Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1996-01-17
1997-08-19
Haley, Jacqueline
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
548132, 548227, 5483195, 548544, 548253, 514364, 514376, 514389, 514425, A61K 3140, A61K 3142, C07D20746, C07D23134
Patent
active
056589352
DESCRIPTION:
BRIEF SUMMARY
This is a national stage application of PCT/EP94/00481 filed Feb. 19, 1994 and published as WO 94/21607.
The present invention relates to substituted hetero-cycles, their preparation and their use as medicines, in particular as inhibitors of blood platelet aggregation.
EP-A 449 079 and EP-A 530 505 describe hydantoin derivatives which have platelet aggregation-inhibiting effects. EP-A 512 831 describes compounds which prevent fibrinogen binding to blood platelets and, as a result, the aggregation of the platelets. Further investigations showed that the compounds of the present invention are also potent inhibitors of blood platelet aggregation.
The present invention relates to novel heterocycles of the general formula I ##STR2## in which Z.sup.1 denotes ##STR3## Z.sup.2 denotes ##STR4## or --CH.sub.2 --; Y denotes --(CH.sub.2).sub.m CO--, where m stands for an integer from 1 to 4, or denotes --CHR.sup.s --CO-- or ##STR5## r denotes an integer from 0 to 3; A denotes --CHR.sup.1 --, --NR.sup.1 -- or X.sup.1 --C.sub.6 H.sub.4 --CH.dbd.C<; ; -C.sub.14)-aryl-(C.sub.1 -C.sub.8)-alkoxy, which can also be substituted in the aryl radical, optionally substituted (C.sub.6 -C.sub.14)-aryloxy, amino or mono- or di-((C.sub.1 -C.sub.18)-alkyl)amino; ##STR6## or --(CH.sub.2).sub.n --NH--X or --(CH.sub.2).sub.p --C.sub.6 H.sub.4 --(CH.sub.2).sub.q --NH--X or --(CH.sub.2).sub.p --C(.dbd.NX)--NH.sub.2 or --(CH.sub.2).sub.p --C.sub.6 H.sub.4 --(CH.sub.2).sub.q --C(.dbd.NX)--NH.sub.2, in which n stands for a number from 1 to 6, p and q independently of one another stand for a number from 0 to 3 and t stands for a number from 0 to 2, but where, if A denotes --CHR.sup.1 -- or --NR.sup.1, B and Z.sup.2 denote --CH.sub.2 --, Y denotes --(CH.sub.2).sub.m CO--, in which m is an integer from 1 to 4, R denotes hydrogen and r is the number 1, then, not at the same time ##STR7## or --(CH.sub.2).sub.n' NH--X or --(CH.sub.2).sub.p' --C(.dbd.NX)--NH.sub.2, in which n' stands for a number from 1 to 4, p' stands for a number from 1 to 3 and t' stands for the numbers 1 or 2; -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)-arylcarbonyl, 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, cyano, hydroxyl, (C.sub.1 -C.sub.6)-alkoxy or amino or a radical of the formula II -C.sub.6)-alkyl, trifluoro-(C.sub.1 -C.sub.6)-alkyl, (C.sub.1 -C.sub.6)-alkoxycarbonyl, (C.sub.1 -C.sub.6)-alkylcarbonyl, optionally substituted (C.sub.6 -C.sub.14)-arylcarbonyl, (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, cyano, hydroxyl, (C.sub.1 -C.sub.6)-alkoxy or amino; --C(.dbd.NX)--NH.sub.2 in which p and q stand for a number from 0 TO 3; (C.sub.1 -C.sub.4)-alkyl and the phenyl can be unsubstituted or mono- or polysubstituted by identical or different radicals from the series hydroxyl, amino, (C.sub.1 -C.sub.4)-alkoxy, imidazolyl, indolyl, pyrrolidinyl, hydroxypyrrolidinyl, phenyl or halogen; --CO--NH--R.sup.4 ; be mono- or polysubstituted by identical or different radicals from the series hydroxyl, hydroxycarbonyl, aminocarbonyl, mono- or di-((C.sub.1 -C.sub.18)-alkyl)aminocarbonyl, amino-(C.sub.2 -C.sub.18)-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.18)-alkylaminocarbonyl, (C.sub.6 -C.sub.14)-aryl-(C.sub.1 -C.sub.8)-alkoxycarbonyl, 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, halo
REFERENCES:
patent: 5389614 (1995-02-01), Konig et al.
patent: 5397796 (1995-03-01), Zoller et al.
patent: 5424293 (1995-06-01), Zoller et al.
Breipohl Gerhard
Jablonka Bernd
Just Melitta
Klingler Otmar
Knolle Jochen
Haley Jacqueline
Hoechst Aktiengesellschaft
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