Nisshin Flour Milling Co., Ltd.

Nisshin Seifun Group Inc.

Akiko Shingai

Shigeru Hiramoto

Masashi Suzuki

Makoto Yanai

Norio Oshida

Koji Kawamura

Nobuhiro Kinoshita

Orie Yasuda

Masako Takasu

Yukio Saito

Shigeo Hatanaka

Cyclic depsipeptides represented by the formulawherein: R is a straight or branched alkyl group of 5-20 carbon atoms or a straight or branched alkoxymethyl group of 5-15-carbon atoms; A, B, D, E and F independently each other are alanine, valine, leucine, isoleucine, phenylalanine, etc.; W and Z independently each other are aspartic acid, asparagine, glutamic acid or glutamine; and m and n independently each other is 0 or 1, or pharmacologically acceptable salts thereof. The present compounds are prepared according to a method conventionally used in peptide synthesis. The present compounds are useful as an agent for promoting the production of apolipoprotein E, a therapeutic agent for neurologic damages, a therapeutic agent for dementia, an agent for inhibiting the production of apolipoprotein B, an agent for promoting the production of apolipoprotein A1 or a therapeutic agent for hyperlipemia.

Cyclic depsipeptides and drugs containing the same as the active ingredient

A depsipeptide containing N-substituted glycine residue having the formula (1) or (2):

Depsipeptides containing N-substituted glycine residue

The present invention provides a new depsipeptide derivative having a piperazinone ring within the molecule which is represented by formula (1)

Depsipeptide derivatives bearing piperazinone rings

Depsipeptides represented by the formula (1):

Depsipeptides and drugs containing the same as the active ingredient

A depsipeptide containing a non-natural amino acid(s) having the formula (1)

Depsipeptides containing non-natural amino acids

The present invention provides a bicyclic depsipeptide having the formula (1)

Bicyclic depsipeptides

A depsipeptide containing N-substituted glycine residue having the formula (1) or (2): ##STR1## (wherein R.sub.1 is a straight or branched alkyl group of 5-20 carbon atoms or a straight or branched alkoxymethyl group of 5-15 carbon atoms; R.sub.2 is a group of the formula --A--B--W--(D).sub.m --(E).sub.n, --A--B--W--(D).sub.m --(E).sub.n --F or --A--B--W--(D).sub.m --(E).sub.n --F--Z; R.sub.3 is a hydroxyl group, a lower alkoxy group, a benzyloxy group, or a group of the formula --Z, --Z--G or --Z--G--J; A, B, D, E, F, G and J independently are an N-substituted glycine residue or a residue of an amino acid selected from the group consisting of alanine, valine, leucine, serine, etc.; W and Z independently are a residue of an amino acid selected from the group consisting of an aspartic acid, a glutamic acid, etc.; at least one of A, B, D, E, F, G and J is an N-substituted glycine residue) or a pharmacologically acceptable salt thereof. The above depsipeptides have a promoting activity on the production of apolipoprotein E, and are useful as a therapeutic agent for neurologic damages, especially dementia, and hyperlipemia.

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Saitama-ken, Japan

Akiko Shingai