Protein kinase inhibitors for treatment of neurological...

Details Protein kinase inhibitors for treatment of neurological... Protein kinase inhibitors for treatment of neurological...

C - Chemistry, Metallurgy

07

D

C07D 498/22 (2006.01) A61K 31/40 (2006.01) A61K 31/407 (2006.01) A61K 31/5377 (2006.01) A61K 31/55 (2006.01) A61K 31/553 (2006.01) C07D 487/14 (2006.01) C07D 519/00 (2006.01)

Patent

CA 2203767

The invention features novel derivatives of K-252a e.g. (II-4) as well as novel bis-N-substituted derivatives of staurosporine of Formula (I). The invention also features a method for treating diseased neuronal cells involving the administration of either the novel staurosporine derivatives or specified functional derivatives of K-252a. In the formula (I): [Stau] -N(CH3)- W-N(CH3)-[Stau], [Stau] represents a residue of formula (a) and W represents a radical of the formula: -C(=Y)-NH-W'-NH-C(=Y)- where W' is a hydrocarbylene radical of 2-20 carbon atoms and Y is O or S. In formula (II-4) R1, R2, Z1, and Z2 are each H; X is CH2OH; and R is OCH3.

La présente invention concerne de nouveaux dérivés de K-252a, par exemple (II-4), ainsi que de nouveaux dérivés à substitution bis-N de staurosporine de formule (I). Elle concerne également un procédé pour traiter les cellules neuronales malades, consistant à administrer soit les nouveaux dérivés de staurosporine, soit les dérivés fonctionnels décrits de K-252a. Dans la formule (I): [Stau]-N(CH¿3?)-W-N(CH¿3?)-[Stau], [Stau] représente un résidu de la formule (a) et W représente un radical de la formule -C(=Y)-NH-W'-NH-C(=Y)- où W' est un radical hydrocarbylène de 2-20 atomes de carbone et Y est O ou S. Dans la formule (II-4), R?1¿, R?2¿, Z?1¿, et Z?2¿ sont chacun H; X est CH¿2?OH; et R est OCH¿3?.

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