Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Phosphorus containing other than solely as part of an...
Patent
1996-07-09
1999-03-30
Criares, Theodore J.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Phosphorus containing other than solely as part of an...
514142, 514144, A61K 31675, A61K 3166
Patent
active
058889914
DESCRIPTION:
BRIEF SUMMARY
This application is a 371 of PCT/AT95/00055 filed Mar. 20, 1995.
The present invention relates to the use of phosphorus derivatives of alkaloids for producing a medicament for treating endocrinopathies.
The term endocrinopathies indicates syndromes in which dyshormonisms are the main cause and determinative of the disease. The causes of such syndromes may reside in diseases of the endocrinal glands, e.g. in an increased hormone production or in a hormome hunger or in a complete absence of hormones, in dysfunctions of the endocrinal glands due to regulatory processes, in derailed hormone formation as a consequence of pathological enzyme systems or in a changed responsiveness of various organs to hormones.
Osteoporosis also can be counted among the endocrinopathies, this being the quantitative reduction of the bone tissue with a retained bone structure due to an increased bone degradation and/or a reduced bone formation, accompanied by the increased occurrence of heparin-containing mast cells in the bone marrow. The etiology of this disease is largely unclear, yet there are strong hints indicating that it is at least very much encouraged by an estrogen deficiency due to the incidence of menopause.
An article by H. Resch et al. (Calcif. Tissue Int. (1989) 45:209-213) proposes the combined administration of calcitonin and a cyclical hormone replacement therapy for the treatment of osteoporosis. Furthermore, in Acta Endocrinologica 1990, 123, p. 14-18, the same author has described the cyclical estrogen/progestogen replacement therapies for treating osteoporosis. The results of these studies indicate that hormone treatment of patients suffering from osteoporosis seems to be promising.
In Osteoporosis, Wilhelm Maudrich Publishers, Wien-Munchen-Bern, 1989, B.E.C. Nordin also argues that at least in women the increased bone resorption involved with osteoporosis presumably goes back to a decreasing functioning of the ovaries, the androstenedione produced by the suprarenal cortex being the only estrogen source after menopause, from which in turn only slight amounts of estradiole are being produced. A small amount of estradiol is formed by the peripheral conversion from testosteron, which in turn is partly formed from the androstenedione of the suprarenal cortex and partly is formed in the post-menopausal ovary. In view of this rather complex mechanism, it is hard to say which hormonal changes are responsible for the increasing bone resorption in menopause. Since the latter is reversible by an estrogen therapy, it is probably due to the decrease of the entire effective estrogen activity (estradiol and estrone). However, the ovary insufficiency need not necessarily have a direct effect on the bones; indirectly it would act via changes in the calcitonin secretion. In the direct post-menopausal phase, the serum calcium and the urine calcium certainly will increase without an increase in the calcium resorption, and in this case the calcium demand may even rise to up to 35 mmol/day. As regards the effects of various hormones or the deficiencies thereof, respectively, on osteoporosis, reference is made to the last-mentioned publication by B.E.C. Nordin.
AT PS 377 988 and AT PS 354 644 disclose methods of producing novel phosphorus derivatives of alkaloides and novel salts of alkaloid derivatives of thiophosphoric acid, respectively. Such compounds have a pharmacological activity and may be used as cytostatic agents. Compound ##STR1## is disclosed in AT 377988 in Example 1.
Surprisingly it has now been found that the phosphorus derivatives of alkaloids disclosed in AT PS 377 988 and AT PS 354 644, respectively, can be used for the production of medicaments for the treatment of endocrinopathies, in particular for the treatment of osteoporosis.
Methods of producing phosphorus derivatives of alkaloids of the general formula (I) ##STR2## wherein m and n=1, 2 or 3; R.sup.1, R.sup.2 and R.sup.3 are each independently H or methoxy, wherein R.sup.1 and R.sup.2 or R.sup.2 and R.sup.3 together also can represent a methylene dioxy gro
REFERENCES:
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Jagiello-Wojtowicz, E., et al. `Effect of Single . . . ` Drugs Under Experimental and Clinical Research, vol. 18, 1992, pp. 85-87.
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