US 9,808,472 B2
Biomarkers for treatment of neoplastic disorders using androgen-targeted therapies
Vincent C. O. Njar, Glen Burnie, MD (US); Amina Zoubeidi, Vancouver (CA); Karen Ferrante, Boston, MA (US); Eva Corey, Seattle, WA (US); and Douglas Jacoby, Wellesley, MA (US)
Assigned to Tokai Pharmaceuticals, Inc., Boston, MA (US); University of Washington, Seattle, WA (US); and University of Maryland, Baltimore, Baltimore, MD (US)
Appl. No. 14/758,938
Filed by Tokai Pharmaceuticals, Inc., Boston, MA (US); University of Washington, Seattle, WA (US); and University of Maryland, Baltimore, Baltimore, MD (US)
PCT Filed Aug. 12, 2014, PCT No. PCT/US2014/050793
§ 371(c)(1), (2) Date Jul. 6, 2015,
PCT Pub. No. WO2015/023710, PCT Pub. Date Feb. 19, 2015.
Claims priority of provisional application 61/865,038, filed on Aug. 12, 2013.
Claims priority of provisional application 61/990,570, filed on May 8, 2014.
Claims priority of provisional application 62/002,110, filed on May 22, 2014.
Prior Publication US 2016/0038511 A1, Feb. 11, 2016
Int. Cl. A61K 31/58 (2006.01); C07J 43/00 (2006.01); C12Q 1/68 (2006.01)
CPC A61K 31/58 (2013.01) [C07J 43/003 (2013.01); C12Q 1/6886 (2013.01); C12Q 2600/156 (2013.01); C12Q 2600/158 (2013.01)] 4 Claims
OG exemplary drawing
 
1. A method of overcoming enzalutamide resistance by:
administering a pharmaceutical composition that delivers a therapeutically effective amount of compound of formula I,

OG Complex Work Unit Drawing
or a pharmaceutically acceptable salt thereof wherein R1 is H and R2 is benzimidazole;
wherein the administering achieves downregulation of androgen receptor (AR) level in prostate cancer cells in a subject whose cancer has been demonstrated to be resistant to enzalutamide.