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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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3.发明授权Use of multivalent synthetic ligands of surface nucleolin for treating cancer or inflammation 有权使用表面核仁素的多价合成配体治疗癌症或炎症公开(公告)号：US08497349B2
公开(公告)日：2013-07-30
申请号：US12298511
申请日：2007-04-22
CPC分类号： C07K14/4705 , A61K38/00 , A61K38/02 , A61K38/16 , C07K14/47
摘要： A method for treating disorders involving deregulation of cell proliferation and/or angiogenesis comprising the administration of an effective amount of a multivalent synthetic compound comprising a support on which at least 3 pseudopeptide units are grafted, said compound being of formula (I).
摘要翻译： 一种用于治疗涉及细胞增殖和/或血管生成失调的病症的方法，包括施用有效量的多价合成化合物，所述多价合成化合物包含其上至少3个假肽单元被接枝的载体，所述化合物为式（I）。
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4.发明申请USE OF MULTIVALENT SYNTHETIC LIGANDS OF SURFACE NUCLEOLIN FOR TREATING CANCER OR INFLAMMATION 有权用于治疗癌症或炎症的表面核素的多种合成配体的使用公开(公告)号：US20110065649A1
公开(公告)日：2011-03-17
申请号：US12298511
申请日：2007-04-22
IPC分类号： A61K38/16 , A61K38/08 , C07K7/06 , A61K38/12 , C07K7/64 , A61K38/10 , C07K7/08 , C07K14/00 , A61P35/00 , A61P29/00 , A61P37/06 , A61P17/00 , G01N33/53
CPC分类号： C07K14/4705 , A61K38/00 , A61K38/02 , A61K38/16 , C07K14/47
摘要： A method for treating disorders involving deregulation of cell proliferation and/or angiogenesis comprising the administration of an effective amount of a multivalent synthetic compound comprising a support on which at least 3 pseudopeptide units are grafted, said compound being of formula (I).
摘要翻译： 一种用于治疗涉及细胞增殖和/或血管生成失调的病症的方法，包括施用有效量的多价合成化合物，所述多价合成化合物包含其上至少3个假肽单元被接枝的载体，所述化合物为式（I）。
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5.发明申请Novel synthetic peptide vaccines for HIV: the CBD epitope as an effective immunogen to elicit broadly neutralizing antibodies against HIV 有权用于HIV的新型合成肽疫苗：CBD表位作为有效的免疫原，以引发广泛中和抗HIV的抗体公开(公告)号：US20100247618A1
公开(公告)日：2010-09-30
申请号：US12073887
申请日：2008-03-11
申请人： Ara Hovanessian , Jean Paul Briand , Sylviane Muller , Bernard Krust , Josette Svab , Elias Said
发明人： Ara Hovanessian , Jean Paul Briand , Sylviane Muller , Bernard Krust , Josette Svab , Elias Said
IPC分类号： A61K9/127 , A61K38/08 , A61K38/10 , A61K38/16 , A61K38/14 , A61K38/12 , C07K7/06 , A61K39/00 , C07K7/08 , C07K14/00 , C07H21/04 , C07K14/435 , A61P31/18 , C12Q1/70 , G01N33/68 , C07K16/00
CPC分类号： C07K14/005 , A61K39/12 , A61K39/21 , A61K2039/505 , A61K2039/545 , A61K2039/55566 , C07K16/1063 , C07K2317/21 , C12N2740/16122 , C12N2740/16134 , G01N33/56988
摘要： The present invention relates to peptides, referred to as CBD-1, CBD-2, CBM-1/TH-1, CBM-1/TH-2, CBM-2/TH-1, CBM-2/TH-2 and C-20 peptides, which are antigenic and elicit protective immune response against HIV infection. Compositions, pharmaceutical compositions and vaccines comprising these antigenic peptides are also encompassed by the present invention, as well as neutralizing antibodies which inhibit infection of primary CD4+ T lymphocytes by various HIV isolates. Methods for diagnosis of HIV are also disclosed.
摘要翻译： 本发明涉及称为CBD-1，CBD-2，CBM-1 / TH-1，CBM-1 / TH-2，CBM-2 / TH-1，CBM-2 / TH-2和 C-20肽，其是抗原性的并且引起针对HIV感染的保护性免疫应答。 包含这些抗原肽的组合物，药物组合物和疫苗也包括在本发明中，以及中和抗体，其通过各种HIV分离物抑制原代CD4 + T淋巴细胞的感染。 还公开了用于诊断HIV的方法。
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