Astellas Pharma Gmbh

Hiroaki Hoshii

Nobuyuki Shiraishi

Yuji Kondo

Takayuki Goto

Shingo Yamasaki

Wataru Hamaguchi

Tomofumi Takuwa

Satoshi Hayashibe

Eriko Honjo

Daisuke Suzuki

Seiji Yoshimura

Noriyuki Kawano

Takanori Koike

Hideyuki Watanabe

Kazushi Watanabe

Takatoshi Kanayama

Takahiko Tobe

Ryosuke Munakata

Daisuke Sasuga

Kayoko Mihara

Hiroki Fukudome

Tomoaki Kawano

Junya Ohmori

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.

[Problem] A compound, which can be used for preventing or treating diseases, in which 11&#x3b2;-hydroxysteroid dehydrogenase type 1 (11&#x3b2;-HSD1) is concerned, in particular, diabetes, insulin resistance, dementia, schizophrenia and depression, is provided. [Means for Solution] It was found that a triazole derivative, in which one of the 3- and 5-positions of the triazole ring has (di)alkylmethyl or cycloalkyl, each of which is substituted with &#x2014;O&#x2014; (aryl or a heterocyclic group, each of which may be substituted, or lower alkylene-cycloalkyl), and the other thereof has aryl, a heterocyclic group or cycloalkyl, each of which may be substituted, or a pharmaceutically acceptable salt thereof exhibits potent 11&#x3b2;-HSD1 inhibitory action. From the above, the triazole derivative of the present invention can be used for preventing or treating diabetes, insulin resistance, dementia, schizophrenia and depression.

Triazole derivative or salt thereof

To provide a compound which is useful as an NMDA receptor antagonist. The present inventors have studied a compound having an NMDA receptor antagonistic action, and confirmed that the fused indane compound of the present invention has an excellent NMDA receptor antagonistic action, thereby completed the present invention. The fused indane compound of the present invention has an excellent NMDA receptor antagonistic action and can be used as a prophylactic and/or therapeutic agent for Alzheimer's disease, cerebrovascular dementia, Parkinson's disease, intractable depression, attention deficit hyperactivity disorder, migraines, or the like.

Fused indane compound

Provided is a compound that is an NMDA receptor antagonist having a broader safety margin, and is useful as an agent for treating or preventing Alzheimer's disease, cerebrovascular dementia, Parkinson's disease, ischemic apoplexy, or pain. A novel compound or a salt thereof, which is characterized in that it has an amino group and R(lower alkyl, cycloalkyl, -lower alkylene-aryl, aryl which may be substituted, and the like) on carbon atoms of indane, cyclopenta[b]thiophene, cyclopenta[b]furan, cyclopenta[b]pyridine, or cyclopenta[c]pyridine ring, or 2,3 -dihydro-1-benzofuran, 2,3-dihydro-1-benzothiophene, indoline ring, or the like, and has Rand R(the same or different, each lower alkyl or aryl) on carbon atoms beside them, and an NMDA receptor antagonist comprising the same as an active component.

Aminoindane derivative or salt thereof

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Tokyo, Japan

Hiroaki Hoshii