The 9, 11-cycloendoperoxide pro-drugs of prostaglandin...

C - Chemistry – Metallurgy – 07 – D

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C07D 317/06 (2006.01) A61K 31/357 (2006.01) A61P 27/00 (2006.01)

Patent

CA 2494146

9,11-Cycloendoperoxide derivatives of biologically active prostaglandin analogs, and particularly of the ocular hypotensive drugs Bimatoprost, Latanaprost, Unoprostone, Travoprost and prostaglandin H2 1-ethanolamide or of structurally closely related analogs, are pro-drugs which hydrolyze under physiological conditions to provide prostaglandin analogues that are capable of providing sustained ocular and other in vivo concentrations of the respective drugs. The compounds of the invention have the formula shown below where the variables have the meaning defined in the specification.

L'invention porte sur des dérivés 9,11-cycloendoperoxyde des analogues de prostaglandines biologiquement actives, et notamment sur des médicaments contre l'hypotension oculaire tels que Bimatoprost, Latanaprost, Unoprostone, Travoprost et la prostaglandine H¿2? 1-éthanolamide ou sur des analogues de structure étroitement similaire. Ces dérivés comprennent des promédicaments qui s'hydrolysent dans des conditions physiologiques afin de produire des analogues de protaglandines capables de former des concentrations oculaires à libération prolongée et autres concentrations in vivo de médicaments. Les composés de l'invention ont la formule indiquée ci-après dans laquelle les variables sont définies dans le descriptif.

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