公开(公告)号：US09284322B2

公开(公告)日：2016-03-15

申请号：US14616313

申请日：2015-02-06

Applicant: Research Triangle Institute

Inventor： Frank Ivy Carroll ,  Pauline Wanjiku Ondachi

IPC: C07D401/00 ,  C07D487/08 ,  A61K31/407 ,  C07D401/14 ,  C07D409/14

CPC classification number: C07D487/08 ,  A61K31/407 ,  C07D401/14 ,  C07D409/14

Abstract: Provided herein are compounds and methods of preparation of compounds that are capable of functioning as agonists or antagonists of a nicotinic receptor. Also provided are pharmaceutical compositions comprising one or more of these compounds, which may further comprise one or more additional therapeutic agents. Further provided are methods of treatment of various conditions that may be responsive to such activity at the nicotinic receptors, such as nicotine dependence.

公开(公告)号：US20150141416A1

公开(公告)日：2015-05-21

申请号：US14537124

申请日：2014-11-10

Applicant: Research Triangle Institute ,  Dignity Health d/b/a St. Joseph's Hospital and Medical Center and Barrow Neurological Institute ,  Virginia Commonwealth University

Inventor： Frank Ivy Carroll ,  Bruce E. Blough ,  Hernan A. Navarro ,  S. Wayne Mascarella ,  Ana Zamfira Muresan ,  M. Imad Damaj ,  Ronald J. Lukas

IPC: C07D265/32

CPC classification number: C07D265/32 ,  A61K31/5375

Abstract: The invention provides hydroxybupropion analogues capable of inhibiting the reuptake of one or more monoamines and/or acting as antagonists at nicotinic acetylcholine receptors. The compounds may selectively bind to one or more monoamine transporters, including those for dopamine, norepinephrine, and serotonin and/or may selectively bind to one or more nicotinic acetylcholine receptor subtypes. Such compounds may be used to treat conditions that are responsive to modification of monoamine levels and/or antagonism of nicotinic acetylcholine receptors, including drug dependency, depression, and obesity.

Abstract translation: 本发明提供能够抑制一种或多种单胺再摄取和/或在烟碱型乙酰胆碱受体上作为拮抗剂的羟基安非他丁类似物。 所述化合物可以选择性地结合一种或多种单胺转运蛋白，包括用于多巴胺，去甲肾上腺素和5-羟色胺的单胺转运蛋白和/或可以选择性地结合一种或多种烟碱型乙酰胆碱受体亚型。 这些化合物可用于治疗对单胺水平的修饰和/或烟碱乙酰胆碱受体的拮抗作用有反应的病症，包括药物依赖性，抑郁症和肥胖症。