Dioxopyrrolo pyrrole derivatives

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

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514259, 514292, 514299, 514366, 514411, 514421, 544284, 546 81, 546112, 548151, 548453, A61K 3140, A61K 31495, C07D40304, C07D48706

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active

056864590

ABSTRACT:
Novel dioxopyrrolo-pyrrole derivatives of the formula ##STR1## as well as hydrates or solvates thereof, which inhibit thrombin-induced or Factor Xa-induced platelet aggregation and fibrinogen clotting in blood plasma. The derivatives can be manufactured from the corresponding maleimides which are N-substituted by .alpha.-amino carboxylic acids of the formula HN(R.sup.2)CH(R.sup.4)COOH, or functional derivatives thereof; and ketones or aldehydes of the formula R.sup.5 C(O)R.sup.6.

REFERENCES:
patent: 4912107 (1990-03-01), Kleinschroth et al.
Aly, et al. Non-Decarboxylative 1,3-Dipolar Cycloadditions of Imines of .alpha.-Amino Acids as a Route to Proline Derivatives, Tetrahedron, vol. 50, No. 10, pp. 3159-3168 (1994).
Grigg, et al., The Decarboxylative Route to Azomethine Ylides. Stereochemistry of 1,3-Dipole Formation, J. Chem. Soc., Chem. Commun. pp. 47-49 (1987).
Grigg, et al. X=Y-ZH Systems as Potential 1,3-Dipoles, Part 11. Stereochemistry of 1,3-Dipoles Generated by the Decarboxylative Route to Azomethine Ylides, J. Chem. Soc. Perkin Trans. I pp. 2693-2701 (1988).
Grigg, et al., The Decarboxylative Route to Azomethine Ylides. Mechanism of 1,3-Dipole Formation, J. Chem. Soc. Chem. Commun. pp. 49-51 (1987).

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