Nisshin Flour Milling Co., Ltd.

Nisshin Seifun Group Inc.

Kyorin Pharmaceutical Co., Ltd.

Nisshin Pharma Inc.

Nobuhiro Kinoshita

Makoto Yanai

Shigeru Hiramoto

Norio Oshida

Koji Kawamura

Masashi Suzuki

Akiko Shingai

Orie Yasuda

Masako Takasu

Noriyoshi Sueda

Masato Horigome

Katsutoshi Miura

Koichi Katsuyama

Kazuhiko Yamada

Yoko Tsukada

Fumihisa Nakata

Toshihiro Takahashi

Yoshiyuki Tahara

Hitoshi Inoue

Masahiro Ueno

Hiroki Kato

Satoko Fuchizawa

Koichi Katasuyama

This invention relates to a medicament containing as an active ingredient, a novel propanolamine having a 1,4-benzodioxane ring or a pharmaceutically acceptable salt thereof: The present compound is represented by the above formula wherein Rmay be the same or different and each represents a hydrogen atom, a halogen atom, a hydroxy group, a (C&#x2013;C)alkyl group, a (C&#x2013;C)alkoxy group, a (C&#x2013;C)alkylsulfonamido group, or a phenyl group; Reach represents a hydrogen atom or a (C&#x2013;C)alkyl group; and A represents any of a benzene ring, a pyridine ring and a pyrimidine ring. This compound is useful as a prophylactic or therapeutic agent for diabetes, obesity, hyperlipemia, depression, a respiratory disease, or a gastrointestinal disease.

Propanolamine derivative having 1, 4-benzodioxane ring

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.

Urea derivatives of formula (I) ##STR1## wherein the valuable groups are as defined in the specification, which possess both an ACAT inhibitory activity and an antioxidative activity. Those derivatives are useful in the prophylaxis and treatment of hypercholesterolemia and atherosclerosis.

Urea derivatives and their use as ACAT inhibitors

Urea derivatives of formula (1) ##STR1## wherein the valuable groups are as defined in the specification, which possess both an ACAT inhibitory activity and an antioxidative activity. Those derivatives are useful in the prophylaxis and treatment of hypercholesterolemia and atherosclerosis.

Disclosed is a rhodanine derivative of formula (I). A rhodanine derivative of formula (I) ##STR1## wherein R.sup.1 is hdyrogen, C.sub.1 -C.sub.8 alkyl, carboxyl(C.sub.1 -C.sub.4)alkyl or (C.sub.1 -C.sub.4)alkoxycarbonyl(C.sub.1 -C.sub.4)alkyl;

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Saitama-ken, Japan

Nobuhiro Kinoshita