C - Chemistry – Metallurgy – 07 – H
Patent
C - Chemistry, Metallurgy
07
H
C07H 19/10 (2006.01) A61K 9/00 (2006.01) A61K 31/70 (2006.01) C07H 19/06 (2006.01)
Patent
CA 2325460
Contraceptive activity as well as anti-viral protection can be provided by contraceptive compositions containing a pyrimidine-based nucleoside or nucleotide exhibiting spermicidal or sperm-immobilizing activity. In one example, the active ingredient contains a thymine ring (e.g. AZT) that has 5- halo, 6-alkoxy substitution. Additional improvements in anti-HIV activity for certain AZT derivatives are seen by providing the pentose ring of AZT with aryl phosphate substitution.
La présente invention concerne la possibilité d'instaurer une activité contraceptive ainsi que de conférer une protection antivirale en utilisant des compositions contraceptives contenant un nucléoside à base de pyrimidine ou un nucléotide faisant preuve d'une activité spermicide ou d'immobilisation du sperme. Dans l'un des exemples, le principe actif contient un cycle thymine, c'est le cas notamment de l'AZT, présentant une substitution 5-halo, 6-alcoxy. L'invention concerne également d'autres améliorations de l'activité anti-VIH de certains dérivés de l'AZT, améliorations que l'on obtient grâce à une substitution aryl-phosphate sur le cycle pentose de l'AZT.
D'cruz Osmond
Uckun Fatih M.
Venkatachalam Taracad
Goudreau Gage Dubuc
Parker Hughes Institute
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