Ono Pharmaceutical Co., Ltd.

Ono Pharmaceuticalco.,ltd.

Tetsuya Sekiguchi

Hiroshi Yamamoto

Atsushi Naganawa

Kensuke Kusumi

Kazuhiro Otsuki

Koji Shinozaki

Akito Kakuuchi

Shigeyuki Nonaka

Takuya Nishio

Takeshi Matsushita

Akiharu Ishida

Tatsuya Komagata

Yasuko Yamamoto

Yasuyuki Okabe

The compound of the formula (I-1): wherein all the symbols have the same meanings as described in the specification, has two cyclic groups, particularly phenoxy groups at specific substitution positions and thus has high human S1Pantagonistic activity. The compound may therefore be used as a therapeutic agent for S1P-mediated diseases such as diseases resulting from vascular constriction, fibrosis, and respiratory diseases.

Phenyl derivative

Provision of orally-available and low-toxic somatostatin receptor subtype 2 agonist. Since the compound represented by the general formula (I): wherein all symbols represent the same meanings as those described in the description, a salt thereof, an N-oxide thereof, a solvate thereof, or a prodrug thereof is non-peptidic low-molecular compound which has strong somatostatin receptor subtype 2 agonist activity, the compound is orally-available. Additionally, since the compound is low-toxic, the compound is useful for the prevention and/or treatment of the somatostatin related diseases such as acromegaly or gastrointestinal obstruction.

Compound having agonistic activity on somatostatin receptor, and use thereof for medical purposes

An object of the present invention is to provide a compound having strong human S1Pantagonistic activity in order to develop a useful medicament for therapy of a S1P-mediated disease such as a disease resulting from vascular constriction, fibrosis and respiratory disease. The compound represented by the general formula (I), wherein all the symbols have the same meanings as described in the specification, has a halogen atom or a haloalkyl group and a phenoxy group at certain substitution sites, and thus has strong human S1Pantagonistic activity. Therefore, the compound can be a therapeutic agent for a S1P-mediated disease, such as a disease resulting from vascular constriction, fibrosis and respiratory disease. 

The present invention provides a somatostatin receptor subtype 2 agonist. A disclosed compound represented by the general formula (I): wherein all symbols have the same definitions as described in the specification;a salt thereof, an N-oxide thereof or a solvate thereof, or a prodrug of the foregoing is a low-molecular compound having strong somatostatin receptor subtype 2 agonistic activity, and thus can be administered in a simple manner, has high stability and has low toxicity. Therefore, the present compound is useful for prophylaxis and/or therapy of somatostatin-related diseases such as acromegaly and gastrointestinal obstruction.

Compound having somatostatin receptor agonistic activity and pharmaceutical use thereof

Provision of orally-available and low-toxic somatostatin receptor subtype 2 agonist. Since the compound represented by the general formula (I): [wherein all symbols represent the same meanings as those described in the description] a salt thereof, an N-oxide thereof, a solvate thereof, or a prodrug thereof is non-peptidic low-molecular compound which has strong somatostatin receptor subtype 2 agonist activity, the compound is orally-available. Additionally, since the compound is low-toxic, the compound is useful for the prevention and/or treatment of the somatostatin related diseases such as acromegaly or gastrointestinal obstruction.

The compound represented by the formula (I-1): wherein all the symbols have the same meanings as described in the specification, has two cyclic groups, particularly phenoxy groups at specific substitution positions and thus has high human S1Pantagonistic activity. The compound may therefore be used as a therapeutic agent for S1P-mediated diseases such as diseases resulting from vascular constriction, fibrosis and respiratory diseases.

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Osaka, Japan

Tetsuya Sekiguchi