发明名称 |
(20R) and (20S)-24-(<i>p</i>-toluenesulfonyloxy)-25,26,27-trinorvitamin D<sub>3 </sub>analogs and their uses |
摘要 |
This invention discloses (20R) and (20S)-24-(p-toluenesulfonyloxy)-25,26,27-trinorvitamin D3 analogs, and especially (20R)-25,26,27-trinor-24-(p-methylphenylsulfonate)-vitamin D3, its biological activities, and pharmaceutical uses therefor. This compound exhibits relatively little calcemic activity and does not promote cellular differentiation of HL-60 leukemia cells, but rather kills the cells. This cell death activity is found in small cell lung carcinoma also, but not in prostate, bone or ovarian cancer cells. This compound thus causes specific cell death in the absence of changes in calcium levels and without general toxicity in an animal. Therefore it might serve as a useful therapy for treatment of some forms of cancer, such as leukemia and lung cancer. |
申请公布号 |
US9290447(B2) |
申请公布日期 |
2016.03.22 |
申请号 |
US201213451317 |
申请日期 |
2012.04.19 |
申请人 |
Wisconsin Alumni Research Foundation |
发明人 |
DeLuca Hector F.;Clagett-Dame Margaret;Plum Lori A.;Barycki Rafal |
分类号 |
A61K31/593;C07C401/00 |
主分类号 |
A61K31/593 |
代理机构 |
Andrus Intellectual Property Law, LLP |
代理人 |
Andrus Intellectual Property Law, LLP |
主权项 |
1. A compound of the structure:where X is selected from the group consisting of hydrogen and a hydroxy-protecting group. |
地址 |
Madison WI US |