Seldar Pharma Inc.

Astellas Pharma Gmbh

Yamanouchi Pharmaceutical Company Ltd.

Tomofumi Takuwa

Norio Seki

Tsukasa Ishihara

Itsuro Shimada

Takafumi Shimizu

Kyoichi Maeno

Hiroyuki Hisamichi

Noriko Ishikawa

Makoto Takeuchi

Takayuki Goto

Yuji Kondo

Noriyuki Kawano

Wataru Hamaguchi

Nobuyuki Shiraishi

Masahiro Iwata

Hiroaki Hoshii

Eriko Honjo

Miki Kobayashi

Hiroyuki Kaizawa

Ryushi Seo

Ryota Shiraki

Issei Tsukamoto

Kiyoshi Yahiro

To provide a pharmaceutical, in particular a compound which can be used as a therapeutic agent for irritable bowel syndrome (IBS). It was found that a tetrahydroisoquinolin-1-one derivative having an amide group at the 4-position or a pharmaceutically acceptable salt thereof has an excellent bombesin 2 (BB2) receptor antagonistic action. It is also found that the tetrahydroisoquinolin-1-one derivative is highly effective on bowel movement disorders. From the above, the tetrahydroisoquinolin-1-one derivative of the present invention is useful as a therapeutic agent for diseases associated with a BB2 receptor, in particular IBS.

Tetrahydroisoquinolin-1-one derivative or salt thereof

A sulfur-containing bicyclic compound of the present invention has a PAM action of GABA. A composition containing the sulfur-containing bicyclic compound. And, a method for preventing and/or treating schizophrenia, CIAS, cognitive impairment, fragile X syndrome, autism spectrum disorder, spasticity, anxiety disorder, substance addiction, pain, fibromyalgia, or Charcot-Marie-Tooth disease by administering the sulfur-containing bicyclic compound.

Sulfur-containing bicyclic compound

A sulfur-containing bicyclic compound having a PAM action of GABA, and it use for preventing and/or treating schizophrenia, CIAS, cognitive impairment, fragile X syndrome, autism spectrum disorder, spasticity, anxiety disorder, substance addiction, pain, fibromyalgia, or Charcot-Marie-Tooth disease. A pharmaceutical composition for preventing and/or treating schizophrenia, cognitive impairment associated with schizophrenia (CIAS), cognitive impairment, fragile X syndrome, autism spectrum disorder, spasticity, anxiety disorder, substance addiction, pain, fibromyalgia, Charcot-Marie-Tooth disease, or the like, which has a positive allosteric modulator (PAM action) of GABA.

[Problems] To provide a pharmaceutical, in particular a compound which can be used as a therapeutic agent for irritable bowel syndrome (IBS). [Means for Solving Problems] It was found that a tetrahydroisoquinolin-1-one derivative having an amide group at the 4-position or a pharmaceutically acceptable salt thereof has an excellent bombesin 2 (BB2) receptor antagonistic action. It is also found that the tetrahydroisoquinolin-1-one derivative is highly effective on bowel movement disorders. From the above, the tetrahydroisoquinolin-1-one derivative of the present invention is useful as a therapeutic agent for diseases associated with a BB2 receptor, in particular IBS.

The present invention relates to a compound which is represented by the following general formula and has type 4 phosphodiesterase inhibitory action, and uses and an intermediate compound thereof. (wherein

Phenylpyridinecarbonylpiperazinederivative

2-Oxo-1,2-dihydro-1,8-naphthyridine derivatives characterized by bearing a specific substituent, &mdash;X&mdash;R , at the 3-position and a cyclic substituent, R , at the 4-position; or salts thereof. The derivatives and the salts are useful as drugs, particularly preventive or therapeutic agents for respiratory diseases related to PDE IV.

Naphthyridine derivatives

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Tokyo, Japan

Tomofumi Takuwa