C - Chemistry – Metallurgy – 07 – K
Patent
C - Chemistry, Metallurgy
07
K
C07K 11/00 (2006.01) A61K 38/03 (2006.01) A61K 38/15 (2006.01) C07K 4/00 (2006.01) C07K 5/06 (2006.01) C07K 5/072 (2006.01) C07K 5/103 (2006.01) C07K 5/113 (2006.01) C07K 7/06 (2006.01) A61K 38/00 (2006.01)
Patent
CA 2259159
Depsipeptides represented by general formula (1) or pharmacologically acceptable salts thereof, wherein R1 represents linear or branched C5-20 alkyl or linear or branched C5-15 alcoxymethyl; R2 represents -A-B, -A-B-W, -A-B-W-D or -A-B-W-D-E; and R3 represents hydroxy, lower alkoxy, benzyloxy, -Z, -Z-G or -Z-G-J, wherein A, B, D, E, G and J independently represent each an amino acid residue selected from among alanine, valine, leucine, isoleucine, serine, threonine, lysine, hydroxylysine, arginine, cysteine, methionine, phenylalanine, tyrosine, aspartic acid, asparagine, glutamic acid, glutamine, etc. optionally bonded to N-(C1-4 alkyl); W and Z independently represent each an animo acid residue selected from among aspartic acid, asparagine, glutamic acid, glutamine, alanine, serine, and lysine. These depsipeptides have the effects of promoting apolipoprotein E production and are useful as remedies for nerve injury and, in particular, remedies for dementia. They are also useful as remedies for hyperlipemia.
Cette invention se rapporte à des dépsipeptides représentés par la formule générale (1) ou à des sels de ces composés acceptables sur le plan pharmacologique. Dans cette formule, R¿1? représente alkyle C¿5-20? linéaire ou ramifié ou alcoxyméthyle C¿5-15? linéaire ou ramifié; R¿2? représente -A-B, -A-B-W, -A-B-W-D ou -A-B-W-D-E; and R¿3? représente hydroxy, alcoxy inférieur, benzyloxy, -Z, -Z-G ou -Z-G-J, où A, B, D, E, G et J représentent chacun séparément un reste d'acide aminé choisi parmi alanine, valine, leucine, isoleucine, sérine, thréonine, lysine, hydroxylysine, arginine, cystéine, méthionine, phénylalanine, tyrosine, acide aspartique, asparagine, acide glutamique, glutamine, etc., avec liaison éventuelle à N-(alkyle C¿1-4?); W et Z représentent chacun séparément un reste d'acide aminé choisi parmi acide aspartique, asparagine, acide glutamique, glutamine, alanine, sérine et lysine. Ces dépsipeptides ont pour effet de promouvoir la production d'apolipoprotéines E et sont utiles comme remèdes contre les lésions nerveuses et, en particulier, comme remèdes contre la démence. Ils sont également utiles comme remèdes contre l'hyperlipémie.
Hiramoto Shigeru
Kawamura Koji
Kinoshita Nobuhiro
Oshida Norio
Shingai Akiko
Nisshin Flour Milling Co. Ltd.
Nisshin Seifun Group Inc.
Ogilvy Renault Llp/s.e.n.c.r.l.,s.r.l.
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