Eisai R&d Management Co., Ltd.

Mercian Corporation

Other

Eisai Company, Limited

Masashi Yoshida

Toshio Tsuchida

Takashi Nakashima

Mitsuo Nagai

Susumu Takeda

Yoshihiko Kotake

Jun Niijima

Tomohiro Sameshima

Tomio Takeuchi

Kiyoshi Okamoto

Satoshi Yamamoto

Kunio Isshiki

Kazuyuki Dobashi

Yoshiharu Mizui

Toshimitsu Uenaka

Naoto Kawamura

Takao Yamori

Masanori Fujita

Motoko Matsufuji

Naoki Asai

Takashi Sakai

Tomonari Yamada

Akifumi Okuda

Masao Iwata

Kumiko Kishi

Koji Norihisa

Keisuke Komeda

Asako Kuroda

Kaname Konuki

Hazuki Nagai

Yoshio Fukuda

Manabu Sasho

Hiroshi Ishihara

Regina Mikie Kanada

Kazuhiro Machida

Keizo Sato

Takashi Kamahara

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 the compound of formula (I) in a solid form which, as a bulk medicament for pharmaceutical manufacture, is uniform, has a high purity, and is easy to work with. The invention further provides a process for preparing this compound, and pharmaceutical compositions containing the same. A solid form of (8E,12E,14E)-7-{(4-cycloheptylpiperazin-1-yl)carbonyl}oxy-3,6,16,21-tetrahydroxy-6,10,12,16,20-pentamethyl-18,19-epoxytricosa-8,12,14-trien-11-olide which has uniform specifications and is easy to work with was developed.

Macrolide compound in solid form, process for preparation thereof, and pharmaceutical composition containing the same

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.

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

Process for producing isocoumarins and intermediates for the same

Process for producing isocoumarines and intermediates for the same

An anti-rusting composition in solution form is prepared by dissolving anti-rusting agent in an organic solvent having a permeability greater than water, mixing the solution with a permeable water-proofing agent dissolved in a petroleum based solvent. The anti-rusting composition in solution form is applied to the surface of a desired material and the anti-rusting and water proofing agents permeate into the material from the surface thereof through capillary walls. When the solvent evaporates, a gel layer forms and a strong water-proof layer is obtained to isolate the air phase from the material.

Durable anti-rusting method

Growing community of inventors

Shizuoka, Japan

Masashi Yoshida