Acetamide-phenylbenzamide derivative and method of use thereof

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Acetamide-phenylbenzamide derivatives modulate P-glycoprotein and cytochrome P450 enzymes to enhance the efficacy of anticancer drugs, addressing multidrug resistance and improving oral bioavailability and brain distribution.

JP2026086798APending Publication Date: 2026-05-26HEALTH HOPE PHARMA HK LTD

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Patent Information

Application Number: JP2026024149
Authority / Receiving Office: JP · JP
Patent Type: Applications
Current Assignee / Owner
Priority Date: 2020-10-07
Filing Date: 2026-02-18
Publication Date: 2026-05-26

Application Information

Patent Timeline

07 Oct 2020

Priority

18 Feb 2026

Application

JP2026024149

26 May 2026

Publication

JP2026086798A

IPC: C07D405/12; C07D401/12; C07D403/12; C07D417/12; C07D405/14; C07D403/14; C07D417/14; C07D487/04; C07D471/04; C07D401/14; C07D311/24; C07D407/12; C07D413/12; C07D413/14; A61P35/00; A61K31/4178; A61K31/4709; A61K31/498; A61K31/4433; A61K31/416; A61K31/427; A61K31/4196; A61K31/4184; A61K31/4985; A61K31/4375; A61K31/352; A61K31/36; A61K31/41; A61K31/5377; A61K31/4155; A61K31/357; A61K31/4245; A61K31/424; A61K31/4045; A61K31/506; A61K31/444; A61K31/4439

CPC: C07D401/12; C07D403/12; C07D405/12; C07D405/14; C07D417/12; C07D403/14; C07D401/14; C07D471/04

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Application Domain

Organic chemistry Antineoplastic agents

Technology Topics

Side effectIsozyme

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AI Technical Summary

Technical Problem

Existing anticancer drugs become ineffective due to multidrug resistance caused by overexpressed P-glycoprotein and cytochrome P450 enzymes, leading to reduced oral bioavailability and brain distribution, necessitating compounds that modulate these enzymes to improve drug efficacy and reduce side effects.

Method used

Development of acetamide-phenylbenzamide derivatives that modulate P-glycoprotein and cytochrome P450 enzymes, enhancing the bioavailability and brain distribution of therapeutic agents while minimizing adverse effects.

Benefits of technology

The compounds increase the sensitivity of tumor cells to anticancer drugs, improve oral bioavailability, and enhance brain delivery of therapeutic agents, overcoming multidrug resistance and reducing toxic side effects.

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Abstract

The present invention provides compounds for the regulation of P-glycoprotein and cytochrome P450 (e.g., CYP3A4 and CYP3A5 isoforms) enzymes, which a) significantly improve the bioavailability of substrates of these enzymes, including anticancer drugs, b) overcome multidrug resistance in tumors, and c) reduce serious side effects while improving the delivery of P-glycoprotein substrates to the brain. [Solution] Compounds of formula (I), as well as their prodrugs and pharmaceutically acceptable salts, are provided. Further disclosure relates to pharmaceutical compositions containing the compounds, methods of use, and methods for preparing them. TIFF2026086798000135.tif39128

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