Henkel & Cie G.m.b.h.

Henkel Kommanditgesellschaft Auf Aktien

Henkel Kommanditgesellschaft Auf Aktien (henkel Kgaa)

Manfred Schmidt-Dunker

Christian Gloxhuber

Walter Ploger

Wolfgang Greb

Helmut Blum

Karl-Heinz Worms

Matthias Potokar

A method for the treatment of diseases relating to the abnormal deposition or dissolution of difficultly soluble calcium salts in the body or mouths of warm-blooded animals which consists of administering orally, parenterally or topically to said warm-blooded animals, a safe but effective amount of at least one pharmacologically acceptable aminoalkane diphosphonic acid derivative or a water-soluble salt thereof.

Method of treatment of calcium disorders using aminoalkane-diphosphonic

Aqueous solutions of .sup.99 technetium salts wherein the .sup.99 technetium is in reduced valencey state, when administered to mammals, permit identification of the skeleton and of calcareous tumors by scintigraphy (radiographic scanning). The solutions are conveniently prepared by mixing one ore more phosphonic acids (or their salts) with one or more reducing salts, and adding the mixture to an aqueous solution of a pharmaceutically acceptable .sup.99 pertechnetate salt. Reduction of the valence of the technetium occurs rapidly, and the resulting solution is adequately stable for use in scintigraphy. The phosphonic acid and reducing salt components can be premixed. Aqueous solutions of the premix are stable for long periods of time in the absence of free oxygen and the premix is stable to air so long as it is dry.

Compositions for preparation of aqueous solutions of salts of lower

Aqueous solutions of .sup.99 technetium salts wherein the .sup.99 technetium is in reduced valencey state, when administered to mammals, permit identification of the skeleton and of calcareous tumors by scintigraphy (radiographic scanning). The solutions are conveniently prepared by mixing one or more phosphonic acids (or their salts) with one or more reducing salts, and adding the mixture to an aqueous solution of a pharmaceutically acceptable .sup.99 pertechnetate salt. Reduction of the valence of the technetium occurs rapidly, and the resulting solution is adequately stable for use in scintigraphy. The phosphonic acid and reducing salt components can be premixed. Aqueous solutions of the premix are stable for long periods of time in the absence of free oxygen and the premix is stable to air so long as it is dry.

Compositions for preparation of aqueous solutions of low valence .sup.99

The water-soluble calcitonins and the water-soluble pharmaceutically-acceptable compounds of acidic nature which are effective against Paget's disease and which contain at least two acidic groups separated by not more than two carbon atoms act synergistically in inhibiting a pathological increased calcium metabolism rate (including the solubilization of bone calcium which occurs in Paget's disease). The components in combination, when administered in respectively preferred amounts, inhibit or arrest loss of calcium by the bones of the body with less severe side effects than those caused by equivalent therapeutic doses of the calcitonin alone or by equivalent therapeutic doses of the compounds of acidic nature alone.

Composition and method for the treatment of disorders of calcium

Pyrrolidone-5,5-diphosphonic acids having the formula ##STR1## wherein R is a member selected from the group consisting of hydrogen and alkyl having from 1 to 6 carbon atoms; as well as their water-soluble salts. The pyrrolidone-5,5-diphosphonic acids are excellent sequestering agents especially for alkaline earth metal ions. They are stabilizers for percompounds and are useful in the delaying of the setting times for gypsum. In addition, the compounds are useful as cosmetic preparations such as toothpastes and mouthwashes where they prevent formation of tartar and plaque and are useful in therapy in the treatment of diseases related to the abnormal deposition or dissolution of difficultly soluble calcium salts in the animal body.

Pyrrolidone-5,5-diphosphonic acids

Azacycloalkane-2,2-diphosphonic acids having the formula ##EQU1## wherein R is a member selected from the group consisting of hydrogen and alkyl having from 1 to 3 carbon atoms and n is an integer from 3 to 5; as well as their water-soluble salts. The azacycloalkane-2,2-diphosphonic acids are excellent sequestering agents especially for alkaline earth metal ions. They are stabilizers for percompounds and are useful in the delaying of the setting times for gypsum. In addition, the compound are useful in cosmetic preparations such as toothpastes and mouthwashes where they prevent formation of tartar and plaque and are useful in therapy in the treatment of diseases related to the abnormal deposition or dissolution of difficultly soluble calcium salts in the animal body.

Azacycloalkane-2,2-diphosphonic acids

Therapeutic methods employing cyclic aminophosphonic acids having the formula ##EQU1## wherein R is a member selected from the group consisting of hydrogen and alkyl having from 1 to 6 carbon atoms and n is an integer from 1 to 4; as well as their water-soluble salts. The cyclic aminophosphonic acids are excellent sequestering agents especially for alkaline earth metal ions, useful in cosmetic preparations such as toothpastes and mouthwashes where they prevent formation of tartar and plaque and in therapy in the treatment of diseases related to the abnormal deposition or dissolution of difficulty soluble calcium salts in the animal body.

Therapeutic methods employing cyclic aminophosphonic acids

A method for the treatment of diseases relating to the abnormal deposition or dissolution of difficutly soluble calcium salts in the body of warm-blooded animals which consists of administering orally, parenterally or topically to said warm-blooded animals, a safe but effective amount of at least one pharmacologically acceptable phosphonoalkane-polycarboxylic acid and water-soluble salts thereof.

Method of treatment of calcium disorders using

A method for the treatment of diseases relating to the abnormal deposition or dissolution of difficulty soluble calcium salts in the body or mouths of warm-blooded animals which consists of administering orally, parenterally or topically to said warm-blooded animals, a safe but effective amount of at least one pharmacologically acceptable aminoalkane diphosphonic acid derivative or a water-soluble salt thereof.

Method of treatment of calcium disorders using aminoalkane-diophosphonic

Pyrrolidone-5,5-diphosphonic acids having the formula ##EQU1## wherein R is a member selected from the group consisting of hydrogen and alkyl having from 1 to 6 carbon atoms; as well as their water-soluble salts. The pyrrolidone-5,5-diphosphonic acids are excellent sequestering agents especially for alkaline earth metal ions. They are stabilizers for percompounds and are useful in the delaying of the setting times for gypsum. In addition, the compounds are useful as cosmetic preparations such as toothpastes and mouthwashes where they prevent formation of tartar and plaque and are useful in therapy in the treatment of diseases related to the abnormal deposition or dissolution of difficultly soluble calcium salts in the animal body.

Azacycloalkane-2,2-diphosphonic acids having the formula ##EQU1## wherein R is a member selected from the group consisting of hydrogen and alkyl having from 1 to 3 carbon atoms and n is an integer from 3 to 5; as well as their water-soluble salts. The azacycloalkane-2,2-diphosphonic acids are excellent sequestering agents especially for alkaline earth metal ions. They are stabilizers for percompounds and are useful in the delaying of the setting times for gypsum. In addition, the compound are useful in cosmetic preparations such as toothpastes and mouthwashes where they prevent formation of tartar and plaque and are useful in therapy in the treatment of diseases related to the abnormal deposition or dissolution of difficulty soluble calcium salts in the animal body.

Growing community of inventors

Dusseldorf, Germany

Manfred Schmidt-Dunker