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Crystal form of pyrazolo[1,5-a]pyridine compound, and medicine composition and application of crystal form

A compound and composition technology, applied in the field of pharmaceutical compositions containing the crystal form, can solve problems such as different properties of active pharmaceutical ingredients

Active Publication Date: 2019-06-11
SUNSHINE LAKE PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0012] However, different salts and solid forms of pharmaceutically active ingredients may have different properties

Method used

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  • Crystal form of pyrazolo[1,5-a]pyridine compound, and medicine composition and application of crystal form
  • Crystal form of pyrazolo[1,5-a]pyridine compound, and medicine composition and application of crystal form
  • Crystal form of pyrazolo[1,5-a]pyridine compound, and medicine composition and application of crystal form

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0074] Example 1N-(5-(3-cyanopyrazol[1,5-a]pyridin-5-yl)-2-methoxypyridin-3-yl)-2,4-difluorobenzenesulfonamide Monosodium salt crystal form

[0075] 1. Preparation of title monosodium salt crystal form

[0076] Add acetone (40mL) and N-(5-(3-cyanopyrazol[1,5-a]pyridin-5-yl)-2-methoxypyridin-3-yl)-2 in the reaction flask, 4-Difluorobenzenesulfonamide (2.00g, 4.53mmol), stirred at room temperature, added a solution of sodium hydroxide (190mg, 4.75mmol) in water (2mL), heated to 60±5°C and stirred for 30 minutes, cooled to 25±5 ℃, suction filtration, the filtrate was added to the reaction flask, the temperature was controlled at 25±5℃, isopropanol (40mL) was added, stirred at room temperature for 1h, suction filtration, and the solid was dried at 60℃ for 24h to obtain a yellow solid (1.27g, 60.5%).

[0077] 2. Identification of the title monosodium salt crystal form

[0078] (1) Through inductively coupled plasma mass spectrometry analysis, the salt-forming ratio of the co...

Embodiment 2

[0081] Embodiment 2 pharmacokinetic experiment

[0082] The LC / MS / MS system used for analysis includes Agilent 1200 series vacuum degassing oven, binary syringe pump, orifice autosampler, column oven, and Agilent G6430 triple quadrupole mass spectrometer with electrospray ionization (ESI) source . Quantitative analysis was carried out in MRM mode, and the parameters of MRM conversion are shown in Table A:

[0083] Form A:

[0084] multiple reaction detection scan

490.2→383.1

Fragmentation voltage

230V

capillary voltage

55V

Drying gas temperature

350℃

atomizer

40psi

drying gas flow rate

10L / min

[0085] Agilent XDB-C18, 2.1×30 mm, 3.5 μM column was used for analysis, and 5 μL of sample was injected. Analysis conditions: the mobile phase is 0.1% formic acid aqueous solution (A) and 0.1% formic acid methanol solution (B). The flow rate was 0.4 mL / min. The mobile phase gradient is shown in Table B:

[0086]...

Embodiment 3

[0093] Embodiment 3 stability test

[0094] Take an appropriate amount of sample (100 ~ 200mg), spread it in a clean petri dish, and spread it into a thin layer with a thickness of ≤ 5mm. Humidity), light (visible light 4500lx±500lx, ultraviolet light not less than 0.7W h / m 2 , 25±2°C, 60%±5% relative humidity) and normal temperature (25±2°C, 65%±5% relative humidity) for stability test (high temperature, high humidity light and room temperature for 10 days), Sampling was carried out on the 5th day and 10th day respectively, and the impurity content was calculated by the peak area normalization method using an HPLC instrument. The instrument and test conditions are shown in Table 2.

[0095] Table 2: Instruments and Test Conditions

[0096]

[0097]

[0098] Experimental conclusion: The experimental results show that the sodium salt crystal form prepared by the present invention has no obvious change in appearance and purity under high temperature (60°C) and high humid...

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Abstract

The invention provides a monosodium salt crystal form of a pyrazolo[1,5-a]pyridine compound and an application of the monosodium salt crystal form. The invention also relates the crystal form or a pharmaceutical composition thereof, and an application of the crystal form or the pharmaceutical composition in preparing medicines for treating and preventing high proliferative diseases.

Description

field of invention [0001] The invention belongs to the field of medicine, and relates to a base addition salt crystal form of a pyrazol[1,5-a]pyridine compound and its application, in particular to N-(5-(3-cyanopyrazol[1,5- a] monosodium salt crystal form of pyridin-5-yl)-2-methoxypyridin-3-yl)-2,4-difluorobenzenesulfonamide (compound shown in formula (I)) and its application, further It relates to a pharmaceutical composition comprising said crystal form. The crystal form or the pharmaceutical composition can be used to inhibit or regulate protein kinase activity in biological samples, and can be used to prevent, treat, treat or alleviate proliferative diseases or pulmonary fibrosis in patients. Background of the invention [0002] Phosphoinositide 3-kinase (PI3 kinase or PI3K), as a family of lipid kinases, plays an important regulatory role in many cellular processes, such as cell survival, reproduction and differentiation. As the main influencing factor in the downstre...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D471/04A61K31/4427A61K45/06A61P35/04A61P35/00
Inventor 习宁孙明明
Owner SUNSHINE LAKE PHARM CO LTD
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