Sanraku Incorporated

Mercian Corporation

Sanraku-Ocean Co., Ltd.

Rokuro Okamoto

Takeo Yoshioka

Hiroshi Tone

Tomio Takeuchi

Tomoyuki Ishikura

Yoshio Watanabe

Kazuhiko Okamura

Yasuo Fukagawa

Tsutomu Sawa

Naoto Kawamura

Kaichiro Kominato

Hamao Umezawa

Masataka Shirai

Toshio Tsuchida

Akihiro Yoshimoto

Akira Takamatsu

Kageaki Kouno

Norio Shibamoto

Azuma Watanabe

Akira Arisawa

Shin-ichi Hirano

Osamu Jodo

Mitsuyasu Okabe

Hiroshi Iguchi

Ryoichi Miyata

Ikuo Kojima

Kohki Kiyoshima

Hiroshi Nishida

Hiroyuki Chiba

Tsumoru Fukumoto

Takashi Adachi

Hiroshi Naganawa

Masao Yamamoto

Taiji Inui

Sadafumi Omura

Kuniaki Tatsuta

Hiroshi Tanaka

Yasutaka Shimauchi

Joji Sasaki

Naoki Agata

Hitosi Agematu

Koji Takeda

Yutaka Hara

Miharu Maeda

Shunro Mori

Kiyoshi Kimura

Yasuo Okajima

Reijko Yamamoto

Tomoyuki Kioka

Rei Kaneto

Toshihiko Kumamoto

Yasushi Okumura

Koichiro Kominato

Tsutomu Inoue

A method for introducing hydroxyl groups into vitamin D compound at the 1.alpha.- and/or 25-positions in the presence of a cyclodextrin compound by the use of a reaction mixture containing a microorganism being capable of hydroxylating vitamin D compound or a enzyme produced from the microorganism, is disclosed.

Method for the biological preparation of hydroxyvitamin D compounds

A DNA fragment or a restriction enzyme-digested DNA fragment, the DNA fragment containing a gene, acyA, encoding a 3-acylation enzyme for macrolide antibiotics, characterized by being derived from a strain belonging to the genus Streptomyces, having a size of about 1.8 kb or about 3.2 kb, and having a DNA base sequence shown in a restriction enzyme map shown in FIG. 1(A) or FIG. 1(B), respectively, in the attached drawing. 3-Acylated macrolide antibiotics can be produced advantageously using macrolide antibiotics-producing bacteria transformed with vector plasmids having inserted therein the DNA fragment.

Genes encoding a 3-acylation enzyme for macrolide antibiotics

A DNA fragment containing acyB gene coding for an enzyme capable of acylating the 4'-position of a macrolide antibiotic, said DNA fragment being derived from a microorganism of the genus Streptomyces, having a size of about 3.1 kb and being characterized by the restriction endonuclease map shown in FIG. 1 , and a DNA restriction fragment resulting from digestion with a restriction endonuclease; a recombinant DNA plasmid containing this DNA fragment; a microorganism transformed with this recombinant plasmid; and a process for producing a 4'-acylated macrolide antibiotic by using the transformant.

DNA coding for enzyme capable of acylating the 4'-position of macrolide

Antibiotic Mer-AF1032A represented by the following formula (I) and its isomer antibiotic Mer-AF1032B are disclosed. Also disclosed are a method for preparing the antibiotics comprising the cultivation of a strain belonging to genus Penicillium and a pharmaceutical composition comprising one of these antibiotics and useful as an antifungal agent. ##STR1##

Antibiotics Mer-AF1032A and Mer-AF1032B

4-Hydroxypyridine derivative represented by the following formula ##STR1## wherein R represents a methyl group or an isopropyl group, and the method for preparing the derivative comprising the step of cultivating a strain belonging to Streptomyces karnatakensis are disclosed. Also disclosed are the pharmaceutical composition comprising the same and a method for treating circulatory diseases comprising the step of administering said compound to a patient.

4-hydroxypyridine derivatives, useful for treating circulatory diseases

Adriamycin derivatives represented by formula (I) ##STR1## wherein R denotes a divalent hydrocarbon group,

Conjugate of adriamycin and cyclodextrin

A process for producing 2-azetidinone derivatives represented by formula ##STR1## wherein R.sup.1 denotes a protecting group of a hydroxyl group,

Process for producing azetidinone derivatives

An angolamycin derivative represented by the following formula ##STR1## wherein X represents an acetyl, methanesulfonyl, methylthio, benzoyl or methoxy group. This compound is useful as a medicament such as antibacterial agent and an animal feed additive.

Angolamycin derivatives

This invention provides a blood typing training kit comprising a red blood cell model and an antiserum model with no use of human blood in experiments for blood agglutination and in learning of blood typing, the red blood cell model being an easily available granule which can be suspended in water such as agarose bead, Sepharose, cellulose, Sephadex, cellulofine, alginate, tamarind polysaccharide, gelatin, xanthan gum, etc. or the saccharide- or protein-bound form thereof and the antiserum model being lectin, boric acid-containing liquid or immunoglobulin G.

Bloodless blood typing training kit

14-Trifluoromethanesulfonyloxydaunomycin represented by the following formula ##STR1## and its salt. This compound is useful as an intermediate for production of adriamycin.

Anthracycline derivatives

This invention relates to a process for preparing an antibiotic D788-7 wherein, after culturing carborubicin-producing bacteria, the obtained culture liquid is extracted in acidic conditions while stirring to be absorbed to synthetic resin, followed by desorption from the resin and elution with acetone and the resulting acetone solution containing carborubicin is converted into an antibiotic D788-7 by photo radiation, for obtaining D788-7 in the purified form from the reaction solution. The production yield for D788-7 is extremely high and its use as an antitumor agent can be made possible.

Process for preparing antibiotics D788-7

Tylosin derivatives represented by the following general formula (I): ##STR1## [wherein R denotes a hydrogen atom, acetyl, propionyl or a radical of Si(R.sup.2).sub.3 (in which R.sup.2 is a lower alkyl group), and R.sup.1 stands for a hydrogen atom or a radical of Si(R.sup.2 .sub.3 ] are useful as intermediates for the synthesis of 4'-acyl derivatives of tylosin because, after introduction of any desired acyl group at the 4'-hydroxyl group, the silyl protective group can be readily removed without liberation of the acyl group. This invention also provides processes for producing the tylosin derivatives. More specifically, it provides a melthod of selectively protecting 2'- and 4''-hydroxyl groups of tylosin (those of higher reactivity among the hydroxyl groups involved); a method of selectively protecting only the 4''-hydroxyl group of tylosin; a method of selectively protecting the 3- and 4''-hydroxyl groups of 2'-O-acyltylosin; and a method of protecting 3-, 2'- and 4''-hydroxyl groups of tylosin.

Tylosin derivatives and processes for producing the same

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

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

Compounds of the following general formula ##STR1## wherein R.sup.1 and R.sup.2 represent a hydrogen atom or a lower alkanoyl group;

Derivatives of macrolide antibiotics

Growing community of inventors

Fujisawa, Japan

Rokuro Okamoto