Monophosphates as mutual prodrugs of anti-inflammatory...

C - Chemistry – Metallurgy – 07 – F

Patent

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C07F 9/12 (2006.01) A61K 31/661 (2006.01) A61K 31/665 (2006.01) A61K 31/675 (2006.01) A61P 11/06 (2006.01) C07F 9/58 (2006.01) C07F 9/6503 (2006.01) C07F 9/6558 (2006.01)

Patent

CA 2670730

A mutual prodrug of an AISTM and a .beta.-agonist in formulation for delivery by aerosolization to inhibit pulmonary inflammation and bronchoconstriction is described. The mutual prodrug is preferably formulated in a small volume solution (10-500 µL) dissolved in a quarter normal saline having pH between about 5.0 and 7.0 for the treatment of respiratory tract inflammation and bronchoconstriction by an aerosol having mass median average diameter predominantly between about 1 to 5 µ, produced by nebulization or by dry powder inhaler.

L'invention porte sur un promédicament mutuel d'un modulateur de la transduction du signal anti-inflammatoire et d'un .beta.-agoniste, formulé pour être administré sous forme d'aérosol afin d'inhiber l'inflammation pulmonaire et la bronchoconstriction. De préférence, le promédicament mutuel est formulé en une solution à petit volume (10-500 µL) dissoute dans une solution saline à 0,225% NaCl d'un pH compris entre environ 5,0 et environ 7,0, que l'on utilise pour traiter l'inflammation pulmonaire et la bronchoconstriction, sous la forme d'un aérosol possédant un diamètre moyen massique essentiellement compris entre environ 1 et environ 5 µ, aérosol qui est produit par nébulisation ou par un inhaleur de poudre sèche.

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