C - Chemistry – Metallurgy – 07 – H
Patent
C - Chemistry, Metallurgy
07
H
C07H 19/073 (2006.01) A61K 31/00 (2006.01) A61K 31/513 (2006.01) A61K 31/535 (2006.01) A61K 31/557 (2006.01) A61K 31/7072 (2006.01) A61K 31/7076 (2006.01) A61K 45/06 (2006.01) A61K 47/48 (2006.01) A61P 31/18 (2006.01) C07C 233/36 (2006.01) C07C 233/78 (2006.01) C07C 237/24 (2006.01) C07C 271/20 (2006.01) C07C 335/08 (2006.01) C07C 335/32 (2006.01) C07D 207/333 (2006.01) C07D 211/58 (2006.01) C07D 215/56 (2006.01) C07D 233/90 (2006.01) C07D 235/30 (2006.01) C07D 401/06 (2006.01) C07D 401/12 (2006.01) C07D 40
Patent
CA 2316999
Disclosed are multibinding compounds which inhibit the enzyme HIV reverse transcriptase, an enzyme which catalyzes the conversion of viral RNA to single stranded DNA. The multibinding compounds of this invention containing from 2 to 10 ligands covalently attached to one or more linkers. Each multibinding compound comprises at least one nucleoside reverse transcriptase inhibitor and at least one non-nucleoside reverse transcriptase inhibitor. The multibinding compounds of this invention are useful to inhibit HIV reverse transcriptase in vivo, and accordingly to inhibit HIV replication in vivo.
La présente invention concerne des composés à liaisons multiples inhibiteurs de la transcriptase inverse du VIH, enzyme catalyseur de la conversion de l'ARN viral en ADN monobrin. Les composés à liaisons multiples de l'invention contiennent de 2 à 10 ligands reliés par covalence à un ou plusieurs lieurs. Chaque composé à liaisons multiples comprend au moins un inhibiteur de transcriptase inverse des nucléosides, et au moins un inhibiteur de transcripteur inverse des non-nucléosides. Les composés à liaisons multiples de l'invention conviennent pour l'inhibition in vivo de la transcriptase inverse du VIH, et par conséquent, pour l'inhibition de la réplication in vivo du VIH.
Aggen James
Griffin John H.
Mammen Mathai
Oare David
Advanced Medicine Inc.
Theravance Inc.
Torys Llp
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