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    • 6. 发明申请
    • NOVEL STEROIDS WITH PREGNANE SKELETON, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM AND PROCESS FOR PREPARING SAME
    • 带有PREGNANE SKELETON的新型甾体化合物,含有它们的药物组合物及其制备方法
    • WO1993025570A1
    • 1993-12-23
    • PCT/HU1993000035
    • 1993-06-08
    • RICHTER GEDEON VEGYÉSZETI GYAR RT.MAHO, SándorTUBA, ZoltánGERE, AnikóVITTAY, PálKISS, BélaPALOSI, ÉvaSZPORNY, LászlóFRANCSICSNÉ CZINEGE, ErzsébetBOORNÉ, MEZEI, AnnaBALOGH, GáborGÖROG, Sándor
    • RICHTER GEDEON VEGYÉSZETI GYAR RT.
    • C07J43/00
    • C07D239/42C07D239/48C07D239/50C07D491/10C07J43/003
    • The invention relates to novel, therapeutically active 21-aminosteroids of formula (I) with pregnane skeleton, wherein two of X, Y and Z mean a nitrogen atom each and the third one is a methine group; R and R represent, independently from each other, a primary amino group bearing as substituent a branched-chain C4-8alkyl, -alkenyl or -alkynyl group, or a C4-10cycloalkyl group comprising 1 to 3 ring(s) and being optionally substituted by C1-3alkyl group(s); or R and R stand together for a spiro-heterocyclic secondary amino group containing at most 10 carbon atoms and optionally at least one oxygen atom as additional heteroatom; or one of R and R means an unsubstituted heterocyclic secondary amino group containing 4 to 7 carbon atoms and the other one is an above-identified primary amino group, an above-identified spiro-heterocyclic secondary amino group, or a heterocyclic secondary amino group containing 4 to 7 carbon atoms and substituted by C1-4alkyl group(s); and n is 1 or 2, as well as their acid addition salts and pharmaceutical compositions containing these compounds. Furthermore, the invention relates to a process for the preparation of the above compounds. The compounds of formula (I) possess antioxidant, particularly lipid peroxidation-inhibiting effect, and therefore they may useful for the treatment of pathologic sequels of lipid peroxidation occurring in mammals, including man.
    • 本发明涉及具有孕烷骨架的式(I)的新型治疗活性的21-氨基甾体,其中X,Y和Z中的两个分别表示氮原子,第三个是次甲基; R 1和R 2彼此独立地表示带有支链C4-8烷基, - 烯基或 - 炔基的取代基的伯氨基或包含1〜3个环的C 4-10环烷基( s)并任选被C 1-3烷基取代; 或R 1和R 2连在一起用于含有至多10个碳原子和任选的至少一个氧原子作为附加杂原子的螺杂环仲氨基; 或者R 1和R 2中的一个是指含有4〜7个碳原子的未取代的杂环仲氨基,另一个是上述的伯氨基,上述的螺杂环仲氨基或 含有4-7个碳原子并被C 1-4烷基取代的杂环仲氨基; 和n为1或2,以及它们的酸加成盐和含有这些化合物的药物组合物。 此外,本发明涉及制备上述化合物的方法。 式(I)化合物具有抗氧化剂,特别是脂质过氧化抑制作用,因此它们可用于治疗哺乳动物(包括人)中发生的脂质过氧化物的病理遗传。