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    Alpha-substituted omega-3 lipids that are activators or modulators of the peroxisome proliferators-activated receptor (PPAR)
    4.
    发明授权
    Alpha-substituted omega-3 lipids that are activators or modulators of the peroxisome proliferators-activated receptor (PPAR) 有权
    作为过氧化物酶体增殖物激活受体（PPAR）的活化剂或调节剂的α-取代的ω-3脂质

    公开(公告)号：US08399516B2

    公开(公告)日：2013-03-19

    申请号：US12446615

    申请日：2007-11-01

    申请人： Morten Bryhn ,  Anne Kristin Holmeide ,  Jenny Rosman

    发明人： Morten Bryhn ,  Anne Kristin Holmeide ,  Jenny Rosman

    IPC分类号： A01N37/00

    CPC分类号： C07C323/54 ,  A23D9/00 ,  A61K49/0004 ,  C07C57/03 ,  C07C57/12 ,  C07C69/587 ,  C07C211/20 ,  C07C229/30 ,  C07F9/091 ,  C07F9/106 ,  C07H15/04

    摘要： Omega-3 lipid compounds of the general formula (I): wherein R1 and R2 are the same or different and may be selected from a group of substituents consisting of hydrogen, a hydroxy group, an alkyl group, a halogen atom, an alkoxy group, an acyloxy group, an acyl group, an alkenyl group, an alkynyl group, an aryl group, an alkylthio group, an alkoxycarbonyl group, a carboxy group, an alkylsulfinyl group, an alkylsulfonyl group, an amino group, and an alkylamino group; X represents a carboxylic acid or a derivative thereof, a carboxylate, a carboxylic anhydride or a carboxamide; and Y is a C6 to C22 alkene with two or more double bonds, having E and/or Z configuration, are disclosed. Also disclosed are pharmaceutical compositions and lipid compositions comprising such compounds, and to such compounds for use as medicaments in particular for the treatment of cardiovascular and metabolic diseases.

    摘要翻译： 通式（I）的ω-3脂质化合物：其中R 1和R 2相同或不同，并且可以选自氢，羟基，烷基，卤素原子，烷氧基 酰氧基，烯基，炔基，芳基，烷硫基，烷氧基羰基，羧基，烷基亚磺酰基，烷基磺酰基，氨基和烷基氨基; X表示羧酸或其衍生物，羧酸酯，羧酸酐或羧酰胺; 并且Y是具有两个或更多个双键的具有E和/或Z构型的C6至C22烯烃。 还公开了包含这些化合物的药物组合物和脂质组合物，以及用作特别用于治疗心血管和代谢疾病的药物的这种化合物。

    Compounds
    6.
    发明授权
    Compounds 有权
    化合物

    公开(公告)号：US08034842B2

    公开(公告)日：2011-10-11

    申请号：US12111589

    申请日：2008-04-29

    申请人： Morten Bryhn ,  Jan Kopecky ,  Anne Kristin Holmeide

    发明人： Morten Bryhn ,  Jan Kopecky ,  Anne Kristin Holmeide

    IPC分类号： A61K31/20

    CPC分类号： C07C57/03 ,  C07C69/587 ,  C07C69/618 ,  C07C69/65 ,  C07C69/732 ,  C07C69/734 ,  C07C229/30 ,  C07C233/09 ,  C07C235/28 ,  C07C237/16 ,  C07C317/44 ,  C07C323/54 ,  C07D209/48 ,  C07D263/22 ,  C07D263/24 ,  C11C3/00

    摘要： Compounds of formula (I); wherein R1 and R2 are the same or different and may be selected from the group consisting of a hydrogen atom, a hydroxy group, an alkyl group, a halogen atom, an alkoxy group, an acyloxy group, an acyl group, an alkenyl group, an alkynyl group, an aryl group, an alkylthio group, an alkoxycarbonyl group, an alkylsulfinyl group, an alkylsulfonyl group, an amino group, and an alkylamino group; and X represents a carboxylic acid group, a carboxylate group, or a carboxamide group; or any pharmaceutically acceptable salt, solvate, complex or pro-drug thereof, with the provisos that the compound of formula (I) is not (all-Z)-4,7,10,13,16,19-docosahexaenoic acid (DHA), alpha-methyl-DHA, alpha-methyl DHA methyl ester, alpha-methyl-DHA ethyl ester or alpha-hydroxy DHA ethyl ester, are disclosed. A fatty acid composition and a pharmaceutical composition comprising such compounds are also disclosed. The use of such compounds as medicaments, in particular for the treatment of diabetes type 2, is also disclosed.

    摘要翻译： 式（I）化合物; 其中R1和R2相同或不同，可以选自氢原子，羟基，烷基，卤素原子，烷氧基，酰氧基，酰基，烯基， 炔基，芳基，烷硫基，烷氧基羰基，烷基亚磺酰基，烷基磺酰基，氨基和烷基氨基; X表示羧酸基，羧酸酯基或羧酰胺基; 或其任何药学上可接受的盐，溶剂化物，复合物或前药，条件是式（I）化合物不是（全Z）-4,7,10,13,16,19-二十二碳六烯酸（DHA ），α-甲基-DHA，α-甲基DHA甲酯，α-甲基-DHA乙酯或α-羟基DHA乙酯。 还公开了脂肪酸组合物和包含这些化合物的药物组合物。 还公开了使用这些化合物作为药物，特别是用于治疗2型糖尿病的化合物。