Eisai Company, Limited

Eisai R&d Management Co., Ltd.

Masanobu Shinoda

Fumiyoshi Matsuura

Richard S Clark

Tetsuya Kawahara

Takashi Inoue

Kazuto Yamazaki

Eita Emori

Sadakazu Miyashita

Hideki Yoshitomi

Shunji Kasai

Hitoshi Harada

Taro Hihara

Shigeki Hibi

Katsuya Tagami

Yasushi Okamoto

Naoki Kobayashi

Hirotoshi Numata

Isao Yamatsu

Takashi Yamanaka

Manabu Murakami

Kiyoshi Oketani

Shuichi Suzuki

Motoji Kogushi

Hiroko Kobayashi

Shuhei Miyazawa

Masato Ueda

Mitsuaki Miyamoto

Fumihiro Ozaki

Kazuo Okano

Nobuaki Sato

Akiharu Kajiwara

Nobuhisa Watanabe

Ieharu Hishinuma

Atsuhiko Kubota

Junichi Nagakawa

Hiroshi Tanaka

Itaru Tsukada

Atsushi Kamada

Makoto Kotake

Hideaki Fujisaki

Taro Terauchi

Toshiyuki Matsuoka

Yoshimitsu Naoe

Daisuke Iida

Akifumi Kimura

Osamu Ito

Ken-ichi Chiba

Naoto Ono

Syuhei Miyazawa

Yoshiaki Oohashi

Hiroki Terauchi

Toshihiko Kaneko

Shigeto Negi

Keisuke Matsuyama

Koukichi Harada

Kenji Hayashi

Tsutomu Kawata

Kazunobu Kira

Koichi Abe

Hiroshi Azuma

Manabu Sasho

Shinsuke Hirota

Norihito Ohi

Kaname Miyamoto

Takao Omae

Kaoru Murata

Kazutomi Kusano

Katsutoshi Nishiura

Takashi Musha

Mamoru Miyazawa

Naoki Ozeki

Susumu Inoue

Kaya Ohashi

Masaharu Gotoda

So Yasui

Teiji Takigawa

Atsushi Takemura

Tsutomu Kawada

Masaki Mikamoto

Yoshihiko Hisatake

Takashi Seiki

Taro Hibara

Takashi Musya

Ken-Ichi Chiba

Keni-Ichi Chiba

Takashii Musha

By oral administration of a compound represented by the following Formula (I): the blood level of Compound (IV): which has an excellent inhibitory action against blood coagulation factor VIIa and the anticoagulant action, reaches a level sufficient for expression of its pharmacological actions. Therefore, the compound of the present invention is useful as a therapeutic and/or prophylactic agent for diseases caused by thrombus formation. 

Prodrug of triazolone compound

A novel chemical compound useful as a therapeutic or prophylactic agent for acid-related diseases is provided, which has an excellent inhibitory effect against gastric acid secretion, an excellent effect of maintaining the inhibitory effect against gastric acid secretion, thereby maintaining intragastric pH high for a long time, and having more safety and appropriate physicochemical stability. Provided is a compound represented by where Rand Rmay be the same or different and each represent a hydrogen atom or a C1-C6 alkyl group; Rrepresents (5,5-dimethyl-1,3-dioxan-2-yl)methoxy group, 5,7-dioxaspiro[2.5]oct-6-ylmethoxy group, 1,5,9-trioxaspiro[5.5]undec-3-ylmethoxy group, or (2,2-dimethyl-1,3-dioxan-5-yl)methoxy group; R, R, Rand Rrepresent a hydrogen atom, halogen atom, C1-C6 alkyl group, C1-C6 haloalkyl group, C1-C6 alkoxy group or C1-C6 haloalkoxy group; and Wrepresents a single bond, methylene or ethylene group, a salt thereof or a solvate of these.

Benzimidazole compound

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

The present invention provides novel carboxylic acid derivatives useful as an insulin sensitizer, a salt thereof or a hydrate of them, and a medicament comprising the derivative as the active ingredient. Specifically, it provides a carboxylic acid derivative represented by the following formula (I): (wherein Y, L, X, T, Z, U, M and W are defined in the specification) and a salt thereof, and ester thereof or a hydrate of them.

Carboxylic acid derivative, a salt thereof or an ester of them, and medicament comprising it

Carboxylic acid compound or salt or hydrate thereof useful as insulin sensitizer, represented by the formula wherein Rrepresents hydrogen, hydroxyl, halogen, carboxyl, or Calkyl, L represents single bond or C-alkylene, C-alkenylene, or C-alkynylene, M represents single bond or C-alkylene, C-alkenylene, or C-alkynylene, T represents single bond, or C-alkylene, C-alkenylene, or C-alkynylene, W represents carboxyl, represents single bond, X represents single bond, oxygen, &#x2014;NRCQO&#x2014;, &#x2014;OCQNR&#x2014;, &#x2014;CQNRO&#x2014;, ONRCQ&#x2014;, &#x2014;QSO&#x2014;, or &#x2014;SOQ&#x2014;, Y represents 5- to 14-membered aromatic group, and ring Z represents 5- to 14-membered aromatic group.

Carboxylic acid derivative and salt thereof

A cyclic amidine derivative represented by the formula: [wherein R, Rand Rrepresent hydrogen, Calkyl, aryl-Calkyl, etc.; R, Rand Rrepresent hydrogen, Calkyl, etc.; Z represents 0 or 1; Rrepresents hydrogen, Calkyl, Calkyloxycarbonyl, etc.; n represents 1 or 2; Yrepresents a single bond, &#x2014;CH&#x2014;, etc.; Yrepresents a single bond, &#x2014;CO&#x2014;, etc.; Ar represents hydrogen, a group represented by the formula: [wherein R-Rrepresent hydrogen, Calkyl, hydroxyl, Calkoxy, etc., and Rand Ror Rand Rmay bond together to form a 5- to 8-membered heterocycle], etc.]or a salt thereof.

Cyclic amidine derivatives

An object of the present invention is to provide a novel chemical compound useful as a therapeutic or prophylactic agent for acid-related diseases, having an excellent inhibitory effect against gastric acid secretion, an excellent effect of maintaining the inhibitory effect against gastric acid secretion, thereby maintaining intragastric pH high for a long time, and having more safety and appropriate physicochemical stability. Provided is a compound represented by 

The present invention provides a novel compound having an excellent PPAR agonist action. More specifically, it provides a compound represented by the following formula, a salt thereof, an ester thereof or a hydrate of them. Wherein a, b and c are the same as or different from one another and each represents 0 to 4; Rto Rare the same as or different from one another and each represents a hydrogen atom, a hydroxyl group, a cyano group, a halogen atom, etc.; represents a single bond or a double bond;

Cyclic compound and PPAR agonist

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)

The present invention provides a novel carboxylic acid derivative, a salt thereof or a hydrate of them which is useful as an insulin sensitizer, and a medicament comprising the derivative as the effective ingredient. More specifically, it provides a carboxylic acid compound represented by the formula (I), a salt thereof or a hydrate of them. In the formula, Ar represents a 6- to 14-membered aromatic ring group which may have at least one substituent; R, R, R, R, R, R, Rand Rare the same as or different from each other and each represents a hydrogen atom, a halogen atom, a hydroxyl group, a Calkyl group or a Calkoxy group; X represents an oxygen atom or a methylene group; Y represents a group represented by the formula (II) or (III): (wherein Z represents a group represented by the formula (IV): (wherein R, R, Rand Rare the same as or different from each other and each represents a hydrogen atom, a halogen atom, a hydroxyl group, a Calkyl group or a Calkoxy group)); m is 0 or 1; and n is 0 or 1.

Carboxylic acids

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

The present invention provides a medicament comprising a benzene compound useful as an insulin sensitizer, a salt thereof or a hydrate of them and a derivative of them as the active ingredient. Specifically, it provides a benzene compound represented by the following formula, a salt thereof or a hydrate of them. In the formula, X represents 1) a Caryl group which may have one or more substituents or 2) a 5- to 10-membered heteroaryl group which may have one or more substituents; Y represents a group represented by the formula: (in the above formulae, R, Rand Rare the same as or different from one another and each represents a hydrogen atom, a halogen atom, a Calkyl group, a Calkoxy group, or a Ccycloalkyl group) etc.; Z represents a group represented by the formula: (in the formula, m represents an integer of 0 to 2; R, Rand Rare the same as or different from one another and each represents a hydrogen atom, a halogen atom, a Calkyl group, a Calkoxy group, a Ccycloalkyl group, a halogenated Calkyl group, a halogenated Calkoxy group etc.); and R, R, Rand Rare the same as or different from one another and each represents a hydrogen atom, a halogen atom, a Calkyl group, a Calkoxy group, a Ccycloalkyl group etc.

Benzene compound and salt thereof

Novel carboxylic acid derivatives of general formula (I), salts of the same, esters thereof, or hydrates of them, which are useful as insulin resistance improvers; and drugs containing the derivatives as the active ingredient. In said formula, Ris hydrogen, hydroxyl, alkyl, or the like; L is a single bond, a double bond, alkylene, or the like; M is a single bond, alkylene, or the like; T is a single bond, alkylene, or the like; W is carboxyl, &#x2014;CON(R)R, or the like;represents a single or double bond; X is oxygen, alkenylene, or the like; Y is an aromatic hydrocarbon group which may contain a heteroatom, or the like; and Z is an aromatic hydrocarbon group which may contain a heteroatom.

Carboxylic acid derivatives and drugs containing the same

A benzothiazole derivative or a pharmacologically acceptable salt thereof of the following formula, as defined in the claims, which is useful as a preventive or therapeutic agent for diseases on which functions of suppressing leukotrienes and thromboxanes production are effective: ##STR1##

Benzothiazole compounds which are substituted by pyridymethyl

A benzothiazole derivative or a pharmacologically acceptable salt thereof which is useful as a preventive or therapeutic agent for diseases on which functions of suppressing leukotrienes and thromboxanes production are effective. A benzothiazole derivative represented by the following general formula (I): ##STR1##

Pyridyl substituted benzothiazole compounds which have useful

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Ibaraki, Japan

Masanobu Shinoda