Uses of 1-amino-3-(N,N-dimethylamino)-propylidene-1,1-bisphosphonic acid
OwnerEmilio J.A. Roldan, Anibal Perez-Lloret +3inventors
InventorsEmilio J.A. Roldan, Anibal Perez-Lloret, Guillermo Vazquez, Ricardo Boland, Sokrates E. Papapoulos
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Abstract
The present invention relates to a method for maintaining a healthy bone structure by administering to a patient a bone health promoting effective amount of a medicament containing 1-amino-3-(N,N-dimethylamino)-propylidene-1,1-bisphosphonic acid, any of its soluble salts or any of its hydrates.
Claims31
Use of 1-amino-3-(N,N-dimethylamino)-propylidene-1,1-bisphosphonic acid, any of its soluble salts or any of its hydrates, for the manufacture of a medicament for selective modulation of osteoblasts.
Use according to any of the foregoing claims wherein the selective modulation comprises a transient increase of the Ca2+-levels in the osteoblasts.
Use of 1-amino-3-(N,N-dimethylamino)-propylidene-1,1-bisphosphonic acid, any of its soluble salts or any of its hydrates, for the manufacture of a medicament for the maintenance of a healthy bone structure.
Use of 1-amino-3-(N,N-dimethylamino)-propylidene-1,1-bisphosphonic acid, any of its soluble salts or any of its hydrates, for the manufacture of a medicament for the prevention of osteopathies in healthy patients.
Use of 1-amino-3-(N,N-dimethylamino)-propylidene-1,1-bisphosphonic acid, any of its soluble salts or any of its hydrates, for the manufacture of a medicament for the treatment of patients who have recently undergone treatment with corticosteroids.
Use of 1-amino-3-(N,N-dimethylamino)-propylidene-1,1-bisphosphonic acid, any of its soluble salts or any of its hydrates, for the manufacture of a medicament for post-treatment of osteopathies wherein an anti-resorptive activity is not desired.
Use of 1-amino-3-(N,N-dimethylamino)-propylidene-1,1-bisphosphonic acid, any of its soluble salts or any of its hydrates, for the manufacture of a medicament for the treatment of children having an osteopathy.
Use according to any of the foregoing claims wherein 1-amino-3-(N,N-dimethylamino)-propylidene-1,1-bisphosphonic acid, or any of its soluble salts or any of its hydrates, will—after the application of the medicament in a patient—be present at extracellular concentrations in a range between 10−6M and 10−10M.
Use of 1-amino-3-(N,N-dimethylamino)-propylidene-1,1-bisphosphonic acid, any of its soluble salts or any of its hydrates, for the manufacture of a medicament for the stimulation of those signaling cascades and reaction mechanisms mediating the action of 1-amino-3-(N,N-dimethylamino)-propylidene-1,1-bisphosphonic acid, any of its soluble salts or any of its hydrates, which can be blocked by Ca2+-channel blockers.
Use according to any of the foregoing claims wherein 1-amino-3-(N,N-dimethylamino)-propylidene-1,1-bisphosphonic acid, any of its soluble salts or any of its hydrates, is used in doses of 0.01 to 1000 mg/oral application.
Use according to any of the foregoing claims wherein 1-amino-3-(N,N-dimethylamino)-propylidene-1,1-bisphosphonic acid, any of its soluble salts or any of its hydrates, is used in doses of 0.02 to 200 mg/parenteral application.
Use of 1-amino-3-(N,N-dimethylamino)-propylidene-1,1-bisphosphonic acid, any of its soluble salts or any of its hydrates, for the manufacture of a medicament for the mobilization of Ca2+-ions from IP3-sensitive stores.
Use of 1-amino-3-(N,N-dimethylamino)-propylidene-1,1-bisphosphonic acid, any of its soluble salts or any of its hydrates, according to any of the foregoing claims wherein 1-amino-3-(N,N-dimethylamino)-propylidene-1,1-bisphosphonic acid or any of its soluble salts or any of its hydrates is combined with at least one substance selected from the group comprising calcium salts, calcium citrate, calcium carbonate, other amino-substituted bisphosphonates, pharmaceutically active fluorine-containing salts, vitamins of the D-Group and their metabolites, cholecalciferol, calcifediol, calcitriol, ergocalciferol, PTH, anabolic hormones, estrogens, substances with estrogenic activity on the bone, progestogens, androgens, growth hormones, peptides with growth hormone activity, selective modulators of the estrogenic receptor, raloxifene.
Use of 1-amino-3-(N,N-dimethylamino)-propylidene-1,1-bisphosphonic acid, any of its soluble salts or any of its hydrates, according to any of the foregoing claims, wherein the medicament is applied before, during or after treatment with other amino-substituted bisphosphonates.
A method for screening for Ca2+-channel blockers comprising the steps:
- treatment of cells having Ca2+-channels with a putative Ca2+-channel blocker;
- contacting the cells with 1-amino-3-(N,N-dimethylamino)-propylidene-1,1-bisphosphonic acid, any of its soluble salts or any of its hydrates;
- measuring a response as a result of the contacting step.
A method for screening for functional analogues of 1-amino-3-(N,N-dimethylamino)-propylidene-1,1-bisphosphonic acid, any of its soluble salts or any of its hydrates, comprising the steps:
- treatment of cells having Ca2+-channels with Ca2+-channel blockers;
- contacting the cells with the putative functional analogue which, in the absence of any Ca2+-channel blockers, is known to cause a Ca2+-ion influx into the cells;
- measuring a response as a result of the contacting step.
A method for the selective modulation of osteoblasts and/or for the maintenance of a healthy bone structure and/or for the prevention of osteopathies in healthy patients and/or for the treatment of patients who have recently undergone treatment with corticosteroids, and/or for post-treatment of osteopathies where an anti-resorptive activity is not desired, and/or for the treatment of children having an osteopathy and/or for the stimulation of those signaling cascades and reaction mechanisms mediating the action of 1-amino-3-(N,N-dimethylamino)-propylidene-1,1-bisphosphonic acid or any of its soluble salts or any of its hydrates, which can be blocked by Ca2+-channel blockers, and/or for the mobilization of Ca2+ ions from IP3-sensitive stores, comprising
- administering 1-amino-3-(N,N-dimethylamino)-propylidene-1,1-bisphosphonic acid or any of its soluble salts or any of its hydrates alone or in combination with a pharmaceutical carrier to a patient, the 1-amino-3-(N,N-dimethylamino)-propylidene-1,1-bisphosphonic acid or any of its soluble salts or any of its hydrates being administered in doses of 0.1 to 1000 mg/oral application or 0.02 to 200 mg/parenteral application.
Dependencies are inferred from the claim text.