МИЛН Джилл К. (US),ДЖИРОУСЕК Майкл Р. (US),БЕМИС Джин Э. (US),ВУ Чи Б. (US)
申请号：
RU2012112461/04
公开号：
RU2012112461A
申请日:
2010.08.31
申请国别(地区):
RU
年份:
2013
代理人:
摘要：
1. A molecular conjugate containing niacin and a fatty acid selected from omega-3 fatty acids or fatty acids that are metabolized in vivo to omega-3 fatty acids, where the conjugate contains at least one amide. A compound of Formula I or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, enantiomer or stereoisomer thereof； wherein each of R, R and R is independently selected from the group consisting of —H, —D, —Cl, —F, —CN, —NH, - NH (C-C1-6alkyl), -N (C-C1-6alkyl), -NH (C (O) C-C1-6alkyl), -N (C (O) C-C1-6alkyl), -C (O) H, -C (O ) C-C1-6alkyl, -C (O) OC-C1-6alkyl, -C (O) NH, -C (O) NH (C-C1-6 alkyl), -C (O) N (C-C1-6 alkyl), -C-C1-6alkyl, -OC-C1-6alkyl, -S (O) C-C1-6alkyl and -S (O) C-C1-6alkyl； each of W and W independently represents zero, O, S, NH, NR or W and W together may form an imidazolidine or piperazine group, provided that W and W cannot simultaneously represent O； each a, b, c, and d independently represents —H, —D, —CH, —OCH, —OCHCH, or —C (O) OR, —OZ or benzyl, or two of a, b, c, and d, together with the single carbon atom to which they are attached, they can form a cycloalkyl or heterocycle； each n, o, p and q are independently 0 or 1； each L is independently -O-, -S-, -S (O) - , -S (O) -, -SS-, or each g is independently 2, 3, or 4； each h is independently 1, 2, 3, or 4； each R is independently H or C-C1-6 alkyl or both R groups together with a nitrogen atom to which they are attached may form a heterocycle； to each R independently is e, B, or a straight or branched C-C1-6 alkyl which may optionally be substituted by OH, NH, COR, CONH, phenyl, CHOH, imidazole or arginine； each e independently represents H or any of the side chains of natural amino acids； each Z independently represents —H or1. Молекулярный конъюгат, содержащий ниацин и жирную кислоту, выбранную из омега-3 жирных кислот или жирных кислот, которые метаболизируются in vivo до омега-3 жирных кислот, где конъюгат содержит по меньшей мере один амид.2. Соединение Формулы Iили
