Eisai Company, Limited

Naoki Tokuhara

Mitsuo Nagai

Hiroyuki Yoshimura

Shigeki Hibi

Seiichi Kobayashi

Katsuya Tagami

Makoto Okita

Kouichi Kikuchi

Takayuki Hida

Shinya Abe

Seiko Higashi

Yasushi Okamoto

Takashi Sato

Naoki Kobayashi

Kenji Tai

Yumiko Nagasaka

Toshihiko Yamauchi

Akira Ishibashi

Heterocycle-containing carboxylic acid derivative and drug containing the same

Carboxylic acid derivatives having fused rings

Retinoic acid agonists as preventive and therapeutic agents for nephritis

Described is a heterocycle-containing carboxylic acid derivative represented by the following formula (I):

The present invention provides remedies for graft-versus-host disease (GVHD) and graft rejection reactions in organ transplantation which comprise retinoic acid receptor (RAR) agonists as an active ingredient. Main examples thereof include 9-(4-methoxy-2,3,6-trimethylphenyl)-7,8-dimethylnona-2,4,6,8-tetraen-1-oic acid, 4-&lsqb;(E)-2-(5,6,7,8-tetrahydro-5,5,8,8-tetramethylnaphthalen-2-yl)propenyl&rsqb;benzoic acid, 4-&lcub;2-&lsqb;5-(4,7-dimethylbenzofuran-2-yl)pyrroyl&rsqb;&rcub;benzoic acid, 4-&lcub;2-&lsqb;5-(5-chloro-7-ethylbenzofuran-2-yl)pyrrolyl&rsqb;&rcub;benzoic acid and 4-&lcub;2-&lsqb;5-(4,7-dimethylbenzothiophen-2-yl)pyrrolyl&rsqb;&rcub;benzoic acid.

Methods for preventing, inhibiting or treating graft rejection reactions in graft-versus-host disease (GVHD) and organ transplantation

Fused-ring carboxylic acid derivatives

The present invention provides a medicament exhibiting excellent retinoic acid receptor agonism. A Carboxylic acid derivative having a fused ring which is represented by the following formula or a pharmacologically acceptable salt thereof: ##STR1## {wherein the symbol ##STR2## represents a single bond or a double bond; X, Y, Z, P, Q, U, V and W are each a group represented by the formula: --O-- or --S--, or a group represented by the formula: ##STR3## [wherein R.sup.k (k: 1 to 8) is hydrogen, halogeno, optionally substituted lower alkyl or the like, with either of R.sup.7 and R.sup.8 being a group represented by the formula: ##STR4## (wherein A and B are each independently an optionally substituted aromatic hydrocarbon ring or an optionally substituted unsaturated heterocycle; and D is optionally protected carboxyl)]}.

Heterocycle-containing carboxylic acid derivative and drug containing

Growing community of inventors

Tsukuba, Japan

Naoki Tokuhara