Sigma-tau Industrie Farmaceutiche Riunite S.p.a.

Farmitalia Carlo Erba S.p.a.

Farmitalia Carlo Erba

Mauro Gobbini

Patrizia Ferrari

Piero Melloni

Marco Torri

Aldemio Temperilli

Luigi Bernardi

Loredana Valentino

Giuseppe Bianchi

Gabriella Traquandi

Sergio Mantegani

Alberto Cerri

Mara Ferrandi

Luisa Quadri

Laura Chiodini

Giorgio Fedrizzi

Enzo Brambilla

Maria A Cervini

Daniel Ruggieri

Walter Cabri

Marco Santagostino

Marco Frigerio

Daniela Ruggieri

Rosamaria Micheletti

Sergio De Munari

Simona Sputore

Giuseppe Marazzi

Giulio Carzana

Piero Enrico Scotti

Marco Pozzi

Alessandra Benicchio

Roberto Villa

The present invention relates to new diterpenoid derivatives of formula (I), processes for their preparation, and to pharmaceutical compositions containing them for the treatment of cardiovascular disorders, urinary incontinence, asthma, or Alzheimer's disease and/or to prevent obstructive vascular lesions consequently to arteriotomy and/or angioplasty, and to prevent organ damage in hypertensive patients.

Diterpenoid derivatives endowed of biological properties

New aminooxime derivatives at position 3 of 2- and/or 4-substituted androstanes and androstenes, processes for their preparation, and to pharmaceutical compositions containing them for the treatment of cardiovascular disorders, such as heart failure and hypertension. In particular compounds having the general formula (I) are described, where the radicals have the meanings described in detail in the application. 

Aminooxime derivatives of 2- and/or 4-substituted androstanes and androstenes as medicaments for cardiovascular disorders

Compounds of formula (I) wherein: the groups are as defined in the description, are useful for the preparation of medicaments for the treatment of cardiovascular disorders, in particular heart failure and hypertension. The compounds are inhibitors of the enzymatic activity of the Na+, K+-ATPase. They are useful for the preparation of a medicament for the treatment of a disease caused by the hypertensive effects of endogenous ouabain, such as renal failure progression in autosomal dominant polycystic renal disease (ADPKD), preeclamptic hypertension and proteinuria and renal failure progression in patients with adducin polymorphisms. 

Azaheterocyclyl derivatives of androstanes and androstenes as medicaments for cardiovascular disorders

An improved process is described for the preparation of compounds with general formula (I) and particularly for the preparation of the compound (E,Z) 3-(2-aminoethoxyimino)-androstane-6,17-dione, in which n&equals;1 and R &equals;R &equals;H

Process for the preparation of (E,Z) 3-(2-aminoethoxyimino)-androstane-6, 17-dione and its analogues

New seco-D steroid derivatives, processes for their preparation and pharmaceutical compositions are provided, which are active on the cardiovascular system. The seco-D steroid derivatives have the following general formula (I): ##STR1##

Seco-d steroids active on the cardiovascular system, processes for their

Seco-D steroid derivatives having the formula ##STR1## wherein R, R.sup.1, R.sup.2 and R.sup.3 have the meanings specified in the specification, useful as cardiovascular agents and pharmaceutical compositions containing same, are disclosed.

Seco-D steroids active on the cardiovascular system and pharmaceutical

An improvement in a process for producing 3.beta.,14.beta.-dihydroxyethianaldehyde is disclosed wherein the oxidation of the lactone ring of digitoxigenin-3-acetate is conducted with an alkaline periodate in the presence of a catalytic amount of ruthenium tetroxide obtained in situ by reacting RuO.sub.2 hydrate or RuCl.sub.3 with the alkaline periodate.

Process for the preparation of 3 .beta., 14

Cyclopentanperhydrophenantren-17.beta.-(3-furyl)-3-derivatives and pharmaceutical compositions containing same for the treatment of cardiovascular disorders such as heart failure and hypertension, are disclosed.

Cyclopentanperhydrophenanthren-17.beta.-(3-furyl)-3-derivatives and

The present invention relates to new cyclopentanperhydrophenanthren-17-(hydroxy or alkoxy)-17-(aryl or heterocyclyl)-3.beta.-derivatives, active on the cardiovascular system, to a process for their preparation and to pharmaceutical compositions containing them. The invention relates to compounds of general formula (I) ##STR1## wherein X is O or S and R, R.sup.1 and R.sup.2 is selected from various groups.

Cyclopentanperhydrophenanthren-17.beta.-(hydroxy or

14-Deoxy-14.alpha.-cardenolides 3.beta.-thioderivatives and pharmaceutical compositions comprising same for treating cardiovascular disorders, such as heart failure and hypertension, are disclosed.

14-deoxy-14.alpha.-cardenolides 3.beta.-thioderivatives and

Digitoxigenin and dihydrodigitoxigenin 3.beta.-derivatives, a process for their preparation and pharmaceutical compositions containing same for the treatment of cardiovascular disorders such as heart failure and hypertension are disclosed.

Digitoxigenin and dihydrodigitoxigenin 3.beta.-derivatives and

t-alkyl eroline derivatives of formula I are produced ##STR1## wherein (R.sub.1 =H, OCH.sub.3 and R.sub.2 H) or (R.sub.1 +R.sub.2 =a ring bond and R.sub.3 =H, optionally substituted nicotinynoyl or 1-oxo-2-cyclopenten-3-yl); and their pharmaceutically acceptable salts. A process for the preparation of these derivatives from lysergol and a t-alkyl alcohol is also described, as are pharmaceutical compositions containing them.

t-alkyl ergoline derivatives

##STR1## Compounds I [R.sub.1 =H or C.sub.1 -C.sub.3 alkyl, R.sub.2 =an (alkyl-substituted) aminodeoxy or aminodideoxy or aminotrideoxy sugar residue of the D and L series, the glycosidic linkage being .alpha. or .beta.] and their pharmaceutically acceptable salts are useful as antihypertensive agents. Their preparation and use as well as pharmaceutical compositions containing them are also described.

Aminoglycoside steroids, a process for their preparation, their use and

##STR1## Compounds I (either R.sub.1 =OH, C.sub.1 -C.sub.4 alkoxy and R.sub.2 =H, C.sub.1 -C.sub.4 alkyl, or R.sub.1 +R.sub.2 =a chemical bond; R.sub.3 =an aminodeoxy or aminodideoxy or aminotrideoxy sugar residue of the D and L series, the glycosidic linkage being .alpha. or .beta.: and either R.sub.4 =OH and R.sub.5 =H or R.sub.4 +R.sub.5 =a chemical bond) and their pharmaceutically acceptable salts are useful as antihypertensive agents. Their preparation and use as well as pharmaceutical compositions containing them are also described.

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Mercallo, Italy

Mauro Gobbini