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2-METHYLENE-19,26-DINOR-(20R,22E,25R)-VITAMIN D ANALOGS

机译:2-亚甲基-19,26-异或-(20R,22E,25R)-维生素D模拟

摘要

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.
机译:本发明公开了2-亚甲基-19,26-dinor-(20R,22E,25R)-维生素D类似物,特别是2-亚甲基-19,26-dinor-(20R,22E,25R)-1α,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转录活性以及显着活性,从而证明其可用作抗癌剂并用于治疗皮肤病,例如牛皮癣和皮肤病,例如皱纹,皮肤松弛,皮肤干燥和皮脂分泌不足。与天然激素1α,25-二羟基维生素D3相比,该化合物在体内对骨钙动员的活性也非常低,并且在肠道中的钙运输活性也较高,因此可用于治疗人类以及肾脏的自身免疫性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。

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