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1. 发明申请

WO2008132552A2 NOVEL LIPID COMPOUNDS 审中-公开
标题翻译：新型脂肪化合物
公开(公告)号：WO2008132552A2
公开(公告)日：2008-11-06
申请号：PCT/IB2007/004588
申请日：2007-11-01
申请人： PRONOVA BIOPHARMA NORGE AS , HOLMEIDE, Anne, Kristin , ROSMAN, Jenny
发明人： HOLMEIDE, Anne, Kristin , ROSMAN, Jenny
IPC分类号： C07C33/02 , C07C43/178 , C07C69/007 , C07C69/24 , C07C69/40 , C07C69/587
CPC分类号： C07H15/04 , A23D9/00 , A61K31/045 , A61K31/047 , A61K31/075 , A61K31/10 , A61K31/22 , A61K31/225 , A61K31/232 , A61K31/255 , A61K31/265 , A61K31/661 , A61K45/06 , A61K49/0004 , C07C57/03 , C07C57/12 , C07C69/007 , C07C69/24 , C07C69/40 , C07C69/587 , C07C69/96 , C07C211/20 , C07C229/30 , C07C305/14 , C07C323/14 , C07C323/54 , C07F9/091 , C07F9/106 , C07F9/113 , A61K2300/00
摘要： Omega-3 lipid compounds of the general formula (I): wherein R 1 and R 2 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; P represents a hydrogen atom, (Formula II) wherein P 2 , P 3 , and P 4 are chosen from a hydrogen atom, an alkyl group, and a C 14 -C 22 alkenyl group, wherein the alkyl and alkenyl groups are optionally substituted with a hydroxy group, (Formula III), (Formula IV), or (Formula V); and Y is a C 14 -C 22 alkenyl group with at least one double bond, having E and/or Z configuration; or any pharmaceutically acceptable complex, solvate, salt or pro-drug thereof, with the proviso that R 1 and R 2 are not simultaneously a hydrogen atom. 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，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，羧基，烷基亚磺酰基，烷基磺酰基基团，氨基和烷基氨基; P表示氢原子，（式II）其中P 2，P 3，和P 4选自氢原子，烷基基团和C 14 -C 22烯基，其中烷基和烯基任选被羟基取代，（式III），（式IV），或（式V）; 并且Y是具有至少一个具有E和/或Z构型的双键的C 14-14 -C 22烯基; 或其任何药学上可接受的复合物，溶剂合物，盐或前药，条件是R 1和R 2不同时为氢原子。还公开了包含这些化合物的药物组合物和脂质组合物，以及用作药物的这种化合物，特别是用于治疗心血管和代谢疾病。

2. 发明申请

WO2008142482A2 COMPOSITION 审中-公开
标题翻译：组成
公开(公告)号：WO2008142482A2
公开(公告)日：2008-11-27
申请号：PCT/IB2007004613
申请日：2007-11-01
申请人： PRONOVA BIOPHARMA NORGE AS , HOLMEIDE ANNE KRISTIN , ROSMAN JENNY
发明人： HOLMEIDE ANNE KRISTIN , ROSMAN JENNY
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脂类化合物的组合物，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。

3. 发明申请

WO2008053331A1 ALPHA-SUBSTITUTED OMEGA-3 LIPIDS THAT ARE ACTIVATORS OR MODULATORS OF THE PEROXISOME PROLIFERATORS-ACTIVATED RECEPTOR (PPAR). 审中-公开
标题翻译： ALPHA-替代的OMEGA-3脂肪酸，其是过氧化物酶促反应物受体（PPAR）的激活剂或调节剂。
公开(公告)号：WO2008053331A1
公开(公告)日：2008-05-08
申请号：PCT/IB2007/003305
申请日：2007-11-01
申请人： PRONOVA BIOPHARMA NORGE A/S , BRYHN, Morten , HOLMEIDE, Anne Kristin , ROSMAN, Jenny
发明人： BRYHN, Morten , HOLMEIDE, Anne Kristin , ROSMAN, Jenny
IPC分类号： C07C69/587 , A61K31/202 , A61K31/232 , A61P1/16 , A61P29/00 , A61P3/04 , A61P3/10 , C07C229/30 , C07C323/54 , C07C57/13 , C07C69/602 , C07C69/732 , C07C69/734 , C11C3/00 , A61K49/00
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 R 1 and R 2 are the same or different and may be selected from a group of substitu- ents 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 al- kynyl group, an aryl group, an alkylthio group, an alkoxycarbonyl group, a car- boxy group, an alkylsulfmyl 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 C 16 to C 22 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，并且可以选自以下的取代基：的氢原子，羟基，烷基，卤素原子，烷氧基，酰氧基，酰基，烯基，炔丙基，芳基，烷硫基，烷氧基羰基羧甲基，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; 并且公开了具有E和/或Z构型的具有两个或更多个双键的-C 22 C 12 -C 16烷基。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。

4. 发明申请

WO2011089529A4 SALICYLATE FATTY ACID DERIVATIVES 审中-公开
标题翻译：水杨酸脂肪酸衍生物
公开(公告)号：WO2011089529A4
公开(公告)日：2011-10-27
申请号：PCT/IB2011000250
申请日：2011-01-20
申请人： PRONOVA BIOPHARMA NORGE AS , HOVLAND RAGNAR , SKJAERET TORE , ROSMAN JENNY
发明人： HOVLAND RAGNAR , SKJAERET TORE , ROSMAN JENNY
IPC分类号： C07C233/49 , A61K31/166 , A61K31/167 , A61K31/194 , A61P3/00 , A61P29/00 , C07C65/19 , C07C233/55 , C07C233/64 , C07C321/20
CPC分类号： C07C323/60 , C07C59/60 , C07C69/734 , C07C235/08 , C07C235/10 , C07C235/12 , C07C235/16 , C07C235/60 , C07C237/22 , C07C265/04 , C07C271/16 , C07C271/20 , C07C271/28 , C07C275/42 , C07C323/52
摘要： Fatty acid conjugates of salicylate derivatives and compositions thereof are disclosed. Further disclosed are methods for treating and/or preventing an inflammatory disease including inflammation and/or inflammatory bowel disease (IBD), dyslipidemia including mixed dyslipidemia and/or hypertriglyceridemia, elevated blood lipids including, e.g., triglycerides and/or cholesterol, metabolic syndrome, peripheral insulin resistance, diabetes, atherosclerosis; a method for lowering non-HDL cholesterol; and a method for raising HDL-cholesterol comprising the administration of an effective amount of at least one compound according to the present disclosure.
摘要翻译：公开了水杨酸酯衍生物的脂肪酸缀合物及其组合物。进一步公开了用于治疗和/或预防包括炎症和/或炎性肠病（IBD）的炎性疾病，包括混合性血脂异常和/或高甘油三酯血症的血脂异常，升高的血脂包括例如甘油三酯和/或胆固醇，代谢综合征，外周胰岛素抵抗，糖尿病，动脉粥样硬化; 降低非HDL胆固醇的方法; 和用于升高HDL-胆固醇的方法，其包括施用有效量的根据本公开的至少一种化合物。

5. 发明申请

WO2011089529A1 SALICYLATE FATTY ACID DERIVATIVES 审中-公开
标题翻译：盐酸脂肪酸衍生物
公开(公告)号：WO2011089529A1
公开(公告)日：2011-07-28
申请号：PCT/IB2011/000250
申请日：2011-01-20
申请人： PRONOVA BIOPHARMA NORGE AS , HOVLAND, Ragnar , SKJÆRET, Tore , ROSMAN, Jenny
发明人： HOVLAND, Ragnar , SKJÆRET, Tore , ROSMAN, Jenny
IPC分类号： C07C233/49 , A61K31/166 , A61K31/167 , A61K31/194 , A61P3/00 , A61P29/00 , C07C65/19 , C07C233/55 , C07C233/64 , C07C321/20
CPC分类号： C07C323/60 , C07C59/60 , C07C69/734 , C07C235/08 , C07C235/10 , C07C235/12 , C07C235/16 , C07C235/60 , C07C237/22 , C07C265/04 , C07C271/16 , C07C271/20 , C07C271/28 , C07C275/42 , C07C323/52
摘要： Fatty acid conjugates of salicylate derivatives and compositions thereof are disclosed. Further disclosed are methods for treating and/or preventing an inflammatory disease including inflammation and/or inflammatory bowel disease (IBD), dyslipidemia including mixed dyslipidemia and/or hypertriglyceridemia, elevated blood lipids including, e.g., triglycerides and/or cholesterol, metabolic syndrome, peripheral insulin resistance, diabetes, atherosclerosis; a method for lowering non-HDL cholesterol; and a method for raising HDL-cholesterol comprising the administration of an effective amount of at least one compound according to the present disclosure.
摘要翻译：公开了水杨酸衍生物的脂肪酸共轭物及其组合物。进一步公开的是用于治疗和/或预防包括炎症和/或炎症性肠病（IBD），血脂异常，包括混合型血脂异常和/或高甘油三酯血症的升高的血脂，包括例如甘油三酯和/或胆固醇，代谢综合征，外周胰岛素抵抗，糖尿病，动脉粥样硬化; 降低非HDL胆固醇的方法; 以及提高HDL-胆固醇的方法，其包括施用有效量的至少一种根据本公开的化合物。

6. 发明申请

WO2008142482A3 OMEGA-3 LIPID COMPOUNDS 审中-公开
公开(公告)号：WO2008142482A3
公开(公告)日：2008-11-27
申请号：PCT/IB2007/004613
申请日：2007-11-01
申请人： PRONOVA BIOPHARMA NORGE AS , HOLMEIDE, Anne Kristin , ROSMAN, Jenny
发明人： HOLMEIDE, Anne Kristin , ROSMAN, Jenny
IPC分类号： C07C33/02 , C07C43/178 , C07C69/007 , C07C69/24 , C07C69/40 , C07C69/587 , C07C69/96 , C07C309/67 , C07C323/14 , C07F9/113 , A61K31/045 , A61K31/075 , A61K31/10 , A61K31/047 , A61K31/22
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 R 1 and R 2 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 (-CH 2 OH) or a pro-drug thereof, or a carboxamide, or any pharmaceutically acceptable complex, salt, solvate, or pro-drug, with the provisos that: R 1 and R 2 are not simultaneously hydrogen.

7. 发明申请

WO2008139261A9 OMEGA-3 LIPID COMPOUND 审中-公开
标题翻译： OMEGA-3脂质化合物
公开(公告)号：WO2008139261A9
公开(公告)日：2009-11-12
申请号：PCT/IB2007004590
申请日：2007-11-02
申请人： PRONOVA BIOPHARMA NORGE AS , HOLMEIDE ANNE KRISTIN , ROSMAN JENNY
发明人： HOLMEIDE ANNE KRISTIN , ROSMAN JENNY
IPC分类号： A61K31/045 , A61K8/55 , A61K31/047 , A61K31/075 , A61K31/10 , A61K31/22 , A61K31/225 , A61K31/232 , A61K31/255 , A61K31/265 , A61K31/661 , A61P3/04 , A61P3/06 , A61P17/06 , A61P27/00
CPC分类号： A61K31/225 , A61K31/045 , A61K31/22 , A61K31/232 , A61K2300/00
摘要： The present invention relates to a lipid composition comprising at least omega-3 polyunsaturated alcohols, or pro-drugs thereof, which omega-3 polyunsaturated alcohols, or pro-drugs thereof, comprising at least (all-Z)-5,8,11,14,17-eicosapentaen- 1-ol, or pro-drug thereof, and (all-Z)-4,7,10,13,16,19-docosahexaen-1-ol, or pro-drug thereof, and their use as a pharmaceutical, in particular for the treatment of elevated triglyceride levels. The invention also relates to methods for the preparation of these pro-drugs from marine oils.
摘要翻译：本发明涉及包含至少ω-3多不饱和醇或其前药的脂质组合物，其中ω-3多不饱和醇或其前药至少包含（全Z）-5,8,11 ，14,17-二十碳五烯-1-醇或其前体药物，和（全Z）-4,7,10,13,16,19-二十二碳六烯-1-醇或其前药，及其用作药物，特别是用于治疗升高的甘油三酯水平。本发明还涉及从海洋油制备这些前药的方法。

8. 发明申请

WO2009134147A1 LIPID COMPOSITIONS CONTAINING DERIVATIVES OF EPA AND DHA AN THEIR USE THEREOF 审中-公开
标题翻译：含有EPA和DHA衍生物的脂肪组合物及其用途
公开(公告)号：WO2009134147A1
公开(公告)日：2009-11-05
申请号：PCT/NO2009/000170
申请日：2009-04-30
申请人： PRONOVA BIOPHARMA NORGE AS , HOLMEIDE, Anne Kristin , ROSMAN, Jenny , HOVLAND, Ragnar
发明人： HOLMEIDE, Anne Kristin , ROSMAN, Jenny , HOVLAND, Ragnar
IPC分类号： C07C33/02 , A61K31/10 , A61K31/232 , A61K31/661 , A61P3/06 , A61P3/10 , A61P9/00 , C07C305/14 , C07C69/24 , C07F9/113
CPC分类号： A61K31/10 , A61K31/232 , A61K31/661 , C07C69/96 , C07C215/10 , C07C279/14 , C07C305/14 , C07F9/113
摘要： The present invention relates to a lipid composition comprising at least pro-drugs of omega-3 polyunsaturated alcohols, which pro-drugs of omega-3 polyunsaturated alcohols comprise at least one pro-drug of (all-Z) 5,8,11,14,17-eicosapentaen-1-ol, and at least one pro-drug of (all-Z)-4,7,10,13,16,19-docosahexaen-1-ol and their use as a pharmaceutical, in particular for the treatment of elevated triglyceride levels. The invention also relates to methods for the preparation of these pro-drugs from marine oils.
摘要翻译：本发明涉及一种脂质组合物，其至少包含ω-3多不饱和醇的前药，ω-3多不饱和醇的前药包含至少一种（全Z）5,8,11， 14,17-二十碳五烯-1-醇和至少一种（全Z）-4,7,10,13,16,19-二十二碳六烯-1-醇的前药，及其作为药物的用途，特别是用于治疗升高的甘油三酯水平。本发明还涉及从海洋油制备这些前药的方法。

9. 发明申请

WO2008132552A3 OMEGA-3 LIPID COMPOUNDS 审中-公开
标题翻译： OMEGA-3脂质化合物
公开(公告)号：WO2008132552A3
公开(公告)日：2009-01-15
申请号：PCT/IB2007004588
申请日：2007-11-01
申请人： PRONOVA BIOPHARMA NORGE AS , HOLMEIDE ANNE KRISTIN , ROSMAN JENNY
发明人： HOLMEIDE ANNE KRISTIN , ROSMAN JENNY
IPC分类号： C07C33/02 , A61K31/045 , A61K31/047 , A61K31/075 , A61K31/10 , A61K31/22 , C07C43/178 , C07C69/007 , C07C69/24 , C07C69/40 , C07C69/587 , C07C69/96 , C07C309/67 , C07C323/14 , C07F9/113
CPC分类号： C07H15/04 , A23D9/00 , A61K31/045 , A61K31/047 , A61K31/075 , A61K31/10 , A61K31/22 , A61K31/225 , A61K31/232 , A61K31/255 , A61K31/265 , A61K31/661 , A61K45/06 , A61K49/0004 , C07C57/03 , C07C57/12 , C07C69/007 , C07C69/24 , C07C69/40 , C07C69/587 , C07C69/96 , C07C211/20 , C07C229/30 , C07C305/14 , C07C323/14 , C07C323/54 , C07F9/091 , C07F9/106 , C07F9/113 , A61K2300/00
摘要： Omega-3 lipid compounds of the general formula (1): wherein P represents a hydrogen atom, Formulas (a), (b), (c) or (d) and (e), Y is a C14-C22 alkenyl group with at least one double bond, having E and/or Z, configuration;., or any pharmaceutically acceptable complex, solvate, salt or pro-drug thereof, with the proviso that R1 and R2 are not simultaneously a hydrogen atom. 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（1）的ω-3脂质化合物：其中P表示氢原子，式（a），（b），（c）或（d）和（e）中，Y为C 14 -C 22烯基，具有E和/或Z构型的至少一个双键，或其任何药学上可接受的复合物，溶剂合物，盐或前药，条件是R 1和R 2不同时为氢原子。还公开了包含这些化合物的药物组合物和脂质组合物，以及用作药物的这种化合物，特别是用于治疗心血管和代谢疾病。

10. 发明申请

WO2008139261A3 OMEGA-3 LIPID COMPOUND 审中-公开
标题翻译： OMEGA-3脂质复合物
公开(公告)号：WO2008139261A3
公开(公告)日：2009-08-20
申请号：PCT/IB2007004590
申请日：2007-11-02
申请人： PRONOVA BIOPHARMA NORGE AS , HOLMEIDE ANNE KRISTIN , ROSMAN JENNY
发明人： HOLMEIDE ANNE KRISTIN , ROSMAN JENNY
IPC分类号： A61K31/045 , A61K8/55 , A61K31/047 , A61K31/075 , A61K31/10 , A61K31/22 , A61K31/225 , A61K31/232 , A61K31/255 , A61K31/265 , A61K31/661 , A61P3/04 , A61P3/06 , A61P17/06 , A61P27/00
CPC分类号： A61K31/225 , A61K31/045 , A61K31/22 , A61K31/232 , A61K2300/00
摘要： The present invention relates to a lipid composition comprising at least omega-3 polyunsaturated alcohols, or pro-drugs thereof, which omega-3 polyunsaturated alcohols, or pro-drugs thereof, comprising at least (all-Z)-5,8,11,14,17-eicosapentaen- 1-ol, or pro-drug thereof, and (all-Z)-4,7,10,13,16,19-docosahexaen-1-ol, or pro-drug thereof, and their use as a pharmaceutical, in particular for the treatment of elevated triglyceride levels. The invention also relates to methods for the preparation of these pro-drugs from marine oils.
摘要翻译：本发明涉及包含至少ω-3多元不饱和醇或其前药的脂质组合物，所述ω-3多元不饱和醇或其前药至少包含（全部为Z）-5,8,11 ，14,17-二十碳五烯-1-醇或其前体药物和（全-Z）-4,7,10,13,16,19-二十二碳六烯-1-醇或其前体药物及其它们的前药用作药物，特别是用于治疗升高的甘油三酯水平。本发明还涉及由海洋油制备这些前药的方法。

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