Organic compounds -- part of the class 532-570 series – Organic compounds – Heterocyclic carbon compounds containing a hetero ring...
Reexamination Certificate
2011-03-22
2011-03-22
Chandrakumar, Nizal S (Department: 1625)
Organic compounds -- part of the class 532-570 series
Organic compounds
Heterocyclic carbon compounds containing a hetero ring...
Reexamination Certificate
active
07910738
ABSTRACT:
The present invention provides novel fluorophilic compounds having structure VIIwherein Q is a carbonyl group, a protected carbonyl group, a hydroxy methine group, or a protected hydroxy methine group; R1is a C1-C20aliphatic, C2-C20cycloaliphatic, or C2-C20aromatic radical comprising at least one functional group susceptible to reaction with nucleophilic fluoride ion or an electrophilic fluorinating agent; R2is hydrogen or a C1-C10aliphatic radical; and R3is hydrogen or a C1-C10aliphatic radical. The fluorophilic compounds are provided in both racemic and enantiomerically enriched forms and are useful as intermediates in the preparation of novel PET imaging agents and probes useful in the discovery and performance assessment of PET imaging agents. The fluorophilic compounds are particularly useful in the preparation of PET imaging agents and probes having a high affinity for VMAT-2, a biomarker implicated in human diabetes and other illnesses such as Parkinson's disease.
REFERENCES:
patent: 2843591 (1958-07-01), Brossi et al.
patent: 4193998 (1980-03-01), Szantay et al.
patent: 5278308 (1994-01-01), Kung
patent: 1068261 (1959-11-01), None
patent: WO9316730 (1993-09-01), None
patent: WO2005077946 (2005-08-01), None
patent: WO2007005283 (2007-01-01), None
patent: WO2007130365 (2007-11-01), None
patent: WO2008154243 (2008-12-01), None
Goswami et al. Nuclear Medicine and Biology, 33, 2006, 685-694.
Popp et al., “Synthesis of Potential Antineoplastic Agents XXVI: 1,3,4,6,7,11b-Hexahydro-9,10-dimethoxy-2H-benso[a]2-quinolizinone Derivatives”, Journal of Pharmaceutical Sciences, vol. 67, No. 6, pp. 871-873, XP-002513807, Jun. 1978.
PCT International Search Report dated Feb. 18, 2009.
PCT International Search Report dated Apr. 3, 2009.
Zheng et al., “Computational Neural Network Analysis of the Affinity of Lobeline and Tetrabenazine Analogs for the Vesicular Monoamine Transporter-2”, Bioorganic & Medicinal Chemistry, vol. 15, pp. 2975-2992, 2007.
Kung et al., “Characterization of Optically Resolved 9-Fluoropropyl-Dihydrotetrabenzaine as a Potential PET Imaging Agent Targeting Vesicular Monoamine Transporters”, Nuclear Medicine and Biology, vol. 34, pp. 239-246, 2007.
Goswami et al., “Fluoroalkyl Derivatives of Dihydrotetrabenazine as Positron Emission Tomography Imaging Agents Targeting Vesicular Monoamine Transporters”, Nuclear Medicine and Biology, vol. 33, pp. 685-694, 2006.
Kilbourn et al., “Pharmacokinetics of [18F]Fluoroalkyl Derivatives of Dihydrotetrabenazine in Rate and Monkey Brain”, Nuclear Medicine and Biology, vol. 34, pp. 233-237, 2007.
Amarasinghe Kande Kankanamalage Dayarathna
Dinn Sean Richard
Johnson Bruce Fletcher
Rishel Michael James
Caruso Andrew J.
Chandrakumar Nizal S
General Electric Company
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