Mitsubishi Tanabe Pharma Corporation

Kureha Chemical Industry Company, Limited

Mitsubishi Pharma Corporation

Kureha Kagaku Kogyo K.k.

Kureha Kagahu Kogyo K.k.

Masanori Minoguchi

Hiroyuki Satoh

Satoru Kumazawa

Koji Teshima

Akira Nishiyama

Takanobu Kuroita

Hideki Horiuchi

Masahiro Bougauchi

Toshihiko Tanaka

Tokushi Hanano

Takayuki Ishige

Eyji Yoshida

Shinichirou Ono

Isao Ichinose

Yasunori Morio

Kouji Kanzaki

Sumie Sekiguchi

Shin-ichiro Ono

Masakazu Nakano

Shin-Ichiro Ono

Provided is an ORL-1 receptor agonist having improved bioavailability based on superior metabolic stability and strong and high selectivity, as compared to conventional compounds. A compound represented by the formula (I) wherein each symbol is as defined in the claims.

Benzimidazole compound and pharmaceutical use thereof

The present invention aims to provide a stable form of (R)-2-{3-[1-(acenaphthen-1-yl)piperidin-4-yl]-2,3-dihydro-2-oxo-benzimidazol-1-yl}-N-methylacetamide, which is free of problems of water adsorption and the like, and shows superior water solubility. The present invention provides a crystal and a salt of (R)-2-{3-[1-(acenaphthen-1-yl)piperidin-4-yl]-2,3-dihydro-2-oxo-benzimidazol-1-yl}-N-methylacetamide in a crystal form.

Benzimidazole compound in crystal form and salt thereof

The present invention has been made based on the finding that a compound acting on the ORL-1 receptor as an agonist acts as a non-photic entrainment factor, and advances the circadian rhythm phase, and provides a novel therapeutic agent for a sleep disorder such as circadian rhythm sleep disorder, more particularly, an agent for the prophylaxis and/or treatment of a sleep disorder, which contains an ORL-1 receptor agonist, and a novel compound useful as such agent for the prophylaxis and/or treatment.

Remedy for sleep disturbance

The present invention relates to a phenoxypropylamine compound of the formula (I) wherein each symbol is as defined in the specification, an optically active compound thereof or a pharmaceutically acceptable salt thereof and hydrates thereof, which simultaneously show selective affinity for and antagonistic activity against 5-HTreceptor, as well as 5-HT reuptake inhibitory activity, and can be used as antidepressants quick in expressing an anti-depressive effect.

Phenoxypropylamine compounds

Disclosed herein is a process for preparing a cis-azole derivative represented by the general formula (I) ##STR1## wherein R.sup.1 and R.sup.2 denote each a hydrogen atom or an alkyl group, R denotes a halogen atom, a nitro group, a cyano group, an alkyl group, a haloalkyl group or a phenyl group, A denotes a nitrogen atom or a methine group, and n stands for an integer of 1-5, which comprises reducing an azolylmethyloxabicyclohexane derivative represented by the general formula (VI) ##STR2## wherein R.sup.1, R.sup.2, R, A and n have the same meanings as defined above. A fungicidal composition comprising the azolylmethyloxabicyclohexane derivative represented by the above-mentioned general formula (VI) is also desclosed.

Cis-azole derivatives, intermediates thereof and fungicidal compositions

Disclosed is a 3-(unsubstituted or substituted benzyl)-1-alkyl-2-oxocyclopentane carboxylic acid alkyl ester derivative as represented by the general formula (I): ##STR1## where R.sup.1 and R.sup.2 are each a lower alkyl group;

3-(Unsubstituted or substituted benzyl)-1-alkyl-2-oxocyclopentane

Azolylmethyloxabicyclohexane derivatives and fungicidal compositions

Disclosed is a 1,3,2-dioxathiolan-S-oxide derivative as represented by the general formula (I): ##STR1## (where R.sub.1 and R.sub.2 are identical to or different from each other and each is a hydrogen atom or a lower alkyl group;

1,3,2-dioxathiolan-s-oxide derivatives, method for preparation, and use

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Tokyo, Japan

Masanori Minoguchi