Shionogi Company Limited

Shionogi Seiyaku Kabushiki Kaisha

Yoshimi Kawamura

Koichi Matsumoto

Tadashi Yoshida

Eiji Kondo

Hiroshi Itazaki

Naoki Tsuji

Toshiyuki Kamigauchi

Shigeru Matsutani

Kentaro Tanaka

Kouichi Matsumoto

Jun'ichi Shoji

Hitoshi Arita

Susumu Kamata

Bunji Kageyama

Shigeo Yagi

Takao Konishi

Toshiyuki Kato

Ryuji Sakazaki

Tamio Fujiwara

Yoshiyuki Hayashi

Teruo Hattori

Shinzo Matsuura

Kenzo Koizumi

Junichi Shoji

Hiroyoshi Tani

Mikao Mayama

Kenji Sugita

Isao Horibe

Masaaki Kobayashi

Yukio Miyake

Keizo Inoue

Mitsuo Ebata

Novel antibiotic stalobacins H-1 and I-1 having physico-chemical properties as shown in Table 4 are provided, which are excellent antibiotics showing marked effects on Gram-positive bacteria.

Antibiotic stalobacins

Sequiterpene derivatives having antiviral activity

Novel antibiotic stalobacins A to I having physico-chemical properties as shown in Tables 1 to 4 are provided, which are excellent antibiotics showing marked effects on Gram-positive bacteria.

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

Glycopeptide antibiotics PA-45052 which are produced by Nocardia orientalis PA-45052, show potent activity against gram-positive bacteria, especially against methicillin-resistant bacteria, and stimulate growth of animals.

Glycopetide antibiotic PA-45052-B

A compound of the formula: ##STR1## wherein the wave line means .alpha.-bond or .beta.-bond, which compound is useful as a phospholipase A.sub.2 inhibitor. Process for the production of the compound, pharmaceutical composition containing the compound, and a cell culture of a microorganism Thielavia terricola RF-143 producing the compound are also provided.

Phospholipase A2 inhibitor

The compounds of the formula: ##STR1## wherein R is ##STR2## or H, wherein X is NH.sub.2 and Y is CH.sub.3 ; or X is OH and Y is H, and their pharmaceutically acceptable salts. The compounds have a potent activity against gram-positive bacteria, especially, methicillin-resistant bacteria.

Novel glycopeptide antibiotics

Antibiotics DO-248-A and DO-248-B of the following Formula I: ##STR1## wherein R is ethyl or isopropyl, have antibacterial activity against acid-fast bacteria. DO-248-A, DO-248-B, or their pharmaceutically acceptable salts are, as an active ingredient of anti-fast-acid drugs, orally or parenterally administered to human beings or animal. DO-248-A and DO-248-B are prepared by incubating an antibiotic DO-248-A- and/or DO-248-B-producing microorganism belonging to genus Streptoverticillium in a medium and recovering antibiotic DO-248-A and/or DO-248-B from the culture broth.

Antibiotics DO-248-A and B and process for preparing the same

.beta.-Galactosidase inhibitors GT-2558, GT-2558-A, and GT-2558-B produced by a strain Streptomyces lydicus PA-5726, and their derivatives, acetyl-GT-2558-A and acetyl-GT-2558-B, useful as diagnostatic aid in .beta.-galactosidase deficiency, used in purification of enzymes, in research of new .beta.-galactosidase, in controlling sweetness of lactose-containing foods and in fermentation industry.

.beta.-Galactosidase inhibitor GT-2558 and its derivatives

New antibiotics having .beta.-lactamase inhibitory activity, PA-41746-B and C of the formula ##STR1## wherein R is carboxymethylsulfinyl (PA-41746-B) or formylsulfinyl (PA-41746-C) and the pharmaceutically acceptable salts being useful as a medicament, a veterinary drug and a disinfectant for inhibiting the growth of gram-positive and gram-negative pathogenic microorganisms and a process for preparing the same, being characterized by cultivating Streptomyces pluracidomyceticus in a suitable medium and isolating PA-41746-B and/or PA-41746-C from the culture broth.

Growing community of inventors

Minoo, Japan

Yoshimi Kawamura