Mesylate C crystal form of amide derivatives as well as preparation method and application thereof
A technology of nicotinamide and mesylate, which is applied in the preparation of organic compounds, chemical instruments and methods, medical preparations containing active ingredients, etc., can solve the problems of stability and bioavailability differences, affecting drug efficacy and other issues
Inactive Publication Date: 2014-10-01
SHANGHAI SUNTRONG BIOTECH
View PDF3 Cites 8 Cited by
- 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
the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View moreImage
Smart Image Click on the blue labels to locate them in the text.
Smart ImageViewing Examples
Examples
Experimental program
Comparison scheme
Effect test
Embodiment 1
[0023] Dissolve 500mg of the mesylate salt of nicotinamide derivatives into 20ml of dimethylformamide solution, slowly add pure water until the solution is cloudy, let it stand at room temperature for 12 hours, then filter and vacuum dry to obtain a white powder that is smoke Form C of mesylate salt of amide derivatives.
[0024] The mesylate C crystal form of nicotinamide derivatives provided by the present invention is detected by an automatic moisture meter, and its water content is 2.5-4.5%.
the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More PUM
| Property | Measurement | Unit |
|---|---|---|
| water content | aaaaa | aaaaa |
Login to View More
Abstract
The invention discloses a mesylate C crystal form of amide derivatives as well as a preparation method and application thereof. The XRPD (X-ray powder diffraction) of the mesylate C crystal form of amide derivatives has diffraction peaks at the places in which 2*theta is equal to 5.978, 10.961, 11.201, 11.821, 12.202, 13.602, 14.023, 14.619, 15.821, 17.72, 18.739, 19.72, 20.9, 22.261, 23.139, 24.117, 24.996, 25.478, 25.899, 26.921, 28.081, 29.098, 30.38, 31.058, 31.701, 33.284 and 33.845, wherein the error range of the value of 2*theta is 0.2. The mesylate C crystal form of amide derivatives provided by the invention can be applied to medicines for treating advanced non-small cell lung cancer, gastric cancer, liver cancer and breast cancer; moreover, the qualitative and quantitative information of the crystal form is of great significance for further researches on the curative effect of the solid medicines.
Description
technical field [0001] The invention relates to molecularly targeted antineoplastic drugs, in particular to a mesylate C crystal form of nicotinamide derivatives and 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 mesylate salt of the above-mentioned nicotinamide derivatives. [0003] As we all know, different crystal forms of the same drug may have significant differences in stability and bioavailability, which will affect the e...
Claims
the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More Application Information
Patent Timeline
Login to View More Patent Type & Authority Applications(China)
IPC IPC(8): C07D213/82C07C303/44C07C309/04A61K31/444A61P35/00
CPCC07D213/82
Inventor 于迎渌陈金瑶弋东旭
Owner SHANGHAI SUNTRONG BIOTECH