NEPRILYSIN INHIBITORS Russian patent published in 2018 - IPC C07D231/14 C07D231/20 C07D249/04 C07D261/18 C07D263/38 C07D405/12 A61K31/415 A61K31/4192 A61K31/42 A61K31/421 A61P9/04 A61P9/12 A61P13/12 

Abstract RU 2650114 C2

FIELD: medicine; pharmaceuticals.

SUBSTANCE: invention relates to a compound of formula IIa or IIb

, in which a) Ra and Rb are H; and R2 is H; and R7 is -CH2CF2CH3 or -CH2CF2CF3; or R2 is -C1-6alkyl or -C(O)-C1-6alkyl and R7 is H; or b) Ra is selected from -CH3, -OCH3 and Cl and Rb is H; or Ra is selected from H, -CH3, Cl and F and Rb is Cl; or Ra is H and Rb is selected from -CH3 and -CN; and R2 is selected from -C1-6alkyl and -(CH2)2-3OH and R7 is selected from H and -C1-6alkyl; or c) Ra is H and Rb is F; or Ra is F and Rb is H; R2 is selected from -C1-6alkyl and -(CH2)2-3OH; and R7 is selected from H and -C1--6alkyl. Invention also relates to a compound of formula III, a compound of formula V, to an individual compound, to a compound of formula VIa or VIb, to a compound of formula VIIa or VIIb, to a pharmaceutical composition, having neprilysin (NEP) inhibition activity, to the use of the compound.

EFFECT: technical result is obtaining novel compounds having neprilysin (NEP) inhibition activity and which can be used in the treatment of hypertension, heart failure or kidney disease.

13 cl, 8 ex

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RU 2 650 114 C2

Authors

Fleri Melissa

Khyuz Adam D.

Dates

2018-04-09Published

2013-08-07Filed