Ube Industries, Inc.

Santen Pharmaceutical Co., Ltd.

Santen Pharmaceuticalco., Ltd.

Hiroshi Nishida

Masahiko Hagihara

Ken-ichi Komori

Kazutaka Kido

Takeshi Matsugi

Hidetoshi Sunamoto

Tomio Kimura

Shigeru Ushiyama

Noriaki Iwase

Shigeyuki Kono

Eiji Okanari

Makoto Okudo

Tadashi Nakajima

Masaaki Matoyama

Masaaki Ito

Hideaki Hara

Masakazu Hatano

Kenji Nishikawa

Hirofumi Matsunaga

Yasunori Tsuzaki

Tomokazu Fujimoto

Atsushi Shimazaki

Akira Takama

Ken-Ichi Komori

A novel &#x3b1;-halogen-substituted thiophene compound or a pharmacologically acceptable salt thereof, which has a potent LPA receptor-antagonist activity and is useful as a medicament is provided. A compound represented by the general formula (I) wherein A represents, a phenyl ring, a thiophene ring, or an isothiazole ring; Ris the same or different, and represents a halogen atom, or a C-Calkyl group; Rrepresents a hydrogen atom, or a C-Calkyl group; p represents an integer of 0 to 5; V represents CRwherein Rrepresents a hydrogen atom, an amino group, a nitro group, or a C-Calkoxy group, or V represents a nitrogen atom; and X represents a halogen atom, or a salt thereof.

Halogen-substituted heterocyclic compound

The invention provides a novel &#x3b1;-halogen-substituted thiophene compound salt that has a potent LPA receptor antagonistic action and is useful as a medicament. The salt is represented by the general formula (I):  

Halogen-substituted heterocyclic compound salt

A novel &#x3b1;-halogen-substituted thiophene compound or a pharmacologically acceptable salt thereof, which has a potent LPA receptor-antagonist activity and is useful as a medicament is provided.

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

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 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

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Ube, Japan

Hiroshi Nishida