Senju Pharmaceutical Co., Ltd.

Takahiro Sakaue

Kazumi Ogata

Shinji Ohmori

Kazuhiko Ito

Hidetoshi Nakao

Shinya Ogino

Masahito Iemura

Hideki Tsuruoka

Sachiko Matsuura

Rie Nagao

Yuuichi Isowaki

Noriko Saito

Yasuko Umegaki

Sachiko Inoue

Takahiro Ogawa

Masayuki Nakamura

Yutaka Inoue

Takaaki Deguchi

Shogo Sameshima

Yuichi Isowaki

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

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

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

This invention provides a therapeutic composition for pancreatitis 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. The pharmaceutical composition of this invention can be used with advantage in the prevention and treatment of pancreatitis.

Therapeutic composition for pancreatitis

This invention provides a novel steroid derivative having the structure of an ester between the carboxyl group of a quinolonecarboxylic acid and the alcoholic hydroxyl group in 21-position of asteroid compound, which has the following formula (I) (wherein R is a hydrogen atom, a methyl group or a hydroxyl group) or a pharmacologically acceptable salt thereof. ##STR1## The compound of this invention has high antibacterial activity and antiinflammatory activity.

Steroid derivatives

An antiinflammatory, antiallergic or hepatic disorders inhibitory agent containing a compound of the following formula or a pharmaceutically acceptable salt thereof as an active ingredient ##STR1## (wherein n represents 0 or 1; R.sub.1 means hydrogen or an alkyl group; R.sub.2 and R.sub.3 are the same or different and independently mean a hydroxyl group, a lower alkoxy group or an amino group or R.sub.2 and R.sub.3 together form an imino group; provided that R.sub.1 means an alkyl group where n=0 and R.sub.2 and R.sub.3 are the same or different and independently mean a hydroxyl group or a lower alkoxy group).

Glutathione derivatives

A hypotensive agent and antiglaucoma agent which comprise a compound represented by the following formula: ##STR1## (wherein R.sub.1 is hydrogen, or a lower alkyl or lower alkoxy group; R.sub.2 is an isopropylamino, tert-butylamino, 2-(2-methoxyphenyl)ethyl-1-amino, 4-(2-methoxyphenyl)!-1-piperazinyl or 4-piperonyl-1-piperazinyl group, provided however that in the case of R.sub.1 being hydrogen, R.sub.2 is neither isopropylamino nor tert-butylamino group) or its pharmacologically acceptable salt.

Growing community of inventors

Itami, Japan

Takahiro Sakaue