Local anesthetics with selective-sensory nerve blockade
AssigneeChildren's Medical Center Corporation
InventorsDaniel S. Kohane, Yueqin Zheng
Life of this patent
Estimating the term…
Abstract
Provided herein are compounds that are local anesthetics and useful for inducing selective sensory nerve blockade. Also provided are pharmaceutical compositions and kits comprising the compounds, and methods of inducing selective sensory nerve blockade by administering the compounds and/or compositions to a subject.
Claims32
A compound of Formula (II):
- wherein:
- R1 is substituted or unsubstituted alkyl;
- R2 is substituted or unsubstituted alkyl;
- R3 is hydrogen, or substituted or unsubstituted alkyl;
- R4 is hydrogen, substituted or unsubstituted alkyl, or is joined with R5 or R6 to form a heterocyclyl ring;
- R5 is substituted or unsubstituted alkyl, or is joined with R4 to form a heterocyclyl ring;
- R6 is substituted or unsubstituted alkyl, or is joined with R4 to form a heterocyclyl ring;
- R7 is hydrogen, substituted or unsubstituted alkyl, or halogen;
- R8 is substituted or unsubstituted alkyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted heteroaryl, or substituted or unsubstituted aryl;
- A is O, S, or NRA;
- RA is hydrogen or substituted or unsubstituted alkyl;
- X− is a counterion;
- and
- n is 1, 2, 3, 4, 5, or 6;
- provided that if A is NRA, then R3 is H;
- R8 is not substituted or unsubstituted aryl;
- and the compound is not:
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A method of inducing selective sensory nerve blockade, the method comprising administering to a subject in need thereof, a compound of Formula (I):
- wherein:
- R1 is substituted or unsubstituted alkyl;
- R2 is substituted or unsubstituted alkyl;
- R3 is hydrogen, or substituted or unsubstituted alkyl;
- R4 is hydrogen, substituted or unsubstituted alkyl, or is joined with R5 or R6 to form a heterocyclyl ring;
- R5 is substituted or unsubstituted alkyl, or is joined with R4 or R6 to form a heterocyclyl ring;
- R6 is substituted or unsubstituted alkyl, or is joined with R4 or R5 to form a heterocyclyl ring;
- R7 is hydrogen, substituted or unsubstituted alkyl, or halogen;
- R9 is —(C═O)-A-R8 or -A1-(C═O)—R10;
- R8 is substituted or unsubstituted alkyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted heteroaryl, or substituted or unsubstituted aryl;
- R10 is substituted or unsubstituted alkyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted heteroaryl, or substituted or unsubstituted aryl;
- A is O, S, or NRA;
- A1 is O, S, or NRA;
- RA is hydrogen or substituted or unsubstituted alkyl;
- X− is a counterion;
- and
- n is 1, 2, 3, 4, 5, or 6.
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Dependencies are inferred from the claim text.