Senju Pharmaceutical Co., Ltd.

Shiseido Company, Limited

Takeda Chemical Industries, Inc.

Yoshitomi Pharmaceutical Industries, Ltd.

Oga Research, Inc.

Kazumi Ogata

Takahiro Sakaue

Shinji Ohmori

Kazuhiko Ito

Hidetoshi Nakao

Masahito Iemura

Hideki Tsuruoka

Shinya Ogino

Yuuichi Isowaki

Sachiko Matsuura

Rie Nagao

Noriko Saito

Kenichi Yoshida

Yasuko Umegaki

Osamu Kawahira

Sachiko Inoue

Takahiro Ogawa

Kenichi Tomita

Keiichi Uehara

Itaru Yamamoto

Masayuki Nakamura

Yujiro Yamamoto

Yutaka Inoue

Takaaki Deguchi

Norio Shimamoto

Yoshihisa Sato

Shogo Sameshima

Yoshie Ozaki

Takahiro Matsumoto

Shuuichi Nishihata

Reiko Matsuda

Eri Inoue

Shoji Yoshida

Kyozo Yamamoto

Shuzo Iwata

Kyouzo Yamamoto

Yuichi Isowaki

Yoshimasa Abe

Kazuhiko Yamada

Keiko Suetsugu

Emiko Takasu

Genta Maruyama

Shunji Sogo

A melanin eliminator preparation comprising a metal chelate compound represented by the following formula (I), wherein M denotes a metal, and R denotes hydroxyl, O-lower alkyl, an amine bonded at N, an amino acid bonded at N, or a peptide bonded at N, or a pharmacologically acceptable salt thereof.

Melanin eliminator preparation

A novel &#x3b1;-lipoic acid derivative represented by the following formula (I). It has a tyrosinase inhibiting activity, melanin production inhibitory activity, and elastase inhibiting activity. (I) (In the formula, M represents a metal and A denotes an amino acid residue bonded through the nitrogen atom.). 

Method of suppressing melanin production by metal chelates of lipoyl amino acid derivatives

L-Ascorbic acid-2-O-maleic acid-&agr;-tocopherol diester.1-propanol adduct or its pharmacologically acceptable salt; cosmetic components, antioxidants, radical scavengers, anti-inflammatory agents and elastase inhibitors containing the same as the active ingredient; and a process for producing the above-described adduct characterized by comprising extracting a solution containing L-ascorbic acid-2-O-maleic acid-&agr;-tocopherol diester with a solvent, distilling off the solvent, and adding to the residue 1-propanol mixed with an organic solvent followed by crystallization.

L-ascorbic acid-2-o-maleic acid-a-tocopherol diester 1-propanol adduct and process for producing the same

The present invention provides novel vitamin E derivatives represented by the following formula (I) wherein: R and R are the same or different and each denotes hydrogen or methyl, R denotes an S-linked SH compound (glutathione, &ggr;-glutamylcysteine, cysteine, penicillamine, an ester thereof or cysteamine), and R denotes hydroxyl, a N-substituted amino acid (glycine, &bgr;-alanine, &ggr;-aminobutyric acid, 5-aminovaleric acid, &egr;-aminocaproic acid, anthranilic acid, tranexamic acid, proline, an ester thereof, aminoethylsulfonic acid , aminoethylsulfinic acid) or serotonin, or a pharmacologically acceptable salt thereof, which are useful as hepatopathy suppressing agents, anticataract agents, cerebral metabolism improving agents, antioxidants and cosmetic components.

Vitamin E derivatives

Hydroquinone derivatives

Urocanic acid derivatives useful as antiallergic agents represented by the following formula (I) or a pharmacologically acceptable salt thereof:

Urocanic acid derivatives

A medicament for reducing side effects of adrenocortical hormones comprising a phosphodiester compound of the following formula or a pharmacologically acceptable salt thereof

Agents for relieving side effects of adrenal cortex hormone

The present invention provides a piperazine derivative of the following formula or a pharmacologically acceptable salt thereof ##STR1## wherein R.sub.1 represents a benzene ring, naphthalene ring, quinoline ring, indole ring or chroman ring that may be substituted by lower alkyl, lower alkoxy and/or hydroxy; R.sub.2 and R.sub.3 independently represent hydrogen or lower alkyl. The compound of the present invention has potent antiallergic activity and can therefore be used with advantage in the treatment of various allergic diseases.

Piperazine derivative

The present invention provides a pharmaceutical composition for the therapy of acne vulgaris which comprises a phosphoric diester compound of the following formula or a pharmacologically acceptable salt thereof ##STR1## wherein R.sub.1 and R.sub.2 may be the same or different and each represents hydrogen or methyl.

Therapeutic drug for acne vulgaris

This invention provides a benzylpiperazine derivative of formula (I) and a pharmacologically acceptable salt thereof ##STR1## wherein R.sub.1 represents a pyridine ring or a group of either formula (IV) or formula (V); R.sub.2 represents hydrogen or lower alkyl ##STR2## wherein R.sub.3 represents hydrogen, lower alkyl, a pyridine ring or a benzene ring which may be substituted by halogen; X represents halogen ##STR3## wherein R.sub.4 and R.sub.5 may be the same or different and each represents hydrogen, lower alkyl, lower alkoxy, halogen or carboxy.

Benzylpiperazine derivative

1. A corticoid derivative of the general formula ##STR1## wherein R represents hydrogen, hydroxy, methyl or methylene; inclusive of the acylation product thereof where the 17-position of the steroid skeleton is hydroxy and the ketone form thereof where R is hydroxy, or a physiologically acceptable salt thereof. Since the corticosteroid derivative of this invention is readily soluble in water and has antiallergic, antiinflammatory and antioxidant activities, it can be used with advantage in the prevention and therapy of various allergic diseases, inflammatory diseases, cataract and various ischemic organ diseases.

Corticoid derivatives and pharmaceutical and cosmetic compositions

An improved method for isolating and purifying a glutathione derivative is disclosed. More particularly, the invention provides a method for isolating and purifying S-(1, 2-dicarboxyethyl)glutathione or its pharmacologically acceptable salt from a reaction mixture available upon reacting glutathione or its salt with either fumaric acid or its salt or maleic acid or its salt, which comprises a first step of converting the S-(1, 2-dicarboxyethyl)glutathione or salt thereof in the reaction mixture to the corresponding copper salt, dissolving the copper salt in an aqueous solution of acetic acid, formic acid or propionic acid, and removing the contaminant glutathione, oxidized glutathione and fumaric acid copper salts with the aid of activated carbon and a second step of dissolving or suspending the isolated S-(1,2-dicarboxyethyl)glutathione copper salt in water and blowing hydrogen sulfide gas through the resulting aqueous solution or suspension to remove copper.

Method for isolation and purification of S-(1,2-dicarboxyethyl)

Presented is a novel quinolonecarboxylic acid derivative of the formula I and its pharmaceutically acceptable salt: ##STR1## wherein R.sub.1 is hydrogen, halogen or lower alkoxy, R.sub.2 is hydrogen, lower alkyl, lower alkoxy, --NH.sub.2, --NHCOCH.sub.3 or halogen,

Quinolonecarboxylic acid derivatives

This invention provides a phosphoric diester of formula (I) which is available on di-esterification of phosphoric acid with L-ascorbic acid involving its 5-hydroxyl group and tocopherol involving its hydroxyl group or a pharmacologically acceptable salt thereof. ##STR1## The compound of the invention can be used with advantage as an antioxidant (radical-scavenging) agent and a prophylactic and therapeutic agent for ischemic organ disorders (e.g. myocardial infarction, heart failure, arrhythmia, cerebral infarction, stroke (cerebral apoplexy), renal failure, etc.).

Phosphoric diester

This invention provides an antiallergic composition which comprises a phosphoric diester compound of the following formula or a pharmacologically acceptable salt thereof ##STR1## wherein R.sub.1 and R.sub.2 are the same or different and each represents hydrogen or methyl.

Antiallergic composition comprising a phosphoric diester compound

Growing community of inventors

Toyonaka, Japan

Kazumi Ogata