49643-95-0Relevant academic research and scientific papers
ANDROSTANE DERIVATIVES WITH ACTIVITY AS PURE OR PREDOMINANTLY PURE STIMULATORS OF SERCA2A FOR THE TREATMENT OF HEART FAILURE
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Paragraph 0149-0150; 0259; 0263-0264, (2021/04/16)
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+/K+ ATPase. 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.
ISTAROXIME-CONTAINING INTRAVENOUS FORMULATION FOR THE TREATMENT OF ACUTE HEART FAILURE (AHF)
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Paragraph 128-129; 138, (2020/09/19)
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.
Structure-based design and synthesis of novel potent Na+,K +-ATPase inhibitors derived from a 5α,14α-androstane scaffold as positive inotropic compounds
De Munari, Sergio,Cerri, Alberto,Gobbini, Mauro,Almirante, Nicoletta,Banfi, Leonardo,Carzana, Giulio,Ferrari, Patrizia,Marazzi, Giuseppe,Micheletti, Rosella,Schiavone, Antonio,Sputore, Simona,Torri, Marco,Zappavigna, Maria Pia,Melloni, Piero
, p. 3644 - 3654 (2007/10/03)
The design, synthesis, and biological properties of novel inhibitors of the Na+,K+-ATPase as potential positive inotropic compounds are reported. Following our model of superposition between cassaine and digitoxigenin, digitalis-like
