C - Chemistry – Metallurgy – 07 – H
Patent
C - Chemistry, Metallurgy
07
H
C07H 19/173 (2006.01) A61K 31/506 (2006.01) A61K 31/7064 (2006.01) A61K 31/7076 (2006.01) C07D 405/04 (2006.01) C07D 409/04 (2006.01) C07D 473/00 (2006.01) C07H 19/06 (2006.01) C07H 19/073 (2006.01) C07H 19/16 (2006.01)
Patent
CA 2163520
The present invention relates to the discovery that certain dideoxynucleoside analogs which contain a dideoxy ribofuranosyl moiety having an L-configuration (as opposed to the naturally occurring D-configuration) exhibit unexpected activity against Hepatitis B virus (HBV). In particular, the compounds according to the present invention show potent inhibition of the replication of the virus in combination with very low toxicity to the host cells (i.e., animal or human tissue). Compounds according to the present invention exhibit primary utility as agents for inhibiting the growth or replication of HBV, HIV and other retroviruses, most preferably HBV. The compound 1-(2,3-dideoxy-beta-L- ribofuranosyl)-5-fluorocytosine is shown to be a potent anti-HIV agent with low toxicity to host cells. In a preferred embodiment a .beta.-L nucleoside compound according to the following structure is provided: Image
L'invention concerne la découverte que certains analogues de didésoxy nucléosides contenant une fraction didésoxy ribofuranosyle présentant une configuration L (à la différence de la configuration D naturelle) présentent une activité inattendue contre le virus de l'hépatite B. Les composés de l'invention présentent notamment une puissante inhibition de la réplication du virus en combinaison avec une très faible toxicité vis-à-vis des cellules hôtes (c'est-à-dire, des tissus animaux ou humains). Les composés de l'invention présentent une utilité principale comme agents destinés à inhiber la croissance et la réplication du virus de l'hépatite B, du VIH et d'autres rétrovirus, de préférence le virus de l'hépatite B. On a démontré que le composé 1-(2,3-didésoxy-béta-L-ribofuranosyle)-5-fluorocytosine constitue un agent puissant anti-VIH présentant une faible toxicité à l'égard de cellules hôtes.
Cheng Yung-Chi
Lin Tai-Shun
Cassan Maclean
Yale University
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