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

Rostaquo S.p.a.

Cvie Therapeutics Limited

Seismic Pharmaceuticals

Windtree Therapeutics, Inc.

Alberto Cerri

Patrizia Ferrari

Giuseppe Bianchi

Piero Melloni

Mara Ferrandi

Marco Torri

Elena Folpini

Luigi Bernardi

Marco Santagostino

Nicoletta Almirante

Mauro Gobbini

Maria Pia Zappavigna

Luisa Quadri

Silvia Armaroli

Giulio Carzana

Giorgio Fedrizzi

Marcella Rocchetti

Carlotta Ronchi

Antonio Zaza

Leonardo Banfi

Walter Cabri

Marco Frigerio

Rosamaria Micheletti

Giuseppe Marazzi

Paolo Barassi

Simona Sputore

Gloria Padoani

Shih-Che Hsu

Giusseppe Bianchi

Andrea Luraghi

Francesco Peri

Eleonora Torre

Maria Luisa Quadri

Monica Florio

Tiziana Cova

Giuseppe Giacalone

Maco Torri

Barbara Moro

Piero Enrico Scotti

Marco Pozzi

Alessandra Benicchio

Rosamaria Michaeletti

Shin-Che Hsu

Compounds and compositions for the activation of SERCA2a are disclosed. In particular, provided are compounds that act as predominantly pure or pure SERCA2a activators while only moderately inhibiting the Na/KATPase. In general, the disclosed compounds are derivatives of androstane having the formula (I). Also disclosed herein are pharmaceutical compositions comprising one or more of the compounds of formula (I) for use for the treatment of heart failure.

Androstane derivatives with activity as pure or predominantly pure stimulators of SERCA2a for the treatment of heart failure

Disclosed are compounds of formula (I), wherein X, Y, Z are annular atoms comprised in a five-membered carbocyclic or heterocyclic ring, selected from the group consisting of CH, NH, N, O, S; said carbocyclic or heterocyclic ring being optionally substituted with amino (C-C) linear or branched alkyl or guanidine or guanidino (C-C) linear or branched alkyl; with the proviso that the heterocycle ring is not furyl; n is 0 or 1; R is H or OH; the dotted line represents an optional double bond C&#x2550;C; the thick line represents a bond in the &#x3b2; configuration; the wavy line represents a bond both in the &#x3b1; and &#x3b2; configuration; their enantiomeric and/or diastereomeric mixtures, their pharmaceutically acceptable salts, their solvates, hydrates; their metabolite and metabolic precursors. The compounds of formula (I) are for use as medicaments, in particular for the treatment of acute or chronic heart failure. Oral administration is also possible.

17beta-heterocyclyl-digitalis like compounds for the treatment of heart failure

New crystalline forms of 17&#x3b2;-(3-Furyl)-5-&#x3b2;androstane-3&#x3b2;,14&#x3b2;,17&#x3b1;-triol are described together with pharmaceutical composition containing the same and methods for their preparation. In particular new Forms B, C, D, E and H are here described.

Crystalline rostafuroxin

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. Said compounds are used 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. 

Amino derivatives of 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

New aminoalkoxyimino derivatives at position 3 of substituted B-homoandrostanes and B-heteroandrostanes, 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.

Amino derivatives of beta-homoandrostanes and beta-heteroandrostanes

An inner salt of L-carnitine is prepared by reduction, with a suitable reducing agent, of a compound of formu (I): where Xand X, which may be the same or different, are hydroxy, C-Calkoxy, phenoxy, halogen, or Xand X, when taken together are an oxygen atom and the resulting compound is a derivative of succinic anhydride; Y is halogen, a mesyloxy or a tosyloxy group, and subsequent treatment with water, then with a base and then with trimethylamine.

Process for preparing R-(-)carnitine from S-(-)-chlorosuccinic acid or from a derivative thereof

An inner salt of L-carnitine is prepared by reduction, with a suitable reducing agent, of a compound of formula (I):where Xand X, which may be the same or different, are hydroxy, C&#x2013;Calkoxy, phenoxy, halogen, or Xand X, when taken together are an oxygen atom and the resulting compound is a derivative of succinic anhydride; Y is halogen, a mesyloxy or a tosyloxy group, and subsequent treatment with water, then with a base and then with trimethylamine.

Process for preparing R-(&#x2212;)-carnitin from S-(&#x2212;)-chlorosuccinic acid or from a derivative thereof

Process for preparing R-(-) -carnitine from S-(-)-chlorosuccinic acid or from a derivative thereof

Novel 17-hydroxyiminoalkyl and 17-hydroxyiminomethylalkenyl steroids of the general formula (I) ##STR1## where A, R.sup.1 and R.sup.2 are defined in the specification are disclosed. The compounds have cardiovascular activity. Pharmaceutical compositions containing compounds of formula (I) are also disclosed for the treatment of heart failure and hypertension.

17-hydroxyiminoalkyl and 17-hydroxyiminomethylalkenyl

1,5-Disubstituted 5a-methylperhydroinden-3a-ol derivatives of formula (I): ##STR1## where either

1,5-disubstituted 7A-methylperhydroinden-3A-ol derivatives, useful in

New 17-�3-imino-2-alkyl propenyl!-14.beta.-hydroxy-5.beta.-androstane derivatives active on the cardiovascular system by inhibiting Na+,K+-ATPase, a process for their preparation, and to pharmaceutical compositions for the treatment of cardiovascular disorders, such as heart failure and hypertension.

17-(3-imino-2-alkylpropenyl)-5.beta., 14.beta.-androstane derivatives

The invention describes hydrazino and hydroxyamino-14.beta.-hydroxyandrostane derivatives having general formula (I): ##STR1## wherein the symbol means .alpha. or .beta. configuration and A, B, R.sup.1, R.sup.2, R.sup.3, and R.sup.4 have the meanings given in the description and their use in the treatment of cardiovascular disorders such as heart failure and hypertension.

Hydrazino and hydroxyamino-14-.beta.-hydroxyandrostane derivatives

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Milan, Italy

Alberto Cerri