Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Radical -xh acid – or anhydride – acid halide or salt thereof...
Patent
1999-01-04
2000-03-14
Henley, III, Raymond
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Radical -xh acid, or anhydride, acid halide or salt thereof...
A61K 31205
Patent
active
060373733
DESCRIPTION:
BRIEF SUMMARY
This is a 371 of PCT/IT97/00113 filed May 15, 1997.
The present invention relates to a novel therapeutic use of L-acetylcarnitine, L-isovalerylcarnitine, L-propionylcarnitine or pharmacologically acceptable salts thereof for increasing the levels of IGF-1 (insulin-like growth factor 1) for the therapeutic treatment or prophylaxis of cytological disorders or diseases related to IGF-1. More particularly, the present invention relates to the use of L-acetylcarnitine, L-isovalerylcarnitine, L-propionylcarnitine or pharmacologically acceptable salts thereof for the therapeutic treatment or prophylaxis of individuals in whom IGF-1 contributes towards the pathogenesis of a particular disease or provokes cytological disorders.
Like other growth factors, IGF-1 promotes cell growth and differentiation. The administration of IGF-1 obtained as a protein purified by molecular biology methods has made it possible to confirm the effects observed in vitro with cells, on animal models and in man. Essentially, the action of IGF- 1 is similar to that of insulin, that is to say an increase in the uptake of glucose, a reduction in ketones and fatty acids in the serum and an increase in protein synthesis. In accordance with these and other metabolic effects, clinical studies have been undertaken in order to evaluate the efficacy of IGF-1 in a range of diseases. IGF- 1 has been administered to patients with type-II diabetes, to cachectic patients, to patients with ischemic damage at the neuronal, myocardial or renal level, and has been proposed for repairing and regenerating tissues (W.L. Lowe, Insulin-like growth factors, Scientific American Science and Medicine p. 62, March 1996).
From the above, it is clear that the administration of IGF-1 may be therapeutically useful in various morbid conditions. Examples of diseases or disorders which may be prevented, cured or improved by the administration of IGF-1 include neuropathies of the optic nerve and of the olfactory nerve, neuralgia of the trigeminal nerve, Bell's paralysis, amyotrophic lateral sclerosis and other motor neuron diseases, degeneration of the retina, osteoporosis, arthropathy, arthritis, cervical spondylosis and hernia of the intervertebral discs, clinical syndromes of reduced height, cachexia, acute or chronic hepatic necrosis, Turner's syndrome, sarcopoenia, growth hormone insensitivity syndromes, diabetes, obesity, asthenia in general and in particular myasthenia and heart asthenia, immunodeficiences and reperfusion injuries. IGF- 1 moreover appears to be useful for the cicatrization of wounds, the healing of ulcers, the treatment of burns, tissue regeneration in general and in particular that of cutaneous, intestinal and hepatic tissue, and the formation of dentine.
Unfortunately, the administration of IGF- 1 in man brings about undesirable effects such as oedema, pain in the temporomandibular joint and arthralgia. These symptoms are such as to prevent the administration of IGF-1 from being recommended or are responsible for interrupting the treatment. It is therefore necessary to find novel substances which are capable of inducing the production of IGF- 1.
According to the present invention, the administration of L-acetylcarnitine, L-isovalerylcarnitine, L-propionylcarnitine or pharmacologically acceptable salts thereof is capable of inducing the production of IGF- 1 without the undesirable effects produced by the administration of exogenous IGF-1.
In the description which follows, the expression pharmacologically acceptable salt of L-acetylcarnitine, of L-isovalerylcannitine or of L-propionylcarnitine is understood to refer to any salt of the above with an acid which does not give rise to undesirable toxicity or side-effects. Such acids are well known to pharmacologists and to experts in the pharmaceutical field.
Non-limiting examples of such salts are: chloride; bromide; iodide; aspartate, in particular hydrogen aspartate; citrate, in particular hydrogen citrate; tartrate; phosphate, in particular hydrogen phosphate; fumarate, in particular hydrogen fumarate
REFERENCES:
patent: 5227518 (1993-07-01), Cavazza
patent: 5240961 (1993-08-01), Shug
patent: 5656628 (1997-08-01), Weil et al.
W.G. Sannita, et al., Documenta Ophthalmologica, vol. 70, pp. 89-96, "Effects of Intravenous L-acetylcarnitine on Retinal Oscillatory Potentials", 1988.
D.J. Paulson, et al., Cardiovascular Research, vol. 20, No. 79 pp. 536-541, "Protection of the Ischaemic Myocardium by L-propionylcarnitine: Effects on the Recovery of Cardiac Output After Ischaemia and Reperfusion, Carnitine Transport, and Fatty Acid Oxidation", 1986.
A.J. Liedtke, et al., American Journal of Physiology, vol. 255, No. 1, Pt. 2, pp. H169-H176, "Effects of L-propionylcarnitine on Mechanical Recovery During Reflow in Intact Hearts", 1988.
C. Adembri, et al., Histology and Histopathology, vol. 9, No. 4, pp. 683-690, "Ischemia-Reperfusion of Human Skeletal Muscle During Aortiliac Surgery: Effects of Acetylcarnitine", 1994.
J.A. Leipala, et al., Journal of Applied Physiology, vol. 71, No. 4, pp. 1518-1522, "Protection of the Reperfused Heart by L-propionylcarnitine", 1991.
Henley III Raymond
Mendes s.r.l.
Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.
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