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US 12,378,268 B2Granted
Heterocyclic THR-β receptor agonist compound and preparation method and use therefor
AssigneeHepagene Therapeutics (HK) Limited
InventorsShanghai Yu, Ben Li
Life of this patent
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Abstract
A chemical compound shown in formula (I) below and an isomer thereof or a pharmaceutically acceptable salt thereof. The compound improves THR-β agonistic activity while also improving selectivity for THR-α, thereby improving pharmaceutical quality.
Claims24
A compound shown in formula (I) or a stereoisomer thereof or a pharmaceutically acceptable salt thereof,
- wherein
- R1 and R2 are each independently selected from a halogen atom or a C1-6 alkyl group;
- R3 and R4 are each independently selected from hydrogen, a C1-6 alkyl group, an unsubstituted phenyl group, a phenyl group substituted with at least one substituent selected from a halogen atom, a trifluoromethyl group, a C1-6 alkyl group, a C1-6 alkoxyl group or a cyano group, an unsubstituted naphthyl group, a naphthyl group substituted with at least one substituent selected from a halogen atom, a trifluoromethyl group, a C1-6 alkyl group, a C1-6 alkoxyl group or a cyano group,
- or R3, R4, and adjacent
- jointly form the following six-membered ring
- wherein V is an unsubstituted five-to ten-membered aryl group, a five-to ten-membered aryl group substituted with at least one substituent selected from a halogen atom, a trifluoromethyl group, a C1-6 alkyl group, a C1-6 alkoxyl group or a cyano group, an unsubstituted five-to ten-membered heteroaryl group containing 1 or 2 heteroatoms selected from N, S and O, or a five-to ten-membered heteroaryl group that is substituted with at least one substituent selected from a halogen atom, a trifluoromethyl group, a
- C1-6 alkyl group, a C1-6 alkoxyl group or a cyano group and that contains one or two heteroatoms selected from N, S or O;
- R5 is selected from H or a C1-6 alkyl group;
- R6, R7, and R5 are each independently a C1-6 alkyl group;
- X is selected from —O— or —CH2—;
- Y is selected from —O— or —CH2—;
- Z and Z′ are each independently selected from —O— or —NH—;
- L is selected from —O—, —S— or —CH2—;
- and
- n is 1, 2 or 3;
- wherein the halogen atom is selected from F, Cl or Br.
13 more elements
Dependencies are inferred from the claim text.