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

The United States of America, as Represented by the Secretary, Department of Health and Human Services

The United States of America as Represented by the Secretary of

P2d, Inc.

Raptor Pharmaceutical Corp

Other

USA as Represented by Secretary of the Navy

The University of North Carolina at Chapel Hill

World Health Organization

Axonyx, Inc.

Pharmagroup International

Advance Biofactures Corporation

Torreypines Therapeutics, Inc.

Giordano, Tony

Brossi, Arnold

Arnold Brossi

Nigel H Greig

Harold W Holloway

Qian-Sheng Yu

Timothy T Soncrant

Donald K Ingram

Gordon Powers

Anthony J Giordano

Michael Alan Sturgess

Diane M Davidson

Tada Utsuki

Qiang-Sheng Yu

Karen T Y Shaw

William Douglas Figg

Xiaoxiang Zhu

Stanley I Rapoport

Tony Giordano

Arthur E Jacobson

Xiao-Shu He

Marvin Hausman

Helmut Schmidhammer

Malgarzota Brzostowska

Xiao-shu He

Xue F Pei

William D Figg

Kuo-Hsiung Lee

Tian-Shung Wu

Kenneth F Bastow

Fu-Lian Hsu

Peter Kerekes

John R Atack

S Rapoport

Setsu Iijima

Edward L Spangler

Danilo C Massari

Peter Buchs

Bernhard Schonenberger

Timothy T Sencrant

Linyi Wei

Anthony Giordano

Karen Ty Shaw

Malgorzata Brzostowska

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

The present invention provides compounds and methods of administering compounds to a subject that can reduce &#x3b2;APP production and that is not toxic in a wide range of dosages. The present invention also provides non-carbamate compounds and methods of administering such compounds to a subject that can reduce &#x3b2;APP production and that is not toxic in a wide range of dosages. It has been discovered that either the racemic or enantiomerically pure non-carbamate compounds can be used to decrease &#x3b2;APP production.

Agents useful for reducing amyloid precursor protein and treating dementia and methods of use thereof

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.

Compounds of Formula I are described: preferably subject to the proviso that either (a) Rand Rtogether form &#x2014;O&#x2014;CH(R)&#x2014;O&#x2014;, or (b) Rand Rtogether form &#x2014;O&#x2014;CH(R)&#x2014;O&#x2014;, wherein Ris H, halo, or loweralkyl. Pharmaceutical salts, formulations, and methods of using the same in the treatment of cancer are also described. 

Tylophorine analogs as antitumor agents

The present invention provides compounds and methods of administering compounds to a subject that can reduce &#x3b2;APP production and that is not toxic in a wide range of dosages. The present invention also provides non-carbamate compounds and methods of administering such compounds to a subject that can reduce &#x3b2;APP production and that is not tocix in a wide range of dosages. It has been discovered that either the racemic or enantiomerically pure non-carbamate compounds can be used to decrease &#x3b2;APP production.

Agents useful for reducing amyloid precursor protein and treating demantia and methods of use thereof

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 present invention relates to eseroline, N.sup.1 -noreseroline, and N.sup.1 -benzylnoreseroline phenyl carbamate analogues which provide highly potent and selective cholinergic agonist and blocking activity and their use as pharmaceutical agents. The invention further relates to improvements in therapeutic methods related to diseases such as glaucoma, myasthenia gravis, alzheimer's disease and to improvements in therapy related to organophosphate poisoning. The invention further provides for selective acetyl-cholinesterase and butyrylcholinesterase agents and a method for inhibiting these esterases.

Phenylcarbamates of (-)-eseroline, (-)-N1-noreseroline and

One aspect of the present invention provides for the separation of a racemic mixture or a mixture enriched with one or other enantiomer, said mixture comprising the enantiomers of the compound of the formula: ##STR1## wherein R is CN or CONHR' where R' is a C.sub.1 -C.sub.6 alkyl, hydrogen, or benzyl, and R.sub.1 is C.sub.1 -C.sub.6 alkyl or benzyl. Another aspect of the present invention provides a method of preparing a compound of the formula: ##STR2## wherein R is H, C.sub.1 -C.sub.6 alkyl or benzyl, and wherein R.sub.2, R.sub.3, and R.sub.4 are C.sub.1 -C.sub.6 alkyl or benzyl.

Resolution and reduction of physostigmine intermediates and derivatives

An improved method of cholinomimetic therapy for cognitive impairments associated with aging and Alzheimer's disease comprising treating a patient with an effective amount of phenserine or a pharmaceutically acceptable salt and derivatives.

Method for treating cognitive disorders with phenserine

Substituted carbamates of tricyclic compounds which have a cyclic sulfer atom, provide highly potent and selective cholinergic agonist and blocking activity are useful as pharmaceutical agents. Cholinergic disease are treated with these compounds such as glaucoma, Myasthenia Gravis, Alzheimer's disease. Methods for inhibiting esterases, acetylcholinesterase and butyrylcholinesterase are also provided.

Carbamate analogs of thiaphysovenine and method for inhibiting

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

Growing community of inventors

Bethesda, MD, United States of America

Arnold Brossi