首页> 外国专利> Biologically active 1,3-bis-aromatic-prop-2-en-1-ones, 1,3-bis-aromatic-propan-1-ones, and 1,3-bis-aromatic-prop-2-yn-1-ones

Biologically active 1,3-bis-aromatic-prop-2-en-1-ones, 1,3-bis-aromatic-propan-1-ones, and 1,3-bis-aromatic-prop-2-yn-1-ones

机译:具有生物活性的1,3-双-芳族丙-2-烯-1-酮,1,3-双-芳族丙-1-酮和1,3-双-芳族丙-2-炔-1 -那些

摘要

The invention relates to the use of 1,3-bis-aromatic-prop-2-en-1-ones (chalcones), 1,3-bis-aromatic-propan-1-ones (dihydrochalcones), and 1,3-bis-aromatic-prop-2-yn-1-ones for the preparation of pharmaceutical compositions for the treatment or prophylaxis of a number of serious diseases including i) conditions relating to harmful effects of inflammatory cytokines, ii) conditions involving infection by Helicobacter species, iii) conditions involving infections by viruses, iv) neoplastic disorders, and v) conditions caused by microorganisms or parasites. The invention also relates to novel chalcones and dihydrochalcones (especially alkoxy substituted variants) having advantageous substitution patterns with respect to their effect as drug substances, and methods of preparing them, as well as to pharmaceutical compositions comprising the novel chalcones. Moreover, the present invention relates to a method for the isolation of Leishmania fumarate reductase, QSAR methodologies for selecting potent compounds for the above-mentioned purposes.
机译:本发明涉及1,3-双-芳族丙-2-烯-1(查尔酮),1,3-双-芳族丙-1-酮(二氢查尔酮)和1,3-的用途。制备用于治疗或预防许多严重疾病的药物组合物的双芳香族丙-2-炔-1-酮,包括:i)与炎性细胞因子有害影响有关的病症,ii)幽门螺杆菌感染所致的病症; iii)涉及病毒感染的疾病,iv)肿瘤性疾病和v)微生物或寄生虫引起的疾病。本发明还涉及新颖的查耳酮和二氢查耳酮(尤其是烷氧基取代的变体),就它们作为药物的作用而言具有有利的取代方式,及其制备方法,以及涉及包含所述新颖查耳酮的药物组合物。而且,本发明涉及一种分离富马利什曼原虫还原酶的方法,该方法用于选择用于上述目的的有效化合物的QSAR方法。

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