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COMPUESTOS, COMPOSICIONES, KITS Y METODOS DE USO PARA TRATAR ORAL Y TOPICAMENTE EL ACNE Y OTRAS CONDICIONES DE LA PIEL MEDIANTE ADMINISTRACION DE UN ANALOGO DE VITAMINA D QUE CONTIENE 19-NOR, CON O SIN UN RETINOIDE.
专利权人:
WISCONSIN ALUMNI RESEARCH FOUNDATION.*
发明人:
HECTOR F. DELUCA,MARGARET CLAGETT-DAME,LORI A. PLUM,RAFAL BARYCKI,NIRCA J. NIEVES,MARY E. KAISER
申请号:
MX2011000850
公开号:
MX353142B
申请日:
2007.12.31
申请国别(地区):
MX
年份:
2017
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)-la-hydroxy-bishomopregnacalciferol, 19-nor- 26,27-dimethylene-20(S)-2-methylene-la,25-dihydroxyvitamin D3, 2-methylene-la,25- dihydroxy-( 17E)- 17(20)-dehydro- 19-nor-vitamin D3, 2-methylene- 19-nor-(24R)- 1 a,25- dihydroxyvitamin D2, 2-methylene-(20R,25S)-19,26-dinor-la,25-dihydroxyvitamin D3, 2- methylene- 19-nor- 1 a-hydroxy-pregnacalciferol, 1 a-hydroxy-2-methylene- 19-nor- homopregnacalciferol, (20R)- 1 a-hydroxy-2-methylene- 19-nor-bishomopregnacalciferol, 2- methylene- 19-nor-(20S)- 1 a-hydroxy-trishomopregnacalciferol, 2-methylene-23,23-difluoro- 1 a-hydroxy- 19-nor-bishomopregnacalciferol, 2-methylene-(20S)-23,23 -difluoro- 1 a-hydroxy- 19-nor-bishomopregnancalciferol, (2 -(3 'hydroxypropyl- 1 ',2 ' -idene)- 19,23,24-trinor-(20S)- la-hydroxyvitamin D3, 2-methylene- 18, 19-dinor-(20S)-la,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-carboxyla te, retinoyl t- butyrate, retinoyl pinacol, retinoyl cholesterol, an isomer thereof, a prodrug thereof for oral compositions, an ester thereof, a salt thereof, and/or, a solute thereof. Combinations of such active ingredients de
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