Cvie Therapeutics Limited

Seismic Pharmaceuticals

Windtree Therapeutics, Inc.

Marcella Rocchetti

Patrizia Ferrari

Alberto Cerri

Mara Ferrandi

Carlotta Ronchi

Antonio Zaza

Giuseppe Bianchi

Paolo Barassi

Shih-Che Hsu

Eleonora Torre

Giusseppe Bianchi

Andrea Luraghi

Francesco Peri

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

Growing community of inventors

Brugherio, Italy

Marcella Rocchetti