Claims
- 1. A compound of formula I, ##STR16## wherein X, Y and Q are independently selected from the group consisting of nitrogen and CH;
- W is selected from the group consisting of hydrogen and --NR.sup.0 R.sup.00 ;
- Z is selected from the group consisting of nitrogen, CH and C--OH;
- A, E, and G are independently selected from the group consisting of a valency bond and an alkylene chain --(CH.sub.2).sub.n- ;
- B is a valency bond or when Z is nitrogen, B is a carbonyl group;
- D is a side chain of the formula --(CHR.sup.3).sub.m --COO-- or .dbd.CR.sup.3 --COO--;
- n is 1-5;
- m is 0 or 1;
- R.sup.1 and R.sup.2 are independently selected from the group consisting of hydrogen, C.sub.1-6 alkyl, and aryl or R.sup.1 and R.sup.2 together form a carbocyclic five-membered or six-membered ring,
- R.sup.3 is selected from the group consisting of hydrogen, --OR.sup.5 and --NR.sup.6 R.sup.7 ;
- R.sup.4 is selected from the group consisting of hydrogen and --OR.sup.5 ;
- R.sup.5 is selected from the group consisting of hydrogen, C.sub.1-6 alkyl, aryl and arylC.sub.1-6 alkyl;
- R.sup.6 is selected from the group consisting of hydrogen, C.sub.1-6 alkyl and arylC.sub.1-6 alkyl;
- R.sup.7 is selected from the group consisting of hydrogen, C.sub.1-6 alkyl, arylC.sub.1-6 alkyl, acyl, C.sub.1-4 alkylsulfonyl and arylsulfonyl;
- R.sup.0 and R.sup.00 are independently selected from the group consisting of hydrogen, C.sub.1-6 alkyl, aryl, arylC.sub.1-6 alkyl, hetaryl, acyl and a carbocyclic or heterocyclic ring which is unsubstituted or substituted at least once with a C.sub.1-6 alkyl, or R.sup.0 and R.sup.00 together with the nitrogen to which they are bound form a five-membered or six-membered ring which is unsubstituted or substituted at least once with a C.sub.1-6 alkyl,
- as well as conformational isomers and pharmacologically acceptable salts thereof.
- 2. The compound according to claim 1, wherein R.sup.0 and R.sup.00 together with the nitrogen to which they are bound form a five-membered or six-membered ring which is unsubstituted or substituted at least once with a C.sub.1-6 alkyl and contains 1-3 additional heteroatoms.
- 3. The compound according to claim 1, wherein n is selected from the group consisting of 1, 2 and 3.
- 4. The compound according to claim 1, wherein each aryl is a phenyl residue.
- 5. The compound according to claim 1, wherein each acyl is independently selected from the group consisting of formyl, acetyl, propionyl, butyryl and benzoyl residues.
- 6. The compound according to claim 1, wherein arylsulfonyl is selected from the group consisting of benzene sulfonic acid and toluene sulfonic acid.
- 7. A compound according to claim 1, wherein said compound is selected from the group consisting of
- 1-[(5S)-2-oxo-3-(3,4,5,6-tetrahydro-2H-[1, 4']bipyridinyl-4-yl)-oxazolidin-5-ylmethyl]piperidine-4-carboxylic acid
- 1-[(rac)-2-oxo-3-(3,4,5,6-tetrahydro-2H-[1,4']bipyridinyl-4-yl)-oxazolidin-5-ylmethyl]-piperidine-4-carboxylic acid
- {1-[(rac)-2-oxo-3-(3,4,5,6-tetrahydro-2H-[1, 4']bipyridinyl 4-yl)-oxazolidin-5-ylmethyl]-piperidin-4-ylidene}-acetic acid
- {4-hydroxy-1-[2-oxo-3-(3,4,5,6-tetrahydro-2H-[1,4']bipyridinyl-4-yl)-oxazolidin-5-ylmethyl]-piperidin-4-yl}-acetic acid
- 1-[4-methyl-2-oxo-3-(3,4,5,6-tetrahydro-2H-[1,4']bipyridinyl-4-yl)-oxazolidin-5-ylmethyl]-piperidine-4-carboxylic acid
- 1-[2-oxo-4-phenyl-3-(3,4,5,6-tetrahydro-2H-[1, 4']bipyridinyl-4-yl)-oxazolidin-5-ylmethyl]-piperidine-4-carboxylic acid
- 1-[2-oxo-3-(1-pyrimidine-4-yl-piperidine-4-yl) oxazolidin-5-ylmethyl]-piperidine-4-carboxylic acid
- 1-{3-[1-(2-benzylamino-pyrimidine-4-yl)-piperidine-4-yl]-2-oxo-oxazolidin-5-ylmethyl}-piperidin-4-carboxylic acid
- 4-hydroxy-4-[2-oxo-3-(3,4,5,6-tetrahydro-2H-[1, 4']bipyridinyl 4-yl)-oxazolidin-5-ylmethyl]-cyclohexanecarboxylic acid
- (5S)-1-[5-methyl-2-oxo-3-(3,4,5,6-tetrahydro-2H-[1,4']bipyridinyl-4-yl) -oxazolidin-5-ylmethyl]-piperidine-4-carboxylic acid
- 1-[2-oxo-3-(3,4,5,6-tetrahydro-2H-[1,4']bipyridinyl-4-yl)-4-(3-trifluoromethylphenyl)-oxazolidin-5-ylmethyl]-piperidine-4-carboxylic acid, and
- 1-[4-(4-chloro-phenyl)-2-oxo-3-(3,4,5,6-tetrahydro-2H -[1,4']bipyridinyl-4-yl)-oxazolidin-5-ylmethyl]-piperidine-4-carboxylic acid
- and the conformational isomers and pharmacologically acceptable salts thereof.
- 8. A pharmaceutical composition for inhibiting the aggregation of blood platelets, comprising an aggregation inhibiting amount of at least one compound according to claim 6 in combination with a pharmaceutically acceptable carrier.
- 9. A method for inhibiting blood platelet aggregation, comprising administering an amount of a compound according to claim 1 effective to inhibit blood platelet aggregation to a patient in need of such treatment.
- 10. A method for treating a condition caused by a thromboembolic occurrence resulting from blood platelet aggregation, comprising administering an amount of a compound according to claim 1 effective to inhibit blood platelet aggregation to a patient in need of such treatment.
- 11. The method according to claim 10, wherein said condition caused by a thromboembolic occurrence is selected from the group consisting of stroke, myocardial infarction and arterial occlusion.
Priority Claims (1)
Number |
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195 24 765 .5 |
Jul 1995 |
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Parent Case Info
This application is a continuation of Ser. No. 08/973,877 filed Jan. 1, 1998, abandoned, which is the national phase of PCT/EP96102939, filed Jul. 4, 1996 published as WO 97/03072 on Jan. 30, 1997.
US Referenced Citations (2)
Continuations (1)
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973877 |
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