Acid-sensitive compounds, preparation and uses thereof

Details Acid-sensitive compounds, preparation and uses thereof Acid-sensitive compounds, preparation and uses thereof

C - Chemistry, Metallurgy

07

D

C07D 317/34 (2006.01) A61K 47/48 (2006.01) A61P 9/10 (2006.01) C07D 319/06 (2006.01) C07J 41/00 (2006.01)

Patent

CA 2421179

The invention concerns novel acid-sensitive compounds comprising at least a hydrophilic substituent and a cyclic orthoester which is acid-sensitive, and their salts. Said compounds are useful for forming conjugates (liposomes, complexes, nanoparticles, ) with biologically active substances and for releasing them in cell tissues or compartments whereof the pH is acid, either as non-ionic surfactant to stabilise particles encapsulating a biologically active substance then destabilising them in an acid medium, or as vector covalently bound to a therapeutic molecule so as to release said therapeutic molecule in cell tissues or compartments whereof the pH is acid.

Nouveaux composés acidosensibles comprenant au moins un substituant hydrophile et un orthoester cyclique qui est acidosensible, et leurs sels. Ces composés sont utiles soit pour former des conjugués (liposomes, complexes, nanoparticules ...) avec des substances biologiquement actives et les libérer dans des tissus ou compartiments cellulaires dont le pH est acide, soit en tant qu'agent de surface non-ionique pour stabiliser des particules encapsulant une substance biologiquement active puis les déstabiliser en milieu acide, ou encore en tant que vecteur lié covalemment à une molécule thérapeutique afin de libérer ladite molécule thérapeutique dans les tissus ou compartiments cellulaires dont le pH est acide.

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