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US 2026/0226035 A1Published application
Thiochroman derivative and preparation method therefor and use thereof
AssigneeShanghai Institute of Materia Medica, Chinese Academy of Sciences
InventorsYushe YANG, Dan ZHANG, Zhengyu LU
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Abstract
A thiochroman derivative and a preparation method therefor and a use thereof are provided. The structure of the thiochroman derivative is as shown in general formula (I), and the definition of each substituent is as described in the description and the claims. The thiochroman derivative can be used as a selective estrogen receptor degrader and antagonist for treating estrogen receptor positive diseases.
Claims11
A compound represented by general formula (I), or a racemate, enantiomer, diastereomer, or mixture thereof, or pharmaceutically acceptable salt thereof:
- wherein,
- R1 is selected from OH, COOH, B(OH)2, halogen, C1-C6 alkyl, halogenated C1-C6 alkyl or C1-C6 alkoxy;
- R2 is selected from H, OH, COOH, halogen, cyano, C1-C6 alkyl, C1-C6 alkoxy, halogenated C1-C6 alkyl or hydroxy-substituted C1-C6 alkyl;
- or R1, R2 together with the connected benzene ring form a benzo 5-6 membered heteroaryl;
- X is selected from S, S(O)2 or O;
- ring A is selected from C3-C6 cycloalkyl, 5-8 membered heterocyclyl, C6-C10 aryl or 5-8 membered heteroaryl;
- each R3 is independently selected from hydrogen, halogen, cyano, C1-C6 alkylthio C1-C6 alkylCO—, C1-C6 alkylSO2—, amino, —NH(C1-C6 alkyl), —N(C1-C6 alkyl)(C1-C6 alkyl), —SO2NH2, —C(O)NH2, C1-C6 alkyl, C1-C6 alkoxy, halogenated C1-C6 alkyl, halogenated C1-C6 alkoxy or halogenated C1-C6 alkylthio;
- o is 0, 1, 2, 3, or 4;
- Y1, Y2 are independently selected from CR4 or N;
- each R4 is independently selected from hydrogen, halogen, cyano, C1-C6 alkylthio, C1-C6 alkylCO—, C1-C6 alkylSO2—, amino, —NH(C1-C6 alkyl), —N(C1-C6 alkyl)(C1-C6 alkyl), —SO2NH2, —C(O)NH2, C1-C6 alkyl, C1-C6 alkoxy, halogenated C1-C6 alkyl, halogenated C1-C6 alkoxy or halogenated C1-C6 alkylthio;
- m is 0, 1, 2, 3 or 4;
- Z1-Z2 is selected from O—Z2, NH—Z2, S—Z2, S(O)—Z2, S(O)2—Z2, O—(C1-C6 alkylene)-Z2, O-(halogenated C1-C6 alkylene)-Z2, NH—(C1-C6 alkylene)-Z2 or NH-(halogenated C1-C6 alkylene)-Z2;
- Z2, Z3 are independently selected from CH or N;
- n is 1, 2 or 3;
- R5 is C1-C6 alkyl, optionally substituted by one or more substituents selected from the group consisting of halogen, cyano, hydroxy, carboxyl, amino, methoxy or —SO2CH3;
- the premise is that when X is S or S(O)2, ring A is selected from C3-C6 cycloalkyl, 5-8 membered heterocyclyl, C6-C10 aryl or 5-8 membered heteroaryl;
- when X is O, ring A is selected from C3-C6 cycloalkyl, 5-8 membered heterocyclyl or 5-8 membered heteroaryl.
14 more elements
Dependencies are inferred from the claim text.