Taisho Pharmaceutical Co., Ltd.

Akito Yasuhara

Hiroshi Ohta

Kazunari Sakagami

Atsuro Nakazato

Tsuyoshi Shibata

Shuji Yamamoto

Kumi Abe

Xiang-Min Sun

Yuko Araki

Toshio Nakamura

Masato Hayashi

Shigeyuki Chaki

Hiroki Urabe

Seiji Masuda

Yohei Matsuda

Kanako Yamamoto

Yoshihisa Shirasaki

Minoru Moriya

Youichi Shimazaki

Kazuhide Konishi

Kumiko Okada

Hiroshi Kawamoto

Ryoko Dean

Shiho Hirota

The present invention aims to provide novel compounds of formula [I] or pharmaceutically acceptable salts thereof that are based on a glycine uptake inhibiting action and which are useful in the prevention or treatment of such diseases as schizophrenia, Alzheimer's disease, cognitive dysfunction, dementia, anxiety disorders (generalized anxiety disorder, panic disorder, obsessive-compulsive disorder, social anxiety disorder, posttraumatic stress disorder, specific phobia, acute stress disorder, etc.), depression, drug addiction, spasm, tremor, pain, and sleep disorder: 

Glycine transporter inhibiting substances

Provided is a novel compound represented by formula [I] or a pharmaceutically acceptable salt thereof having antagonistic activity against group II metabolism-type glutamic acid (m-Glu) receptors. The compound or pharmaceutically acceptable salt thereof is useful as a prophylactic or therapeutic agent for diseases such as new mood disorders (depressive and bipolar disorders), anxiety disorders (generalized anxiety disorder, panic disorder, obsessive-compulsive disorder, social anxiety disorder, post-traumatic stress disorder, specific phobias, and acute stress disorder), schizophrenia, Alzheimer's disease, cognitive dysfunction, dementia, drug dependence, convulsions, tremors, pain, sleep disorders, and the like. 

Ethinyl-pyrazole derivative

The present invention aims to provide novel compounds of formula [I] or pharmaceutically acceptable salts thereof that are based on a glycine uptake inhibiting action and which are useful in the prevention or treatment of such diseases as schizophrenia, Alzheimer's disease, cognitive dysfunction, dementia, anxiety disorders (generalized anxiety disorder, panic disorder, obsessive-compulsory disorder, social anxiety disorder, posttraumatic stress disorder, specific phobia, acute stress disorder, etc.), depression, drug addiction, spasm, tremor, and sleep disorder: 

A drug effective for the treatment and prevention of psychiatric disorders such as schizophrenia, anxiety and related ailments thereof, depression, bipolar disorder and epilepsy. The drug antagonizes the action of group II metabotropic glutamate receptors and shows high activity in oral administration A 2-amino-bicyclo[3.1.0]hexane-2,6-dicarboxylic ester derivative represented by formula [I]  [wherein R1 and R2 are identical or different, and each represents a hydrogen atom, a C1-10alkyl group or the like; X represents a hydrogen atom or a fluorine atom; Y represents &#x2014;OCHR3R4 or the like (wherein R3 and R4 are identical or different, and each represents a hydrogen atom, a C1-10alkyl group or the like; and n represents integer 1 or 2)], a pharmaceutically acceptable salt thereof or a hydrate thereof.

2-amino-bicyclo[3.1.0] hexane-2, 6-dicarboxylic ester derivative

A drug effective for the treatment and prevention of psychiatric disorders such as schizophrenia, anxiety and related ailments thereof, depression, bipolar disorder and epilepsy. The drug antagonizes the action of group II metabotropic glutamate receptors and shows high activity in oral administration. A 2-amino-bicyclo[3.1.0]hexane-2,6-dicarboxylic ester derivative represented by formula [I] 

2-amino-bicyclo[3.1.0]hexane-2, 6-dicarboxylic ester derivative

A drug effective for the treatment and prevention of psychiatric disorders such as schizophrenia, anxiety and related ailments thereof, depression, bipolar disorder and epilepsy. The drug antagonizes the action of group II metabotropic glutamate receptors and shows high activity in oral administration A 2-amino-bicyclo[3.1.0]hexane-2,6-dicarboxylic ester derivative represented by formula [I] [wherein Rand Rare identical or different, and each represents a hydrogen atom, a Calkyl group or the like; X represents a hydrogen atom or a fluorine atom; Y represents &#x2014;OCHRRor the like (wherein Rand Rare identical or different, and each represents a hydrogen atom, a Calkyl group or the like; and n represents integer 1 or 2)], a pharmaceutically acceptable salt thereof or a hydrate thereof.

2-amino-bicyclo(3.1.0) hexane-2,6-dicarboxylic ester derivative

2-amino-bicyclo (3.1.0) hexane-2,6-dicarboxylic ester derivative

2-amino-bicyclo [3.1.0] hexane-2,6-dicarboxylic ester derivative

One object of the present invention is to provide a drug that is effective in treatments for and prevention of psychiatric disorders and in treatments for and prevention of neurological diseases, inhibiting a Group II metabotropic glutamate receptor. The object is solved by a 2-amino-bicyclo[3.1.0]hexane-2,6-dicarboxylic acid derivative represented by formula [I]: (wherein Rand Rare the same or different, and each represents a hydrogen atom, Calkyl group, etc; X represents a hydrogen atom or a fluorine atom; and Y represents an amino group, &#x2014;SR, &#x2014;S(O)R, &#x2014;SCHRR, &#x2014;S(O)CHRR, &#x2014;NHCHRR, &#x2014;N(CHRR)(CHRR), &#x2014;NHCORor &#x2014;OCOR), a pharmaceutically acceptable salt thereof, or a hydrate thereof and so on.

2-Aminobicyclo[3.1.0]hexane-2,6-dicarboxylic acid derivative

An antidepressant comprising, as an active ingredient, a compound having an antagonistic effect on group II metabotropic glutamate receptors, as well as a 2-amino-3-alkoxy-6-fluoro-bicyclo[3.1.0]hexane-2,6-dicarboxylic acid derivative of Formula [I]: [wherein Rand R, which may be the same or different, each represent a hydroxyl group, a Calkoxy group, etc.; Rrepresents a Cacyl group, a Calkoxy-Cacyl group, etc.; and Rand R, which may be the same or different, each represent a hydrogen atom, a Calkyl group, etc.] or a pharmaceutically acceptable salt or hydrate thereof.

6-Fluorobicyclo[3.1.0]hexane derivatives

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Tokyo, Japan

Akito Yasuhara