Eisai R&d Management Co., Ltd.

Yu Yoshida

Toshihiko Kaneko

Koichi Ito

Koki Kawano

Noritaka Kitazawa

Nobuaki Sato

Teiji Kimura

Mamoru Takaishi

Takashi Doko

Takeo Sasaki

Hiroaki Hagiwara

Takehiko Miyagawa

Yoshiaki Ohashi

Keiichi Sorimachi

Yoshihisa Kobayashi

Toshiaki Tanaka

Yoshihiko Norimine

Makoto Kotake

Taro Terauchi

Shinsuke Hirota

Yoichi Kita

Yoshimitsu Naoe

Daisuke Shinmyo

Yuji Kazuta

Daiju Hasegawa

Toshiyuki Uemura

Tamaki Hoshikawa

Nobuhiro Sato

Koji Hagiwara

Ayumi Takemura

Toru Watanabe

Kogyoku Shin

Eriko Doi

George Moniz

Huiming Zhang

Kunitoshi Takeda

Jaemoon Lee

Takafumi Motoki

Farid Benayoud

Takashi Fukuyama

Carsten T Beuckmann

Yasuaki Kamada

Toshiyuki Ohfusa

Annie Zhu Wilcoxen

Tomoyuki Shibuguchi

Takaaki Harada

Hikaru Yoshimura

Toshiki Kurokawa

Hironori Fukumoto

Taro Asaba

George Anthony Moniz

Provided are compounds represented by the following formulas (I), (II), (III) and (IV) having orexin type 2 receptor-activating activity, or their pharmaceutically acceptable salts. 

Substituted piperidine compounds and their use

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

Pentacyclic heterocycles

The present invention provides compounds represented by formulas (1) to (VI) or pharmaceutically acceptable salts thereof: 

Pentacyclic compound

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

Pyranodipyridine compound

Disclosed is a compound represented by the formula (I): or a pharmacologically acceptable salt thereof, which is effective as a therapeutic or prophylactic agent for a disease induced by A&#x3b2;, wherein Arrepresents an imidazolyl group which may be substituted with a C1-6 alkyl group, or the like; Arrepresents a phenyl group which may be substituted with a C1-6 alkoxy group, or the like; Xrepresents a double bond, or the like; and Het represents a triazolyl group or the like which may be substituted with a C1-6 alkyl group or the like, or the like.

Polycyclic compound

The present disclosure provides compounds and methods that are useful for the preparation of compounds useful as orexin-2 receptor antagonists.

Methods and compounds useful in the synthesis of orexin-2 receptor antagonists

A cyclopropane compound represented by the following formula (A) or a pharmaceutically acceptable salt thereof has orexin receptor antagonism, and therefore has a potencial of usefulness for the treatment of sleep disorder for which orexin receptor antagonism is effective, for example, insomnia: wherein Q represents &#x2014;CH&#x2014; or a nitrogen atom, Rand Reach independently represent a Calkyl group and the like, Rrepresents a hydrogen atom and the like, R, R, Rand Reach independently represent a hydrogen atom, a halogen atom, a Calkyl group and the like, R, Rand Reach independently represent a hydrogen atom, a halogen atom and the like, and Rrepresents a hydrogen atom and the like.

Cyclopropane compound

The present invention relates to a novel two cyclic cinnamide compound and a pharmaceutical agent comprising the compound as an active ingredient. The two cyclic cinnamide compound represented by the general formula (I): whereinrepresents a single bond or a double bond; Arrepresents a phenyl group or pyridinyl group that may be substituted with 1 to 3 substituents; Rand Reach represent a C1-6 alkyl group, a hydroxyl group, or the like; Zrepresents a methylene group or vinylene group, which may be substituted with 1 or 2 substituents selected from Substituent Group A1, an oxygen atom, or an imino group that may be substituted with a substituent selected from Substituent Group A1; and p, q, and r each represent an integer of 0 to 2, which has an effect of reducing A&#x3b2;40 and A&#x3b2;42 production, and thus is particularly useful as a prophylactic or therapeutic agent for a neurodegenerative disease caused by A&#x3b2; such as Alzheimer's disease or Down's syndrome.

Two cyclic cinnamide compound

A compound represented by the formula (I): or a pharmacologically acceptable salt thereof, wherein Arrepresents an imidazolyl group or the like which may be substituted with a C1-6 alkyl group, Arrepresents a phenyl group or the like which may be substituted with a C1-6 alkoxy group, Xrepresents a double bond or the like and Het represents a triazolyl group or the like which may be substituted with a C1-6 alkyl group or the like, is effective as a therapeutic or prophylactic agent for a disease caused by A&#x3b2;.

Imidazoyl pyridine compounds and salts thereof

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Tsukuba, Japan

Yu Yoshida