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

Windtree Therapeutics, Inc.

Cvie Therapeutics Limited

Seismic Pharmaceuticals

Mara Ferrandi

Patrizia Ferrari

Giuseppe Bianchi

Alberto Cerri

Piero Melloni

Marco Frigerio

Paolo Barassi

Luigi Bernardi

Mauro Gobbini

Luisa Quadri

Marco Torri

Marina Mauro

Marcella Rocchetti

Carlotta Ronchi

Antonio Zaza

Nicoletta Almirante

Loredana Valentino

Giulio Carzana

Maria Pia Zappavigna

Leonardo Banfi

Francesco Peri

Tiziana Cova

Eleonora Torre

Roberto Villa

Shih-Che Hsu

Barbara Moro

Maco Torri

Giusseppe Bianchi

Andrea Luraghi

Giuseppe Giacalone

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

Compositions for intravenous infusion of istaroxime, or a metabolite of istaroxime, in human patients suffering from heart failure are disclosed. Likewise, methods for extended infusion of istaroxime or its metabolites in individuals with heart failure are disclosed. In particular, some methods disclosed herein include the infusion of istaroxime, or a metabolite thereof, for a period of time that is greater than six hours in order to improve cardiac relaxation without triggering arrhythmogenic events in an individual suffering from heart failure. Other methods include administration of istaroxime until certain plasma concentration thresholds of istaroxime metabolites are achieved. Also disclosed are istaroxime metabolites with selective SERCA2a activation.

Istaroxime-containing intravenous formulation for the treatment of acute heart failure (AHF)

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

Compound of formula (I), wherein the symbol have the meaning reported in the text; for preparing a medicament for the prevention and/or treatment of proteinuria, glomerulosclerosis or renal failure.

5-&#x3b2;, 14-&#x3b2;-androstane derivatives useful for the treatment of proteinuria, glomerulosclerosis and renal failure

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 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

17-Aryl -5.alpha.,14.beta.-androstane, androstene and androstadiene derivatives of formula (I): ##STR1## wherein the symbol --- represents a single or a double bond; when the double bond is not present in the 4 or 5 position, the hydrogen in position 5 has the .alpha. configuration; Y is oxygen or guanidinoimino, when --- in position 3 is a double bond; Y is hydroxy, OR.sup.2 or SR.sup.2, when in position 3 is a single bond and has an .alpha. or .beta. configuration; R is a substituted or unsubstituted aryl ring; and R.sup.1 is hydrogen, methyl, ethyl or n-propyl substituted by OH or NR.sup.4 R.sup.5.

17-aryl and 17-heterocyclyl-14.beta.-5.alpha.-androstane, androstene and

17-Heterocyclyl-5.alpha.-14.beta.-androstane, androstene and androstadiene of formula (I): ##STR1## wherein: Y is oxygen or guanidinoimino, when a double bond exists at position 3; Y is hydroxy, OR.sup.2 or SR.sup.2, when a single bond exists at position 3; R is a saturated or unsaturated mono- or biheterocyclic ring, containing one or more heteroatoms selected from the group consisting of oxygen, sulfur, and nitrogen, unsubstituted or substituted by one or more of halogen, hydroxymethyl, alkoxy, amino, alkylamino, dialkylamino, cyano, nitro, sulfonamido, C.sub.1 -C.sub.6 lower alkyl or COR.sup.3 ; and R.sup.1 is hydrogen, methyl, ethyl or n-propyl substituted by OH or NR.sup.4 R.sup.5.

17-heterocyclyl-14beta-5alpha-androstane, androstene and androstadiene

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

A therapeutical method for treating hypertension is disclosed which comprises administering to a patient in need thereof an effective amount of an imino derivative of 3.beta., 14.beta.-dihydroxyetianaldehyde, particularly 17.beta.-guanidinoiminomethyl-5.beta.-androstan-3.beta.,14.beta.-diol.

Therapeutical method for the treatment of hypertension

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Milan, Italy

Mara Ferrandi