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US 12,600,716 B2Granted
Compounds for modulating activity of FXR and uses thereof
AssigneeGannex Pharma Co., Ltd.
InventorsBailing Yang, Gudmundsson Kristjan, Liuyu Dong, James Chen
Life of this patent
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Abstract
Provided are a compound for modulating the activity of FXR having a structure of formula (I), a pharmaceutically acceptable salt, an ester or a stereoisomer thereof.
Claims19
A compound for modulating the activity of FXR having a structure of formula (I), or a pharmaceutically acceptable salt, an ester or a stereoisomer thereof:
- wherein:
- R1, R2 and R3 are independently selected from H, halogen, unsubstituted or halogen substituted C1-6 alkyl and unsubstituted or halogen substituted C1-6 alkoxy, provided that at least one of R1, R2 and R3 is not hydrogen, R0 is selected from unsubstituted or halogen substituted C1-6 alkyl, C3-6 cycloalkyl and C4-7 alkylcycloalkyl;
- X1 and X2 are independently selected from H and halogen;
- moiety —O—Z attaches to the naphthalene ring, wherein Z is a residue selected from 5-10 membered aryl and 5-10 membered heteroaryl optionally having one or more hetero atoms selected from N, O and S, wherein the 5-10 membered aryl or 5-10 membered heteroaryl is substituted by R4 and is optionally further substituted by R5;
- wherein R4 is selected from —COOH, —CH2COOH, —NHSO2CF3, —SO2NH—C1-6 alkyl, —SO3H, —CONHSO2—C1-6 alkyl, —CONHSO2—C3-6 cycloalkyl, —CONHSO2-5-10 membered aryl and —CONHSO2-5-10 membered aryl substituted by C1-6 alkyl at the aryl, and wherein R5 is selected from H, C1-6 alkyl, halogen, C1-6 haloalkyl, —O—(C1-6 alkyl) and —NH—(C1-6 alkyl).
2 more elements
Dependencies are inferred from the claim text.