发明授权
US07902364B2 Alpha-fluoroalkyl tetrabenazine and dihydrotetrabenazine imaging agents and probes
有权
α-氟烷基丁苯那嗪和二氢丁苯那嗪成像剂和探针
- 专利标题： Alpha-fluoroalkyl tetrabenazine and dihydrotetrabenazine imaging agents and probes
- 专利标题（中）： α-氟烷基丁苯那嗪和二氢丁苯那嗪成像剂和探针
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申请号： US11947215申请日： 2007-11-29
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公开(公告)号： US07902364B2公开(公告)日： 2011-03-08
- 发明人: Michael James Rishel , Kande Kankanamalage Dayarathna Amarasinghe , Sean Richard Dinn , Bruce Fletcher Johnson
- 申请人： Michael James Rishel , Kande Kankanamalage Dayarathna Amarasinghe , Sean Richard Dinn , Bruce Fletcher Johnson
- 申请人地址： US NY Niskayuna
- 专利权人： General Electric Company
- 当前专利权人： General Electric Company
- 当前专利权人地址： US NY Niskayuna
- 代理商 Andrew J. Caruso
- 主分类号： C07D455/06
- IPC分类号： C07D455/06
摘要：
The present invention provides novel alpha-fluoroalkyl compounds having structure I and the corresponding dihydrotetrabenazine compounds IV wherein R1 is a C1-C10 fluorinated aliphatic radical; R2 is hydrogen or a C1-C10 aliphatic radical; and R3 is hydrogen or a C1-C10 aliphatic radical. The alpha-fluoroalkyl compounds are provided in both racemic and enantiomerically enriched forms and may comprise either or both of fluorine-18 and fluorine 19. The alpha-fluoroalkyl compounds are shown to possess high affinity for VMAT-2, a biomarker implicated in human diabetes. The alpha-fluoroalkyl compounds comprising a fluorine-18 group are useful as PET imaging agents targeting the VMAT-2 biomarker. The non-radiolabled alpha-fluoroalkyl compounds are useful as probes for the discovery of PET imaging agents.
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