Eisai Company, Limited

Takashi Yamanaka

Shigeki Hibi

Kazuo Hirota

Ieharu Hishinuma

Junichi Nagakawa

Shinya Abe

Shuhei Miyazawa

Isao Yamatsu

Katsuya Tagami

Hiroyuki Yoshimura

Mitsuo Nagai

Hisashi Shibata

Kouichi Kikuchi

Yorihisa Hoshino

Kaname Miyamoto

Naoyuki Shimomura

Tsuneo Wakabayashi

Yasushi Okamoto

Takayuki Hida

Makoto Asada

Norimasa Miyamoto

Seiko Higashi

Kenji Tai

Aichi Ogasawara

Takaaki Kameyama

Masanori Mizuno

Takashi Mori

Toshihiko Kaneko

Shigeru Souda

Seiichiro Nomoto

Norihiro Ueda

Tetsuya Kawahara

Makoto Okita

Manabu Murakami

Tsutomu Kawata

Masanobu Shinoda

Takashi Inoue

Kiyoshi Oketani

Junsaku Nagaoka

Naoki Kobayashi

Hidetoshi Kawashima

Toru Horie

Naoko Nagaoka

Hirotoshi Numata

Makoto Ikeda

Yoshitake Ogata

Hiromitsu Yokohama

Tsutomu Yoshimura

Koichi Katayama

Yasunori Akita

Tohru Horie

Kenzo Muramoto

Koukichi Harada

Kenichi Chiba

Toshihiko Yamauchi

Yorohisa Hoshino

Akiko Nakahama

Akiyoshi Uchiyama

Mono- or polyenic carboxylic acid derivatives

To provide novel compounds relating to retinoid which can substitute for retinoic acid used for preventing and treating several diseases and having antagonism against retinoid. Heterocyclic compounds represented by the general formula (1-I) or physiologically acceptable salts thereof:

Compounds of the formula and compounds of the formula ##STR1## or their salts have the potent ability to bind to retinoic acid receptors thus useful in treating psoriasis and rheumatoid arthritis.

Mono-or polyenic carboxylic acid derivatives

To provide a compound which exhibits a serotonin antagonism and an acetylcholine release accelerating activity at a well-balanced activity ratio. An aminobenzoic acid derivative represented by the general formula (I) or (II) or a pharmacologically acceptable salt thereof: ##STR1## �wherein R.sup.1 represents a group represented by the formula: ##STR2## {wherein A represents a group represented by formula --CH.sub.2 --X--CH.sub.2 -- (wherein X represents O, &gt;N--R.sup.6 or&gt;CHR.sup.7 (wherein R.sup.6 represents lower alkyl and R.sup.7 represents hydrogen or lower alkoxy)), etc.; D and E each represents a group represented by formula --(CH.sub.2).sub.3 --, etc., and R.sup.2 represents lower alkyl, etc.}; R.sup.9 represents alkynyl; R.sup.10 represents amino, etc-; R.sup.11 represents halogen; R.sup.12 and R.sup.13 each represent lower alkyl; a is an integer of 1 to 5; and b is an integer of 0 to 5!.

Aminobenzoic acid derivatives

The present invention provides a therapeutic agent for fundamentally preventing, treating or ameliorating dermatosis, such as, non-infectious dermatosis, which include psoriasis and atopic dermatitis. The therapeutic agent comprises a glycerol derivative represented by the formula (I): ##STR1## wherein A is a group represented by the formula: ##STR2## or single bond; R.sup.1 is a group represented by the formula: ##STR3## wherein R.sup.2 is a methoxyphenyl group or methyl group, X is an atom or atomic group which may become an anion or a group represented by the formula: ##STR4## or a pharmacologically acceptable salt thereof as an active ingredient.

Therapeutic agent for dermatosis

To provide a treating or ameliorating agent for joint diseases accompanied with arthritis, preferably, a rheumatoid arthritis or ameliorating agent, which exerts excellent pharmaceutical effects. The active ingredient is a quinone derivative represented by the following general formula (I) or pharmacologically acceptable salts thereof: ##STR1## wherein n is 0 or an integer of 1 to 12 and R is a methyl or methoxy group.

Therapeutic agent for treating joint diseases associated with arthritis

To provide a compound which exhibits a serotonin antagonism and an acetylcholine release accelerating activity at a well-balanced activity ratio. An aminobenzoic acid derivative represented by the general formula (I) or (II) or a pharmacologically acceptable salt thereof: ##STR1## �wherein R.sup.1 represents a group represented by the formula: ##STR2## {wherein A represents a group represented by formula --CH.sub.2 --X--CH.sub.2 -- (wherein X represents O, &gt;N--R.sup.6 or &gt;CHR.sup.7 (wherein R.sup.6 represents lower alkyl and R.sup.7 represents hydrogen or lower alkoxy)), etc.; D and E each represents a group represented by formula --(CH.sub.2).sub.3 --, etc., and R.sup.2 represents lower alkyl, etc.}; R.sup.9 represents alkynyl; R.sup.10 represents amino, etc.; R.sup.11 represents halogen; R.sup.12 and R.sup.13 each represent lower alkyl; a is an integer of 1 to 5; and b is an integer of 0 to 5!.

To provide a compound which exhibits a serotonin antagonism and an acetylcholine release accelerating activity at a well-balanced activity ratio. An aminobenzoic acid derivative represented by the general formula (I) or (II) or a pharmacologically acceptable salt thereof: ##STR1## [wherein R.sup.1 represents a group represented by the formula ##STR2## etc., {wherein A represents a group represented by formula --CH.sub.2 --X--CH.sub.2 -- (wherein X represents O, &gt;N--R.sup.6 or &gt;CHR.sup.7 (wherein R.sup.6 represents lower alkyl and R.sup.7 represents hydrogen or lower alkoxy)), etc.; D and E each represents a group represented by formula --(CH.sub.2).sub.3 --, etc., and R.sup.2 represents lower alkyl, etc.}; R.sup.9 represents alkynyl; R.sup.10 represents amino, etc.; R.sup.11 represents halogen; R.sup.12 and R.sup.13 each represent lower alkyl; a is an integer of 1 to 5; and b is an integer of 0 to 5].

A benzothiazole derivative or a pharmacologically acceptable salt thereof of the following formula, as defined in the claims, which is useful as a preventive or therapeutic agent for diseases on which functions of suppressing leukotrienes and thromboxanes production are effective: ##STR1##

Benzothiazole compounds which are substituted by pyridymethyl

An aminobenzoic acid derivative represented by the following general formulas (I), (I-2) or (I-3), or a pharmacologically acceptable salt thereof, which exhibits a serotonin antagonism and an acetylcholine release accelerating activity at a well-balanced activity ratio and which is efficacious as a drug for patients with gastrointestinal unindentified complaints: ##STR1## wherein R.sup.1 represents a group such as an alkynyl or cyanoalkyl group; R.sup.2 represents a group such as an amino or acylamino group; R.sup.3 represents a halogen atom; X represents --O-- or --NH--; and A represents an oxygen or sulfur atom.

Process for preparing aminobenzoic acid derivatives

An aminobenzoic acid derivative represented by the following formulas (I-2) or (I-3), or a pharmacologically acceptable salt thereof, which exhibits a serotonin antagonism and an acetylcholine release accelerating activity at a well-balanced activity ratio and which is efficacious as a drug for patients with gastrointestinal unindentified complaints: ##STR1## wherein R.sup.1 represents a group such as an alkynyl or cyanoalkyl group; R.sup.2 represents a group such as an amino or acylamino group; R.sup.3 represents a halogen atom; X represents --O-- or --N--; and A represents an oxygen or sulfur atom.

Growing community of inventors

Ibaraki, Japan

Takashi Yamanaka