公开(公告)号：US07470703B1

公开(公告)日：2008-12-30

申请号：US11210206

申请日：2005-08-23

申请人： Duane D. Miller ,  Bob M. Moore, II ,  Suni Mustafa ,  Dennis R. Feller ,  Supriya A. Bavadekar

发明人： Duane D. Miller ,  Bob M. Moore, II ,  Suni Mustafa ,  Dennis R. Feller ,  Supriya A. Bavadekar

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。