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2-methylene-(17Z)-17(20)-dehydro-19,21-dinor-vitamin D analogs

机译:2-亚甲基-(17Z)-17(20)-脱氢-19,21-二价维生素D类似物

摘要

This invention discloses 2-methylene-(17Z)-17(20)-dehydro-19,21-dinor-vitamin D analogs, and specifically 2-methylene-(17Z)-17(20)-dehydro-19,21-dinor-1, 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 has significant calcemic activity in vivo having about the same bone calcium mobilization activity and intestinal calcium transport activity as the native hormone 1,25-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-(17Z)-17(20)-脱氢-19,21-二价维生素D类似物,特别是2-亚甲基-(17Z)-17(20)-脱氢-19,21-二价维生素D类似物。 -1、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。该化合物在体内还具有显着的钙化活性,其骨钙动员活性和肠内钙运输活性与天然激素1,25-二羟基维生素D3大致相同,因此可用于治疗人类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。

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