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 9/576 (2006.01) C07F 9/6561 (2006.01)
Patent
CA 2136822
The present invention relates to thio-substituted cyclic phosphonate compounds including bisphosphonates, phosphonoal- kylphosphinates, 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 treating or preventing 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. These compounds may be monocyclic or bicyclic and have general structure (I) provided that at least one of R1, R2, and R3 is SR6 or R8SR6.
La présente invention se rapporte à des composés de phosphonate cycliques et thio-substitués, y compris des biphosphonates, des phosphoalkylphosphonates, des phosphonocarboxylates et des phosphonosulfonates, ainsi qu'à leurs sels et esters pharmaceutiquement acceptables. La présente invention se rapporte en outre à des compositions pharmaceutiques contenant une dose efficace et sûre d'un composé de l'invention, ainsi que des excipients pharmaceutiquement acceptables. Enfin, l'invention se rapporte à des procédés de traitement et de prévention d'états pathologiques caractérisés par un métabilisme anormal de calcium et de phosphate chez les humains ou d'autres mammifères y compris des procédés de traitement et de prévention de l'ostéoropose et de l'arthrite, en particulier la polyarthrite rhumatoïde et l'ostéoarthrite. Ce procédé consiste à administrer, à un humain ou un autre mammifère nécessitant un tel traitement, une dose sûre et efficace ou d'une composition de la présente invention. Ces composés peuvent être mono ou bicycliques, et présentent la structure générale (I) à condition qu'au moins un élément parmi R1, R2, R3 représente SR6 ou R8SR6.
Ebetino Frank H.
Francis Marion D.
Kaas Susan M.
Kirby Eades Gale Baker
Procter & Gamble Pharmaceuticals Inc.
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