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公开(公告)号：US09243030B2
公开(公告)日：2016-01-26
申请号：US12993427
申请日：2008-05-22
申请人： Jean Paul Briand , Gilles Guichard , Jose Courty , Robert H. Zimmer , Chantal Devin , Annie Lang , Haixang Zhang , Ara Hovanessian
发明人： Jean Paul Briand , Gilles Guichard , Jose Courty , Robert H. Zimmer , Chantal Devin , Annie Lang , Haixang Zhang , Ara Hovanessian
CPC分类号： C07K5/06086 , A61K38/00 , C07K7/06
摘要： The present invention relates to new optically pure compounds displaying an improved anticancer activity compared to previously known complex mixtures of stereoisomers thereof. Such compounds are of formula (I): wherein each X independently represents any amino acid; n is 0 or 1; m is an integer between 0 and 3; k is an integer of at least 3; Psi is a reduced bond of formula replacing the peptide amide bond between Lys and Pro; and wherein Lys residues in pseudopeptide units of said compound of formula (I) are either all in L configuration or all in D configuration. A method for preparing such compounds, and therapeutic uses thereof are also provided. The synthetic method involves the selective reduction of the peptide bond between Lys and Pro in a dipeptide intermediate with borane. The therapeutic uses are against cancer, inflammation and for wound healing.
摘要翻译： 本发明涉及与先前已知的其立体异构体的复合混合物相比显示改善的抗癌活性的新的光学纯化合物。 这样的化合物具有式（I）：其中每个X独立地表示任何氨基酸; n为0或1; m是0和3之间的整数; k是至少3的整数; Psi是取代Lys和Pro之间的肽酰胺键的式的还原键; 并且其中所述式（I）化合物的假肽单元中的Lys残基全部为L构型或全部为D构型。 还提供了制备这些化合物的方法及其治疗用途。 合成方法包括用二硼化物中间体与硼烷选择性还原Lys和Pro之间的肽键。 治疗用途是针对癌症，炎症和伤口愈合。
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公开(公告)号：US20110201559A1
公开(公告)日：2011-08-18
申请号：US12993427
申请日：2008-05-22
申请人： Jean Paul Briand , Gilles Guichard , José Courty , Robert Zimmer , Chantal Devin , Annie Lang , Haixiang Zhang
发明人： Jean Paul Briand , Gilles Guichard , José Courty , Robert Zimmer , Chantal Devin , Annie Lang , Haixiang Zhang
CPC分类号： C07K5/06086 , A61K38/00 , C07K7/06
摘要： The present invention relates to new optically pure compounds displaying an improved anticancer activity compared to previously known complex mixtures of stereoisomers thereof. Such compounds are of formula (I): wherein each X independently represents any amino acid; n is 0 or 1; m is an integer between 0 and 3; k is an integer of at least 3; Psi is a reduced bond of formula replacing the peptide amide bond between Lys and Pro; and wherein Lys residues in pseudopeptide units of said compound of formula (I) are either all in L configuration or all in D configuration. A method for preparing such compounds, and therapeutic uses thereof are also provided. The synthetic method involves the selective reduction of the peptide bond between Lys and Pro in a dipeptide intermediate with borane. The therapeutic uses are against cancer, inflammation and for wound healing.
摘要翻译： 本发明涉及与先前已知的其立体异构体的复合混合物相比显示改善的抗癌活性的新的光学纯化合物。 这样的化合物具有式（I）：其中每个X独立地表示任何氨基酸; n为0或1; m是0和3之间的整数; k是至少3的整数; Psi是取代Lys和Pro之间的肽酰胺键的式的还原键; 并且其中所述式（I）化合物的假肽单元中的Lys残基全部为L构型或全部为D构型。 还提供了制备这些化合物的方法及其治疗用途。 合成方法包括用二硼化物中间体与硼烷选择性还原Lys和Pro之间的肽键。 治疗用途是针对癌症，炎症和伤口愈合。
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