Ortho ester lipids

A - Human Necessities – 61 – K

Patent

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Details

A61K 9/127 (2006.01) A01N 43/40 (2006.01) C07D 493/08 (2006.01)

Patent

CA 2388864

The present invention provides ortho ester lipids and their derivatives that, upon certain pH conditions, undergo hydrolysis with concomitant or subsequent headgroup cleavage. These ortho ester lipids can advantageously be formulated into liposomes. The liposome formulations are useful in nucleic acid transfection and entrapment/delivery of conventional small molecules and therapeutic agents. Moreover, the liposomes comprising compounds of the present invention are useful as drug delivery vehicles.

La présente invention concerne des lipides d'ortho-esters et leurs dérivés, composés qui, dans certaines conditions de pH, subissent une hydrolyse avec un clivage de groupe de tête subséquent ou concomitant. Ces lipides d'ortho-esters peuvent être avantageusement utilisés dans des formulations de liposomes destinées à la transfection d'acides nucléiques et au piégeage ou à l'administration de petites molécules classiques et d'agents thérapeutiques. De plus, les liposomes contenant les composés de la présente invention peuvent être utilisés comme véhicules d'administration de médicaments.

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