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tioli as intermediate in preparation of selective agents on histamine receptors and process for the production of these tioli

机译:提奥利作为制备组胺受体选择剂的中间体,以及这些提奥利的生产方法

摘要

New furan derivs. of formula (I), and their N-oxides, hydrates and salts: (where R1 andR2 are H, lower alkyl, cycloalkyl, lower alkenyl, aralkyl, or a lower alkyl gp. interrupted by O or NR4, or NR1R2 is a heterocyclic ring opt. contg. an O atom or NR4 gp; A is 1-6C alkylene; R3 is H, lower alkyl, lower alkenyl or alkoxyalkyl; R4 is H or lower alkyl; X is CH2, O or S; Y is S, O, NR5 or CHR6; R5 is H, NO21 CN, lower alkyl, aryl, alkylsulphonyl or arylsulphonyl; R6 is NO2, arylsulphonyl or alkylsulphonyl; m = 2-4, n = 1 or 2 or can be O when X is S or CH2). (I) are histamine H2 receptor antagonists. They inhibit histamine-induced gastric hypersecretion without affecting smoth-muscle contraction induced by histamine. They can also be used to treat allergic symptoms, e.g. urticaria.
机译:新的呋喃衍生物。式(I)的式(I)及其N-氧化物,水合物和盐:(其中R 1和R 2为H,低级烷基,环烷基,低级烯基,芳烷基或低级烷基,被O或NR 4中断,或NR 1 R 2为杂环环,包括一个O原子或NR4 gp; A为1-6C亚烷基; R3为H,低级烷基,低级烯基或烷氧基烷基; R4为H或低级烷基; X为CH2,O或S; Y为S, O,NR5或CHR6; R5为H,NO21 CN,低级烷基,芳基,烷基磺酰基或芳基磺酰基; R6为NO2,芳基磺酰基或烷基磺酰基; m = 2-4,n = 1或2;或者当X为S或L时可以为O CH2)。 (I)是组胺H 2受体拮抗剂。它们抑制组胺诱导的胃分泌过多,而不影响组胺诱导的平滑肌收缩。它们也可以用于治疗过敏症状,例如。荨麻疹。

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