Southern Research Institute

Merck Sharp + Dohme Corp.

Other

The University of North Carolina at Chapel Hill

University of Rochester

The UAB Research Foundation (The University of Alabama at Birmingham)

Joseph A Maddry

Subramaniam Ananthan

John A Secrist, Iii

Robert C Reynolds

F George Njoroge

Cecil D Kwong

Hollis S Kezar, Iii

Neng-Yang Shih

John J Piwinski

Feng Geng

Abhijit Roychowdhury

Frank W Bennett

Ashok Arasappan

Jeremy Clark

Anita T Fowler

Maurizio Grimaldi

Judith Varady Hobrath

Srikanth Venkatraman

Vinay M Girijavallabhan

Francisco Velazquez

Vishal Verma

Yuhua Huang

Ashish Kumar Pathak

Joseph A Kozlowski

Peter Anthony Crooks

John A Montgomery

Ling Tong

Malcolm Maccoss

Bandarpalle B Shankar

Seong Heon Kim

Corinne E Augelli-Szafran

Eric J Sorscher

Kamal N Tiwari

Rudolph L Juliano

Bing Yang

William Perry Janzen

David S Goldfarb

Syed Kaleem Ahmed

George F Njoroge

Lynn Rasmussen

Xin Ming

Robert A Galemmo, Jr

Ellie Lucille White

Krister Wennerberg

Canhong Cao

Regina Huelgas

Andrew B West

Jacob Valiyaveettil

John A Secrist

Hollis S Kezar

Robert A Galemmo

John A Iii Secrist

Hollis S Iii Kezar

Iii Hollis S Kezar

Iii John A Secrist

Methods for enhancing memory and/or learning and prevent neurodegeneration by administration of certain heterocyclic and aromatic compounds are described. The methods are particularly useful for treating patients suffering from a neurodegenerative disease such as (without limitation) Alzheimer's, Parkinsons's, Lou Gehrig's (ALS) disease or memory or learning impairment. A neuronal human cell-based assay that assess NF-kB gene up-regulation using a luciferase reporter is also provided that screens for compounds useful in methods for enhancing memory or learning.

Treatment of neurodegenerative diseases, causation of memory enhancement, and assay for screening compounds for such

The present disclosure is concerned with benzo annulene compounds that are capable of inhibiting a viral infection and methods of treating viral infections such as, for example, chikungunya, Venezuelan equine encephalitis, dengue, influenza, and zika, using these compounds. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

Benzo annulenes as antiviral agents

Methods of administering an oligonucleotide of interest into a cell in vitro or in vivo are described. In the methods, a small organic compound active agent is concurrently administered to the cell in an amount effective to increase the delivery of the oligonucleotide into the cell, and/or increase the activity of said oligonucleotide in the cell. Compositions useful for carrying out the method are also described.

Small molecules that enhance the activity of oligonucleotides

The invention provides methods of enhancing memory and/or learning and prevent neurodegeneration, comprising administering therapeutically effective amounts of certain heterocyclic and aromatic compounds to a patient in need thereof. In one aspect, the invention provides methods of treating patients suffering from a neurodegenerative disease, such as but not limited to, Alzheimer's, Parkinsons's, Lou Gehrig's (ALS) disease, and/or memory or learning impairment. The invention further provides neuronal human cell-based assays that assess NF-kB gene upregulation using a luciferase reporter, wherein the assays identify compounds that are useful in enhancing memory or learning.

The present invention provides compounds of Formula (I): and tautomers, isomers, and esters of said compounds, and pharmaceutically acceptable salts, solvates, and prodrugs of said compounds, wherein each of R, R, X, Y, Z, R, R, R, R, R, R, R, R, R, Rand n is selected independently and as defined herein. Compositions comprising such compounds are also provided. The compounds of the invention are effective as inhibitors of HCV, and are useful, alone and together with other therapeutic agents, in treating or preventing diseases or disorders such as viral infections and virus-related disorders. 

Substituted pyridine and pyrimidine derivatives and their use in treating viral infections

Provided are novel LRRK2 kinase inhibitors and methods of treating disease states using these inhibitors. Examples of LRRK2 kinase inhibitors are compounds of the formula: or derivatives thereof. An example is 1-(piperidin-1-yl)-2-((3-(thiophen-2-yl)-[1,2,4]triazolo[4,3-b]pyridazin-6-yl)thio)butan-1-one. Particular uses include treating neurodegenerative diseases, cancer, autoimmune diseases and leprosy.

Triazolopyridazine compounds, use as inhibitors of the kinase LRRK2, and methods for preparation thereof

Compound represented by the formulae: wherein each R individually is H or aliphatic acyl or aromatic acyl group; X is selected from the group consisting of hydrogen, fluoro, chloro, bromo, iodo, alkoxy, alkyl, haloalkyl, alkenyl, haloalkenyl, alkynyl, amino, monoalkylamino, dialkylamino, cyano, aryl and nitro; pharmaceutically acceptable salts thereof, prodrugs thereof and mixtures thereof are used as inhibitors of orthopoxviruses and for treating patients suffering from an orthopoxvirus infection such as, but not limited to, smallpox, cowpox, monkeypox and camelpox.

Use of 4'-thio-2&#x2032;-deoxynucleosides as anti orthopoxvirus agents

Provided are compounds which generally have a triketone structure. Examples of the compounds include derivatives of 1,3-cyclohexanedione, such as: 1,3-cyclohexanedione, 2-propanoyl-5-cyclohexyl-; 1,3-cyclohexanedione, 2-propanoyl-5-[4-fluorophenyl]-; 1,3-cyclohexanedione, 2-acetyl-5-[thien-2-yl]-; 1,3-cyclohexanedione, 2-acetyl-5-butyl-; and 1,3-cyclohexanedione, 2-propanoyl-5-[bicyclo[2.2.1]hept-2-en-5-yl]-. The compounds can be used to alter the lifespan of eukaryotic organisms and treat inflammation.

Compounds and methods for altering lifespan of eukaryotic organisms

The present invention provides compounds of Formula (A): (Chemical formula should be inserted here as it appears on abstract in paper form) (A) and tautomers, isomers, and esters of said compounds, and pharmaceutically acceptable salts, solvates, and prodrugs of said compounds, wherein wherein each of R, R, X, Y, Z, R, R, R, R, R, R, R, R, R, R, R, R, and n is selected independently and as defined herein. Compositions comprising such compounds are also provided. The compounds of the invention are effective as inhibitors of HCV, and are useful, alone and together with other therapeutic agents, in treating or preventing diseases or disorders such as viral infections and virus-related disorders. 

Ethenyl-substituted pyridine and pyrimidine derivatives and their use in treating viral infections

The present invention provides compounds of Formula (I): and tautomers, isomers, and esters of said compounds, and pharmaceutically acceptable salts, solvates, and pro-drugs of said compounds, wherein each of R, R, X, Y, Z, R, R, R, R, R, R, R, R, R, Rand n is selected independently and as defined herein. Compositions comprising such compounds are also provided. The compounds of the invention are effective as inhibitors of HCV, and are useful, alone and together with other therapeutic agents, in treating or preventing diseases or disorders such as viral infections and virus-related disorders.

Ethynyl-substituted pyridine and pyrimidine derivatives and their use in treating viral infections

The present invention provides compounds of Formula (I): (Chemical formula should be inserted here as it appears on abstract in paper form) (I) and tautomers, isomers, and esters of said compounds, and pharmaceutically acceptable salts, solvates, and prodrugs of said compounds, wherein each of R, R, X, Y, Z, R, R, R, R, R, R, R, R, R, R, and n is selected independently and as defined herein. Compositions comprising such compounds are also provided. The compounds of the invention are effective as inhibitors of HCV, and are useful, alone and together with other therapeutic agents, in treating or preventing diseases or disorders such as viral infections and virus-related disorders. 

AZO-substituted pyridine and pyrimidine derivatives and their use in treating viral infections

Diazoimidazole compounds for activating Cl-secretion are disclosed that can be used for treating cystic fibrosis.

Activating C1- secretion

The present invention provides for the preparation and use of ribo- and deoxyribo-nucleosides and polynucleotide analogs. The polynucleotide analogs are made of polynucleosides which contain sulfonate and sulfonamide linkages.

Polynucleotide analogs containing sulfonate and sulfonamide

Growing community of inventors

Birmingham, AL, United States of America

Joseph A Maddry