Southern Research Institute

Merck Sharp + Dohme Corp.

Biocryst, Inc.

Biocryst Pharmaceuticals, Inc.

Cornell University

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

The Penn State Research Foundation

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

H. Lee Moffitt Cancer Center and Research Institute, Inc.

Cornell Center for Technology, Enterprise and Commercialization

John A Secrist, Iii

John A Montgomery

Kamal N Tiwari

Mark D Erion

Steve E Ealick

Joseph A Maddry

Robert C Reynolds

Wayne C Guida

F George Njoroge

Subramaniam Ananthan

Hollis S Kezar, Iii

Anita T Fowler

Cecil D Kwong

Neng-Yang Shih

John J Piwinski

Feng Geng

Abhijit Roychowdhury

Frank W Bennett

Ashok Arasappan

William B Parker

Jeremy Clark

William L Hinds, Jr, Legal Representative

Steven Ealick

Srikanth Venkatraman

Vinay M Girijavallabhan

Francisco Velazquez

Eric J Sorscher

Vishal Verma

Yuhua Huang

Shri Niwas

Joseph A Kozlowski

Peter Anthony Crooks

Kenneth Alan Jacobson

Ling Tong

Bandarpalle B Shankar

Malcolm Maccoss

Seong Heon Kim

Anthony E Pegg

James R Piper

Wayne Charles Guida

Carl R Johnson

Robert F Struck

David I Scheer

Herbert M Blatter

Charles A Krauth

Heaok Kim Jeong

Zhican Qu

Carroll Temple

Donald R Kahn

Suhaib M Siddiqi

L Lee Bennett

Y Fumer Shealy

Regina Huelgas

Shridhar Bale

Diane E McCloskey

William R Waud

Xiangmin Cui

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

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

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 crystal structure of the complex of S-adenosylmethionine methyl ester with h&#x39b;doMetDC F223A, a mutant where the stacking of the aromatic rings of F7, adenine and F223 would be eliminated. The structure of this mutant with the ester shows that the ligand still maintains a syn conformation aided by pi-pi interactions to F7, hydrogen bonds to the backbone of Glu67, and electrostatic interactions. Several series of AdoMet substrate analogues with a variety of substituents at the 8 position of adenine were synthesized and analyzed for their ability to inhibit hAdoMetDC. To understand these results, virtual modeling of the enzyme inhibitor complexes and the crystal structures of human AdoMetDC with 5'-deoxy-5&#x2032;-[N-methyl-N-[2-(aminooxy)ethyl]amino-8-methyl]adenosine (MAOEMA) and 5&#x2032;-deoxy-5&#x2032;-[N-methyl-N-[4-(aminooxy)butyl]amino-8-ethyl]adenosine (MAOBEA) at the active site have been determined experimentally.

5',-substituted adenosynes preparation thereof and use as inhibitors of S-adenosylmethionine decarboxylase

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

Patients suffering from cancer are treated by being administered a compound represented by the following formula:  

Preparation of thioarabinofuranosyl compounds and use thereof

Compounds represented by the formula 1:  

4'-thio-L-xyloy furanosyl nucleosides, precursors thereof, preparation and use thereof

A host cell stably transformed or transfected by a vector including a DNA sequence encoding for mutant purine nucleoside cleavage enzymes is provided. The transformed or transfected host cell can be used in combination with a purine substrate to treat tumor cells and/or virally infected cells. A nucleotide sequence encoding mutantderived purine nucleoside phosphorylase proteins which can be used in conjunction with an appropriate substrate to produce toxins which impair abnormal cell growth is also provided. A method is detailed for the delivery of toxin by generation within target cells or by administration and delivery to the cells from without. Novel purine nucleosides are detailed that yield a cytotoxic purine upon enzymatic cleavage. A synthetic process for nucleosides is also detailed.

Mutant purine nucleoside phosphorylase proteins and cellular delivery thereof

2-Chloro-9-(2-deoxy-2-fluoro-&#x3b2;-D-arabinofuranosyl)-9H-purin-6-amine is synthesized by reacting a 2-chloro-6-substituted purine with a protected and activated 2-deoxy-2-fluoro-D-arabinofiranose; and reacting with a base such as ammonia to provide 2-chloro-9-(2-deoxy-2-fluoro-&#x3b2;-D-arabinofuranosyl)-9H-purin-6-amine. When the purine reactant is substituted in the 6 position with a halogen, a reaction step with an alkoxide is carried out prior to the reaction with ammonia.

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4'-thio-L-xylo furanosyl nucleosides, precursors thereof, preparation and use thereof

Thioarabinofuranosyl compounds and use thereof

The present invention provides a procaryotic host cell stably transformed or transfected by a vector including a DNA sequence encoding for mutant purine nucleoside phosphorylase or hydrolase. The transformed or transfected procaryotic host cell can be used in combination with a purine substrate to treat tumor cells and/or virally infected cells. The present invention provides nucleotide sequences encoding mutantderived purine nucleoside phosphorylase proteins which can be used in conjunction with an appropriate substrate to produce toxins which impair abnormal cell growth. The invention provides for delivery of the toxin by generation within target cells or by administration and delivery to the cells from without.

Growing community of inventors

Birmingham, AL, United States of America

John A Secrist, Iii