Substituted 5-membered ring heterocycles, their preparation and

Details Substituted 5-membered ring heterocycles, their preparation and Substituted 5-membered ring heterocycles, their preparation and

1996-07-19

1999-11-09

Higel, Floyd D.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Peptide containing doai

514 18, 514 19, 514385, 514389, 514391, 514398, 5483181, 5483185, 5483191, A61K 3702, A61K 31415, C07D23376, C07D23396, C07D22372, C07D26344

Patent

active

059814926

DESCRIPTION:

BRIEF SUMMARY
The present invention relates to substituted 5-membered ring heterocycles, their preparation and their use as medicines, in particular as inhibitors of blood platelet aggregation.
EP-A-449 079, EP-A-530 505, EP-A-566 919 and WO-A-93/18057 describe hydantoin derivatives which exhibit thrombocyte aggregation-inhibiting effects. EP-A 512 831 mentions pyrrolidone derivatives which prevent the binding of fibrinogen to blood platelets and hence aggregation of the platelets. Further investigations demonstrated that the compounds of the present invention are also strong inhibitors of blood platelet aggregation.
The present invention relates to 5-membered ring heterocycles of the general formula I, ##STR2## in which W represents R.sup.1 --A--C(R.sup.13) or R.sup.1 --A--CH.dbd.C; (C.sub.3 -C.sub.7)-cycloalkylene, phenylene, phenylene-(C.sub.1 -C.sub.6)-alkyl, (C.sub.1 -C.sub.6)-alkylene-phenyl or phenylene-(C.sub.2 -C.sub.6)-alkenyl, or a divalent radical of a 5-membered or 6-membered saturated or unsaturated ring which can contain 1 or 2 nitrogen atoms and can be substituted once or twice by (C.sub.1 -C.sub.6)-alkyl or doubly bonded oxygen or sulphur; (C.sub.2 -C.sub.6)-alkenylene, phenylene, phenylene-(C.sub.1 -C.sub.3)-alkyl or (C.sub.1 -C.sub.3)-alkylene-phenyl; NHS(O).sub.2 or R.sup.10 CO; -C.sub.8)-alkyl, (C.sub.3 -C.sub.8)-cycloalkyl, optionally substituted (C.sub.6 -C.sub.14)-aryl, or (C.sub.6 -C.sub.14)-aryl-(C.sub.1 -C.sub.8)-alkyl which is optionally substituted in the aryl radical; --NH--(CH.sub.2).sub.p, where p can represent an integer from 0 to 3; -C.sub.6)-alkylcarbonyl, (C.sub.1 -C.sub.6)-alkoxycarbonyl, (C.sub.1 -C.sub.18)-alkylcarbonyloxy-(C.sub.1 -C.sub.6)-alkoxycarbonyl, optionally substituted (C.sub.6 -C.sub.14)-aryloxycarbonyl, (C.sub.6 -C.sub.14)-aryl-(C.sub.1 -C.sub.6)-alkoxycarbonyl which can also be substituted in the aryl radical, (R.sup.8 O).sub.2 P(O), cyano, hydroxyl, (C.sub.1 -C.sub.6)-alkoxy, (C.sub.6 -C.sub.14)-aryl-(C.sub.1 -C.sub.6)-alkoxy which can also be substituted in the aryl radical, or amino; where R' and R", independently of each other, have the meanings of X; (C.sub.6 -C.sub.14)-aryl, (C.sub.6 -C.sub.14)-aryl-(C.sub.1 -C.sub.8)-alkyl which is optionally substituted in the aryl radical, or (C.sub.3 -C.sub.8)-cycloalkyl; (C.sub.6 -C.sub.14)-aryl, (C.sub.6 -C.sub.14)-aryl-(C.sub.1 -C.sub.8)-alkyl which is optionally substituted in the aryl radical, (C.sub.3 -C.sub.8)-cycloalkyl, (C.sub.2 -C.sub.8)-alkenyl, (C.sub.2 -C.sub.8)-alkynyl, (C.sub.2 -C.sub.8)-alkenylcarbonyl, (C.sub.2 -C.sub.8)-alkynlcarbonyl, pyridyl, R.sup.11 NH, R.sup.4 CO, COOR.sup.4, CON(CH.sub.3)R.sup.14, CONHR.sup.14, CSNHR.sup.14, COOR.sup.15, CON(CH.sub.3)R.sup.15 or CONHR.sup.15 ; be substituted once or more than once by identical or different radicals R.sup.4' ; di-((C.sub.1 -C.sub.18)-alkyl)-aminocarbonyl, amino-(C.sub.2 -C.sub.18)-alkylamino-carbonyl, amino-(C.sub.1 -C.sub.3)-alkyl-phenyl-(C.sub.1 -C.sub.3)-alkylamino-carbonyl, (C.sub.1 -C.sub.18)-alkylcarbonylamino-(C.sub.1 -C.sub.3)-alkylphenyl-(C.sub.1 -C.sub.18)-alkylaminocarbonyl, (C.sub.1 -C.sub.18)-alkylcarbonylamino-(C.sub.2 -C.sub.18)-alkylaminocarbonyl, (C.sub.6 -C.sub.14)-aryl-(C.sub.1 -C.sub.8)-alkoxy-carbonyl which can also be substituted in the aryl radical, amino, mercapto, (C.sub.1 -C.sub.18)-alkoxy, (C.sub.1 -C.sub.18)-alkoxycarbonyl, optionally substituted (C.sub.3 -C.sub.8)-cycloalkyl, halogen, nitro, trifluoromethyl or the radical R.sup.5 ; -C.sub.14)-aryl-(C.sub.1 -C.sub.8)-alkyl which is optionally substituted in the aryl radical, a monocyclic or bicyclic 5- to 12-membered heterocyclic ring which can be aromatic, partially hydrogenated or completely hydrogenated and which can contain one, two or three identical or different heteroatoms from the group nitrogen, oxygen and sulphur, a radical R.sup.6 or a radical R.sup.6 CO--, where the aryl radical and, independently thereof, the heterocycle radical can be substituted once or more than once by identical or different radicals from the group (C.sub.1 -C.sub.18)-alkyl, (C.sub.1 -C.sub.

REFERENCES:
patent: 3300510 (1967-01-01), Auburn et al.
patent: 5389614 (1995-02-01), Konig et al.
patent: 5397796 (1995-03-01), Zoller et al.
patent: 5424293 (1995-06-01), Zoller et al.

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