Nonsteroidal and steroidal compounds with potent androgen receptor down-regulation and anti prostate cancer activity
Patent Number: US20160038476
 
Executive Summary:
  • Invention Type: Therapeutic
  • Patent Status: Pending
  • Patent Link: https://patents.google.com/patent/US20160038476/
  • Research Institute: University of Maryland - Baltimore
  • Disease Focus: Prostate cancer
  • Basis of Invention: Non-condensed isoquinolines, Diazoles, Non-condensed pyridines, heterocyclic compounds
  • How it works: The invention describes the synthesis of novel nonsteroid and steroid-mimetic compounds that result in androgen receptor down-regulation. Androgen receptors play crucial roles in the development and advancement of prostate cancer. Therefore, downregulation of androgen receptors results in apoptosis and inhibits proliferation
  • Lead Challenge Inventor: Vincent Njar
  • Inventors: Vincent C.O. Njar, Puranik Purushottamachar
  • Development Stage: Pre-clinical
  • Novelty:
    • Synthesis of androgen receptor downregulating compounds that are effective against all splice variants and increased activity
  • Clinical Applications:
    • Prevention and/or therapeutic for prostate cancer

General Description:
Androgen receptors are key players in the development and advancement of prostate cancer and are, therefore, well-established targets for therapeutic intervention. However, current treatment approaches have a limited response of 12-24 months, and the disease becomes castration-resistant. In addition, androgen receptors have multiple splicing variants, and current drugs do not target all different variants. The current invention describes novel compounds with enhanced androgen receptor downregulating activity that is effective against all splicing variants.
 
Strengths:
  • Enhanced physiochemical and pharmacokinetic properties
  • Selective
  • Reduced drug resistance
  • Targets all androgen receptor splice variants

Patent Status:
Filing date: 2014-04-04
 
Inventor Bio: Vincent Njar
http://www.medschool.umaryland.edu/profiles/Njar-Vincent/