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Design and Selection Parameters to Accelerate the Discovery of Novel Central Nervous System Positron Emission Tomography (PET) Ligands and Their Application in the Development of a Novel Phosphodiesterase 2A PET Ligand

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    Design and Selection Parameters to Accelerate the Discovery of Novel Central Nervous System Positron Emission Tomography (PET) Ligands and Their Application in the Development of a Novel Phosphodiesterase 2A PET Ligand
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    † Neuroscience Medicinal Chemistry, Pfizer Inc., Cambridge, Massachusetts 02139, United States
    ‡ Neuroscience Medicinal Chemistry, Pfizer Inc., Groton, Connecticut 06340, United States
    § BioImaging Center, Precision Medicine, Pfizer Inc., Groton, Connecticut 06340, United States
    ∥ Neuroscience Research Unit, Pfizer Inc., Cambridge, Massachusetts 02139, United States
    ⊥ Data Analytical Group, Groton Center of Chemistry, Groton, Connecticut 06340, United States
    *Phone: +1 617 395 0640. Fax: +1 860 686 5285. E-mail: [email protected]
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    Journal of Medicinal Chemistry

    Cite this: J. Med. Chem. 2013, 56, 11, 4568–4579
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    https://doi.org/10.1021/jm400312y
    Published May 7, 2013
    Copyright © 2013 American Chemical Society
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    Abstract

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    To accelerate the discovery of novel small molecule central nervous system (CNS) positron emission tomography (PET) ligands, we aimed to define a property space that would facilitate ligand design and prioritization, thereby providing a higher probability of success for novel PET ligand development. Toward this end, we built a database consisting of 62 PET ligands that have successfully reached the clinic and 15 radioligands that failed in late-stage development as negative controls. A systematic analysis of these ligands identified a set of preferred parameters for physicochemical properties, brain permeability, and nonspecific binding (NSB). These preferred parameters have subsequently been applied to several programs and have led to the successful development of novel PET ligands with reduced resources and timelines. This strategy is illustrated here by the discovery of the novel phosphodiesterase 2A (PDE2A) PET ligand 4-(3-[18F]fluoroazetidin-1-yl)-7-methyl-5-{1-methyl-5-[4-(trifluoromethyl)phenyl]-1H-pyrazol-4-yl}imidazo[5,1-f][1,2,4]triazine, [18F]PF-05270430 (5).

    Copyright © 2013 American Chemical Society

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    Supporting Information

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    The full data set of the PET ligand database, an extended version of Table 2 with individual parameters of CNS PET MPO (ClogP, ClogD, MW, HBD, TPSA, and pKa), and a CNS PET MPO calculator in Excel format. This material is available free of charge via the Internet at http://pubs.acs.org.

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    Cite this: J. Med. Chem. 2013, 56, 11, 4568–4579
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