Ono Pharmaceutical Co., Ltd.

Ono Pharmaceuticalco.,ltd.

Toshihiko Nagase

Atsushi Naganawa

Kaoru Kobayashi

Kousuke Tani

Toru Maruyama

Takayuki Maruyama

Tohru Kambe

Hideyuki Yoshida

Masaki Asada

Akio Nishiura

Masami Narita

Yoshihiko Nakai

Tsutomu Shiroya

Atsushi Kinoshita

Shinsei Fujimura

Nobutaka Abe

Michiaki Kadode

Kazutoyo Sato

Ken Yoshikawa

Kiyoto Sakata

Shigeki Yamamoto

A compound represented by formula (I), wherein

Phenylacetic acid compound

A medicinal composition for inhalation containing a continuous-release type prodrug of an EP2 agonist topically exhibits a prolonged bronchodilating and antiinflammatory effects. Namely, the medicinal composition for inhalation containing a continuous-release type prodrug of an EP2 agonist is useful as a safe preventive and/or a remedy for respiratory diseases (for example, asthma, pulmonary injury, pulmonary fibrosis, pulmonary emphysema, bronchitis, chronic obstructive pulmonary disease, adult respiratory distress syndrome, cystic fibrosis, pulmonary hypertension or the like) without causing any systemic effect such as lowering blood pressure. Thus, a safe and useful remedy for respiratory diseases is provided.

Medicinal composition for inhalation

The present invention relates to a carboxylic acid compound of formula (I): wherein Ris H, alkyl; m is 2, 3; n is 0-2; Ris phenyl, naphthyl, benzofuran, benzothiophene; Q is &#x2014;CH&#x2014;O-Cyc1, &#x2014;CH-Cyc2, -L-Cyc3; Rand Reach independently is hydrogen, alkyl or taken together form tetrahydro-2H-pyran; a pharmaceutically acceptable salt thereof, a method for producing a process of the preparation thereof and a pharmaceutical agent comprising the same as an active ingredient. The compound of formula (I) have an antagonizing activity against PGEreceptor, specifically EPreceptor which is subtype thereof, and are useful for the prevention and/or treatment of itching, pain, urinary disturbance or stress disease.

Carboxylic acid compounds

The pharmaceutical composition comprising the compound of the invention having 8-azaprostaglandin skeleton represented by formula (I) (wherein, all the symbols have the same meanings as that of the specification) a salt thereof, a solvate thereof or a cyclodextrin clathrate thereof, or a prodrug thereof and them as active ingredient have EPagonistic action and thus are considered useful for the prevention and/or treatment of immunological diseases, asthma, neuronal cell death, arthritis, lung failure, pulmonary fibrosis, pulmonary emphysema, bronchitis, chronic obstructive pulmonary disease, liver damage, acute hepatitis, nephritis, renal insufficiency, hypertension, myocardial ischemia, systemic inflammatory response syndrome, sepsis, hemophagous syndrome, macrophage activation syndrome, Still's disease, Kawasaki disease, burn, systemic granulomatosis, ulcerative colitis, Crohn's disease, hypercytokinemia at dialysis, multiple organ failure, shock and glaucoma, etc. Furthermore, the compounds also have an action of accelerating bone formation, so it is expected to be useful for the prevention and/or treatment of diseases associated with loss in bone mass, for example, primary osteoporosis, secondary osteoporosis, bone metastasis of cancer, hypercalcemia, Paget's disease, bone loss, osteonecrosis, bone formation after bone operation, alternative treatment for bone grafting.

8-azaprostaglandin derivatives and medical use thereof

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Osaka, Japan

Toshihiko Nagase