Mineralocorticoid receptor antagonists

Details Mineralocorticoid receptor antagonists Mineralocorticoid receptor antagonists

A - Human Necessities

61

K

A61K 31/56 (2006.01) A61P 5/42 (2006.01) C07J 7/00 (2006.01)

Patent

CA 2680533

Compounds of the formula (I) are provided having a steroid skeleton and substitution characteristics in the A and B rings of the steroid skeleton effective for mineralocorticoid receptor antagonism, and rings C and D of the steroid skeleton having substituents thereon according to formula (I), wherein R1 is -OH or =O; R2 is (C1-3)alkyl or (C2- 3)alkenyl; R3 is selected from formulas (IIa), (IIb), (IIc).These compounds are useful in the treatment of inter alia aldosteronism, hypokalemia, hypertension, congestive heart failure, heart fibrosis, renal failure and restenosis.

L'invention concerne des composés de formule (I) qui sont fournis en ayant un squelette stéroïde et des caractéristiques de substitution dans les cycles A et B du squelette stéroïde efficaces pour l'antagoniste de récepteurs de minéralocorticoïdes, et des cycles C et D du squelette stéroïde ayant des substituants selon la formule (I), où R1 est -OH ou =O; R2 est un alkyle (C1-3) ou un alcynyle (C2- 3); R3 est sélectionné parmi (Iia, Iib, Iic). Ces composés sont utiles dans le traitement de, entre autre, l'hyperaldostéronisme, l'hypokaliémie, l'hypertension artérielle, l'insuffisance cardiaque congestive, la fribose cardiaque, l'insuffisance rénale et la resténose.

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