公开(公告)号：EP2094640A1

公开(公告)日：2009-09-02

申请号：EP07825558.5

申请日：2007-11-01

申请人： Pronova BioPharma Norge AS

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 R1 and R2 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 C16 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.

公开(公告)号：EP2217224A1

公开(公告)日：2010-08-18

申请号：EP08846228.8

申请日：2008-11-06

申请人： Pronova BioPharma Norge AS

发明人： HOLMEIDE, Anne Kristin

IPC分类号： A61K31/10 ,  A23L1/29 ,  A61K31/22 ,  A61K8/46 ,  C07C321/14 ,  C07C321/18 ,  C07C323/03 ,  C07C323/05

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

摘要： The present invention relates to lipid compounds of the general formula (I): wherein • R1 is selected 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 selected from hydrogen and a C1-C6 alkyl group; and X is selected from O, S, SO, SO2, Si or Se; • n = 1 or 3; and • P1 is selected from a hydrogen, a C10-C21 alkyl, a C10-C21 alkenyl having 1-6 double bonds, and a C10-C21 alkynyl having 1-6 triple bonds, optionally substituted; or P1 is represented by: wherein P2, P3 and P4 are selected from a hydrogen, an alkyl, alkenyl, alkynyl, optionally substituted; or P1 is a phosphonate or a phosphate ester, represented by or P1 is a sulphonate or a sulphate ester, represented by wherein P5 is a hydrogen or 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 such compounds for use as medicaments, in particular for the treatment of diseases related to the cardiovascular, metabolic and inflammatory disease area.

公开(公告)号：EP2427415A1

公开(公告)日：2012-03-14

申请号：EP10772077.3

申请日：2010-05-07

申请人： Pronova BioPharma Norge AS

发明人： HOVLAND, Ragnar ,  HOLMEIDE, Anne Kristin ,  SKJÆRET, Tore ,  BRÆNDVANG, Morten

IPC分类号： C07C57/03 ,  A61K31/19 ,  A61K31/22 ,  A61P19/02 ,  A61P29/00 ,  A61P3/10 ,  A61P9/10 ,  C07C69/587

CPC分类号： C07D263/26 ,  A61K31/19 ,  A61K31/22 ,  A61K31/421 ,  A61K45/06 ,  C07B2200/07 ,  C07C51/367 ,  C07C59/60 ,  C07C67/31 ,  C07C69/675 ,  C07C69/68 ,  C07C69/708

摘要： The present disclosure relates to lipid compounds of the general formula (I): R1-O-C(R2)(R3) -X (I) wherein R
1 is a C
10 -C
22 alkyl group, a C
10 -C
22 alkenyl group having 1-6 double bonds, or a C
10 -C
22 alkynyl group having 1-6 triple bonds; R
2 and R
3 are the same or different and may be chosen from different substituents; and X is a carboxylic acid or a derivative thereof, such as a carboxylic ester, a carboxylic anhydride, a phospholipid, triglyceride, or a carboxamide; or a pharmaceutically acceptable salt, solvate, solvate of such salt or a prodrug thereof. The present disclosure also relates to pharmaceutical compositions and lipid compositions comprising at least one compound according to the present disclosure, 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.

公开(公告)号：EP2217558A1

公开(公告)日：2010-08-18

申请号：EP08844938.4

申请日：2008-10-30

申请人： Pronova Biopharma Norge AS

发明人： HOLMEIDE, Anne Kristin ,  HOVLAND, Ragnar

IPC分类号： C07C69/587 ,  C07C69/734 ,  A61K31/19 ,  A61P3/10

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; and 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 HbAIc, 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).

公开(公告)号：EP2102139A2

公开(公告)日：2009-09-23

申请号：EP07874033.9

申请日：2007-11-01

申请人： Pronova Biopharma Norge AS

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

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.