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1. 发明授权

US08193171B2 13,13-dimethyl-des-C,D analogs of 1α,25-dihydroxy-19-nor-vitamin D3 compounds and topical composition dosage forms and methods of treating skin conditions thereof 有权
标题翻译： 1α，25-二羟基-19-去甲维生素D3化合物的13,13-二甲基-de-C，D类似物和局部组合物剂型及治疗其皮肤病症的方法
公开(公告)号：US08193171B2
公开(公告)日：2012-06-05
申请号：US12357702
申请日：2009-01-22
申请人： Hector F. DeLuca , Margaret Clagett-Dame , Lori A. Plum , Rafal R. Sicinski , Katarzyna Plonska-Ocypa , Nirca J. Nieves , Pawel Grzywacz
发明人： Hector F. DeLuca , Margaret Clagett-Dame , Lori A. Plum , Rafal R. Sicinski , Katarzyna Plonska-Ocypa , Nirca J. Nieves , Pawel Grzywacz
IPC分类号： A61K31/047 , C07C35/17 , C07C401/00 , A61P17/00
CPC分类号： C07C401/00 , C07C2601/14
摘要： 13,13-Dimethyl-des-C,D analogs of 1α,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-methylene-cyclohexane-1,3-diol, (1R,3R)-5-[(Z)-(S)-11′-hydroxy-5′,5′,7′,11′-tetramethyl-dodec-2′-enylidene]-2-methylene-cyclohexane-1,3-diol, (1R,3R)-5-[(E)-(R)-11′-hydroxy-5′,5′,7′,11′-tetramethyl-dodec-2′-enylidene]-2-methylene-cyclohexane-1,3-diol, and (1R,3R)-5-[(Z)-(R)-11′-hydroxy-5′,5′,7′,11′-tetramethyl-dodec-2′-enylidene]-2-methylene-cyclohexane-1,3-diol.
摘要翻译： 1α，25-二羟基-19-去甲维生素D3化合物的13,13-二甲基-D-脱氧-D类似物及其局部组合物剂型，以及其皮肤病症的治疗方法。示例性的活性药物成分包括（1R，3R）-5 - [（E） - （S）-11'-羟基-5'，5'，7'，11'-四甲基 - 十二烷-2'-亚基] -2 亚甲基环己烷-1,3-二醇，（1R，3R）-5 - [（Z） - （S）-11'-羟基-5'，5'，7'，11'-四甲基 - （1R，3R）-5 - [（E） - （R）-11'-羟基-5'，5'，7'，11' 和（1R，3R）-5 - [（Z） - （R）-11'-羟基-5'，5'，5'-二甲基环己烷-1,3-二醇 '，7'，11'-四甲基 - 十二烷-2'-亚炔基] -2-亚甲基 - 环己烷-1,3-二醇。

2. 发明申请

US20090186950A1 13,13-Dimethyl-des-C,D Analogs of 1Alpha,25-Dihydroxy-19-Nor-Vitamin D3 Compounds and Topical Composition Dosage Forms and Methods of Treating Skin Conditions Thereof 有权
标题翻译： 1Alpha，25-二羟基-19-不维生素D3化合物的13,13-二甲基-D-C，D类似物和局部组合物剂型及其治疗皮肤病症的方法
公开(公告)号：US20090186950A1
公开(公告)日：2009-07-23
申请号：US12357702
申请日：2009-01-22
申请人： Hector F. DeLuca , Margaret Clagett-Dame , Lori A. Plum , Rafal R. Sicinski , Katarzyna Plonska-Ocypa , Nirca J. Nieves , Pawel Grzywacz
发明人： Hector F. DeLuca , Margaret Clagett-Dame , Lori A. Plum , Rafal R. Sicinski , Katarzyna Plonska-Ocypa , Nirca J. Nieves , Pawel Grzywacz
IPC分类号： A61K31/047 , C07C35/17 , A61P35/00
CPC分类号： C07C401/00 , C07C2601/14
摘要： 13,13-Dimethyl-des-C,D analogs of 1α,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)-11′-hydroxy-5′,5′,7′,11′-tetramethyl-dodec-2′-enylidene]-2-metylene-cyclohexane-1,3-diol, and (1R,3R)-5-[(Z)-(R)-11′-hydroxy-5′,5′,7′,11′-tetramethyl-dodec-2′-enylidene]-2-metylene-cyclohexane-1,3-diol.
摘要翻译： 1α，25-二羟基-19-去甲维生素D 3化合物的13,13-二甲基-D-C，D类似物及其局部组合物剂型，以及其皮肤病症的治疗方法。示例性的活性药物成分包括（1R，3R）-5 - [（E） - （S）-11'-羟基-5'，5'，7'，11'-四甲基 - 十二烷-2'-亚基] -2 （1R，3R）-5 - [（Z） - （S）-11'-羟基-5'，5'，7'，11'-四甲基 - 十二烷基-2- （1R，3R）-5 - [（E） - （R）-11'-羟基-5'，5'，7'，11' （1R，3R）-5 - [（Z） - （R）-11'-羟基-5'，5'，5'-二甲基环己烷-1,3-二醇 '，7'，11'-四甲基 - 十二烷-2'-亚炔基] -2-亚甲基 - 环己烷-1,3-二醇。

3. 发明申请

US20110082121A1 1-Desoxy-2-Methylene-19-Nor-Vitamin D Analogs and Their Uses 有权
标题翻译： 1-脱氧-2-亚甲基-19-维生素D类似物及其用途
公开(公告)号：US20110082121A1
公开(公告)日：2011-04-07
申请号：US12895478
申请日：2010-09-30
申请人： Hector F. DeLuca , Katarzyna M. Barycka , Izabela Sibilska , Lori A. Plum , Margaret Clagett-Dame , Rafal Barycki , Rafal R. Sicinski , Katarzyna Plonska-Ocypa
发明人： Hector F. DeLuca , Katarzyna M. Barycka , Izabela Sibilska , Lori A. Plum , Margaret Clagett-Dame , Rafal Barycki , Rafal R. Sicinski , Katarzyna Plonska-Ocypa
IPC分类号： A61K31/593 , C07C35/21 , C07F9/28 , A61P13/12 , A61P19/10 , A61P17/06 , A61P35/00
CPC分类号： C07C401/00 , C07F9/5325
摘要： This invention discloses 1-desoxy-2-methylene-19-nor-vitamin D analogs, and specifically (20S)-25-hydroxy-1-desoxy-2-methylene-19-nor-vitamin D3 and pharmaceutical uses therefor. This compound exhibits relatively high binding activity and pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to the monocyte thus evidencing use as an anti-cancer agent especially for the treatment or prevention of leukemia, colon cancer, breast cancer, skin cancer or prostate cancer.
摘要翻译：本发明公开了1-脱氧-2-亚甲基-19-去甲维生素D类似物，特别是（20S）-25-羟基-1-脱氧-2-亚甲基-19-去甲维生素D3及其药物用途。该化合物在阻止未分化细胞的增殖和诱导其分化为单核细胞方面表现出相对较高的结合活性和明显的活性，从而证明其用作抗癌剂，特别是用于治疗或预防白血病，结肠癌，乳腺癌，皮肤癌或前列腺癌。

4. 发明申请

US20120157418A1 2-Methylene-19-Nor-Vitamin D Analogs and Their Uses 有权
标题翻译： 2-亚甲基-19-维生素D类似物及其用途
公开(公告)号：US20120157418A1
公开(公告)日：2012-06-21
申请号：US13278846
申请日：2011-10-21
申请人： Hector F. DeLuca , Izabela Sibilska , Lori A. Plum , Margaret Clagett-Dame , Rafal R. Sicinski , Katarzyna M. Barycka , Katarzyna Plonska-Ocypa , Rafal Barycki
发明人： Hector F. DeLuca , Izabela Sibilska , Lori A. Plum , Margaret Clagett-Dame , Rafal R. Sicinski , Katarzyna M. Barycka , Katarzyna Plonska-Ocypa , Rafal Barycki
IPC分类号： A61K31/593 , C07F7/18 , C07F9/53 , A61P35/02 , A61P19/08 , A61P19/10 , C07C401/00 , A61P35/00
CPC分类号： C07C401/00 , C07F7/1804 , C07F9/5325
摘要： This invention discloses 2-methylene-19-nor-vitamin D analogs, and specifically (20S)-25-hydroxy-2-methylene-19-nor-vitamin D3 and (20R)-25-hydroxy-2-methylene-19-nor-vitamin D3, as well as pharmaceutical uses therefor. These compounds exhibit relatively high binding activity and pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to the monocyte thus evidencing use as an anti-cancer agent especially for the treatment or prevention of osteosarcoma, leukemia, colon cancer, breast cancer, skin cancer or prostate cancer. Although these compounds have relatively low calcemic activities they may also be useful in the treatment of bone diseases due to their ability to act as prodrugs in vivo.
摘要翻译：本发明公开了2-亚甲基-19-去甲维生素D类似物，特别是（20S）-25-羟基-2-亚甲基-19-去甲维生素D3和（20R）-25-羟基-2-亚甲基-19- 维生素D3，以及其用途。这些化合物在阻止未分化细胞的增殖并诱导其分化为单核细胞方面表现出相对较高的结合活性和显着的活性，从而证明其用作抗癌剂，特别是用于治疗或预防骨肉瘤，白血病，结肠癌，乳腺癌，皮肤癌或前列腺癌。虽然这些化合物具有相对较低的血钙活性，但是由于它们在体内作为前药的能力，它们也可用于治疗骨骼疾病。

5. 发明授权

US08642579B2 1-desoxy-2-methylene-19-nor-vitamin D analogs and their uses 有权
标题翻译： 1-脱氧-2-亚甲基-19-维生素D类似物及其用途
公开(公告)号：US08642579B2
公开(公告)日：2014-02-04
申请号：US12895478
申请日：2010-09-30
申请人： Hector F. DeLuca , Katarzyna M. Barycka , Izabela Sibilska , Lori A. Plum , Margaret Clagett-Dame , Rafal Barycki , Rafal R. Sicinski , Katarzyna Plonska-Ocypa
发明人： Hector F. DeLuca , Katarzyna M. Barycka , Izabela Sibilska , Lori A. Plum , Margaret Clagett-Dame , Rafal Barycki , Rafal R. Sicinski , Katarzyna Plonska-Ocypa
IPC分类号： A61K31/59 , C07C401/00
CPC分类号： C07C401/00 , C07F9/5325
摘要： This invention discloses 1-desoxy-2-methylene-19-nor-vitamin D analogs, and specifically (20S)-25-hydroxy-1-desoxy-2-methylene-19-nor-vitamin D3 and pharmaceutical uses therefor. This compound exhibits relatively high binding activity and pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to the monocyte thus evidencing use as an anti-cancer agent especially for the treatment or prevention of leukemia, colon cancer, breast cancer, skin cancer or prostate cancer.
摘要翻译：本发明公开了1-脱氧-2-亚甲基-19-去甲维生素D类似物，特别是（20S）-25-羟基-1-脱氧-2-亚甲基-19-去甲维生素D3及其药物用途。该化合物在阻止未分化细胞的增殖和诱导其分化为单核细胞方面表现出相对较高的结合活性和明显的活性，从而证明其用作抗癌剂，特别是用于治疗或预防白血病，结肠癌，乳腺癌，皮肤癌或前列腺癌。

6. 发明授权

US08518917B2 2-methylene-19-nor-vitamin D analogs and their uses 有权
标题翻译： 2-亚甲基-19-维生素D类似物及其用途
公开(公告)号：US08518917B2
公开(公告)日：2013-08-27
申请号：US13278846
申请日：2011-10-21
申请人： Hector F. DeLuca , Izabela Sibliska , Lori A. Plum , Margaret Clagett-Dame , Rafal R. Sicinski , Katarzyna M. Barycka , Katarzyna Plonska-Ocypa , Rafal Barycki
发明人： Hector F. DeLuca , Izabela Sibliska , Lori A. Plum , Margaret Clagett-Dame , Rafal R. Sicinski , Katarzyna M. Barycka , Katarzyna Plonska-Ocypa , Rafal Barycki
IPC分类号： C07C401/00 , A61K31/59
CPC分类号： C07C401/00 , C07F7/1804 , C07F9/5325
摘要： This invention discloses 2-methylene-19-nor-vitamin D analogs, and specifically (20S)-25-hydroxy-2-methylene-19-nor-vitamin D3 and (20R)-25-hydroxy-2-methylene-19-nor-vitamin D3, as well as pharmaceutical uses therefor. These compounds exhibit relatively high binding activity and pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to the monocyte thus evidencing use as an anti-cancer agent especially for the treatment or prevention of osteosarcoma, leukemia, colon cancer, breast cancer, skin cancer or prostate cancer. Although these compounds have relatively low calcemic activities they may also be useful in the treatment of bone diseases due to their ability to act as prodrugs in vivo.
摘要翻译：本发明公开了2-亚甲基-19-去甲维生素D类似物，特别是（20S）-25-羟基-2-亚甲基-19-去甲维生素D3和（20R）-25-羟基-2-亚甲基-19- 维生素D3，以及其用途。这些化合物在阻止未分化细胞的增殖并诱导其分化为单核细胞方面表现出相对较高的结合活性和显着的活性，从而证明其用作抗癌剂，特别是用于治疗或预防骨肉瘤，白血病，结肠癌，乳腺癌，皮肤癌或前列腺癌。虽然这些化合物具有相对较低的血钙活性，但是由于它们在体内作为前药的能力，它们也可用于治疗骨骼疾病。

7. 发明授权

US07534777B2 Des-C,D analogs of 1α,25-dihydroxy-19-norvitamin D3 有权
标题翻译： 1α，25-二羟基-19-去甲维生素D3的Des-C，D类似物
公开(公告)号：US07534777B2
公开(公告)日：2009-05-19
申请号：US11512705
申请日：2006-08-30
申请人： Hector F. DeLuca , Katarzyna Plonska-Ocypa , Rafal Sicinski , Pawel Grzywacz , Lori A. Plum , Margaret Clagett-Dame
发明人： Hector F. DeLuca , Katarzyna Plonska-Ocypa , Rafal Sicinski , Pawel Grzywacz , Lori A. Plum , Margaret Clagett-Dame
IPC分类号： A61K31/45 , C07D401/00
CPC分类号： C07C401/00 , C07B2200/07 , C07C35/17 , C07C45/292 , C07C45/30 , C07C47/19 , C07C403/08 , C07C2601/14 , C07F7/1804 , Y02P20/55
摘要： Des-C,D 2-methylene-19-norvitamin D3 analogs are provided including compounds of formula 1, in which R1 is a straight or branched chain alkyl or alkylene group having from 8 to 27 carbons and bearing an OY3 group; and Y1, Y2 and Y3 are independently selected from H or hydroxy-protecting groups. Such compounds may be used in preparing pharmaceutical compositions and are useful in treating a variety of biological conditions.
摘要翻译：提供了包含式1化合物的Des-C，D 2 - 亚甲基-19-诺维生素D3类似物，其中R 1是具有8至27个碳并具有OY 3基团的直链或支链烷基或亚烷基; Y 1，Y 2和Y 3独立地选自H或羟基保护基。这样的化合物可用于制备药物组合物，并且可用于治疗各种生物学条件。

8. 发明申请

US20110195941A1 Methods of Use To Orally and Topically Treat Acne and Other Skin Conditions By Administering a 19-NOR Containing Vitamin D Analog With or Without a Retinoid 审中-公开
公开(公告)号：US20110195941A1
公开(公告)日：2011-08-11
申请号：US13087764
申请日：2011-04-15
申请人： Margaret Clagett-Dame , Hector F. DeLuca , Nirca J. Nieves , Lori A. Plum , Mary E. Kaiser
发明人： Margaret Clagett-Dame , Hector F. DeLuca , Nirca J. Nieves , Lori A. Plum , Mary E. Kaiser
IPC分类号： A61K31/59 , A61P17/00
CPC分类号： A61K31/59 , A61K8/67 , A61K9/0014 , A61K9/0053 , A61K9/0095 , A61K31/203 , A61K47/10 , A61K47/44 , A61K2800/92 , A61Q19/00 , A61Q19/004 , A61Q19/08
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)-1α-hydroxy-bishomopregnacalciferol, 19-nor-26,27-dimethylene-20(S)-2-methylene-1α,25-dihydroxyvitamin D3, 2-methylene-1α,25-dihydroxy-(17E)-17(20)-dehydro-19-nor-vitamin D3, 2-methylene-19-nor-(24R)-1α,25-dihydroxyvitamin D2, 2-methylene-(20R,25S)-19,26-dinor-1α,25-dihydroxyvitamin D3, 2-methylene-19-nor-1α-hydroxy-pregnacalciferol, 1α-hydroxy-2-methylene-19-nor-homopregnacalciferol, (20R)-1α-hydroxy-2-methylene-19-nor-bishomopregnacalciferol, 2-methylene-19-nor-(20S)-1α-hydroxy-trishomopregnacalciferol, 2-methylene-23,23-difluoro-1α-hydroxy-19-nor-bishomopregnacalciferol, 2-methylene-(20S)-23,23-difluoro-1α-hydroxy-19-nor-bishomopregnancalciferol, (2-(3′ hydroxypropyl-1′,2′-idene)-19,23,24-trinor-(20S)-1α-hydroxyvitamin D3, 2-methylene-18,19-dinor-(20S)-1α,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-cis-retinoic acid, all-trans-retinoic acid, (2E,4E,6Z,8E)-3,7-dimethyl-9-(2,6,6-trimethyl-1-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-methoxyphenyl]-2-napthoic acid, 4-[1-(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 thereof, and/or, a solute thereof. Combinations of such active ingredients demonstrate synergistic efficacy.

9. 发明授权

US08143238B2 Methods of increasing epidermal skin thickness by topical administration of a 19-nor containing vitamin D compound 有权
标题翻译：通过局部施用19-不含维生素D化合物来增加表皮皮肤厚度的方法
公开(公告)号：US08143238B2
公开(公告)日：2012-03-27
申请号：US12399070
申请日：2009-03-06
申请人： Hector F. DeLuca , Margaret Clagett-Dame , Lori A. Plum , Nirca J. Nieves , Jamie Ahrens
发明人： Hector F. DeLuca , Margaret Clagett-Dame , Lori A. Plum , Nirca J. Nieves , Jamie Ahrens
IPC分类号： A61K31/59 , C07D401/00
CPC分类号： A61K31/59
摘要： 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)-1α-hydroxy-bishomopregnacalciferol, 19-nor-26,27-dimethylene-20(S)-2-methylene-1α,25-dihydroxyvitamin D3, 2-methylene-19-nor-(24R)-1α,25-dihydroxyvitamin D2, 2-methylene-1α,25-dihydroxy-(17E)-17(20)-dehydro-19-nor-vitamin D3, 2-methylene-(20R,25S)-19,26-dinor-1α,25-dihydroxyvitamin D3, 2-methylene-18,19-dinor-(20S)-1α,25-dihydroxyvitamin D3, 2-methylene-19-nor-1α-hydroxy-pregnacalciferol, 1α-hydroxy-2-methylene-19-nor-homopregnacalciferol, (20R)-1α-hydroxy-2-methylene-19-nor-bishomopregnacalciferol, 2-methylene-(20S)-19-nor-1α-hydroxy-trishomopregnacalciferol, 2-methylene-(20R)-23,23-difluoro-1α-hydroxy-19-nor-bishomopregnacalciferol, 2-methylene-(20S)-23,23-difluoro-1α-hydroxy-19-nor-bishomopregnacalciferol, 2-(3′hydroxypropyl-1′,2′-idene)-19,23,24-trinor-(20S)-1α-hydroxyvitamin D3, or 13,13-dimethyl-des-C,D analog of (20S)-2-methylene-1α,25-dihydroxy-19-nor-vitamin D3, and pharmaceutical topical formulations and topical dosage forms thereof using a pharmaceutically suitable carrier vehicle.
摘要翻译：包括局部施用治疗有效剂量的包含维生素D类似物的活性药物成分的方法，所述维生素D类似物包括2-亚甲基-19-去甲基-20（S）-1α-羟基 - （2H） - 二亚甲基-1α，25-二羟基维生素D3，2-亚甲基-19-去甲 - （24R）-1α，25-二羟基维生素D 2，2-亚甲基 -1α，25-二羟基 - （17E）-17（20） - 脱氢-19-去甲维生素D3，2-亚甲基 - （20R，25S）-19,26-二酮-1α，25-二羟基维生素D3，亚甲基-18,19-二（20S）-1α，25-二羟基维生素D 3，2-亚甲基-19-去甲-1α-羟基 - 孕代孕甾醇，1α-羟基-2-亚甲基-19-去高孕孕甾烷醇（20R） -1α-羟基-2-亚甲基-19-去氧胆钙孕激醇，2-亚甲基 - （20S）-19-去甲-α-羟基 - 三孕代孕甾醇，2-亚甲基 - （20R）-23,23-二氟-1α-羟基（20S）-23,23-二氟-1α-羟基-19-去氧胆钙孕激醇，2-（3'-羟基脯氨酸（20S）-2-亚甲基 - （20S）-1α-羟基维生素D3或13,13-二甲基-de-C，D类似物， 1α，25-二羟基-19-去甲维生素D3，以及使用药学上合适的载体载体的药物局部制剂及其局部剂型。

10. 发明申请

US20090227545A1 METHODS OF INCREASING EPIDERMAL SKIN THICKNESS BY TOPICAL ADMINISTRATION OF A 19-NOR CONTAINING VITAMIN D COMPOUND 有权
标题翻译：通过19-NOR含维生素D化合物的局部给药增加皮肤厚度的方法
公开(公告)号：US20090227545A1
公开(公告)日：2009-09-10
申请号：US12399070
申请日：2009-03-06
申请人： Hector F. DeLuca , Margaret Clagett-Dame , Lori A. Plum , Nirca J. Nieves , Jamie Ahrens
发明人： Hector F. DeLuca , Margaret Clagett-Dame , Lori A. Plum , Nirca J. Nieves , Jamie Ahrens
IPC分类号： A61K31/59 , A61P17/00
CPC分类号： A61K31/59
摘要： 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)-1α-hydroxy-bishomopregnacalciferol, 19-nor-26,27-dimethylene-20(S)-2-methylene-1α,25-dihydroxyvitamin D3, 2-methylene-19-nor-(24R)-1α,25-dihydroxyvitamin D2, 2-methylene-1α,25-dihydroxy-(17E)-17(20)-dehydro-19-nor-vitamin D3, 2-methylene-(20R,25S)-19,26-dinor-1α,25-dihydroxyvitamin D3, 2-methylene-18,19-dinor-(20S)-1α,25-dihydroxyvitamin D3, 2-methylene-19-nor-1α-hydroxy-pregnacalciferol, 1α-hydroxy-2-methylene-19-nor-homopregnacalciferol, (20R)-1α-hydroxy-2-methylene-19-nor-bishomopregnacalciferol, 2-methylene-(20S)-19-nor-1α-hydroxy-trishomopregnacalciferol, 2-methylene-(20R)-23,23-difluoro-1α-hydroxy-19-nor-bishomopregnacalciferol, 2-methylene-(20S)-23,23-difluoro-1α-hydroxy-19-nor-bishomopregnacalciferol, 2-(3′hydroxypropyl-1′,2′-idene)-19,23,24-trinor-(20S)-1α-hydroxyvitamin D3, or 13,13-dimethyl-des-C,D analog of (20S)-2-methylene-1α,25-dihydroxy-19-nor-vitamin D3, and pharmaceutical topical formulations and topical dosage forms thereof using a pharmaceutically suitable carrier vehicle.
摘要翻译：增加人皮肤中表皮层厚度的方法，包括局部施用治疗有效剂量的包含维生素D类似物的活性药物成分，所述维生素D类似物包括2-亚甲基-19-去甲-20（S）-1α-羟基 - （2H） - 二亚甲基-1α，25-二羟基维生素D3，2-亚甲基-19-去甲 - （24R）-1α，25-二羟基维生素D 2，2-亚甲基 -1α，25-二羟基 - （17E）-17（20） - 脱氢-19-去甲维生素D3，2-亚甲基 - （20R，25S）-19,26-二牛醇-1α，25-二羟基维生素D3，亚甲基-18,19-二烯 - （20S）-1α，25-二羟基维生素D3，2-亚甲基-19-去甲-alpha-羟基 - 孕代孕甾醇，1α-羟基-2-亚甲基-19-去高孕孕甾烷醇（20R） 1-羟基-2-亚甲基-19-去氧胆钙孕激醇，2-亚甲基 - （20S）-19-去甲-α-羟基 - 三孕代孕甾醇，2-亚甲基 - （20R）-23,23-二氟-1α-羟基（20S）-23,23-二氟-alpha-hydroxy-19-nor-bish-19-nor-bishomopregnacalciferol，2- 孕激素钙，2-（3'-羟基丙基-1'，2'-亚苯基）-19,23,24-三硝基 - （20S）-1α-羟基维生素D3或13,13-二甲基-de-C，D类似物（ 20S）-2-亚甲基-1α，25-二羟基-19-去甲维生素D3，以及使用药学上合适的载体载体的药物局部制剂及其局部剂型。

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