首页> 外国专利> Innovative compounds that are potent inhibitors of the + / ca2 + exchange mechanism and are useful in the treatment of arrhythmias.

Innovative compounds that are potent inhibitors of the + / ca2 + exchange mechanism and are useful in the treatment of arrhythmias.

机译:是+ / ca2 +交换机制的有效抑制剂的创新化合物,可用于治疗心律不齐。

摘要

"INNOVATIVE COMPOUNDS THAT ARE POWERFUL INHIBITORS OF THE ^ + ^ / Ca ^ 2 + ^ EXCHANGE MECHANISM AND ARE USEFUL IN ARRYTHMA TREATMENT" Therapeutically active compounds of formula (I) are described: where X is -O-, -CH-2 ~ - or -C (O) -; Z is - CHR ~ 9 ~ - or valence bond; Y is -CH ~ 2 ~ -, -C (O) -, CH (OR ~ 10 ~) -, -CH (NR ~ 11R ~ 12 ~) -, -O-, -S-, -S (O) - or -S (O ~ 2 ~) -, provided that when Z is a valence bond, Y is not C (O); the dotted line represents an optional double bond, in which case Z is -CR ~ 9 ~ - and Y is -CH-, C (OR ~ 10 ~) -, or -C (NR ~ 11 ~ R ~ 12 ~) - ; R ~ 1 ~ is - (CH ~ 2 ~) ~ n ~ NR ~ 4 ~ R ~ 7 ~ or one of the following groups: n is 1 - 4, R ~ 2 ~ and R ~ 3 ~ are independently H, lower alkyl , lower alkoxy, -NO ~ 2 ~, halogen, -CF ~ 3 ~, -OH, -NHR ~ 8 ~ or -COOH, R @ 4 and R @ 7 ~ are independently H, lower alkyl or hydroxy-lower alkyl R5 is H, lower alkoxy, -CF3-, -NH2- or -CN; R ~ 6 ~ is -NO ~ 2 ~, -NR ~ 14 ~ R ~ 19 ~, -CF ~ 3 ~ or R ~ 8 ~ and R ~ 16 ~ are independently H or acyl, R ~ 9 ~ is H or alkyl lower, R10 is H, alkylsulfonyl or acyl; R 11 and R 12 are independently H, lower alkyl or acyl, R 13 and R 18 are independently H or -OR 20, R 14 and R 19 are independently H, acyl, alkylsulfonyl, C (S) NHR ~ 17 ~ or C (O) NHR ~ 17 ~, R ~ 15 ~ is H or NH ~ 2 ~, R ~ 17 ~ is H or lower alkyl, R ~ 20 ~ is H or acyl, and its salts and esters for pharmaceutical purposes. The compounds are potent inhibitors of the Na ^ + ^ / Ca ^ 2 + ^ exchange mechanism.
机译:“是^ + ^ / Ca ^ 2 + ^交换机制的强抑制剂并且可用于红斑病治疗的创新化合物”描述了式(I)的治疗活性化合物:其中X为-O-,-CH-2〜 -或-C(O)-; Z为-CHR〜9〜-或价键; Y是-CH〜2〜-,-C(O)-,CH(OR〜10〜)-,-CH(NR〜11R〜12〜)-,-O-,-S-,-S(O) -或-S(O〜2〜)-,当Z为价键时,Y不是C(O);虚线表示可选的双键,在这种情况下,Z为-CR〜9〜-,Y为-CH-,C(OR〜10〜)-或-C(NR〜11〜R〜12〜)- ; R〜1〜为-(CH〜2〜)〜n〜NR〜4〜R〜7〜或下列基团之一:n为1-4,R〜2〜和R〜3〜独立为H,较低烷基,低级烷氧基,-NO〜2〜,卤素,-CF〜3〜,-OH,-NHR〜8〜或-COOH,R 4和R 7〜独立地为H,低级烷基或羟基-低级烷基R5为H,低级烷氧基,-CF3-,-NH2-或-CN; R〜6〜为-NO〜2〜,-NR〜14〜R〜19〜,-CF〜3〜或R〜8〜和R〜16〜独立为H或酰基,R〜9〜为H或烷基较低的R 10为H,烷基磺酰基或酰基; R 11和R 12独立地为H,低级烷基或酰基,R 13和R 18独立地为H或-OR 20,R 14和R 19独立地为H,酰基,烷基磺酰基,C(S)NHR〜17〜或C (O)NHR〜17〜,R〜15〜是H或NH〜2〜,R〜17〜是H或低级烷基,R〜20〜是H或酰基,及其盐和酯类用于医药目的。这些化合物是Na ^ + ^ / Ca ^ 2 + ^交换机制的有效抑制剂。

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