Thio-substituted phosphonate compounds

C - Chemistry – Metallurgy – 07 – F

Patent

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Details

C07F 9/38 (2006.01) A61K 31/66 (2006.01) C07F 9/547 (2006.01)

Patent

CA 2188066

The present invention relates to novel sulfur-containing phosphonate compounds and novel thio-substituted compounds, including bisphosphonates, phosphonoalkylphosphonates, phosphonocarboxylates, and phosphonosulfonates, and the pharmaceutically-acceptable salts and esters thereof. The present invention further relates to pharmaceutical compositions containing a safe and effective amount of a compound of the present invention, and pharmaceutically-acceptable excipients. Finally, the present invention relates to methods for osteoprotective treatment and prevention of pathological conditions characterized by abnormal calcium and phosphate metabolism in humans or other mammals, including treating or preventing osteoporosis and arthritis, especially rheumatoid arthritis and osteoarthritis. This method comprises administering to a human or other mammal in need of such treatment of a safe and effective amount of a compound or composition of the present invention, or a compound or composition disclosed herein. Novel sulfur-containing compounds of the present invention have general structure (I). Novel thio-substituted compounds of the present invention have structure (II), provided that at least one of R, R2, R3 or R5 is SR6 or R8SR6. Finally, the present invention relates to the treatment of arthritis in humans or other mammals in need of such treatment comprising administering to said human or other mammal a safe and effective amount of a thio-substituted phosphonate compound having structure (III), provided that at least one of R1, R2, R3 or R5 must be SR6 or R8SR6.

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