(3R)-3-amino-4-carboxybutyraldehyde derivatives inhibiting the release of interleukin-1/beta

This invention relates to new (3R)-3-amino-4-carboxy-butyraldehyde derivatives of general formula (I), The invention relates to a new (3R)-3-amino-4-carboxybutyraldehyde derivatives of general formula(I) wherein X represents a Calkyloxycarbonyl, an optionally substituted phenyl-(Calkyloxy)-carbonyl,...

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Hauptverfasser: Bajusz, Sandor, Veghelyi, Iren, Nemeth, Klara, Barabas, Eva, Juhasz, Attila, Lango, Jozsef, Lavich, Emilia, Mohai, Zsuzsanna, Moravcsik, Imre, Taschler, Zsuzsanna, Toth, Gabor
Format: Patent
Sprache:eng
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Zusammenfassung:This invention relates to new (3R)-3-amino-4-carboxy-butyraldehyde derivatives of general formula (I), The invention relates to a new (3R)-3-amino-4-carboxybutyraldehyde derivatives of general formula(I) wherein X represents a Calkyloxycarbonyl, an optionally substituted phenyl-(Calkyloxy)-carbonyl, a Calkylcarbonyl or an optionally substituted phenyl-(Calkyl)-carbonyl group, n represents 1 or 0, Y represents, in the case when n=1, a tetrapeptide of general formula Y-Y-Y-Y, a tripeptide of general formula Y-Y-Yor a dipeptide of general formula Y-Yor an amino acid residue of general formula Y, or in the case when n=0, an -hydroxyacyl-tripeptide of general formula Q-Y-Y-Y, an -hydroxyacyl-dipeptide of general formula Q-Y-Yor an -hydroxyacyl-aminoacyl residue of general formula Q-Y; wherein Y-Yrepresent a residue selected from the group of the following L- or D-amino acids: alanine, alloisoleucine, cyclohexyl-glycine, phenyl-alanine, glutamine, histidine, isoleucine, leucine, lysine, methionine, pipecolic acid, proline, tyrosine and valine; and Q-Qrepresent an acyl group selected from the following -hydroxyacids of R or S configuration: 2-cycloheptyl-2-hydroxy-acetic acid, 2-cyclohexyl-2-hydroxyacetic acid, 3-cyclohexyllactic acid, 3-phenyllactic acid, 2-hydroxy-3-methylbutyric acid, 2-hydroxy-3-methylvaleric acid, mandelic acid or lactic acid, and salts thereof formed with organic or inorganic bases, and pharmaceutical compositions containing the same. The compounds of general formula (I) of the invention are valuable inhibitors of the interleukin-1 converting enzyme.