IP Library › Granted Patent US 12,343,347
Granted Patent B2
US 12,343,347 · App. 17/527,428 · Granted Jul 1, 2025

Pro-drugs of riluzole and their method of use for the treatment of amyotrophic lateral sclerosis

Inventors: Allen B. Reitz (Lansdale, PA); Garry Robert Smith (Royersford, PA)
Assignee: Biohaven Therapeutics Ltd.
A61K31/541A61K31/428A61K31/4439A61K31/454A61K31/4725A61K31/496A61K31/5377
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Quick Facts
Patent No.
US 12,343,347
App. No.
17/527,428
Granted
Jul 1, 2025
Kind
B2
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 1Λ2. Pro-drugs of riluzole have enhanced stability to hepatic metabolism and are delivered into systemic circulation by oral administration, and then cleaved to release rihizole 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 rihizole from a pro-drug agent.

Claims (5)

1. A method for treating a non-proliferative disease in which riluzole is clinically relevant, said method comprising administering to a subject an effective amount of at least one compound of the formula (II):

including hydrates, solvates, pharmaceutically acceptable salts, and complexes thereof, wherein:

R 12a , R 12b , R 12c , R 12d , and R 12e are each independently selected from the group consisting of hydrogen, deuterium, halogen, trifluoromethyl, trifluoromethoxy, optionally substituted C1-C6 alkyl, and optionally substituted C1-C6 alkoxy.

2. The method of claim 1 , wherein the at least one compound of the formula (II) is administered in a composition further comprising at least one excipient.

3. The method of claim 1 , wherein the disease in which riluzole is clinically relevant is amyotrophic lateral sclerosis, bipolar disorder, treatment resistant and major depression, obsessive-compulsive disorder, spinal muscular atrophy, radiation therapy, multiple sclerosis, chronic cerebellar ataxia, cervical spondylotic myelopathy, spinal cord injury, hereditary cerebellar ataxia, Tourette syndrome, autism spectrum disorder, schizophrenia, fragile X syndrome, Parkinson's Disease, or Huntington's disease.

Assignments (1)
SECURITY INTEREST Recorded May 1, 2025
From: BIOHAVEN THERAPEUTICS LTD
To: BEETLEJUICE SA LLC, AS PURCHASER AGENT
Reel/Frame 071147/0260 →
Continuity (4)
Division 16518008 · Jul 22, 2019
Division 14410647
Provisional Application 61663573 · Jun 23, 2012
Related Publication 20220072006A1 · Mar 10, 2022
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