C - Chemistry – Metallurgy – 07 – J
Patent
C - Chemistry, Metallurgy
07
J
C07J 63/00 (2006.01) A61K 31/56 (2006.01) A61P 31/14 (2006.01) A61P 31/18 (2006.01) C07J 53/00 (2006.01)
Patent
CA 2322868
Betulin and dihydrobetulin acyl derivatives according to the present invention have been found to have potent anti-HIV activity. The compounds of the present invention have formulae (I) or pharmaceutically acceptable salts thereof; wherein R1 is a C2-C20 substituted or unsubstituted carboxyacyl, R2 is a C2-C20 substituted or unsubstituted carboxyacyl; and R3 is hydrogen, halogen, amino, optionally substituted mono-- or di-alkylamino, or -OR4, where R4 is hydrogen, C1-4 alkanoyl, benzoyl, or C2-C20 substituted or unsubstituted carboxyacyl; wherein the dashed line represents an optional double bond between C20 and C29.
La présente invention concerne des dérivés acyles de bétuline et de dihydrobétuline présentant une forte activité anti-VIH. La présente invention concerne notamment des composés, ou les sels pharmaceutiquement acceptables de ceux-ci, de formule: I, dans laquelle R1 représente carboxyacyle C2-C20 substitué ou non substitué; R2 représente carboxyacyle C2-C20 substitué ou non subtitué; et R3 représente hydrogène, amino, monoalkylamino ou dialkylamino éventuellement substitué, ou -OR4, R4 représentant hydrogène, alkanoyle C1-4, benzoyle, ou carboxyacyle C2-C20 substitué ou non subtitué, la ligne pointillée représentant une éventuelle double liaison entre C20 et C29.
Cosentino Louis Mark
Lee Kuo-Hsiung
Sun I-Chen
Wang Hui-Kang
Bbi Biotech Research Laboratories Inc.
Mbm Intellectual Property Law Llp
Panacos Pharmaceuticals Inc.
The University Of North Carolina At Chapel Hill
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