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    • 1. 发明申请
    • COMPOSITIONS AND METHODS FOR TREATING OSTEOPORESIS
    • 组合物和方法治疗骨质疏松症
    • WO2017214579A1
    • 2017-12-14
    • PCT/US2017/036876
    • 2017-06-09
    • THE REGENTS OF THE UNIVERSITY OF CALIFORNIA
    • PILZ, RenateBOSS, GerardKALYANARAMAN, Hema
    • A61K31/409A61K31/555A61P19/08C07D487/22
    • A61K31/555A61P19/08
    • In alternative embodiments, provided are compounds, including formulations and pharmaceutical compositions, and methods of making and using them, for treating, ameliorating, preventing or reversing osteoporesis, including post-menopausal osteoporosis. In alternative embodiments, provided are methods for, and uses of nitrosyl-cobinamide (NO-Cbi) for: treating, ameliorating, preventing or reversing osteoporosis; preventing bone loss due to estrogen deficiency; inhibiting osteoclast differentiation; reducing osteoclast numbers; preventing estrogen deficiency-induced osteocyte apoptosis; increasing serum cGMP concentration; increasing bone formation or bone mass, or increasing trabecular bone volume, trabecular number, and trabecular bone mineral density; increasing osteoblast numbers or regulating osteoblastic gene expression, comprising administering a nitrosyl-cobinamide (NO-Cbi), or a bioisostere, stereoisomer, tautomer, hydrate, solvate or pharmaceutically acceptable salt thereof to: an individual; an individual with osteoporosis or at risk of developing osteoporosis.
    • 在备选的实施方案中,提供了包括制剂和药物组合物,以及制备和使用它们的化合物,用于治疗,改善,预防或逆转骨质疏松症,包括绝经后骨质疏松症。 在替代实施方案中,提供了用于治疗,改善,预防或逆转骨质疏松症的亚硝酰 - 甲酰胺(NO-Cbi)的方法和用途; 防止雌激素缺乏导致的骨质流失; 抑制破骨细胞分化; 减少破骨细胞数量; 预防雌激素缺乏诱导的骨细胞凋亡; 增加血清cGMP浓度; 增加骨形成或骨质量,或增加小梁骨量,小梁数量和小梁骨矿物质密度; 增加成骨细胞数量或调节成骨细胞基因表达,所述方法包括向个体施用亚硝酰基 - 甲酰胺(NO-Cbi)或其生物电子等排体,立体异构体,互变异构体,水合物,溶剂化物或药学上可接受的盐; 一名患有骨质疏松症或有发生骨质疏松症风险的人。