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US 5,686,421 AGranted
Hydantoin derivates
AssigneeHoechst Aktiengesellschaft
InventorsWolfgang Konig, Melitta Just, Bernd Jablonka
Life of this patent
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Abstract
Hydantoin derivatives of the formula I ##STR1## in which n is 3 or 4, R.sup.1 is alkyl or a radical of the formula R'--NH--C.dbd.N--R" with R' and R" being hydrogen or alkyl, and R.sup.2 is hydrogen, --NH--CO--NH.sub.2 and optionally substituted alkyl, and a process for the preparation thereof and the use thereof for inhibiting platelet aggregation, are described.
Claims13
A compound of the formula I ##STR29## in which n is an integer 3 or 4;
- R.sup.1 is C.sub.1 -C.sub.6 -alkyl or a radical of the formula II ##STR30## in which R' and R" are, independently of one another, hydrogen or C.sub.1 -C.sub.6 -alkyl;
- R.sup.2 is hydrogen, --NH--CO--NH.sub.2 or C.sub.1 -C.sub.18 -alkyl which is optionally substituted one or more times by identical or different radicals from the series comprising hydroxyl, carbamoyl, carboxyl, carboxamido, amino, mercapto, C.sub.1 -C.sub.18 -alkoxy, guanidino, C.sub.3 -C.sub.8 -cycloalkyl, halogen, nitro, trifluoromethyl and a radical R.sup.3, where
- R.sup.3 is C.sub.6 -C.sub.14 -aryl, C.sub.8 -C.sub.14 -aryl-C.sub.1 -C.sub.8 -alkyl or a mono- or bicyclic 5- to 12-membered heterocyclic ring which can be aromatic, partially hydrogenated or completely hydrogenated and which can contain as hetero element one, two or three identical or different nitrogen, oxygen or sulfur atoms, where the aryl and, independently of one another, the heterocyclic radical is optionally substituted one or more times by identical or different radicals from the series comprising C.sub.1 -C.sub.18 -alkyl, C.sub.1 -C.sub.18 -alkoxy, halogen, hydroxyl, nitro and trifluoromethyl;
- or is a radical R.sup.4 ;
- where
- R.sup.4 is NR.sup.5 R.sup.6 ;
- OR.sup.5 ;
- SR.sup.5 ;
- an amino-acid side-chain;
- a residue of a natural or unnatural amino acid, imino acid, optionally N--C.sub.1 -C.sub.8 -alkylated or C.sub.6 -C.sub.14 -aryl-C.sub.1 -C.sub.8 -alkylated azaamino acid or a dipeptide in which the peptide linkage can be reduced to NH--CH.sub.2, and the esters and amides thereof, where free functional groups can optionally be replaced by hydrogen or hydroxymethyl or protected by the protective groups customary in peptide chemistry;
- or is a radical COR.sup.4' in which R.sup.4' is defined as R.sup.4 ;
- R.sup.5 is hydrogen, optionally amino group-substituted C.sub.1 -C.sub.18 -alkyl, C.sub.6 -C.sub.14 -aryl, C.sub.6 -C.sub.14 -aryl-C.sub.1 -C.sub.8 -alkyl, C.sub.1 -C.sub.18 -alkylcarbonyl, C.sub.1 -C.sub.18 -alkyloxycarbonyl, C.sub.6 -C.sub.14 arylcarbonyl, C.sub.6 -C.sub.12 -aryl-C.sub.1 -C.sub.8 -alkylcarbonyl, C.sub.6 -C.sub.18 -aryl-C.sub.1 -C.sub.18 -alkyloxycarbonyl, a residue of a natural or unnatural amino acid, imino acid, optionally N--C.sub.1 -C.sub.8 -alkylated or C.sub.6 -C.sub.14 -aryl-C.sub.1 -C.sub.8 -alkylated azaamino acid or a dipeptide in which the peptide linkage can be reduced to NH--CH.sub.2 ;
- R.sup.5 is hydrogen, C.sub.1 -C.sub.18 -alkyl, C.sub.6 -C.sub.12 -aryl or C.sub.6 -C.sub.12 -aryl-C.sub.1 -C.sub.8 -alkyl;
- or a physiologically acceptable salt thereof.
11 more elements
Dependencies are inferred from the claim text.