Substituted benzimidazole derivative and use thereof
AssigneeChengdu FANXI Biopharma Co., Ltd.
InventorsNiefang Yu, Xin Chen, Hao Li, Xiaoyu Liu
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Abstract
The present invention relates to a substituted benzimidazole derivative as represented by formula (I) and a pharmaceutically acceptable salt, a polymorph, a tautomer, a stereoisomer, a hydrate, a solvate or an isotopic variant of the derivative. The compound is a PPAR α and/or PPAR δ agonist, therefore the compound can be used for treating and/or preventing diseases associated with by PPAR α and/or PPAR δ, such as non-alcoholic steatohepatitis, Duchenne muscular dystrophy syndrome, Alzheimer's disease, tumors and PBC (primary biliary cholangitis)
Claims13
A compound represented by formula (I) or a pharmaceutically acceptable salt, polymorph, tautomer, stereoisomer, hydrate, solvate or isotopic variant thereof:
- wherein,
- R1 is selected from H, —CN, —NO2, —CF3, —OCF3, —CO2H, OH, halogen, amino, alkyl, alkenyl, haloalkyl, haloalkenyl, heteroalkyl, heterocycloalkyl, arylalkyl, cycloalkyl, aryl, heterocycloaryl, heterocycloarylalkyl, heterocycloalkyl, heterocycloalkenyl, alkoxy, alkoxyalkyl, alkenyloxy, alkynyloxy, amino, alkylamino, aminoalkyl, alkylaminocarbonyl, sulfonyl, alkylsulfonyl, alkylsulfinyl, aminosulfonyl, or acyl, each of which is un-substituted or substituted with one or more substituents selected from the group consisting of halogen, —CF3, alkyl, alkenyl, alkynyl, hydroxyl, hydroxyalkyl, alkoxy, and alkoxyalkyl;
- R2 is selected from H, —CN, —NO2, —CF3, —OCF3, —CO2H, OH, —CONHR5, —CSNHR6, —SR7, halogen, amino, alkyl, alkenyl, haloalkyl, haloalkenyl, heteroalkyl, heterocycloalkyl, arylalkyl, cycloalkyl, aryl, heterocycloaryl, heterocycloarylalkyl, heterocycloalkyl, heterocycloalkenyl, alkoxy, alkoxyalkyl, alkylamino, alkylaminocarbonyl, sulfonyl, alkylsulfonyl, alkylsulfinyl, or aminosulfonyl, each of which is un-substituted or substituted with one or more substituents selected from the group consisting of halogen, —CF3, alkyl, alkenyl, alkynyl, hydroxy, hydroxyalkyl, alkoxy, and alkoxyalkyl;
- R3 is selected from H, —CN, —NO2, —CF3, —OCF3, —CO2H, OH, —SR7, halogen, amino, alkyl, alkoxy, alkoxyalkyl, heteroalkyl, heterocycloalkyl, arylalkyl, cycloalkyl, heterocycloarylalkyl, heterocycloalkyl, heterocycloalkenyl, alkenyloxy, alkynyloxy, alkylamino, aminoalkyl, or alkylaminocarbonyl, each of which is un-substituted or substituted with one or more substituents selected from the group consisting of halogen, —CF3, alkyl, alkenyl, alkynyl, hydroxy, hydroxyalkyl, alkoxy, and alkoxyalkyl;
- R4 is selected from H, —CN, —NO2, —CF3, —OCF3, —SR7, halogen, amino, alkyl, alkoxy, alkoxyalkyl, heteroalkyl, heterocycloalkyl, arylalkyl, cycloalkyl, heterocycloarylalkyl, heterocycloalkyl, heterocycloalkenyl, alkenyloxy, alkynyloxy, alkylamino, aminoalkyl, alkylaminocarbonyl, each of which is un-substituted or substituted with one or more substituents selected from the group consisting of halogen, —CF3, alkyl, alkenyl, alkynyl, hydroxy, hydroxyalkyl, alkoxy, and alkoxyalkyl;
- R5 is selected from H, alkyl, heterocycloalkyl, arylalkyl, cycloalkyl, aryl, heterocycloaryl, heterocycloarylalkyl, heterocycloalkyl, or heterocycloalkenyl;
- R6 is selected from H, alkyl, heterocycloalkyl, arylalkyl, cycloalkyl, aryl, heterocycloaryl, heterocycloarylalkyl, heterocycloalkyl, or heterocycloalkenyl;
- R7 is selected from H, alkyl, heterocycloalkyl, cycloalkyl, aryl, heterocycloaryl, heterocycloalkyl, or heterocycloalkenyl;
- m, n and p are each independently an integer selected from 0-6;
- and
- X, Y and Z are each independently selected from —O—, —S—, —NH—, —SO2—, —CONH— or (CH2)q, wherein q is an integer selected from 1-4.
Dependencies are inferred from the claim text.