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US 10,934,263 B2Granted
Charged ion channel blockers and methods for use
AssigneeNocion Therapeutics, Inc.
InventorsBridget McCarthy Cole, James Lamond Ellis
Life of this patent
Estimating the term…
Abstract
The invention provides compounds of Formula (I), or pharmaceutically acceptable salts thereof: The compounds, compositions, methods and kits of the invention are useful for the treatment of pain, cough, itch, and neurogenic inflammation.
Claims20
A compound represented by Formula (I)
- wherein:
- Y− is a pharmaceutically acceptable anion;
- RF and RG together with the N+ to which they are attached form a pyridinium ring substituted by one or more substituents, wherein at least one of said substituents is selected from the group consisting of a substituted or unsubstituted C3-C6 cycloalkyl, substituted and unsubstituted 3- to 15-membered heterocyclyl, a substituted or unsubstituted phenyl, alkoxy, or CO2R2A, wherein R2A is selected from H, D, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl;
- RA and RB are each independently selected from halogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, nitrile, ORI, NRJRK, NRLC(O)RM, CO2RT, C(O)RU, and C(O)NRVRW;
- RC is selected from H, D, halogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, nitrile, ORI, NRJRK, NRLC(O)RM, CO2RT, C(O)RU, and C(O)NRVRW;
- or RB and vicinal RC together with the carbon atoms to which they are attached form a substituted or unsubstituted 3-7-membered cycloalkyl or a substituted or unsubstituted aryl;
- each of RI, RJ, RK, RL, RM, RT, RU, RV, and RW is independently selected from H, D, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, or substituted or unsubstituted alkynyl;
- X is —NRZC(O)—;
- RZ is selected from H, D, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl;
- and
- each of RD and RE is independently selected from H, D, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, cycloalkyl, aryl, or heteroaryl;
- or RD and RE together with the carbon to which they are attached form a substituted or unsubstituted C3-C7 cycloalkyl or a substituted or unsubstituted heterocyclic ring;
- or RD and RZ together with the carbon and the —N—C(O)— to which they are attached form an optionally substituted 5-8-membered lactam.
10 more elements
Dependencies are inferred from the claim text.