7-substituted derivatives of 3,5-dihydroxyhept-6-ynoic acids and corresponding lactones and their use as hypercholeserolemics
AssigneeHoechst Aktiengesellschaft
InventorsKurt Kesseler, Wilhelm Bartmann, Gunther Wess, Ernold Granzer
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Abstract
7-Substituted 3,5-dihydroxyhept-6-ynoic acids and the derivatives thereof of the formula I ##STR1## as well as the corresponding lactones of the formula II ##STR2## in which R and R.degree. have the specified meanings, a process for the preparation of these compounds, the use thereof as pharmaceuticals and pharmaceutical products are described. In addition, new intermediates for the preparation of the compounds of the formula I or formula II are described.
Claims8
A compound of the formula I ##STR42## or a corresponding lactone of the formula II ##STR43## where, in formulae I and II, R is a radical of formula a ##STR44## in which R.sup.1 and R.sup.2 are, independently of one another, a straight-chain or branched alkyl or alkenyl radical having up to 6 carbon atoms, a saturated or up to doubly unsaturated cyclic hydrocarbon radical having 3-6 carbon atoms or a phenyl radical which is optionally substituted by 1-3 identical or different radicals selected from the group consisting of straight-chain or branched alkyl having up to 4 carbon atoms, halogen, alkoxy having up to 4 carbon atoms and hydroxyl, and
- X.dbd.Y--Z is a group of the formula N.dbd.CR.sup.4 --CR.sup.5, in which
- R.sup.4 and R.sup.5 are, independently of one another, hydrogen, a straight-chain or branched alkyl or alkenyl radical having up to 6 carbon atoms, a saturated or up to doubly unsaturated cyclic hydrocarbon radical having 3-6 carbon atoms or a phenyl radical which is optionally substituted by 1-3 identical or different radicals selected from the group consisting of straight-chain or branched alkyl having up to 4 carbon atoms, halogen, alkoxy having up to 4 carbon atoms and hydroxyl, and
- R.sup.0 is hydrogen, a straight-chain or branched alkyl radical having up to 6 carbon atoms, alkali metal or ammonium, or a physiologically tolerated salt thereof.
A pharmaceutical composition for the prophylaxis and treatment of hypercholesterolemia comprising an amount effective for use in the therapy of a mammal of a compound as claimed in claim 10 or a physiologically tolerated salt thereof, together with a pharmaceutically acceptable carrier.
Dependencies are inferred from the claim text.