Nisshin Flour Milling Co., Ltd.

Nisshin Seifun Group Inc.

Nisshin Pharma Inc.

Kyorin Pharmaceutical Co., Ltd.

Makoto Yanai

Masashi Suzuki

Norio Oshida

Koji Kawamura

Shigeru Hiramoto

Nobuhiro Kinoshita

Akiko Shingai

Orie Yasuda

Masako Takasu

Toshihiro Takahashi

Masahiro Ueno

Hiroaki Satoh

Haruhiko Kikuchi

Noriyoshi Sueda

Koichi Itoh

Koichiro Hagihara

Setsuko Mino

Hitoshi Inoue

Kohei Inomata

Masato Horigome

Hiroyuki Yamazaki

Koichi Katsuyama

Katsutoshi Miura

Kazuhiko Yamada

Takao Kishiye

Toru Hayakawa

Yoko Tsukada

Fumihisa Nakata

Tsutomu Takasawa

Kouji Kawamura

Hiroyuki Ikemoto

Nobuhiro Yahata

Yoshikuni Suzuki

Hiroaki Yamada

Toshiji Sugai

Toshio Suguro

Kiochiro Hagihara

Koichi Katasuyama

Satoko Fuchizawa

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

Optically active 1,4-benzodioxin-2-carboxylic acid derivatives and process for producing the same

Disclosed are optically active alcohols having formula (1) and (2)

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

Optically active 1,4-benzodioxine-2-carboxylic acid derivatives and process for producing the same

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

Bicyclic depsipeptides

There is disclosed a multidrug resistance inhibitor for overcoming a multidrug resistance of cancer, or an agent for enhancing the activity of anti-cancer agents, which comprises as an active ingredient a compound of formula (I) or a pharmaceutically acceptable salt thereof: ##STR1## wherein n is an integer of 5 to 12,

Multidrug resistance inhibitors

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.

Isoprene derivatives of formula (I) ##STR1## wherein m is an integer of 0 to 3,

Isoprene derivatives

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.

Growing community of inventors

Saitama-ken, Japan

Makoto Yanai