Ono Pharmaceutical Co., Ltd.

Ono Pharmaceuticals Co., Ltd.

Tohru Kambe

Toru Maruyama

Kousuke Tani

Shinsaku Yamane

Satoshi Nakayama

Kaoru Kobayashi

Mikio Ogawa

Tsutomu Shiroya

Kenji Sasaki

Yoshikazu Goto

Takayuki Maruyama

Hideyuki Yoshida

Akio Nishiura

Takashi Konemura

Shoji Nojima

Nobutaka Abe

Taihei Nishiyama

Toshihiko Nagase

Yoshihiko Nakai

Isamu Sugimoto

Shinsei Fujimura

Yusuke Tanaka

Hideki Moriguchi

Tatsunori Ino

Shinichiro Tsujiyama

Kiyoto Sakata

Yohei Ueda

A compound represented by general formula (I) (in the formula, all symbols are as described in the description) or a salt thereof has a potent nerve-protecting and/or -repairing activity, and therefore can be used as a therapeutic agent for neuropathy (e.g., chronic inflammatory demyelinating polyneuropathy, Guillain-Barre syndrome, periarteritis nodosa, allergic vasculitis, diabetic peripheral neuropathy, entrapment neuropathy, peripheral neuropathy associated with the administration of a chemotherapeutic drug, or peripheral neuropathy associated with Charcot-Marie-Tooth disease).

Benzene derivative

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) (in the formula, all symbols are as described in the description) or a salt thereof has a potent nerve-protecting and/or -repairing activity, and therefore can be used as a therapeutic agent for neuropathy (e.g., chronic inflammatory demyelinating polyneuropathy, Guillain-Barre syndrome, periarteritis nodosa, allergic vasculitis, diabetic peripheral neuropathy, entrapment neuropathy, peripheral neuropathy associated with the administration of a chemotherapeutic drug, or peripheral neuropathy associated with Charcot-Marie-Tooth disease). 

A method for producing a compound, such as 2-propanyl 4-{(3S,5aR,6R,7R,8aS)-6-[(1E,3R)-4-(2,5-difluorophenoxy)-3-hydroxy-1-buten-1-yl]-7-hydroxyoctahydro-2H-cyclopenta[b]oxepin-3-yl}butanoate, and a novel intermediate suitable for the method, whereby the compound can be stably supplied with a high total reaction yield, by changing the starting material and improving the metathesis reaction, asymmetric reduction reaction and the like.

Method for producing bicyclic compound

Provided is a compound which has strong intraocular pressure lowering action and has no side effect on eyes such as ocular stimulating property, humor protein rise etc. Since a compound represented by the formula (I): (wherein definition of each group is as described in the specification), or a salt thereof, a solvate thereof, or a prodrug thereof has strong 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.

Provided is a compound which has strong and sustaining intraocular pressure lowering action and, further, has no fear of side effect on eyes. Since a compound represented by the formula (I): wherein definition of each group is as described in the specification, or a salt thereof, a solvate thereof, or a prodrug thereof has strong and sustaining intraocular pressure lowering action 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 pharmaceutical composition for topical administration for prevention and/or treatment of diseases associated with decrease in bone mass comprising an EPagonist as an active ingredient. An EPagonist, in which includes a compound possessing prostaglandin skeleton as a representative, possesses promoting action on bone formation, so it is useful for prevention and/or treatment of diseases associated with decrease in bone mass (bone diseases such as primary osteoporosis, secondary osteoporosis, bone metastasis of cancer, hypercalcemia, Paget's disease, bone loss and bone necrosis, postoperative osteogenesis, alternative therapy for bone grafting).

Pharmaceutical composition for treatment of diseases associated with decrease in bone mass comprising EP4 agonist as active ingredient

An 8-azaprostaglandin represented by formula (I) (wherein all symbols have the same meanings as described in the specification), a pharmaceutically acceptable salt thereof or a cyclodextrin clathrate thereof. Since the compound represented by formula (I) binds to EP2 subtype among PGE receptor strongly, it is useful for preventive and/or treatment for immune diseases, allergic diseases, neuronal cell death, dysmenorrhea, premature birth, abortion, baldness, retinal neuropathy such as glaucoma, erectile dysfunction, arthritis, pulmonary injury, pulmonary fibrosis, pulmonary emphysema, bronchitis, chronic obstructive pulmonary disease, hepatic injury, acute hepatitis, liver cirrhosis, shock, nephritis, renal failure, circulatory diseases, systemic inflammatory response syndrome, sepsis, hemophagocytosis syndrome, macrophage activation syndrome, still disease, Kawasaki Disease, burn, systemic granuloma, ulcerative colitis, Crohn disease, hypercytokinemia at dialysis, multiple organ failure, or bone diseases etc.

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Osaka, Japan

Tohru Kambe