Methods for treating neurological conditions (WO2011159945)

Wassilios G Meissner
Expert Opinion on Therapeutic Patents. 2012-06-15; 22(7): 847-852
DOI: 10.1517/13543776.2012.699524

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1. Expert Opin Ther Pat. 2012 Jul;22(7):847-52. doi: 10.1517/13543776.2012.699524.
Epub 2012 Jun 15.

Methods for treating neurological conditions (WO2011159945).

Meissner WG(1).

Author information:
(1)Centre de référence atrophie multisystématisée, France.

This patent application claims that inhibition of p21-activated kinases (PAK)
reverses, partially reverses or delays clinical signs in neurological conditions
(main claim for Huntington’s disease (HD), substance abuse and addiction,
Parkinson’s disease, depression, bipolar disorder, anxiety disorder,
posttraumatic stress disorder and neurofibromatosis). Several compounds with a
pyrido-[2,3-d]pyrimidine-7(8H)-one core and high affinity to the catalytic domain
of PAK1-4 are described in the patent. These PAK inhibitors are hypothesized to
exert beneficial effects on clinical symptoms via modulation of dendritic spine
morphology and/or synaptic function. Preliminary preclinical data suggest that
PAK inhibition may be an interesting approach for the treatment of HD,
neurofibromatosis and fragile X syndrome, while data for other neurological
conditions are missing. Current limitations call for a comprehensive
characterization of the role of PAK dysfunction in neurological disorders before
further testing the effect of PAK inhibitors in relevant preclinical models. If
ever, it will probably take many years before the most promising compounds will
head to the clinic for further assessment in patients with neurological

DOI: 10.1517/13543776.2012.699524
PMID: 22697132 [Indexed for MEDLINE]

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