TY - PAT
T1 - PROTEIN KINASE TARGETED THERAPEUTICS
AU - Watterson, Daniel
N1 - filingdate: 2009-9-24
issueddate: 2011-4-5
Status: published
attorneydocketnumber: 2006-087-01
PY - 2010/1/21
Y1 - 2010/1/21
N2 - MAP Kinase Targeted Therapeutics
NU 2006-087
Inventors
Linda J. Van Eldik
Daniel Martin Watterson*
Abstract
Northwestern researchers have identified and validated a novel compound with significant potential in the treatment of neurological diseases. In addition to the specific compound, this invention includes medicinal chemistry refinement which improves the bioavailability of small molecular inhibitors of protein kinases or protein kinase-medicated cellular stress response pathways. The investigators identified a small molecule p38? MAPK inhibitor which presents great therapy potential for CNS disorders in which proinflammatory cytokine overproduction is a component, such as Alzheimers (AD) and related indications, Parkinson's, multiple sclerosis, and traumatic brain injury. The CNS kinase inhibitor features a number of significant characteristics, making it an ideal candidate for CNS therapy. These include improved molecular properties having good oral bioavailability, blood-brain barrier penetrance, metabolic stability, and non-toxicity in in vivo rodent models. Furthermore, the inhibitor exhibited significant in vitro inhibition selectivity for only the p38? MAPK isoform.
Applications
Therapeutics: Small Molecule for CNS
Advantages
High oral bioavailability
Improved blood-brain barrier penetrance
Increased metabolic stability
Non-toxicity in rodent models
Highly selective inhibition
Publications
Munoz L, Ranaivo HR, Roy SM, Hu W, Craft JM, McNamara LK, Chico LW, Van Eldik LJ and Watterson DM (2007) A novel p38? MAPK inhibitor suppresses brain proinflammatory cytokine up-regulation and attenuates synaptic dysfunction and behavioral deficits in an Alzheimer's disease mouse model. Journal of Neuroinflammation. 4: 21.
IP Status
Issued US Patent No. 7,919,485
Marketing Contact
Allan Nader, PhD
Invention Manager
(e) [email protected]
(p) 847-497-4456
AB - MAP Kinase Targeted Therapeutics
NU 2006-087
Inventors
Linda J. Van Eldik
Daniel Martin Watterson*
Abstract
Northwestern researchers have identified and validated a novel compound with significant potential in the treatment of neurological diseases. In addition to the specific compound, this invention includes medicinal chemistry refinement which improves the bioavailability of small molecular inhibitors of protein kinases or protein kinase-medicated cellular stress response pathways. The investigators identified a small molecule p38? MAPK inhibitor which presents great therapy potential for CNS disorders in which proinflammatory cytokine overproduction is a component, such as Alzheimers (AD) and related indications, Parkinson's, multiple sclerosis, and traumatic brain injury. The CNS kinase inhibitor features a number of significant characteristics, making it an ideal candidate for CNS therapy. These include improved molecular properties having good oral bioavailability, blood-brain barrier penetrance, metabolic stability, and non-toxicity in in vivo rodent models. Furthermore, the inhibitor exhibited significant in vitro inhibition selectivity for only the p38? MAPK isoform.
Applications
Therapeutics: Small Molecule for CNS
Advantages
High oral bioavailability
Improved blood-brain barrier penetrance
Increased metabolic stability
Non-toxicity in rodent models
Highly selective inhibition
Publications
Munoz L, Ranaivo HR, Roy SM, Hu W, Craft JM, McNamara LK, Chico LW, Van Eldik LJ and Watterson DM (2007) A novel p38? MAPK inhibitor suppresses brain proinflammatory cytokine up-regulation and attenuates synaptic dysfunction and behavioral deficits in an Alzheimer's disease mouse model. Journal of Neuroinflammation. 4: 21.
IP Status
Issued US Patent No. 7,919,485
Marketing Contact
Allan Nader, PhD
Invention Manager
(e) [email protected]
(p) 847-497-4456
M3 - Patent
M1 - 7919485
ER -