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Solid form of pyrazolopyridine compound

A compound and crystal technology, applied in the field of medicine, can solve the problems of indetermination of compound crystal form, solubility, stability inspection, etc., and achieve the effect of weak hygroscopicity and good solubility

Inactive Publication Date: 2016-06-15
SUNSHINE LAKE PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the above-mentioned reports have not carried out XPRD, DSC, IR and other measurements on the obtained crystal form, nor have they been investigated for their solubility in preparations, and their stability has not been determined. Crystalline state

Method used

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  • Solid form of pyrazolopyridine compound
  • Solid form of pyrazolopyridine compound
  • Solid form of pyrazolopyridine compound

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0091] Embodiment 1: the preparation of formula (I) compound amorphous

[0092] Add the compound of formula (I) (2g) and dichloromethane (500mL) into the flask, heat to reflux and then stir until the solid is completely dissolved to form a clear solution, transfer the solution to the BUCHIMiniSprayDryer (B-290) machine to spray dry, set the parameters As follows: the inlet air temperature is about 100°C, the outlet air temperature is about 60°C, the air inlet flow rate is 100%, and the feeding rate of the pump is 30% to form particles. Collect the particles, and use the PANalyticalEmpyrean diffractometer to detect the XRPD pattern of the particles, as attached Figure 9 shown.

[0093] The term "inlet air temperature" used in the present invention refers to the temperature at which the solution just enters the spray dryer, and "outlet air temperature" refers to the temperature of the gas coming out of the spray dryer.

[0094] According to the condition of the instrument, ga...

Embodiment 2-15

[0095] Embodiment 2-15: Preparation of formula (I) compound crystal form I

Embodiment 2

[0097] Formula (I) compound (0.2g), (prepared by Example 1) and methanol (21mL) were added in the flask, heated to reflux, stirred until the solid was completely dissolved to form a clear solution, the solution was slowly cooled to room temperature, sealed and stirred for about 2 Day to form crystals, filter the crystals and wash with methanol, then vacuum dry at about 40°C for about 7h, the X-ray powder diffraction pattern of the dried sample is about 2θ at 25.47, 17.69, 27.23, 8.99, 6.68, 14.24, 20.27 and There is a peak at 19.67 degrees, XRPD as figure 1 shown.

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Abstract

A novel crystalline form or amorphousof formula (I) and preparation method thereof are disclosed in present invention, wherein the novel crystalline form is substantially pure crystalline form I, form II, form III or form IV. The novel crystalline forms disclosed herein have good solubility, low hydroscopicity and good stability at high temperature (60 DEG C), high humidity (RH is 90%+ / -5%) and / or under light (4500+ / -500 Lux), which benefit for storage, meet the requirements of drug stability and therefore, making formula (I) suitable for formulation preparation and with high bioavailability.

Description

[0001] Related patent application information [0002] This application relates to the priority application of Chinese Patent Application No. 201310487493.1 submitted to the State Intellectual Property Office on October 17, 2013, wherein the entire content of the application is hereby incorporated by reference. technical field [0003] The present invention relates to the field of medicine, in particular to a new crystal form or an amorphous pyrazolopyridine compound, and further specifically to a new crystal form or an amorphous N-[4,6-diamino-2-[1-[ Methyl (2-fluorophenyl)methyl]-1H-pyrazolo[3,4-B]pyridin-3-yl]-5-pyrimidinyl]-N-methylcarbamate. Background technique [0004] Riociguat, also known as N-[4,6-diamino-2-[1-[(2-fluorophenyl)methyl]-1H-pyrazolo[3,4-B]pyridine-3- Base]-5-pyrimidinyl]-N-methylcarbamate, the structure of which is shown in formula I, riociguat is the first new class of guanylate cyclase (sCG) agonist, which directly activates sCG , to enhance its s...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D471/04A61K31/506A61P9/00A61P7/02A61P9/10A61P9/12A61P15/00
CPCC07D401/04C07F5/022A61K31/506A61P7/02A61P7/06A61P9/00A61P9/10A61P9/12A61P15/00A61P15/10C07D471/04
Inventor 廖守主范卫杰王仲清
Owner SUNSHINE LAKE PHARM CO LTD