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Pyridine substituted by isopentenamide and arolamine as Glyt-1 inhibitors
专利权人:
F. HOFFMANN-LA ROCHE AG
发明人:
KOLCZEWSKI SABINE,PINARD EMMANUEL,STALDER HENRI
申请号:
PE2011001308
公开号:
PE20120500A1
申请日:
2010.01.19
申请国别(地区):
PE
年份:
2012
代理人:
摘要:
A compound made from a derivative of methyleneglycol (I),Among them, R1 is h, C1-C7 (CH2) n-cho, among others; R2 is h, halogen, oh, C1-C7 tar; AR is arilo or alternative heterosexual, replacing with halide, C1-C7 tar, c1oxy C1-C7 tar; R is C1-C7, C3-C7, arilo et al; n is 0, 1, 2 or 3. The most popular compounds are: rac-2-fluoro-n (1-methyl-3-phenyl-piperidin-3-il) - 4,6-difluoromethyl-phenyltriphenylaniline, rac-2-methyl-n - (1-methyl-3-phenyl-piperidin-3-il) - 4,6There are others A preparation procedure and a drug synthesis were also mentioned. These compounds are inhibitors of glycerol-1 (Glyt-1), which can be used to treat psychosis, pain, schizophrenia, attention deficit, Alzheimer's disease and so on.REFERIDA A UN COMPUESTO DERIVADO DE PIPERIDINA DE FORMULA (I), DONDE R1 ES H, ALQUILO C1-C7, (CH2)n-CHO, ENTRE OTROS; R2 ES H, HALOGENO, OH, ALQUILO C1-C7, ENTRE OTROS; Ar ES ARILO O HETEROARILO OPCIONALMENTE SUSTITUIDOS CON HALOGENO, ALQUILO C1-C7, ALCOXI C1-C7, ENTRE OTROS; R ES ALQUILO C1-C7, CICLOALQUILO C3-C7, ARILO, ENTRE OTROS; n ES 0, 1, 2 O 3. SON COMPUESTOS PREFERIDOS: RAC-2-FLUOR-N-(1-METIL-3-FENIL-PIPERIDIN-3-IL)-4,6-BIS-TRIFLUORMETIL-BENZAMIDA, RAC-2-METOXI-N-(1-METIL-3-FENIL-PIPERIDIN-3-IL)-4,6-BIS-TRIFLUORMETIL-BENZAMIDA, RAC-2-ETIL-N-(1-METIL-3-FENIL-PIPERIDIN-3-IL)-4,6-BIS-TRIFLUORMETIL-BENZAMIDA, ENTRE OTROS. TAMBIEN ESTA REFERIDA A UN PROCEDIMIENTO DE PREPARACION Y A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON INHIBIDORES DEL TRANSPORTADOR DE GLICINA 1 (GLYT-1) Y SON UTILES EN EL TRATAMIENTO DE LA PSICOSIS, DOLOR, ESQUIZOFRENIA, DEFICIT DE ATENCION, ENFERMEDAD DE ALZHEIMER, ENTRE OTROS
来源网站:
中国工程科技知识中心
来源网址:
http://www.ckcest.cn/home/

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