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Polyunsaturated fatty acids for the treatment of diseases related to cardiovascular, metabolic and inflammatory disease areas

A technology of unsaturated fatty acids and lipids, which is applied in cardiovascular system diseases, metabolic diseases, blood diseases, etc., and can solve problems such as limited stability in vivo, lack of biological specificity, and PUFA not being widely used in therapeutic drugs

Active Publication Date: 2012-05-16
PRONOVA BIOPHARMA NORGE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0013] PUFAs have not achieved widespread use as therapeutic drugs due to their limited in vivo stability and their lack of biospecificity

Method used

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  • Polyunsaturated fatty acids for the treatment of diseases related to cardiovascular, metabolic and inflammatory disease areas
  • Polyunsaturated fatty acids for the treatment of diseases related to cardiovascular, metabolic and inflammatory disease areas
  • Polyunsaturated fatty acids for the treatment of diseases related to cardiovascular, metabolic and inflammatory disease areas

Examples

Experimental program
Comparison scheme
Effect test

Embodiment i

[0102] R 1 =C 14

[0103]

[0104] Category B

[0105] ●Derived from monounsaturated fatty acids

[0106] ●R 1 is C with 1 double bond 10 -C 22 Alkenyl

[0107] Embodiment ii:

[0108] R 1 =C 18

[0109]

[0110] Embodiment iii:

[0111] R 1 =C 14

[0112] Category C:

[0113] ●Derived from polyunsaturated fatty acids

[0114] ●R 1 is C with 5 double bonds 20 Alkenyl

Embodiment iv

[0116] R 1 = C with Z double bond interrupted by 5 methylene groups 20

[0117]

[0118] Category D:

[0119] ●Derived from polyunsaturated fatty acids

[0120] ●R 1 is C with 6 double bonds 22 Alkenyl

Embodiment v

[0122] R 1 = C with a Z double bond interrupted by 6 methylene groups 22

[0123]

[0124] Category E:

[0125] ●Derived from polyunsaturated fatty acids

[0126] ●R 1 is C with 3 double bonds 18 Alkenyl

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Abstract

The present disclosure relates to lipid compounds of the general formula (I): R1-O-C(R2)(R3) -X (I) wherein R1 is a C10-C22 alkyl group, a C10-C22 alkenyl group having 1-6 double bonds, or a C10-C22 alkynyl group having 1-6 triple bonds; R2 and R3 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.

Description

[0001] priority [0002] This application claims priority to US Provisional Patent Application 61 / 176,503, filed May 8, 2009, the contents of which are incorporated by reference. technical field [0003] The disclosure of the present application relates to a lipid compound of general formula (I) or a pharmaceutically acceptable salt, solvate, solvate of said salt, or a prodrug: [0004] [0005] in [0006] ●R 1 is C 10 -C 22 Alkyl, C with 1-6 double bonds 10 -C 22 Alkenyl, or C with 1-6 triple bonds 10 -C 22 Alkynyl; [0007] ●R 2 and R 3 the same or different and may be selected from hydrogen atom, hydroxyl, alkyl, halogen atom, alkoxy, acyloxy, acyl, alkenyl, alkynyl, aryl, alkylthio, alkoxycarbonyl, carboxyl , alkylsulfinyl, alkylsulfonyl, amino and alkylamino, provided that R 2 and R 3 cannot all be hydrogen atoms; or [0008] ●R 2 and R 3 together form cycloalkyl groups such as cyclopropane, cyclobutane, cyclopentane or cyclohexane; [0009] • X is a...

Claims

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Application Information

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IPC IPC(8): C07C57/03A61K31/19A61K31/22A61P19/02A61P29/00A61P3/10A61P9/10C07C69/587
CPCC07C59/60A61K31/421C07C69/68A61K31/19C07C69/708C07C67/31C07C69/675C07C51/367C07D263/26A61K31/22C07B2200/07A61K45/06A61P1/00A61P1/04A61P1/16A61P19/02A61P29/00A61P3/04A61P3/06A61P7/00A61P9/10A61P3/10A61K31/195C07C57/03
Inventor R.霍夫兰A.K.霍尔迈德T.斯克杰雷特M.布伦德范格
Owner PRONOVA BIOPHARMA NORGE