Compounds with hydroxycarbonyl-halogenoalkyl side chain
    2.
    发明授权
    Compounds with hydroxycarbonyl-halogenoalkyl side chain 失效
    具有羟基羰基 - 卤代烷基侧链的化合物

    公开(公告)号:US06737417B2

    公开(公告)日:2004-05-18

    申请号:US10149752

    申请日:2002-06-13

    IPC分类号: C07J100

    摘要: The present invention provides a compound consisting of a moiety and a group chemically bonded to said moiety, wherein said moiety contains a compound having low activity following oral administration or its parent scaffold and said group has the following general formula (1): in which R1 represents a hydrogen atom, etc., R2 represents a C1-C7 halogenoalkyl group, etc., m represents an integer of 2 to 14, and n represents an integer of 2 to 7, or enantiomers of the compound, or hydrates or pharmaceutically acceptable salts of the compound or enantiomers thereof. The above compound is advantageous in pharmaceutical use because the group of general formula (1) allows compounds such as anti-estrogenic ones to show a significantly increased activity following oral administration when attached to the parent scaffolds of the compounds.

    摘要翻译: 本发明提供由部分和化学键合到所述部分的基团组成的化合物,其中所述部分含有口服后具有低活性的化合物或其母体支架,并且所述基团具有以下通式(1):其中R 1表示 氢原子等,R2表示C1-C7卤代烷基等,m表示2〜14的整数,n表示2〜7的整数,或该化合物的对映异构体或其水合物或药学上可接受的盐 其化合物或其对映异构体。 上述化合物在药物用途中是有利的,因为通式(1)的基团允许化合物如抗雌激素的化合物在连接到化合物的母体支架上时在口服给药后显示出显着增加的活性。

    Compounds with hydroxycarbonyl-halogenoalkyl side chains
    4.
    发明申请
    Compounds with hydroxycarbonyl-halogenoalkyl side chains 审中-公开
    具有羟基羰基 - 卤代烷基侧链的化合物

    公开(公告)号:US20050192449A1

    公开(公告)日:2005-09-01

    申请号:US11115134

    申请日:2005-04-27

    摘要: The present invention provides a compound consisting of a moiety and a group chemically bonded to said moiety, wherein said moiety contains a compound having low activity following oral administration or its parent scaffold and said group has the following general formula (1): in which R1 represents a hydrogen atom, etc., R2 represents a C1-C7 halogenoalkyl group, etc., m represents an integer of 2 to 14, and n represents an integer of 2 to 7, or enantiomers of the compound, or hydrates or pharmaceutically acceptable salts of the compound or enantiomers thereof. The above compound is advantageous in pharmaceutical use because the group of general formula (1) allows compounds such as anti-estrogenic ones to show a significantly increased activity following oral administration when attached to the parent scaffolds of the compounds.

    摘要翻译: 本发明提供了由部分和化学键合到所述部分的基团组成的化合物,其中所述部分含有口服后具有低活性的化合物或其母体支架,所述基团具有以下通式(1):其中R R 1表示氢原子等,R 2表示C 1 -C 7卤代烷基等 m表示2〜14的整数,n表示2〜7的整数,或该化合物的对映异构体,或其化合物或其对映异构体的水合物或药学上可接受的盐。 上述化合物在药物用途中是有利的,因为通式(1)的基团允许化合物如抗雌激素的化合物在连接到化合物的母体支架上时在口服给药后显示出显着增加的活性。