Novel indenone derivatives and uses thereof
AssigneeAmyloid Solution Inc.
InventorsSeong Muk KIM, Hye Ju KIM
Life of this patent
Estimating the term…
Abstract
The present disclosure relates to a novel indenone derivative or an isomer or pharmaceutically acceptable salt thereof, and use thereof. The indenone derivative according to the present disclosure may be effectively used for the prevention or treatment of a neurodegenerative brain disease by (i) inhibiting amyloid-beta aggregation and/or disaggregating amyloid-beta aggregates, (ii) inhibiting tau protein aggregation and/or disaggregating tau protein aggregates, and/or (iii) inhibiting the hyperphosphorylation of tau protein.
Claims12
A compound of Formula 1 below or an isomer or pharmaceutically acceptable salt thereof:
- wherein, in Formula 1,
- X is a direct bond or O;
- Y is O or S;
- n is an integer from 0 to 5;
- m is an integer from 1 to 5;
- R1 is halogen, C1-6 alkyl, C6-10 aryl, —C1-6 alkyl-C6-10 aryl, or 5- or 6-membered heteroaryl, wherein the C1-6 alkyl, the C6-10 aryl, the —C1-6 alkyl-C6-10 aryl, and the 5- or 6-membered heteroaryl may each independently be unsubstituted or substituted with 1 to 4 halogens, hydroxy, CN, —NH2, —CF3, C1-6 alkyl, —C1-6 alkyl-CN, —O—C1-6 alkyl, —NH—C1-6 alkyl, or —N(C1-6 alkyl)2;
- R2 is 5- or 6-membered heteroaryl, wherein the 5- or 6-membered heteroaryl may be unsubstituted or substituted with 1 to 4 halogens, —CF3, or C1-6 alkyl;
- R3 is C6-10 aryl, 5- or 6-membered heteroaryl, or 5- to 10-membered heterocyclyl, wherein the C6-10 aryl, the 5- or 6-membered heteroaryl, and the 5- to 10-membered heterocyclyl may each independently be unsubstituted or substituted with 1 to 4 halogens, hydroxy, CN, —NH2, —CF3, C1-6 alkyl, —C1-6 alkyl-CN, —O—C1-6 alkyl, —NH—C1-6 alkyl, or —N(C1-6 alkyl)2;
- and
- the heteroaryl is an aromatic heterocycle containing 1 to 4 heteroatoms selected from N, O, and S, and the heterocyclyl is an aliphatic heterocycle containing 1 to 4 heteroatoms selected from N, O, and S.
10-12. (canceled)
14-17. (canceled)
Dependencies are inferred from the claim text.