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

Free PLX5622 crystal form and preparation method thereof

A crystal form and crystallization technology, which is applied in the fields of medicine and chemistry, can solve the problems of PLX5622, such as the undiscovered crystal form

Pending Publication Date: 2022-07-22
上海皓鸿生物医药科技有限公司
View PDF2 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] However, so far, PLX5622 has not found any crystal form

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
  • Free PLX5622 crystal form and preparation method thereof
  • Free PLX5622 crystal form and preparation method thereof
  • Free PLX5622 crystal form and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0127] Example 1 Preparation of PLX5622 crystal form A crystal form

Embodiment 11

[0129] 1 g of the compound of formula I was mixed with 50% of the excipient hypromellose acetate succinate (HPMCAS) and dissolved in 30 mL of THF, and the obtained solution was spray-dried at an inlet temperature of 80° C., shaken, mixed and dissolved to obtain a solution to be sprayed. The above-obtained solution was sprayed on a BUCHI Mini Spray Dryer B-290 type spray dryer. The inlet air temperature of the spray dryer was 95-100°C, the outlet air temperature was 80°C, and the nitrogen flow rate was 450-605 L / hr. The obtained sample was vacuum-dried at 50±5°C for 40 hours to obtain an off-white solid. X-ray powder diffraction sees figure 1 shown.

Embodiment 12

[0131] 10 g of the compound of formula I was mixed with 50% auxiliary material hypromellose acetate succinate (HPMCAS) and dissolved in 300 mL of THF, and the obtained solution was spray-dried at an inlet temperature of 80° C., shaken, mixed and dissolved to obtain a solution to be sprayed. The above-obtained solution was sprayed on a BUCHI Mini Spray Dryer B-290 type spray dryer. The inlet air temperature of the spray dryer was 95-100°C, the outlet air temperature was 80°C, and the nitrogen flow rate was 450-605 L / hr. The obtained sample was vacuum dried at 50±5°C for 40 hours to obtain an off-white solid. The resulting off-white solid is PLX5622 Form A described herein.

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 relates to a free PLX5622 crystal form and a preparation method thereof. The invention provides crystal forms A, B, C, D, E and F of a free alkali PLX5622 compound with a chemical name of 6-fluoro-N-((5-fluoro-2-methoxypyridine-3-yl) methyl)-5-((5-methyl-1H-pyrrolo [2, 3-b] pyridine-3-yl) methyl) pyridine-2-amine and a preparation method thereof, the structural formula of the compound in the formula I is as follows: the physical and chemical properties of the crystal form A provided by the invention are relatively stable; the crystal form B is better in microglial cell elimination effect and more stable in drug effect; according to the present invention, the crystal form I, the hydrate crystal form C, the solvate crystal form D, the solvate crystal form E and the solvate crystal form F have characteristics of good crystallinity, good granularity and strong fluidity from the solid state form, the crystal form preparation method is simple, and more choices are provided for the research of the I compound free alkali PLX5622 medicinal crystal form.

Description

technical field [0001] The invention relates to a new crystal form of free state PLX5622 and a preparation method thereof, belonging to the technical fields of medicine and chemistry. Background technique [0002] PLX5622 is a CSF1R colony stimulating factor-1 receptor inhibitor, and its chemical structure is shown in formula I: [0003] [0004] PLX5622 is a highly selective, blood-brain barrier-permeable, orally potent CSF1R inhibitor (IC 50 = 0.016 μM; K i = 5.9 nM), PLX5622 was able to deplete microglia and reduce the number of perivascular macrophages and circulating immune cells. The study found that depletion of microglia with the CSF1R inhibitor PLX5622 partially prevented short-term memory impairment caused by prolonged Ang II infusion, and the improvement of cognition by PLX5622 was independent of changes in blood-brain barrier permeability. This is an important step in the development of CSF1R therapeutics, and further research is needed to develop a treatme...

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): C07D471/04A61P25/28A61P25/00A61P17/14A61P25/08A61P35/02A61P35/00A61P27/02A61K31/444
CPCC07D471/04A61P25/28A61P25/00A61P17/14A61P25/08A61P35/02A61P35/00A61P27/02A61K31/444C07B2200/13
Inventor 曹铭王广勇黄宗穗陈玉凤张飞雄杨顺平李朝平焦磊周治国杨绍波高强郑保富
Owner 上海皓鸿生物医药科技有限公司
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