Abstract: A method of, or the use of compounds of the invention for, treating the cognitive impairments associated with Down syndrome, the method or use comprising treating or administering to a person with an effective amount of phenserine and isomers thereof or a pharmaceutically acceptable salt and derivatives thereof.
Abstract: Phenserine compounds and pharmaceutically acceptable salts thereof are found to be useful in the management or treatment of diabetes and/or complications, such as vascular dementia, and insulin resistance, associated with diabetes. The phenserine compounds of the invention are carbamates that inhibit the activity of acetylcholinesterase.
Abstract: Described is the efficient synthesis of an easy to manipulate and utilize, soluble tartrate salt of a potent, reversible butyrylcholinesterase inhibitor, (?)-(3aS)-3a-methyl-1,2,3,3a,8,8a-hexahydropyrrolo-[2,3-b]indol-5-yl N—4?-isopropylphenylcarbamate (“MHI tartrate”), for use in altering the enzymatic activity of butyrylcholinesterase and/or acetylcholinesterase in a subject exhibiting or predicted to exhibit cognitive disorders associated with diabetes. Subjects may be suffering from or predicted to suffer from abnormal acetylcholinesterase and/or butyrylcholinesterase activity levels or from an inability to metabolize or catabolize blood sugar normally. The method comprises administering to the subject an effective amount of MHI tartrate dispensable in discrete pharmaceutically useful dosages. MHI tartrate effectively inhibits both acetylcholinesterase and butyrylcholinesterases and additionally is highly selective for butyrylcholinesterase over acetylcholinesterase.
Abstract: The present invention provides peptide analogs and peptide mimetics that inhibit pleated sheet formation in amyloid ?-peptide, pharmaceutical compositions thereof and their therapeutic use. The inhibitory peptides possess activity as inhibitors in the formation of amyloid-like deposits and are useful in the treatment of Alzheimer's Disease.
Abstract: An improved transdermal delivery composition is provided containing a low molecular weight fatty acid, and a long chain fatty acid or a long chain fatty acid lower alkyl ester, wherein the long chain is between about 1 to about 21 carbons long and preferably, contains at least one cis-olefinic bond. Preferred long chain components are oleic acid and ethyl oleate while the preferred low molecular weight fatty acid is propionic acid. The product may be used for treating a cognitive disorder by administering phenserine through a subject's skin.
Abstract: The present invention provides peptide analogs and peptide mimetics that inhibit pleated sheet formation in amyloid &bgr;-peptide, pharmaceutical compositions thereof and their therapeutic use. The inhibitory peptides possess activity as inhibitors in the formation of amyloid-like deposits and are useful in the treatment of Alzheimer's Disease.
Abstract: A method for treating cognitive impairments associated with aging or Alzheimer's disease which comprises treating a patient at risk for having the cognitive impairment with an effective amount of a highly selective butyrylcholinesterase inhibitor which is N8-benzylnorcymserine, N1-phenethylnorcymserine, N1, N8-bisnorcymserine, N1-N8-bisbenzylnorphysostigmine, N1, N8-bisbenzylnorphenserine, N1, N8-bisbenzylnorcymserine, or pharmaceutical acceptable salts thereof.
Type:
Grant
Filed:
February 7, 2002
Date of Patent:
January 27, 2004
Assignee:
Axonyx, Inc.
Inventors:
Nigel H. Greig, Qian-Sheng Yu, Arnold Brossi, Timothy T. Soncrant, Marvin Hausman
Abstract: A process for preparing phenserine compounds which are known acetylcholinesterase inhibitors from physostigmine compounds by hydrolysis to form an eseroline compound which is then condensed with an isocyanate.