(3r)-3-amino-4-carboxybutyraldehyde derivatives inhibiting...

C - Chemistry – Metallurgy – 07 – K

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C07K 5/02 (2006.01) A61K 38/07 (2006.01) C07K 7/02 (2006.01) C07K 14/81 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2288332

The invention relates to new (3R)-3-amino-4-carboxybutyraldehyde derivatives of general formula (I), wherein X represents a C1-4 alkyloxycarbonyl, an optionally substituted phenyl-(C1-2 alkyloxy)-carbonyl, a C1-4 alkylcarbonyl or an optionally substituted phenyl-(C1-3 alkyl)-carbonyl group, n represents 1 or 0, Y represents, in the case when n = 1, a tetrapeptide of general formula Y 4-Y3-Y2-Y1, a tripeptide of general formula Y3-Y2-Y1 or a dipeptide of general formula Y2-Y1 or an amino acid residue of general formula Y1, or in the case when n = 0, an .alpha.-hydroxyacyl-tripeptide of general formula Q4- Y3-Y2-Y1, an .alpha.-hydroxyacyl-dipeptide of general formula Q3-Y2-Y1 or an .alpha.-hydroxyacyl-aminoacyl residue of general formula Q2-Y1; wherein Y1-Y4 represent 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-Q4 represent an acyl group selected form the following .alpha.-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.beta. converting enzyme.

L'invention concerne de nouveaux dérivés de (3R)-3-amino-4-carboxybutyraldehyde de formule générale (I), dans laquelle X représente un groupe alkyle oxycarbonyle C¿1-4?, un groupe phényl-(alkyloxy C¿1-2?)-carbonyle éventuellement substitué, un groupe alkylcarbonyle C¿1-4? ou bien un groupe phényl-(alkyl C¿1-3?)-carbonyle éventuellement substitué, n vaut 1 ou 0, Y représente, dans le cas où n = 1, un tétrapeptide de formule générale Y¿4?-Y¿3?-Y¿2?-Y¿1?, un tripeptide de formule générale Y¿3?-Y¿2?-Y¿1? ou bien un dipeptide de formule générale Y ¿2?-Y¿1? ou encore un résidu aminoacide de formule générale Y¿1?, ou bien dans le cas où n = 0, un tripeptide d'.alpha.-hydroxyacyle de formule générale Q¿4?-Y¿3?-Y¿2?-Y¿1?, un dipeptide d'.alpha.-hydroxyacyle de formule générale Q¿3?-Y¿2?-Y¿1? ou bien un résidu .alpha.-hydroxyacyl-aminoacyle de formule générale Q¿2?-Y¿1?, où Y¿1?-Y¿4? représentent un résidu choisi dans le groupe des acides aminés L ou D suivants: alanine, alloisoleucine, cyclohexyl-glycine, phényl-alanine, glutamine, histidine, isoleucine, leucine, lysine, méthionine, acide pipécolique, proline, tyrosine et valine, et Q¿2?-Q¿4? représentent un groupe acyle choisi parmi les .alpha.-hydroxyacides de configuration R ou S suivants: acide 2-cycloheptyl-2-hydroxyacétique, acide 2-cyclohexyl-2-hydroxyacétique, acide 3-cyclohexyllactique, acide 3-phényllactique, acide 2-hydroxy-3-méthylbutyrique, acide 2-hydroxy-3-méthylvalérique, acide mandélique ou acide lactique, ainsi que leurs sels formés avec des bases organiques ou inorganiques, et des compositions pharmaceutiques les contenant. Les composés de formule générale (I) sont de précieux inhibiteurs de l'enzyme de conversion de l'interleukine-1.beta..

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