Mercian Corporation

Eisai R&d Management Co., Ltd.

Other

Eisai Company, Limited

Dainippon Pharmaceutical Company, Limited

Sanraku Incorporated

Merican Corporation

Toshio Tsuchida

Takashi Nakashima

Mitsuo Nagai

Masashi Yoshida

Yoshihiko Kotake

Jun Niijima

Yoshio Fukuda

Susumu Takeda

Regina Mikie Kanada

Tomohiro Sameshima

Masahi Yoshida

Tomio Takeuchi

Kiyoshi Okamoto

Takeo Yoshioka

Rokuro Okamoto

Satoshi Yamamoto

Kunio Isshiki

Hiroshi Tone

Kazuyuki Dobashi

Yoshiharu Mizui

Naoto Kawamura

Toshimitsu Uenaka

Masanori Fujita

Takao Yamori

Motoko Matsufuji

Naoki Asai

Kazuhiro Machida

Takashi Sakai

Tomonari Yamada

Akifumi Okuda

Koji Norihisa

Ryoichi Miyata

Hazuki Nagai

Kaname Konuki

Asako Kuroda

Keisuke Komeda

Kumiko Kishi

Masao Iwata

Hiroshi Harada

Shiro Kato

Naoki Matsumoto

Takao Narita

Akihito Fujii

Yasuhide Aritoku

Katsura Kaneko

Yoichiro Hirose

Kunihiro Toyoda

Mikie Regina Kanada

The present invention provides polypeptides that participate in the biosynthesis of the pladienolide macrolide compounds, DNA that encodes these polypeptides and variants of this DNA, transformants that maintain all or a portion of this DNA or variant thereof, and a method of producing the pladienolide macrolide compounds using these transformants. More particularly, it provides an isolated pure DNA that contains at least one region encoding a polypeptide that participates in pladienolide biosynthesis; polypeptide encoded by this DNA; a self-replicating or integrated-replicating recombinant plasmid carrying this DNA; a transformant maintaining this DNA; and a method of producing a pladienolide, characterized by culturing this transformant on culture medium and collecting pladienolide from this culture medium.

DNA coding for polypeptide participating in biosynthesis of pladienolide

The present invention provides a DNA participating in biological transformation of a macrolide compound 11107B. The present invention provides, particularly, a DNA participating in biological transformation of a macrolide compound 11107B represented by the formula (I) into a 16-position hydroxy macrolide compound 11107D represented by the formula (II), the DNA encoding a protein having 16-position hydroxylating enzymatic activity or ferredoxin, to a method of isolating the DNA, to a protein encoded by the DNA, a plasmid carrying the DNA, a transformant obtained by transforming using the plasmid and a method of producing a 16-position hydroxy compound by using the transformant. 

DNA participating in hydroxylation of macrolide compound

The present invention relates to a compound represented by the formula (I): (wherein, R, R, Rand Rare the same as or different from one another and each represents a hydroxyl group etc.), a pharmacologically acceptable salt thereof or a hydrate of them. The compound (I) of the present invention suppresses angiogenesis, in particular, suppresses VEGF production in a hypoxic condition and is useful as a therapeutic agent for treating solid cancer.

Physiologically active substances

The present invention provides a novel bioactive substance having an antitumor activity and a process for producing it, and a medical use thereof. Namely, it provides a 12-membered ring macrolide compound represented by the following formula obtained from the incubation solution ofsp. Mer. 11107 or a variant thereof, a pharmacologically acceptable salt thereof or a hydrate of them, and a process for producing it. 

Bioactive substance

A compound represented by the following general formula (I): (I) wherein Rand Rare the same or different and each represents optionally substituted Calkoxy, etc.; a pharmaceutically acceptable salt thereof or hydrates of the same. The compound (1) inhibits angiogenesis and inhibits the production of VEGF particularly under hypoxic conditions, which makes it useful as a remedy for solid cancer.

Heterocyclic macrolide pharmaceutical agent, a method of producing the same and use of the same

Compounds represented by the following general formula (I), pharmacologically acceptable salts thereof or hydrates of the same: (I) wherein W represents and R, R, R, R, R, Rand Rare the same or different and each represents hydrogen, etc. Because of inhibiting angiogenesis and inhibiting the production of VEGF particularly in hypoxia, the compounds (I) are useful as remedies for solid cancer.

A method of manufacturing a pipecolamide derivative, characterized in that pipecolic acid or an acid salt thereof is reacted with an amine in an inert solvent in the presence of a condensing agent such as dicyclohexylcarbodiimide, 1-ethyl-2-(2-dimethylaminopropyl)carbodiimide, methanesulfonyl chloride or phosphoryl chloride. Pipecolamide derivatives, particularly in optically active forms thereof can be efficiently and economically manufactured without harmful gas by-products.

Method for producing pipecolamide derivative

Disclosed are a process for preparation of an optically active 7-substituted 3-(2-aminopropyl)indole compound and an intermediate therefor. In the above preparation process, 7-substituted indole is reacted with L- or DL-serine in the presence of a tryptophan-synthesizing enzyme originating in microorganisms to form corresponding 7-substituted L-tryptophan, and it is subjected, if necessary, to reduction, protection, exchange and elimination.

Process for the preparation of optically active 7-substituted-3-(2-aminopropyl)indole derivatives and intermediates therefor

The present invention provides a novel bioactive substance having an antitumor activity and a process for producing it, and a medical use thereof. Namely, it provides a 12-membered ring macrolide compound represented by the following formula obtained from the incubation solution ofsp. Mer. 11107 or a variant thereof, a pharmacologically acceptable salt thereof or a hydrate of them, and a process for producing it

Process for producing isocoumarins and intermediates for the same

Process for producing isocoumarines and intermediates for the same

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

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

Anthracycline derivatives

Growing community of inventors

Shizuoka, Japan

Toshio Tsuchida