19.08.2013 Views

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

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

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

SHOW MORE
SHOW LESS

You also want an ePaper? Increase the reach of your titles

YUMPU automatically turns print PDFs into web optimized ePapers that Google loves.

According to a second object of the invention, there is provided a process for<br />

the preparation of the compounds of the invention.<br />

In particular, said method includes the step of providing an appropriate alcohol<br />

M (suitably protected, if required) and a suitable precursor of the D moiety,<br />

such as, for instance, an epoxide, which can be reacted with M to give the M-D<br />

element. This in turn is further coupled to a suitably protected M' moiety, using,<br />

for instance, a glycosylation reaction, thus yielding a new entity, which is then<br />

treated to remove the protecting groups of both the M and M' moieties and<br />

optionally reduced to provide the final M'-D-M entity. This is then added to a<br />

solution of the scaffold, which already bears the linker Y moiety, in order to<br />

obtain a compound of the invention.<br />

In the above mentioned cases, wherein in the compound of formula (I) the Z<br />

scaffold is represented by pentaerythhtol or bispentaerythritol dendrimers and<br />

Q is a 1, 2 , 3-triazole, the preparation process include the step wherein a<br />

starting pseudo-saccharidic moiety corresponding to the X moiety but bearing<br />

an azide (-N 3 ) terminal residue is coupled via a 1,3-dipolar cycloaddition with<br />

the dendrimer moiety.<br />

In a third object of the invention, there are disclosed the compounds of formula<br />

(I) as antiinfective and anti-viral medicaments against HIV virus (Human<br />

Immunodeficiency Virus), Dengue virus, Ebola virus, Hepatitis C virus, SARS<br />

and Mycobacterium tuberculosis.<br />

In another aspect of said third object, there are provided the compounds of<br />

formula (Ia) as antiinfective and anti-viral medicaments against HIV virus<br />

(Human Immunodeficiency Virus), Dengue virus, Ebola virus, Hepatitis C virus,<br />

SARS and Mycobacterium tuberculosis infections.<br />

In a further aspect of the present invention, there are the compounds of<br />

formula (Ib) as antiinfective and anti-viral medicaments against HIV virus

Hooray! Your file is uploaded and ready to be published.

Saved successfully!

Ooh no, something went wrong!