Substituted amino compounds, their preparation and their use as

Details Substituted amino compounds, their preparation and their use as Substituted amino compounds, their preparation and their use as

1995-07-18

1997-10-28

Conrad, Joseph

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

514398, 514555, 546152, 5483185, 562439, 562440, 562443, A61K 3147, A61K 31415, A61K 31205

Patent

active

056818386

DESCRIPTION:

BRIEF SUMMARY
The present invention relates to substituted amino compounds, their preparation and their use as inhibitors of blood platelet aggregation.
EP-A 449 079 describes hydantoin derivatives which exhibit thrombocyte-aggregation-inhibiting effects. Further research has shown that the compounds of the present invention are also strong inhibitors of blood platelet aggregation.
The present invention relates to compounds of the general formula I -N(R.sup.2)-(CH.sub.2).sub.n -R.sup.3 (I) -C.sub.6)-alkylene, (C.sub.5 -C.sub.6)-cycloalkylene, phenylene, phenylene-(C.sub.1 -C.sub.6)-alkyl, phenylene-(C.sub.2 -C.sub.6)-alkenyl, phenylene-(C.sub.1 -C.sub.6)-alkylidene and hetylene, where Het represents a 5- or 6-membered ring which can contain up to 3 hetero atoms from the group comprising nitrogen, oxygen and sulphur, and which can be substituted once or twice by (C.sub.1 -C.sub.6)-alkyl or doubly bonded oxygen or sulphur; B denotes a divalent radical from the group comprising (C.sub.1 -C.sub.6)-alkylene, (C.sub.2 -C.sub.6)-alkenylene, phenylene, carbonyl and hetylene, where Het is defined as indicated above; D denotes a divalent radical from the group comprising nitrogen, oxygen, sulphur, carbonyl, carbonyloxy, oxycarbonyl, carbonylimino, iminocarbonyl, iminocarbonylimino and iminothiocarbonylimino, or a natural or unnatural amino acid, imino acid or azaamino acid which is linked in a peptide-like manner via the C- and N-termini, -C(.dbd.NH)-NH-X.sup.1, where o and p represent an integer from 0 to 3; -C.sub.6)-alkoxy, (C.sub.1 -C.sub.6)-alkylcarbonyl, (C.sub.1 -C.sub.6)-alkoxycarbonyl, (C.sub.6 -C.sub.14)-aryloxycarbonyl, (C.sub.6 -C.sub.14)-arylcarbonyl, (C.sub.1 -C.sub.18)-alkylcarbonyloxy-(C.sub.1 -C.sub.6)-alkoxycarbonyl, (C.sub.6 -C.sub.14)-aryl-(C.sub.1 -C.sub.6)-alkoxycarbonyl, cyano, hydroxyl or amino; R' and R" are, independently of each other, defined as X.sup.1 ; --COOR.sup.4, --CO-N(CH.sub.3)-R.sup.4, --CO-NH-R.sup.4 or --CS-NH-R.sup.4 ; tetrazolyl; optionally substituted once or more than once by identical or different radicals from the group comprising hydroxyl, hydroxycarbonyl, aminocarbonyl, mono- or di-(C.sub.1 -C.sub.18)-alkylaminocarbonyl, amino-(C.sub.2 -C.sub.14)-alkylaminocarbonyl, amino-(C.sub.1 -C.sub.3)alkylphenyl-(C.sub.1 -C.sub.3)alkylaminocarbonyl, (C.sub.1 -C.sub.18)-alkylcarbonylamino-(C.sub.1 -C.sub.3)-alkylphenyl-(C.sub.1 -C.sub.3)alkylaminocarbonyl, (C.sub.1 -C.sub.18)-alkylcarbonylamino-(C.sub.2 -C.sub.14)-alkylaminocarbonyl, phenyl-(C.sub.1 -C.sub.8)-alkoxycarbonyl, amino, mercapto, (C.sub.1 -C.sub.18)-alkoxy, (C.sub.1 -C.sub.18)-alkoxycarbonyl, (C.sub.3 -C.sub.8)-cycloalkyl, halogen, nitro, trifluoromethyl or a radical R.sup.5 ; -C.sub.8)-alkyl, a monocyclic 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 sulphur atoms, or denotes a radical R.sup.6, where the aryl radical and, independently thereof, the heterocycle radical can optionally be substituted once or more than once by identical or different radicals from the group comprising (C.sub.1 -C.sub.18)-alkyl, (C.sub.1 -C.sub.18)-alkoxy, halogen, nitro or trifluoromethyl; side chain, a natural or unnatural amino acid residue, imino acid residue, 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 residue or dipeptide residue, in which the peptide bond can be reduced to NH-CH.sub.2, as well as esters and amides thereof, where free functional groups can optionally be substituted by hydrogen or hydroxymethyl or can be protected by protective groups which are customary in peptide chemistry, or denotes a radical --COR.sup.6', in which R.sup.6' is defined as R.sup.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)-alkoxycarbonyl, (C.sub.6 -C.sub.14)-arylcarbonyl, (C.sub.6 -C.sub.14)-aryl-(C.sub.1 -C.sub.8)-alkylcarbonyl, (C.sub.6 -C.sub.14)-aryl-(C.sub.1 -C

REFERENCES:
Int. J. of Peptide and Protein Research, 23(2), 203-211 1984.

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