Chemical compounds

Details Chemical compounds Chemical compounds

2006-03-28

2006-03-28

Berch, Mark L. (Department: 1624)

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Phosphorus containing other than solely as part of an...

C514S086000, C544S243000, C544S244000, C544S118000, C544S105000

Reexamination Certificate

active

07018989

ABSTRACT:
Aryl substituted phosphoryl derivatives of the formulaIn which Ar is phenyl, naphthyl, or pyridyl, Y is O or S, X1is O, NR3, S, CR3R4, CR3W1or CW1W2, X2and X6are a bond or X6is CH2and X2is O, NR3, S, CR3R4, CR3W1or CW1W2, R3and R4are H, alkyl or phenyl, groups, W1and W2are heteroatoms, X3is alkylene, X4is oxygen or CH2, X5is a bond or CH2, Z is O, NR5, S, alkyl or phenyl, R5is H, alkyl or phenyl, J is H, alkyl, phenyl, or a heterocyclic or polycyclic group, Q is O, NR6, S, CR6R7, CR6W3or CW3W4, R6and R7are H, alkyl or phenyl, and W3and W4are hetero atoms, T1and T2are H or CH2R8, R8is H, OH or F, or T1and T2together are —CH═CH— or —C(R9)(R10)C(R11)(R12)—, R9is H, halogeno, CN, NH2, CO-alkyl, or alkyl, R10, R11, and R12are H, N3, halogen, CN, NH2, CO-alkyl, or alkyl, and B is a purine or pyrimidine base, have antiviral activity, as for example against HIV. Particularly preferred are thymine and adenine derivatives of amino acid phenoxyphosphoroamidates. A typical embodiment is 2′,3′-dideoxy-2′,3′-didehydrothymidine 5′-(phenyl methoxy alaninyl) phosphoroamidate which can be prepared from phenyl methoxy alaninyl phosphorochloridate and 2′,3′-dideoxy-2′,3′-didehydrothymidine.

REFERENCES:
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