4818-01-3Relevant academic research and scientific papers
(3R)-3-amino-4-carboxybutyraldehyde derivatives inhibiting the release of interleukin-1/beta
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, (2008/06/13)
The invention relates to a new (3R)-3-amino-4-carboxybutyraldehyde derivatives of general formula(I) wherein X represents a C1-4alkyloxycarbonyl, an optionally substituted phenyl-(C1-2alkyloxy)-carbonyl, a C1-4alkylcarbonyl or an optionally substituted phenyl-(C1-3alkyl)-carbonyl group, n represents 1 or 0, Y represents, in the case when n=1, a tetrapeptide of general formula Y4-Y3-Y2-Y1, a tripeptide of general formula Y3-Y2-Y1or a dipeptide of general formula Y2-Y1or an amino acid residue of general formula Y1, or in the case when n=0, an α-hydroxyacyl-tripeptide of general formula Q4-Y3-Y2-Y1, an α-hydroxyacyl-dipeptide of general formula Q3-Y2-Y1or an α-hydroxyacyl-aminoacyl residue of general formula Q2-Y1; wherein Y1-Y4represent 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 Q2-Q4represent an acyl group selected from the following α-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-1β converting enzyme.
