Aromatic hydrocarbon receptor modulator and use thereof

By developing an aromatic hydrocarbon receptor modulator with a specific structure, the problem of difficult to effectively regulate aromatic hydrocarbon receptors in the prior art is solved, and the multifunctional drug effect in the treatment of immune-related diseases and other health problems is achieved.

WO2025066914A1 Publication Date: 2025-04-03DEMING YAOTAI BIOTECH (SHENZHEN) CO LTD
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Patent Information

Application Number
PCT/CN2024/118483
Authority / Receiving Office
WO · WO
Patent Type
Applications
Current Assignee / Owner
Priority Date
2023-09-28
Filing Date
2024-09-12
Publication Date
2025-04-03

AI Technical Summary

Technical Problem

The prior art is difficult to effectively regulate aromatic hydrocarbon receptors (AHRs), thus lacking effective drug means in the treatment of immune-related diseases.

Method used

An aromatic hydrocarbon receptor modulator with a specific structure was developed to regulate the activity of AHR through the chemical structure described in its general formula (I). This compound can be used to prepare drugs for the treatment of central nervous system diseases, cancer, obesity, and plays a role in immunomodulation, hematopoiesis, cell cycle or intestinal barrier.

Benefits of technology

The aromatic hydrocarbon receptor modulator can effectively activate or inhibit AHR, thereby providing new drug means in the treatment of immune-related diseases and other health problems, improving therapeutic efficacy and drug versatility.

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Abstract

Disclosed in the present invention are an aromatic hydrocarbon receptor modulator, which has the following general formula (I) W is C = C or SA1、A2、A3 are independently a connecting key or C, and m is an integer between 1 to 7; each R1 and R3 are independently H, D, halogen, CN, OR, SR, N(R)R, -C(O)R, -C(O)OR, RC(O)O-, S(O)nR, unsubstituted or 1 to 6 Ra substituted C1-C8 alkyl, C2-C8 alkenyl, C2-C8 alkynyl or C3-C10 cycloalkyl; A4 is independently O or NR4; R2 is H, D or -(CH2O)aC(O)(CH2)b(O)c(CH(Rc))d(CH2CH2O)eRc; Rc is independently H, D, C1-C8 alkyl, NH2-, (C1-C8 alkyl) NH -, (C1-C8 alkyl) 2N-, NH2(C1-C8) alkyl-. The aromatic hydrocarbon receptor modulator of the present invention has good activity in a drug for treating cancer and obesity, or in immunoregulation, hematopoiesis, cell cycle, or intestinal barrier.
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