Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Patent
1998-10-26
2000-10-17
Criares, Theodore J.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heterocyclic carbon compounds containing a hetero ring...
514206, 514208, 514213, 514215, A61K 31545, A61K 3155
Patent
active
061332542
DESCRIPTION:
BRIEF SUMMARY
The present invention refers to a new therapeutic use as immunosuppressive agent of a compound of formula I ##STR2## wherein R represents hydrogen or chlorine.
As known, immunity is concerned with the recognition and disposal of foreign antigenic material which is present in the body. Typically the antigens are in the form of particulate matters (i.e., cells, bacteria, etc.) or large proteins or polysaccharide molecules which are recognized by the immune system as being "non-self", i.e., detectably different from or foreign to the animal's own constituents. Potential antigens can be a variety of substances, often proteins, which are most frequently located on the outer surfaces of cells. For example, potential antigens can be found on pollen grains, tissue grafts, animal parasites, viruses, and bacteria. Once the antigenic material is recognized as "non-self" by the immune system, natural (non-specific) and/or adaptive immune responses can be initiated and maintained by the action of specific immune cells, antibodies and the complement system. Under certain conditions or disease states, an animal's immune system may recognize its own constituents as "non-self" and initiate an immune response against "self" material.
An immune response can be carried out by the immune system by means of natural or adaptive mechanisms, each of which are composed of both cell-mediated and humoral elements. Natural mechanisms for immune response refer to those mechanisms involved in essentially non-specific immune reactions which involve the complement system and myeloid cells, such as macrophages, mast cells and polymorphonuclear leukocytes (PMN), in reacting to certain bacteria, viruses, tissue damage and other antigens. These natural mechanisms provide what is referred to as natural immunity. Adaptive mechanisms for immune response refer to those mechanisms which are mediated by lymphocytes (T and B cells) and antibodies which can respond selectively to thousands of different materials recognized as "non-self". These adaptive mechanisms provide what is referred to as adaptive immunity and lead to a specific memory and a permanently altered pattern of response in adaptation to the animal's own environment. Adaptive immunity can be provided by the lymphocytes and antibodies separately or, more commonly, can be provided by the interaction of lymphocytes and antibodies with the complement system and myeloid cells of the natural mechanisms of immunity. The antibodies provide the humoral element of the adaptive immune response and the T-cells provide the cell-mediated element of the adaptive immune response.
More particular by adaptive mechanisms of immune response involve the actions against specific antigens of antibody secreted by B-lymphocytes (or B-cells) as well as the actions of various T-lymphocytes (or T-cells) on a specific antigen, on B-cells, on other T-cells or on macrophages.
The cell-mediated immune response is controlled and monitored by the T-cells through a variety of regulatory messenger compounds secreted by the myeloid cells and the lymphocyte cells. Through the secretion of these regulatory messenger compounds, the T-cells can regulate the proliferation and activation of other immune cells such as B-cells, macrophages, PMN and other T-cells. For example, upon binding a foreign antigen, a macrophage or other antigen presenting cell can secrete interleukin-1 (IL-1) which activates the Helper T-cells. T-cells in turn secrete certain lymphokines, including interleukin-2 (IL-2) and .gamma.-interferon, each of which have a variety of regulatory effects in the cell-mediated immune response.
The ability of the immune system, and in particular the cell-mediated immune system, to discriminate between "self" and "non-self" antigens is vital to the functioning of the immune system as a specific defense against invading microorganisms. "Non-self" antigens are those antigens on substances in the body which are detectably different (or from foreign to) the animals own constituents and "self" antigens are those antigens whi
REFERENCES:
patent: 3991052 (1976-11-01), Berg et al.
patent: 4001086 (1977-01-01), Berg et al.
Patent Abstract of Japan, vol. 96, No. 12 Dec. 26, 1996.
Chemical Abstracts, vol. 113, No. 11, Sep. 10, 1990, Columbus, Ohio Abstract No. 94510t G.F. Gause et al.
Criares Theodore J.
Gruppo Lepetit S.p.A.
Gupta Balaram
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