C - Chemistry – Metallurgy – 07 – H
Patent
C - Chemistry, Metallurgy
07
H
C07H 19/173 (2006.01) A61K 31/7088 (2006.01) A61K 47/48 (2006.01) A61P 15/00 (2006.01) A61P 15/18 (2006.01) A61P 31/00 (2006.01) A61P 31/18 (2006.01) C07D 411/04 (2006.01) C07F 9/6561 (2006.01) C07H 19/073 (2006.01) C07K 5/00 (2006.01) C07K 5/06 (2006.01) C07K 5/12 (2006.01)
Patent
CA 2717788
The present invention relates to fatty acid and fatty alcohol substituted nucleoside derivatives and nucleoside and nucleoside derivatives substituted on multivalent scaffolds (e.g., polymers, peptides, polycarboxylic acid substituted compounds, compounds containing polycycloSaligenyl groups) that display potent anti-HIV activity. Furthermore, they show enhanced activity against multi-drug resistant, R5, and cell-associated virus. Some of them also display activity against other sexually transmitted pathogens and sperm. The present invention provides their methods of synthesis, composition of matter, and methods of use. Emphasis is placed on their application as topical microbicides to treat or prevent sexual transmission of disease, especially HIV/ AIDS.
La présente invention concerne des dérivés nucléosidiques substitués par des acides gras et des alcools gras et des dérivés nucléosidiques substitués sur des structures multivalentes (par exemple, polymères, composés substitués par un acide polycarboxylique, composés contenant des groupes polycyclosaligényle) qui manifestent une puissante activité anti-VIH. Ils présentent, de plus, une activité renforcée contre les virus multirésistants aux médicaments, R5, et cellulaires. Certains d'entre eux manifestent également une activité contre d'autres pathogènes transmis sexuellement et le sperme. La présente invention concerne leurs procédés de synthèse, des compositions les contenant et leurs procédés d'utilisation. L'accent est placé sur leur application sous forme de microbicides topiques pour traiter ou prévenir la transmission sexuelle de maladies, notamment le VIH/SIDA.
Agrawal Hitesh Kumar
Doncel Gustavo F.
Parang Keykavous
Bennett Jones Llp
Board Of Governors For Higher Education State Of Rhode Island And Provi Dence Plantations
Eastern Virginia Medical School
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