Eisai Company, Limited

Eisai R&d Management Co., Ltd.

Mercian Corporation

Merican Corporation

Jun Niijima

Yoshihiko Kotake

Takeshi Nagasu

Nozomu Koyanagi

Kentaro Yoshimatsu

Hiroshi Yoshino

Norihiro Ueda

Tatsuo Watanabe

Kyosuke Kitoh

Toshimi Okada

Mitsuo Nagai

Takashi Nakashima

Toshio Tsuchida

Kappei Tsukahara

Hiroyuki Sugumi

Makoto Asada

Regina Mikie Kanada

Atsumi Iijima

Yoshio Fukuda

Takashi Sakai

Naoki Asai

Toru Haneda

Masashi Yoshida

Tomohiro Sameshima

Toshimitsu Uenaka

Susumu Takeda

Naoko Tsukahara

Masahi Yoshida

Kiyoshi Okamoto

Satoshi Yamamoto

Kazuyuki Dobashi

Yoshiharu Mizui

Naoto Kawamura

Takao Yamori

Masanori Fujita

Motoko Matsufuji

Eiichi Yamamoto

Daisuke Ito

Akifumi Okuda

Tomonari Yamada

Keisuke Komeda

Kumiko Kishi

Masao Iwata

Koji Norihisa

Shinya Abe

Shigeto Negi

Keigo Tanaka

Osamu Asano

Masayuki Matsukura

Atsushi Kamada

Kazutaka Nakamoto

Kazumasa Nara

Manabu Sasho

Kazuhiro Yoshizawa

Ikuo Kushida

Hirofumi Kuroda

Kyosuke Kito

Atsumi Yamaguchi

Mamoru Miyazawa

So Yasui

Katsuji Nakamura

Keizo Sato

Yoko Ito

Takuma Minamisono

Jun-ichi Kamata

Yuki Kosaka

Hirovuki Sugumi

Mikie Regina Kanada

The present invention provides crystals of (1R,3R,15E,28R,29R,30R,31R,34R,36R,39S,41R)-29,41-Difluoro-34,39-bis(sulfanyl)-2,33,35,38,40,42-hexaoxa-4,6,9,11,13,18,20,22,25,27-decaaza-34&#x3bb;,39&#x3bb;-diphosphaoctacyclo[28.6.4.10.10000]dotetraconta-5,7,9,11,15,19,21,23,25-nonaene-34,39-dione (Compound (I)) ammonium salts, Compound (I) sodium salts, or Compound (I), possessing a potential to be used as drug substance in pharmaceuticals.

Salts of compounds and crystals thereof

Crystals, amorphous substances, salts, and hydrates of a salt of methyl N-[3-(6,7-dimethoxy-2-methylaminoquinazolin-4-yl)phenyl]terephthalamic acid having PDE4 inhibitory action are provided. These compounds are useful for treating allergic diseases such as atopic dermatitis.

Crystals, amorphous substances or salts of methyl N-[3-(6,7-dimethoxy-2-methylaminoquinazolin-4-yl) phenyl] terephthalamic acid

[4-(3-aminophenyl)-6,7-dimethoxyquinazolin-2-yl]methylamine with a favorable yield and high purity can be produced by subjecting a compound represented by the following formula (I) to a step of reacting with methylamine and a step of deprotection if desired: wherein L represents a protective group of amino.

Method for producing quinazoline derivative

It is an object of the present invention to provide an efficient method for manufacturing heterocycle-substituted pyridine derivatives. The present invention provides a method for manufacturing a compound represented by the following formula (I):   

Method for manufacturing heterocycle substituted pyridine derivatives

There is provided a heterocycle-substituted pyridine derivative's salt or a crystal thereof. The present invention provides an acid addition salt of 3-(3-(4-(pyridin-2-yloxymethyl)-benzyl)-isoxazol-5-yl)-pyridin-2-yl amine or a crystal thereof as well as process for producing the same.

Heterocycle-substituted pyridine derivative's salt or crystal thereof

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.

An object of the present invention is to provide a process, or the like, suitable for the industrialization of effective deprotection reaction without using a toxic solvent as well as to provide a process, or the like, for preparing a water-soluble azole prodrug effectively. The present invention provides a process for preparing a salt represented by Formula (I); (wherein X represents a fluorine atom bonded at position 4 or position 5 of a phenyl group) comprising the steps of: (a) carrying out a deprotection reaction of a compound represented by Formula (II); (wherein X represents a fluorine atom bonded at position 4 or position 5 of a phenyl group)in the presence of a carbocation scavenger.

Process for preparation of water-soluble azole prodrugs

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.

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

Fused polycyclic heterocycle derivatives

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Tsukuba, Japan

Jun Niijima