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6 - aminosubstituierte n - pyrrolyl 3 pyridazinamine, their manufacture and pharmaceutical compositions containing anti hypertensive.

机译:6-氨基取代基正吡咯基3哒嗪胺,其制造和药物组合物含有抗高血压药。

摘要

New N-pyrrolyl-3-pyridazine-amines having a further aminic substituent in the 6 position of the formula (I), CHEM wherein R, R1, R2 and R3 are hydrogen or lower alkyl, R4 is e.g. hydrogen or lower alkyl, R5 and R6 are e.g. lower alkyl or taken together with the adjacent nitrogen atom represent a saturated 5 - 6 membered heterocyclic ring which may contain a further heteroatom, R7 and R8 represent hydrogen or, taken together, a 1,3-butadienylene radical forming a benzo system fused with the pyridazine ring, for example N-2,5-dimethyl-1H-pyrrol-1-yl)- 6-morpholino-3-pyridazineamine or N-(2,5-dimethyl-1H-pyrrol- 1-yl)-4-(4-hydroxypiperidino)-1-phthalazineamine, and their pharmaceutically acceptable salts are made e.g. by contacting a hydrazino derivate of the formula (II), wherein the substituents have the same meaning as above or an acid addition salt thereof with a dicarbonyl compound of the formula (III), wherein the substituents have the same meaning as above, or a functional derivative thereof in the presence of an acid catalyst at a temperature between 15 DEG C and 120 DEG C. The new compounds can be used as antihypertensive agents.
机译:在式(I)的6位具有另一个氨基取代基的新的N-吡咯基-3-哒嗪-胺,其中R,R 1,R 2和R 3为氢或低级烷基,R 4为例如N。氢或低级烷基,R 5和R 6例如为低级烷基或与相邻的氮原子一起表示饱和的5-6元杂环,该环可含有其他杂原子,R7和R8表示氢,或与形成1,3-丁二烯基的苯并系统稠合的1,3-丁二烯基哒嗪环,例如N-2,5-二甲基-1H-吡咯-1-基)-6-吗啉代-3-哒嗪胺或N-(2,5-二甲基-1H-吡咯-1-基)-4-制备(4-羟基哌啶子基)-1-酞嗪胺及其药学上可接受的盐,例如使式(II)的肼衍生物或其酸加成盐与式(II)的肼衍生物或其酸加成盐与式(III)的二羰基化合物接触,或在15℃至120℃之间的温度下,在酸催化剂的存在下,其功能衍生物。该新化合物可用作抗高血压药。

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