Check patentability & draft patents in minutes with Patsnap Eureka AI!

Triazole compounds, medical composition thereof and preparation and application of triazole compounds

A compound, triazole technology, applied in the field of pharmacology, can solve problems such as no obvious progress in research

Active Publication Date: 2013-05-22
KUNMING INST OF BOTANY - CHINESE ACAD OF SCI +1
View PDF4 Cites 4 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Since the Wnt / β-catenin signaling pathway is related to many cancers and diseases, the out-of-control Wnt / β-catenin signaling pathway can be used as a good way to treat diseases related to the Wnt / β-catenin signaling pathway, but at this stage There has been no significant progress in the research

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
  • Triazole compounds, medical composition thereof and preparation and application of triazole compounds
  • Triazole compounds, medical composition thereof and preparation and application of triazole compounds
  • Triazole compounds, medical composition thereof and preparation and application of triazole compounds

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] Preparation of compounds of the present invention:

[0042] Synthetic route such as figure 1 Shown:

[0043] (1) Preparation of intermediate 1 from Lycorine: 5-methyl-4-vinyl-5,6-dihydro-[1,3]dioxolo[4,5-j]phenanthridine:

[0044] Lycorine (28.7mg, 0.1mmol) was dissolved in N,N-dimethylformamide (DMF) (5mL), added iodomethane (MeI) (17.0mg, 0.12mmol), at 50℃ The reaction was stirred for 12 hours under reduced pressure, and the solvent was distilled off under reduced pressure and used directly in the next reaction; under the condition of nitrogen protection, the compound (30.2mg, 0.1mmol) obtained in the previous step was dissolved in tert-butanol (t-BuOH) ( 5mL ), add potassium tert-butoxide (t-BuOK) (30mg) and then reflux for 4h. After the reaction, add ammonium chloride solution, then add diethyl ether to extract twice (2×10ml), then wash with ammonium chloride solution for 2 times (2×10ml), washed twice with saturated brine (2×10ml), the organic layer was washed w...

Embodiment 2

[0086] Table 1 shows the results of activation of the Wnt signaling pathway by the compound obtained in Example 1.

[0087] Table 1 The results of compound activation of Wnt signaling pathway activity

[0088] sample name

Synergistic activation of the Wnt reporter gene doubles the compound concentration

HLYC-60

1.25μM

HLYC-67

2.5μM

[0089] HLYC-68

1.25μM

HLYC-69

5μM

[0090] Experimental results:

[0091] Compounds hlyc60, hlyc67, hlyc68 and hlyc69 can activate the reporter gene system of the canonical Wnt signaling pathway in a Wnt3a receptor-dependent manner.

[0092] The invention utilizes the reporter gene system of the canonical Wnt signaling pathway to screen compounds. Compounds hlyc60, hlyc67, hlyc68 and hlyc69 were found to cooperate with Wnt3a dose-dependently to activate the reporter gene system of the canonical Wnt signaling pathway ( figure 1 ).

Embodiment 3

[0094] The compound combination medicine tablet of embodiment 1:

[0095]The preparation of the pharmaceutical combination tablet of the compound of the embodiment 1 of the present invention as the active ingredient: use the compound of the embodiment 1 as the active ingredient of the medicine, use the excipient described in Table 2 as the auxiliary material composition for preparing the combination medicine tablet, and mix according to the ratio Than make the tablet sample that every tablet contains 5 ~ 60mg of the compound pharmaceutical composition of embodiment 1, table 2 provides the formula ratio of common tablet:

[0096] Table 2 The bulk drug and adjuvant formula of the compound combination medicine tablet of the embodiment of the present invention 1

[0097]

[0098] The method of preparing a certain amount of the compound of Example 1 and excipients and auxiliary materials into different doses of tablet preparations is to uniformly mix several excipients and auxil...

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 invention provides triazole compounds hlyc60, hlyc67, hlyc68 and hlyc69 as Wnt signal path agonists, a medical composition with the triazole compounds as active components, a preparation method of the triazole compounds, and application of the compounds provided by the invention in preparation of medicines for adjusting Wnt signal path, medicines for preventing and treating classical Wnt signal path related diseases and stem cell amplifying medicines.

Description

technical field [0001] The invention belongs to the field of pharmacy, and specifically relates to a triazole compound used as a Wnt signaling pathway agonist, its pharmaceutical composition, its preparation method and its application in pharmacy. Background technique [0002] The Wnt signal transduction pathway is a highly conserved signal transduction pathway in the evolution of organisms, regulating and controlling many life activities. In the early development of animals, Wnt signaling determines a series of important events such as the formation of the dorsal-ventral axis, germ layer establishment, somite differentiation, tissue or organ formation, and directly controls proliferation, differentiation, polarization, apoptosis and anti-apoptosis and so on cell fate. More than a dozen members of Wnt proteins are involved in different signal transduction pathways by interacting with different receptors on the cell membrane. These pathways are mainly divided into the canon...

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
IPC IPC(8): C07D401/14A61K31/473A61P25/28A61P19/02A61P29/00A61P19/10A61P3/00
Inventor 郝小江陈铎之尹俊林李林汪胜
Owner KUNMING INST OF BOTANY - CHINESE ACAD OF SCI
Features
  • R&D
  • Intellectual Property
  • Life Sciences
  • Materials
  • Tech Scout
Why Patsnap Eureka
  • Unparalleled Data Quality
  • Higher Quality Content
  • 60% Fewer Hallucinations
Social media
Patsnap Eureka Blog
Learn More

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

© 2025 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com