Stabilized formulation of selective ligands of retinoic acid...

A - Human Necessities – 61 – K

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A61K 31/44 (2006.01) A61K 9/06 (2006.01) A61K 9/08 (2006.01) A61K 9/10 (2006.01) A61K 47/06 (2006.01) A61K 47/10 (2006.01) A61K 47/14 (2006.01) A61K 47/24 (2006.01) A61K 47/32 (2006.01) A61K 47/44 (2006.01)

Patent

CA 2434030

The present invention relates to a method of administering a compound of Formula I wherein R1 is hydrogen or C1-6-alkyl; R2 is C1-6-alkyl or adamantyl; R3 is C1-6-alkyl or hydroxy; or R2 and R3 taken together are -(CR6R7)n-; R4 is C2-8-alkyl, C2-8-alkenyl, C2-8-alkynyl, -OCH2R5 or C2-8-alkanoyl, or hydrogen when R3 is hydroxy; R5 is C1-6-alkyl, C2-6-alkenyl or C2-6-alkynyl; R6 and R7 are hydrogen or C1-6-alkyl; Y is oxygen or sulfur; and n is 3, 4, or 5, or a pharmaceutically acceptable salts of carboxylic acid of formula (I), wherein said method comprises the step of admixing said compound in solid form with a topical carrier to form a topical formulation within seven days prior to first topical administration of said compound.

L'invention porte sur un procédé d'administration d'un composé de formule (I), dans laquelle R?1 ¿désigne un hydrogène ou alkyle C¿1-6?; R?2¿ désigne un alkyle C¿1-6 ?ou adamantyle ; R?3¿ désigne un alkyle C¿1-6? ou hydroxy ; ou R?2¿ et R?3¿, pris ensemble, désignent (CR?6¿R?7¿)¿n?-; R?4¿ désigne un alkyle C¿2-8?, alcényle C¿2-8?, alcynyle C¿2-8?, -OCH¿2?R¿5? ou alcanoyle C¿2-8?-, ou hydrogène lorsque R?3¿ désigne un hydroxy; R?5¿ désigne un alkyle C¿1-6?, alcényle C¿2-6 ?ou alcynyle C¿2-6?; R?6¿ et R?7¿ désignent un hydrogène ou alkyle C¿1-6?; Y désigne un oxygène ou soufre; et n désigne 3, 4, ou 5, ou un sel pharmaceutiquement acceptable d'acide carboxylique de formule (I). Le procédé de cette invention consiste à ajouter ce composé sous forme solide avec un support topique de manière à obtenir une formulation topique en sept jours avant la première administration topique de ce composé.

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