Novel use of complexes of metabolites of angiotensin II receptor antagonists with nep inhibitors
A receptor antagonist, angiotensin technology, applied in the field of drug application, can solve problems such as untargeted drugs, and achieve the effect of good antihypertensive effect
- Summary
- Abstract
- Description
- Claims
- Application Information
AI Technical Summary
Problems solved by technology
Method used
Image
Examples
Embodiment 1
[0091] Preparation of AHU377 free acid:
[0092] Add 2.1g of AHU377 calcium salt and 40mL of isopropyl acetate into a 250mL single-necked bottle, add 4.5mL of 2mol / L hydrochloric acid at room temperature and stir to dissolve. Separate the liquid, collect the organic layer, and wash the organic layer twice with 20 mL of water; desolvate under reduced pressure at 35°C to obtain the free acid of AHU377.
Embodiment 2
[0094] Preparation of complex:
[0095]
[0096] At room temperature, add 2.36g of AHU377 free acid, EXP31742g and 40mL of acetone obtained according to the method of Example 1 into a 250mL three-neck flask, and dissolve; add 1.3 equivalents of calcium hydroxide solid and 1mL of water relative to AHU377 at room temperature, and stir at room temperature for 10h , add 40mL of acetone, and react for another 8h, filter through a Buchner funnel under nitrogen protection, rinse the solid with acetone to obtain a white solid, dry in vacuum at 35°C for 8h, dry to obtain 3.5g of solid, and the purity of HPLC is 99% , the molar ratio of EXP3174 and AHU377 in the obtained product is 1:1 through content test calculation.
[0097] The X-ray powder diffraction spectrogram of gained product is as figure 1 As shown, the DSC spectrum is as figure 2 shown.
[0098] By comparing with the XRD patterns of EXP3174 and AHU377 calcium, it is found that there are obvious differences in the XRD...
Embodiment 3
[0111] Preparation of complex:
[0112]
[0113] At room temperature, add 2.36g of AHU377 free acid, EXP31742g and 40mL of acetone obtained according to the method of Example 1 into a 250mL three-necked flask, and dissolve it; Stir for 6 hours, add 40 mL of acetone, and react for another 8 hours. Under nitrogen protection, filter through a Buchner funnel, rinse the solid with acetone to obtain a white solid, dry in vacuum at 50°C for 8 hours, and dry to obtain 3.1 g of the solid, which is calculated by the content test It can be seen that the molar ratio of EXP3174 and AHU377 in the obtained product is 1:1.
[0114] The DSC spectrogram of gained product is as Figure 5 shown.
[0115] Elemental analysis, found value: C: 58.51%; H: 5.41%; N: 10.25%. Theoretical value (according to (EXP3174·AHU377)3-·1.5Ca2+·2H2O): C: 58.68%; H: 5.46%; N: 10.41%.
[0116] The TG spectrogram of gained product is as Figure 6 As shown, the water content of the obtained product measured by ...
PUM
Abstract
Description
Claims
Application Information
- R&D Engineer
- R&D Manager
- IP Professional
- Industry Leading Data Capabilities
- Powerful AI technology
- Patent DNA Extraction
Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.
© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com