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Claims for Patent: 5,142,051

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Claims for Patent: 5,142,051

Title: N-phosphonylmethoxyalkyl derivatives of pyrimidine and purine bases and a therapeutical composition therefrom with antiviral activity
Abstract:This invention relates to new nucleotide analogues and solves the technical problem of their use as biologically active compounds. The subject of this invention are N-(2-phosphonylmethoxyethyl) and N-(3-hydroxy-2-phosphonylmethoxypropyl) derivatives of pyrimidine and purine bases, easily accessible from heterocyclic bases andd their N-(2-hydroxyethyl) or N-(2,3-dihydroxypropyl) derivatives. Some of the compounds, according to this invention, exhibit a marked antiviral activity or can be converted into such active compounds by chemical transformations.
Inventor(s): Holy; Antonin (Horni Pocernice, CS), Rosenberg; Ivan (Praha, CS), De Clercq; Erik D. A. (Leuven, BE)
Assignee: Ceskoslovenska Akademie Ved (Praha, CS) Rega Institut (Leuven, BE)
Application Number:07/074,900
Patent Claims: 1. A compound of the formula ##STR3## wherein B is selected from the group consisting of uracil-1-yl,

cytosin-1-yl,

5-methylcytosin-1-yl,

thymin-1-yl,

5-fluoruracil-1-yl,

guanin-9-yl,

guanin-7-yl,

adenin-3-yl,

hypoxanthin-9-yl,

2-methyladenin-9-yl,

2-methylthioadenin-9-yl,

2-aminoadenin-9-yl,

2-aminopurin-9-yl,

N.sup.6 -dimethyladenin-9-yl,

8-bromoadenin-9-yl,

8-hydroxyadenin-9-yl,

6-hydroxylaminopurin-9-yl,

6-hydrazinopurin-9-yl,

6-thiopurin-9-yl,

purin-9-yl, and

xanthin-9-yl.

2. The compound of claim 1, wherein B is selected from the group consisting of uracil-1-yl, cytosin-1-yl, 5-methylcytosin-1-yl, thymin-1-yl, and 5-fluorouracil-1-yl.

3. The compound of claim 2, wherein B is cytosin-1-yl.
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