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US 4,734,406 AGranted
3-pyridylmethylnaphthyl derivatives and composition containing them useful to inhibit thromboxane synthetase
AssigneeHoechst Aktiengesellschaft
InventorsHans-Hermann Lau, Wilhelm Bartmann, Gerhard Beck, Gunther Wess
Life of this patent
Estimating the term…
Abstract
Compounds of the formula I ##STR1## in which R.sup.1, R.sup.2, R.sup.3 and Y have the indicated meanings, their physiologically tolerated acid addition salts, and a process for the preparation of these compounds, are described. The compounds inhibit thromboxane synthetase and can thus be used as medicaments.
Claims4
A compound of the formula I ##STR14## in which:
- R.sup.1 denotes hydrogen or, in the 2-, 4-, 5- or 6- position, halogen, a straight chain or branched alkyl radical having 1-6 carbon atoms, a cycloalkyl radical having 3-7 carbon atoms, a phenyl C.sub.1 -C.sub.2 -alkyl radical or a phenyl radical, each of which can be substituted 1-3 times in the phenyl nucleus by halogen, alkyl and/or alkoxy, each having 1-6 carbon atoms, or denotes a hydroxyl radical or an alkoxy radical having 1-6 carbon atoms,
- R.sup.2 denotes a hydroxyl radical, halogen, an alkoxy radical having 1-6 carbon atoms, or a phenoxy radical which can be substituted 1-3 times in the phenyl nucleus by halogen, trifluoromethyl, alkyl and/or alkoxy, each having 1-6 carbon atoms,
- R.sup.3 denotes hydrogen, a cycloalkyl radical having 3-7 carbon atoms, a straight-chain or branched alkyl radical having 1-8 carbon atoms, a straight-chain or branched unsaturated aliphatic hydrocarbon radical having up to 8 carbon atoms and up to 3 double or triple bonds, a phenyl radical which can be substituted 1-3 times in the phenyl nucleus by halogen, trifluoromethyl, hydroxyl, alkyl and/or alkoxy, each having 1-6 carbon atoms, or denotes a 2-, 3- or 4-pyridyl radical which can be substituted in the 4- or 5- position by C.sub.1 - C.sub.4 -alkyl,
- Y denotes a radical of the formula CO.sub.2 R.sup.5, ##STR15## or CH.sub.2 OH, R.sup.5 denoting hydrogen, a straight chain or branched alkyl radical having up to 8 carbon atoms, a straight-chain or branched unsaturated aliphatic hydrocarbon radical having up to 6 carbon atoms, a cycloaliphatic hydrocarbon radical having 3 to 7 carbon atoms, an araliphatic hydrocarbon radical having 7 to 10 carbon atoms, or a physiologically tolerated metal ion, NH.sub.4 ion or an ammonium ion which is derived from a primary, secondary or tertiary amine, or a tetraalkylammonium ion,
- R.sup.6 denoting hydrogen, a straight chain or branched alkyl radical having 1-6 carbon atoms, a cycloaliphatic hydrocarbon radical having 3-7 carbon atoms, an araliphatic hydrocarbon radical which has 7-10 carbon atoms and can be substituted 1-3 times in the aryl nucleus by halogen, trifluoromethyl, alkyl and/or alkoxy, each having 1-6 carbon atoms, or denoting a phenyl radical which can be substituted 1-3 times in the phenyl nucleus by halogen, trifluoromethyl, alkyl and/or alkoxy, each having 1-6 carbon atoms,
- R.sup.7 denoting hydrogen, a straight chain or branched alkyl radical having 1-6 carbon atoms, or
- R.sup.6 and R.sup.7 together denoting a --(CH.sub.2).sub.n --group with n= 3-6, or a --(CH.sub.2).sub.p --Z--(CH.sub.2).sub.p -- group with p=2 or 3,
- Z being oxygen or N--R.sup.8,
- R.sup.8 denoting hydrogen or a straight-chain or branched alkyl radical having 1-6 carbon atoms,
- or a physiologically tolerated acid addition salt thereof, with the exception of the compounds of the formula 1 in which, when Y denotes the radicals --CONH.sub.2 or COOR.sup.5, with R.sup.5 denoting hydrogen or C.sub.1 -C.sub.6 -alkyl, R.sup.1 and R.sup.3 represent hydrogen.
7 more elements
Dependencies are inferred from the claim text.