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Triazole derivatives
专利权人:
エフ.ホフマン-ラ ロシュ アーゲー
发明人:
ヘナー,マリウス,ヴィッヒマン,ユルゲン
申请号:
JP2018517504
公开号:
JP2018531253A6
申请日:
2016.10.04
申请国别(地区):
JP
年份:
2018
代理人:
摘要:
The present invention relates to compounds of formula I It is methyl that wherein R1, which is CH3 R1, ethyl, CF3, CH2OH, cyclopropyl or containing cyanogen or R1 and R1 can be formed together a l, l- dioxo-tetrahydros-thiophene -3-yl rings R is hydrogen, methyl, ethyl, isopropyl, tertiary butyl, cyclopropyl, hydroxmethyl or 2 propyl -2-ol RJ is CI, F, CF3, containing cyanogen, methyl, methoxyl group, isopropyl or cyclopropyl R4 is hydrogen, methyl, F or CI Or to a pharmaceutically acceptable salt or acid addition salt, a kind of racemic mixture is arrived, or to its corresponding enantiomer and/or optical isomer and/or its stereoisomer. Compounds of formula I can be used for psychiatric disorders, such as the treatment of schizophrenia, bipolar disorder, obsessional neurosis or autistic spectrum disorder. It has surprisingly been found that I is the compound of structure shown in the general formula of EAAT3 inhibitor. Excitatory amino acid transporter 3 (EAAT3), it is equally referred in the research mankind as solute carrier family 1, component 1 (systematic Gene Name: SLC1A1) and in rodent be used as excitatory amino acid bracket 1 (EAAC1), it is through crust and the high-affinity anionic amino acid conveyer found in neuron in hippocampus, basal ganglion (corpus straitum, thalamus) and olfactory bulb. EAAT3 is run with the aminoglutaric acid concentration local in excitatory synapse buffering,
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