Eisai R&d Management Co., Ltd.

Mercian Corporation

Eisai Company, Limited

Takashi Sakai

Yoshihiko Kotake

Jun Niijima

Naoki Asai

Takashi Nakashima

Satoshi Yamamoto

Tomohiro Sameshima

Naoto Kawamura

Susumu Takeda

Akifumi Okuda

Kiyoshi Okamoto

Mitsuo Nagai

Toshio Tsuchida

Masashi Yoshida

Kazuyuki Dobashi

Yoshiharu Mizui

Toshimitsu Uenaka

Takao Yamori

Masanori Fujita

Regina Mikie Kanada

Motoko Matsufuji

Daisuke Ito

Tomonari Yamada

Keisuke Komeda

Kumiko Kishi

Masao Iwata

Koji Norihisa

Katsura Kaneko

Taira Kato

Process for producing compound of Formula: wherein P, Pand Rare the same as defined below, characterized by comprising reacting a compound represented by Formula (7): wherein Pmeans a protecting group for hydroxy group; and Het means a 1-phenyl-1H-tetrazol-5-yl group, with a compound represented by Formula (8): wherein Pmeans a protecting group for hydroxy group; and Rmeans a phenyl group which may be substituted, in the presence of a base.

Process for total synthesis of pladienolide B and pladienolide D

A process for producing a compound represented by Formula (11): wherein P, P, P, Pand Rare the same as defined herein, characterized by including reacting a compound represented by Formula (12): with a compound represented by Formula (13): in the presence of a catalyst.

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

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

Physiologically active substances

Growing community of inventors

Ibaraki, Japan

Takashi Sakai