Ono Pharmaceutical Co., Ltd.

Ono Pharmaceuticals Co., Ltd.

Ono Pharmaceuticalco.,ltd.

Kousuke Tani

Toru Maruyama

Tohru Kambe

Shinsaku Yamane

Kaoru Kobayashi

Masaki Asada

Satoshi Nakayama

Mikio Ogawa

Satonori Higuchi

Masaya Hirobe

Shuichi Ohuchida

Hirotsugu Takano

Tohru Kotani

Kazuhiro Fuchibe

Tsutomu Shiroya

Ryo Oikawa

Takayuki Maruyama

Masami Narita

Yoshikazu Goto

Akio Nishiura

Toshihiko Nagase

Toshihide Watanabe

Seiji Ogawa

Isamu Sugimoto

Shinsei Fujimura

Kazumi Moriyuki

Koji Yoshida

Shiro Shibayama

Hideyuki Yoshida

Hiroshi Ochiai

Akihiro Kinoshita

Maki Iwahashi

Tetsuya Sugiyama

Masahiko Terakado

Yoshihiko Nakai

Tetsuo Obitsu

Takahiro Nekado

Atsushi Shimabukuro

Keisuke Hanada

Nobutaka Abe

Hikaru Sugihara

Miki Kasano

Shigeki Yamamoto

Michiaki Kadode

Yoshiyuki Aratani

Kiyoto Sakata

A medicinal agent for the prevention and/or treatment of diseases caused by EPreceptor activation is disclosed. A compound having antagonistic activity against the EPreceptor is contained as an active ingredient in the medicinal agent. The compound represented by the following general formula (I) as defined in the specification, a salt, an N-oxide, or a solvate thereof, or a prodrug of these is useful as a medicinal component having antagonistic activity against the EPreceptor for the prevention and/or treatment of diseases caused by EPreceptor activation.

Tricyclic spiro compound

Since a compound represented by the general formula (I) (wherein definition of each group is as described in the specification), a salt thereof, a solvate thereof, or a prodrug thereof has strong and sustaining intraocular pressure lowering activity and, further, has no side effect on eyes such as ocular stimulating property (hyperemia, corneal clouding etc.), aqueous humor protein rise etc., it has high safety, and can be an excellent agent for preventing and/or treating glaucoma etc.

Bicyclic compound and use thereof for medical purposes

Since a compound represented by the general formula (I) (wherein definition of each group is as described in the specification), a salt thereof, a solvate thereof, or a prodrug thereof has strong and sustaining intraocular pressure lowering activity and, further, has no side effect on eyes such as ocular stimulating property (hyperemia, corneal clouding etc.), aqueous humor protein rise etc., it has high safety, and can be an excellent agent for preventing and/or treating glaucoma etc. 

A compound represented by general formula (I): (wherein in the formula, all the symbols have the same meanings as those described in the specification), or a pharmaceutically acceptable salt thereof is useful as a medicament's active ingredient having an EPreceptor antagonistic activity, in preventing and/or treating disease caused by activation of an EPreceptor.

EP4 antagonist

A medicinal agent for the prevention and/or treatment of diseases caused by EPreceptor activation is disclosed. A compound having antagonistic activity against the EPreceptor is contained as an active ingredient in the medicinal agent. The compound represented by the following general formula (I) as defined in the specification, a salt, an N-oxide, or a solvate thereof, or a prodrug of these is useful as a medicinal component having antagonistic activity against the EPreceptor for the prevention and/or treatment of diseases caused by EPreceptor activation. 

A medicinal agent for the prevention and/or treatment of diseases caused by EPreceptor activation. A compound having antagonistic activity against the EPreceptor is contained as an active ingredient in the medicinal agent. The compound represented by the following general formula (I) as defined in the specification, a salt, an N-oxide, or a solvate thereof, or a prodrug of these is useful as a medicinal component having antagonistic activity against the EPreceptor for the prevention and/or treatment of diseases caused by EPreceptor activation. 

Provided is an EP2 agonist having excellent safety. A compound represented by general formula (I) (wherein all symbols are as defined in the description), a salt or N-oxide of the compound, or a solvate or prodrug of the compound or the salt or N-oxide has an EP2 agonist activity and is highly safe, and is therefore useful as a medicine, particularly a therapeutic agent for diseases associated with EP2 receptors, such as immune diseases, allergic diseases, neuronal death, dysmenorrhea, premature birth, miscarriage, baldness, ocular diseases, erectile dysfunction, arthritis, lung injury, pulmonary fibrosis, pulmonary emphysema, bronchitis, chronic obstructive pulmonary disease, bone diseases and cartilage injury.

Compound having EP2 agonist activity

A compound represented by general formula (I) wherein all symbols are as defined in the specification, a salt or N-oxide of the compound, or a solvate or prodrug of the compound or the salt or N-oxide has a selective EP2 agonist activity and is highly safe, and is therefore useful as a drug, especially as a therapeutic agent for EP2 receptor-related diseases including immune diseases, allergic diseases, neuronal death, dysmenorrhea, premature birth, miscarriage, baldness, ocular diseases, erectile dysfunction, arthritis, lung injury, pulmonary fibrosis, pulmonary emphysema, bronchitis, chronic obstructive pulmonary disease, bone diseases, cartilage injury and others. 

Compound having selective EP2 agonist activity

The present invention provides a compound having ALXR agonist activity. Specifically, the invention provides a compound having ALXR agonist activity represented by general formula (I) wherein all the symbols are as defined in the specification, a salt thereof, a solvate thereof, or a prodrug thereof as well as an agent containing the same as an active ingredient for preventing and/or treating an ALXR-associated disease, such as an inflammatory bowel disease, an autoimmune disease, a chronic inflammatory disease, asthma, pulmonary fibrosis, atopic dermatitis, ischemia-reperfusion injury, myocardial infarction, or Alzheimer's disease. 

ALXR agonist compound

A compound that can be a therapeutic agent for underactive bladder which has low risk of side effects and can be administered orally is provided. Furthermore, a crystal which is advantageous in view of the stability, long-term storage, handleability, easiness of the drug preparation or the like as a drug substance of medicaments is provided. Since a salt of 2-[(2-{(1R,5R)-2-oxo-5-[(1E,4S)-7,8,8-trifluoro-4-hydroxy-4-methyl-1,7-octadien-1-yl]cyclopentyl}ethyl)thio]-1,3-thiazole-4-carboxylic acid or a diastereomeric mixture thereof and 4-piperidinemethanol is a chemically very stable crystal, it can be stored for a long time, and is very useful as a drug substance of medicaments.

Amine salt and crystals thereof

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Osaka, Japan

Kousuke Tani