公开(公告)号：US20050159440A1

公开(公告)日：2005-07-21

申请号：US11029247

申请日：2005-01-04

Applicant: John Neumeyer ,  Jean Bidlack ,  Xiao-Hui Gu

Inventor： John Neumeyer ,  Jean Bidlack ,  Xiao-Hui Gu

IPC: A61K31/485 ,  A61K51/04 ,  C07D221/28 ,  A61K31/4745

CPC classification number: C07D221/28 ,  A61K31/485 ,  A61K51/0455

Abstract: The invention is based in part on the discovery that nonselective ε agonists that possess μ receptor-mediated effects in addition to their ε agonist effects can decrease cocaine self-administration more effectively and with fewer undesirable side effects than can highly selective ε agonists. The invention includes a number of new compounds having both nonselective ε opioid receptor agonist activity and additional activity at μ opioid receptors. These compounds are useful for the treatment of cocaine abuse, and can also be radiolabeled for use as imaging agents, e.g., the N-fluoroalkyl and iodoalkyl derivatives can be used, respectively, for positron emission tomography (PET) and single photon computed tomography (SPECT) brain imaging.

Abstract translation: 本发明部分基于以下发现：除了其ε-激动剂效应之外，具有μ受体介导的作用的非选择性ε-激动剂可以比高选择性ε激动剂更有效地减少可卡因自身给药并且具有更少的不希望的副作用。 本发明包括许多具有非选择性的ε阿片受体激动剂活性和在μ阿片受体的附加活性的新化合物。 这些化合物可用于治疗可卡因滥用，并且也可以放射性标记用作成像剂，例如，N-氟烷基和碘代烷基衍生物可分别用于正电子发射断层摄影（PET）和单光子计算机断层摄影（ SPECT）脑成像。