C - Chemistry – Metallurgy – 07 – F
Patent
C - Chemistry, Metallurgy
07
F
C07F 9/547 (2006.01) A61K 31/66 (2006.01) C07F 9/38 (2006.01) C07F 9/572 (2006.01) C07F 9/576 (2006.01) C07F 9/60 (2006.01) C07F 9/6561 (2006.01)
Patent
CA 2136821
The present invention relates to a quaternary nitrogen-containing, saturated or unsaturated monocyclic and bicyclic ring containing phosphonate and the pharmaceutically-acceptable salts and esters thereof, having the following structure: (see fig. I) wherein (a) each X and Y are independently selected from nil, O, S, NR1 and N+(R2)2; if no R1 is N+(R2)2, then at least one of X or Y must be N+(R2)2; (b) m and n and m+n are integers from 0 to 5; p and q and p+q are integers from 0 to 3; (c) s is an integer from 0 to 2 and when m + n = O and X is nil, s = 2; (d) each R1 is independently selected from the group consisting of nil, N+(R2)3, R9SR6, SR6, hydrogen, hydroxy; unsubstituted or substituted C1-C8 alkyl, -OR3, -CO2R3, -O2CR3, NR3 2, -N(R3)C(O)R3, -C(O)N(R3)2, halogen, -C(O)R3 arylalkyl, nitro, unsubstituted or substituted aryl, and combinations thereof; -64- (e) each R2 is independently selected from the group consisting of nil; a substituted or unsubstituted C1-C35 alkyl, substituted or unsubstituted phenyl, benzyl, or R9SR6; (f) each R3 is independently selected from the group consisting of hydrogen~ substituted or unsubstituted C1-C8 alkyl, and R9SR6. (g) each R6 is independently selected from the group consisting of H, -C(O)R7, C(O)OR7, C(S)OR7,C(S)R7, C(O)NR7 2; C(S)NR7 2, wherein R7 is hydrogen, or substituted or unsubstituted C1-C8 alkyl; (h) R is COOH, SO3H2, PO3H2, or P(O)(OH)R4, wherein R4 is substituted or unsubstituted C1-C8 alkyl; and (i) R9 is substituted or unsubstituted C1-C8 alkyl. 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 treating or preventing pathological conditions characterized by abnormal calcium and phosphate metabolism in humans or other mammals. 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.
Ebetino Frank H.
Francis Marion D.
Kaas Susan M.
Kirby Eades Gale Baker
Procter & Gamble Pharmaceuticals Inc.
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