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

University of Miami

University of Southern California

University of Oregon

State of Oregon

Victor E Marquez

Kenneth Alan Jacobson

Peter A Jones

Stephen H Hughes

Sheldon B Greer

Paul L Boyer

Jonathan Cheng

Bao-Han C Vu

Maqbool A Siddiqui

Eric U Selker

Cindy B Matsen

Pamela L Russ

The invention provides for novel 2-Deoxyadenosine compounds, which can treat HIV infection at low cytotoxicity values. Substitution at the 4'-position provided compounds which demonstrated low cytotoxicity values in an ATP-based cytotoxicity assay.

C4'-substituted-2-deoxyadenosine analogs and methods of treating HIV

Zebularine has hypomethylating activity, and can be used to inhibit, reverse, and/or reduce DNA methylation in vivo and in vitro. Methods are provided for treating methylation-linked conditions through the application of 2-pyrimidinone derivatives, such as Zebularine. Compositions, including pharmaceutical compositions, comprising such derivatives are also provided. Also provided are kits for use in inhibiting DNA methylation, which kits include an amount of a 2-pyrimidinone derivative.

Inhibitor of DNA methylation

The present invention provides novel nucleoside and nucleotide derivatives that are useful agonist or antagonists of P1 and P2 receptors. For example, the present invention provides a compound of formula A-M, wherein A is modified adenine or uracil and M is a constrained cycloalkyl group. The adenine or uracil is bonded to the constrained cycloalkyl group. The compounds of the present invention are useful in the treatment or prevention of various diseases including airway diseases (through A, A, P2Yreceptors), cancer (through A, P2 receptors), cardiac arrhythmias (through A1 receptors), cardiac ischemia (through A, Areceptors), epilepsy (through A, P2X receptors), and Huntington's Disease (through Areceptors).

Methanocarba cycloalkyl nucleoside analogues

The present invention provides novel nucleoside and nucleotide derivatives that are useful agonists or antagonists of P1 or P2 receptors. For example, the present invention provides a compound of formula A-M, wherein A is modified adenine or uracil and M is a constrained cycloalkyl group. The adenine or uracil is bonded to the constrained cycloakyl group. The compounds of the present invention are useful in the treatment or prevention of various diseases including airway diseases (through A, A, P2Yreceptors), cancer (through A, P2 receptors), cardiac arrhythmias (through Areceptors), cardiac ischemia (through A, Areceptors), epilepsy (through A, P2X receptors), and Huntington's Disease (through Areceptors).

Methanocarba cycloakyl nucleoside analogues

The embodiments described herein concern 5-substituted pyrimidine derivatives of conformationally locked nucleoside analogues and to the use of these derivatives as anti-viral and anti-cancer agents. The compounds are of the formula:wherein B is uracil-1-yl or cytosin-1-yl having a 5-substituent selected from halogen, alkyl, alkenyl, and alkynyl, with the proviso that where B is uracil-1-yl, the 5-substituent is not methyl. The compounds are useful in the treatment of Herpes simplex virus (HSV).

5-Substituted pyrimidine derivatives of conformationally locked nucleoside analogues

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Montgomery Village, MD, United States of America

Victor E Marquez