Eisai R&d Management Co., Ltd.

Eisai Company, Limited

Atsushi Kamada

Fumihiro Ozaki

Nobuaki Sato

Itaru Tsukada

Kazumasa Nara

Yoshimitsu Naoe

Toshihiko Kaneko

Richard S Clark

Tetsuya Kawahara

Noritaka Kitazawa

Kazuo Okano

Atsushi Sasaki

Tomohiro Matsushima

Tadashi Okabe

Manabu Sasho

Shinichi Hamaoka

Takahisa Sakaguchi

Takaaki Suzuki

Shuhei Miyazawa

Mitsuaki Miyamoto

Isao Sugiyama

Akiharu Kajiwara

Nobuhisa Watanabe

Norio Karibe

Ieharu Hishinuma

Hideyuki Adachi

Kazuki Miyazaki

Hiroshi Tanaka

Masanobu Shinoda

Fumiyoshi Matsuura

Hiroki Ishihara

Makoto Kotake

Kazuhide Ashizawa

Taro Terauchi

Shuji Shirotori

Tadashi Nagakura

Toshiyuki Matsuoka

Shuichi Suzuki

Kohtarou Kodama

Motoji Kogushi

Osamu Ito

Akifumi Kimura

Hiroko Kobayashi

Mamoru Miyazawa

Naoto Ono

Ken-ichi Chiba

Kazunori Wakasugi

Yoshiaki Oohashi

Syuhei Miyazawa

Shinya Abe

Shigeto Negi

Koichi Ito

Naoyuki Shimomura

Masato Ueda

Mitsuo Nagai

Kenzo Muramoto

Jun Niijima

Keiko Takahashi

Tsutomu Kawata

Hitoshi Harada

Norihito Ohi

Hiroshi Ishihara

Kazuhiro Yoshizawa

Taiju Nakamura

Hiromitsu Yokohama

Yusuke Ayata

Takashi Musha

Itaru Arimoto

Tohru Arai

Masaharu Gotoda

Masayoshi Ohkuro

Hiroki Terauchi

Keizo Sato

Tsutomu Kawada

Takashi Musya

Jiro Sonoda

Osamu Takenaka

Naoko Suzuki

Takashii Musha

Keni-Ichi Chiba

Ken-Ichi Chiba

Tadashi c/o Tsukuba Research Laboratories Okabe

Shinichi Tsukuba Res Lab Eisai Co Ltd Hamaoka

Yusuke c/o Eisai Co Ltd Ayata

Itaru c/o Eisai Co Ltd Arimoto

Kazuhiro c/o Eisai Co Ltd Yoshizawa

Sachiko Kikuchi

The present invention provides a compound represented by the following formula (I); [wherein T represents a single bond, a C1-C4 alkylene group which may have a substituent and the like; formula (I-1) represents a single bond or a double bond; A represents a single bond, a bivalent 5- to 14-membered heterocyclic group which may have a substituent and the like; Y represents a single bond and the like; Z represents a methylene group and the like; ring G represents a phenylene group and the like which may condense with a 5- to 6-membered ring and may have a heteroatom; Rand Rare the same as or different from each other and represent a hydrogen atom and the like; W represents a single bond and the like; R' represents 1 to 4 independent hydrogen atoms and the like; and R&#x2033; represents 1 to 4 independent hydrogen atoms and the like] or a salt thereof, or a hydrate thereof.

Selective estrogen receptor modulator

The invention provides acid addition salts of the compounds represented by formula (1) or (2), or crystals thereof, and processes for preparing the same. The salts or crystals have HGFR inhibitory activity and excellent physical properties (solubility, safety, etc.) and are therefore useful as anti-tumor agents, angiogenesis inhibitors and inhibitors for metastasis for a various types of tumor. 

Phenoxypyridine derivative salts and crystals thereof, and process for preparing the same

It is possible to commercially advantageously prepare 1-{1-[2-(7-methoxy-2,2-dimethyl-4-oxochroman-8-y)ethyl]piperidin-4-yl}-N-methyl-1H-indole-6-carboxamide by coupling (7-methoxy-2,2-dimethyl-4-oxochroman-8-yl)acetaldehyde, which is obtained by oxidizing 8-(2-hydroxyethyl)-7-methoxy-2,2-dimethylchroman-4-one, with N-methyl-1-(piperidin-4-yl)-1H-indole-6-carboxamide.

Method for producing indole derivative having piperidine ring

The present invention provides a compound represented by the following formula (I); [wherein T represents a single bond, a C1-C4 alkylene group which may have a substituent and the like;&#x2003;&#x2003;(I-1)formula (I-1) represents a single bond or a double bond; A represents a single bond, a bivalent 5- to 14-membered heterocyclic group which may have a substituent and the like; Y represents a single bond and the like; Z represents a methylene group and the like; ring G represents a phenylene group and the like which may condense with a 5- to 6-membered ring and may have a heteroatom; Rand Rare the same as or different from each other and represent a hydrogen atom and the like; W represents a single bond and the like; R' represents 1 to 4 independent hydrogen atoms and the like; and R&#x2033; represents 1 to 4 independent hydrogen atoms and the like] or a salt thereof, or a hydrate thereof.

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

A process for preparing a compound represented by the formula (I): comprising reacting a compound represented by the formula (II) or salt thereof: with a compound represented by the formula (III): in the presence of a condensation reagent,wherein Rrepresents 1) optionally substituted azetidin-1-yl, 2) optionally substituted pyrrolidin-1-yl, 3) optionally substituted piperidin-1-yl, etc.; R, R, Rand Rmay be the same or different and each represents hydrogen or fluorine; and Rrepresents hydrogen or fluorine.

Process for preparing phenoxypyridine derivatives

A crystal of a 4-(3-chloro-4-(cyclopropylaminocarbonyl)aminophenoxy)-7-methoxy-6-quinolinecarboxamide hydrochloride, hydrobromide, p-toluenesulfonate, sulfate, methanesulfonate or ethanesulfonate, or a solvate thereof.

Crystalline form of the salt of 4-(3-chloro-4-(cyclopropylaminocarbonyl)aminophenoxy)-7-methoxy-6-quinolinecarboxamide or the solvate of the salt and a process for preparing the same

The present invention provides a compound represented by the following formula (I); [wherein T represents a single bond, a C1-C4 alkylene group which may have a substituent and the like;formula (I-1) represents a single bond or a double bond; A represents a single bond, a bivalent 5- to 14-membered heterocyclic group which may have a substituent and the like; Y represents a single bond and the like; Z represents a methylene group and the like; ring G represents a phenylene group and the like which may condense with a 5- to 6-membered ring and may have a heteroatom; Rand Rare the same as or different from each other and represent a hydrogen atom and the like; W represents a single bond and the like; R' represents 1 to 4 independent hydrogen atoms and the like; and R&#x2033; represents 1 to 4 independent hydrogen atoms and the like] or a salt thereof, or a hydrate thereof.

A 2-iminoimidazole derivative represented by the formula: {wherein R, Rand Rrepresent hydrogen, optionally substituted Calkyl, etc.; Rrepresents hydrogen, Calkyl, Calkyloxycarbonyl, etc.; Yrepresents a single bond, &#x2014;CH&#x2014;, etc.; Yrepresents a single bond, &#x2014;CO&#x2014;, etc.; and Ar represents hydrogen, a group represented by the formula: [wherein R&#x2013;Rrepresent hydrogen, Calkyl, hydroxyl, Calkoxy, etc., and Rand Ror Rand Rmay bond together to form a 5- to 8-membered heterocycle], etc.}or salt thereof.

2-iminoimidazole derivatives (2)

A 2-iminopyrrolidine derivative represented by the formula: {wherein ring B represents a benzene ring, pyridine ring, etc.; R&#x2013;Rrepresent hydrogen, halogen, Calkyl, etc.; Rrepresents hydrogen, Calkyl, Calkoxy-Calkyl, etc.; Rrepresents hydrogen, Calkyl, Calkyloxycarbonyl, etc.; Yrepresents a single bond, &#x2014;CH&#x2014;, etc.; Yrepresents a single bond, &#x2014;CO&#x2014;, etc.; and Ar represents hydrogen, a group represented by the formula: [wherein R&#x2014;Rrepresent hydrogen, Calkyl, hydroxyl, Calkoxy, etc.; and Rand Ror Rand Rmay bond together to form a 5- to 8-membered heterocyclic ring], etc.},or a salt thereof.

2-iminopyrrolidine derivatives

Phthalazine compounds and therapeutic agents for erectile dysfunction

Benzopiperidine derivatives

Phthalazine derivatives and remedies for erectile dysfunction

Intermediates useful for the manufacture of carbapenem and a stereoselective manufacturing method therefor

Growing community of inventors

Tsukuba, Japan

Atsushi Kamada