ORAL COMPOSITIONS OF CARDIAC SARCOMERE INHIBITORS Russian patent published in 2024 - IPC A61K31/4245 A61K31/415 A61K9/28 A61P9/04 

FIELD: medicine; pharmaceutics.

SUBSTANCE: group of inventions relates to pharmaceutics and can be used to treat cardiac diseases. Disclosed is a cardiac sarcomere inhibiting composition containing (R)-N-(5-(5-ethyl-1,2,4-oxadiazol-3-yl)-2,3-dihydro-1H-inden-1-yl)-1-methyl-1H-pyrazole-4-carboxamide or its hydrate, solvate, polymorph or its pharmaceutically acceptable salt, filler, binder, baking powder, surfactant and lubricant. Disclosed is a tablet containing a core comprising an intragranular component containing (R)-N-(5-(5-ethyl-1,2,4-oxadiazol-3-yl)-2,3-dihydro-1H-indene-1-yl)-1-methyl-1H-pyrazole-4-carboxamide or its hydrate, solvate, polymorph or its pharmaceutically acceptable salt, filler, binder, disintegrant and surfactant, as well as extragranular component containing filler, disintegrant and lubricant. Group of inventions also relates to a method of producing said tablet, a method of treating heart disease, which is hypertrophic cardiomyopathy (HCM) or heart failure with preserved ejection fraction (HFpEF), as well as to use of said composition or tablet for preparing a medicament for treating said heart disease.

EFFECT: invention provides reduction of cardiac sarcomere hypercontraction, reduces activity of ATPase of cardiac myosin and thus reduces contractility of cardiomyocytes.

42 cl, 3 dwg, 9 tbl, 12 ex