Therapeutic derivatives of diphosphonates
OwnerJohn F. Hartmann, Dan Farcasiuinventors
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Abstract
Novel chemotherapeutic agents having utility in treating infectious diseases such as periodontal disease, certain urinary tract infections, infectious urinary tract stones, and bone cancer, are obtained by combining chemically a diphosphonate compound with a therapeutic agent effective against the foregoing diseases.
Claims20
A method for preparing a compound of the formula A--(V).sub.m --(R).sub.n --Z, wherein A is the residue of a pharmaceutically active antibiotic chemical entity, V is O, S, NR', CONR', CO--O, O--CO, O--CO--O, CO--S, S--CO, S--CO--S, NR'--CO, OCO--NR', NR'--CO--O, NR'--CO--NR", CO--NR", CO--NR'--NR", NR'--NR"--CO, NR'--C(.dbd.NH)--NR" or NR'--C(.dbd.NH)--NH--C(.dbd.NH)--NR" wherein R, R' and R" are H or an organic or heteroorganic group, and m and n are each 1, or one of m and n is 0,
- comprising reacting a pharmaceutically active antibiotic entity of the formula A--V' wherein V' is halogen, OH, SH, NR'R", COOR', CO--X wherein X is halogen or azido, O--CO--X wherein X is halogen, O--CO--OR', CO--SR', S--CO--X, NR'--CO--X, NR'--NHR", NR'--CN, NR'--C(.dbd.NH)--NH--CN, or metal (covalently bound or ionic),
- with a diphosphonate compound of the formula V'--R--Z wherein V' and R have the previous meanings and Z is ##STR10## which optionally may be protected, the composition of V' in the pharmaceutically active chemical entity of formula A--V' and in the diphosphonate compound of formula V'--R--Z being different and being selected to permit a condensation reaction therebetween.
Dependencies are inferred from the claim text.