Compositions and methods for treating bone deficit conditions

A - Human Necessities – 61 – K

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A61K 31/54 (2006.01) A61K 31/38 (2006.01) A61K 31/395 (2006.01) A61K 31/47 (2006.01) A61K 31/549 (2006.01) A61P 19/08 (2006.01)

Patent

CA 2235481

Compounds containing two aromatic systems covalently linked through a linker containing one or more atoms, or "linker" defined as including a covalent bond per se so as to space the aromatic systems at a distance 1.5-15.ANG., are effective in treating conditions associated with bone deficits. The compounds can be administered to vertebrate subjects alone or in combination with additional agents that promote bone growth or that inhibit bone resorption. They can be screened for activity prior to administration by assessing their ability to effect the transcription of a reporter gene coupled to a promoter associated with a bone morphogenetic protein and/or their ability to stimulate calvarial growth in model animal systems.

L'invention porte sur des composés à deux systèmes aromatiques, liés par covalence par un liant à un ou plusieurs atomes ou par un liant défini comme incluant per se une liaison covalente espaçant les systèmes aromatiques d'une distance comprise entre 1,5 et 15 .ANG., et s'avérant efficaces pour le traitement des états liés à un déficit osseux. Lesdits composés s'administrent à des vertébrés, seuls ou associés à des additifs qui favorisent la croissance osseuse ou inhibent la résorption osseuse. On peut en évaluer l'activité avant administration en vérifiant leur capacité à effectuer la transcription d'un gène reporter couplé à un promoteur associé à une protéine morphogénétique osseuse et/ou leur capacité à stimuler la croissance de la voûte crânienne dans des systèmes de modèles animaux.

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