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    Sulphur containing lipids for use as food supplement or as medicament
    2.
    发明授权
    Sulphur containing lipids for use as food supplement or as medicament 有权
    含硫脂质用作食品补充剂或药物

    公开(公告)号：US08759558B2

    公开(公告)日：2014-06-24

    申请号：US13054212

    申请日：2009-07-13

    申请人： Anne Kristin Holmeide ,  Ragnar Hovland ,  Morten Brændvang

    发明人： Anne Kristin Holmeide ,  Ragnar Hovland ,  Morten Brændvang

    IPC分类号： C11D1/28 ,  A61K31/10

    CPC分类号： C07C323/54 ,  A23L33/12 ,  C07C317/44 ,  C07C323/52 ,  C07C323/55 ,  C07C323/56 ,  C07C323/61 ,  C07C2601/04

    摘要： The present invention relates to lipid compounds of the general formula (I): wherein R1 is selected from a C10-C22 alkyl, a C10-C22 alkenyl having 1-6 double bonds, and a C10-C22alkynyl having 1-6 triple bonds; R2 and R3 are the same or different and may be selected from a group of different substituents; Y is selected from sulphur, sulfoxide, and sulfone; and X represents a carboxylic acid or a derivative thereof, a carboxylic ester, a carboxylic anhydride or a carboxamide; or a pharmaceutically acceptable salt, complex or solvate thereof.The invention also relates to pharmaceutical compositions and lipid compositions comprising such compounds, and to such compounds for use as medicaments or for use in therapy, in particular for the treatment of diseases related to the cardiovascular, metabolic and inflammatory disease area.

    摘要翻译： 本发明涉及通式（I）的脂质化合物：其中R1选自C10-C22烷基，具有1-6个双键的C10-C22烯基和具有1-6个三键的C10-C22炔基; R2和R3相同或不同，并且可以选自不同取代基的一组; Y选自硫，亚砜和砜; X表示羧酸或其衍生物，羧酸酯，羧酸酐或羧酰胺; 或其药学上可接受的盐，复合物或溶剂合物。 本发明还涉及包含这种化合物的药物组合物和脂质组合物，以及用作药物或用于治疗，特别是用于治疗与心血管，代谢和炎性疾病区域有关的疾病的化合物。

    NOVEL SULPHUR CONTAINING LIPIDS FOR USE AS FOOD SUPPLEMENT OR AS MEDICAMENT
    4.
    发明申请
    NOVEL SULPHUR CONTAINING LIPIDS FOR USE AS FOOD SUPPLEMENT OR AS MEDICAMENT 有权
    含有新鲜的含硫脂肪作为食物补充剂或作为药物使用

    公开(公告)号：US20110190395A1

    公开(公告)日：2011-08-04

    申请号：US13054212

    申请日：2009-07-13

    申请人： Anne Kristin Holmeide ,  Ragnar Hovland ,  Morten Brændvang

    发明人： Anne Kristin Holmeide ,  Ragnar Hovland ,  Morten Brændvang

    IPC分类号： A61K31/202 ,  C07C57/03 ,  A61P9/00 ,  A61P3/04 ,  A61P1/16 ,  A61P9/10 ,  A61P3/10 ,  A61P29/00

    CPC分类号： C07C323/54 ,  A23L33/12 ,  C07C317/44 ,  C07C323/52 ,  C07C323/55 ,  C07C323/56 ,  C07C323/61 ,  C07C2601/04

    摘要： The present disclosure relates to lipid compounds of general formula (I) wherein R1 is chosen from a C10-C22 alkyl group, a C10-C22 alkenyl group having 1-6 double bonds, and a C10-C22 alkynyl group having 1-6 triple bonds; R2 and R3 are the same or different and may be selected from different substituents; Y is chosen from sulphur, sulfoxide, and sulfone; and X is a carboxylic acid or a derivative thereof, a carboxylic ester, a carboxylic anhydride, or a carboxamide; or a pharmaceutically acceptable salt, complex, or solvate thereof. The present disclosure also relates to pharmaceutical compositions and lipid compositions comprising such compounds, and methods of using such compounds such as for treating diseases related to cardiovascular, metabolic, and/or inflammatory diseases.

    摘要翻译： 本公开内容涉及通式（I）的脂质化合物，其中R 1选自C 10 -C 22烷基，具有1-6个双键的C 10 -C 22烯基和具有1-6个三价的C 10 -C 22炔基 债券 R2和R3相同或不同并且可以选自不同的取代基; Y选自硫，亚砜和砜; 和X是羧酸或其衍生物，羧酸酯，羧酸酐或羧酰胺; 或其药学上可接受的盐，络合物或溶剂化物。 本公开还涉及包含这些化合物的药物组合物和脂质组合物，以及使用这些化合物的方法，例如用于治疗与心血管，代谢和/或炎性疾病有关的疾病。

    DHA DERIVATIVES AND THEIR USE AS MEDICAMENTS
    5.
    发明申请
    DHA DERIVATIVES AND THEIR USE AS MEDICAMENTS 审中-公开
    DHA衍生物及其作为药物使用

    公开(公告)号：US20100267828A1

    公开(公告)日：2010-10-21

    申请号：US12740377

    申请日：2008-10-30

    申请人： Anne Kristin Holmeide ,  Ragnar Hovland

    发明人： Anne Kristin Holmeide ,  Ragnar Hovland

    IPC分类号： A61K31/232 ,  C07C69/587 ,  C07C67/00 ,  C12P7/64 ,  A61P3/10 ,  A61P3/04 ,  A61P29/00

    CPC分类号： C07C69/587 ,  C07C67/26 ,  C07C67/28 ,  C07C69/63

    摘要： The present disclosure relates to compounds of the general formula (I): wherein R1 and R2 are the same or different and are chosen from 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; or any pharmaceutically acceptable salt, solvate, complex, or pro-drug thereof; and their use as medicaments for the treatment of various diseases and conditions, for example, reduction of elevated triglyceride levels, i.e., hypertriglyceridemia, reduction of non-HDL cholesterol, reduction of glucose and HbA1c, and improvement of insulin resistance. The present disclosure also relates to a pharmaceutical composition comprising compounds of formula (I), as well as to processes for preparing compounds according to formula (I).

    摘要翻译： 本公开内容涉及通式（I）的化合物：其中R 1和R 2相同或不同，并且选自氢原子，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; 或其药学上可接受的盐，溶剂化物，复合物或前体药物; 以及它们作为用于治疗各种疾病和病症的药物的用途，例如降低甘油三酯水平升高，即高甘油三酯血症，降低非HDL胆固醇，降低葡萄糖和HbA1c以及改善胰岛素抵抗。 本公开还涉及包含式（I）化合物的药物组合物，以及用于制备根据式（I）的化合物的方法。

    Alpha-substituted omega-3 lipids that are activators or modulators of the peroxisome proliferators-activated receptor (PPAR)
    6.
    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
    7.
    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。

    COMPOSITION
    8.
    发明申请
    COMPOSITION 审中-公开
    组成

    公开(公告)号：US20110166228A1

    公开(公告)日：2011-07-07

    申请号：US12446249

    申请日：2007-11-01

    申请人： Anne Kristin Holmeide ,  Jenny Rosman

    发明人： Anne Kristin Holmeide ,  Jenny Rosman

    IPC分类号： A61K31/202 ,  A61P3/10 ,  A61P9/10

    CPC分类号： C07F9/113 ,  A61K31/045 ,  A61K31/047 ,  A61K31/075 ,  A61K31/10 ,  A61K31/22 ,  A61K31/225 ,  A61K31/232 ,  A61K31/255 ,  A61K31/265 ,  A61K31/661 ,  A61K45/06 ,  C07C69/007 ,  C07C69/24 ,  C07C69/40 ,  C07C69/587 ,  C07C69/96 ,  C07C305/14 ,  C07C323/14 ,  A61K2300/00

    摘要： The present invention relates to compositions comprising at least omega-3 lipid compounds substituted at the 2-positions having therapeutic activity. More specifically, the present invention relates to a composition comprising at least omega-3 lipid compounds substituted at the 2-position, counted from the functional group (X) of the omega-3 lipid compound, wherein the omega-3 lipid compounds comprise: a compound of general formula (I): and a compound of formula (II): wherein R1 and R2 are the same or different and are chosen from 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, a carboxy group, an alkylsulfinyl group, an alkylsulfonyl group, an amino group, and an alkylamino group; and X represents a carboxylic acid or a derivative thereof, a carboxylate, a carboxylic anhydride, a hydroxymethyl (—CH2OH) or a pro-drug thereof, or a carboxamide, or any pharmaceutically acceptable complex, salt, solvate, or pro-drug, with the provisos that: R1 and R2 are not simultaneously hydrogen.

    摘要翻译： 本发明涉及包含至少在具有治疗活性的2位置取代的ω-3脂质化合物的组合物。 更具体地说，本发明涉及从ω-3脂质化合物的官能团（X）计数的至少包含在2位被取代的ω-3脂质化合物的组合物，其中ω-3脂质化合物包含： 通式（I）的化合物和式（II）的化合物：其中R 1和R 2相同或不同，并且选自氢原子，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; 羧酸酐，羧酸酐，羟甲基（-CH 2 OH）或其前药或羧酰胺，或任何药学上可接受的复合物，盐，溶剂合物或前药， 条件是：R1和R2不同时为氢。

    Novel Compounds
    9.
    发明申请
    Novel Compounds 有权
    新型化合物

    公开(公告)号：US20080300306A1

    公开(公告)日：2008-12-04

    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： A61K31/202 ,  A61P3/00 ,  A61P29/00 ,  C07C51/00 ,  C07C57/02 ,  C07C57/03

    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。

    Lipid compounds for use in cosmetic products, as food supplement or as a medicament
    10.
    发明授权
    Lipid compounds for use in cosmetic products, as food supplement or as a medicament 有权
    用于化妆品的脂质化合物，作为食品补充剂或药物

    公开(公告)号：US08741966B2

    公开(公告)日：2014-06-03

    申请号：US12741890

    申请日：2008-11-06

    申请人： Anne Kristin Holmeide

    发明人： Anne Kristin Holmeide

    IPC分类号： A61K31/095 ,  A61K31/10 ,  A61K31/21 ,  C07C317/08 ,  C07C69/52 ,  C07C321/18 ,  C07C303/00

    CPC分类号： A61K31/00 ,  A23L33/115 ,  A61K8/46 ,  A61K2800/92 ,  A61Q19/06 ,  C07C323/12

    摘要： The present disclosure relates to lipid compounds of formula (I): wherein: R1 is chosen from a C10-C21 alkyl, a C10-C21 alkenyl having 1-6 double bonds, and a C10-C21 alkynyl having 1-6 triple bonds; R2 and R3 are the same or different and are chosen from hydrogen and a C1-C6 alkyl; X is chosen from O, S, SO, SO2, Si, and Se; n=1 or 3; and P1 is chosen from hydrogen; a C10-C21 alkyl, a C10-C21 alkenyl having 1-6 double bonds, a C10-C21 alkynyl having 1-6 triple bonds, optionally substituted; a group of formula (II) or formula (III), wherein P2, P3, and P4 are chosen from hydrogen, an alkyl, an alkenyl, and an alkynyl, optionally substituted; and a group of formula (IV) or formula (V), wherein P5 is chosen from hydrogen and a C1-C6 alkyl; or a pharmaceutically acceptable salt, complex, or solvate thereof. Also disclosed are pharmaceutical compositions and lipid compositions comprising such compounds, and methods of use thereof, for example in the treatment of diseases related to cardiovascular, metabolic, and inflammatory conditions.

    摘要翻译： 本公开涉及式（I）的脂质化合物：其中：R 1选自C 10 -C 21烷基，具有1-6个双键的C 10 -C 21烯基和具有1-6个三键的C 10 -C 21炔基; R2和R3相同或不同，并且选自氢和C1-C6烷基; X选自O，S，SO，SO2，Si和Se; n = 1或3; P1选自氢; C10-C21烷基，具有1-6个双键的C10-C21烯基，具有1-6个三键的C10-C21炔基，任选取代的; 式（II）或式（III）的基团，其中P2，P3和P4选自氢，烷基，烯基和炔基，任选取代; 和式（IV）或式（V）的基团，其中P 5选自氢和C 1 -C 6烷基; 或其药学上可接受的盐，络合物或溶剂化物。 还公开了包含这些化合物的药物组合物和脂质组合物及其使用方法，例如用于治疗与心血管，代谢和炎性病症有关的疾病。