Yohimbine dimers exhibiting binding selectivities for &agr;2 adrenergic receptors
    1.
    发明授权
    Yohimbine dimers exhibiting binding selectivities for &agr;2 adrenergic receptors 失效
    育亨宾二聚体显示α2肾上腺素能受体的结合选择性

    公开(公告)号:US06638943B2

    公开(公告)日:2003-10-28

    申请号:US10106521

    申请日:2002-03-25

    IPC分类号: A61K31475

    CPC分类号: C07D519/00

    摘要: The present invention relates to yohimbine dimer compounds, pharmaceutical compositions containing such dimer compounds, methods of making such dimer compounds, and uses thereof. The yohimbine dimer compounds include compounds of formula (I): where R is any linker molecule which affords a yohimbine dimer that has activity as an &agr;2-AR antagonist and has selectivity for an &agr;2-AR subtype over another &agr;2-AR subtype.

    摘要翻译: 本发明涉及育亨宾二聚体化合物,含有这种二聚体化合物的药物组合物,制备这种二聚体化合物的方法及其应用。 育亨宾二聚体化合物包括式(I)化合物:其中R是提供具有作为α2-AR拮抗剂的活性的育亨宾二聚体并且对α2-AR亚型具有对另一α2-AR亚型的选择性的任何连接分子。

    Yohimbine derivatives and use thereof
    2.
    发明授权
    Yohimbine derivatives and use thereof 失效
    育亨宾衍生物及其用途

    公开(公告)号:US07470703B1

    公开(公告)日:2008-12-30

    申请号:US11210206

    申请日:2005-08-23

    IPC分类号: A61K31/4745 C07D471/16

    CPC分类号: C07D471/16

    摘要: Yohimbine derivatives are disclosed having modification of the C-16 carboxyl group to include a sidechain and where the resulting derivative does not possess a second yohimbine pharmacophore (i.e., the compound is not a yohimbine dimer). The yohimbine derivatives of the present invention are preferably characterized by selective activity as α2c-AR antagonists. Use of the compounds, or pharmaceutical composition containing them, for treating or preventing an α2c adrenergic receptor mediated condition or disorder, and for antagonizing activity of an α2c adrenergic receptor are also disclosed.

    摘要翻译: 公开了育亨宾衍生物,其具有C-16羧基的修饰以包括侧链,并且其中所得衍生物不具有第二育亨宾药效团(即,该化合物不是育亨宾二聚体)。 优选本发明的育亨宾衍生物的特征在于作为α2c-AR拮抗剂的选择性活性。 还公开了化合物或含有它们的药物组合物用于治疗或预防α2c肾上腺素能受体介导的病症或病症以及拮抗α2c肾上腺素能受体的活性的用途。

    Tri-aryl/heteroaromatic cannabinoids and use thereof
    7.
    发明授权
    Tri-aryl/heteroaromatic cannabinoids and use thereof 有权
    三芳基/杂芳族大麻素及其用途

    公开(公告)号:US09139546B2

    公开(公告)日:2015-09-22

    申请号:US13024643

    申请日:2011-02-10

    IPC分类号: C07D307/42 C07D307/46

    CPC分类号: C07D307/42 C07D307/46

    摘要: Cannabinoid derivatives according to formula (I) are disclosed wherein, X, Y, R1, R2, and W can have the definitions provided herein. Without limitation, use of such compounds, their salts or pro-drug, or compositions containing the compounds, salts, or pro-drug, to modify the activity of CB1 and CB2 receptors and treat conditions mediated by these receptors.

    摘要翻译: 公开了根据式(I)的大麻素衍生物,其中X,Y,R 1,R 2和W可具有本文提供的定义。 不限于此,使用这些化合物,其盐或前药,或含有化合物,盐或前药的组合物来改变CB1和CB2受体的活性并治疗由这些受体介导的病症。