1,2,4-Triazole derivatives, their preparation and

专利名称：1,2,4-Triazole derivatives, their preparation

and their use for treating hypertension orrespiratory tract disorders

发明人：Stemp, Geoffrey, Beecham

pharmaceuticals,Burrell, Gordon

申请号：EP90305690.1申请日：19900524公开号：EP0399834A3公开日：19910717

摘要：Compounds of formula (I) and pharmaceutically acceptable salts thereof:wherein either one of R₁ and R₂ is hydrogen and the other is nitro, cyano, halo, CF₃ C₂F₅,formyl, aldoxime, CF₃O, NO₂-CH=CH-, NC-CH=CH-; a group RX-wherein R is C₁₋₆ alkyl,aryl or heteroaryl either of which may be optionally substituted by one, two or three ofC₁₋₄ alkyl, C₁₋₄ alkoxy, nitro, halo, CF₃ and cyano; and x is C=O, O.C=O, C=O.O, CHOH, SO,SO₂, O.SO, O.SO₂, CONH, O.CONH, C=S, O.C=S, C=S.O, CH.SH, SONH, SO₂NH, O.SONH,O.SO₂NH, CO-CH=CH, C=NHOH, C=NNH₂; or a group RRNZ- wherein R and R areindependently hydrogen or C₁₋₆ alkyl and Z is C=O, SO or SO₂; or a group (RO)₂P(O)Wwherein R is hydrogen or C₁₋₆ alkyl and W is O or a bond; or R₁ is a C₃₋₈ cycloalkyl groupor a C₁₋₆ alkyl group optionally substituted by a group which is hydroxy, C₁₋₆ alkoxy,amino optionally substituted by one or two C₁₋₆ alkyl groups, C₁₋₇ alkanoylamino, C₃₋₈cycloalkyloxy or C₃₋₈ cycloalkylamino; and R₂ is hydrogen; or one of R₁ and R₂ is nitro,cyano or C₁₋₃ alkylcarbonyl and the other is a different group selected from nitro, cyano,halo, C₁₋₃ alkylcarbonyl, methoxy or amino optionally substituted by one or two C₁₋₆

alkyl or by C₂₋₇ alkanoyl; or R₁ and R₂ together with the carbon atoms to which they areattached, form 2,1,3-oxadiazole; either one of R₃ and R₄ is hydrogen or C₁₋₄ alkyl and theother is C₁₋₄ alkyl; or R₃ and R₄ together are C₂₋₅ polymethylene; R₅ is hydrogen,hydroxy, C₁₋₆ alkoxy or C₁₋₇ acyloxy; and R₆ is hydrogen; or R₅ and R₆ together form abond; R₇ is C₁₋₆ alkyl or phenyl C₁₋₄ alkyl optionally substituted in the phenyl ring by upto three moieties selected from C₁₋₄ alkyl, C₁₋₄ alkoxy or halo; and R₈ is amino, hydrogenor methyl; which are potassium channel activators, a process for their preparation andtheir pharmaceutical use.

申请人：Beecham Group p.l.c.

地址：SB House Great West Road Brentford Middlesex TW8 9BD GB

国籍：GB

代理机构：Tocher, Pauline

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