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COMPOUNDS AND METHODS FOR INHIBITING AN NHE-MEDIATED ANTI-PORT IN THE TREATMENT OF DISORDERS ASSOCIATED WITH DELAY OF LIQUID OR SALT OVERLOAD AND DISEASES OF THE GASTROINTESTINAL TRACT
专利权人:
ЭРДЕЛИКС ИНК. (US)
发明人:
ЛИДБЕТТЕР Майкл (US),БЭЛЛ Ной (US),ЛЬЮИС Джейсон (US),ДЖЕЙКОБС Джеффри (US),КАРРЕРАС Кристофер (US)
申请号:
RU2015107019
公开号:
RU2015107019A
申请日:
2013.08.20
申请国别(地区):
RU
年份:
2016
代理人:
摘要:
1. A compound having the following structure of formula (I): or a stereoisomer, prodrug or pharmaceutically acceptable salt thereof, wherein: (a) n is an integer of 2 or more; (b) Core is a core moiety having two or more sites on it to attach two or more NHE-inhibiting low molecular weight groups; (c) L is a bond or linker connecting said crustal group to said two or more NHE-inhibiting low molecular weight groups; and (d) NHE (Na + / H + exchanger) is an NHE-inhibiting low molecular weight moiety having the following structure of formula (XI): wherein: B is selected from the group consisting of aryl and heterocyclyl; each R is independently selected from the group consisting of hydrogen , halogen, possibly substituted Ci-alkyl, possibly substituted Ci-alkoxy, possibly substituted Cioalkyl, possibly substituted heterocyclyl, possibly substituted heterocyclylalkyl, possibly substituted aryl, possibly substituted heteroaryl, hydroxyl, oxo, cyano, nitro, -NRR, -NRC (= O) R, -NRC (= O) OR, -NRC (= O) NRR, -NRSOR, -NRS (O) NRR, -C (= O) OR, -C (= O) R, -C (= O) NRR, -S (O) R and -SONRR, where R, R and R are independently selected from a group consisting of hydrogen, C1-6 alkyl or a bond joining an NHE-inhibiting low molecular weight group to L, provided that at least one of them is a bond joining an NHE-inhibiting low molecular weight group to L; R and R are independently selected from the group consisting of hydrogen, possibly substituted C1-6 alkyl, possibly substituted cycloalkyl, possibly substituted cycloalkylalkyl, possibly substituted aryl, possibly substituted aralkyl, but substituted heterocyclyl and optionally substituted heteroaryl; or R and R form together with the nitrogen to which they are bound, possibly1. Соединение, имеющее следующую структуру формулы (I):или его стереоизомер, пролекарство или фармацевтически приемлемая соль,где:(а) n равен целому числу 2 или более;(б) Core представляет собой коровую группировку, имеющую два или более сайтов на ней для п
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