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5-acyl-1,4-dihydropyridines for control of disorders of CNS with modulating action on potassium channels certain such novel compounds and their preparation

机译:5-酰基-1,4-二氢吡啶类化合物,用于控制中枢神经系统疾病,具有调节钾通道的作用,某些新型化合物及其制备方法

摘要

The use of 1-alkyl-3,5-diacyl-2,6-dimethyl-6-aryl-1,4-dihydropyridines of formula (I) is claimed in the prepn. of selective potassium channel modulating medicaments for treating CNS disorders. R1 = 6-10C aryl (opt. substd. by 1-5 of NO2, CN, halogen, CF3 and 1-6C alkylthio); R2 = 1-8C alkyl, phenyl, 1-8C alkoxy or phenoxy; R3 = 1-8C alkyl or phenyl; R4 = 1-4C alkyl. The following cpds. (I) are new: 1-(5-acetyl-4-(R')-1,2,6-trimethyl-1,4-dihydropyridin-3-yl)-ethanone; and 5-acetyl-4-(R")-1,2,6-trimethyl-1,4-dihydropyridine-3-carboxylic acid methyl ester. R' = 2,4,5-, 2,3,5- or 3,4,5-trichlorophenyl, 2,3- or 3,4-dichlorophenyl, 4-chlorophenyl or 4-fluorophenyl; R" = 4-chlorophenyl, 2,3- or 3,4-dichlorophenyl, 3- or 4-nitrophenyl, 3,4,5-trifluorophenyl, 4-fluorophenyl or 4-chloro-3-trifluoromethylphenyl. The prepn. of new and known (I) is claimed (see 'Preparation').
机译:制备中要求保护式(I)的1-烷基-3,5-二酰基-2,6-二甲基-6-芳基-1,4-二氢吡啶的使用。选择性钾通道调节药物治疗中枢神经系统疾病。 R1 = 6-10C芳基(最好被NO2,CN,卤素,CF3和1-6C烷硫基的1-5取代); R2 = 1-8C烷基,苯基,1-8C烷氧基或苯氧基; R3 = 1-8C烷基或苯基; R 4 = 1-4C烷基。以下cpds。 (I)是新的:1-(5-乙酰-4-(R')-1,2,6-三甲基-1,4-二氢吡啶-3-基)-乙酮;和5-乙酰基-4-(R”)-1,2,6-三甲基-1,4-二氢吡啶-3-羧酸甲酯R'= 2,4,5-,2,3,5-或3,4,5-三氯苯基,2,3-或3,4-二氯苯基,4-氯苯基或4-氟苯基; R“ = 4-氯苯基,2,3-或3,4-二氯苯基,3-或4-硝基苯基,3,4,5-三氟苯基,4-氟苯基或4-氯-3-三氟甲基苯基。的准备。要求对新的和已知的(I)进行声明(请参阅“准备”)。

著录项

  • 公开/公告号IL116387A

    专利类型

  • 公开/公告日2000-11-21

    原文格式PDF

  • 申请/专利权人 BAYER AKTIENGESELLSCHAFT;

    申请/专利号IL19950116387

  • 发明设计人

    申请日1995-12-14

  • 分类号C07D211/90;A61K31/445;A61P25/00;

  • 国家 IL

  • 入库时间 2022-08-22 01:25:07

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