[EN] 2-METHYLENE-20(21)-DEHYDRO-19,24,25,26,27,-PENTANOR-VITAMIN D ANALOGS<br/>[FR] ANALOGUES DE 2-MÉTHYLÈNE-20(21)-DÉSHYDRO-19,24,25,26,27-PENTANOR-VITAMINE D
申请人:WISCONSIN ALUMNI I RES FOUNDATION
公开号:WO2013012644A1
公开(公告)日:2013-01-24
This invention discloses 2-methylene-20(21)-dehydro-19,24,25,26, 27-pentanor-vitamin D analogs, and specifically 2-methylene-20(21)-dehydro-19,24,25,26,27-pentanor-1α-hydroxyvitamin 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 lower in vivo intestinal calcium transport activity as 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 secondary hyperparathyroidism and renal osteodystrophy. This compound may also be used for the treatment or prevention of obesity.
这项发明揭示了2-亚甲基-20(21)-去氢-19,24,25,26,27-五环-维生素D类似物,特别是2-亚甲基-20(21)-去氢-19,24,25,26,27-五环-1α-羟基维生素D3,以及其药用。该化合物显示出相对较高的转录活性,以及在阻止未分化细胞增殖和诱导它们分化成单核细胞方面的显著活性,因此表明可用作抗癌剂,用于治疗银屑病等皮肤疾病以及皱纹、松弛皮肤、干燥皮肤和皮脂分泌不足等皮肤状况。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和肠钙转运活性较低,因此可用于治疗人类的自身免疫性疾病或炎症性疾病,以及继发性甲状旁腺功能亢进和肾性骨营养不良。该化合物还可用于肥胖的治疗或预防。