Sanraku-ocean Co., Ltd.

Sanraku Incorporated

Panlabs, Inc.

Tomoyuki Ishikura

Takeo Yoshioka

Yasuo Fukagawa

Tomio Takeuchi

Hamao Umezawa

Akihiro Yoshimoto

Kageaki Kouno

Yasutaka Shimauchi

Rokuro Okamoto

Tsutomu Sawa

Kazuhiko Okamura

Yasushi Okumura

Joseph Lein

Toshikazu Oki

Yoshio Watanabe

Azuma Watanabe

Osamu Jodo

Yasue Matsuzawa

Noritaka Chida

Yasuo Fugakawa

Mitsuyasu Okabe

Katsuro Kubo

Kenichi Yamamoto

Norio Shibamoto

Yoshiaki Yagi

Michikatsu Sato

Shoji Hirata

Hiroyasu Tobe

Yukio Takatsuki

Yukio Tsuchiyama

Hiroshi Naganawa

Masao Yamamoto

Kuniaki Tatsuta

Hamao Umezawa, Deceased

Hiroshi Tanaka

Kohki Kiyoshima

Machiko Watanabe

Shizuka Fujii

Miharu Maeda

Kouki Fujii

Yasuyuki Kato

Kaoru Yamada

A compound represented by the formula ##STR1## wherein R.sub.1 represents a lower alkyl group or a lower haloalkyl group; R.sub.2 represents a lower alkyl group, a lower haloalkyl group, an aralkyl group, or a group of the formula --COOR.sub.4 or --SO.sub.2 R.sub.5 in which R.sub.4 represents an aralkyl group or a substituted or unsubstituted alkyl group and R.sub.5 represents an alkyl group or a substituted or unsubstituted aryl group; and R.sub.3 represents a hydrogen atom or a carboxyl protecting group which can be easily split off. This compound is useful in the production of a 6-(disubstituted amino)carbapenem-series antibiotic. The compounds of the formula ##STR2## wherein R.sub.1 and R.sub.2 are as defined above are important intermediates for the synthesis of the compounds of formula (I) and/or the aforesaid di-(substituted amino) carbapenem-series antibiotics.

6-(disubstituted amino)carbapenem compounds

Optically active azetidinones

Disclosed are anthracycline antibiotics of a formula (I): ##STR1## in which R.sup.1 and R.sup.2 are hydroxyl groups, R.sup.3 is ethyl group, R.sup.4 is methoxycarbonyl group and X represents daunosamine-rhodenose or daunosamine-deoxyfucose; or

Anthracycline antibiotics

New anthracycline antibiotics of a formula (I) are provided, which are usable as an anticancer agent ##STR1## (where R represents a hydrogen atom or a hydroxyl group). The antibiotics (I) can be produced by incubation of a dye-nonproductive or hardly dye-productive mutant strain which has an ability of converting .alpha.-citromycinone or .beta.-isorhodomycinone into the antibiotics (I), in the presence of .alpha.-citromycinone or .beta.-isorhodomycinone in a pertinent nutrient medium.

Anthracycline antibiotics DCP-1 and 2

Compounds represented by formula ##STR1## wherein Y.sup.1 and Y.sup.2 are identical or different, and respectively denote benzoylamino groups or phthalimide groups. This compound is useful for inhibition of dipeptidase.

Aminoethylcysteine derivatives

A compound represented by the formula ##STR1## wherein R.sub.1 represents a lower alkyl group or a lower haloalkyl group; R.sub.2 represents a lower alkyl group, a lower haloalkyl group, an aralkyl group, or a group of the formula --COOR.sub.4 or --SO.sub.2 R.sub.5 in which R.sub.4 represents an alkyl group or a substituted or unsubstituted aralkyl group and R.sub.5 represents an alkyl group or a substituted or unsubstituted aryl group; and R.sub.3 represents a hydrogen atom or a carboxyl protecting group which can be easily split off. This compound is useful in the production of a 6-(disubstituted amino)carbapenem-series antibiotic.

6-(disubstituted amino)carbapenam compounds

A cyclodextrin adsorbing material composed of a water-insoluble resin substrate to which a ligand having such a size as to be included by cyclodextrin is chemically bonded via a spacer radical; a method of separating and purifying cyclodextrin from an aqueous solution containing it, which comprises bringing said aqueous solution into contact with the above adsorbing material to adsorb cyclodextrin on the adsorbing material, and subjecting the adsorbing material to a desorption treatment to recover cyclodextrin; and a method of increasing the amount of cyclodextrin yielded, which comprises carrying out a cyclodextrin-forming reaction by an enzymatic method in the presence of the above adsorbent material.

Cyclodextrin adsorbing-material

An azetidinone derivative of the formula ##STR1## wherein R.sub.1 represents a formyl group, a carboxyl group, an acetyloxy group or a group of the formula ##STR2## in which R.sub.2 and R.sub.3 each represent a lower alkyl group or together represent a lower alkylene group, and Z represents a hydrogen atom or an amino-protecting group.

3-(CHFCH.sub.3)-azetidinone intermediates

Partially methylated cyclodextrins with enhanced solubility in water have an average degree of methylation of hydroxyl groups at different positions in all the glucose units involved of about 53-64% for the 2-position, about 38-51% for the 3-position and about 70-100% for the 6-position. The partially methylated cyclodextrins are prepared by reacting .beta.-cyclodextrin with more than about 30 equivalent proportions based on the .beta.-cyclodextrin of dimethyl sulfate and more than about 30 equivalent proportions of an alkali metal hydroxide, wherein the concentration of reactants is greater than 10% (wt/wt).

Partially methylated cyclodextrins and process for producing the same

The antibiotics designated obelmycins exhibit high proliferation inhibiting action against leukemia cells and are effective as anti-cancer agents.

Novel anthracycline antibiotics

Novel anthracycline antibiotics characteristic of Ring A of the anthracycline skeleton are produced by microorganisms belonging to the genus Streptomyces and are useful as anti-cancer agents. The antibiotics designated D-788-6 to -10 are shown by general formula: ##STR1## wherein Y represents a group shown by: ##STR2##

Novel tylosin derivatives are represented by formula: ##STR1## wherein R represents a hydrogen atom, an acetyl group or a propionyl group; X represents a group --CO-- or --SO.sub.2 --; Y represents a fluorine atom, an acetyl group, a methanesulfonyl group, a methylthio group, a benzoyl group or a methoxy group bound to the benzyl group at the 2-position or 4-position; and Z represents a hydrogen atom or a D-mycinose residue: ##STR2## The tylosin derivatives which are antibiotics of macrolide type provide improved antibacterial activity and improved ability of absorption and excretion in vivo.

Tylosin derivatives

This invention is to provide a new microbial process for producing daunomycin by a mutant strain belonging to the genus Streptomyces.

Process for producing daunomycin

A group of novel depsipeptide antibiotics, neoviridogriseins I, II and III are produced by fermentation of Streptomyces sp. P8648 (FERM-P 3562; ATCC 31289). The antibiotics are highly active against Gram-positive bacteria and mycoplasmas.

Antibiotics, neoviridogriseins, and their method of production

An aminocarboxylic acid derivative represented by the formula ##STR1## wherein R.sub.1 and R.sub.2, independently from each other, represent a hydrogen atom or an alkyl group which may have a substituent, and Y represents --NH-- or --S--, provided that when Y represents --NH--, at least one of R.sub.1 and R.sub.2 represents an alkyl group which may have a substituent. These compounds have excellent inhibitory activity on dipeptidase in animals, and are useful for administration in combination with carbapenem antibiotics.

Aminocarboxylic acid derivatives

Growing community of inventors

Chigasaki, Japan

Tomoyuki Ishikura