' is a hydrogen atom or an alkyl C.sub.1 -C.sub.8 group, by reaction of carbon monoxide with the corresponding hydrocarbyl halides, having the halogen bound to a non-tertiary carbon atom, in the presence of catalysts which are salts of cobalt hydrocarbonyl, or precursors thereof, in a hydro-alcoholic or alcoholic solvent and in the presence of bases. The process is characterized in that the catalytic system composed by the salt of cobalt hydrocarbonyl is supported on an anion exchange resin. The process permits to operate also continuously, in any case allowing an easy recovery, recycle and regeneration of the catalysts. The products obtained, i.e. carboxylic acids, esters and alkaline salts thereof, are utilized as intermediates for organic syntheses particularly for fine chemistry (phytopharmaceuticals, pharmaceuticals, etc.).

Process for preparing carboxylated organic compounds

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Bologna, Italy

Gianfranco Cainelli