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US 12,162,851 B2Granted
Charged ion channel blockers and methods for use
AssigneeNocion Therapeutics, Inc.
InventorsBridget McCarthy Cole, James Lamond Ellis
Life of this patent
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Abstract
The invention provides compounds of Formula (I), or pharmaceutically acceptable salts thereof. The compounds, compositions, methods and kits of the invention are particularly useful for the treatment of itch and other dermal conditions.
Claims26
A compound represented by Formula (I):
- wherein:
- Y− is a pharmaceutically acceptable anion;
- RA, RB, and RC are each independently selected from H, D, halogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, ORI, CN, CF3, NRJRK, NRLC(O)RM, S(O)RN, S(O)2RN, SO2RORP, SO2NRQRR, SO3RS, CO2RT;
- C(O)RU, and C(O)NRVRW;
- each of RI, RJ, RK, RL, RM, RN, RO, RP, RQ, RR, RS, RT, RU, RV, and RW is independently selected from H, D, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl;
- RJ and RK or RV and RW or RQ and RR can also be taken together with the nitrogen to which they are attached to form a substituted or unsubstituted 5, 6, 7, or 8 membered ring;
- or
- RA, RB, and/or RC can be taken together with the phenyl ring to which they are attached can form a fused bicyclic or tricyclic ring system;
- R1, R2, R3, R4, R5, and R6 are independently selected from hydrogen, C1-C4 alkyl, cycloalkyl, C1-C4 heteroalkyl, aryl or heteroaryl;
- or R1, R2, R3, R4, R5, and/or R6 together with the carbon(s) to which they are attached form a substituted or unsubstituted cycloalkyl or a substituted or unsubstituted heterocyclic;
- n is 0, 1, 2, 3, 4 and 5;
- RF and RG together with the N+ form a ring selected from a substituted or unsubstituted ring selected from:
- wherein R7 is hydrogen or a substituted or unsubstituted alkyl, and
- RH is benzyl or substituted benzyl.
11 more elements
A compound represented by Formula (I):
- wherein:
- Y− is a pharmaceutically acceptable anion;
- R1, R2, R3, R4, R5, and R6 are independently selected from hydrogen, C1-C4 alkyl, C1-C4 heteroalkyl, aryl or heteroaryl;
- n is 0, 1, 2, 3, 4 and 5;
- and
- q is 3.
3 more elements
Dependencies are inferred from the claim text.