Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Ester doai
Patent
1998-01-20
2000-04-04
Geist, Gary
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Ester doai
514550, 514557, A01N 3702
Patent
active
06046237&
DESCRIPTION:
BRIEF SUMMARY
This invention relates to the use of certain non-.beta.-oxidizable fatty acid analogues for the manufacture of medicaments for the treatment of hyperlipidermic conditions, such as for reducing the concentration of cholesterol and triglycerides, and for inhibition of the oxidative modification of low density lipoprotein (LDL) in the blood of mammals. These medicaments also have a preventive effect on growth of tumour cells and may therefore be used in treatment of various terms of cancer diseases. The invention also relates to a method for preparing a medicament based on the mentioned fatty acid analogues, and also relates to a new compound having all of the above given favourable therapeutical effects.
Excess of cholesterol and triglycerides in blood has been shown to accelerate the development of ateriosclerosis and is a risk factor for myocardial infarction. Accordingly, a reduction of excess of lipids in blood by diets or drugs is used as a preventative measure in people at risk due to high levels of cholesterol and triglycerides and high platelet activation.
In this connection reference is made to European Patent Specification No. 345.038 (NORSK HYDRO A.S., priority of GB-8813012 of Jun. 2, 1988) which discloses the use of non-.beta.-oxidizable fatty acid analogues of the general formula (I): from 8-22 carbon atoms, X represents O, S, SO, and SO.sub.2, and R represents hydrogen or C.sub.1 -C.sub.4 alkyl, for the manufacture of a medicament for the treatment of hyperlipaemic conditions and for reducing the concentration of cholesterol and triglycerides in the blood of mammals. The EP-specification also discloses the preparation of compounds of the actual non-.beta.-oxidizable fatty acid analogues wherein the substituent X represents O, S, SO, SO.sub.2, respectively. The EP-specification reports that the compounds in question exhibit favourable hypolipidemic effects in blood of mammals, such as rats, and possess low toxicity measured as increase in liver weight and increased peroxisomal .beta.-oxidation. The patent concludes that the compounds in question are potentially useful as medicinal compounds. For further considerations we refer to the EP-specification.
It has now been found that the analogues of the above mentioned non-.beta.-oxidizable fatty acid have broader area of applications as an ingredient in drugs than the ones reported in the European Patent Specification No. 0.345.038. Further, it has been found that analogues with other election for the substituent X in the compound of formula (I), exhibit, as will be evident from the below specification, generally more potent pharmaceutical effects, also regarding the previously disclosed teaching of treatment of hyperlipidermic conditions for reducing the concentration of cholesterol and triglycerides. Current research suggests that prevention of atherosclerosis must take into consideration not just lowering plasma cholesterol and triglycerides, but also decreasing the susceptibility of LDL to oxidative damage. Oxidatively modified LDL--but not native LDL--has a number of characteristic properties that may initiate formation of foam cells and promote the development of fatty streaks, the earliest lesions in atherosclerosis. It could therefore be expected that preventing LDL modification could alternate foam cell formation and the development of plaques. It is well known that natural long-chain fatty acids, particularly polyunsaturated fatty acids of the main origin, are effective in lowering plasma triglyceride but not cholesterol levels in man. Moreover, as a lipid radical-propagated peroxidation chain reaction, in which the polyunsaturated fatty acids contained in the LDL are rapidly oxidized to lipid hydroperoxides, high supplementation of main based diets rich in .omega.-3-fatty acids may rather increase LDL oxidation.
The antiatherogenic properties of probucol are supposed to be related to its antioxidant effect rather than to its relatively weak hypocholesterolemic potency.
New strategies have been developed to search for compounds that are l
REFERENCES:
patent: 5093365 (1992-03-01), Berge et al.
Sadak, S. A.; Basmadjian, G.P.J. Labelled Compd. Radiopharm. 20(4), 487-494, 1983.
Schwarz, K.; Fredga, A. Chem Abstract 80:10264, 1974.
STN International, File CA, Chemical Abstracts, vol. 124, No. 9, Feb 26, 1996, (Columbus Ohio, US), Froeyland, Livar et al: "Tetradecylthioacetic acid incorporated into very low density lipoprotein: changes in the fatty acid composition and reduced plasma lipids in cholesterol-fed hamsters", Abstract No. 115981, and J. Lipid Res. (1995), 36 (12), 2529-40.
Berge Rolf
Songstad Jon
Deemie Robert W.
Geist Gary
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