SMIT Kameron (US),СМИТ Камерон (US),FLERI Melissa (US),ФЛЕРИ Мелисса (US),GENDRON Roland (US),ГЕНДРОН Роланд (US),KHADSON Rajan (US),ХАДСОН Райан (US),KHJUZ Adam D. (US),ХЬЮЗ Адам Д. (US)
申请号：
RU2013132524/04
公开号：
RU0002605557C2
申请日:
2011.12.14
申请国别(地区):
RU
年份:
2016
代理人:
摘要：
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； -C0-5alkylene-OH； -C1-6alkyl； -C3-7cycloalkyl； -C0-2alkylene-O-C1-6alkyl； -C(O)R20； -C0-1alkylene-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； -C1-2alkylene-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, -C1-8alkyl, -C1-3alkylene-C6-10aryl, -C0-6alkylene 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 R1P 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), ,Изобр
