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Mesylate solvate crystal of nicotinamide derivatives and preparation method and application of mesylate solvate crystal

A technology of mesylate and nicotinamide is applied in the field of mesylate solvate crystals of nicotinamide derivatives and the preparation thereof, and can solve the problems affecting the curative effect, stability and bioavailability of drugs, etc. The effect of significant bioavailability and good high temperature stability

Active Publication Date: 2014-10-08
SHANGHAI SUNTRONG BIOTECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] As we all know, different crystal forms of the same drug may have significant differences in their stability and bioavailability, which will affect the efficacy of the drug

Method used

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  • Mesylate solvate crystal of nicotinamide derivatives and preparation method and application of mesylate solvate crystal
  • Mesylate solvate crystal of nicotinamide derivatives and preparation method and application of mesylate solvate crystal
  • Mesylate solvate crystal of nicotinamide derivatives and preparation method and application of mesylate solvate crystal

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Experimental program
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Effect test

Embodiment 1

[0042] Dissolve 90mg of pyridinecarboxamide derivatives in 3ml of dimethylformamide, slowly add 6ml of isopropanol at room temperature, and leave it sealed for 72 hours. The precipitated crystals are mesylate dimethylformamide solvate crystals.

Embodiment 2

[0044] Dissolve 90mg of pyridinecarboxamide derivatives in 3ml of dimethylformamide, slowly add 6ml of acetone at room temperature, and seal it for 72 hours. The precipitated crystals are mesylate dimethylformamide solvate crystals.

Embodiment 3

[0046] Dissolve 90mg of pyridinecarboxamide derivatives in 3ml of dimethylformamide, slowly add 6ml of methyl ethyl ketone at room temperature, and seal it for 72 hours. The precipitated crystals are mesylate dimethylformamide solvate crystals .

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Abstract

The invention discloses a mesylate solvate crystal of nicotinamide derivatives and a preparation method and application of the mesylate solvate crystal. The mesylate solvate crystal of nicotinamide derivatives is a mesylate dimethylformamide solvate crystal and has the characteristic parameters that the crystal system is a triclinic system; the space group is P-1; the cell parameters are as follows: a is 8.9418(2) angstrom, b is 9.4513(2) angstrom, c is 19.5111(4) angstrom, alpha is 76.489(1), beta is 84.199(1), and gamma is 61.952(1); the cell volume V is 1414.91(5) cubic angstrom; the number Z of asymmetry units in cells is equal to 2. The mesylate solvate crystal of nicotinamide derivatives provided by the invention has high high-temperature stability, high humidity stability and illumination stability, is applied to medicines for treating advanced non-small cell lung cancer, gastric carcinoma, liver cancer or breast cancer and is obvious in bioavailability, and the provided qualitative and quantitative information has significance for further researching the curative effect of the solid drugs.

Description

technical field [0001] The invention relates to molecular targeting antineoplastic drugs, in particular to mesylate solvate crystals of nicotinamide derivatives, a preparation method and application thereof. Background technique [0002] Niacinamide derivatives (aptinib), molecular formula C 25 h 27 N 5 o 4 S, whose chemical name is N-[4-(1-cyanocyclopentyl)phenyl]-2-(4-pyridylmethyl)amino-3-pyridinecarboxamide, is a molecularly targeted antineoplastic drug, It is a typical small molecule vascular endothelial growth factor tyrosine kinase inhibitor, which can be used to treat advanced non-small cell lung cancer, gastric cancer, liver cancer and breast cancer. Chinese invention patent CN101676267 discloses the preparation method and application of the above nicotinamide derivative methanesulfonate. [0003] As we all know, different crystal forms of the same drug may have significant differences in stability and bioavailability, which will affect the efficacy of the drug...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D213/82C07C309/04C07C303/44A61K31/455A61P35/00
CPCC07D213/82
Inventor 于迎渌陈金瑶弋东旭
Owner SHANGHAI SUNTRONG BIOTECH
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