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US 12,630,536 B2Granted
Cyanotriazine derivative, preparation method therefor, and application thereof
AssigneeChengdu FANXI Biopharma Co., Ltd.
InventorsXiaoyu Liu, Niefang Yu, Xin Chen, Hao Li
Life of this patent
Estimating the term…
Abstract
A compound represented by structural formula (I) and a pharmaceutically acceptable salt thereof and a pharmaceutical composition comprising the compound or the pharmaceutically acceptable salt thereof, can be used for treating diseases such as obesity, hyperlipidemia, hypercholesterolemia, and diabetes and also for treating other diseases such as NASH, atherosclerosis, cardiovascular diseases, hypothyroidism, thyroid cancer and other related disorders and diseases
Claims7
A compound with a structure represented by formula (I) or a pharmaceutically acceptable salt, a tautomer, a stereoisomer, a hydrate, or an isotopic derivative thereof:
- structural formula (I)
- wherein,
- R1 is selected from:
- H, —CN, —NO2, —CF3, —OCF3, —CO2H, —OH, ethynyl, halogen, amino, alkyl, alkenyl, haloalkyl, haloalkenyl, heteroalkyl, heterocycloalkyl, arylalkyl, cycloalkyl, aryl, heterocycloarylalkyl, heterocycloalkenyl, alkoxy, alkoxyalkyl, alkenyloxy, alkynyl, alkylalkynyl, alkynyloxy, alkylalkynyloxy, alkynyloxy, alkylamino, aminoalkyl, alkylaminocarbonyl, sulfonyl, alkylsulfonyl, alkylsulfinyl, aminosulfonyl, and acyl;
- and wherein the ethynyl, amino, alkyl, alkenyl, haloalkyl, haloalkenyl, heteroalkyl, heterocycloalkyl, arylalkyl, cycloalkyl, aryl, heterocycloarylalkyl, heterocycloalkenyl, alkoxy, alkoxyalkyl, alkenyloxy, alkynyl, alkylalkynyl, alkynyloxy, alkylalkynyloxy, alkynyloxy, alkylamino, aminoalkyl, alkylaminocarbonyl, sulfonyl, alkylsulfonyl, alkylsulfinyl, aminosulfonyl, and acyl may be substituted by one or more substituents-selected from the group consisting of halogen, —CF3, alkyl, alkenyl, alkynyl, hydroxyl, hydroxyalkyl, alkoxy, alkoxyalkyl, amino, alkylamino, and cycloalkylamino;
- R2 is selected from:
- H, alkyl, alkenyl, haloalkyl, haloalkenyl, heteroalkyl, heterocycloalkyl, arylalkyl, cycloalkyl, aryl, heterocycloaryl, heterocycloarylalkyl, heterocycloalkenyl, alkoxy, alkoxyalkyl, alkylamino, alkylaminocarbonyl, alkynyl, alkylalkynyl, alkynyloxy, alkylalkynyloxy, sulfonyl, alkylsulfonyl, alkylsulfinyl, and aminosulfonyl;
- and wherein the alkyl, alkenyl, haloalkyl, haloalkenyl, heteroalkyl, heterocycloalkyl, arylalkyl, cycloalkyl, aryl, heterocycloaryl, heterocycloarylalkyl, heterocycloalkenyl, alkoxy, alkoxyalkyl, alkylamino, alkylaminocarbonyl, alkynyl, alkylalkynyl, alkynyloxy, alkylalkynyloxy, sulfonyl, alkylsulfonyl, alkylsulfinyl, and aminosulfonyl may be substituted by one or more substituents selected from the group consisting of halogen, —CF3, alkyl, alkenyl, alkynyl, hydroxyl, hydroxyalkyl, alkoxy, alkoxyalkyl, amino, alkylamino, and cycloalkylamino;
- R3 is selected from:
- H, —CN, —NO2, —CF3, —OCF3, —CO2H, —OH, halogen, amino, alkyl, alkoxy, alkoxyalkyl, heteroalkyl, heterocycloalkyl, arylalkyl, cycloalkyl, heterocycloarylalkyl, heterocycloalkenyl, alkenyloxy, alkynyl, alkylalkynyl, alkynyloxy, alkylalkynyloxy, alkylamino, aminoalkyl, and alkylaminocarbonyl;
- and wherein the amino, alkyl, alkoxy, alkoxyalkyl, heteroalkyl, heterocycloalkyl, arylalkyl, cycloalkyl, heterocycloarylalkyl, heterocycloalkenyl, alkenyloxy, alkynyl, alkylalkynyl, alkynyloxy, alkylalkynyloxy, alkylamino, aminoalkyl, and alkylaminocarbonyl may be substituted by one or more substituents are selected from the group consisting of halogen, —CF3, alkyl, alkenyl, alkynyl, hydroxyl, hydroxyalkyl, alkoxy, alkoxyalkyl, amino, alkylamino, and cycloalkylamino;
- R4 and R5 are each Br, and R4 and R5 are respectively attached to C3- and C5-positions on a corresponding benzene ring;
- R6 is —CN;
- and
- X is selected from:
- covalent bond, —O—, —S—, —NH—, —SO2—, —CONH— or —(CH2)q-, X— is attached to carbon atoms on C4-, C5-, C6- and C7-positions of a benzimidazole ring, and q is 0, 1, 2, and 3.
13 more elements
A compound with a structure represented by formula (I) or a pharmaceutically acceptable salt, a tautomer, a stereoisomer, a hydrate or an isotopic derivative thereof:
- structural formula (I)
- wherein,
- R1 is selected from:
- H, —CN, —NO2, —CF3, —OCF3, —CO2H, —OH, ethynyl, halogen, amino, alkyl, alkenyl, haloalkyl, haloalkenyl, heteroalkyl, heterocycloalkyl, arylalkyl, cycloalkyl, aryl, heterocycloarylalkyl, heterocycloalkenyl, alkoxy, alkoxyalkyl, alkenyloxy, alkynyl, alkylalkynyl, alkynyloxy, alkylalkynyloxy, alkynyloxy, alkylamino, aminoalkyl, alkylaminocarbonyl, sulfonyl, alkylsulfonyl, alkylsulfinyl, aminosulfonyl, and acyl;
- and wherein the ethynyl, amino, alkyl, alkenyl, haloalkyl, haloalkenyl, heteroalkyl, heterocycloalkyl, arylalkyl, cycloalkyl, aryl, heterocycloarylalkyl, heterocycloalkenyl, alkoxy, alkoxyalkyl, alkenyloxy, alkynyl, alkylalkynyl, alkynyloxy, alkylalkynyloxy, alkynyloxy, alkylamino, aminoalkyl, alkylaminocarbonyl, sulfonyl, alkylsulfonyl, alkylsulfinyl, aminosulfonyl, and acyl may be substituted by one or more substituents selected from the group consisting of halogen, —CF3, alkyl, alkenyl, alkynyl, hydroxyl, hydroxyalkyl, alkoxy, alkoxyalkyl, amino, alkylamino, and cycloalkylamino;
- R2 is selected from:
- H, alkyl, alkenyl, haloalkyl, haloalkenyl, heteroalkyl, heterocycloalkyl, arylalkyl, cycloalkyl, aryl, heterocycloaryl, heterocycloarylalkyl, heterocycloalkenyl, alkoxy, alkoxyalkyl, alkylamino, alkylaminocarbonyl, alkynyl, alkylalkynyl, alkynyloxy, alkylalkynyloxy, sulfonyl, alkylsulfonyl, alkylsulfinyl, and aminosulfonyl;
- and wherein the alkyl, alkenyl, haloalkyl, haloalkenyl, heteroalkyl, heterocycloalkyl, arylalkyl, cycloalkyl, aryl, heterocycloaryl, heterocycloarylalkyl, heterocycloalkenyl, alkoxy, alkoxyalkyl, alkylamino, alkylaminocarbonyl, alkynyl, alkylalkynyl, alkynyloxy, alkylalkynyloxy, sulfonyl, alkylsulfonyl, alkylsulfinyl, and aminosulfonyl may be substituted by one or more substituents selected from the group consisting of halogen, —CF3, alkyl, alkenyl, alkynyl, hydroxyl, hydroxyalkyl, alkoxy, alkoxyalkyl, amino, alkylamino, and cycloalkylamino;
- R3 is selected from:
- H, —CN, —NO2, —CF3, —OCF3, —CO2H, —OH, halogen, amino, alkyl, alkoxy, alkoxyalkyl, heteroalkyl, heterocycloalkyl, arylalkyl, cycloalkyl, heterocycloarylalkyl, heterocycloalkenyl, alkenyloxy, alkynyl, alkylalkynyl, alkynyloxy, alkylalkynyloxy, alkylamino, aminoalkyl, and alkylaminocarbonyl;
- and wherein the amino, alkyl, alkoxy, alkoxyalkyl, heteroalkyl, heterocycloalkyl, arylalkyl, cycloalkyl, heterocycloarylalkyl, heterocycloalkenyl, alkenyloxy, alkynyl, alkylalkynyl, alkynyloxy, alkylalkynyloxy, alkylamino, aminoalkyl, and alkylaminocarbonyl may be substituted by one or more substituents selected from the group consisting of halogen, —CF3, alkyl, alkenyl, alkynyl, hydroxyl, hydroxyalkyl, alkoxy, alkoxyalkyl, amino, alkylamino, and cycloalkylamino;
- R6 is —CN;
- X is selected from:
- covalent bond, —O—, —S—, —NH—, —SO2—, —CONH— or —(CH2)q-, X— is attached to carbon atoms on C4-, C5-, C6- and C7-positions of a benzimidazole ring, and q is 0, 1, 2, and 3;
- and
- R4 and R5 are each difluoromethyl, and R4 and R5 are respectively attached to C3- and C5-positions on a corresponding benzene ring.
13 more elements
A compound with a structure represented by formula (I) or a pharmaceutically acceptable salt, a tautomer, a stereoisomer, a hydrate or an isotopic derivative thereof:
- structural formula (I)
- wherein,
- R1 is selected from:
- H, —CN, —NO2, —CF3, —OCF3, —CO2H, —OH, ethynyl, halogen, amino, alkyl, alkenyl, haloalkyl, haloalkenyl, heteroalkyl, heterocycloalkyl, arylalkyl, cycloalkyl, aryl, heterocycloarylalkyl, heterocycloalkenyl, alkoxy, alkoxyalkyl, alkenyloxy, alkynyl, alkylalkynyl, alkynyloxy, alkylalkynyloxy, alkynyloxy, alkylamino, aminoalkyl, alkylaminocarbonyl, sulfonyl, alkylsulfonyl, alkylsulfinyl, aminosulfonyl, and acyl;
- and wherein the ethynyl, amino, alkyl, alkenyl, haloalkyl, haloalkenyl, heteroalkyl, heterocycloalkyl, arylalkyl, cycloalkyl, aryl, heterocycloarylalkyl, heterocycloalkenyl, alkoxy, alkoxyalkyl, alkenyloxy, alkynyl, alkylalkynyl, alkynyloxy, alkylalkynyloxy, alkynyloxy, alkylamino, aminoalkyl, alkylaminocarbonyl, sulfonyl, alkylsulfonyl, alkylsulfinyl, aminosulfonyl, and acyl may be substituted by one or more substituents selected from the group consisting of halogen, —CF3, alkyl, alkenyl, alkynyl, hydroxyl, hydroxyalkyl, alkoxy, alkoxyalkyl, amino, alkylamino, and cycloalkylamino;
- R2 is selected from:
- H, alkyl, alkenyl, haloalkyl, haloalkenyl, heteroalkyl, heterocycloalkyl, arylalkyl, cycloalkyl, aryl, heterocycloaryl, heterocycloarylalkyl, heterocycloalkenyl, alkoxy, alkoxyalkyl, alkylamino, alkylaminocarbonyl, alkynyl, alkylalkynyl, alkynyloxy, alkylalkynyloxy, sulfonyl, alkylsulfonyl, alkylsulfinyl, and aminosulfonyl;
- and wherein the alkyl, alkenyl, haloalkyl, haloalkenyl, heteroalkyl, heterocycloalkyl, arylalkyl, cycloalkyl, aryl, heterocycloaryl, heterocycloarylalkyl, heterocycloalkenyl, alkoxy, alkoxyalkyl, alkylamino, alkylaminocarbonyl, alkynyl, alkylalkynyl, alkynyloxy, alkylalkynyloxy, sulfonyl, alkylsulfonyl, alkylsulfinyl, and aminosulfonyl may be substituted by one or more substituents selected from the group consisting of halogen, —CF3, alkyl, alkenyl, alkynyl, hydroxyl, hydroxyalkyl, alkoxy, alkoxyalkyl, amino, alkylamino, and cycloalkylamino;
- R3 is selected from:
- H, —CN, —NO2, —CF3, —OCF3, —CO2H, —OH, halogen, amino, alkyl, alkoxy, alkoxyalkyl, heteroalkyl, heterocycloalkyl, arylalkyl, cycloalkyl, heterocycloarylalkyl, heterocycloalkenyl, alkenyloxy, alkynyl, alkylalkynyl, alkynyloxy, alkylalkynyloxy, alkylamino, aminoalkyl, and alkylaminocarbonyl;
- and wherein the amino, alkyl, alkoxy, alkoxyalkyl, heteroalkyl, heterocycloalkyl, arylalkyl, cycloalkyl, heterocycloarylalkyl, heterocycloalkenyl, alkenyloxy, alkynyl, alkylalkynyl, alkynyloxy, alkylalkynyloxy, alkylamino, aminoalkyl, and alkylaminocarbonyl may be substituted by one or more substituents selected from the group consisting of halogen, —CF3, alkyl, alkenyl, alkynyl, hydroxyl, hydroxyalkyl, alkoxy, alkoxyalkyl, amino, alkylamino, and cycloalkylamino;
- R6 is —CN;
- X is selected from:
- covalent bond, —O—, —S—, —NH—, —SO2—, —CONH— or —(CH2)q-, X— is attached to carbon atoms on C4-, C5-, C6- and C7-positions of a benzimidazole ring, and q is 0, 1, 2, and 3;
- and
- R4 and R5 are each trifluoromethyl, and R4 and R5 are respectively attached to C3- and C5-positions on a corresponding benzene ring.
13 more elements
A compound which is selected from the following compounds and pharmaceutically acceptable salts thereof:
Dependencies are inferred from the claim text.