N-SUBSTITUTED BETA-CARBOLINIUM COMPOUNDS AS POTENT P-GLYCOPROTEIN INDUCERS
    5.
    发明公开
    N-SUBSTITUTED BETA-CARBOLINIUM COMPOUNDS AS POTENT P-GLYCOPROTEIN INDUCERS 审中-公开
    N-取代的β-咔啉化合物作为有效的β-糖蛋白诱导剂

    公开(公告)号:EP3227291A1

    公开(公告)日:2017-10-11

    申请号:EP15807703.2

    申请日:2015-10-21

    CPC分类号: C07D471/14 C07D471/04

    摘要: The present invention relates to the N-substituted beta-carbolinium compounds of general formula A and formulae I and II wherein, R1 and R2 groups are selected from halogens or trifluoromethyl; R3 group is selected from hydrogen or methyl; Ar is selected from aryl and heteroaryl, X is selected from halogens; and R1 and R2 groups may be attached to any position on ring E. The present invention particularly relates to synthesis and p-glycoprotein induction activity of the N-substituted beta-carbolinium compounds. In addition, the invention relates to methods of using compounds for treating or preventing Alzheimer's disease.

    摘要翻译: 本发明涉及通式A和式I和II的N-取代的β-咔啉鎓化合物,其中R 1和R 2基团选自卤素或三氟甲基; R 3基团选自氢或甲基; Ar选自芳基和杂芳基,X选自卤素; 并且R 1和R 2基团可以连接到环E上的任何位置。本发明特别涉及N-取代的β-咔啉鎓化合物的合成和β-糖蛋白诱导活性。 另外,本发明涉及使用化合物治疗或预防阿尔茨海默氏病的方法。

    ALKYLIDENE PHOSPHONATE ESTERS AS P-GLYCOPROTEIN INDUCERS
    7.
    发明公开
    ALKYLIDENE PHOSPHONATE ESTERS AS P-GLYCOPROTEIN INDUCERS 有权
    亚烷基膦酸酯作为P-糖蛋白诱导剂

    公开(公告)号:EP3209671A1

    公开(公告)日:2017-08-30

    申请号:EP15787031.2

    申请日:2015-09-16

    摘要: The present invention relates to the alkylidene phosphonate esters of formula I wherein, R1 is selected from a group consisting of hydrogen or alkyl group; R2 is selected from a group consisting of hydrogen, hydroxy, alkyl, alkoxy, nitro, halogen, amino, N- substituted alkylamino; alkyl group is selected from a group consisting of methyl, ethyl and isopropyl; Ar is selected from a group consisting of aryl, substituted aryl, fused aryl, heteroaryl, and substituted heteroaryl. The present invention particularly relates to synthesis and p-glycoprotein induction activity of the alkylidene phosphonate esters. In addition, the invention relates to methods of using compounds for treating or preventing Alzheimer's disease.

    摘要翻译: 本发明涉及式I的亚烷基膦酸酯,其中R 1选自氢或烷基; R2选自氢,羟基,烷基,烷氧基,硝基,卤素,氨基,N-取代的烷基氨基; 烷基选自甲基,乙基和异丙基; Ar选自由芳基,取代的芳基,稠合的芳基,杂芳基和取代的杂芳基组成的组。 本发明特别涉及亚烷基膦酸酯的合成和p-糖蛋白诱导活性。 另外,本发明涉及使用化合物治疗或预防阿尔茨海默氏病的方法。