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

Rupatadine fumarate compound

A technology of rupatadine fumarate, compound, applied in the field of medicine

Active Publication Date: 2014-07-23
海思科制药(眉山)有限公司
View PDF4 Cites 2 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Clinically used antiallergic drugs have only antihistamine activity, but no PAF antagonism

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
  • Rupatadine fumarate compound
  • Rupatadine fumarate compound
  • Rupatadine fumarate compound

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] Using 3-chloromethyl-5-methyl-pyridine hydrochloride and deratadine as raw materials, using triethylamine as a base, reacting at room temperature in a mixed solvent of acetone and ethyl acetate (volume ratio 1:1) to obtain the free base, Salt-forming reaction of free base and fumaric acid in ethanol to obtain crude rupatadine fumarate, stirring and washing the crude product three times in a mixed solvent of acetone and ethyl acetate (volume ratio 1:5) to obtain the rupatadine fumarate of the present invention. compound.

[0020] Powder X-ray diffraction: using Cu-K radiation, the X-ray powder diffraction (XRPD) spectrum of this compound is shown in the attached figure 1 . Differential scanning calorimetry: the differential thermal analysis (DSC) spectrum of this compound is shown in the attached figure 2 .

Embodiment 2

[0022] Using 3-chloromethyl-5-methyl-pyridine hydrochloride and deratadine as raw materials, using triethylamine as a base, reacting at room temperature in a mixed solvent of acetone and ethyl acetate (volume ratio 1.5: 1) to obtain the free base, Salt-forming reaction of free base and fumaric acid in ethanol to obtain crude rupatadine fumarate, stirring and washing the crude product twice in a mixed solvent of acetone and ethyl acetate (volume ratio 1:6) to obtain the present invention compound of. The crystal map is attached figure 1 and 2 .

Embodiment 3

[0024] Using 3-chloromethyl-5-methyl-pyridine hydrochloride and deratadine as raw materials, using triethylamine as a base, reacting at room temperature in a mixed solvent of acetone and ethyl acetate (volume ratio 1.5: 1) to obtain the free base, Salt-forming reaction of free base and fumaric acid in ethanol to obtain crude rupatadine fumarate, stirring and washing the crude product twice in a mixed solvent of acetone and ethyl acetate (volume ratio 1:8) to obtain the present invention compound of. The crystal form spectrum is the same as in Example 1.

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 a rupatadine fumarate compound which has dual effects of antihistamine and antagonistic platelet activating factor (PAF). According to the research, allergy and inflammatory diseases are multi-factor complex processes caused by generation and release of various different media; histamine is the most inflammatory medium appearing in allergy early symptom, and the disease symptoms including sneezing, rhinocnesmus, tearing, running nose, skin itch, wheal and the like are mostly caused by histamine H1 receptor. And PAF also can cause bronchial constriction and increased permeability of the vessel, so that running nose, nasal congestion, wheal and itch are caused; meanwhile, the PAF is also a main cause of asthma. The antiallergic drug which is clinically used only has an antihistamine activity effect, but does not have a PAF antagonistic effect.

Description

technical field [0001] The invention belongs to the technical field of medicine, in particular to a rupatadine fumarate compound. Background technique [0002] Allergic disease is a complex multifactorial disease. With the control of infectious diseases and the improvement of industrialization, it shows a trend of increasing year by year all over the world. According to the epidemiological survey results of allergic diseases in 30 countries published by the World Allergy Organization, 22% (250 million people) of the total population of 1.2 billion in these countries suffer from various allergic diseases, such as anaphylaxis. Rhinitis, asthma, urticaria, eczema, etc. [0003] With regard to current clinical treatment of allergic rhinitis and allergic urticaria drugs in China, there are mainly antihistamines chlorpheniramine (chlorpheniramine), astemizole (astemizole), terfenadine (allergic urticaria) Di), cetirizine (Xintemin), loratadine (Keminon), etc., chlorpheniramine h...

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 Patents(China)
IPC IPC(8): C07D401/14C07C57/15A61K31/4545A61P37/08
Inventor 陈洪陈九龙冯卫
Owner 海思科制药(眉山)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