Indole and benzofuran fused isoquinuclidene derivatives and processes for preparing them
    62.
    发明授权
    Indole and benzofuran fused isoquinuclidene derivatives and processes for preparing them 有权
    吲哚和苯并呋喃稠合的亚奎宁衍生物及其制备方法

    公开(公告)号:US09150584B2

    公开(公告)日:2015-10-06

    申请号:US13749593

    申请日:2013-01-24

    申请人: DemeRx, Inc.

    IPC分类号: C07D491/22 C07D471/22

    摘要: Provided herein are indole and benzofuran fused isoquinuclidene derivatives. Also provided herein are processes, preferably enantioselective processes, for preparing such derivatives including processes for preparing (−) and (+) noribogaine or a salt thereof, in substantially enantiomerically pure forms.

    摘要翻译: 本文提供的是吲哚和苯并呋喃稠合的亚奎宁衍生物。 本文还提供用于制备此类衍生物的方法,优选对映选择性方法,包括以基本上对映体纯的形式制备( - )和(+)诺布恩或其盐的方法。

    Tetrandrine derivatives with substituted 5-carbon, preparation method and use thereof
    63.
    发明授权
    Tetrandrine derivatives with substituted 5-carbon, preparation method and use thereof 有权
    具有取代的5碳的替康德林衍生物,其制备方法和用途

    公开(公告)号:US09133207B2

    公开(公告)日:2015-09-15

    申请号:US14239759

    申请日:2012-08-20

    摘要: The present invention belongs to the field of natural medicine and pharmaceutical chemistry and specifically relates to novel 5-substituted tetrandrine derivatives of formula (I) and a pharmaceutically acceptable adduct, complex and salt thereof, to a process for the preparation of these compounds, pharmaceutical compositions containing such compounds and their use in preparing antineoplastic medicaments.

    摘要翻译: 本发明属于天然药物和药物化学领域,具体涉及式(I)的新型5-取代四甲基环戊二烯衍生物及其药学上可接受的加合物,其络合物和盐,用于制备这些化合物,药物 含有这些化合物的组合物及其在制备抗肿瘤药物中的用途。

    Morphinan derivative
    68.
    发明授权
    Morphinan derivative 有权
    吗啡衍生物

    公开(公告)号:US08952030B2

    公开(公告)日:2015-02-10

    申请号:US14343218

    申请日:2012-09-07

    摘要: A morphinan derivative represented by the following general formula (I): (in the formula, R1 represents hydrogen, C1-6 alkyl, cycloalkylalkyl (the cycloalkyl moiety has 3 to 6 carbon atoms, and the alkylene moiety has 1 to 5 carbon atoms), aralkyl (the aryl moiety has 6 to 10 carbon atoms, and the alkylene moiety has 1 to 5 carbon atoms) and the like, R2 represents hydrogen, C1-6 alkyl, C3-6 cycloalkyl, C6-10 aryl, aralkyl (the aryl moiety has 6 to 10 carbon atoms, and the alkylene moiety has 1 to 5 carbon atoms) and the like, R3, R4 and R5 represent hydrogen, hydroxy, carbamoyl, C1-6 alkoxy, C6-10 aryloxy and the like, R6a, R6b, R7, R8, R9, and R10 represent hydrogen and the like, X represents O or CH2, and Y represents C═O, SO2, an atomic bond and the like), or an acid addition salt thereof is used as an analgesic.

    摘要翻译: 由以下通式(I)表示的吗啡喃衍生物:(式中,R 1表示氢,C 1-6烷基,环烷基烷基(环烷基部分具有3〜6个碳原子,亚烷基部分具有1〜5个碳原子) ,芳烷基(芳基部分具有6〜10个碳原子,亚烷基部分具有1〜5个碳原子)等,R 2表示氢,C 1-6烷基,C 3-6环烷基,C 6-10芳基,芳烷基( 芳基部分具有6至10个碳原子,亚烷基部分具有1至5个碳原子)等,R 3,R 4和R 5表示氢,羟基,氨基甲酰基,C 1-6烷氧基,C 6-10芳氧基等,R 6a ,R6b,R7,R8,R9和R10表示氢等,X表示O或CH2,Y表示C = O,SO2,原子键等)或其酸加成盐作为 镇痛药