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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
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  • 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

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  • Rupatadine fumarate compound
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  • 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.

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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

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Application Information

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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
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