N,N-disubstituted arylcycloalkylamines, the salts thereof, pharmaceutical compositions containing these compounds and the use thereof and processes for preparing them
AssigneeKarl Thomae GmbH
InventorsRoland Maier, Peter Muller, Eberhard Woitun, Rudolf Hurnaus, Michael Mark, Bernhard Eisele, Ralph-Michael Budzinski, Gerhard Hallermayer
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Abstract
The invention relates to N,N-disubstituted arylcycloalkylamines of general formula ##STR1## wherein n, m, A, X and R.sup.1 to R.sup.7 are defined as in claim 1, the isomers, isomer mixtures and salts thereof, which have valuable properties, particularly an inhibitory effect on cholesterol biosynthesis.
Claims2
A method of inhibiting cholesterol biosynthesis in a warm-blooded animal which comprises administering to said animal an effective amount of a N,N-disubstituted arylcycloalkylamine of formula ##STR17## or an enantiomer, diastereomer or physiologically acceptable salt thereof.
A method of inhibiting cholesterol biosynthesis in a warm-blooded animal which comprises administering to said animal an effective amount of an N,N-disubstituted arylcycloalkylamine of formula I ##STR18## wherein n is the integer 1 or 2;
- m is the integer 0 or 1;
- A is a single bond, a straight-chained or branched C.sub.1-17 -alkylene group, a C.sub.2-17 alkenylene group or a C.sub.2-4 -alkynylene group;
- X is a carbonyl or sulphonyl group;
- R.sup.1 is a straight-chained or branched C.sub.1-5 -alkyl group;
- R.sup.2 is a straight-chained or branched C.sub.1-5 -alkyl group which may be substituted by one or two hydroxy groups, by an alkoxy or by an alkylcarbonyloxy group having 1 to 5 carbon atoms in the alkyl moiety, the alkyl moiety being straight-chained or branched, by an alkoxycarbonyloxy group, whilst the above-mentioned substituents may not be bound in position 1 of the alkyl group and two of these groups may not be bound to the same carbon atom, or by an aminocarbonyl, alkylaminocarbonyl, dialkylaminocarbonyl, cyano or alkylcarbonyl group;
- R.sup.3, R.sup.4 and R.sup.5, which may be identical or different, each are a hydrogen atom or an alkyl group;
- R.sup.6 is a hydrogen atom, a straight-chained or branched C.sub.1-6 -alkyl group, a C.sub.3-6 -cycloalkyl group, an allyl or propargyl group or an optionally halogen-substituted benzyl group;
- R.sup.7 is a hydrogen atom, a C.sub.3-6 -cycloalkyl group, a phenyl group optionally substituted by an alkyl group, by one or two halogen atoms or by a trifluoromethyl group, or R.sup.7 is a naphthyl or tetrahydronaphthyl group or a thienyl group optionally substituted by a halogen atom or by an alkyl group;
- whilst A cannot be a single bond if X is a sulphonyl group and R.sup.7 is a hydrogen atom, and
- unless otherwise specified the above-mentioned alkyl and alkoxy moleties may each contain 1 to 3 carbon atoms and the above-mentioned halogen atoms may each be a fluorine, chlorine or bromine atom, or an enantiomer, diastereomer or physiologically acceptable salt thereof.
Dependencies are inferred from the claim text.