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US 12,269,816 B2Granted
Benzothiophene compound, preparation method therefor and use thereof
AssigneeSichuan Kelun-Biotech Biopharmaceutical Co., Ltd.
InventorsJinming Liu, Yun Ren, Qiang Tian, Hongmei Song, Tongtong Xue, Jingyi Wang
Life of this patent
Estimating the term…
Abstract
A compound represented by formula (I) or a pharmaceutically acceptable salt, a stereoisomer, a tautomer, a polymorph, a solvate, an N-oxide, an isotope labeled compound, a metabolite or a prodrug thereof, a pharmaceutical composition and a pill container comprising same, a preparation method therefor, and the use thereof in the preparation of drugs for preventing or treating STING-mediated related diseases.
Claims29
A compound of formula (I):
- wherein
- both X1 and X3 are —O—;
- X2 is C1-6 alkylene, wherein the C1-6 alkylene, is optionally substituted with one or more substituents independently selected from the group consisting of halogen, cyano, hydroxy, C1-6 alkyl and C1-6 alkoxy;
- L1 is —(C(R8)2)p—;
- L2 is —C(O)—;
- L3 is —(C(R9)2)q—;
- A1 is —C(O)—ORa;
- R1 and R4 are H;
- R2 and R3 are the same or different, and are each independently selected from the group consisting of H, halogen, cyano, —ORa, —SRa, —S(O)Ra, —S(O)2Ra, —NRaRb, —C(O)—NRaRb, —NRa—C(O)—Ra, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-6 cycloalkyl, 3-6 membered heterocyclyl, C6-10 aryl and 5-10 membered heteroaryl, wherein the C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-6 cycloalkyl, 3-6 membered heterocyclyl, C6-10 aryl and 5-10 membered heteroaryl are each optionally substituted with one or more substituents independently selected from the group consisting of halogen, C1-6 alkyl, C1-6 haloalkyl, cyano, hydroxy and C1-6 alkoxy;
- R5 is selected from the group consisting of H, C1-6 alkyl, C3-10 cycloalkyl and 3-10 membered heterocyclyl, wherein the C1-6 alkyl, C3-10 cycloalkyl and 3-10 membered heterocyclyl are each optionally substituted with one or more substituents independently selected from the group consisting of halogen, cyano, hydroxy, C1-6 alkyl, C3-10 cycloalkyl, 3-10 membered heterocyclyl, C1-6 haloalkyl, C1-6 alkoxy, C1-6 haloalkoxy, —NRaRb, —CO2Ra and —S(O)2Ra;
- R6 is ORa or —C(O)2R7;
- R7 is selected from the group consisting of H and C1-6 alkyl;
- R8 is each independently selected from the group consisting of H and C1-6 alkyl;
- R9 is each independently selected from the group consisting of H and C1-6 alkyl;
- Ra and Rb are each independently selected from the group consisting of H and C1-6 alkyl wherein the C1-6 alkyl is optionally substituted with one or more substituents independently selected from the group consisting of hydroxy, halogen and C1-6 alkyl;
- m and n are each independently selected from the group consisting of 0, 1, 2 and 3;
- and
- p and q are each independently selected from the group consisting of 1, 2, and 3,
- or a pharmaceutically acceptable salt, a stereoisomer, a tautomer, a polymorph, a solvate, an N-oxide, or an isotope-labeled compound thereof.
16 more elements
Dependencies are inferred from the claim text.