Abstract: Pharmaceutical compositions of the invention include substituted riluzole pro drugs useful for the treatment of amyotrophic lateral sclerosis (ALS) and related disorders through the release of riluzole, especially to avoid patient to patient variability in first pass, hepatic metabolism promoted by Cyp 1?2. Pro-drugs of riluzole have enhanced stability to hepatic metabolism and are delivered into systemic circulation by oral administration, and then cleaved to release riluzole in the plasma via either an enzymatic or general biophysical release process. The invention further includes pro-drugs of riluzole useful for the treatment of disease states that can be treated with riluzole through the release of riluzole from a pro-drug agent.
Type:
Grant
Filed:
July 22, 2019
Date of Patent:
December 14, 2021
Assignee:
Biohaven Pharmaceutical Holding Company Limited
Abstract: Pharmaceutical compositions of the invention include substituted riluzole pro drugs useful for the treatment of amyotrophic lateral sclerosis (ALS) and related disorders through the release of riluzole, especially to avoid patient to patient variability in first pass, hepatic metabolism promoted by Cyp 1A2. Pro-drugs of riluzole have enhanced stability to hepatic metabolism and are delivered into systemic circulation by oral administration, and then cleaved to release riluzole in the plasma via either an enzymatic or general biophysical release process. The invention further includes pro-drugs of riluzole useful for the treatment of disease states that can be treated with riluzole through the release of riluzole from a pro-drug agent.
Type:
Grant
Filed:
June 24, 2013
Date of Patent:
July 23, 2019
Assignee:
Biohaven Pharmaceutical Holding Company Limited
Abstract: Pharmaceutical compositions of the invention include substituted riluzole prodrugs useful for the treatment of cancers including melanoma, breast cancer, brain cancer, and prostate cancer through the release of riluzole. Prodrugs of riluzole have enhanced stability to hepatic metabolism and are delivered into systemic circulation by oral administration, and then cleaved to release riluzole in the plasma via either an enzymatic or general biophysical release process.
Type:
Grant
Filed:
March 15, 2013
Date of Patent:
August 8, 2017
Assignees:
Biohaven Pharmaceutical Holding Company Limited, Rutgers, The State University of New Jersey
Inventors:
Garry R. Smith, Allen B. Reitz, Mark McDonnell, Suzie Chen, Matthew D. Vera, Benjamin E. Blass, Jeffery C. Pelletier, Venkata N. Velvadapu, Jay E. Wrobel