Ube Industries, Inc.

Santen Pharmaceutical Co., Ltd.

Santen Pharmaceuticalco., Ltd.

Takeshi Matsugi

Masahiko Hagihara

Ken-ichi Komori

Hiroshi Nishida

Kazutaka Kido

Hidetoshi Sunamoto

Tadashi Nakajima

Masakazu Hatano

Hideaki Hara

Yasunori Tsuzaki

Atsushi Shimazaki

Akira Takama

Tomokazu Fujimoto

Hisayuki Seike

Ken-Ichi Komori

A compound represented by formula (1) or salt thereof and a production intermediate thereof are created. The compound exhibited an excellent antioxidation action in a microsome lipid peroxidation measuring system using a rat liver microsome. Therefore, the compound or salt thereof is useful as an antioxidant. The present invention also provides use of a compound represented by the formula (1) or a pharmaceutically acceptable salt thereof for production of an antioxidant. 

Indazole derivative or salt thereof and production intermediate thereof, and antioxidant using same, and use of indazole derivative or salt thereof

As a result of intensive studies for the purpose of finding a new medicinal use of an indazole derivative, it was found that an indazole derivative inhibits glutamate-induced retinal neuronal cell death in rat fetal retinal neuronal cells, in other words, the indazole derivative acts directly on the retinal neuronal cells and exhibits an effect of protecting retinal neuronal cells. Accordingly, the indazole derivative is useful for the prevention or treatment of an eye disease associated with retinal neuronal cell damage or retinal damage.

Protective agent for retinal neuronal cell comprising indazole derivative as active ingredient

A method for treating a disease in which Rho kinase is involved. The method is carried out by administering to a patient in need thereof a pharmaceutically effective amount of a compound of the following formula or a pharmaceutically acceptable salt thereof: 

Methods for treating a disease in which Rho kinase is involved

An object of the present invention is to create a novel indazole derivative having a spiro ring structure in a side chain, which is useful as a pharmaceutical, and to find a new pharmacological activity of the derivative. The present invention compound is represented by the general formula [I] and has an excellent Rho kinase inhibitory activity. In the formula, the ring X represents a benzene ring or a pyridine ring; Rand Rrepresent halogen, H, OH, alkoxy, cycloalkyloxy, aryloxy, alkyl, cycloalkyl or the like; Rrepresents halogen, H or the like; Rand Rrepresent halogen, H or the like; Rand Rrepresent H, alkyl or the like; and m, n, p and q represent an integer of 0 to 3. In this connection, each group may have a substituent.

Indazole derivative having spiro ring structure in side chain

A subject of the present invention is to find utility of a combination of a Rho kinase inhibitor having a novel action and a &#x3b2;-blocker as a therapeutic agent for glaucoma. Actions of reducing intraocular pressure are complemented and/or enhanced each other by combining the Rho kinase inhibitor with the &#x3b2;-blocker. For the administration mode, each drug can be administered in combination or in mixture.

Remedy for glaucoma comprising Rho kinase inhibitor and &#x3b2;-blocker

A method for treating a disease in which Rho kinase is involved. The method is carried out by administering to a patient in need thereof a pharmaceutically effective amount of a compound of the following formula or a pharmaceutically acceptable salt thereof: wherein the ring X is a benzene ring or a pyridine ring; Rand Rare hydrogen or alkyl or together form a cycloalkene ring; Ris hydrogen, substituted alkyl, unsubstituted alkenyl, carboxyl or an ester or an amide thereof, amino or a cyano; Ris hydrogen, hydroxyl, substituted or unsubstituted alkoxy, unsubstituted alkenyloxy, unsubstituted cycloalkyloxy, substituted or unsubstituted alkyl, unsubstituted alkenyl, unsubstituted cycloalkyl, amino, substituted or unsubstituted alkylamino, nitro, cyano or a monocyclic heterocycle; and Ris a halogen atom or a hydrogen atom.

An object of the present invention is to create a novel indazole derivative useful as a drug and to find a novel pharmacological action of the derivative. The compound of the present invention is represented by the formula [I] and has an excellent Rho kinase inhibiting action. In the formula, a ring X is a benzene ring or a pyridine ring; Rand Rare H or alkyl; Rand Rare halogen, H, OH, alkoxy, alkenyloxy, alkynyloxy, cycloalkyloxy, cycloalkenyloxy, aryloxy, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, aryl, carboxy, hydrocarbonyl, alkylcarbonyl, etc.; and Ris halogen atom, H, OH, alkoxy, aryloxy, alkyl or aryl. Each group can be substituted. 

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Ikoma, Japan

Takeshi Matsugi