专利号:WO-2024146880-A1 优先权日:2023-01-03 标题:Fluoro-oxysterols positron emission tomography (pet) radiotracers 发明人:POIROT MARC; COURBON FRÉDÉRIC; SAMADI MOHAMMAD; DE MEDINA PHILIPPE; SILVENTE POIROT SANDRINE; BRILLOUET SÉVERINE 权利人:INST NAT SANTE RECH MED; CENTRE NAT RECH SCIENT; UNIV TOULOUSE III – PAUL SABATIER; INST CLAUDIUS REGAUD; CT HOSPITALIER UNIVERSITAIRE TOULOUSE; UNIV DE LORRAINE 摘要:Radiopharmaceuticals-based biomedical imaging plays a growing role in cancer management, including diagnosis, tumor staging and aggressiveness and treatment monitoring. Even though 18Fluoro-2-deoxy glucose and 18Fluoroestradiol are currently used for some types of breast cancer, a need remains to develop other candidate compounds which are useful as radiotracers in a different/ broader range of cancer types. Thus, it is described a family of 18F radiolabeled compounds of formula (I) (wherein one of R2, R4, R5, R6, R7 and R12 is 18F) for use as Positron Emission Tomography imaging agents for the detection of cancers and metastatic sites thereof, as well as for monitoring and predicting the efficacy of a cancer treatment, wherein the cancer is associated to cholesterol-5,6- epoxide hydrolase and/or lip-hydroxy steroid dehydrogenase type (2) overexpression. To overcome the issues linked to the lifetime of the radioisotope 18F and, to ensure an effective synthesis of the 18F radiolabeled compounds of formula (I), a group of novel intermediate compounds in the synthesis thereof is also described.
专利号:WO-2010071772-A2 优先权日:2008-12-15 标题:Synthesis of 3b-amino-5-cholestene and related 3b-halides involving i-steroid and retro-i-steroid rearrangements
专利号:US-8889840-B2 优先权日:2009-10-29 标题 :Vascular leakage inhibitor 发明人:KWON YOUNG-GUEN; SUH YOUNG-GER 权利人:KWON YOUNG-GUEN; SUH YOUNG-GER; UNIV YONSEI IACF 摘要:The present disclosure relates to a novel vascular leakage inhibitor. The novel vascular leakage inhibitor of the present disclosure inhibits the apoptosis of vascular endothelial cells, inhibits the formation of actin stress fibers induced by VEGF, enhances the cortical actin ring structure, and improves the stability of the tight junctions (TJs) between vascular cells, thereby inhibiting vascular leakage. The vascular leakage inhibitor of the present disclosure has the activity of not only reducing vascular permeability but also recovering the integrity of damaged blood vessels. Accordingly, the vascular leakage inhibitor of the present disclosure can prevent or treat various diseases caused by vascular leakage. Since the vascular leakage inhibitor of the present disclosure is synthesized from commercially available or easily synthesizable cholesterols, it has remarkably superior feasibility of commercial synthesis.
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合成参考文献
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