Eisai R&d Management Co., Ltd.

Eisai Company, Limited

Naoki Ozeki

Hitoshi Harada

Susumu Inoue

Shigeto Negi

Kenji Hayashi

Hiroyuki Chiba

Yuki Komatsu

Yoshiaki Sato

Seiichi Kobayashi

Naoyuki Shimomura

Keisuke Matsuyama

Osamu Asano

Manabu Murakami

Nobuhisa Watanabe

Tsutomu Kawata

Masanobu Shinoda

Takashi Inoue

Fumiyoshi Matsuura

Toshihiko Naito

Toshikazu Shimizu

Manabu Sasho

Nobuyuki Yasuda

Junsaku Nagaoka

Seiji Yoshikawa

Tatsuo Horizoe

Hiroshi Ishihara

Isao Tanaka

Kaoru Murata

Mamoru Miyazawa

Hiroe Minami

Katsutoshi Nishiura

Masaharu Gotoda

Kaya Ohashi

Teiji Takigawa

Toyokazu Haga

Yoshihiko Hisatake

Hiroshi Akamatsu

The present invention relates to calcium bis[(2S)-3-[3-[(2S)-3-(4-chloro-2-cyanophenoxy) -2-fluoropropoxy]phenyl]-2-isopropoxypropionate] represented by formula (I), a hydrate thereof, a crystal of the compound of formula (I), and a crystal of the hydrate of the compound of formula (I) which are useful as pharmaceuticals, and to processes for producing the same, and intermediates therefore, and processes for production thereof. There is need for (2S)-3-[3-[(2S)-3-(4 -chloro-2-cyanophenoxy)-2-fluoropropoxy]phenyl]-2-isopropoxypropionic acid, in the form of a drug substance, purified so as to minimize a residual solvent content and having a uniformized specification and a highly favorable workability, and a process for producing the same. Crystalline calcium bis[(2S)-3-[3-[(2S)-3-(4 -chloro-2-cyanophenoxy)-2-fluoropropoxy]phenyl]-2-isopropoxypropionate], a calcium salt of (2S) -3-[3-[(2S)-3-(4-chloro-2-cyanophenoxy)-2-fluoropropoxy]phenyl]-2-isopropoxypropionic acid, solves the above problem.

Calcium bis [(2S)-3-[3-[(2S)-3-(4-chloro-2-cyanophenoxy)-2-fluoropropoxy]phenyl ]-2-isopropoxypropionate] and intermediate thereof

Crystals of 5-[2-amino-4-(2-furyl)pyrimidin-5-yl]-1-methylpyridin-2(1H)-one having a diffraction peak at a diffraction angle (2&#x3b8;&#xb1;0.2&#xb0;) of 9.7&#xb0; and/or 21.9&#xb0; in a powder X-ray diffraction are suitable for an active ingredient of a preventing and therapeutic agent for diseases such as constipation. Crystals of 5-[2-amino-4-(2-furyl)pyrimidin-5-yl]-1-methylpyridin-2(1H)-one hydrate and amorphous 5-[2-amino-4-(2-furyl)pyrimidin-5-yl]-1-methylpyridin-2(1H)-one hydrate are also suitable for an active ingredient of a preventing and therapeutic agent for diseases such as constipation.

Crystals of pyrimidine compound and process for producing the same

Crystalline and amorphous pyrimidine compounds and processes for preparing pyrimidine compounds

The present invention provides a preventive or therapeutic agent for diabetes mellitus and diabetic complications, which is a new type based on an adenosine A2 receptor antagonist action. That is, it provides a novel condensed imidazole compound which has an adenosine A2 receptor antagonist action, is effective for preventing or treating diabetes mellitus and diabetic complications, and is represented by the formula (I);(wherein Rrepresents e.g. an amino group which may be substituted with an alkyl group; Rrepresents e.g. hydrogen atom, an alkyl group, a cycloalkyl group or an alkyl group, alkenyl group or alkynyl group which may be substituted with hydrox etc.; Rrepresents e.g. an optionally substituted alkyl group, alkenyl group, alkynyl group, aryl group, heteroaryl group, pyridinone group, pyrimidinone group or piperadinone group; Ar represents e.g. an optionally substituted aryl or heteroaryl group; and Q and W are the same as or different from each other and each represents N or CH), a pharmacologically acceptable salt or hydrates thereof.

Condensed imidazole compounds and a therapeutic agent for diabetes mellitus

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Tsukuba, Japan

Naoki Ozeki