Thio-substituted nitrogen-containing heterocyclic...

C - Chemistry – Metallurgy – 07 – F

Patent

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C07F 9/547 (2006.01) A61K 31/675 (2006.01) C07F 9/38 (2006.01) C07F 9/553 (2006.01) C07F 9/572 (2006.01) C07F 9/576 (2006.01) C07F 9/58 (2006.01) C07F 9/59 (2006.01) C07F 9/6506 (2006.01) C07F 9/6512 (2006.01) C07F 9/6561 (2006.01)

Patent

CA 2136820

The present invention relates to thio-substituted, nitrogen-containing heterocyclic phosphonate 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 treating or preventing pathological conditions characterized by abnormal calcium and phosphate metabolism in humans and 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 have general structure (I) in which at least one of R1, R~, R3 or R5 must be SR6 orR8SR6..

a présente invention porte sur des composés hétérocycliques axotés du phosphonate à substitut thio, notamment des bisphosphonates, des phosphonoalkylphosphonates, des phosphonocarboxylates et des phosphonosulfonates ainsi que les sels et esters de ces composés pharmaceutiquement acceptables. La présente invention porte en outre sur des compositions pharmaceutiques contenant une quantité sûre et efficace d'un composé de la présente invention et des excipients pharmaceutiquement acceptables. Elle porte, enfin, sur des méthodes de traitement ou de prévention des états pathologiques caractérisés par un métabolisme anormal du calcium et des phosphates chez les êtres humains et d'autres mammifères, notamment le traitement ou la prévention de l'ostéoporose et de l'arthrite, en particulier l'arthrite rhumatoïde et l'arthrose. Cette méthode consiste notamment à administrer à des êtres humains ou à d'autres mammifères ayant besoin d'un tel traitement une quantité sûre et efficace d'un composé ou d'une composition de la présente invention. Ces composés ont une structure générale (I) dans laquelle au moins le R1 ou le R

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