Diaryl-substituted five-membered heterocycle derivative

C - Chemistry – Metallurgy – 07 – D

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C07D 249/06 (2006.01) A61K 31/4192 (2006.01) A61K 31/427 (2006.01) A61K 31/436 (2006.01) A61K 31/437 (2006.01) A61K 31/4375 (2006.01) A61K 31/4439 (2006.01) A61K 31/4709 (2006.01) A61K 31/4725 (2006.01) A61K 31/496 (2006.01) A61K 31/498 (2006.01) A61K 31/517 (2006.01) A61K 31/5377 (2006.01) A61P 1/06 (2006.01) A61P 9/10 (2006.01) A61P 25/04 (2006.01) A61P 25/16 (2006.01) A61P 25/18 (2006.01) A61P 25/22 (2006.01) A61P 25/28 (2006.01) A61P 25/30 (2006.01) A61P 29/00 (2006.01) C07D 401/04 (2006.01) C07D 401/14

Patent

CA 2558278

A compound represented by the formula (I): [wherein X1 represents oxygen, etc.; X2 represents nitrogen, etc.; X3 represents nitrogen, etc.; X4 represents nitrogen, etc.; and R1 represents the formula (II-1): (A) ring A (wherein X5 represents sulfur, etc.; A1 represents carbon, etc.; A2 represents nitrogen, etc.; and ring A represents phenyl, etc.)] or a pharmaceutically acceptable salt of the compound. They have mGluR1 inhibitory activity and are useful in the prevention or treatment of convulsion, acute pains, inflammatory pains, chronic pains, brain disorders such as brain infarction or transient cerebral ischemic attack, mental function disorders such as schizophrenia, anxiety, drug dependence, Parkinson's disease, or gastrointestinal disorders.

Un composé représenté par la formule (I) : [dans laquelle X¿1? représente de l'oxygène, etc., X¿2? représente de l'azote, etc., X¿3? représente de l'azote, etc. et R?1¿ représente la formule (II-1) : (A) cycle A (dans laquelle X¿5? représente du soufre, etc., A¿1? représente du carbone, etc., A¿2? représente de l'azote, etc. et le cycle A représente un phényle, etc.)] ou un sel du composé pouvant être accepté en termes pharmaceutiques. Ils possèdent une activité d'inhibiteur de type mGluR1 et sont utiles dans la prévention ou le traitement des convulsions, des douleurs aiguës, des douleurs inflammatoires, des douleurs chroniques, des troubles du cerveau tels qu'un infarctus du cerveau ou une attaque ischémique cérébrale transitoire, des troubles de la fonction mentale tels que la schizophrénie, l'anxiété, la dépendance aux drogues, la maladie de Parkinson, ou des troubles gastro-intestinaux.

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