Bone acting agents

C - Chemistry – Metallurgy – 07 – J

Patent

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C07J 41/00 (2006.01) A61K 31/66 (2006.01) C07F 9/40 (2006.01) C07J 43/00 (2006.01) C07J 51/00 (2006.01) C07J 71/00 (2006.01) C07J 73/00 (2006.01)

Patent

CA 2059421

36/RJN18 18258 TITLE OF THE INVENTION NOVEL BONE ACTING AGENTS ABSTRACT OF THE INVENTION Described are new agents for treating bone disorders associated with a reduction in bone mass and abnormalities in bone resorption or bone formation including osteoporosis, Paget's disease, bone metastases and malignant hypercalcemia. The agents are hydroxyl containing steroidal hormones, having bone resorption antagonist or bone formation stimulatory activity, covalently linked through the hydroxyl group via a bond hydrolyzable in the human body, e.g. carbamate or carbonate, which is further covalently linked to an amino, or hydroxy substituted 36/RJN18 -i- 18258 alkylidene-1,1-bisphosphonate, through the respective amino or hydroxy group. The alkyl bisphosphonate moiety confers bone affinity. The agent acts by delivering the steroidal hormone directly to the bone target site where it is released for bone resorption antagonist or bone formation stimulatory action by hydrolysis of the hydrolyzable covalent bond.

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