13,13-dimethyl-des-c,d analogs of...

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C - Chemistry, Metallurgy

07

C

C07C 35/17 (2006.01) A61K 31/047 (2006.01) A61P 17/00 (2006.01) A61P 17/06 (2006.01) A61P 35/00 (2006.01) C07C 401/00 (2006.01) C07F 7/18 (2006.01)

Patent

CA 2712748

13,13-Dimethyl-flfes-C,D analogs of 1.alpha.,25-dihydroxy-19-nor-vitamin D3 compounds and topical composition dosage forms thereof, and methods of treating skin conditions thereof. Exemplary active pharmaceutical ingredients include (1R,3R)-5-[(E)-(S)-11'-hydroxy- 5,5',7',11 '-tetramethyl-dodec-2'- enylidene]-2-metylene-cyclohexane-1,3-diol, (1R,3R)-5-[(Z)-(S)-11 '-hydroxy-5',5',7',11 '-tetramethyl-dodec-2'-enylidene]- 2-metylene-cyclohexane-1,3-diol, (1R,3R)-5-[(E)-(R)-1 1 '-hydroxy-5',5',7',11 '-tetramethyl-dodec-2'-enylidene]-2-metylene- cyclohexane-1,3-diol, and (1R,3R)-5-[(Z)-(R)-11'-hy-droxy-5',5',7',11'-tetramethyl-dodec-2'- enylidene] - 2-metylene-cyclohexane- 1,3 -diol.

L'invention porte sur des analogues 13,13-diméthyl-des-C,D de composés de la,25-dihydroxy-19-nor-vitamine D3 et sur des formes posologiques de compositions topiques de ceux-ci, ainsi que sur des procédés de traitement d'états pathologiques de la peau par ceux-ci. Des exemples d'ingrédients pharmaceutiques actifs comprennent le (1R,3R)-5-[(E)-(S)-11'-hydroxy- 5',5',7',11'-tétraméthyl-dodéc-2'-énylidène]-2-méthylènecyclohexane-l,3-diol, le (1R,3R)-5-[(Z)-(S)-11'-hydroxy-5',5',7',11'-tétraméthyl-dodéc-2'-énylidène]-2-méthylènecyclohexane-l,3-diol, le (1R,3R)-5-[(E)-(R)-l 1'-hydroxy-5',5',7',11'-tétraméthyl-dodéc-2'-énylidène]-2-méthylènecyclohexane-l,3-diol et le (1R,3R)-5-[(Z)-(R)-11'-hydroxy-5',5',7',11'-tétraméthyl-dodéc-2'- énylidène]-2-méthylènecyclohexane-1,3-diol.

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