The present invention relates to the carbocyclic compound field, particularly the derivative dihydro-abrotine phenyl urethan of the arteannuin of sesquiterpene lactones.

Acquired immune deficiency syndrome (AIDS) is to cause the damaging defective of human immunologic function by a kind of infectious disease that HIV (human immunodeficiency virus) infection causes, it is a kind of worldwide, the infectious disease of lethal.Have 2,000 ten thousand people to infect HIV (human immunodeficiency virus) at present in the world approximately, AIDS stadium patient reaches 6,000,000, has half people dead approximately.China was no exception, and acquired immune deficiency syndrome (AIDS) has been imported China in 1984, present HIV the infected's 890 examples of having found of China, and Chinese carrier's 740 examples wherein, AIDS phase patient 5 examples, the AIDS patient is still constantly increasing.

Anti-hiv drug, that first is reported is suramin (Suramin), found the activity of AZT concrete anti AIDS virus such as (Azidothymidine take off foster nucleoside) in 1985, carried out clinical research in 1986, AZT was used for the treatment of the medicine of acquired immune deficiency syndrome (AIDS) as first by drugs approved by FDA in 1987.So far in the world wide screening hundreds of kind noval chemical compound and prescription thereof arranged, and comprise tens kinds of natural drugs and Chinese medicine.Up to the present, the medicine that is used for the treatment of acquired immune deficiency syndrome (AIDS) by drugs approved by FDA trichosanthin (GLQ in AZT, DDI (didanosine), DDC (zalcitabine), natural drug and the Chinese medicine only ₂₃) by FDA approval carrying out clinical observation, but these several medicines all exist dissimilar toxicity, use 4-6 after week as AZT, bone marrow depression appears in patient, then develop into serious anemia, can produce drug resistance after using 6 months separately, and AZT can not have inhibitory action to the virus that infects in the macrophage, thereby can not remove a hidden danger, cost an arm and a leg simultaneously.DDC and DDI exist peripheroneural toxicity, promptly occur after 6 weeks of taking medicine, and use heavy dose, have both made drug withdrawal that sequela was still arranged in 1 year.Trichosanthin has been found neural poison in clinic trial, momentary dementia appears in severe patient, even stupor, and experimentation shows the macrophage of trichosanthin processing infected by HIV, produce and release solubility toxicant, people's brain cell is had serious destruction.

Up to the present worldwide being removed seldom in hundreds of kind medicine and prescription, natural drug, single medicinal material and the herbal mixture by having of experimentation and evaluation, number has separated effective ingredient, as: Japan's report glycyrrhizin, lentinan etc., the Herba Violae effective ingredient of California, USA university report etc., and number average experimentizes with crude extract mostly, mostly be nucleoside in the chemical compound, adenosine or peptide derivative.And to 1992 in world's acquired immune deficiency syndrome (AIDS) conference that Amsterdam, the Netherlands (Amsterdam) is held, do not see that yet drug research has breakthrough.

The object of the invention is: a kind of chemical effective ingredient and derivant of extracting from Chinese medicine thereof is provided, and they are low, the inexpensive anti-AIDS class medicines of toxicity.Overcome the shortcoming of AZT, DDI, DDC medicine.Another object of the present invention is the compositions with formula I compound anti-AIDS-virus.A further object of the invention is with formula I chemical compound or contains the application of the Drug therapy AIDS disease of desalinating compound.

The objective of the invention is to reach like this: adopted China to have the Chinese medicine Herba Artemisiae Annuae of affluent resources, it is the arteannuin (artemisinin) that extracts in the plant Artemisia annua (Artemisia annua L..), and then synthesizing dihydro arteannuin phenyl urethan makes a breakthrough using of anti AIDS virus, thereby the object of the invention has just reached promptly fully, the invention provides the chemical compound as general formula (I)...

 

https://patents.google.com/patent/CN1051451C/en?oq=CN1051451C抗艾滋病病毒药物组合物---青蒿素类药物，如青蒿琥酯等，是一种高效的抗艾滋病病毒药物