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Salt of aromatic heterocyclic derivative and application thereof

A drug and hydrochloride technology, applied in the field of medicine, can solve problems such as the research of no compound salt or its crystal form, and achieve the effects of good water solubility, good stability, and good pharmacokinetic properties

Active Publication Date: 2020-06-05
DONGGUAN HEC NEW DRUG R&D CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there is no research on the salt of the compound or its crystal form in the prior art

Method used

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  • Salt of aromatic heterocyclic derivative and application thereof
  • Salt of aromatic heterocyclic derivative and application thereof
  • Salt of aromatic heterocyclic derivative and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0091] Embodiment 1 Hydrochloride salt crystal form A of the present invention

[0092] 1. Preparation of hydrochloride crystal form A

[0093] Get the compound shown in formula (I) (5.0g) and dissolve in ethyl acetate (40mL), then get hydrochloric acid (0.64g) and dissolve in ethyl acetate (5mL), it is slowly added dropwise to containing formula ( I) In the ethyl acetate solution of the compound shown, a white solid was precipitated immediately, suspended for 4 hours, filtered and dried to obtain the hydrochloride crystal form A product.

[0094] 2. Identification of Hydrochloride Form A

[0095] Identified by Empyrean X-ray powder diffraction (XRPD) analysis: using Cu-Kα radiation, with the following characteristic peaks expressed in angle 2θ: 7.64°±0.2°, 8.49°±0.2°, 13.51°±0.2°, 16.73°±0.2 °,17.09°±0.2°,17.50°±0.2°,18.66°±0.2°,19.06°±0.2°,19.66°±0.2°,22.74°±0.2°,23.26°±0.2°,23.58°±0.2°, 24.46°±0.2°, 25.39°±0.2°, 25.87°±0.2°, 26.94°±0.2°, 30.03°±0.2°, 31.43°±0.2°, 32.14°±...

Embodiment 2

[0096] Embodiment 2 Citrate crystal form B of the present invention

[0097] 1. Preparation of citrate crystal form B

[0098] Get compound (0.5g) shown in formula (I) in round bottom flask, add dichloromethane (10mL), dissolve at room temperature clear, add citric acid (0.249g) (compound shown in formula (I) and citric acid The molar ratio is 1 / 1.2), no obvious phenomenon, a large amount of white solids are precipitated after 1h, suspended for 12h, filtered and dried to obtain citrate crystal form B product.

[0099] 2. Identification of citrate crystal form B

[0100] (1) Analysis and identification by Empyrean X-ray powder diffraction (XRPD): using Cu-Kα radiation, with the following characteristic peaks expressed in angle 2θ: 5.66°±0.2°, 6.84°±0.2°, 7.72°±0.2°, 9.54 °±0.2°,11.31°±0.2°,13.69°±0.2°,16.22°±0.2°,17.00°±0.2°,19.17°±0.2°,20.56°±0.2°,22.99°±0.2°,23.92°± 0.2°, 25.86°±0.2°, 28.21°±0.2°, 30.05°±0.2°, 32.61°±0.2°, 34.43°±0.2°, 36.48°±0.2°, 37.63°±0.2°. The XRPD p...

Embodiment 3

[0102] Embodiment 3 Sulfate crystal form A of the present invention

[0103] 1. Preparation of sulfate crystal form A

[0104] Take the compound (2g) shown in formula (I) in a round bottom flask, add ethyl acetate (10mL), warm up to 50 ° C to dissolve, then add sulfuric acid (0.6g) dropwise (dissolved in 2mL ethyl acetate, formula ( 1) The molar ratio of the compound shown in 1) to sulfuric acid is 1 / 1.2), and a white solid is separated out immediately, and after being suspended for 12 hours, it is filtered and dried to obtain about 2.3g of sulfate crystal form A product in total.

[0105] 2. Identification of sulfate crystal form A

[0106] Identified by Empyrean X-ray powder diffraction (XRPD) analysis: using Cu-Kα radiation, with the following characteristic peaks expressed in angle 2θ: 9.76°±0.2°, 14.55°±0.2°, 15.65°±0.2°, 16.35°±0.2 °,17.95°±0.2°,18.93°±0.2°,19.37°±0.2°,19.64°±0.2°,20.22°±0.2°,20.98°±0.2°,21.38°±0.2°,21.81°±0.2°, 22.18°±0.2°, 23.22°±0.2°, 23.60°±0.2°, ...

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PUM

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Abstract

The invention relates to a salt of an aromatic heterocyclic derivative and application thereof. The invention also relates to a pharmaceutical composition containing the salt, and an application of the salt or the pharmaceutical composition of the salt in preparation of drugs for preventing, treating or alleviating diseases related to the 5-HT6 receptor, especially Alzheimer's disease.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to salts of aromatic heterocyclic derivatives and uses thereof, in particular to 3-(difluoromethyl)-1-((3-fluorophenyl)sulfonyl)-4-(piperazine The salts of -1-yl)-1H-indole, the crystal forms of the salts and their uses further relate to pharmaceutical compositions comprising the salts or the crystal forms of the salts. Background technique [0002] A variety of central nervous system diseases such as anxiety and depression are related to the disturbance of neurotransmitter 5-hydroxytryptamine (5-HT) or serotonin. As the main regulatory neurotransmitter in the brain, the neurotransmitter 5-hydroxytryptamine (5-HT) functions by 1 , 5-HT 2 , 5-HT 3 , 5-HT 4 , 5-HT 5 , 5-HT 6 and 5-HT 7 mediated by a large family of receptors. Based on high levels of 5-HT in the brain 6 receptor mRNA, it has been proposed that 5-HT 6 The receptors may play a role in the pathology and treatment...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D209/10A61K31/496A61P3/04A61P1/00A61P25/00A61P25/22A61P25/18A61P25/14A61P25/16A61P25/28
CPCA61P1/00A61P3/04A61P25/00A61P25/14A61P25/16A61P25/18A61P25/22A61P25/28C07D209/10
Inventor 金传飞钟文和许腾飞
Owner DONGGUAN HEC NEW DRUG R&D CO LTD
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