Phosphorous prodrugs

C - Chemistry – Metallurgy – 07 – F

Patent

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Details

C07F 9/547 (2006.01) A61K 31/675 (2006.01) A61K 31/70 (2006.01) C07C 69/732 (2006.01) C07C 271/44 (2006.01) C07F 9/40 (2006.01) C07F 9/6561 (2006.01) C07H 19/10 (2006.01) C07H 19/20 (2006.01) C07H 19/207 (2006.01)

Patent

CA 2083386

The composition and methods of synthesis of several prodrugs are described, These methods may be used to convert negatively charged phosphorous bearing drugs into neutrally charged; lipid soluble prodrugs which are able to passively diffuse into cells and through biological membranes. Prodrugs for a variety of antiviral and anti-leukemic agents are described. A class of prodrugs which undergo degradation by an elimination reaction to form a carbon-carbon double bond is described. This elimination reaction is triggered by esterase.

La composition et des procédés de synthèse de plusieurs promédicaments sont décrits. On peut utiliser ces procédés afin de transformer des médiacments porteurs de phosphore de charge négative en promédicaments solubles dans des lipides de charge neutre, lesquels peuvent se diffuser passivement dans des cellules et à travers des membranes biologiques. L'invention concerne également des promédicaments destinés à une variété d'agents anti-viraux et anti-leucémiques. De plus, l'invention concerne une classe de promédicaments subissant une dégradation par réaction d'élimination afin de former une double liaison carbone-carbone. La réaction d'élimination est déclenchée par une estérase.

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