On May 22, 2003, Walker, Daniel P.; Jacobsen, Jon E.; Acker, Brad A.; Groppi, Vincent E.; Piotrowski, David W. published a patent.Application of 280752-78-5 The title of the patent was Preparation of N-(azabicyclyl)arylamides for therapeutic use as nicotinic acetylcholine receptor agonists. And the patent contained the following:
N-(azabicyclyl)arylamides, such as RNR1C(:X)W [R = azabicyclyl; R1 = H, alkyl, cycloalkyl, haloalkyl, aryl; W = heteroaryl; X = O, S], were prepared for therapeutic use as nicotinic acetylcholine receptor agonists. These amides are useful for the treatment of central nervous system disorders, such as cognitive and attention deficit symptoms of Alzheimer’s, neurodegeneration associated with diseases such as Alzheimer’s disease, pre-senile dementia (mild cognitive impairment), senile dementia, schizophrenia, psychosis, attention deficit disorder, attention deficit hyperactivity disorder, mood and affective disorders, amyotrophic lateral sclerosis, borderline personality disorder, traumatic brain injury, behavioral and cognitive problems associated with brain tumors, AIDS dementia complex, dementia associated with Down’s syndrome, dementia associated with Lewy Bodies, Huntington’s disease, depression, general anxiety disorder, age-related macular degeneration, Parkinson’s disease, tardive dyskinesia, Pick’s disease, post traumatic stress disorder, dysregulation of food intake including bulimia and anorexia nervosa, withdrawal symptoms associated with smoking cessation and dependent drug cessation, Gilles de la Tourette’s Syndrome, glaucoma, neurodegeneration associated with glaucoma, or symptoms associated with pain. Thus, amide I was prepared in 71% yield by an amidation reaction of 1,4-benzodioxane-6-carboxylic acid with 3-(R)-aminoquinuclidine dihydrochloride using DIEA and HATU in MeCN at -10°. The prepared amides were assayed for human α7-5HT3 receptor binding activity. The experimental process involved the reaction of (6-Bromo-2,3-dihydrobenzo[b][1,4]dioxin-2-yl)methanol(cas: 280752-78-5).Application of 280752-78-5
The Article related to azabicyclic heteroaryl amide preparation nicotinic acetylcholine receptor agonist, Alkaloids: Alkaloids Containing One Nitrogen Atom At A Bridgehead and other aspects.Application of 280752-78-5
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