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：EP0399834B1公开日：19940720

摘要：B2751/Abs Compounds of formula (I) and pharmaceutically acceptable saltsthereof: (I) wherein a and b together form an -O- linkage or a bond or (when R2 ishydrogen), CH2; J is O or NH; either Y is N and R2 is hydrogen; or Y is C-R1 wherein eitherone 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 RxXwherein Rx is C1-6 alkyl, aryl orheteroaryl either of which may be optionally substituted by one, two or three of C1-4alkyl, 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 RyRzNZ- wherein Ry and Rz areindependently hydrogen or C1-6 alkyl and Z is C=O, SO or SO2; or a group (RwO)2P(O)Wwherein Rw is hydrogen or C1-6 alkyl and W is O or a bond; or R1 is a C3-8 cycloalkylgroup or a C1-6 alkyl group optionally substituted by a group which is hydroxy, C1-6alkoxy, amino optionally B2751 substituted by one or two C1-6 alkyl groups, C1-7alkanoylamino, C3-9 cycloalkyloxy or C3-9 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 selectedfrom nitro, cyano, halo, C1-3 alkylcarbonyl, methoxy or amino optionally substituted byone or two C1-6 alkyl or by C2-7 alkanoyl; or R1 and R2 together with the carbon atomsto which they are attached, form 2,1,3-oxadiazole; either one of R3 and R4 is hydrogen orC1-4 alkyl and the other is C1-4 alkyl; or R3 and R4 together are C2-5 polymethylene; R5is hydrogen, hydroxy, C1- alkoxy or C1-7 acyloxy; and R6 is hydrogen; or R5 and R6together form a bond; R7 is C1-6 alkyl or phenyl C1-4 alkyl optionally substituted in thephenyl ring by up to three moieties selected from C1-4 alkyl, C1-4 alkoxy or halo; and R8is amino, hydrogen or methyl; which are potassium channel activators, a process for theirpreparation and their pharmaceutical use.

申请人：BEECHAM GROUP PLC

地址：GB

国籍：GB

代理机构：Tocher, Pauline

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