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1,2,4 - triazole derivatives, their production and their use in the treatment of high blood pressure or respiratory disease.

机译:1,2,4-三唑衍生物,其生产及其在治疗高血压或呼吸道疾病中的用途。

摘要

Compounds of formula (I) and pharmaceutically acceptable salts thereof: CHEM 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 RxX-wherein Rx is C1-6 alkyl, aryl or heteroaryl either of which may be optionally substituted by one, two or three of C1-4 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 RyRzNZ- wherein Ry and Rz are independently hydrogen or C1-6 alkyl and Z is C=O, SO or SO2; or a group (RwO)2P(O)W wherein Rw is hydrogen or C1-6 alkyl and W is O or a bond; or R1 is a C3-8 cycloalkyl group or 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, C3-8 cycloalkyloxy 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 are attached, form 2,1,3-oxadiazole; either one of R3 and R4 is hydrogen or C1-4 alkyl and the other 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 a bond; R7 is C1-6 alkyl or phenyl C1-4 alkyl optionally substituted in the phenyl ring by up to three moieties selected from C1-4 alkyl, C1-4 alkoxy or halo; and R8 is amino, hydrogen or methyl; which are potassium channel activators, a process for their preparation and their pharmaceutical use.
机译:式(I)的化合物及其药学上可接受的盐:其中R1和R2中的一个是氢,另一个是硝基,氰基,卤素,CF3 C2F5,甲酰基,醛肟,CF3O,NO2-CH = CH- NC-CH = CH-; RxX基团,其中Rx是C1-6烷基,芳基或杂芳基,它们中的任一个可以任选地被C1-4烷基,C1-4烷氧基,硝基,卤素,CF3和氰基中的一个,两个或三个取代;并且x是C = O,OC = O,C = OO,CHOH,SO,SO2,O.SO,O.SO2,CONH,O.CONH,C = S,OC = S,C = SO,CH.SH ,SONH,SO2NH,O.SONH,O.SO2NH,CO-CH = CH,C = NHOH,C = NNH2;或基团RyRzNZ-,其中Ry和Rz独立地是氢或C1-6烷基,并且Z是C = O,SO或SO2;或基团(RwO)2 P(O)W,其中R w为氢或C 1-6烷基,W为O或键。或R 1为C 3-8环烷基或C 1-6烷基,其任选地被羟基取代,C 1-6烷氧基,氨基,任选地被一个或两个C 1-6烷基取代,C 1-7烷酰基氨基,C 3- 8个环烷氧基或C3-8环烷基氨基; R 2为氢;或R 1和R 2之一是硝基,氰基或C 1-3烷基羰基,另一个是选自硝基,氰基,卤素,C 1-3烷基羰基,甲氧基或氨基的不同基团,其任选地被一个或两个C 1-6烷基或被C 2-7烷酰基; R1和R2与它们所连接的碳原子一起形成2,1,3-恶二唑; R3和R4之一是氢或C1-4烷基,另一个是C1-4烷基。 R3和R4一起是C2-5聚亚甲基;或R 5是氢,羟基,C 1-6烷氧基或C 1-7酰氧基; R6是氢; R5和R6一起形成键;或R 7是C 1-6烷基或苯基C 1-4烷基,在苯环中任选被至多三个选自C 1-4烷基,C 1-4烷氧基或卤素的部分取代; R8是氨基,氢或甲基;它们是钾通道激活剂,其制备方法及其药物用途。

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