Santen Pharmaceutical Co., Ltd.

Ube Industries, Inc.

Asahi Glass Company, Limited

Santen Pharmaceuticalco., Ltd.

Tadashi Nakajima

Takeshi Matsugi

Masakazu Hatano

Hideaki Hara

Masahiko Hagihara

Ken-ichi Komori

Hidetoshi Sunamoto

Hiroshi Nishida

Kazutaka Kido

Takashi Nakano

Yasushi Matsumura

Yoshitomi Morizawa

Nobuaki Mori

Eiichi Shirasawa

Hideshi Sasakura

Masaaki Kageyama

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

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. 

Indazole derivatives

A fluorine-containing prostaglandin derivative of the formula (1) (or a salt thereof) and a medicine containing it, particularly, a preventive or therapeutic medicine for an eye disease: ##STR1## wherein A is a vinylene group or the like, R.sup.1 is an aryloxyalkyl group or the like, R.sup.2 and R.sup.3 are hydrogen atoms or the like, and Z is OR.sup.4 (wherein OR.sup.4 is a hydrogen atom or an alkyl group) or the like.

Difluoroprostaglandin derivatives and their use

Growing community of inventors

Ikoma, Japan

Tadashi Nakajima