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    • 5. 发明申请
    • A METHOD OF EXTENDING THE DOSE RANGE OF VITAMIN D COMPOUNDS
    • 一种延长维生素D化合物剂量范围的方法
    • WO2009026265A1
    • 2009-02-26
    • PCT/US2008/073535
    • 2008-08-19
    • WISCONSIN ALUMNI RESEARCH FOUNDATIONDELUCA, Hector, F.PIKE, John, W.SHEVDE, NirupamaPLUM, Lori, A.CLAGETT-DAME, Margaret
    • DELUCA, Hector, F.PIKE, John, W.SHEVDE, NirupamaPLUM, Lori, A.CLAGETT-DAME, Margaret
    • A61K31/00A61K31/59A61K31/593A61K31/663A61K45/06A61P19/08A61P19/10A61P5/18
    • A61K45/06A61K31/565A61K31/593A61K2300/00
    • Inhibitors of bone calcium resorption are administered, and calcium intake in the subject's diet is restricted, to allow high doses of vitamin D compounds or mimetics to be given with the intent of treating diseases such as metabolic bone diseases, hyperparathyroidism, cancer, psoriasis, and autoimmune diseases without the dangers of calcification of kidney, heart, and aorta. Inhibitors of bone calcium resorption include the bis-phosphonates, OPG (osteoprotegerin) or the soluble RANKL (receptor activator of NF-κB ligand) receptor known as sRANK (soluble RANK which is the protein expressed by the NF-κB gene), and function to block the availability of calcium from bone thereby preventing hypercalcemia and the resulting calcification of soft tissues. Thus, high doses of lα,25-dihydroxyvitamin D3 (1,25-(OH)2D3), its analogs, prodrugs, or mimetics can be utilized to treat the target disease with minimal risk to a patient. Specifically, alendronate is shown to block the bone calcium mobilization activity of both 1,25-(OH)2D3 and its very potent analog, 2-methylene-19-nor-(20S)-lα,25-dihydroxyvitamin D3, as long as the subject being treated is on a low calcium diet.
    • 施用骨钙吸收的抑制剂,受限饮食中的钙摄入受到限制,以允许给予高剂量的维生素D化合物或模拟物,其目的是治疗诸如代谢性骨疾病,甲状旁腺功能亢进,癌症,牛皮癣和 自身免疫性疾病,无肾脏,心脏和主动脉钙化的危险。 骨钙吸收抑制剂包括称为sRANK的双膦酸盐,OPG(骨保护素)或可溶性RANKL(NF-βB配体受体活化剂)受体(可溶性RANK,其是由NF-κB基因表达的蛋白质), 并且具有阻止骨从钙的可用性的作用,从而防止高钙血症和由此产生的软组织钙化。 因此,可以利用高剂量的la,25-二羟基维生素D3(1,25-(OH)2D3),其类似物,前药或模拟物来以最小的风险对患者进行目标疾病的治疗。 具体来说,阿仑膦酸被证明阻止1,25-(OH)2D3及其非常有效的类似物,2-亚甲基-19-去甲(20S)-la,25-二羟基维生素D 3的骨钙动员活性,只要 被治疗的对象是低钙饮食。