COMPOSES, COMPOSITIONS, KITS ET PROCEDES D'UTILISATION POUR TRAITER DE MANIERE ORALE ET TOPIQUE L'ACNE ET D'AUTRES ETATS DE LA PEAU PAR ADMINISTRATION D'UN ANALOGUE DE VITAMINE D CONTENANT DU 19-NOR AVEC OU SANS RETINOIDE

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专利权人:

WISCONSIN ALUMNI RESEARCH FOUNDATION

发明人:

CLAGETT-DAME, MARGARET,DELUCA, HECTOR F.,NIEVES, NIRCA J.,PLUM, LORI A.,KAISER, MARY E.,BARYCKI, RAFAL

申请号：

CA2674063

公开号：

CA2674063C

申请日:

2007.12.31

申请国别(地区):

CA

年份:

2016

代理人:

摘要：

Oral and topical pharmaceutical compositions, kits and methods of treatment thereof for treating various skin disorder including acne, psoriasis, ichthyosis, photoaging, photodamaged skin, and, skin cancer. Exemplary vitamin D analogs as active pharmaceutical ingredients include 2-methylene-19-nor-20(S)-l.alpha.-hydroxy-bishomopregnacalciferol, 19-nor- 26,27-dimethylene-20(S)-2-methylene-l.alpha.,25-dihydroxyvitamin D3, 2-methylene-l.alpha.,25- dihydroxy-( 17E)- 17(20)-dehydro- 19-nor-vitamin D3, 2-methylene- 19-nor-(24R)- 1 .alpha.,25- dihydroxyvitamin D2, 2-methylene-(20R,25S)-19,26-dinor-l.alpha.,25-dihydroxyvitamin 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- 19-nor-(20S)- 1 .alpha.-hydroxy-trishomopregnacalciferol, 2-methylene-23,23-difluoro- 1 .alpha.-hydroxy- 19-nor-bishomopregnacalciferol, 2-methylene-(20S)-23,23 -difluoro- 1 .alpha.-hydroxy- 19-nor-bishomopregnancalciferol, (2 -(3 'hydroxypropyl- 1 ',2 ' -idene)- 19,23,24-trinor-(20S)- l.alpha.-hydroxyvitamin D3, 2-methylene- 18, 19-dinor-(20S)-l.alpha.,25-dihydroxyvitamin D3, a stereoisomer thereof, a prodrug thereof in oral compositions, a salt thereof, and/or a solute thereof. Compounds that activate retinoic acid receptors, such as retinoyls and retinoyl esters, include 13-cw-retmoic acid, all-trafls-retinoic acid, (2E,4E,6Z,8E)-3,7-dimethyl-9- (2,6,6-trimethyl-l-cyclohexeneyl)nona-2,4,6,8-tetraenoic acid, 9-(4-methoxy-2,3,6-trimethyl- phenyl)-3,7-dimethyl-nona-2,4,6, 8-tetraenoic acid, 6- [3 -( 1 -adamantyl)-4-methox yphenyl] -2- napthoic acid, 4-[l-(3,5,5,8,8-pentamethyl-tetralin-2-yl)ethenyl]benzoic acid, retinobenzoic acid, ethyl 6-[2-(4,4-dimethylthiochroman-6-yl)ethynyl]pyridine-3-carboxylate, retinoyl t- butyrate, retinoyl pinacol, retinoyl cholesterol, an isomer thereof, a prodrug thereof for oral compositions, an ester thereof, a salt

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