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公开(公告)号：US11512107B2
公开(公告)日：2022-11-29
申请号：US17191281
申请日：2021-03-03
发明人： Glenn C. Micalizio
摘要： The present disclosure relates to stereodefined polycyclic (e.g., tetracyclic) compounds that contain quaternary centers at one or multiple ring fusions, synthetic methods for preparing such compounds, and methods of using such compounds to treat a disease, such as a brain tumor and, particularly, a glioma.
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公开(公告)号：US20230018615A1
公开(公告)日：2023-01-19
申请号：US17818873
申请日：2022-08-10
发明人： Glenn C. Micalizio
摘要： Methods for producing enantiodefined polycyclic compounds, particularly tetracyclic compounds, are provided. More particularly, synthetic methods for producing biologically active enantiodefined steroidal compositions of both natural (“nat-”) and unnatural (“ent-”) absolute stereochemistry are provided. An exemplary method for manufacturing a tetracyclic compound comprises a step of forming a hydrindane intermediate through coupling of a suitably functionalized enyne with a suitably functionalized alkyne and subsequently performing an intramolecular ring-closing reaction to form the tetracyclic compound. Steroidal compounds obtained by this method and methods of using such steroidal compounds in human and/or animal therapeutics and medicines are also provided.
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公开(公告)号：US20210188898A1
公开(公告)日：2021-06-24
申请号：US17191281
申请日：2021-03-03
发明人： Glenn C. Micalizio
摘要： The present disclosure relates to stereodefined polycyclic (e.g., tetracyclic) compounds that contain quaternary centers at one or multiple ring fusions, synthetic methods for preparing such compounds, and methods of using such compounds to treat a disease, such as a brain tumor and, particularly, a glioma.
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公开(公告)号：US11459353B2
公开(公告)日：2022-10-04
申请号：US16637675
申请日：2018-08-16
发明人： Glenn C. Micalizio
摘要： Methods for producing enantiodefined polycyclic compounds, particularly tetracyclic compounds, are provided. More particularly, synthetic methods for producing biologically active enantiodefined steroidal compositions of both natural (“nat-”) and unnatural (“ent-”) absolute stereochemistry are provided. An exemplary method for manufacturing a tetracyclic compound comprises a step of forming a hydrindane intermediate through coupling of a suitably functionalized enyne with a suitably functionalized alkyne and subsequently performing an intramolecular ring-closing reaction to form the tetracyclic compound. Steroidal compounds obtained by this method and methods of using such steroidal compounds in human and/or animal therapeutics and medicines are also provided.
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公开(公告)号：US20210323998A1
公开(公告)日：2021-10-21
申请号：US17272091
申请日：2019-09-05
发明人： Glenn C. Micalizio , Arti B. Gaur
摘要： The present disclosure relates to stereodefined polycyclic (e.g., tetracyclic) compounds that contain quaternary centers at one or multiple ring fusions, synthetic methods for preparing such compounds, and methods of using such compounds to treat a disease, such as a brain tumor and, particularly, a glioma.
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