Wayne State University

University of Michigan

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

Jiri Zemlicka

John Charles Drach

Roger G Ptak

Yao-Ling Qiu

Xinchao Chen

Shaoman Zhou

Samuel Broder

Hiroaki Mitsuya

Sridhar Nimmagadda

Anthony F Shields

Seiji Hayashi

Shashikant Phadtare

Compounds which are active against viruses have the following Formulas: 

2-amino-9-[(2-hydroxymethyl) cyclopropylidenemethyl] purines as antiviral agents

Compounds which are active against viruses have the following formulas: wherein B is a purine or pyrimidine heterocyclic ring or base. In a preferred embodiment, the purine include 6-aminopurine (adenine), 6-hydroxypurine (hypoxanthine), 2-amino-6-hydroxypurine (guanine), 2,6-diamino-purine, 2-amino-6-azidopurine, 2-amino-6-halo substituted purines such as 2-amino-6-chloropurine, 2-amino-6-fluoropurine, 2-amino-6-alkoxypurines such as 2-amino-6-methoxypurine, 2-amino-6-cyclopropylaminopurine, 2-amino-6-alkylamino or 2-amino-6-dialkylamino substituted purines, 2-amino-6-thiopurine, 2-amino-6-alkylthio substituted purines, 3-deazapurines, 7-deazapurines and 8-azapurines. The pyrimidine incorporates cytosine, uracil and thymine, 5-halo substituted cytosines and uracils, 5-alkyl substituted cytosines and uracils including derivatives with a saturated or unsaturated alkyl group and 6-azapyrimidines.

2,2-bis-(hydroxymethyl)cyclopropylidenemethyl-purines and -pyrimidines as antiviral agents

The present invention provides phosphoramidate derivatives of a furanosyluracil analog, FAU, that can effectively deliver FAU monophosphate, or a derivative thereof, intracellularly. FAU-Phosphoramidate diesters can bypass the first step of phosphorylation and be activated intracellularly so as to be converted to nucleoside monophosphates. This results in improved formation of nucleoside triphosphates, and higher incorporation into DNA. The compounds of the invention can be used to treat cancer.

Phosphoramidate derivatives of FAU

2,2-bis-(hydroxymethyl)cyclopropylidenemethyl-purines and pyrimidines as antiviral agents

2-amino-9-[(2-hydroxymethyl) cyclopropylidenemethyl] purine antiviral agents

Compounds which are active against viruses have the following Formulas:wherein B is a purine or pyrimidine heterocyclic ring and is preferably selected from the group consisting of 6-aminopurine (adenine), 2,6-diaminopurine, 2-amino-6-azidopurine, 2-amino-6-cyclopropylaminopurine, 6-hydroxypurine (hypoxanthine), 2-amino-6-halo substituted purines, 2-amino-6-alkoxy substituted purines, 2-amino-6-hydroxypurine (guanine), 3-deazapurines, 7-deaza-purines, 8-azapurines, cytosine, 5-halo substituted cytosines, 5-alkyl substituted cytosines, thymine, uracil and 6-azapyrimidines; X is O; and, Rand Rare alkyl or aryl groups. The compounds of the present invention also include the R- and S-enantiomers of the above compounds. The RX and/or RX can also be amino acid residues with X as NH.

2-hydroxymethylcyclopropylidene methylpurines and -pyrimidines as antiviral agents

2-hydroxymethylcyclopropylidenemethylpurines and -pyrimidines as antiviral agents

Compounds which are active against retroviruses have the following formula

Pyrimidine and purine 1,2-butadiene-4-ols as anti-retroviral agents

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Warren, MI, United States of America

Jiri Zemlicka