Compounds, compositions, and methods for stimulating...

C - Chemistry – Metallurgy – 07 – D

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C07D 471/08 (2006.01) A61K 31/4995 (2006.01) A61K 31/551 (2006.01) C07D 221/00 (2006.01) C07D 223/00 (2006.01) C07D 241/00 (2006.01) C07D 243/00 (2006.01) C07D 263/00 (2006.01) C07D 471/18 (2006.01) C07D 498/18 (2006.01)

Patent

CA 2337377

Compounds that inhibit the peptidyl-prolyl isomerase (rotamase) enzyme activity of the FK-506 binding protein (FKBP) and compositions comprising these compounds are described. The FKBP-inhibiting compounds have a bicyclic [3.3.1], [4.3.1] or polycyclic azaamide nucleus. Pharmaceutical compositions containing such compounds help stimulate the outgrowth of neurites in nerve cells and augmenting nerve regeneration. Methods of treating nerve cells with such compositions are useful to promote repair of neuronal damage caused by disease and physical trauma.

L'invention a trait à des composés qui inhibent l'activité enzymatique de la peptidyl-prolyl isomérase (rotamase) de la protéine de liaison à FK-506 (FKBP), et à des compositions renfermant ces composés. Les composés inhibant FKBP possèdent un noyau azaamide bicyclique [3.3.1], [4.3.1] ou polycyclique. Des compositions pharmaceutiques contenant ces composés contribuent à stimuler l'extension de neurites dans des cellules nerveuses, et à augmenter la régénération des nerfs. Des procédés de traitement de cellules nerveuses à l'aide de ces compositions sont utiles pour activer la réparation de lésions neuronales provoquées par une maladie ou par un traumatisme physique.

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