Pharmaceutical compositions comprising methanediphosphonic acid derivatives and macrocyclic polyethers
AssigneeCiba-Geigy Corporation
InventorsGerard Flesch, Jean-Marie Lehn
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Abstract
The invention relates to pharmaceutical compositions for peroral administration comprising (a) pharmaceutically useful methanediphosphonic acid derivatives, e.g. those of formula I ##STR1## wherein R.sub.1 and R.sub.2 are as defined in the specification, or pharmaceutically acceptable salts thereof, (b) specific macrocyclic polyethers and optionally (c) pharmaceutically acceptable adjuvants. The pharmaceutical compositions are prepared in a manner known per se. A method of treating hypercalcemia and osteolytic bone metastases with these compositions is also disclosed herein.
Claims15
A pharmaceutical composition comprising
- (1) at least one pharmaceutically useful methanediphosphonic acid derivative of formula I ##STR6## wherein R.sub.1 is hydrogen or hydroxy;
- R.sub.2 is --A--R.sub.3, wherein A is lower alkylene;
- and R.sub.3 is
- hydrogen;
- unsubstituted amino or amino which is mono- or disubstituted by lower alkyl,
- or a pharmaceutically acceptable salt thereof;
- (2) at least one macrocyclic polyether of formula II ##STR7## wherein X.sub.1 -X.sub.4 are each independently of the other carboxy, carbamoyl or N-mono- or N,N-disubstituted carbamoyl, or a pharmaceutically acceptable salt thereof;
- and optionally
- (3) pharmaceutically acceptable adjuvants.
A method for the treatment of hypercalcaemia or osteolytic bone metastases in a mammal comprising administering to said mammal a therapeutically effective amount of a pharmaceutical composition comprising (1) at least one pharmaceutically useful methanediphosphonic acid derivative of formula I ##STR10## wherein R.sub.1 is hydrogen or hydroxy;
- R.sub.2 is --A--R.sub.3, wherein A is lower alkylene;
- and R.sub.3 is
- hydrogen;
- unsubstituted amino or amino which is mono- or disubstituted by lower alkyl,
- or a pharmaceutically acceptable salt thereof;
- (2) at least one macrocyclic polyether of formula II ##STR11## wherein X.sub.1 -X.sub.4 are each independently of the other carboxy, carbamoyl or N-mono- or N,N-disubstituted carbamoyl, or a pharmaceutically acceptable salt thereof;
- and optionally (3) pharmaceutically acceptable adjuvants.
Dependencies are inferred from the claim text.