Compounds of formula (I):
[wherein R1 represents a variety of aliphatic diamino or triami- no groups, a 6- or 7- membered heterocyclic ring containing two nitrogens, one of which is optionally substituted or a tetrahydro-1,4-thiazin-4-yl group; R2 represents an optionally mono- or di- alkyl-substituted amino group, a mono- or di-(2-hydroxyethyl)-substituted amino group or an optionally mono- or di- alkyl-substituted aminoethylamino group; and R3 and R4 each represents hydrogen or C1-C4 alkyl or together represent tri- to penta- methylene] and salts thereof may be prepared by reacting an equivalent compound, but in which the groups R1 and R2 are replaced by leaving groups, with compounds R'H (in which free amino groups are optionally protected) and R2H. Various of the compounds have one or more of the following activities: hypoglycaemic activity; the ability to inhibit aggregation of blood platelets; hypotensive activity; or diuretic activity. They can be used in the treatment or prophylaxis of thrombosis, hyperglycaemia, hypertension or oedema and may be formulated as compositions with conventional pharmaceutical carriers or diluents.
式(I)化合物:
[其中 R1 代表各种
脂肪族二
氨基或三
氨基、含有两个硝基(其中一个被任选取代)的 6-或 7-成员杂环或四
氢-1,4-
噻嗪-4-基;R2 代表任选的单-或二-烷基取代的
氨基、单-或二-(2-羟乙基)取代的
氨基或任选的单-或二-烷基取代的
氨基乙
氨基;R3和R4各自代表
氢或C1-C4烷基,或共同代表三亚
甲基至
五亚甲基]及其盐类可通过将等效化合物(但其中基团R1和R2被离去基团取代)与化合物R'H(其中游离
氨基可任选被保护)和R2H反应制备。这些化合物具有以下一种或多种活性:降血糖活性;抑制血小板聚集的能力;降血压活性;或利尿活性。它们可用于治疗或预防血栓形成、高血糖、高血压或
水肿,并可与常规药物载体或稀释剂配制成组合物。