Heterocycle-substituted diphosphonate compounds,...

C - Chemistry – Metallurgy – 07 – F

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C07F 9/58 (2006.01) A61K 31/675 (2006.01) C07F 9/59 (2006.01) C07F 9/645 (2006.01) C07F 9/6509 (2006.01) C07F 9/6512 (2006.01) C07F 9/6521 (2006.01)

Patent

CA 1321198

NOVEL HETEROCYCLE-SUBSTITUTED DIPHOSPHONATE COMPOUNDS, PHARMACEUTICAL COMPOSITIONS, AND METHODS OF TREATING ABNORMAL CALCIUM AND PHOSPHATE METABOLISM ABSTRACT OF THE DISCLOSURE The present invention relates to novel heterocycle-substituted diphosphonic acids, and the pharmaceutically-acceptable salts and esters thereof, in which the diphosphonate-substituted carbon atom moiety is attached to a carbon atom in a nitrogen-containing six membered ring hetero- cycle, preferably a piperidine ring. The heterocycle-substituted diphosphonic acid compounds have the general structure: Image wherein Z is a nitrogen-containing six membered ring heterocycle moiety selected from piperidinyl, diazinyl and triazinyl; m, n and m+n are from about 0 to about 10 Q is a covalent bond or a moiety selected from oxygen, sulfur or nitrogen; and R1, R2, and R3 are substituent groups. 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. dr(ZYA:DR6446a)

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