发明名称 [4-(HETEROARYL) PIPERAZIN-1-YL]-(2,5-SUBSTITUTED -PHENYL)METHANONE DERIVATIVES AS GLYCINE TRANSPORTER 1 (GLYT-1) INHIBITORS FOR THE TREATMENT OF NEUROLOGICAL AND NEUROPSYCHIATRIC DISORDERS
摘要 The present invention relates to compounds of the general formula (I) wherein R1 is-OR1~,-SR1~ or is a heterocycloalkyl group; R1~ is lower alkyl, lower alkyl substituted by halogen or is -(CH2)n-cycloalkyl; R2 is-S(O)2-lower alkyl, -S(O)2NH-lower alkyl, NO2 or CN; X1 is CR3 or N; X2 is CR3~ or N; R3/R3~ are independently from each other hydrogen, halogen, lower alkyl, CN, NO2,-S(O)2-phenyl, -S(O)2-lower alkyl, -S(O)2-pyridin-2, 3 or 4-yl, phenyl, optionnally substituted by one or two substituents selected from the group consisting of NO2 or halogen, or is lower alkyl substituted by halogen or is -C(O)-lower alkyl; n is 0, 1 or 2; and to pharmaceutically acceptable acid addition salts thereof. It has been found that the compounds of general formula (I) are good inhibitors of the glycine transporter 1 (GlyT-1). They may be used in the treatment of schizophrenia.
申请公布号 CA2593463(C) 申请公布日期 2013.10.08
申请号 CA20052593463 申请日期 2005.12.28
申请人 F. HOFFMANN-LA ROCHE AG 发明人 JOLIDON, SYNESE;NARQUIZIAN, ROBERT;NORCROSS, ROGER DAVID;PINARD, EMMANUEL
分类号 C07D277/42;A61K31/496;A61P25/28;C07D277/56;C07D285/08;C07D285/135 主分类号 C07D277/42
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