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combination of substances for the treatment of hypertension and congestive heart failure. (100 - 7516)

机译:合并治疗高血压和充血性心力衰竭的物质。 (100-7516)

摘要

The potassium channel activator has the formula (I), its N-oxides, acid addition salts or quaternary ammonium salts: (A) V = C-R1; T = C-R2; W = C-H; R1 = H, Halo, -CC-, OH, CN, NR6R8, CO2R6 or CONR6R7; R2 = H, halo, 1-4C alkoxy, OH, NR6R8; R6, R7 = independently H or 1-4C alkyl; R8 = H, 1-4C alkyl, formyl, acetyl or trifluoroacetyl; or one of R1, R2 = NO2 and the other is as defined above. (B) V = N or its N-oxide; T = C = R2; W = C-H; (C) V = C-R1'; T = C-H; W = N; R1' = H, CN or NO2; (D) V = N; T = C-H; W = N; R3, R4 independently H or 1-4C alkyl or together form -(CH2)n-; where n = 2-5; R5 = H or OR8; (R8 defined above) R9, R10 = H, CH3 or together form oxo or thioxo; m = 1-3; X = O or NR11; R11 = H, 1-4C alkyl, formyl, acetyl, or CH2OH; Y = CH, C-halo, N, C-formyl or C-CH2OH; Z = CH2, O, S, CH-halo, or NR6; (R6 defined above). An example of (I) is (-)-(3S,4R)-3,4 -dihydro-3-hydroxy-2,2 -dimethyl-4-(3-oxo-1-cyclopent-1-enyloxy)-2H-1-benzopyran-6-carbonitrile; The relative amounts of (a) and (b) is 1:5 to 1:20. @(9pp Dwg.No.0/0)@.
机译:钾通道活化剂具有式(I),其N-氧化物,酸加成盐或季铵盐:(A)V = C-R1; T = C-R2; W = C-H; R1 = H,卤素,-CC-,OH,CN,NR6R8,CO2R6或CONR6R7; R2 = H,卤素,1-4C烷氧基,OH,NR6R8; R6,R7 =独立地为H或1-4C烷基; R8 = H,1-4C烷基,甲酰基,乙酰基或三氟乙酰基;或R 1,R 2 = NO 2中的一个,另一个如上所述。 (B)V = N或其N-氧化物; T = C = R2; W = C-H; (C)V = C-R1′; T = C-H; W = N; R1'= H,CN或NO2; (D)V = N; T = C-H; W = N; R3,R4独立地为H或1-4C烷基或一起形成-(CH2)n-;其中n = 2-5; R5 = H或OR8; (上面的R8定义)R9,R10 = H,CH3或一起形成氧代或硫代代; m = 1-3; X = O或NR11; R11 = H,1-4C烷基,甲酰基,乙酰基或CH 2 OH; Y = CH,C-卤代,N,C-甲酰基或C-CH2OH; Z = CH2,O,S,CH-卤代或NR6; (上面定义的R6)。 (I)的实例为(-)-(3S,4R)-3,4-二氢-3-羟基-2,2-二甲基-4-(3-氧代-1-环戊-1-烯氧基)-2H -1-苯并吡喃-6-腈; (a)和(b)的相对量为1:5至1:20。 @(9pp Dwg.No.0 / 0)@。

著录项

  • 公开/公告号IT9048106D0

    专利类型

  • 公开/公告日1990-07-03

    原文格式PDF

  • 申请/专利权人 SANDOZ AG;

    申请/专利号IT19900048106

  • 发明设计人 HOF ROBERT PAUL;QUAST ULRICH;

    申请日1990-07-03

  • 分类号53135A61KA;

  • 国家 IT

  • 入库时间 2022-08-22 06:16:51

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