Eisai Company, Limited

Eisai R&d Management Co., Ltd.

Richard S Clark

Fumiyoshi Matsuura

Tetsuya Kawahara

Kazuo Okano

Kenzo Muramoto

Shinya Abe

Isao Yamatsu

Hiroyuki Yoshimura

Shuhei Miyazawa

Koukichi Harada

Masanobu Shinoda

Naoyuki Shimomura

Mitsuaki Miyamoto

Takashi Inoue

Kazuto Yamazaki

Eita Emori

Osamu Asano

Shigeru Souda

Yoshimasa Machida

Kouji Yamada

Kouichi Katayama

Hiroshi Obaishi

Kazunobu Kira

Satoshi Katayama

Hajime Tsunoda

Tadashi Nagakura

Yoshimori Sakuma

Shunji Kasai

Hideki Yoshitomi

Sadakazu Miyashita

Shinsuke Hirota

Taro Hihara

Hiroshi Azuma

Takao Omae

Kimiyo Tabata

Kazutomi Kusano

Takeshi Suzuki

Fumihiro Ozaki

Hitoshi Harada

Atsushi Kamada

Atsushi Inoue

Kenichi Chiba

Ryoichi Hashida

Tatsuo Horizoe

Seiji Yoshikawa

Toru Horie

Takashi Mori

Kenichi Kusube

Toshihiko Kaneko

Hironori Ikuta

Nobuaki Sato

Akiharu Kajiwara

Ieharu Hishinuma

Hiroshi Tanaka

Itaru Tsukada

Makoto Kotake

Taro Terauchi

Hiroshi Shirota

Norihito Ohi

Nobuyuki Yasuda

Toshiyuki Matsuoka

Yoshimitsu Naoe

Shuichi Suzuki

Osamu Ito

Motoji Kogushi

Akifumi Kimura

Hiroko Kobayashi

So Yasui

Ken-ichi Chiba

Naoto Ono

Atsushi Takemura

Syuhei Miyazawa

Yoshiaki Oohashi

Nobuhisa Watanabe

Tsutomu Kawata

Naoki Yoneda

Hiromitsu Yokohama

Daisuke Iida

Takashi Musha

Tohru Arai

Kaya Ohashi

Masayoshi Ohkuro

Yasuaki Kamada

Toshiyuki Ohfusa

Mika Aoki

Taro Hibara

Takashi Seiki

Osamu Takenaka

Jiro Sonoda

Hirsohi Shirota

Naoyuki Kimomura

Taisuke Uehara

Masaki Mikamoto

Takashi Musya

Tsutomu Kawada

Ken-Ichi Chiba

The disclosure provides pyrazolo[1,5-a]pyrimidine compounds, and pharmaceutically acceptable salts thereof, having protease-activated receptor 2 (PAR2) inhibitory action, pharmaceutical compositions containing the same, and methods of treatment using the same.

Pyrazolo[1,5-a]pyrimidine compound

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 compound represented by the following general formula (1) or salts thereof or hydrates of the foregoing: wherein R, R, Rand Reach independently represent hydrogen, etc.; Rrepresents optionally substituted phenyl, etc.; Rrepresents optionally substituted C6-10 aryl, etc.; and Zand Zeach independently represent hydrogen.

Triazolone derivatives

A Compound represented by the following general formula (1): wherein R, R, Rand Reach independently represent hydrogen, etc.; Rrepresents optionally substituted phenyl, etc.; Rrepresents optionally substituted C6-10 aryl, etc.; and Zand Zeach independently represent hydrogen or salts thereof or hydrates of the foregoing.

A Compound represented by the following general formula (1), salts thereof or hydrates of the foregoing is a novel compound useful for treatment and/or prevention of diseases associated with thrombus formation, and which is safer with suitable physicochemical stability. [wherein R, R, Rand Reach independently represent hydrogen, etc.; Rrepresents optionally substituted phenyl, etc.; Rrepresents optionally substituted C6-10 aryl, etc.; and Zand Zeach independently represent hydrogen]

A compound represented by the following general formula (1), or a salt thereof has serine protease inhibiting activity, and particularly excellent inhibiting activity against clotting factor VIIa. This compound or a salt thereof is useful as therapeutic and/or prophylactic agents for diseases associated with thrombus formation. [wherein Rrepresents hydrogen, Rrepresents optionally substituted phenyl, etc., Rrepresents optionally substituted C6-10 aryl, etc.].

2,3-dihydro-iminoisoindole derivatives

The present invention is related to compounds represented by the following formula, or salts or hydrates thereof  These are novel compounds that exhibit an excellent DPPIV-inhibiting activity.

Condensed imidazole derivatives

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

The objective of this invention is to provide novel compounds that show excellent DPPIV-inhibiting activity. The present invention provides compounds represented by the general formula (I), salts thereof, or hydrates thereof, [wherein, represents a double bond or a single bond; Xdenotes an oxygen atom or a sulfur atom; Xdenotes a Calkyl group which may have substituents; Zdenotes a nitrogen atom or the formula &#x2014;CR=; Zand Zeach independently denote a nitrogen atom, the formula &#x2014;CR=, a carbonyl group, or the formula &#x2014;NR&#x2014;; R, R, R, and Xeach independently denote a Calkyl group which may have substituents, and such].

Fused 1,3-dihydro-imidazole ring compounds

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

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Ibaraki, Japan

Richard S Clark