POLYCYCLIC THYROID HORMONE b RECEPTOR AGONIST AND USE THEREOF
AssigneeCascade Pharmaceuticals, Inc.
InventorsJingjing Shi, Yishuang Zhao, Zhenwei Zhang, Shengsheng Yang, Linpei Gong, Peng Wang, Xin Zhu, Zheng Zhang
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Abstract
Provided are a polycyclic thyroid hormone β receptor agonist and the use thereof. Specifically, the present invention relates to a compound as represented by formula (1) or a pharmaceutically acceptable form thereof, a pharmaceutical composition containing same, and a preparation method therefor and the use thereof. The compound or pharmaceutical composition can be used for the preparation of a drug for preventing, treating or alleviating diseases regulated by the thyroid hormone β receptor.
Claims20
A compound having a structure of formula (1) or a pharmaceutically acceptable form thereof:
- wherein
- A is
- R1 is H, halogen, —CN, —NH2, —NO2, —OH, or C1-6 alkyl, said C1-6 alkyl is optionally substituted with one or more substituents that are independently deuterium, halogen, —CN, —NH2, —NO2, or —OH;
- R2 and R3 are independently H, halogen, —CN, —NH2, —NO2, —OH, or C1-6 alkyl, said C1-6 alkyl is optionally substituted with one or more substituents that are independently halogen, —CN, —NH2, —NO2, or —OH;
- L is —(C1-4 alkylene)-, —(C1-4 alkylene)-O—, —(C1-4 alkylene)-S—, —(C1-4 alkylene)-NH—, —O—(C1-4 alkylene)-, —S—(C1-4 alkylene)-, —NH—(C1-4 alkylene)-, or —CH═CH—;
- said alkylene is optionally substituted with one or more substituents that are independently deuterium, halogen, —CN, —NH2, —NO2, or —OH;
- ring B is a benzene ring, a naphthalene ring, a furan ring, a thiophene ring, or a pyrrole ring;
- ring B is optionally substituted with one or more R4;
- each R4 is independently H, halogen, —CN, —NH2, —NO2, —OH, C1-6 alkyl, C1-6 alkoxy, 5- to 10-membered heteroaryl, C3-8 cycloalkenyl, or C3-8 cycloalkyl, said C1-6 alkyl, C1-6 alkoxy, 5- to 10-membered heteroaryl, or C3-8 cycloalkyl is optionally substituted with one or more substituents that are independently halogen, —CN, —NH2, —NO2, or —OH;
- X is —C(═O)NR5R6, —COOH, or
- R5 and R6 are independently H, —OH, —S(═O)2R7, C1-6 alkyl, C1-6 alkoxy, C6-10 aryl, or C3-8 cycloalkyl, said —S(═O)2R7, C1-6 alkyl, C1-6 alkoxy, C6-10 aryl, or C3-8 cycloalkyl is optionally substituted with one or more substituents that are independently deuterium, halogen, —CN, —NH2, —NO2, or —OH;
- R7 is H or C1-6 alkyl;
- and
- the pharmaceutically acceptable form is selected from the group consisting of a pharmaceutically acceptable salt, ester, stereoisomer, tautomer, solvate, nitrogen oxide, isotope-labelled compound, metabolite, and prodrug.
A compound or a pharmaceutically acceptable form thereof, wherein the compound is selected from the group consisting of:
- the pharmaceutically acceptable form is selected from the group consisting of a pharmaceutically acceptable salt, ester, stereoisomer, tautomer, solvate, nitrogen oxide, isotope-labelled compound, metabolite, and prodrug.
Dependencies are inferred from the claim text.