Shionogi Company Limited

Shionogi Seiyaku Kabushiki Kaisha

Hiroshi Itazaki

Yoshimi Kawamura

Koichi Matsumoto

Tadashi Yoshida

Toshiyuki Kato

Hitoshi Arita

Wataru Nagata

Tsutomu Aoki

Masuhisa Nakamura

Kunio Hayashi

Yukio Yonetani

Munenori Matsuura

Kenzo Koizumi

Kenji Sugita

Kyo Okada

The present invention relates to a novel aldose reductase inhibitor of the formula: ##STR1## wherein X is methylene or carbonyl;

Aldose reductase inhibitor obtained from Crucibulum sp. RF-3817

The present invention relates to a compound represented by the formula I: ##STR1## which was isolated from the culture of Streptomyces prunicolor PA-48153 and has biological activity such as immunosuppressive activity, antitumor activity and antifungal activity.

Immunosuppressive agent

The present invention relates to an aldose reductase inhibitor represented by the formula: ##STR1## wherein R.sub.1 is (CH.sub.2).sub.2 COOH and R.sub.2 is phenyl or p-hydroxyphenyl, or R.sub.1 and R.sub.2 are combined together to form a group of the formula: ##STR2## which was isolated from the fermentation products of Chaetomella circinoseta RF-3192.

Aldose reductase inhibitor

A compound of the formula (I): ##STR1## wherein R.sup.1, R.sup.2, and R.sup.3 are --COOR.sup.4, --COOR.sup.5, and --COOR.sup.6, respectively; R.sup.4, R.sup.5, and R.sup.6 each is hydrogen, lower alkyl, or alkali metal; W is hydroxyl; X, Y, and Z each is hydrogen or hydroxyl; a dotted line indicates the presence or absence of a single bond; or where W/R.sup.3, X/R.sup.1, and/or Z/R.sup.3 may be combined together, a lactone is formed, which compound is useful as a phospholipase A.sub.2 inhibitor. Process for the production of the compound (I) and a cell culture of a microorganism Circinotrichum falcatisporum RF-641 producing the same are also provided.

Phospholipase A.sub.2 inhibitor

A cyclic tetrapeptide having the formula (I): ##STR1## wherein n is 4 or 3 and a process for preparing the above cyclic tetrapeptide. The cyclic tetrapeptide of the present invention inhibits transformation of cells caused by oncogenes and possesses activities for recovering to a normal cell and for inhibiting proliferation of carcinoma cells. Therefore, the cyclic tetrapeptide of the present invention is useful for an active ingredient of an antitumor agent.

Cyclic tetrapeptide and process for preparing the same

Highly safe new diuretics, i.e., 1,4-benzodioxane and 1,4-benzodioxine derivatives having potent antihypertensive activity but no or little uricesuric activity, which can be administered to human orally, intravenously, or hypodermically at a respective daily dosage of 0.1-2 mg/kg, 0.005-0.1 mg/kg, or 0.02-0.4 mg/kg.

1,4-benzodioxine and 1,4-benzodioxine derivatives and production thereof

A novel process for producing o-hydroxybenzyl alcohols useful as raw materials or intermediates in chemical or pharmaceutical industries, which comprises reacting phenols or naphthols with aromatic boronic acids and aldehydes in the presence of organic carboxylic acids, followed by degradation of the cyclic ester intermediates.

Growing community of inventors

Takarazuka, Japan

Hiroshi Itazaki