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Novel biologically active eburnamenine derivatives, pharmaceutical compositions containing them and process for preparing same.

机译:新的具有生物活性的依伯南宁衍生物,包含它们的药物组合物及其制备方法。

摘要

PCT No. PCT/Hu93/00036 Sec. 371 Date Dec. 8, 1994 Sec. 102(e) Date Dec. 8, 1994 PCT Filed Jun. 8, 1993 PCT Pub. No. WO93/25550 PCT Pub. Date Dec. 23, 1993.The invention relates to novel eburnamenine derivatives of formula (I): IMAGE (I) wherein R1 and R2 as well as R3 and R4, independently from each other, stand for hydrogen, C2-6alkyl group, C2-6alkenyl group; or a C3-10alicyclic group involving 1 to 3 rings, and this latter group may be substituted by a C1-6alkyl or C2-6alkenyl group; or R1 and R2 and/or R3 and R4, together with the adjacent nitrogen atom and optionally with an additional oxygen or nitrogen atom, form a 4- to 6-membered, saturated or unsaturated cyclic group which may be substituted by a C1-6alkyl or C2-6alkenyl group; two of X, Y and Z are nitrogen whereas the third of them means a methine group; n is 1 or 2; W means oxygen or two hydrogen atoms; and the wavy line means alpha -/ alpha -, alpha -/ beta - or beta -/ alpha - steric position, as well as their acid addition salts and solvates. The invention further relates to pharmaceutical compositions containing the above compounds as well as a process for preparing the compounds of formula (I). The compounds of formula (I) possess antioxidant effect and therefore, they are useful for inhibiting the peroxidation of lipids occurring in mammals (including human).
机译:PCT / PCT / Hu93 / 00036号371日期1994年12月8日102(e)日期,1994年12月8日,PCT,1993年6月8日,PCT公开。 WO93 / 25550 PCT公布日期为1993年12月23日。本发明涉及式(I)的新的依伯南宁衍生物:<图像>(I)其中R 1和R 2以及R 3和R 4彼此独立地代表氢,C 2-6烷基,C 2-6烯基;或具有1至3个环的C 3-10脂环族基团,并且后者可以被C 1-6烷基或C 2-6烯基取代;或R 1和R 2和/或R 3和R 4与相邻的氮原子以及任选地与另外的氧或氮原子一起形成可以被C 1-6烷基取代的4至6元饱和或不饱和环状基团或C 2-6烯基;或X,Y和Z中的两个是氮,而第三个是次甲基。 n为1或2; W表示氧或两个氢原子;波浪线表示α-/α-,α-/β-或β-/α-空间位置,以及它们的酸加成盐和溶剂化物。本发明进一步涉及含有上述化合物的药物组合物,以及制备式(I)化合物的方法。式(I)化合物具有抗氧化作用,因此,它们可用于抑制哺乳动物(包括人)中发生的脂质的过氧化。

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