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W0 2011/000721 A1 I||||||||||||||||||||||||||||||||||||||||||||||||||||||||| - Questel

W0 2011/000721 A1 I||||||||||||||||||||||||||||||||||||||||||||||||||||||||| - Questel

W0 2011/000721 A1 I||||||||||||||||||||||||||||||||||||||||||||||||||||||||| - Questel

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and with variable quantities of compound 12. Fig. 9 shows the results of the<br />

trans-infection of CD4+ T lymphocytes by HIV-1 strain 89,6 (dual tropic) after<br />

exposure to BTHP1/DC-SIGN+ cells preincubated with the virus and with<br />

variable quantities of compound 12. Fig. 10 shows the results of the trans-<br />

infection of CD4+ T lymphocytes by HIV BaI after exposure to BTHP1/DC-<br />

SIGN+ cells preincubated with the virus and with variable quantities (10 and<br />

100 μM) of compounds 12, analogue tetravalent mannose (Man4), analogue<br />

tetravalent pseudo-dimannose (12a), boltorn third generation dendrimers<br />

mannosylated (G3Man32) and ps-diMannosylated (G3PS-di24) which is a<br />

third generation dendrimer based on 2,2'-bis(methoxyol)propanoic acid (bis-<br />

MPA). Fig. 11 shows a preferred compound of the invention 12 (SARA 133).<br />

Fig. 12 shows some 2,2'-bis(methoxyol)propanoic acid (bis-MPA) based<br />

dendrimers, while Fig. 13 shows poly(amidoamine) (PAMAM) based dendrons<br />

and dendrimers within the present invention. Fig. 14 shows the dose/response<br />

for the infection of cervical explants with HIV-1 BaL in the presence of<br />

increasing amounts of dendron 12. Data represent p24 levels 3 and 7 days<br />

after infection and are presented as the average of 5 independent experiments<br />

using cervical explants from separate donors.<br />

DETAILED DESCRIPTION OF THE INVENTION<br />

As for the first object of the invention, there are provided compounds of general<br />

formula (I):<br />

[X-Y] -Z (I)<br />

wherein X is a saccharidic or pseudosaccharidic unit, Y is a linker, Z is a<br />

scaffold and a z is the functionality of the scaffold Z , i.e. the number of X unit it<br />

can bind, which is comprised between 1 and 150.<br />

In particular, according to the present invention, X is a M'-D-M group, wherein:

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