Methods of increasing epidermal skin thickness by topical...

A - Human Necessities – 61 – K

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A61K 31/59 (2006.01) A61P 17/00 (2006.01)

Patent

CA 2715811

Methods of increasing the thickness of the epidermal layer in the skin of a human comprising topically administering a therapeutically effective dose of an active pharmaceutical ingredient comprising a vitamin D analog including 2- methylene-19-nor-20(S)-1.alpha.-hydroxy-bishomopregnacalciferol, 19-nor-26,27- dimethylene-20(S)-2-methylene-1.alpha.,25-dihydroxy- vitamin D3, 2-methylene-19-nor-(24R)-1.alpha.,25-dihydroxyvitamin D2, 2- methylene-1.alpha.,25-dihydroxy-(17E)-17(20)-dehydro-19-norvitamin D3, 2-methylene-(20R,25S)-19,26-dinor-1.alpha.,25-dihydroxyvitamin D3, 2- methylene-18,19-dinor-(20S)-1.alpha.,25-dihydrox- yvitamin D3, 2-methylene-19-nor-1.alpha.-hydroxy-pregnacalciferol, 1.alpha.- hydroxy-2-methylene-19-nor-homopregnacalciferol, (20R)-1.alpha.-hydroxy-2-methylene-19-nor-bishomopregnacalciferol, 2-methylene- (20S)-19-nor-1.alpha.-hydroxy-trishomopregnacalciferol, 2-methylene-(20R)-23,23-difluoro-1.alpha.-hydroxy-19-nor- bishomopregnacalciferol, 2-methylene-(20S)-23,23-difluoro-1.alpha.-hy droxy-19-nor-bishomopregnancalciferol, 2-(3'hydroxypropyl-1',2'-idene)- 19,23,24-trinor-(20S)-1.alpha.-hydroxyvitamin D3, or 13,13- dimethyl-des-C,D analog of (20S)-2-methylene-1.alpha.,25-dihydroxy-19-nor- vitamin D3, and pharmaceutical topical formulations and topical dosage forms thereof using a pharmaceutically suitable carrier vehicle.

Linvention concerne des procédés daugmentation de lépaisseur de la couche épidermique dans la peau dun être humain comprenant ladministration topique dune dose thérapeutiquement efficace dun ingrédient pharmaceutique actif comprenant une vitamine D analogue incluant du 2-méthylène-l 9-nor- 20(S)-I a-hydroxy-bishomoprégnacalciférol, de la 19-nor-26,27-diméthylène-20(S)-2-méthylène- la,25-dihydroxyvitamine D3, de la 2-méthylène-19-nor-(24R)-la,25-dihydroxyvitamine D2, de la 2- méthylène- 1 a,25-dihydroxy-( 17E)- 17(20)-dehydro- 19-nor- vitamine D3, de la 2-méthylène- (20R,25S)- 19,26-dinor- 1 a,25-dihydroxyvitamine D3, du 2-méthylène-l 8, de la 19-dinor-(20S)- 1 a,25- dihydroxyvitamine D3, du 2-méthylène-l 9-nor- la-hydroxy-prégnacalciférol, du la-hydroxy-2- méthylène- 19-nor-homoprégnacalciférol, du (20R)- 1 a-hydroxy-2-méthylène- 19-nor- bishomoprégnacalciférol, du 2-méthylène-(20S)-19-nor-la-hydroxy-trishomoprégnacalciférol, du 2-méthylène-(20R)-23,23 -difluoro- 1 a-hydroxy- 19-nor-bishomoprégnacalciférol, du 2- méthylène-(20S)-23,23 -difluoro- 1 a-hydroxy- 19-nor-bishomoprégnancalciférol, de la 2- (3'hydroxypropyl-l',2'-idène)-19,23,24-trinor-(20S)-la-hydroxyvitamine D3, ou du 13,13- diméthyl-cfe.s-C,D analogue de la (20S)-2-méthylène-la,25-dihydroxy-l 9-nor- vitamine D3, et des formules topiques pharmaceutiques et des formes de dosage topique de ceux-ci utilisant un véhicule porteur pharmaceutiquement approprié.

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