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US 12,312,324 B2Granted
Fluorine-containing substituted benzothiophene compound, and pharmaceutical composition and application thereof
AssigneeShanghai Institute of Materia Medica, Chinese Academy of Sciences
InventorsAo Zhang, Meiyu Geng, Chunyong Ding, Zuoquan Xie, Jian Ding, Yan Zhang, Ancheng Shen, Xiyuan Wang
Life of this patent
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Abstract
A fluorine-containing substituted benzothiophene compound and a pharmaceutical composition and an application thereof are described. The compound has the structure as shown in formula (I), in which the definitions of each group and substituent are as described in the description. A preparation method of the compound and an anti-tumor application thereof are also described.
Claims10
A compound of formula I, or its isomer, prodrug, solvate, hydrate or pharmaceutically acceptable salt thereof,
- wherein,
- R1 and R2 are independently selected from the substituted or unsubstituted group consisting of halogen, amino, hydroxyl, carboxyl, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C3-C8 cycloalkyl, C1-C6 alkoxy, C3-C8 cycloalkoxy, 3-8 membered heterocycloalkyl containing 1 to 3 heteroatoms selected from N, O or S, 3-8 membered heterocycloalkoxy containing 1 to 3 heteroatoms selected from N, O or S, C6-C10 aryl, and 3-10 membered heteroaryl containing 1 to 3 heteroatoms selected from N, O or S;
- or R1 and R2 together with the carbon atoms to which they are attached form a 5-14 membered heterocyclic group;
- the substituted in R1 and R2 refers to be independently substituted by one or more substituents selected from the group consisting of halogen, amino, hydroxy, carboxy, C1-C6 alkyl, C3-C8 cycloalkyl, C1-C6 alkoxy, C3-C8 cycloalkoxy, 3-8 membered heterocyclic group containing 1 to 3 heteroatoms selected from N, O or S, C6-C10 aryl, and 3-10 membered heteroaryl containing 1 to 3 heteroatoms selected from N, O or S;
- X1 and X2 are independently selected from the group consisting of H, D, halogen, unsubstituted or halogen-substituted C1-C6 alkyl, unsubstituted or halogen-substituted C1-C6 alkoxy, and cyano;
- X3 is selected from the group consisting of hydrogen, halogen, hydroxy, C1-C3 alkyl, C1-C3 alkoxy;
- n is an integer selected from 0, 1, 2, 3, 4, 5, 6, 7 or 8;
- Y is selected from the group consisting of —OR3, and —N(X4R4) R5,
- wherein,
- X4 is selected from the group consisting of O, S, and NH;
- R3 is selected from the substituted or unsubstituted group consisting of H, carboxy, sulfonic acid group, phosphoryl group, C1-C6 alkyl, C3-C8 cycloalkyl, C6-C10 aryl, 3-10 membered heteroaryl containing 1 to 3 heteroatoms selected from N, O or S, and 3-8 membered heterocycloalkyl containing 1 to 3 heteroatoms selected from N, O or S;
- R4 and R5 are independently selected from the substituted or unsubstituted group consisting of H, carboxy, sulfonic acid group, phosphoryl group, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C3-C8 cycloalkyl, C1-C6 alkoxy, C3-C8 cycloalkoxy, C6-C10 aryloxy, C6-C10 aryl, 3-8 membered heterocycloalkyl containing 1 to 3 heteroatoms selected from N, O or S, and 3-10 membered heteroaryl containing 1 to 3 heteroatoms selected from N, O or S;
- the substituted in R3, R4 and R5 refers to be independently substituted by one or more substituents selected from the group consisting of halogen, hydroxyl, amino, carboxyl, C1-C6 alkyl, C3-C8 cycloalkyl, C1-C6 alkoxy, C3-C8 cycloalkoxy, 3-8 membered heterocyclic group containing 1 to 3 heteroatoms selected from N, O or S, C6-C10 aryl, and 3-10 membered heteroaryl containing 1 to 3 heteroatoms selected from N, O or S.
10 more elements
Dependencies are inferred from the claim text.