National Institutes of Health, a Component of the US Dept. of Health & Human Services

P2d, Inc.

The United States of America As Represented by the Department of Health

Axonyx, Inc.

Pharmagroup International

National Institute of Health

Giordano, Tony

Brossi, Arnold

Soncrant, Timothy T.

Qian-Sheng Yu

Nigel H Greig

Arnold Brossi

Harold W Holloway

Edward J Goetzl

Weiming Luo

David Tweedie

William Douglas Figg

Xiaoxiang Zhu

Tony Giordano

Timothy T Soncrant

Marvin Hausman

Stanley I Rapoport

John R Atack

Nigel H Grieg

Danilo C Massari

William D Figg

A compound, or a pharmaceutically acceptable salt or ester thereof, having a structure of: wherein A, B and D are each oxygen or sulfur, provided that least one of A, B and D is sulfur; and R-Rare each independently hydrogen, hydroxyl, acyl, substituted acyl, acyloxy, substituted acyloxy, alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, alkoxy, substituted alkoxy, aryl, substituted aryl, amino, substituted amino, halogen, heterocycloalkyl, substituted heterocycloalkyl, heteroaryl, substituted heteroaryl, or a thio-containing group.

Thio compounds

Thalidomide analogs that modulate tumor necrosis factor alpha (TNF&#x3b1;) activity and angiogenesis are disclosed. In particularly disclosed embodiments, the thalidomide analogs are isosteric sulfur-containing analogs. Also disclosed are methods of treating a subject with the analogs.

Thalidomide analogs

Thalidomide analogs that modulate tumor necrosis factor alpha (TNF-&#x3b1;) activity and angiogenesis are disclosed. In particularly disclosed embodiments, the thalidomide analogs are isosteric sulfur-containing analogs. Also disclosed are methods of treating a subject with the analogs.

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 N -benzylnorcymserine, N -phenethylnorcymserine, N , N -bisnorcymserine, N -N -bisbenzylnorphysostigmine, N , N -bisbenzylnorphenserine, N , N -bisbenzylnorcymserine, or pharmaceutical acceptable salts thereof.

Highly selective butyrylcholinesterase inhibitors for the treatment and diagnosis of Alzheimer's disease and dementias

A method for preventing or 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.

Highly selective butyrylcholinesterase inhibitors for the treatment and diagnosis of alzheimer's disease and dementias

The synthesis of optically active 5-oxygenated (3S)-1,3-dimethyloxindole-3-acetic acids ##STR1## and their use in the synthesis of optically active (3aS-cis)-eseroline and (3aS-cis)-N.sup.1 -benzylnoreseroline, which are important intermediates in the synthesis of compounds related to (3aS-cis)-physostigmine and carbamate analogs, and of (3aS-cis)-N.sup.1 -benzylnor- and N.sup.1 -norphysostigmine and their carbamate analogs.

Optically active 5-oxygenated (3S)-1,3-dimethyloxindole-3-acetic acids

Highly potent analogs of (-)-physostigmine are provided which are potent inhibitors of acetylcholinesterase and butyrylcholinesterase. These compounds are useful in treatment of glaucoma, Alzheimer's disease, myasthenia gravis, and organophosphate poisoning.

Carbamates related to (-)-physostigmine as cholinergic agents

Growing community of inventors

Lutherville, MD, United States of America

Qian-Sheng Yu