14-deoxy-14.alpha.-cardenolides 3.beta.-thioderivatives and pharmaceutical composition comprising same for treating cardiovascular disorders
AssigneeSigma-Tau Industrie Farmaceutiche Riuntie S.p.A
InventorsMauro Gobbini, Luigi Bernardi, Mara Ferrandi, Piero Melloni, Luisa Quadri, Roberto Villa
Life of this patent
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Abstract
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.
Claims19
14-deoxy-14.alpha.-cardenolides 3.beta.-thioderivatives, having formula (I):
- ##STR6## wherein:
- the symbol --- represents a single or a double bond;
- R is C2-C6 alkyl or C3-C6 alkenyl, substituted by a 2-(2-imidazolinyl) group or one or more OR1 or NR2R3 or C(NH)NR4R5;
- wherein:
- R1 is C2-C4 alkyl substituted by NR6R7;
- R2, R3 are independently C2-C6 alkyl substituted by NR6R7 or R2 and R3 taken together with the nitrogen atom form an unsubstituted or substituted saturated or unsaturated heteromonocylic ring optionally containing another heteroatom chosen from oxygen or sulfur or nitrogen;
- R4, R5 taken together with the nitrogen atom form a penta- or hexa-monoheterocyclic ring;
- R6, R7 taken together with the nitrogen atom form a saturated or unsaturated penta- or hexa-monoheterocyclic ring optionally containing another heteroatom chosen from oxygen or sulfur or nitrogen, or the pharmaceutically acceptable salts thereof.
A pharmaceutical composition comprising a compound of formula (I) or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier and/or diluent thereof.
An orally or parenterally administrable pharmaceutical composition for the treatment of cardiovascular disorders comprising an effective amount of a compound of formula (I) or an equivalent amount of a pharmaceutically acceptable salt thereof and an excipient therefor.
A compound according to claim 19, wherein R4 and R5 taken together with the nitrogen atom form a penta-monoheterocyclic ring.
Dependencies are inferred from the claim text.