Non-steroidal compounds for steroid receptors and uses relating thereto

The present invention relates to non-steroidal compounds which can bind to steroid receptors, and more particularly to compounds that can bind to both a steroid receptor and a radionuclide for either diagnostic or therapeutic purposes. Steroid receptor analogs having good binding affinity for steroi...

Ausführliche Beschreibung

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Bibliographische Detailangaben
Hauptverfasser: Kasina, Sudhakar, Gleave, D. Mark
Format: Patent
Sprache:eng
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Beschreibung
Zusammenfassung:The present invention relates to non-steroidal compounds which can bind to steroid receptors, and more particularly to compounds that can bind to both a steroid receptor and a radionuclide for either diagnostic or therapeutic purposes. Steroid receptor analogs having good binding affinity for steroid receptors and "binding arms" for chelation to metal species such as radionuclides are prepared with all carbon backbones. The analogs very closely approximate the geometries present in natural steroids which are important for effective binding to receptor sites. In addition, metal species binding arms are strategically incorporated into the analog structure in a manner that does not disrupt the analog's receptor binding efficacy. Furthermore, the metal species binding arms may be designed to chelate one or more radionuclides, including radionuclides effective in diagnostic or therapeutic applications. With incorporation of an appropriate steroid receptor binding group, these metal species-bound analogs may be used, for example, to bind androgen receptor sites in the diagnosis or treatment of prostate cancer, or estrogen receptor sites in the diagnosis or treatment of breast and ovarian cancers.