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active compounds on tissue forms of malaria and preparation process.

机译:活性化合物对疟疾的组织形式及其制备过程。

摘要

The invention relates to novel quinoline CONTAINING A function free amine and have anti-malarial properties, especially to novel primaquine or their addition salts with acid and process for their preparation. According to the invention, these new derivatives are schematically represented by the formula PQ-X, WHICH REPRESENTS PQ quinolines CONTAINING A function free amine and have anti-malarial properties, particularly primaquine; X represents an amino acid or peptide 2-4 amino acids; BEING THE UNION PQ-X a covalent bond between the Group AMINA peptidic FREE PQ AND THE GROUP carboxylic X, REMAIN STABLE THE UNION PQ-X in serum and lysosomal hydrolases RESISTANT. In one embodiment of the invention, the amino acid or the first amino acid peptide bound to PQ is acid (TAU) L-glutamic acid or acid (BETA) aspartic JOINED BY ITS GROUP PQ (TAU) - O (BETA )-carboxyl, OR L-pyroglutamic acid, aspartic acid KINGDOM OR A GROUP FOR YOUR PQ (ALFA)-carboxyl.
机译:本发明涉及一种含有游离胺并具有抗疟疾特性的新型喹啉,尤其涉及新型伯氨喹或其与酸的加成盐及其制备方法。根据本发明,这些新的衍生物由式PQ-X示意性表示,其中PQ-喹啉含有游离的功能胺并且具有抗疟疾特性,特别是伯喹啉; X代表氨基酸或2-4个氨基酸的肽;作为UNION PQ-X是AMINA肽组游离PQ和羧基X组之间的共价键,可保持血清和溶酶体水解酶抗性稳定的UNION PQ-X。在本发明的一个实施方案中,结合至PQ的氨基酸或第一氨基酸肽是酸(TAU)L-谷氨酸或天冬氨酸(BETA),其通过其基团PQ(TAU)-O(BETA)-羧基连接,或L-焦谷氨酸,天冬氨酸或PQ(ALFA)-羧基的基团。

著录项

  • 公开/公告号ES2058576T3

    专利类型

  • 公开/公告日1994-11-01

    原文格式PDF

  • 申请/专利权人 LA REGION WALLONNE;

    申请/专利号ES19890402593T

  • 申请日1989-09-21

  • 分类号C07D215/40;C07K5/06;C07K5/10;A61K31/47;A61K37/02;

  • 国家 ES

  • 入库时间 2022-08-22 04:42:49

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