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    • 72. 发明授权
    • 2-methylene-19,26-dinor-(20R,22E,25R)-vitamin D analogs
    • 2-亚甲基-19,26-二烯 - (20R,22E,25R) - 维生素D类似物
    • US08193170B2
    • 2012-06-05
    • US12171113
    • 2008-07-10
    • Hector F. DeLucaGrazia ChielliniPawel GrzywaczLori A. PlumMargaret Clagett-Dame
    • Hector F. DeLucaGrazia ChielliniPawel GrzywaczLori A. PlumMargaret Clagett-Dame
    • A61K31/59C07C401/00C07C35/17A61P17/00
    • C07C401/00C07C2601/14C07C2602/24
    • This invention discloses 2-methylene-19,26-dinor-(20R,22E,25R)-vitamin D analogs, and specifically 2-methylene-19,26-dinor-(20R,22E,25R)-1α,25-dihydroxyvitamin D3, and pharmaceutical uses therefor. This compound exhibits transcription activity as well as pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to the monocyte thus evidencing use as an anti-cancer agent and for the treatment of skin diseases such as psoriasis as well as skin conditions such as wrinkles, slack skin, dry skin and insufficient sebum secretion. This compound also shows very low activity in vivo on bone calcium mobilization and relatively high intestinal calcium transport activity compared to the native hormone 1α,25-dihydroxyvitamin D3, and therefore may be used to treat autoimmune disorders or inflammatory diseases in humans as well as renal osteodystrophy. This compound may also be used for the treatment or prevention of obesity.
    • 本发明公开了2-亚甲基-29,26-二烯 - (20R,22E,25R) - 维生素D类似物,特别是2-亚甲基-19,26-二(20R,22E,25R)-1α,25-二羟基维生素 D3及其制药用途。 该化合物显示转录活性以及阻止未分化细胞增殖并诱导其分化为单核细胞的显着活性,因此证明其用作抗癌剂并用于治疗皮肤疾病如牛皮癣以及皮肤病症如 皱纹,皮肤松弛,皮肤干燥,皮脂分泌不足。 与天然激素1α,25-二羟基维生素D 3相比,该化合物在骨钙动员和体内相对较高的肠钙迁移活性中也显示出非常低的活性,因此可用于治疗人类以及肾脏中的自身免疫疾病或炎性疾病 骨营养不良。 该化合物也可用于治疗或预防肥胖症。
    • 73. 发明授权
    • Methods of increasing epidermal skin thickness by topical administration of a 19-nor containing vitamin D compound
    • 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
    • US08143238B2
    • 2012-03-27
    • US12399070
    • 2009-03-06
    • Hector F. DeLucaMargaret Clagett-DameLori A. PlumNirca J. NievesJamie Ahrens
    • Hector F. DeLucaMargaret Clagett-DameLori A. PlumNirca J. NievesJamie Ahrens
    • A61K31/59C07D401/00
    • A61K31/59
    • 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.
    • 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。
    • 74. 发明授权
    • 2-methylene-(20S,25S)-19,27-dinor-(22E)-vitamin D analogs
    • 2-亚甲基 - (20S,25S)-19,27-二(22E) - 维生素D类似物
    • US08114859B2
    • 2012-02-14
    • US11860863
    • 2007-09-25
    • Hector F. DeLucaMargaret Clagett-DameLori A. PlumGrazia ChielliniPawel Grzywacz
    • Hector F. DeLucaMargaret Clagett-DameLori A. PlumGrazia ChielliniPawel Grzywacz
    • A61K31/593C07C401/00
    • C07C401/00
    • This invention discloses 2-methylene-(20S,25S)-19,27-dinor-(22E)-vitamin D analogs, and specifically 2-methylene-(20S,25S)-19,27-dinor-(22E)-1α,25-dihydroxyvitamin D3, and pharmaceutical uses therefor. This compound exhibits pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to the monocyte thus evidencing use as an anti-cancer agent and for the treatment of skin diseases such as psoriasis as well as skin conditions such as wrinkles, slack skin, dry skin and insufficient sebum secretion. This compound also has little, if any, calcemic activity and therefore may be used to treat autoimmune disorders or inflammatory diseases in humans as well as renal osteodystrophy. This compound may also be used for the treatment or prevention of obesity.
    • 本发明公开了2-亚甲基 - (20S,25S)-19,27-二(22E) - 维生素D类似物,特别是2-亚甲基 - (20S,25S)-19,27-二(22E)-1α ,25-二羟基维生素D3及其药物用途。 该化合物在阻止未分化细胞的增殖并诱导其分化为单核细胞方面表现出显着的活性,从而证明其用作抗癌剂并用于治疗皮肤疾病如牛皮癣以及皮肤病症如皱纹,松弛皮肤, 皮肤干燥,皮脂分泌不足。 该化合物也具有很少(如果有的话)钙活性,因此可用于治疗人体中的自身免疫性疾病或炎性疾病以及肾性骨营养不良。 该化合物也可用于治疗或预防肥胖症。
    • 77. 发明授权
    • 2-methylene-(20S,25S)-19,26-dinor-vitamin D analogs
    • 2-二甲基 - (20S,25S)-19,26-二 - 维生素D类似物
    • US07947666B2
    • 2011-05-24
    • US12343592
    • 2008-12-24
    • Hector F. DeLucaMargaret Clagett-DameLori A. PlumGrazia ChielliniPawel Grzywacz
    • Hector F. DeLucaMargaret Clagett-DameLori A. PlumGrazia ChielliniPawel Grzywacz
    • A61K31/59C07C401/00
    • C07C401/00
    • This invention discloses 2-methylene-(20S,25S)-19,26-dinor-vitamin D analogs, and specifically 2-methylene-(20S,25S)-19,26-dinor-1α,25-dihydroxyvitamin D3, and pharmaceutical uses therefor. This compound exhibits pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to the monocyte thus evidencing use as an anti-cancer agent and for the treatment of skin diseases such as psoriasis as well as skin conditions such as wrinkles, slack skin, dry skin and insufficient sebum secretion. This compound also has little, if any, calcemic activity and therefore may be used to treat autoimmune disorders or inflammatory diseases in humans as well as renal osteodystrophy. This compound may also be used for the treatment or prevention of obesity.
    • 本发明公开了2-亚甲基 - (20S,25S)-19,26-二 - 维生素D类似物,特别是2-亚甲基 - (20S,25S)-19,26-二酮-1α,25-二羟基维生素D 3和药物 用它。 该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显着的活性,从而证明其用作抗癌剂并用于治疗皮肤疾病如牛皮癣以及皮肤病症如皱纹,松弛皮肤, 皮肤干燥,皮脂分泌不足。 该化合物也具有很少(如果有的话)钙活性,因此可用于治疗人体中的自身免疫性疾病或炎性疾病以及肾性骨营养不良。 该化合物也可用于治疗或预防肥胖症。
    • 78. 发明授权
    • 2-methylene-(22E)-25-(1-methylene-hexyl)-26,27-cyclo-22-dehydro-19-nor-vitamin D analogs
    • 2-亚甲基 - (22E)-25-(1-亚甲基 - 己基)-26,27-环-22-脱氢-19-维生素D类似物
    • US07713953B2
    • 2010-05-11
    • US12171094
    • 2008-07-10
    • Hector F. DeLucaRafal BaryckiLori A. PlumMargaret Clagett-Dame
    • Hector F. DeLucaRafal BaryckiLori A. PlumMargaret Clagett-Dame
    • A61K31/59A61K31/593A61K31/592C07C401/00
    • C07C401/00C07C2601/02
    • This invention discloses 2-methylene-(22E)-25-(1-methylene-hexyl)-26,27-cyclo-22-dehydro-19-nor-vitamin D analogs, and specifically 2-methylene-(22E)-25-(1-methylene-hexyl)-26,27-cyclo-22-dehydro-19-nor-1α,24(R)-dihydroxyvitamin D3, and pharmaceutical uses therefor. This compound exhibits relatively high transcription activity as well as pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to the monocyte thus evidencing use as an anti-cancer agent and for the treatment of skin diseases such as psoriasis as well as skin conditions such as wrinkles, slack skin, dry skin and insufficient sebum secretion. This compound also shows lower activity in vivo on bone calcium mobilization and intestinal calcium transport activity compared to the native hormone 1α,25-dihydroxyvitamin D3, and therefore may be used to treat autoimmune disorders or inflammatory diseases in humans as well as renal osteodystrophy. This compound may also be used for the treatment or prevention of obesity.
    • 本发明公开了2-亚甲基 - (22E)-25-(1-亚甲基 - 己基)-26,27-环-22-脱氢-19-去甲维生素D类似物,特别是2-亚甲基 - (22E)-25 - (1-亚甲基 - 己基)-26,27-环-22-脱氢-19-去甲-1α,24(R) - 二羟基维生素D3及其药学用途。 该化合物显示相对较高的转录活性以及阻止未分化细胞增殖并诱导其分化为单核细胞的明显活性,从而证明其用作抗癌剂并用于治疗皮肤疾病如牛皮癣以及皮肤病症 如皱纹,皮肤松弛,皮肤干燥和皮脂分泌不足。 与天然激素1α,25-二羟基维生素D3相比,该化合物在骨钙动员和肠钙转运活性方面的活性也较低,因此可用于治疗人体中的自身免疫性疾病或炎性疾病以及肾性骨营养不良。 该化合物也可用于治疗或预防肥胖症。