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US 2024/0270698 A2Published application
Novel pyrimidine derivative and use thereof
AssigneeKorea Research Institute of Chemical Technology
InventorsPil Ho KIM, Seong Hwan KIM
Life of this patent
Estimating the term…
Abstract
The present invention relates to a novel pyrimidine derivative and a use thereof. The pyrimidine derivative has excellent MLK3 inhibitory activity and LRRK2 inhibitory activity and thus can be utilized in a pharmaceutical composition for preventing or treating cancers, virus infectious diseases, Parkinson's disease, nonalcoholic fatty liver disease, and tuberculosis.
Claims16
A compound, represented by the following Chemical Formula 1, an optical isomer thereof, or a pharmaceutically acceptable salt thereof:
- wherein,
- R1 is at least one substituent selected from the group consisting of a substituted or unsubstituted C4-C12 aryl, a substituted or unsubstituted C4-C12 heterocycloalkyl, a substituted or unsubstituted C4-C12 heterobicycloalkyl, a substituted or unsubstituted C4-C12 cycloalkyl, and a substituted or unsubstituted C4-C12 heteroaryl,
- wherein the substituted aryl, heterocycloalkyl, heterobicycloalkyl, cycloalkyl, or heteroaryl has as a substituent at least one selected from the group consisting of a hydrogen atom,
- X is at least one selected from the group consisting of a hydrogen atom, halogen, hydroxy, a C1-C6 alkyl, and a C1-C6 alkoxy;
- R2 is at least one substituent selected from the group consisting of a hydrogen atom, a C1-C4 alkyl, and acetyl;
- and
- R3 is one substituent selected from the group consisting of a substituted or unsubstituted C4-C12 aryl, a substituted or unsubstituted C4-C12 heterobicycloalkyl, and a substituted or unsubstituted C4-C12 heterobicycloaryl,
- wherein the substituted aryl, heterobicycloalkyl, or heterobicycloaryl has as a substituent at least one selected from the group consisting of a hydrogen atom, halogen, cyano, aldehyde, CF3, SH, trifluoroketone, a C1-C6 alkyl, a C1-C6 alkoxy, a substituted or unsubstituted C4-C12 cycloalkyl, a substituted or unsubstituted C4-C12 heterocycloalkyl, a substituted or unsubstituted C4-C12 aryl, and a substituted or unsubstituted C4-C12 heteroaryl, and
- wherein the substituted cycloalkyl, heterocycloalkyl, aryl, or heteroaryl has as a substituent at least one selected from the group consisting of a hydrogen atom, halogen, NH2, hydroxy, CF3, NO2, methanesulfonate, Boc(tert-butoxycarbonyl), methylketone, aldehyde, a C1-C6 hydroxyalkyl, a C1-C6 alkyloxy, piperazine, and a C1-C6 alkyl.
6 more elements
A compound represented by any one of the following Chemical Formulas 2 to 9, an optical isomer thereof, or pharmaceutically acceptable salt thereof:
- wherein,
- R1 is a substituted or unsubstituted C4-C12 aryl,
- wherein the substituted aryl has as a substituent at least one selected from the group consisting of a hydrogen atom,
- X is at least one selected from the group consisting of a hydrogen atom, halogen, hydroxy, a C1-C6 alkyl, and a C1-C6 alkoxy;
- R2 is at least one selected from the group consisting of a hydrogen atom, a C1-C4 alkyl, and acetyl;
- R4 is at least one selected from the group consisting of a hydrogen atom, halogen, cyano, aldehyde, CF3, SH, trifluoroketone, C1-C6 alkyl, C1-C6 alkoxy, a substituted or unsubstituted C4-C12 cycloalkyl, a substituted or unsubstituted C4-C12 heterocycloalkyl, a substituted or unsubstituted C4-C12 aryl, and a substituted or unsubstituted C4-C12 heteroaryl,
- wherein the substituted cycloalkyl, heterocycloalkyl, aryl, or heteroaryl has as a substituent at least one selected from the group consisting of a hydrogen atom, halogen, NH2, hydroxy, CF3, NO2, methanesulfonate, Boc(tert-butoxycarbonyl), methylketone, aldehyde, a C1-C6 hydroxyalkyl, a C1-C6 alkyloxy, piperazine, and a C1-C6 alkyl;
- and
- R5 is selected from a hydrogen atom, halogen, a C1-C4 alkyl, a C1-C4 alkoxy, hydroxy, a thio C1-C4 alkyl, and amino.
6 more elements
A compound represented by the following Chemical Formula 10, an optical isomer thereof, or a pharmaceutically acceptable salt thereof:
- wherein,
- R1 is a substituted or unsubstituted C4-C12 aryl,
- wherein the substituted aryl has as a substituent at least one selected from the group consisting of a hydrogen atom,
- X is at least one substituent selected from the group consisting of a hydrogen atom, halogen, hydroxy, a C1-C6 alkyl, and a C1-C6 alkoxy;
- R2 is at least one substituent selected from the group consisting of a hydrogen atom, a C1-C4 alkyl, and acetyl;
- R6 is at least one substituent selected from the group consisting of a hydrogen atom, a C1-C6 alkyl, a halo C1-C6 alkylketone, trifluoroketone, acetyl, and Boc(tert-butoxycarbonyl);
- R7 is at least one substituent selected from the group consisting of a hydrogen atom, a C1-C6 alkyl, halogen, and hydroxy;
- n is an integer of 0 or 1;
- and
- m is an integer of 0, 1, or 2.
7 more elements
Dependencies are inferred from the claim text.