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公开(公告)号：EP2280987B1
公开(公告)日：2018-05-23
申请号：EP09731210.2
申请日：2009-04-08
发明人： GIN, David , ADAMS, Michelle , DENG, Kai , PERL, Nicholas , WON, Annie , LIVINGSTON, Philip , RAGUPATHI, Govind
IPC分类号： C07H15/24 , A61K31/704 , A61P37/04
CPC分类号： C07H15/256 , A61K31/7024 , A61K31/704 , A61K39/385 , C07H13/08 , C07H15/24
摘要： The present invention relates to triterpene glycoside saponin-derived adjuvants, syntheses thereof, intermediates thereto, and uses thereof. QS-7 is a potent immuno-adjuvant that is significantly less toxic than QS-21, a related saponin that is currently the favored adjuvant in anticancer and antiviral vaccines. Tedious isolation and purification protocols have hindered the clinical development of QS-7. A novel semi-synthetic method is provided wherein a hydrolyzed prosapogenin mixture is used to synthesize QS-7, QS-21, and related analogs, greatly facilitating access to QS-7 and QS-21 analogs for preclinical and clinical evaluation.
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公开(公告)号：EP2315771A2
公开(公告)日：2011-05-04
申请号：EP09795292.3
申请日：2009-07-13
发明人： DANISHEFSKY, Samuel , ZHU, Jianglong , WAN, Qian , JEON, Insik , KIM, Wooham , NAGORNY, Pavel , LEE, Dongjoo , LIVINGSTON, Philip , RAGUPATHI, Govind
CPC分类号： C07K9/001 , A61K38/00 , A61K39/0011 , A61K2039/6081 , A61K2039/6093 , C07K9/006
摘要： Glycopeptide conjugates, and methods of making and using such conjugates are disclosed. Certain glycopeptide conjugates comprise tumor associated carbohydrate antigens and peptide epitopes. Certain glycopeptide conjugates comprise cyclic peptide scaffolds that display carbohydrate antigens in a clustered fashion. The immunogenicity of select glycopeptide conjugates is demonstrated.
摘要翻译： 公开了糖肽缀合物，以及制备和使用这种缀合物的方法。 某些糖肽缀合物包含肿瘤相关的碳水化合物抗原和肽表位。 某些糖肽缀合物包含以成簇方式展示碳水化合物抗原的环肽支架。 证明了选择的糖肽缀合物的免疫原性。
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公开(公告)号：EP3357931B1
公开(公告)日：2020-07-22
申请号：EP18161023.9
申请日：2009-04-08
发明人： GIN, David , ADAMS, Michelle , DENG, Kai , PERL, Nicholas , WON, Annie , RAGUPATHI, Govind , LIVINGSTON, Philip
IPC分类号： C07H15/256 , C07H1/00
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公开(公告)号：EP2280987A2
公开(公告)日：2011-02-09
申请号：EP09731210.2
申请日：2009-04-08
发明人： GIN, David , ADAMS, Michelle , DENG, Kai , PERL, Nicholas , WON, Annie , LIVINGSTON, Philip , RAGUPATHI, Govind
IPC分类号： C07H15/24 , A61K31/704 , A61P37/04
CPC分类号： C07H15/256 , A61K31/7024 , A61K31/704 , A61K39/385 , C07H13/08 , C07H15/24
摘要： The present invention relates to triterpene glycoside saponin-derived adjuvants, syntheses thereof, intermediates thereto, and uses thereof. QS-7 is a potent immuno-adjuvant that is significantly less toxic than QS-21, a related saponin that is currently the favored adjuvant in anticancer and antiviral vaccines. Tedious isolation and purification protocols have hindered the clinical development of QS-7. A novel semi-synthetic method is provided wherein a hydrolyzed prosapogenin mixture is used to synthesize QS-7, QS-21, and related analogs, greatly facilitating access to QS-7 and QS-21 analogs for preclinical and clinical evaluation.
摘要翻译： 本发明涉及三萜糖苷皂苷衍生的佐剂，其合成，其中间体及其用途。 QS-7是一种有效的免疫佐剂，其毒性明显低于QS-21，这是目前抗癌和抗病毒疫苗中有利的佐剂的相关皂苷。 繁琐的分离和纯化方案阻碍了QS-7的临床发展。 提供了一种新的半合成方法，其中使用水解的前配合物混合物合成QS-7，QS-21及相关类似物，极大地方便了QS-7和QS-21类似物的临床前和临床评估。
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公开(公告)号：EP3868771A1
公开(公告)日：2021-08-25
申请号：EP20186996.3
申请日：2009-04-08
发明人： GIN, David , ADAMS, Michelle , DENG, Kai , PERL, Nicholas , RAGUPATHI, Govind , LIVINGSTON, Philip , WON, Annie
IPC分类号： C07H13/08 , A61K31/7024 , A61P37/04
摘要： The present invention relates to triterpene glycoside saponin-derived adjuvants, syntheses thereof, intermediates thereto, and uses thereof. QS-7 is a potent immuno-adjuvant that is significantly less toxic than QS-21, a related saponin that is currently the favored adjuvant in anticancer and antiviral vaccines. Tedious isolation and purification protocols have hindered the clinical development of QS-7. A novel semi-synthetic method is provided wherein a hydrolyzed prosapogenin mixture is used to synthesize QS-7, QS-21, and related analogs, greatly facilitating access to QS-7 and QS-21 analogs for preclinical and clinical evaluation.
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公开(公告)号：EP0951484A2
公开(公告)日：1999-10-27
申请号：EP98908437.0
申请日：1998-01-13
发明人： DANISHEFSKY, Samuel, J. , DESHPANDE, Prashant, P. , KIM, In J. , LIVINGSTON, Philip , HYUN, Jim, Kim , RAGUPATHI, Govindaswami , PARK, Tae, Kyo
CPC分类号： C07H15/10 , A61K47/643 , A61K47/646
摘要： The present invention provides processes for the preparation of the KH-1 and N3 antigens, as well as related analogues thereof, which are useful as anticancer therapeutics. The present invention also provides various intermediates useful in the preparation of KH-1 and N3 and analogues thereof. Additionally, the invention provides various compositions comprising any of the analogues of KH-1 and N3 available through the methods of the invention and pharmaceutical carriers useful in the treatment of subjects suffering from various forms of epithelial cancer.
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