Bicyclic diphosphonate compounds, pharmaceutical compositions, and methods for treating abnormal calcium and phosphate metabolism
AssigneeP&G Pharmaceuticals, Inc.
InventorsFrank H. Ebetino, Kent W. Buckingham, Jocelyn E. McOsker
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Abstract
The present invention relates to novel compounds having nitrogen-containing, saturated bicyclic cylopentane-fused rings which are geminally disubstituted with phosphonate groups. Most preferred compounds of the present invention have the general structure: ##STR1## The present invention further relates to pharmaceutical compositions containing these novel compounds. Finally, this invention relates to methods for treating or preventing diseases characterized by abnormal calcium and phosphate metabolism by utilizing a compound or pharmaceutical composition of the present invention.
Claims16
A nitrogen-containing, saturated bicyclic cyclopentane ring-containing diphosphonic acid, or a pharmaceutically-acceptable salt thereof, having one of the following formulas:
- ##STR13## wherein m and n are integers from 0 to 3;
- m+n=3;
- each R.sup.1 is independently selected from the group consisting of hydrogen, alkyl having from 1 to 6 carbon atoms, halogen, hydroxy, and --OR.sup.3 ;
- R.sup.2 is R.sup.3 C(O)--, phenyl or benzyl;
- and each R.sup.3 is alkyl having from 1 to 3 carbon atoms.
An Octahydro-1-pyrindine-6,6-diphosphonic acid, or a pharmaceutically-acceptable salt thereof, having the following formula:
- ##STR16## wherein each R.sup.1 is independently selected from the group consisting of hydrogen, alkyl having from 1to 6 carbon atoms, and combinations thereof;
- R.sup.2 is R.sup.3 C(O)--, phenyl, or benzyl;
- and R.sup.3 is selected from the group consisting of hydrogen and alkyl having from 1 to 3 carbon atoms.
A nitrogen-containing, saturated bicyclic cyclopentane ring-containing diphosphonic acid, or a pharmaceutically-acceptable salt thereof, having one of the following formulas:
- ##STR17## wherein m and n are integers from 0 to 5;
- m+n is the integer 0, 1, 2, 4, or 5;
- each R.sup.1 is independently selected from the group consisting of hydrogen, alkyl having from 1 to 6 carbon atoms, --OR.sup.3, --CO.sub.2 R.sup.3, --O.sub.2 CR.sup.3, NR.sup.3.sub.2, --N(R.sup.3)C(O)R.sup.3, --C(O)N(R.sup.3).sub.2, halogen, --C(O)R.sup.3, phenyl, benzyl and nitro;
- R.sup.2 is hydrogen, alkyl having from 1 to 6 carbon atoms, R.sup.3 C(O)--, phenyl, and benzyl;
- each R.sup.3 is independently selected from the group consisting of hydrogen and alkyl having from 1 to 3 carbon atoms.
Dependencies are inferred from the claim text.