Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Carbohydrate doai
Patent
1995-11-29
2000-11-28
Kunz, Gary L.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Carbohydrate doai
514 45, 514 46, 514 49, 514 50, 514261, 514262, 514269, 536 276, 536 2781, 536 2854, 544276, 544277, 534767, A61K 3170, C07H 1902, C07H 1906, C07H 1916
Patent
active
06153594&
DESCRIPTION:
BRIEF SUMMARY
Present invention relates to a group of new compounds of the general formula I: optionally substituted heterocyclic ring system, S being a monosaccharide derivative, O representing an oxygen, and Fa is an acyl group of a mono-unsaturated C18 or 20 fatty acid. The invention also concerns anti viral pharmaceutical and veterinary compositions comprising a compound of formula I alone or in combination with a pharmaceutically acceptable carrier. A further part of this invention is a method for the treatment of a human or animal patient suffering from a viral infection and for reducing the infectious load by administering a compound of formula I. Likewise, certain compounds of formula I can be used as an antibiotic or in the treatment of a cancerous disease.
TECHNICAL BACKGROUND
A large number of serious diseases, such as AIDS, hepatitis B, herpes and gynecological cancer, as a late result of papilloma warts, are caused by viral infections.
Viruses are small infectious agents which are incapable of independent replication and thus are dependent on a host cell to replicate. The genetic material of the virus is either RNA or DNA.
When infecting an organism, the virus attaches to a specific host cell. The virus penetrates the cytoplasmic membrane after attachment and the viral genome is released from the virus particle. The viral genome is usually transported to the cell nucleus where new viral genomes are replicated. New viral protein is synthesized in the cytoplasm and new particles are formed either close to the cytoplasmic or nuclear membrane.
Some virus have genomic material which is directly (DNA viruses) or indirectly (Reverse transcription of RNA, retrovirus) incorporated in the host cell genomes.
Extracellular viruses are neutralized by circulating antibodies and the cellular immune apparatus may attack and remove infected cells. Viruses within the infected cells escape immune surveillance if viral antigens are not exposed on the surface of the cells.
The immune attack on infected organs contributes to disease by a mechanism commonly called virus induced immunopathology.
The mechanisms underlying some of the more important viral diseases differ.
When suffering from an HIV infection, the patient's T helper cells are invaded and destroyed. This leads to an immunodeficiency condition, which makes the patient very susceptible even to infections which normally are conquered by the immune system without any harmful effects for the patient.
The Hepatitis B virus invades the liver cells, and the patient may become very ill when the immune system tries to rid the body of these infected cells. If the infection is not conquered by the immune system at an early stage, the result will be chronic hepatitis. The patient will thus be infectious throughout his life. For a group of patients the chronic hepatitis will develop into cirrhosis or cancer of the liver.
In herpes simplex infections, the virus enters the epidermal cells originally. The herpes simplex virus travels up to a nerve center where it lies latent to break out at intervals. Although not life threatening in most cases, a herpes infection is painful and the patient will be infectious every time an outbreak occurs.
In the papilloma virus, notably in the genital tract of women, the viral genome is located in the nucleus of epithelial cells, but not integrated in the cell chromosomes. This is a persistent condition and with some tumor promoting strains an integration finally occurs which leads to a malignant development. The viral genome in this case has a decisive initiating effect in the process leading to cancer.
If the immune system manages to rid the body of the virus at an early stage, this leads to a life-long immunity. On the other hand, if the virus is too aggressive and avoids the immune apparatus, no immunity is achieved and a continuous infectious state is the result.
As a result of the different mechanisms, the therapeutic strategy would be different for these conditions.
The ultimate goal in the treatment of HIV/AIDS would be to free the patient
REFERENCES:
patent: 3920630 (1975-11-01), Wechter et al.
patent: 3960836 (1976-06-01), Gutowski
patent: 3984396 (1976-10-01), Witkowski et al.
patent: 3998807 (1976-12-01), Moffatt
patent: 4097665 (1978-06-01), Ishida et al.
patent: 4531001 (1985-07-01), Robins et al.
patent: 4740503 (1988-04-01), Hori et al.
patent: 5216142 (1993-06-01), Horrobin et al.
patent: 5405837 (1995-04-01), Weber
Hamamura, et al., "Reactions of 2-Acyloxyisobutyl Halides with Nucleosides . . . ", J. Med. Chem., vol. 19, No. 5, pp. 667-674 (1976).
Rubas, et al., "Treatment of Murine L1210 Lymphoid Leukemia . . . ", Int. J. Cancer: 37, pp. 149-154 (1986).
Ozaki, et al., "5-Fluorouracil Derivatives", Chemical and Pharmaceutical Bulletin, vol. 38, No. 11, pp. 3164-3166 (1990).
B.o slashed.rretzen Bernt
Dalen Are
Myhren Finn
Stokke Kjell Torgeir
Kunz Gary L.
Norsk Hydro AS
LandOfFree
5'-O-acylated antiviral nucleosides does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with 5'-O-acylated antiviral nucleosides, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and 5'-O-acylated antiviral nucleosides will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-1725959