Cyclic depsipeptides and drugs containing the same as the...

C - Chemistry – Metallurgy – 07 – K

Patent

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C07K 11/02 (2006.01) A61K 38/08 (2006.01) A61K 38/15 (2006.01) C07K 7/06 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2258487

Cyclic depsipeptides represented by general formula (1) or pharmacologically acceptable salts thereof, wherein R represents linear or branched C5-20 alkyl or linear or branched C5-15 alkoxymethyl; A, B, D, E and F independently represent each alanine, valine, leucine, isoleucine, phenylalanine, etc.; W and Z independently represent each aspartic acid, asparagine, glutamic acid or glutamine; and m and n independently represent each 0 or 1. These compounds are produced by the conventional methods for synthezing peptides. They are useful as apolipoprotein E production promoters, remedies for nerve injury, remedies for dementia, apolipoprotein B production inhibitors, apolipoprotein A1 production promoters and remedies for hyperlipemia.

Cette invention se rapporte à des dépsipeptides cycliques représentés par la formule générale (1) ou à des sels de ces composés acceptables sur le plan pharmacologique. Dans ladite formule, R représente alkyle C¿5-20? linéaire ou ramifié ou alcoxyméthyle C¿5-15? linéaire ou ramifié; A, B, D, E et F représentent chacun séparément alanine, valine, leucine, isoleucine, phénylalanine, etc.; W et Z représentent chacun séparément de l'acide aspartique, de l'asparagine, de l'acide glutamique ou de la glutamine; et m et n représentent chacun séparément 0 ou 1. Ces composés sont produits par les procédés traditionnels de synthèse de peptides. Ils sont utiles comme promoteurs de production de l'apolipoprotéine E, comme remèdes contre les lésions nerveuses, comme remèdes contre la démence, comme inhibiteurs de production de l'apolipoprotéine B, comme promoteurs de production de l'apolipoprotéine A1 et comme remèdes contre l'hyperlipémie.

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