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

Farmitalia Carlo Erba

Windtree Therapeutics, Inc.

Rostaquo S.p.a.

Cvie Therapeutics Limited

Seismic Pharmaceuticals

Patrizia Ferrari

Giuseppe Bianchi

Alberto Cerri

Piero Melloni

Mauro Gobbini

Mara Ferrandi

Luigi Bernardi

Marco Torri

Luisa Quadri

Loredana Valentino

Paolo Barassi

Gabriella Traquandi

Sergio Mantegani

Aldemio Temperilli

Laura Chiodini

Elena Folpini

Maria Pia Zappavigna

Giorgio Fedrizzi

Marco Frigerio

Nicoletta Almirante

Giulio Carzana

Carlotta Ronchi

Antonio Zaza

Marcella Rocchetti

Leonardo Banfi

Daniel Ruggieri

Walter Cabri

Marco Santagostino

Daniela Ruggieri

Rosamaria Micheletti

Sergio De Munari

Simona Sputore

Silvia Armaroli

Giuseppe Marazzi

Tiziana Cova

Eleonora Torre

Francesco Peri

Andrea Luraghi

Giusseppe Bianchi

Shih-Che Hsu

Alessandra Benicchio

Marco Pozzi

Fabio Macciardi

Giuseppe Giacalone

Maco Torri

Giuliana Salani

Barbara Moro

Piero Enrico Scotti

Maria Luisa Quadri

Rosamaria Michaeletti

Francesco Rossi

Marilena Cipollaro

Liberato Berrino

Antonio Cascino

Amalia Forte

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

Methods and systems are provided herein that are based on the effects of genetic variations on the biological activities associated to rostafuroxin in an individual. In particular, compositions, methods and systems are herein described that are based on an indentified influence on an individual response to rostafuroxin of one or more polymorphisms in an intergenic or intragenic region of a gene selected from the group consisting of KCNS3, THSD7A, FAM46A, LOC389970, HLA-G, and TTC29, and/or a genetic variation in linkage disequilibrium therewith.

Methods and systems for pharmacogenomic treatment of cardiovascular conditions

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

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

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

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

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Varese, Italy

Patrizia Ferrari