Eisai R&d Management Co., Ltd.

Eisai Company, Limited

Taro Terauchi

Nobuaki Sato

Takashi Doko

Yoshimitsu Naoe

Motohiro Soejima

Norihito Ohi

Hitoshi Oinuma

Naohiro Kohmura

Hidenori Seshimo

Toshiaki Tanaka

Yoshinori Takahashi

Fumihiro Ozaki

Mitsuaki Miyamoto

Tetsuya Kawahara

Richard S Clark

Kazuo Okano

Akiharu Kajiwara

Ieharu Hishinuma

Masanobu Shinoda

Hiroshi Tanaka

Fumiyoshi Matsuura

Itaru Tsukada

Kogyoku Shin

Atsushi Kamada

Makoto Kotake

Toshiyuki Matsuoka

Yu Yoshida

Kunitoshi Takeda

Shuichi Suzuki

Yuji Kazuta

Motoji Kogushi

Osamu Ito

Akifumi Kimura

Keiichi Sorimachi

Hiroko Kobayashi

Naoto Ono

Ken-ichi Chiba

Kodo Shikata

Ayumi Takemura

Akira Inomata

Yoshiaki Oohashi

Syuhei Miyazawa

Minako Hashizume

Hachiro Sugimoto

Hisashi Shibata

Tsutomu Kawata

Naoki Asakawa

Masahiro Yonaga

George Moniz

Huiming Zhang

Jaemoon Lee

Takafumi Motoki

Farid Benayoud

Naoki Asai

Nariyasu Mano

Yukio Nishizawa

Takashi Musha

Carsten T Beuckmann

Annie Zhu Wilcoxen

Akinori Akaike

Tsutomu Kawada

Takashi Musya

Takashii Musha

Keni-Ichi Chiba

Ken-Ichi Chiba

George Anthony Moniz

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 compound represented by the formula (I) or pharmacologically acceptable salt thereof exhibits an excellent CRF receptor antagonism wherein X is a nitrogen atom or CH; Ris -A-A; Ais a single bond or a C1-6 alkylene group; Ais a hydrogen atom, a C1-6 alkyl group or a C3-6 cycloalkyl group, etc.; Ris -A-A; Ais a single bond or a C1-6 alkylene group; Ais a hydrogen atom, a C1-6 alkyl group, a C3-6 cycloalkyl group, a non-aromatic heterocyclic group, or a heteroaryl group, etc.; Ris a C1-6 alkyl group, a C3-6 cycloalkyl group, a C1-6 alkoxy group, a C3-6 cycloalkoxy C1-6 alkyl group, di-C1-6 alkyl amino group, a halogen atom, a cyano group, a formyl group, or a carboxyl group, etc; Ris a hydrogen atom or a C1-6 alkoxy group; Ris a halogen atom, a C1-6 alkyl group, or a C1-6 alkoxy group; Ris a hydrogen atom, a C1-6 alkyl group, a C1-6 alkoxy group, a C1-6 alkylthio group, or a C1-6 alkyl sulfinyl group etc.; and Ris a C1-6 alkyl group, a C1-6 alkoxy group, or a C1-6 alkylthio group.

Pyrazolothiazole compound

A compound represented by the following formula (I), or salt thereof exhibits excellent CRF receptor antagonism, and sufficient pharmacological activity, safety and pharmacokinetic properties as a drug. 

[object Object]

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 provides a novel 1H-indazole compound having an excellent JNK inhibitory action. More specifically, it provides a compound represented by the following formula, a salt thereof or a hydrate of them.  Wherein Ris a C-Caromatic cyclic hydrocarbon group etc.; R, Rand Reach independently represent a hydrogen atom, a halogen atom, a cyano group etc.; L is a single bond, or a C-Calkylene group etc.; X is a single bond, or a group represented by &#x2014;CO&#x2014;NH&#x2014; or &#x2014;NH&#x2014;CO&#x2014;, etc.; and Y is a C-Ccycloalkyl group, a C-Caromatic cyclic hydrocarbon group or a 5- to 14-membered aromatic heterocyclic group etc.

The present invention provides a novel 1H-indazole compound having an excellent JNK inhibitory action. More specifically, it provides a compound represented by the following formula, a salt thereof or a hydrate of them. Wherein Ris a C-Caromatic cyclic hydrocarbon group etc.; R, Rand Reach independently represent a hydrogen atom, a halogen atom, a cyano group etc.; L is a single bond, or a C-Calkylene group etc.; X is a single bond, or a group represented by &#x2014;CO&#x2014;NH&#x2014; or &#x2014;NH&#x2014;CO&#x2014;, etc.; and Y is a C-Ccycloalkyl group, a C-Caromatic cyclic hydrocarbon group or a 5- to 14-membered aromatic heterocyclic group etc.

1H-indazole compounds

The present invention provides a novel compound having an excellent JNK inhibitory effect. That is, it provides a compound represented by the following formula, a salt thereof or a hydrate of them. Wherein Rdesignates &#x2014;(CO)&#x2014;(NR)&#x2014;(CR&#x2550;CR)&#x2014;Ar (wherein R, Rand Reach independently designate a hydrogen atom, a halogen atom, hydroxyl group, an optionally substituted Calkyl group or the like;

Pyrazole compound and medicinal composition containing the same

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)

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 novel compound exhibiting an excellent suppressing effect to cell injury caused by radicals and neurotoxicity induced by excitatory nuerotransmitters such as glutamate. Specifically, it provides a compound represented by the following formula, a salt thereof or a hydrate of them. Wherein Z represents a bivalent organic group and the like of from 2 to 3 carbon atom(s) which may have a substituent; and Rrepresents a carboxyl group and the like.

Atisane compounds and use thereof

The present invention provides a novel 1H-indazole compound having an excellent JNK inhibitory action. More specifically, it provides a compound represented by the following formula, a salt thereof or a hydrate of them.Wherein Ris a C-Caromatic cyclic hydrocarbon group etc.; R, Rand Reach independently represent a hydrogen atom, a halogen atom, a cyano group etc.; L is a single bond, or a C-Calkylene group etc.; X is a single bond, or a group represented by &#x2014;CO&#x2014;NH&#x2014; or &#x2014;NH&#x2014;CO&#x2014;, etc.; and Y is a C-Ccycloalkyl group, a C-Caromatic cyclic hydrocarbon group or a 5- to 14-membered aromatic heterocyclic group etc.

1H-indazole compound

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Tsukuba, Japan

Taro Terauchi