US 12,214,058 B2
Imaging methods using deuterated compounds
Jan Marik, Hillsborough, CA (US); Joseph P. Lyssikatos, Piedmont, CA (US); and Simon Peter Williams, Redwood City, CA (US)
Assigned to Genentech, Inc., South San Francisco, CA (US)
Filed by Genentech, Inc., South San Francisco, CA (US)
Filed on Nov. 18, 2022, as Appl. No. 18/056,856.
Application 18/056,856 is a continuation of application No. 16/895,352, filed on Jun. 8, 2020, granted, now 11,504,440.
Application 16/895,352 is a continuation of application No. 16/050,453, filed on Jul. 31, 2018, granted, now 10,675,367, issued on Jun. 9, 2020.
Application 16/050,453 is a continuation of application No. 15/006,997, filed on Jan. 26, 2016, granted, now 10,076,581, issued on Sep. 18, 2018.
Application 15/006,997 is a continuation of application No. PCT/EP2015/060447, filed on May 12, 2015.
Claims priority of provisional application 61/992,717, filed on May 13, 2014.
Prior Publication US 2023/0218782 A1, Jul. 13, 2023
This patent is subject to a terminal disclaimer.
Int. Cl. A61K 51/04 (2006.01); C07B 59/00 (2006.01); C07D 487/04 (2006.01)
CPC A61K 51/0459 (2013.01) [C07B 59/002 (2013.01); C07D 487/04 (2013.01); C07B 2200/05 (2013.01)] 6 Claims
 
1. A method for detecting one or more of neurofibrillary tangles, senile plaques, or tau protein aggregation in a human subject, the method comprising:
obtaining a three-dimensional image of the subject's brain;
administering to the human subject an effective amount of a radiolabeled tracer selected from:

OG Complex Work Unit Chemistry
or a pharmaceutically acceptable salt thereof, wherein the effective amount is sufficient to provide an initial radiation level not greater than 370 MBq;
acquiring three-dimensional images of the subject's brain with a PET camera at one or more time intervals, thereby providing a 3D PET image of the radioactive signal of the tracer at each of the one or more time intervals;
aligning the PET images with one another and, using the MR volumetric image for anatomical delineation, identifying irregular regions of interest in the subject's brain;
measuring the standardized uptake value ratio for each region of interest relative to cerebellum gray at each of the one or more time intervals; and
identifying regions having enhanced standardized uptake value ratios as containing one or more of: neurofibrillary tangles, senile plaques, or tau protein aggregation.