Eisai R&d Management Co., Ltd.

Kodo Shikata

Yoshinori Takahashi

Kogyoku Shin

Taro Terauchi

Kunitoshi Takeda

Minako Hashizume

Akira Inomata

Hisashi Shibata

Carsten T Beuckmann

Toru Sawai

Michiyuki Suzuki

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]

An anxiolytic drug of the invention comprises an orexin receptor antagonist, a pharmacologically acceptable salt thereof, or a solvate thereof as an active ingredient. A method for screening a compound having an anxiolytic action of the invention comprises a step of using orexin-A.

Method of screening for antianxiety drugs

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Tsukuba, Japan

Kodo Shikata