US 10,208,023 B2 · Heterocyclic inhibitors of the sodium channel

Abstract

The invention relates to compounds useful in treating conditions associated with voltage-gated ion channel function, particularly conditions associated with sodium channel activity. More specifically, the invention concerns heterocyclic compounds (e.g., compounds according to any of Formulas (I)-(X) or Compounds (1)-(92) of Table 1) that are that are useful in treatment of conditions such as epilepsy, cancer, pain, migraine, Parkinson's Disease, mood disorders, schizophrenia, psychosis, tinnitus, amyotrophic lateral sclerosis, glaucoma, ischemia, spasticity disorders, obsessive compulsive disorder, restless leg syndrome and Tourette syndrome.

Claims15

Dependent claims

A compound of Formula X:

wherein Het is selected from the group consisting of
R1 is H;
R2 is H or optionally substituted C1 to C6 alkyl;
R3 is H, optionally substituted C1-C6 alkyl, or optionally substituted phenyl;
R4 is C1-C6 alkyl substituted with halo, CN, NO2, CF3, OCF3, COOR′, CONR′2, OR′, SR′, SOR′, SO2R′, NR′2, NR′(CO)R′, NR′C(O)OR′, NR′C(O)NR′2, NR′SO2NR′2, ═NOR′, ═O or NR′SO2R′, wherein each R′ is independently H or an optionally substituted group selected from alkyl, alkenyl, alkynyl, heteroalkyl, heteroalkenyl, heteroalkynyl, heteroaryl and aryl;
and
R5 is H or an optionally substituted C1-C6 alkyl;
or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof.

5 more elements

Dependencies are inferred from the claim text.

Facts

Application

14/771,628Filed 27 Feb 2014 · us provisional application

Priority

1 Mar 2013

Published

US 2016/0016939 A121 Jan 2016

Granted

19 Feb 2019

Term ends

Not estimatedThe source records don’t support an estimate.

Classification26 codes

C07D 403/06
Containing two hetero rings: linked by a carbon chain containing only aliphatic carbon atoms
A61P 25/06
Drugs for disorders of the nervous system: antimigraine agents
A61P 29/00
Non-central analgesic, antipyretic or antiinflammatory agents
C07C 237/08
The carbon skeleton being acyclic and saturated: having the nitrogen atom of at least one of the carboxamide groups bound to an acyclic carbon…

Heterocyclic inhibitors of the sodium channel

Life of this patent

Heterocyclic inhibitors of the sodium channel

Life of this patent

Abstract

Claims15