Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Phosphorus containing other than solely as part of an...
Patent
1993-02-11
1994-02-08
Friedman, S. J.
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
052848396
DESCRIPTION:
BRIEF SUMMARY
The present invention relates to the use of at least one isomer of inositoltrisphosphate (IP.sub.3) for the preparing of a medicament effective as a neuropeptide Y- (NPY-) antagonist and to a pharmaceutical composition comprising at least one specific isomer of IP.sub.3 and a pharmaceutically active compound effective in the cardiovascular, renal and/or cerebral area.
Neuropeptide Y (NPY) is a peptide present in the central and peripheral nervous system. The peptide co-exists with noradrenaline in many neurons and acts as a neurotransmittor per se or synergistically together with noradrenaline. NPY-containing fibres are numerous around arteries especially for arteries in the heart but also arteries in the respiratory tract, the gastrointestinal tract and genitourinary tract. NPY is also present in the cerebrum with effects on e.g. blood pressure and release of different hormones.
NPY per se has vasoconstrictor effects, i.e. there is observed an increased blood pressure, local vasoconstriction and reduced heart rate when the substance is infused to animals.
NPY belongs to the pancreatic polypeptide (PP) family which also includes for example peptide YY (PYY).
In man and animals abnormal NPY-levels are associated with for example the following diseases or conditions:
Diseases pertaining to the vascular system, the heart, blood vessels and the peripheral circulation such as vasospasm, angina, hemorrhage, high blood pressure, cardiac hypertrophy, congestive heart failure and myocardial infarction;
Diseases pertaining to the renal system such as abnormal renal conditions like impaired flow of fluid and renal failure;
Cerebral diseases and diseases related to the central nervous system such as stroke and conditions associated with stroke, cerebral vasospasm and hemorrhage and depression;
Abnormal drink and food intake such as obesity;
Diabetes or complications of diabetes;
Inflammatory diseases such as arthritis;
Respiratory diseases such as asthma;
Regulation of hormone release for example from the pituitary.
When for example well-known drugs effective against hypertension such as .beta.-blockers are used to control the blood pressure, the raised level of NPY is not normalized. This phenomenon is anticipated to be one important reason for the increased incidence of people with high blood pressure to get secondary cardiovascular complications. There are no compounds known to antagonize NPY or the effects of NPY.
According to the present invention it has surprisingly become possible to overcome and reduce the above mentioned disorders by the use of at least one isomer of inositoltrisphosphate (IP.sub.3) for the preparing of a medicament for preventing, alleviating or combatting these diseases and conditions in mammals including man.
In preferred embodiments of the invention the medicament is intended to be used as an NPY-antagonist. In other preferred embodiments of the invention the medicament is intended to be used for preventing, alleviating or combatting diseases pertaining to the heart, blood vessels, the renal system or cerebral diseases.
In addition the present invention relates to a pharmaceutical composition comprising at least one isomer of inositoltrisphosphate (IP.sub.3) in combination with a pharmaceutically active compound effective in the cardiovascular, renal and/or cerebral area.
The invention also covers the use of inositoltrisphosphate (IP.sub.3) in combination with another pharmaceutically active compound for preparing of a medicament for preventing, alleviating or combatting diseases pertaining to the cardiovascular, renal and cerebral diseases in mammals including man.
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 present invention relates to the use of at least one isomer of IP.sub.3 for preparing a medicament for preventing, alleviating or comb
REFERENCES:
patent: 4735936 (1988-04-01), Siren
patent: 4777134 (1988-10-01), Siren
patent: 4797390 (1989-01-01), Siren
Edvinsson Lars
Siren Matti
Friedman S. J.
Perstorp AB
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