申请人:Richter Gedeon Vegyeszeti Gyar Rt.
公开号:US04251658A1
公开(公告)日:1981-02-17
3-(1-Pyrazolyl)-pyridazine derivatives of the formula I, or pharmaceutically acceptable acid addition salts thereof, which decrease high blood pressure and inhibit catabolism or prostaglandins, ##STR1## wherein R.sup.1 is hydrogen or C.sub.1-4 alkyl, R.sup.2 is hydrogen, cyano, carboxyl, carbamoyl, carbaxoyl or C.sub.1-4 alkoxycarbonyl, R.sup.3 is hydrogen or chlorine or --NR.sup.4 NHR.sup.5 or NR.sup.6 R.sup.7, wherein R.sup.4 and R.sup.5 are each hydrogen or C.sub.1-4 alkyl, wherein R.sup.6 and R.sup.7 are each hydrogen or C.sub.1-5 alkyl, C.sub.1-5 hydroxyalkyl, C.sub.3-7 cycloalkyl, phenyl or benzyl, or benzyl or phenylethyl substituted with one or two chlorine atoms or methoxy groups, or a furylmethyl, pyridylmethyl, pyrrolidine or piperazine ring, or when R.sup.7 is hydrogen, R.sup.6 is --(CH.sub.2).sub.n --NR.sup.4 R.sup.5 wherein n is an integer from 1 to 3.
化合物I的3-(1-吡唑基)-吡嗪衍生物或其药学上可接受的酸加成盐,可降低高血压并抑制前列腺素的分解,式中R1为氢或C1-4烷基,R2为氢、氰、羧基、氨基甲酰基、羧甲氧基或C1-4烷氧羧基,R3为氢或氯或--NR4NHR5或NR6R7,其中R4和R5均为氢或C1-4烷基,R6和R7均为氢或C1-5烷基、C1-5羟基烷基、C3-7环烷基、苯基或苄基,或带有一个或两个氯原子或甲氧基取代的苄基或苯乙基,或为呋喃甲基、吡啶甲基、吡咯烷或哌嗪环,当R7为氢时,R6为--(CH2)n--NR4R5,其中n为1至3的整数。