Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1987-03-27
1990-08-07
Robinson, Douglas W.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
514824, A61K 31335
Patent
active
049468669
DESCRIPTION:
BRIEF SUMMARY
This invention relates to the new use of known oxirancarboxylic acids for making lipid-lowering medications. The medications are used for the prevention and treatment of diseases which are based on an increased cholesterol and/or triglyceride concentration.
STATE OF THE ART
EP-A-0 046 590 describes hypoglycemically and hypoketonemically effective phen(alk)oxy-substituted oxirancarboxylic acids which are to be used for the treatment of diabetes. The magazine Biochemical Pharmacology, 33, 465 (1984) reports on the cholesterol and triglyceride concentration-lowering property of 2-[5-(4-chlorphenyl)-pentyl]-oxiran-2-carboxylic-acid-ethylesters.
DESCRIPTION OF INVENTION
It has now been found that the oxirancarboxylic acids, known from EP-A-0 046 590 bring about a definite lowering of the cholesterol and triglyceride concentration. Surprisingly, the extent of the reduction of the cholesterol and triglyceride concentration is considerably greater than one might have expected on the basis of the data collected for 2-[5-(4-chlorphenyl)-pentyl]-oxiran-2-carboxylic-acid-ethyl-esters. The surprisingly intensive reduction of the cholesterol and triglyceride concentration makes it appear that the oxirancarboxylic acids, which are known from EP-A-0 046 590, are suitable for use in the prevention and treatment of those diseases that are based on increased cholesterol and/or triglyceride concentration.
The object of the invention therefore is the use of oxirancarboxylic acids shown in Formula I ##STR2## where R1 is a hydrogen atom, a halogen atom a 1-4C-alkyl group, a 1-4C-alkoxy group, a nitro group, or a trifluoromethyl group; pharmacologically tolerable salts of carboxylic acids, for the production of medications for the prevention and/or treatment of diseases that are based on an increased cholesterol and/or triglyceride concentration.
As 1-4C-alkyl groups, one can consider straight-chain or ramified alkyl remnants with 1 to 4 carbon atoms. Straight-chain alkyl remnants, for example are the methyl-, ethyl-, n-propyl- and n-butyl remnants of which the methyl-and ethyl- remnant are preferred. Ramified alkyl remnants for example are isopropyl-, isobutyl-, secondary-butyl- and tertiary-butyl remnants. As alkyl remnants of 1-4C-alkoxy groups, one can consider both straight-chain and ramified low-alkyl groups. The methoxy group is preferred as 1-4C-alkoxy group.
Halogen atoms are fluorine, chlorine, and bromine atoms of which fluorine and especially chlorine are preferred.
The substituents R1 and R2 of the phenyl ring are preferably in the meta- or para-positions with respect to the (alk)oxyalkylene-oxirancarboxylic acid remnant.
As salts one can consider salts with inorganic and organic bases. As cations for salt formation one uses above all the cations of the alkali metals, earth-alkali metals, or earth metals. By way of example we might mention the salts of lithium, sodium, potassium, magnesium, calcium, and aluminum.
As diseases, which are based on an increased cholesterol and/or triglyceride concentration (hyperlipemia), we might mention primarily all forms of arteriosclerosis, especially coronary sclerosis and all of the pathological changes connected with this, which can be combined under the collective term of "coronary heart disease."
If the compounds in Formula I are used according to the invention for the manufacture of the above-mentioned medications, then the compounds of Formula I (=active substances) are employed either as such or preferably in combination with suitable pharmaceutical auxiliary or carrier substances in the form of tablets, coated tablets, capsules, suppositories, emulsions, suspensions, or solutions, where the active-substance content advantageously is between 0.1 and 95%.
The expert in the field knows, on the basis of his technical knowledge, which auxiliary or carrier substances are suitable for the desirable medication formulations. In addition to solvents, gel-forming agents, suppository foundations, auxiliary tablet substances and other active-substance carriers, one might for examp
REFERENCES:
patent: 4235923 (1980-11-01), Durham
patent: 4324796 (1982-04-01), Eistetter et al.
patent: 4337267 (1982-06-01), Eistetter et al.
patent: 4430339 (1984-02-01), Eistetter et al.
The Merck Manuel, 14th Ed. (1982); pp. 386-389; 970-981; and 1037-1042.
Koundakjian et al., "Metabolic Changes in Fed Rats--Caused by Chronic Administration of Ethyl 2[5(4-chlorophenyl)pentyl]oxirane-2-carboxylate, A New Hypoglycemic Compound", Biochem. Pharmacology, vol. 33, No. 3, pp. 465-473, 1984.
Eistetter Klaus
Wolf Horst
ByK Gulden Lomberg Chemische Fabrik GmbH
Robinson Douglas W.
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