Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1996-05-21
1998-03-10
Trinh, Ba K.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
549348, 549354, 549358, A61K 31335, C07D32304
Patent
active
057262039
DESCRIPTION:
BRIEF SUMMARY
This is a 371 application of PCT/CN 94/00056 dated Jul. 19, 1994 publshied as WO95/03311 Feb. 2, 1995.
FIELD OF THE INVENTION
This invention relates to carbocyclic compounds, in particularly to artemisinin-type new derivatives, their preparation and use in prevention and treatment of AIDS viruses.
BACKGROUND OF THE INVENTION
AIDS is the abbreviation of acquired immunodeficeincy syndrom. In 1981, the first case of AIDS was found in the United States of America. In 1983, Professor Montagnier of the Pasteur institute, France, isolated for the first time a virus from a patient's blood, which was later designated as HIV, there by this disease, AIDS, was proved to be a viral infectious disease characterized by acquired immunodeficiency. Since HIV is T-lymphocytophilic, on one hand it multiplies and releases continuously in these cells and the released virus again invades new T4-lymphocytes; on the other hand, the T4-lymphocytes invaded by this virus may coalesce with other T4-lymphocytes to form syncytia which are unstable and may die easily. The virus multiplies, releases, forms syncytia and dies repeatedly as such, thereby results in profound cellular immunodeficiency, finally destroys human immune function and leads to death. Besides T-lymphocytes, HIV may also invade macrophages, B-lymphocytes, etc., especially it may form chronic infection in macrophages, and may exist for a long time. The development of this disease may be divided into three stages, i.e., HIV-carrier stage, ARC stage and AIDS stage. Once the disease developed to AIDS stage, it progresses rapidly and the 3-year survival rate is less than 10%. At present, approximately 20,000,000 persons are infected by HIV in the world, the number of AIDS patients reached 600,000 and half of them have alreadly died. China is not an exception. AIDS was imported into China in 1984. At present, 890 persons infected by HIV have been found in China among them, 740 HIV-carriers and 5 AIDS patients are Chinese. The number of HIV-infected persons is still continuously increasing.
With regard to anti-HIV agents, the first one reported was Suramin. In 1985, AZT (3'-azido-3'-deoxythymidine), etc., were found to possess anti-HIV activity in vitro. Clinical studies were carried out in 1986, and AZT was approved by FDA of the United States of America as the first drug to be used for the treatment of AIDS in 1987. Up to now, several hundred new compounds and their prescriptions including dozens of natural products and traditional Chinese medicine have been screened in the world. Only AZT, DDI (di-deoxytrophicardyl) and DDC (di-deoxycytidine) are approved by the FDA of the United States of America to be used for the treatment of AIDS; among natural products and traditional Chinese medicinal herbs, such as trichosanthin is approved by the FDA for clinical observation. But all these drugs have different types of toxicity, for example, 4-6 weeks after the use of AZT, inhibition of bone marrow appears, then severe anemia develops; 6 months after the use of AZT alone, drug resistance may be produced; furthermore AZT does not exert inhibitory effect on the virus within infected macrophages thus it cannot remove the hidden peril, and, in addition, its price is high. DDC and DDI produce toxicity to peripharal nerves which appears 6 weeks after drug administration; higher dostage may result in sequelae which may still be present even one year after discontinuation of the drug. Trichosanthin has produced neurotoxicity in clinical trial, and in severe cases temporary dementia and even coma appeared. Experimental studies showed that treatment of HIV-infected macrophages with trichosanthin produced and released a soluble toxic substance which might exert serious destructive effect to human brain cells.
Up to now, experimenal studies and evaluation have been carried out with several hundred drugs and their prescriptions, natural products, single traditional Chinese drugs and composite traditional Chinese drugs in the world. Effective components were seperated from only very few of
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Luo et al, "Helvetica Chimica. Acta", vol. 67, pp. 1515-1521, 1984.
Li Zelin
Luo Xuande
Ma Lin
Zeng Yi
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