Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Patent
1990-01-18
1991-06-04
Friedman, Stanley J.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heterocyclic carbon compounds containing a hetero ring...
A61K 3150, A61K 31495
Patent
active
050214179
DESCRIPTION:
BRIEF SUMMARY
FIELD OF THE INVENTION
The present invention relates to the use of folinic acid compounds belonging to the family of the folinic acid derivatives and analogues comprising in their molecule the 5,6,7,8-tetrahydrofolic acid radical of the formula ##STR1## in which the dashes --- denote a bond with a hydrogen atom in the 4, 5 and/or 10 positions, a bond with an OH group as a substituent of at least one of the two carbonyl groups of the glutamyl residue, or any other suitable group in the 4, 5 and/or 10 positions or as a substituent of at least one of the two carbonyl groups of the glutamyl residue.
PRIOR ART
It is known that folic acid, which corresponds to the systematic nomenclature of N-[4-[[(2-amino-1,4-dihydro-4-oxo-6-pteridinyl)methyl]amino]benzoyl]-L-glu tamic acid, and its alkali metal and alkaline earth metal salts act in the organism as vitamin substances [see Merck Index, 10th edition (1983), pages 602-603].
It is known that folinic acid, which corresponds to the systematic nomenclature of N-[4-[[(2-amino-5-formyl-1,4,5,6,7,8-hexahydro-4-oxo-6-pteridinyl)methyl]a mino]benzoyl]-L-glutamic acid and to the abbreviated nomenclature of 5-formyl-5,6,7,8-tetrahydrofolic acid, and its salts act in the organism as antidotes to folic acid antagonists [see Merck Index, 10th edition (1983), page 603].
It is known that methotrexate, which corresponds to the systematic nomenclature of N-[4-[[(2,4-diamino-6-pteridinyl)methyl]methylamino]benzoyl]-L-glutamic acid and to the abbreviated nomenclature of 4-amino-N.sup.10 -methylfolic acid, is a folic acid antagonist and acts in the organism as an antineoplastic and antimetabolite. More precisely, it is known that methotrexate blocks (i) the conversion of folic acid to folinic acid and (ii) the synthesis of DNA, on the one hand, and acts as a substance which induces blood platelet aggregation, on the other. It is also known that methotrexate has caused accidents when administered to cancer patients [see Merck Index, 10th edition (1983), pages 859-860].
It is known in particular that the article by M. T. SHAW, Scand. J. Haemat., 10, pages 24-27, 1973, relating to pregnant women presenting trophoblastic tumours, refers to a decrease in the number of platelets after the administration of a treatment comprising a combination of methotrexate (administered intravenously or intramuscularly) and folinic acid (administered intramuscularly). The protocol followed and the results provided by said article do not suggest that folinic acid has blood platelet aggregation inhibiting properties, especially since said acid was not used by itself.
It is known that methopterin, which corresponds to the systematic nomenclature of N-[4-[[(2-amino-4-hydroxy-6-pteridinyl)methyl]methylamino]benzoyl]-L-gluta mic acid and is also called N.sup.10 -methylfolic acid, is a folic acid derivative which has been described in U.S. Pat. No. 2,563,707 [see also Merck Index, 10th edition (1983), page 859].
Finally, it is known that 5-methyl-5,6,7,8-tetrahydrofolic acid, which corresponds to the systematic nomenclature of N-[4-[[(2-amino-1,4,5,6,7,8-hexahydro-5-methyl-4-oxo-6-pteridinyl)methyl]a mino]benzoyl]-L-glutamic acid and has the abbreviated nomenclature of 5-N-Me-THF, on the one hand, and folinic acid, on the other, have been proposed in therapy as antistress drugs.
SUBJECT OF THE INVENTION
According to the invention, a novel use of a folinic acid substance or substance analogous to folinic acid as a platelet aggregation inhibitor is proposed.
More precisely, a novel use in therapy of a folinic acid substance or substance analogous to folinic acid is recommended according to the invention, said use being characterized in that a substance selected from the group consisting of 5,6,7,8-tetrahydrofolic acid, its derivatives and mixtures thereof is used in order to obtain a platelet aggregation inhibiting drug intended for a therapeutic indication in cases where it is appropriate to inhibit or reduce blood platelet aggregation.
This novel use in therapy according to the invention is neither descri
REFERENCES:
Stadtler et al.--Onkologie, vol. 7, No. 4, Aug. 1984, 238-242.
Shaw--Scand. J. Haemat., (1973), vol. 10, pp. 24-27.
Cooper et al.--Brit. J. of Haematology, 1976, 32, pp. 387-394.
Nixon--Clinical and Experimental Pharmacology & Physiology, (1979), Suppl. 5, pp. 35-41.
Friedman Stanley J.
Spiral Recherche et Developpement
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