Ono Pharmaceutical Co., Ltd.

Tetsuo Obitsu

Tetsuji Saito

Kousuke Tani

Akio Nishiura

Yoshifumi Kagamiishi

Tomoyuki Hasegawa

Toshiaki Matsui

Hikaru Sugihara

Shinsei Fujimura

Masaki Okamoto

Hiroshi Araki

Yuichi Gemba

Yutaka Mikami

The present invention provides a compound of which active |form| is represented by a formula (A). and which can be injected into a joint cavity which is an affected part of disorders and can be accumulated in the joint cavity to exert the pharmacological effect thereof in a sustained manner, for the purpose of ameliorating cartilage disorders without developing any side effect. A compound according to the present invention, which is represented by a formula (I): (wherein all of symbols are as defined in the description), is a compound that can achieve the above-mentioned purpose. This compound does not exhibit any side effect on the cardiovascular system even when the compound is administered in an effective amount for exhibiting a cartilage regeneration activity, and is therefore extremely useful as a safe and effective preventive and/or therapeutic agent for cartilage disorders. Since a suspension produced using this compound can be injected without requiring the incision of the affected part, it can reduce the burden on patients, and is extremely useful as a medicinal agent.

Compound for treating cartilage disorders

A compound of a formula (I): wherein Rrepresents a C3-10 branched alkyl group which may be substituted; Rrepresents a hydrogen atom or a C1-4 alkyl group which may be substituted; Rrepresents a C1-4 alkyl group which may be substituted or a halogen atom; Rrepresents a C1-4 alkyl group which may be substituted; and ring 1 represents a cyclic group which has planarity and may have a substituent group, a salt thereof, an N-oxide thereof or a solvate thereof, or a prodrug thereof, is useful as a medicinal component having CRF antagonistic activity for the prevention and/or treatment of a neuropsychiatric disease, a peripheral organ disease and the like.

Bicyclic heterocyclic compound

8-(3-pentylamino)-2-methyl-3-(2-chloro-4-methoxyphenyl)-6,7-dihydro-5H-cyclopenta[d]pyrazolo[1,5-a]pyrimidine methanesulfonate of the structural formula (I) has Corticotropin Releasing Factor (CRF) antagonist activity and is useful in treating neuropsychiatric and digestive system diseases.

8-(3-pentylamino)-2-methyl-3-(2-chloro-4-methoxyphenyl)-6,7-dihydro-5H-cyclopenta[d] pyrazolo[1,5-a]pyrimidine methanesulfonate as a CRF antagonist

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Osaka, Japan

Tetsuo Obitsu