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2-METHYLENE-(20E)-20(22)-DEHYDRO-19-NOR-VITAMIN D ANALOGS.

机译:2-亚甲基-(20E)-20(22)-DEHYDRO-19-NOR-Vitamin D ANALOGS。

摘要

This invention discloses 2-methylene-(20E)-20(22)-dehydro-19-nor-vitamin D analogs, and specifically 2-methylene-(20E)-20(22)-dehydro-19-nor-lα,25- 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 similar in vivo intestinal calcium transport activity compared to the native hormone lα,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.
机译:本发明公开了2-亚甲基-(20E)-20(22)-dehydro-19-nor-vitamin D类似物,特别是2-亚甲基-(20E)-20(22)-dehydro-19-nor-lα, 25-二羟基维生素D3及其医药用途。该化合物在阻止未分化细胞的增殖并诱导其向单核细胞的分化中表现出相对较高的转录活性和显着活性,从而证明其可用作抗癌剂并用于治疗皮肤病如牛皮癣和皮肤病例如皱纹,皮肤松弛,皮肤干燥和皮脂分泌不足。与天然激素lα,25-dihydroxyvitamin D3相比,此化合物还显示出较低的体内对骨钙动员的体内活性和类似的体内肠道钙运输活性,因此可以用于治疗自身免疫性疾病或人类的炎症性疾病,以及肾性骨营养不良。该化合物也可用于治疗或预防肥胖。

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