Taisho Pharmaceutical Co., Ltd.

Takeshi Kuwada

Tsuyoshi Shibata

Masato Hayashi

Yoshinori Sekiguchi

Naoki Miyakoshi

Daisuke Wakasugi

Tomoko Ishizaka

Youichi Shimazaki

Nobutaka Hattori

Shin-ichi Shirokawa

Mitsukane Yoshinaga

Shin-Ichi Shirokawa

Nobuyuki Suzuki

Hiroshi Ohta

Takashi Adachi

Shuji Yamamoto

Taketoshi Okubo

Masato Kashimura

Toshihito Kumagai

Dai Nozawa

Takeshi Koami

Yuri Amada

Hiroaki Kamiyama

Yuri Fujisawa

The present invention provides agents for treating or preventing diseases such as mood disorder, anxiety disorder, schizophrenia, Alzheimer's disease, Parkinson's disease, Huntington's chorea, eating disorder, hypertension, gastrointestinal disease, drug addiction, epilepsy, cerebral infarction, cerebral ischemia, cerebral edema, head injury, inflammation, immune-related disease, alopecia, and so forth. Specifically, the invention provides azole derivatives represented by general formula (I), or pharmaceutically acceptable salts thereof that have an antagonistic action against the arginine-vasopressin (AVP) V1b receptor: 

Azole derivative

The present invention provides a 1,2,4-triazolone derivative represented by Formula (1A) having an antagonistic activity on the arginine-vasopressin 1b receptor or a pharmaceutically acceptable salt thereof and provides a pharmaceutical composition comprising the compound or the salt as an active ingredient, in particular, a therapeutic or preventive agent exhibiting favorable pharmacokinetics in a disease such as mood disorder, anxiety disorder, schizophrenia, Alzheimer's disease, Parkinson's disease, Huntington's chorea, eating disorder, hypertension, gastrointestinal disease, drug addiction, epilepsy, cerebral infarction, cerebral ischemia, cerebral edema, head injury, inflammation, immune-related disease, or alopecia. 

1, 2, 4-triazolone derivative and use thereof as an antagonist on the arginine-vasopressin 1B receptor

It is intended to provide a drug which is efficacious against pathological conditions relating to arginine-vasopressin V1b receptor. More particularly speaking, it is intended to provide a drug which has a therapeutic or preventive effect on depression, anxiety, Alzheimer's disease, Parkinson's disease, Huntington's chorea, eating disorders, hypertension, digestive diseases, drug addiction, epilepsy, brain infarction, brain ischemia, brain edema, head injury, inflammation, immune diseases, alopecia and so on. As the results of intensive studies, a novel 1,3-dihydro-2H-indol-2-one compound and a pyrrolidin-2-one compound fused with a heteroaromatic ring, which are highly selective antagonists of arginine-vasopressin V1b receptor, have high metabolic stabilities and show favorable brain penetration and high plasma concentrations, are found, thereby achieving the above objective.

1,3-dihydro-2H-indole-2-one compound and pyrrolidine-2-one compound fused with aromatic heterocycle

A 1,3-dihydro-2H-indol-2-one derivative expressed by Formula 1 (wherein Ris a halogen atom, a Cto Calkyl group, etc., and Ris a hydrogen atom, a halogen atom, etc., or Ris in the 6-position of the indol-2-one and Rand Rjoin together to form a Cto Calkylene group, Ris a halogen atom, a hydroxyl group, etc., and Ris a hydrogen atom, a halogen atom, a Cto Calkyl group, etc., or Ris in the 3-position of the phenyl and Rand Rjoin together to form a methylenedioxy group, Ris a hydrogen atom or a fluorine atom, Ris an ethylamino group, a dimethylamino group, etc., Ris a Cto Calkoxy group, and Ris a Cto Calkoxy group), or a pharmaceutically acceptable salt of this derivative. This is a novel compound that has antagonistic activity against an aruginine-vasopressin V1receptor.

1,3-dihydro-2H-indol-2-one derivative

There is provided a preparation process useful for an efficient synthesis of 6-O-substituted ketolide derivatives by combining a characterized step of introduction of a substituent at the 6-position by selective cleavage of a C&mdash;O bond of the cyclic acetal at the 9-position side via 6,9-cyclic acetal 5-O-desosaminyl erythronolide derivative, a step of conversion into carbonyl groups at the 9- and 3-positions, and a step of 11,12-cyclic carbamation to lead to 6-O-substituted ketolide derivatives.

Process for producing erythromycin derivative

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Tokyo, Japan

Takeshi Kuwada