Bayer Schering Pharma, Medicinal Chemistry, Muellerstrasse 178, 13353 Berlin, Germany.
Expert Opin Ther Pat. 2009 Nov;19(11):1521-34. doi: 10.1517/13543770903312946.
Progesterone receptor agonists are used in female contraception, hormone replacement therapy or some gynecological conditions like endometriosis. The interest for antagonists or selective progesterone receptor modulators (SPRMs) is growing. Recent reports on this class of compounds indicate that they could become the next generation of therapeutics in gynecological treatments.
This overview summarizes the work on progesterone receptor agonists, SPRMs and antagonists reported in the patent literature in the past 4 years.
The focus of the article is the examination of patents, primarily published as WO, EU or US patents since 2005. In some cases, additional data from the public literature is included into the discussion. These data are of substantial interest as the available biological data disclosed in patents are usually limited for new compound classes.
RESULTS/CONCLUSION: Some highly active clusters of compounds have been disclosed in the past 4 years. The current research seems to focus on SPRMs and progesterone receptor antagonists.
孕激素受体激动剂被用于女性避孕、激素替代疗法或某些妇科疾病，如子宫内膜异位症。人们对拮抗剂或选择性孕激素受体调节剂（SPRMs）的兴趣日益浓厚。最近关于这类化合物的报告表明，它们可能成为妇科治疗的下一代治疗药物。
本文概述了过去 4 年专利文献中关于孕激素受体激动剂、SPRMs 和拮抗剂的研究工作。
本文的重点是检查专利，主要是 2005 年以后公布的 WO、EU 或美国专利。在某些情况下，还将来自公共文献的其他数据纳入讨论。这些数据非常重要，因为专利中披露的可用生物数据通常对新化合物类别有限。
结果/结论：过去 4 年中已经披露了一些高活性的化合物簇。目前的研究似乎集中在 SPRMs 和孕激素受体拮抗剂上。
