Lark S.p.a.

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Pierrel Spa

Sicor Societa 'italiana Corticosteroidi S.p.a.

Gaetano Palladino

Mario Riva

Peter MacDonald

Ettore Bigatti

Lucian Toscano

Mario Micciarelli

An improved process for the preparation of doxorubicin, by means of hydrolysis of a doxorubicin ester of a dicarboxylic acid, in acid medium.

Process for the conversion of daunorubicin into doxorubicin

New 16,17-pyrazolino- and 16,17-isopyrazolino-1,4-pregnadiene-derivatives have been prepared, useful as antiinflammatory agents on topical and/or systemic administration. An analogy process for the preparation of 16,17-pyrazolino-1,4-pregnadiene derivatives and the quite surprising conversion of the latter ones to 16,17-isopyrazolino-1,4-pregnadiene derivatives are also disclosed. The results of pharmacological comparative trails of some new products of the present invention v. fluocinolone acetonide are reported.

16,17-Pyrazolino- and 16,17-isopyrazolino-1,4-pregnadiene derivatives

Novel steroids are described together with processes of making them and pharmaceutical compositions containing them. The steroids have pharmaceutical activity, especially anti-inflammatory activity. They are all 2-Bromo-6.beta.-fluoro-pregna-1,4-diene-3,20-diones.

Steroids and process for preparing the same

Pregnane series steroids are disclosed having good anti-inflammatory and anti-rheumatoid arthritic activity with a decreased degree of side effects, e.g., weight loss and sodium retention. The compounds have the formula ##STR1## where X is a keto- or .beta.-hydroxyl group or chlorine, Y is fluorine or chlorine, Z is hydrogen, .alpha.-hydroxyl, .alpha.-methyl or .beta.-methyl, R' is hydrogen or a 2 to 8 carbon acyl group and R is hydrogen, a 2 to 8 carbon acyl group from mono- or di-carboxylic organic acids, a metasulfobenzoic acid residue or phosphoric acid residue. When R' is hydrogen, and Z is .alpha.-hydroxyl the corresponding 16.alpha., 17.alpha.-acetonides and 16.alpha.-acyl derivatives with organic carboxylic acids having from 2 to 8 carbon atoms were prepared.

2-Bromo-6.beta.-fluoro-3-keto-.DELTA..sup.1,4 -steroids of the pregnane

There is disclosed 16 alpha-methyl-17 alpha-bromo-1,4-pregnadiene-21-ol-3,20-dione-type compounds of the formula ##STR1## where R is hydrogen or acyl; X is hydrogen, bromine, or fluorine; Y is hydrogen or oxygen; and Z is hydrogen or .alpha.- or .beta.-oriented fluorine. The compounds are useful in treating rheumatoid arthritis and related inflammatory disorders as well as allergic diseases.

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Milan, Italy

Gaetano Palladino