NEPRILYSIN INHIBITORS Russian patent published in 2016 - IPC C07C281/02 C07D231/14 C07D231/20 C07D231/22 C07D231/40 C07D237/24 C07D239/28 C07D239/34 C07D239/36 C07D239/52 C07D239/54 C07D249/04 C07D249/08 C07D249/10 C07D249/12 C07D249/18 C07D257/04 C07D261/04 C07D261/18 C07D263/34 C07D263/38 C07D277/56 C07D401/04 C07D401/06 C07D403/04 C07D403/06 C07D413/04 C07D471/04 A61K31/41 A61K31/415 A61K31/50 A61K31/505 A61K31/4192 A61K31/4196 A61K31/421 A61K31/426 A61K31/4427 A61K31/497 A61P13/12 

FIELD: chemistry.

SUBSTANCE: invention relates to a compound of formula I, where R¹ is -OR⁷; R² is H; X is selected from a pyrazole, triazole, benzotriazole, tetrazole, oxazole, isoxazole, thiazole, pyridazine, pyrimidine and pyridyl triazole; R³ is absent or is selected from H; halogen; -C_0-5alkylene-OH; -C_1-6alkyl; -C_3-7cycloalkyl; -C_0-2alkylene-O-C_1-6alkyl; -C(O)R²⁰; -C_0-1alkylene-COOR²¹; -C(O)NR²²R²³; -NHC(O)R²⁴; =O; phenyl, optionally substituted with one or two groups independently selected from halogen, -OCH₃, -NHC(O)CH₃ and phenyl; naphthalenyl; pyridinyl; pyrazinyl; and R³, when present, is bonded to carbon atom; R⁴ is selected from H; -OH; -C_1-2alkylene-COOR³⁵; -pyridinyl; and phenyl or benzyl, optionally substituted by one or more groups selected from halogen and -OCH₃; and R⁴, when present, is bonded to carbon atom or a nitrogen atom; a equals 0 or a equals 1; and R⁵ is selected from halogen and -CN; b is equal to 0 or 1, and R⁶ is selected from Cl, F, -OH, -CH₃, -OCH₃ and -CF₃; or b is equal to 2, and R⁶ each is independently selected from halogen, -OH, -CH₃, or -OCH₃, or b is equal to 3, and R⁶ each is independently selected from halogen or -CH₃; R⁷ is selected from H, -C_1-8alkyl, -C_1-3alkylene-C_6-10aryl, -C_0-6alkylene morpholinyl or dioxol-2-one methyl, of formula (a); or a pharmaceutically acceptable salt thereof. Compounds of formula (I) are obtained by condensation of compound of formula 1 with a compound of formula 2, where P¹ is H or tert-butoxycarbonyl; and wherein method further includes removal of protective group of compound of formula 1, when P¹ is tert-butoxycarbonyl. Also compound of formula (I) is obtained by removing protective group of compound of formula (6) or salt thereof; where R^1P is -O-P³, where P³ is methyl. Invention also relates to intermediate compounds of formulae (1) and (6). Compounds of formula (I) are intended for inhibiting neprilysin activity.

EFFECT: compounds having neprilysin inhibiting activity.

19 cl, 9 ex

,(а), ,