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3-INDOLINE DERIVATIVES USEFUL IN THE TREATMENT OF PSYCHIATRIC AND NEUROLOGIC DISORDERS
3-INDOLINE DERIVATIVES USEFUL IN THE TREATMENT OF PSYCHIATRIC AND NEUROLOGIC DISORDERS
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机译:3-吲哚衍生物可用于治疗精神病和神经病
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摘要
The present invention relates to novel 3-indoline derivatives of dopamine D4 receptors. The compounds according to the invention can be used to treat certain psychiatric and neurological disorders, especially various psychoses. The compounds of the invention also exhibit affinity for the 5-HT 2A receptors. In the compounds of the present invention, R1 is acyl, thioacyl or trifluoromethylsulfonyl or R12SO2-, R12OCO or R12SCO-, wherein R12 is alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl or aryl, or R13R14NCO. or R13R14NCS-, and in the latter two, R13 and R14 are independently hydrogen or alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl or aryl, or R13 and R14 together form a pyrrolidinyl, piperidinyl or perhydroazepinyl group with the nitrogen atom to which they are attached. They are attached; n is an integer from 1 to 6; X is a vagymetine group of a carbon or nitrogen atom, and the dotted line starting from X is a bond when X is a carbon atom or a bond, when X is a nitrogen atom or a methine group; R ', R 1 and R 2 are independently hydrogen or alkyl optionally substituted by halogen; and R3-R11 are independently hydrogen or halogen or cyano, nitro, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, amino, alkylamino, dialkylamino, alkylcarbonyl, aminocarbonyl, alkylaminocarbonyl, dialkylaminocarbonyl , alkoxy, alkylthio, alkylsulfonyl, hydroxy, trifluoromethyl or trifluoromethylsulfonyl.
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机译:本发明涉及多巴胺D4受体的新型3-二氢吲哚衍生物。根据本发明的化合物可以用于治疗某些精神病和神经病,尤其是各种精神病。本发明的化合物还显示出对5-HT 2A受体的亲和力。在本发明的化合物中,R 1为酰基,硫代酰基或三氟甲基磺酰基或R 12 SO 2,R 12 OCO或R 12 SCO-,其中R 12为烷基,烯基,炔基,环烷基,环烷基烷基或芳基,或R 13 R 14 NCO。在后两个中,R13和R14独立地是氢或烷基,烯基,炔基,环烷基,环烷基烷基或芳基,或R13和R14一起与它们所组成的氮原子一起形成吡咯烷基,哌啶基或全氢a庚烯基附上。它们已连接; n为1至6的整数; X为碳或氮原子的迷迭香基,当X为碳原子或亚甲基时,以X为起点的点为键。 R',R 1和R 2独立地是氢或任选地被卤素取代的烷基; R 3和R 3 -R 11独立地是氢或卤素或氰基,硝基,烷基,烯基,炔基,环烷基,环烷基烷基,氨基,烷基氨基,二烷基氨基,烷基羰基,氨基羰基,烷基氨基羰基,二烷基氨基羰基,烷氧基,烷硫基,烷基磺酰基,羟基,三氟甲基或三氟甲基磺酰基。
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