Eisai R&d Management Co., Ltd.

Mercian Corporation

Eisai Company, Limited

Merican Corporation

Regina Mikie Kanada

Yoshihiko Kotake

Jun Niijima

Mitsuo Nagai

Takashi Nakashima

Toshio Tsuchida

Yoshio Fukuda

Masahi Yoshida

Takashi Sakai

Naoki Asai

Daisuke Ito

Masashi Yoshida

Tomohiro Sameshima

Susumu Takeda

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

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.

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.

Growing community of inventors

Ibaraki, Japan

Regina Mikie Kanada