Kyowa Hakko Kogyo Co., Ltd.

Koji Suzuki

Akira Karasawa

Haruki Takai

Ichiro Miki

Hiroyuki Ishida

Hiroshi Kase

Akio Ishii

Katsushige Gomi

Etsuo Ohshima

Katsuichi Shuto

Shigeto Kitamura

Hitoshi Arai

Joji Nakamura

Toshiaki Kumazawa

Masayuki Teranishi

Satoshi Nakanishi

Daisuke Machii

Shiro Shirakura

Kimihisa Ueno

Soichiro Sato

Nobuo Kosaka

Seiji Aratake

Tsuyoshi Yamagata

Kaoru Atsuki

Koji Yanagawa

Tsutomu Matsumura

Motoki Miyama

Hiroshi Ishida

Shigeru Aono

Kenji Omori

Masako Uchii

Katsuya Kobayashi

Makoto Yoshida

Ari Kawabe

Takashi Sato

Shinya Fujii

Miho Iwase

Tomomi Sugiyama

Hisakatsu Seo

Takashi Seishi

Yosuke Yamaura

Obase Hiroyuki

Kubo Shizuoka

[wherein m and n may be the same or different and each represents an integer of 1 to 3 wherein m+n is 4 or less; Rrepresents &#x2014;NRR(wherein Rand Rmay be the same or different and each represents a hydrogen atom, substituted or unsubstituted lower alkyl, substituted or unsubstituted aralkyl or the like); Rrepresents the above Formula (II), Formula (IV) or the like; A represents a single bond, &#x2014;C(&#x2550;O)&#x2014;, &#x2014;SO&#x2014;, &#x2014;OC(&#x2550;O)&#x2014; or the like; and Rrepresents substituted or unsubstituted lower alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aralkyl or the like] Bicyclic pyrimidine derivatives represented by the above Formula (I), or quaternary ammonium salts thereof, or pharmaceutically acceptable salts thereof, or the like, are provided. These have anti-inflammatory activities or modulation activities on the functions of TARC and/or MDC and are useful for treating and/or preventing a disease which is related to T cells, such as an allergic disease, an autoimmune disease or transplant rejection.

Bicyclic pyrimidine derivatives

The present invention provides tricyclic compounds which are useful for the treatment of pollakiuria and urinary incontinence and which are represented by general formula (I):

Tricyclic compounds

The present invention relates to indole derivatives represented by formula (I): ##STR1## wherein R.sup.1 and R.sup.2 independently represent hydrogen, lower alkyl, hydroxy, lower alkoxy, halogen, --O--(CH.sub.2).sub.n --OR.sup.5, or ##STR2## R.sup.3 represents hydrogen, lower alkyl, or ##STR3## R.sup.4 represents hydroxy, lower alkoxy, substituted or unsubstituted aryloxy, or --NR.sup.10 R.sup.11, and X represents CO or SO.sub.2, with the proviso that when R.sup.3 is hydrogen or lower alkyl, and X is CO, R.sup.4 is --NR.sup.10 R.sup.11, or pharmaceutically acceptable salts thereof.

Indole derivatives

A pyridine derivative represented by formula (I): ##STR1## wherein the symbols are as defined in the specification, which exhibits selective, potential, and long-lasting inhibitory activity on biosynthesis of thromboxane A.sub.2 and is useful in the treatment and prevention of a broad range of diseases.

Pyridine 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

Growing community of inventors

Mishima, Japan

Koji Suzuki