Mercian Corporation

Eisai Company, Limited

Eisai R&d Management Co., Ltd.

Zaidan Hojin Biseibutsu Kagaku Kenkyu Kai

Mercian Corporation and Eisai Co., Ltd.

Tomohiro Sameshima

Takashi Nakashima

Naoto Kawamura

Susumu Takeda

Mitsuo Nagai

Yoshihiko Kotake

Jun Niijima

Satoshi Yamamoto

Toshio Tsuchida

Masashi Yoshida

Kazuyuki Dobashi

Masanori Fujita

Motoko Matsufuji

Takashi Sakai

Akifumi Okuda

Kiyoshi Okamoto

Yoshiharu Mizui

Toshimitsu Uenaka

Takao Yamori

Naoki Asai

Hiroyuki Kumagai

Tomonari Yamada

Koji Norihisa

Keisuke Komeda

Masao Iwata

Kumiko Kishi

Tomio Takeuchi

Yoshio Watanabe

Takeo Yoshioka

Masaaki Ishizuka

Yasuhiro Funahashi

Kunio Isshiki

Yoshio Fukuda

Taro Semba

Toshiaki Wakabayashi

Hiroyuki Inoue

Regina Mikie Kanada

Tetsuya Someno

Tadashi Fujii

Katsura Kaneko

Taira Kato

Nobuaki Naruse

Rena Kawase

Kazuya Sakai

The present invention provides a novel method of producing the 12-membered ring macrolide compound 11107D having an antitumor activity by biological transformation. Starting material which is the 12-membered ring macrolide compound 11107B represented by the formula (I) is incubated in the presence of a strain belonging to the genus, the genusor the family Micromonosporaceae (for example,sp. AB-1704 strain (FERM BP-8551)), each of which has the ability of transforming the 12-membered ring macrolide compound 11107B into a 11107D substance represented by the formula (II), or a preparation of its cultured myceha and oxygen, and then 11107D substance which is a target material is collected from the treating solution. 

Method of producing macrolide compound

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

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.

Physiologically active substances

A compound represented by formula (I); a process for producing a compound (substance F-1490) of formula (I), wherein X represents &#x2014;O&#x2014; and R represents a hydroxyl group, by using a microorganism belonging to the genus; and asp. F-1490 strain (FERM BP-8287) capable of producing the substance F-1490; and an osteoclast differentiation inhibitory agent containing as an active ingredient the compound represented by formula (I): wherein X represents &#x2014;O&#x2014; or &#x2014;CH&#x2014;, and R represents a hydroxyl group when X represents &#x2014;O&#x2014;, or a hydrogen atom when X represents &#x2014;CH&#x2014;.

Osteoclast differentiation inhibitors

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

Chrysomycin derivative compounds and use as antitumor agents

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Shizuoka, Japan

Tomohiro Sameshima