Benzimidazolone-based cinnamamide derivative as TRPV1 antagonist and pharmaceutical composition for treatment or prevention of pain containing same as active ingredient
AssigneeJmackem Co., Ltd
InventorsJeewoo Lee, Jihyae Ann
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Abstract
The present invention relates to a benzimidazolone-based cinnamamide derivative as a TRPV1 antagonist and a pharmaceutical composition for treating or preventing pain containing the same as an active ingredient. The example compounds provided in one aspect of the present invention block the TRPV1 activation caused by capsaicin, a TRPV1 receptor activator, but induce an appropriate inhibition of about 20% to 80% of pH, thereby the compounds have effects of alleviating pain and effectively reducing side effects such as abnormal body temperature.
Claims10
A compound represented by formula 1 below, a stereoisomer thereof, a solvate thereof, a hydrate thereof or a pharmaceutically acceptable salt thereof:
- wherein:
- X1 and X2 together form a pi bond;
- and
- is unsubstituted or substituted 5-6 membered heteroaryl containing at least one heteroatom selected from the group consisting of N, O and S, or unsubstituted or substituted phenyl,
- wherein the substituted 5-6 membered heteroaryl and the substituted phenyl are independently substituted with at least one substituent selected from the group consisting of:
- C1-7 straight or branched alkyl unsubstituted or substituted with at least one halogen or hydroxy group;
- C2-7 straight or branched alkynyl;
- C3-6 cycloalkyl unsubstituted or substituted with at least one C1-5 straight or branched alkyl;
- 5-6 membered heterocycloalkyl containing at least one heteroatom selected from the group consisting of N and O unsubstituted or substituted with at least one C1-5 straight or branched alkyl;
- —NR1R2;
- —OR3;
- —SR4;
- C6 aryl unsubstituted or substituted with at least one halogen or C1-5 straight or branched alkyl;
- and 5 membered heteroaryl containing at least one heteroatom selected from the group consisting of N, O and S,
- R1 and R2 are independently C1-5 straight or branched alkyl,
- R3 is C1-7 straight or branched alkyl unsubstituted or substituted with at least one halogen, C3-6 cycloalkyl, or C1-5 straight or branched alkyl substituted with C3-6 cycloalkyl unsubstituted or substituted with at least one methyl,
- R4 is C1-7 straight or branched alkyl unsubstituted or substituted with at least one halogen, C3-4 cycloalkyl, or C1-5 straight or branched alkyl substituted with C3-6 cycloalkyl unsubstituted or substituted with at least one methyl.
Dependencies are inferred from the claim text.