Taisho Pharmaceutical Co., Ltd.

Kirin Beer Kabushiki Kaisha

Nisshin Flour Milling Co., Ltd.

Microbial Chemistry Research Foundation

Kaken Chemical Co., Ltd.

Noboru Otake

Haruo Seto

Hiroyuki Kawai

Sadafumi Omura

Kazutoshi Mizoue

Michio Yamagishi

Taku Mizutani

Masanori Sugita

Atsuo Odagawa

Akira Kawashima

Tetsuo Sasaki

Hiroshi Hara

Shigeru Hiramoto

Yoichi Hayakawa

Teruyuki Sakai

Kozo Tanabe

Tomiko Kawasaki

Masaya Nakagawa

Masaru Kamishohara

Kuniaki Tatsuta

Noriyoshi Sueda

Shohachi Nakajima

Kiyoshi Tsuda

Yukio Miyazaki

Yohei Natori

Akira Shibata

Nobuyasu Komeshima

Haruyasu Kinashi

Kanji Imamura

Junichiro Mochizuki

Shigeyuki Mizobuchi

Disclosed is a novel spicamycin derivative represented by the formula (I) or a salt thereof: ##STR1## wherein R represents an alkenyl having a given number of carbon atoms, a haloalkyl having a given number of carbon atoms, CH.sub.3 (CH.sub.2).sub.n CH(OH)-- or CH.sub.3 (CH.sub.2).sub.n-1 CH(OH)--CH.sub.2 -- (wherein n denotes an integer of 9-13), an alkyl with a certain group and a given number of carbon atoms, ##STR2## (wherein a denotes 2, and b denotes an integer of 10-15), CH.sub.3 (CH.sub.2).sub.c SO.sub.2 O(CH.sub.2).sub.d --, ##STR3## (wherein c denotes an integer of 0-3 and d denotes an integer of 10-15), (CH.sub.3).sub.3 Si(CH.sub.2).sub.10 --,

Spicamycin derivatives and the use thereof

Spicamycin derivative represented by the formula (I) or a salt thereof: ##STR1## wherein R represents specific diverse substituents, for example, a linear alkadienyl having from 11 to 13 carbon atoms, and R.sub.1 and R.sub.2 respectively represent H or OH. Examples of specific compounds are 6-[4'-N-(N'-trans,trans 2,4-tridecadienoylglycyl)spicaminyl-amino]purine, and 6-[4'-N-(N'-trans,trans-2,4 dodecadienyoly glycyl) spicaminyl-amino]purine. Comopunds according to this invention are useful as a pharmaceutical for inhibition of a tumor, for example, human colon cancer.

Spicamycin derivatives and their use as anticancer agents

Disclosed is a novel anthracycline compound of the following formula (I): ##STR1## wherein R.sup.1 and R.sup.2 are each a hydroxyl group or a hydrogen atom and satisfy the condition that, when R.sup.2 is a hydroxyl group, R.sup.1 is a hydroxyl group or a hydrogen atom, whereas, when R.sup.2 is a hydrogen atom, R.sup.1 is a hydrogen atom, or an acid addition salt thereof. These compounds can be contained as active ingredients in antitumor agents, whereby good results are attainable.

Anthracycline compounds

Mycotrienin-related compounds called the T-23-X, -XI, -XII, -XIII and -XIV. These compounds are isolated and characterized by structural formula and other identifying data. They are useful in the treatment of tumors.

Mycotrienin-related compounds

An anthracycline compound, Arugomycin, having the physicochemical properties set forth below is produced by aerobically cultivating an Arugomycin-producing Streptomyces strain in a suitable culture medium, and recovering from the culture the anthracycline compound, Arugomycin.

Compound, arugomycin

Mycotrienin-related compounds called the T-23-VIII and T-23-IX substances. These substances are isolated and characterized by structural formula and other identifying data. These substances are useful in the treatment of tumors.

An antibiotic, Spicamycin, having the physicochemical properties set forth below is produced by aerobically cultivating a Spicamycin-producing Streptomyces strain in a suitable culture medium, and recovering from the culture the antibiotic, Spicamycin.

Antibiotic, Spicamycin

The disclosure describes a microbiological process for the preparation of mycotrien-related compounds. The compounds are isolated and characterized by structural formula and other identifying data. The compounds are useful in the treatment of tumors.

Ansatrienols

A novel compound of the formula ##STR1## and the salts thereof, derived from dianemycin, are useful as antiprotozoal and antibacterial agents.

Novel dianemycin derivative

The novel antibiotics represented by the formula ##STR1## wherein either (a) R.sup.1 is hydroxy and R.sup.2 is hydrogen, or (b) R.sup.1 is methoxy and R.sup.2 is hydroxy, and the salt thereof, are produced by the cultivation of the organism Streptomyces hygroscopicus TM-531 under aerobic conditions. They are separated from coproduced Antibiotic TM-531 as disclosed in U.S. Pat. No. 4,269,971 and from each other by chromatography on silica gel.

Antibiotics TM-531 B and TM-531 C

Antibiotic TM-531 having the formula: ##STR1## TM-531 is effective against gram-positive bacteria, plant pathogenic microorganisms and protozoa.

Antibiotic TM-531

Novel lonomycin derivatives, prepared by reacting lonomycin or its salt with an alkali or an alkali metal borohydride, show antibacterial, antiviral and antiprotozoal activity, and have decreased toxicity as compared with lonomycin.

Novel lonomycin derivatives

SY-1 substance has the following formula: ##STR1## The SY-1 substance and esters and salts thereof are antibiotics which have antibacterial, antifungal, antiviral and anticoccidial activity and also increase feed-utilization efficiency in ruminants.

Growing community of inventors

Yokohama, Japan

Noboru Otake