首页> 外国专利> 4,6-Bis (cyclic amino)-pyrazolo/3,4-d/pyrimidine derivs - prepd by e.g. reacting 4,6 -dihalo cpds with cyclic amines

4,6-Bis (cyclic amino)-pyrazolo/3,4-d/pyrimidine derivs - prepd by e.g. reacting 4,6 -dihalo cpds with cyclic amines

机译:4,6-双(环氨基)-吡唑并/ 3,4-d /嘧啶衍生物-由例如使4,6-二卤代cpds与环胺反应

摘要

amino)-pyrazolo/3,4-d/pyrimidine derivs. of formula (I): (where R1 is H, 1-3C alkyl, or phenyl opt. substd. by halogen or OCH; R3 is H, CH3, SCH3, benzylthio, methylsulphinyl or methylsulphonyl; and R4 and R6 are pierazino (ppt. substd. in the 4-posn. by acyl, carbamoyl, benzyl, 1-3C alkyl or 1-3C hydroxyalkyl), morpholino, thiamorpholino, 1-oxido-thiomorpholino 1,1-dioxido-thiomorpholino, hydrazino or alkenediamino, these residues opt. being C-substd. by 1 or 2 1-3C alkyl gps.), e.g. 4-(1-oxido-thiamorpholino)-6-piperazino-1H-pyrazolo/3,4-d/pyridim- idine, and their physiologically tolerable acid addition salts with inorganic or organic acids are new cpds. (I) have hypotensive and, esp. antithrombotic activity. (I) exhibit strong inhibition of thrombocyte aggregation and adhesiveness, this activity being accompanied by strong hypotensive activity when the cpds. carry a piperazino gp.; when the piperazino gp. is 4-substd. by acyl or lower alkyl, the cpds. have no influence on circulation and blood pressure.
机译:氨基)-吡唑并/ 3,4-d /嘧啶衍生物。式(I)的通式:(其中R1是H,1-3C烷基或苯基,优选被卤素或OCH取代; R3是H,CH3,SCH3,苄硫基,甲基亚磺酰基或甲基磺酰基; R4和R6是吡嗪醇(ppt在4位上被酰基,氨基甲酰基,苄基,1-3C烷基或1-3C羟烷基取代),吗啉代,噻吗啉代,1-氧代-硫代吗啉代1,1,2-二氧代-硫代吗啉代,肼基或烯二氨基,这些残基(例如,以1或2个1-3C烷基gps取代C),例如4-(1-氧化-噻吗啉代)-6-哌嗪子基-1H-吡唑并/ 3,4-d /吡啶亚胺以及它们与无机或有机酸的生理上可耐受的酸加成盐是新的cpds。 (I)患有降压症,尤其是抗血栓形成活性。 (I)显示出对血小板聚集和粘附的强烈抑制,当cpds时该活性伴随着强烈的降压活性。携带piperazino GP。当piperazino GP。是4减。通过酰基或低级烷基,cpds。对血液循环和血压没有影响。

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