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    • 9. 发明授权
    • Antipsychotic indolyl derivatives
    • 抗精神病药物吲哚衍生物
    • US06689792B2
    • 2004-02-10
    • US09976321
    • 2001-10-12
    • Michael G. KellyYoung H. Kang
    • Michael G. KellyYoung H. Kang
    • A61K31454
    • C07D209/42C07D209/08C07D209/34C07D403/12
    • Compounds of formula (1) are provided: wherein R1 and R2 are H, OH, F, Cl, Br, I, 1 to 6 carbon alkyl or alkenyl, 1 to 6 carbon alkoxy, aryl, OR5, nitro, amino, CF3 or R1 and R2 are taken together to form a fused ring at the 2,3- or 3,4-positions providing a fused phenyl group or a benzodioxane group, or a 4- or 7-substituted indole group, or a 5- or 8-substituted quinoline group; R3 represents a group selected from hydrogen, a 1 to 6 carbon alkyl, a 1 to 4 carbon alkoxy or a halogen; R4 represents a group selected from hydrogen, 1 to 6 carbon alkyl or R5; R5 is CH2Ph in which the phenyl ring can be optionally substituted by a group selected from OMe, halogen, CF3; X is selected from a group represented by C, CR4, [[CHR4]] and CHCH2; A is selected from a group represented by N, NH, CH and CH2; B is selected from a group represented by ═O, ═S, H and H2; or A and B may be concatenated together to form indole, benzimidazole, indolone or indoline moieties; or a pharmaceutically acceptable salt thereof, as well as pharmaceutical compositions and methods of treating central nervous system disorders utilizing these compounds.
    • 提供式(1)化合物:其中R 1和R 2是H,OH,F,Cl,Br,I,1至6碳烷基或烯基,1至6个碳烷氧基,芳基,OR 5,硝基,氨基,CF 3或R 1 并且R 2一起在2,3或3,4位上形成稠环,提供稠合苯基或苯并二恶烷基,或4-或7-取代的吲哚基,或5-或8-取代的吲哚基, 取代的喹啉基; R 3表示选自氢,1至6个碳烷基,1至4个碳烷氧基或卤素的基团; R 4表示选自氢,1至6个碳烷基或R 5的基团; R 5是CH 2 Ph,其中 苯环可任选被选自OMe,卤素,CF 3的基团取代; X选自C,CR 4,[[CHR]]和CHCH 2表示的基团; A选自N,NH, CH和CH 2; B选自由= O,= S,H和H 2表示的基团;或者A和B可以连接在一起形成吲哚,苯并咪唑,吲哚酮或二氢吲哚部分; 或其药学上可接受的盐,以及利用这些化合物治疗中枢神经系统疾病的药物组合物和方法。