公开(公告)号：US20020188003A1

公开(公告)日：2002-12-12

申请号：US10155012

申请日：2002-05-28

Applicant: Research Triangle Institute

Inventor： Michael J. Kuhar ,  Frank Ivy Carroll ,  John W. Boja ,  Anita H. Lewin ,  Philip Abraham

IPC: C07D413/02 ,  A61K031/46

CPC classification number: C07D451/02 ,  A61K51/0448 ,  A61K2123/00 ,  C07F7/2208

Abstract: Tropane derivatives having a high binding affinity and selectivity for dopamine transporters bear, on the tropane backbone either a carboxylic ester or isoxazole moiety, as well as a substituted phenyl moiety. The compounds have utility both as pharmaceutical and as imaging agents, when one or more atoms are radioactive.

Abstract translation: 对于多巴胺转运蛋白具有高结合亲和性和选择性的托烷衍生物在托烷骨架上具有羧酸酯或异恶唑部分以及取代的苯基部分。 当一个或多个原子是放射性的时，这些化合物既用作药物也可用作成像剂。

公开(公告)号：US20030203934A1

公开(公告)日：2003-10-30

申请号：US10279851

申请日：2002-10-25

Applicant: Research Triangle Institute

Inventor： Michael J. Kuhar ,  Frank I. Carroll ,  John W. Boja ,  Anita H. Lewin ,  Philip Abraham

IPC: C07D451/04 ,  A61K031/46

CPC classification number: C07D451/02 ,  A61K31/439

Abstract: A class of binding ligands for cocaine receptors and other receptors in the brain. Specifically, a novel family of compounds shows high binding specificity and activity, and, in a radiolabeled form, can be used to bind to these receptors, for biochemical assays and imaging techniques. Such imaging is useful for determining effective doses of new drug candidates in human populations. In addition, the high specificity, slow onset and long duration of the action of these compounds at the receptors makes them particularly well suited for therapeutic uses, for example as substitute medication for psychostimulant abuse. Some of these compounds may be useful in treating Parkinson's Disease or depression, by virtue of their inhibitory properties at monoamine transporters.

Abstract translation: 一类可卡因受体和脑中其他受体的结合配体。 具体来说，新型化合物家族显示出高结合特异性和活性，并且以放射性标记的形式可用于结合这些受体，用于生物化学测定和成像技术。 这种成像可用于确定人群中新的候选药物的有效剂量。 此外，这些化合物在受体的高度特异性，缓慢发作和长时间的作用使得它们特别适用于治疗用途，例如作为精神兴奋剂滥用的替代药物。 这些化合物中的一些可能由于其在单胺转运蛋白上的抑制性质而可用于治疗帕金森病或抑郁症。

公开(公告)号：US20030023090A1

公开(公告)日：2003-01-30

申请号：US09956159

申请日：2001-09-20

Applicant: RESEARCH TRIANGLE INSTITUTE

Inventor： Frank I. Carroll ,  Michael J. Kuhar ,  John W. Boja ,  Anita H. Lewin ,  Philip Abraham

IPC: C07D451/02

CPC classification number: C07D451/02 ,  A61K51/0448 ,  A61K2123/00 ,  C07F7/2208

Abstract: The invention relates to novel compounds which show high affinity for cocaine receptors in the brain, particularly dopamine and serotonin transporter sites. The compounds may be used as imaging or pharmaceutical agents, in the diagnosis and treatment of drug addiction, depression, anorexia and neurodegenerative diseases.

Abstract translation: 本发明涉及对脑中可卡因受体表现出高亲和力的新化合物，特别是多巴胺和血清素转运蛋白位点。 该化合物可用作成像或药剂，用于诊断和治疗药物成瘾，抑郁，厌食和神经退行性疾病。