Furocoumarin compound, and preparation method and medical application thereof
What is Al technical title?
Al technical title is built by PatSnap Al team. It summarizes the technical point description of the patent document.
A furanocoumarin and a technology for its application, which are applied in the preparation of new compounds, the preparation of furanocoumarins, and the field of furanocoumarins, can solve the problem that the chemical drug treatment of hypertension cannot meet expectations and reduce the The problems of drug resistance, chemical drug toxicity, etc
Active Publication Date: 2019-09-13
YANBIAN UNIV
View PDF2 Cites 2 Cited by
Summary
Abstract
Description
Claims
Application Information
AI Technical Summary
This helps you quickly interpret patents by identifying the three key elements:
Problems solved by technology
Method used
Benefits of technology
Problems solved by technology
[0003] Although there are many types of antihypertensive drugs in clinical use and various mechanisms of action, due to the different degrees of toxic and side effects of chemical drugs, hypertension drugs with different mechanisms of action have different shortcomings, and antihypertensive drugs with a single mechanism of action often produce Drug resistance, which often prevents chemotherapeutic treatment of hypertension from achieving the desired effect
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 more
Image
Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
Click on the blue label to locate the original text in one second.
Reading with bidirectional positioning of images and text.
Smart Image
Examples
Experimental program
Comparison scheme
Effect test
Embodiment 1
[0023] 1) Stir the dichloromethane solution of chlorosulfonic acid (100 mmol / 20 mL) in an ice bath for 30 min, slowly add xanthotoxin (10 mmol) in batches, and continue the ice bath for 1 h;
[0024] 2) After the reaction is completed, the solvent is removed under reduced pressure, and then slowly added dropwise to the ice-water mixture, filtered with suction, washed, and dried to obtain the white chlorosulfonated product of xanthotoxin;
[0025] 3) Dissolve 5-aminotetrazole (1 mmol) and N,N-diisopropylethylamine (2 mmol) in 10 mL of dichloromethane under an ice bath;
[0026] 4) After cooling down for 30 minutes, add the chlorosulfonated pepper toxin (0.8 mmol) prepared in step 3), continue the reaction for 2 hours, add water for extraction, wash with 10% hydrochloric acid, saturated sodium bicarbonate and saturated saline successively, and filter with suction , dried, and obtained compound S31 by column chromatography; named: 9-methoxy-7-oxo-N-(1 H -tetrazol-5-yl)-7 H -fur...
Embodiment 2
[0029] pharmaceutical composition
[0030] Formulation for 1000 tablets each containing 100 mg of active ingredient:
[0036] talc------------------------------------------------- ------------3 g
[0037] The dosage used should be adapted to the nature and severity of the disease, the route of administration and the age and weight of the patient. The daily dose varies between 0.1 mg-1.0 g, and can be administered once or several times.
[0038] Further prove the medical purposes of compound of the present invention by following test:...
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
Login to view more
Abstract
The invention discloses a furocoumarin compound, and a preparation method and medical application thereof. The furocoumarin compound is a novel compound having vasodilating activity; and the compoundis obtained by structurally modifying and optimizing the natural product xanthotoxin to improve its physical and chemical properties, pharmacological activity and drug-forming properties. The preparation method for the furocoumarin compound provided by the invention has the advantages that raw materials are widely available, reaction conditions are mild, reaction process is simple to operate and reagents used therein are cheap and easily available. The prepared novel furocoumarin compound has effect similar to the effect of xanthotoxin; the study results of isolated vascular ring tension indicate that the relaxation effect of the novel furocoumarin compound on the aortic vessels of rat is stronger than the relaxation effect of xanthotoxin and the positive control drug nifedipine; the cytotoxicity of the novel furocoumarin compound on normal liver cells L02 in vitro is significantly lower than the cytotoxicity of nifedipine; and the results of in-vivo antihypertensive studies show thatthe antihypertensive effect of the novel furocoumarin compound is stronger than the antihypertensive effect of xanthotoxin and nifedipine, so the novel furocoumarin compound can be applied to the preparation of antihypertensive drugs.
Description
technical field [0001] The invention discloses a furinocoumarin compound, which is a new compound; the invention also provides a preparation method and medical application of the furanocoumarin compound, belonging to the technical field of biomedicine. Background technique [0002] Cardiovascular and cerebrovascular diseases have become the number one killer of human health, and hypertension is one of the important causes of cardiovascular and cerebrovascular diseases. At present, according to the report of the World Health Organization, the incidence of hypertension in the world population has exceeded 10%, and the number of hypertensive patients in my country has exceeded 100 million. With the increasing aging of our population, the number of hypertensive patients will further increase. [0003] Although there are many types of antihypertensive drugs in clinical use and various mechanisms of action, due to the different degrees of toxic and side effects of chemical drugs, ...
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
Application Date:The date an application was filed.
Publication Date:The date a patent or application was officially published.
First Publication Date:The earliest publication date of a patent with the same application number.
Issue Date:Publication date of the patent grant document.
PCT Entry Date:The Entry date of PCT National Phase.
Estimated Expiry Date:The statutory expiry date of a patent right according to the Patent Law, and it is the longest term of protection that the patent right can achieve without the termination of the patent right due to other reasons(Term extension factor has been taken into account ).
Invalid Date:Actual expiry date is based on effective date or publication date of legal transaction data of invalid patent.
Login to view more 
Login to view more