Sphingo-guanidines and their use as inhibitors of...

C - Chemistry – Metallurgy – 07 – C

Patent

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C07C 279/08 (2006.01) A61K 31/155 (2006.01) A61P 35/00 (2006.01)

Patent

CA 2748546

The presently disclosed subject matter provides compounds of the formula:(1) and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, R6, R7, and R8 are as defined herein. Also disclosed are methods for making the compounds of the formula as set forth hereinabove, their use in inhibiting sphingosine kinase, and their use in the treatment and/or prevention of diseases and/or conditions associated with undesirable ceramidase or sphingosine kinase activity, including, but not limited to, cancer, cancer metastasis, atherosclerosis, stenosis, inflammation, immunological disorders, asthma, atopic dermatitis, wound healing, and other proliferative diseases.

La présente invention concerne des composés de formule (1) et leurs sels de qualité pharmaceutique, où R1, R2, R3, R4, R5, R6, R7 et R8 sont tels que définis dans la présente invention. La présente invention concerne également des méthodes de fabrication des composés de la formule comme présenté ci-avant, leur emploi dans l'inhibition de la sphingosine kinase, et leur application au traitement prophylactique et/ou thérapeutique de pathologies et/ou d'états pathologiques associés à une activité indésirable de la céramidase ou de la sphingosine kinase, ce qui inclut sans y être limité les cancers, les métastases cancéreuses, l'athérosclérose, la sténose, l'inflammation, les troubles immunologiques, l'asthme, la dermatite atopique, la guérison des blessures et d'autres maladies prolifératives.

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