Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

Methods of treating cancer with aryl hydrocarbon receptor antagonists

A technology of aryl hydrocarbon receptors and antagonists, which can be used in antineoplastic drugs, pharmaceutical formulations, and medical raw materials derived from mammals, and can solve problems such as detection and treatment difficulties

Pending Publication Date: 2021-08-24
EDIGENE BIOTECH INC
View PDF3 Cites 1 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Cancer or malignancy rapidly metastasizes and grows in an uncontrolled manner, making timely detection and treatment extremely difficult

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Methods of treating cancer with aryl hydrocarbon receptor antagonists
  • Methods of treating cancer with aryl hydrocarbon receptor antagonists
  • Methods of treating cancer with aryl hydrocarbon receptor antagonists

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0718] The synthesis of embodiment 1. compound (5)

[0719] Compound (5) can be synthesized, for example, using the Hartwig-Buchwald amination method involving the coupling of a haloimidazopyridine precursor to a protected 2-aminoethylindole, as shown in Scheme 8 below.

[0720] Option 8

[0721]

[0722] For example, compound (5) can be produced by deprotecting the resulting adduct using conventional deprotection methods known in the art.

[0723] Alternatively, the tandem amination-hydrolysis procedure outlined in Scheme 9 below can be used to synthesize compounds (5).

[0724] Option 9

[0725]

Embodiment 2

[0726] Embodiment 2. the synthesis of compound (16)

[0727] In a manner similar to that described in Example 1, compound (16) can be synthesized by the Hartwig-Buchwald method followed by Suzuki coupling and indole deprotection, as shown in Scheme 10 below.

[0728] Scheme 10

[0729]

Embodiment 3

[0730] Example 3. Compounds (5) and (16) Ability to Expand Hematopoietic Stem Cells

[0731] In order to determine the ability of compounds (5) and (16) to inhibit aryl hydrocarbon receptor activity and induce hematopoietic stem cell proliferation, a series of HSC expansion experiments were performed. In a first experiment, compounds (5) and (16) were assessed for their ability to attenuate aryl hydrocarbon receptor signaling. To this end, HepG2 hepatocytes were transiently transfected with a luciferase reporter gene construct under the control of a promoter responsive to aryl hydrocarbon receptor signaling. Cells were seeded in microtiter plates at a density of 25,000 cells per well. In the absence of the aryl hydrocarbon receptor agonist VAF347 (80nM) ( figure 1 ) or exists ( figure 2 ), HepG2 cells were immediately treated with compound (5) or (16). Luciferase activity was subsequently assayed six hours after plating.

[0732] Such as figure 1 and 2 It was shown tha...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

No PUM Login to View More

Abstract

The disclosure relates to aryl hydrocarbon receptor antagonists, such as substituted imidazopyridines and imidazopyrazines, as well as methods of modulating aryl hydrocarbon receptor activity and treating various pathologies, such as cancer, by adminstation of these aryl hydrocarbon receptor antagonists. Additionally, the disclosure provides methods of synthesizing aryl hydrocarbon receptor antagonists, such as substituted imidazopyridines and imidazopyrazines, as well as compositions and kits containing aryl hydrocarbon receptor antagonists that can be used for the treatment of diseases and disorders.

Description

[0001] related application [0002] This application claims priority to US Application No. 62 / 747,064, filed October 17, 2018, the entire contents of which are hereby incorporated by reference. technical field [0003] The present invention relates to aryl hydrocarbon receptor antagonists, such as substituted imidazopyridines and imidazopyrazines, which are useful, for example, in modulating aryl hydrocarbon receptor activity, and methods of treating various pathologies, such as cancer, by administering said aryl hydrocarbon receptor antagonists. Background technique [0004] Cancer remains one of the deadliest threats to human health. In the United States, cancer affects nearly 1.3 million new patients each year and is the second leading cause of death after heart disease, accounting for about a quarter of all deaths. And it is predicted that in the next ten years, cancer may overtake cardiovascular disease and become the number one cause of death. Solid tumors are the ca...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/44A61K31/519A61K45/06A61P35/00A61K35/12C07D471/04C07D487/04C07D519/00A61K35/51
CPCA61K45/06A61P35/00C07D471/04C07D487/04C07D519/00A61K35/12A61K35/51A61K31/4985A61K31/444A61P35/02
Inventor A.博伊塔诺
Owner EDIGENE BIOTECH INC
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com