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

Compounds for use in the treatment of brain diseases

A brain tumor and compound technology, applied in the field of compounds used in brain tumor treatment, can solve problems such as obstacles and achieve the effect of increasing the drug delivery rate

Pending Publication Date: 2020-11-27
UNIV DEGLI STUDI DI ROMA LA SAPIENZA +2
View PDF4 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0012] GlaB acts by hindering the interaction between the transcription factor Gli1 and DNA, thus inhibiting the transcriptional activity of factors belonging to the Gli protein family

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
  • Compounds for use in the treatment of brain diseases
  • Compounds for use in the treatment of brain diseases
  • Compounds for use in the treatment of brain diseases

Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0092] Preparation of GlaB / PEG-cholane formulation

[0093] GlaB can be synthesized as described in Delle Monache, F. et al. (1977), Italian Journal of Chemistry 107(7-8): 403-407 and WO 2014 / 207069 Al.

[0094] PEG-cholane can be synthesized as follows: Salmaso, S. et al. "Self-assembled nanocomposites for protein delivery: supramolecular interactions between PEG-cholane and rh-G-CSF (Self- -assembling nanocomposites for protein delivery: Supramolecular interactions between PEG-cholane and rh-G-CSF)", Journal of Controlled Release (Journal of Controlled Release) 162, 176-184 (2012), and Ambrosio, E. et al. A novel combined strategy for the physical PEGylation of polypeptides", Journal of Controlled Release 226, 35-46 (2016).

[0095] A 1 mL volume of GlaB solution (2.0 mg / mL, 4.4 mM) in methanol was added to 1 mL of PEG in methanol at various concentrations 5kDa - in cholane solution. Methanol was removed under reduced pressure and 1 mL of 10 mM phosphate, 0.15 M NaCl, pH ...

Embodiment 1

[0126] Example 1: Treatment with Compounds of the Invention Reduces Glioma Growth in Vitro

[0127] figure 1 The experimental data in showed that the growth capacity of GL261 murine glioma cells treated with 5 μM GlaB was reduced compared to the same cells treated with vehicle only (DMSO). The treatment was effective between 24 and 48 hours, around the time of the first attempt at tumor cell replication, which relies in part on activation of the Hedgehog signaling pathway.

Embodiment 2

[0128] Example 2: Treatment with Compounds of the Invention Reduces Glioma Growth in Vivo

[0129] figure 2 The experimental data in shows that compared with the volume measured in the mice treated with the control solution (ethanol:2-hydroxypropyl-β-cyclodextrin solution, 1:5v:v), at 4.4mg / kg and The intranasal and intraperitoneal administration of GlaB at a concentration of 35 mg / kg can significantly reduce the volume of glioma in vivo ( figure 2 ). Furthermore, intranasal administration was unexpectedly effective at concentrations approximately 8-fold lower than intraperitoneal concentrations.

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

PropertyMeasurementUnit
volumeaaaaaaaaaa
Login to View More

Abstract

The present invention relates to a compound of formula (1): (1) or an analogue thereof or a pharmaceutically acceptable salt thereof, for use in the treatment of a brain tumor, wherein said compound is administered intranasally and relative pharmaceutical compositions.

Description

technical field [0001] The present invention relates to a method for rapidly and efficiently distributing a compound of formula (I), its analogue or a pharmaceutically acceptable salt thereof used alone or together with other compounds, and related pharmaceutical compositions: [0002] [0003] Specifically, these compounds achieve systemic circulation by intranasal administration. Rapid onset of beneficial effects of rapid treatment and / or prevention of brain tumors is then achieved. Background technique [0004] Glioblastoma is the most widespread and aggressive tumor of the central nervous system (CNS), characterized by high levels of tumor cell invasion and proliferation, and high levels of inflammation and necrosis of nervous tissue (1). Although neurosurgery and the development of new drugs are ongoing, there are currently no effective treatments against the growth of this brain tumor, and patient death occurs within approximately twelve months of pathological diag...

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): A61K31/366A61K45/06A61P35/00A61K9/00A61K9/16A61K9/20A61K47/60
CPCA61K9/0043A61K45/06A61K9/1641A61K9/2031A61K31/366A61P35/00A61P35/04A61K9/08A61K47/40
Inventor C·立马托拉G·达勒桑德罗L·迪马克图里欧P·因芳特B·博特M·莫里F·吉尔咖C·因戈尔莉娜S·波拉多兹P·卡力册提S·萨尔马索M·德马蒂诺F·加司帕里尼D·瓜格里欧
Owner UNIV DEGLI STUDI DI ROMA LA SAPIENZA
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