Zwitterionic compositions and methods as biological response mod

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

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514 76, 514 77, 514564, 424531, A61K 31395

Patent

active

060719192

DESCRIPTION:

BRIEF SUMMARY
BACKGROUND OF THE INVENTION

In the world population, the incidence of cancer is very significant. It is estimated that one in four persons will develop cancer sometime in their life. Half of all persons who develop cancer will die from it. The incidence of cancer-related deaths has been doubling every thirty years in the United States. There are many factors associated with the increasing incidence of disease. Many people live longer, and the incidence may increase due to an aging population. Environmental toxins and/or genetic changes may also play a role in the increase.
There has also been an increase in the incidence of infectious diseases, particularly viral infections. Many virulent strains are now seen. Virally-mediated infections, such as hepatitis (A, B and C) and HIV-type infections have had a significant impact on the population. Some cancers, such as Kaposi's sarcoma, are associated with viral infections.
There are many diseases associated with autoimmune disorders. Rheumatoid arthritis and myasthenia gravis are examples. The etiology of many autoimmune diseases is not clear. Genetic and/or environmental aspects may contribute in several ways to alter hemopoietic and immune responses. Certain drugs may trigger autoimmune responses as well as induce immunosuppressed states.
There are four basic approaches to the treatment of cancer. These approaches are sometimes combined in the form of multimodality therapies. The basic approaches are surgical resection, chemotherapy, radiation and immunotherapy. Alternative approaches include naturopathy, herbal treatments and acupuncture.
Therapies for autoimmune disease have been limited. Primarily, the use of steroids has been a mainstay. Advanced cases of diseases, such as rheumatoid arthritis and myasthenia gravis, rarely respond well.
Infectious disease therapies have had many advances with the use of antibiotics. There have been a few antiviral compounds developed. Their use is fairly limited to a few types of infection. HIV is yet to respond to any significant therapy. Immune therapies have had limited success in hepatitis.
Over the last fifty years, there has been a slow development of various immunotherapies. These have included the use of specific cytokines, chemokines, lymphokines and other immunological substances derived from cell culture research and cloned. In the past, it has been shown that certain fractions of cell cultures have produced specialized responses in tumors. Chemotherapeutic agents and radiation have generated some tumor responses, but have high toxicity.
The need for developing agents and compositions that effectively treat cancer, cancer pain, immunologically-mediated diseases and certain infectious diseases continues to be very important.


SUMMARY OF THE INVENTION

The present invention relates to a method for the treatment of diseases in mammals by the administration of zwitterionic compositions as safe and effective biological response modifiers to the mammals and to the zwitterionic compositions used and the preparation of such zwitterionic compositions for use in treatment.
In particular, the invention concerns a method of treating mammals to stimulate the immunological system and to induce the production of hypercellular bone marrow and extramedullary hematopoiesis in the treated mammal.
The present invention demonstrates that zwitterionic molecules have a definitive effect as a biological response modifier (BRM). Zwitterionic molecules are substances that have neither a negative nor a positive charge. Zwitterions are compounds having a net charge on the molecule which is zero and which have positive and negative groups that are equally ionized in the molecule, and are dipolar molecules containing, for example, hydroxy groups and amino groups and also acid groups, like phosphoric, carboxylic or sulfonic acid groups, and, for example, generally having pK.sub.a in the range of 6.15 to 8.4.
A number of zwitterion compounds may be employed in the treatment of mammal diseases as active ingredients, either alone or in various

REFERENCES:
patent: 4753942 (1988-06-01), O'Sullivan
Stapleton et al., J Pharm Pharmacol 46:745-750, 1994.

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