Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Phosphorus containing other than solely as part of an...
Patent
1996-07-22
1999-02-02
Fay, Zohreh
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Phosphorus containing other than solely as part of an...
A61K 3166
Patent
active
058665579
DESCRIPTION:
BRIEF SUMMARY
Damage of tissues can be induced in many ways. Inducing factors can be correlated with mechanical effects, immunological effects or chemical effects. Microorganisms such as virus, bacteria and fungus can induce tissue damage and exposure to heat, fire, radiation, cold and blows most often results in such damage. Many diseases like asthma, eczema, psoriasis, rheumatoid arthritis, diabetes and arteriosclerosis also involve different types of tissue damage.
The existing treatments of diseases connected to tissue damage and inflammatory conditions are based on drugs such as non steroid antiinflammatory drugs (NSAID), steroids, antibiotics and cytostatics. In some cases also surgical therapy is used.
Existing drugs often suffer from limited effectiveness in combination with serious side effects. Toxic effects appearing from the treatment with NSAID:s can consist of gastrointestinal side effects, allergic reactions and side effects in the central nervous system. Treatment with steroids often results in side effects such as osteoporosis and fractures, increased susceptibility to infections and peptic ulcerations.
According to the present invention it has surprisingly become possible to overcome and reduce the above mentioned injuries and destructions of tissues by the use of an ester of inositoltrisphosphate for the preparation of a medicament for preventing, alleviating or combatting inflammatory conditions in mammals including man.
The invention also covers the use of an ester of inositoltrisphosphate for the preparation of a medicament for preventing, alleviating or combatting tissue damage in mammals including man.
In preferred embodiments of the invention the medicament is intended to be used for preventing, alleviating or combatting tissue damage related to oedema formation and vascular leakage. In other preferred embodiments of the invention the medicament is intended to be used for preventing, alleviating or combatting tissue damage related to burns, rhinitis, asthma and arthritis.
The invention relates to the use of an ester of inositoltrisphosphate for preparing a medicament for preventing, alleviating or combatting for example the following conditions: fire such as burns of first, second or third degree, trauma i.e. wounds or injuries caused by physical damage, or cold; microorganisms such as radiation, sepsis and injuries caused by e.g. bee-stings, snake-bites etc; immunological component is strongly expressed such as rhinitis, hayfever, asthma, psoriasis, vasculitis and eczema. Furthermore the invention relates to treatment of tissue damage and inflammatory conditions related to erythema, herpes and arthritis, injuries caused by or following surgery and operations of grafts, catheters etc. and injuries caused by or occurring in the border zone of an infarct of cardiac type, cerebral type or any other type.
Other injuries of tissues related to diseases such as uveitis, otitis, stomatitis, peritonitis, sinusitis, gastroenteritis, colitis and cystitis are also related to the invention.
The medicament is effective against tissue damage connected to the above mentioned conditions but also to other conditions where tissue damage and inflammations occurs.
From the European Patent No 179439 a pharmaceutical composition comprising as a pharmaceutically active ingredient at least one isomer of inositoltrisphosphate is known. In said patent the effect of this pharmaceutical composition is shown for different areas, such as platelet aggregation.
The production of esters of inositoltrisphosphate and the isolation of the different isomers thereof are disclosed in the European Patent Application No 0269105.
The therapeutic profile of esters of inositoltrisphosphates differs from the profile of inositoltrisphosphates in many important aspects. Chemical properties such as lipophilicity, solubility and pK.sub.A -values are changed which affect the potency and selectivity of the compound.
Furthermore the susceptibility against enzymatic degradation is markedly lowered for esters of inositoltrisphosphates which result i
REFERENCES:
patent: 4515722 (1985-05-01), Yang et al.
P.B. Curtis-Prior, "Prostaglandins, an Introduction to Their Biochemistry, Physiology and Pharmacology," (1976) North-Holland Publishing Company, p. 43.
Gustafsson Torgny
Persson Lars
Rehnberg Nicola
Fay Zohreh
Perstorp AB
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