Taisho Pharmaceutical Co., Ltd.

Kazunari Sakagami

Atsuro Nakazato

Hiroshi Ohta

Akito Yasuhara

Toshihito Kumagai

Kazuyuki Tomisawa

Tsuyoshi Shibata

Shuji Yamamoto

Takeo Taguchi

Xiang-Min Sun

Yuko Araki

Kumi Abe

Toshio Nakamura

Masato Hayashi

Shigeyuki Chaki

Hiroki Urabe

Seiji Masuda

Yohei Matsuda

Kanako Yamamoto

Norikazu Otake

Yoshihisa Shirasaki

Naoki Miyakoshi

Kosuke Kanuma

Minoru Moriya

Youichi Shimazaki

Takashi Hashihayata

Kazuhide Konishi

Kumiko Okada

Hiroshi Kawamoto

Ryoko Dean

Shiho Hirota

Hisanako Ito

Hisanaka Ito

Provided are a fluorine-containing amino acid prodrug represented by general formula (I) that makes a fluorine-containing amino acid which is a group 2 metabotropic glutamate receptor agonist into a prodrug, or a pharmaceutically acceptable salt thereof. More specifically, provided is a prodrug that increases the in vivo exposure and enhances the oral absorbability and other mucosal absorbability of a parent compound that acts on group 2 metabotropic glutamate receptors as an agent for the treatment or prevention of diseases in which group 2 metabotropic glutamate receptors are said to be involved, such as: schizophrenia, anxiety disorder and its related diseases, depression, bipolar disorder, epilepsy, developmental disorders, sleep disorders, and other neuropsychiatric diseases; and drug dependence, cognitive disorders, Alzheimer's disease, Huntington's chorea, Parkinson's disease, movement disorders associated with muscular rigidity, cerebral ischemia, cerebral insufficiency, spinal cord disorders, cephalopathy, and other neurological diseases. 

Prodrug of fluorine-containing amino acid

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

Intermediate and process for producing fluorinated carboxylic acid derivative from the same

Dicarboxylic acid derivatives

Carboxylic acid derivatives and process for producing the same

Carboxylic acid derivatives and process for producing same

Growing community of inventors

Tokyo, Japan

Kazunari Sakagami