Eisai R&d Management Co., Ltd.

Eisai Company, Limited

Shinsuke Hirota

Richard S Clark

Fumiyoshi Matsuura

Hiroshi Azuma

Kazunobu Kira

Takao Omae

Kazutomi Kusano

Tetsuya Kawahara

Naoki Yoneda

Atsushi Inoue

Makoto Kotake

Tadashi Nagakura

Tatsuo Horizoe

Kimiyo Tabata

Yu Yoshida

Yoshiaki Ohashi

Daisuke Iida

So Yasui

Masayoshi Ohkuro

Takashi Fukuyama

Yoshihisa Kobayashi

Yasuaki Kamada

Toru Watanabe

Keigo Tanaka

Nobuaki Sato

Masanobu Shinoda

Kogyoku Shin

Yoshihiko Norimine

Norio Murai

Kunitoshi Takeda

Yoichi Kita

Tamaki Hoshikawa

Koji Hagiwara

Wataru Itano

Nobuhiro Sato

Atsushi Takemura

Toshiyuki Ohfusa

Tomoyuki Shibuguchi

Masaki Mikamoto

Takaaki Harada

Hikaru Yoshimura

Toshiki Kurokawa

Hironori Fukumoto

Richard Clark

The present invention provides compounds represented by formulas (I) to (XVII) or pharmaceutically acceptable salts thereof: 

Pentacyclic heterocycles

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

A compound represented by the formula (I) or a salt thereof: wherein a ring Z is a 5 to 6-membered heteroaromatic ring having one or two heteroatoms in the ring; Xis a hydrogen atom, a hydroxy group, a hydroxy Calkyl group, &#x2014;B(OH), a boronate ester group, a cyclic boronate ester group, a boranyl group, a cyclic boranyl group, &#x2014;BFM, &#x2014;Sn(R)(R)(R), a leaving group, a carboxy group, a formyl group, or &#x2014;NRR; and Xis a hydrogen atom or &#x2014;COR.

Hetero-fused cyclic compound

Compounds represented by formulae (I) to (XXII) or pharmaceutically acceptable salts thereof: 

Pyranodipyridine 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]

In one aspect, the present invention provides compounds having formula (1) or (100), a salt thereof or a hydrate of the foregoing, which compounds exhibit excellent cell adhesion inhibitory action or cell infiltration inhibitory action, and are useful as therapeutic or prophylactic agents for various inflammatory diseases and autoimmune diseases associated with adhesion and infiltration of leukocytes, such as inflammatory bowel disease (particularly ulcerative colitis or Crohn's disease), irritable bowel syndrome; rheumatoid arthritis, psoriasis, multiple sclerosis, asthma and atopic dermatitis.  wherein R10 represents optionally substituted cycloalkyl, etc., R20-23 represent hydrogen, alkyl, alkoxy, etc., R30-32 represent hydrogen, alkyl, oxo, etc., and R40 represents optionally substituted alkyl, etc.

1,2-di(cyclic)substituted benzene compounds

A compound represented by the following general formula (1) or (100), a salt thereof or a hydrate of the foregoing has excellent cell adhesion inhibitory action or cell infiltration inhibitory action, and is useful as a therapeutic or prophylactic agent for various inflammatory diseases and autoimmune diseases associated with adhesion and infiltration of leukocytes, such as inflammatory bowel disease (particularly ulcerative colitis or Crohn's disease), irritable bowel syndrome, rheumatoid arthritis, psoriasis, multiple sclerosis, asthma and atopic dermatitis. 

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Tsukuba, Japan

Shinsuke Hirota