Description:
Current
State of the Art:
Acetylcholine neurotransmission in the peripheral and central
nervous system is responsible for autonomic function (heart beating, breathing)
and cognitive skills including working memory, muscle. Degeneration of the
nervous system and/or cognitive dysfunction/impairment are associated with a variety of
neurological diseases and disorders including but not limited to Senile
Dementia, Schizophrenia, Alzheimer’s, Parkinson’s and Huntington’s Disease.
Top competitors on the market that target acetylcholine
neurotransmission are the Alzheimer’s Disease therapeutics including Donepezil (Aricept), Galantamine (Razadyne) and Rivastigmine (Exelon).
Disadvantages
with the Current Art:
Many of the therapeutics for neurodegenerative disorders can only
treat the symptoms of the disease while failing to slow down the progression of
the disease. In some cases, many patients do not respond to current therapies.
What is needed are therapeutics that can treat the cognitive impairment
associated with neurodegenerative diseases and slow or halt the progression of
the disease.
Advantages of Invention:
A library of tertiary amine analogs of choline were developed and
screened for utility as therapeutic agents for neurological and
neurodegenerative diseases and disorders. Two compounds have been evaluated for
the treatment of cognitive dysfunction/impairment that were also found to have
neuroprotective benefits.
In rodent and simian studies these analogs improved cognition and
working memory in a dose dependent manner.
Patent
Status:
US Patent Issued 6,881,738 (2002) and 7,786,147 (Divisional; 2010); Non-Provisional
(Divisional) filed US2010/0324064
Inventor(s):
J.J. Buccafusco, A.V. Terry, J.W. Beach,
R.R. Jonnala
Case
Number:
GHSU 2000-007