Kyowa Hakko Kogyo Co., Ltd.

Kyowa Hakko Kogyo Kabushiki Kaisha

Masayuki Teranishi

Kazuhiro Kubo

Katsuichi Shuto

Nobuhiro Nakamizo

Yutaka Kasuya

Hiroyuki Obase

Haruki Takai

Ikuo Matsukuma

Hiroshi Kase

Mitsuru Takahashi

Chikara Murakata

Akira Karasawa

Koji Yamada

Yasuo Fujimoto

Shunji Ichikawa

Shigeto Kitamura

Koji Suzuki

Keizo Tatsukawa

Hisayo Nomoto

Kenji Omori

Toru Doiuchi

Teruyuki Tsuruta

Masanobu Kawai

Shinsuke Koshimoto

Phosphorus-containing oligopeptide derivatives are prepared by synthetic methods. The compounds exhibit angiotensin converting enzyme-inhibiting action and are, therefore, useful as anti-hypertensive agents.

Phosphorus-containing peptide derivatives

A quinoline-N-oxide derivative represented by the formula: ##STR1## wherein X is hydroxy, lower alkoxy, lower alkylthio, unsubstituted or substituted aralkyloxy, or unsubstituted or substituted aralkylthio; Y is a hydrogen atom or halogen atom; R.sub.1 is alkylene or alkenylene having 3 to 15 carbon atom; Z is hydroxymethyl, lower alkoxymethyl, unsubstituted or substituted aryloxymethyl, tetrahydropyranyloxymethyl, tetrahydrofuranyloxymethyl, unsubstituted or substituted arylsulfonyloxymethyl, lower alkylthiomethyl, unsubstituted or substituted arylthiomethyl, lower alkylsulfinylmethyl, unsubstituted or substituted arylsulfinylmethyl, lower alkylsulfonylmethyl, unsubstituted or substituted arylsulfonylmethyl, aminomethyl, --CH.sub.2 NHR.sub.2 (wherein R.sub.2 is lower alkyl, unsubstituted or substituted aralkyl, or unsubstituted or substituted aryl), --CH.sub.2 NR.sub.3 R.sub.4 (wherein R.sub.3 and R.sub.4 are lower alkyl, unsubstituted or substituted aralkyl, or unsubstituted or substituted aryl), --CH.sub.2 N.sup.+ R.sub.5 R.sub.6 R.sub.7 (wherein R.sub.5, R.sub.6, and R.sub.7 are lower alkyl, unsubstituted or substituted aralkyl, or unsubstituted or substituted aryl, where the counterion is an anion of acid or a hydroxyl ion), --COR.sub.8 (wherein R.sub.8 is a hydrogen atom, lower alkyl or hydroxy), --CH(OR.sub.9).sub.2 (wherein R.sub.9 is lower alkyl), iminomethyl, hydroxyiminomethyl, or a halogen atom and its salts, can very strongly inhibit the lipoxygenase and considerably suppress production and release of its metabolites, and thus are useful as preventive and healing agents for the diseases caused by the lipoxygenase metabolites.

Quinoline-N-oxide derivative and pharmaceutical composition

Offered is an anticonvulsive composition which comprises an effective amount of a dihydrouracil derivative represented by the formula: ##STR1## [wherein one of A and B is ##STR2## (wherein Y.sub.1, Y.sub.2 and Y.sub.3 are hydrogen atoms, lower alkyl groups, halogen atoms, nitro groups, amino groups, carboxyl groups, lower alkoxycarbonyl groups or trifluoromethyl groups), a naphthyl group or a diphenylmethyl group, and the other is a hydrogen atom, a lower alkyl group, a lower alkenyl group, a cyclopentyl group, a cyclohexyl group or ##STR3## (wherein Z.sub.1, Z.sub.2 and Z.sub.3 are hydrogen atoms, lower alkyl groups, halogen atoms or trifluoromethyl groups), R.sub.1, R.sub.2 and R.sub.3 are hydrogen atoms or lower alkyl groups, and X is an oxygen atom or a sulfur atom] and at least one pharmaceutically acceptable carrier.

Treating convulsions with dihydrouracil derivatives

A new piperidine derivative represented by the formula: ##STR1## wherein X is oxygen, sulfur, carbonyl, hydroxymethylene or methylene; R.sub.1 is straight-chain alkylene having 1-4 carbon atoms with or without lower alkyl substituent(s); (A).sub.m and R.sub.2 are usually used substituents; and Y is a monovalent group or a divalent group and is one of the following three groups: ##STR2## wherein when p is 0, B is --N.dbd.N--, ##STR3## and when p is 1, B is ##STR4## wherein (R.sub.3).sub.n is a usually used substituent, has hypotensive activity.

Hypotensive piperidine derivatives

New piperidine derivatives which have a useful pharmacological activity such as hypotensive activity are prepared.

Piperidine derivatives

A new piperidine derivative represented by the formula: ##STR1## wherein X is oxygen, sulfur, carbonyl, hydroxymethylene or methylene; R is straight-chain alkylene having 1-4 carbon atoms with or without lower alkyl substituent(s); m and n are 0 or 1, and are different from each other (i.e., both m and n are not 0 or 1); and (D).sub.m', R.sup.1 and (R.sup.2)n' are usually used as substituents, has a hypotensive activity.

Piperidine derivatives and pharmaceutical compositions containing same

Novel compounds are disclosed which are useful as agents capable, when applied to citrus tree, of modifying the metabolism and organic acid content of the citrus fruit.

Agents for and method of modifying citrus fruit

This invention relates to certain derivatives of phenylalanine having interesting pharmaceutical properties, in particular, a lipid-lowering activity.

Phenylalanine derivatives

Amino acid-urethane copolymers improved in elongation, tensile strength and flexing endurance are prepared by polymerizing a prepolymer having terminal isocyanate groups, obtained by reacting a polyether polyol having hydroxyl groups substantially at the terminals thereof with an organic polyisocyanate in a ratio in equivalent of the organic polyisocyanate to the polyether polyol of 1.6 to 2.5, either with an amino acid-N-carboxylic acid anhydride or with a polyamino acid polymer obtained by polymerizing an amino acid-N-carboxylic acid anhydride.

Growing community of inventors

Machida, Japan

Masayuki Teranishi