Ono Pharmaceutical Co., Ltd.

Ono Pharmaceuticals Co., Ltd.

Yoshihiko Nakai

Kaoru Kobayashi

Takayuki Maruyama

Atsushi Naganawa

Tetsuji Saito

Shinsuke Hashimoto

Kousuke Tani

Toru Maruyama

Tohru Kambe

Hideyuki Yoshida

Akio Nishiura

Toshihiko Nagase

Shinsei Fujimura

Nobutaka Abe

Kiyoto Sakata

Tetsuji Saitoh

An N-phenylarylsulfonylamide compound of formula (I) (Ris COOH etc.; Ris hydrogen, methyl, etc.; Rand Rare a combination of methyl and methyl, etc.; Ris isopropyl etc.; Ar is thiazolyl, pyridyl, 5-methyl-2-furyl each optionally substituted with methyl; n is zero or 1), a synthetic intermediate for the compound and a process for its preparation. The compound of formula (I) binds to a prostaglandin Ereceptor, especially an EPsubtype receptor, and antagonizes it. It is less affected by protein binding, so it has a satisfactory in vivo activity. Therefore, it is considered to be useful as an analgesic, an antipyretic agent, an agent for the treatment of pollakiuria (frequent urination) and/or lower urinary tract disease syndrome or an antineoplastic agent.

N-phenylarylsulfonamide compound, pharmaceutical composition comprising the compound as active ingredient, synthetic intermediate for the compound and process for its preparation

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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Mishima-gun, Japan

Yoshihiko Nakai