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公开(公告)号：US5677285A
公开(公告)日：1997-10-14
申请号：US379602
申请日：1995-04-26
申请人： Aurelio Romeo , Gunter Kirschner , Hari Manev , Martino Trimarco , Gino Toffano
发明人： Aurelio Romeo , Gunter Kirschner , Hari Manev , Martino Trimarco , Gino Toffano
摘要： Provided are new derivatives of neuraminic acid of formula (I), where Ac represents an acyl residue of an aliphatic, araliphatic, aromatic, alicyclic, or heterocyclic carboxylic acid, including carboxylic amides, their 2-hydrocarbyl-glycosides, and their peracylated derivatives at the hydroxy groups of both these series of amides. These compositions are therapeutically useful in providing a protective effect against the neurotoxicity induced by excitatory amino acids, and can therefore be used in therapies of the central nervous system. ##STR1##
摘要翻译： PCT No.PCT / US93 / 07307 Sec。 371日期1995年04月26日 102（e）日期1995年4月26日PCT提交1993年8月3日PCT公布。 出版物WO94 / 03469 日期1994年2月17日提供了式（I）的神经氨酸的新衍生物，其中Ac表示脂族，芳脂族，芳族，脂环族或杂环羧酸的酰基残基，包括羧酰胺，它们的2-烃基 - 苷， 以及它们在这两系列酰胺的羟基上的过酰基化衍生物。 这些组合物在治疗上可用于提供针对由兴奋性氨基酸诱导的神经毒性的保护作用，因此可用于中枢神经系统的治疗。
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公开(公告)号：US5470949A
公开(公告)日：1995-11-28
申请号：US990960
申请日：1992-12-15
申请人： Robin L. Polt
发明人： Robin L. Polt
CPC分类号： C07K9/001 , C07K1/006 , C07K5/0606 , C07K5/06078 , C07K9/00 , A61K38/00
摘要： A compound of the formula ##STR1## is disclosed. X is selected from the group consisting of aryl, alkyl, imidate ester, imino ester, amidine, azide, isocyanate, and dithiocarbonate. R' is a group selected from the group consisting of groups containing a hydroxyl moiety, groups containing a protected hydroxyl moiety, and groups containing an O-linked sugar. G is a carbon chain of 0-10 carbons and R is not a methyl group and is a group capable of removal under conditions compatible with glycopeptide synthesis. In a preferred form the compound, R is selected from the group consisting of benzylic or allyl groups and X is CPh.sub.2. A method of forming a glycocide from the compound is also disclosed.
摘要翻译： 公开了式（IMAGE）的化合物。 X选自芳基，烷基，亚氨酸酯，亚氨基酯，脒，叠氮化物，异氰酸酯和二硫代碳酸酯。 R'是选自含有羟基部分的基团，含有被保护的羟基部分的基团和含有O-连接的糖的基团的基团。 G是0-10个碳的碳链，R不是甲基，是能够与糖肽合成相容的条件下能除去的基团。 在优选形式的化合物中，R选自苄基或烯丙基，X是CPh2。 还公开了从化合物形成糖基化的方法。
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43.发明授权
公开(公告)号：US4892939A
公开(公告)日：1990-01-09
申请号：US148507
申请日：1988-01-29
申请人： Katsumi Sakai , Kiyoaki Chou , Takeshi Endo
发明人： Katsumi Sakai , Kiyoaki Chou , Takeshi Endo
摘要： New 5-fluorouridine compounds of the general formula: ##STR1## wherein n is an integer of 1 to 3, R' stands for a straight or branched chain alkyl group having 1 to 4 carbon atoms or a benzyl group, and R stands for an amino acid residue selected from the group consisting of alanyl, phenylalanyl, valyl, tyrosyl, 3,4-dihydroxyphenylalanyl and lysyl groups. These compounds possess excellent anti-malignant tumor, anti-viral and immunosuppressive activities.
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公开(公告)号：US12116423B2
公开(公告)日：2024-10-15
申请号：US17461115
申请日：2021-08-30
发明人： Meredith Hay , John Konhilas , Robin L. Polt , Evan Jones , Lajos Szabo
摘要： The present invention provides oligopeptides, in particular, Ang-(1-7) derivatives, and methods for using and producing the same. In one particular embodiment, oligopeptides of the invention have higher blood-brain barrier penetration and/or in vivo half-life compared to the native Ang-(1-7), thereby allowing oligopeptides of the invention to be used in a wide variety of clinical applications including in treatment of cognitive dysfunction and/of impairment.
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公开(公告)号：US20230374076A1
公开(公告)日：2023-11-23
申请号：US18363810
申请日：2023-08-02
申请人： KODE BIOTECH LIMITED
CPC分类号： C07K9/001 , A61K47/545 , A61K47/64 , A61K47/549 , C07K1/1077 , C07K19/00
摘要： The preparation of water dispersible ceramide conjugates and derivatives of sphingolipid analogues is described. The conjugates and analogues are prepared by reacting a succinimidyl carbonate of a β-Ala derivative with the primary amine of a functionalised spacer. Despite their dispersibility in water, the ceramide conjugates and derivatives of sphingolipid analogues spontaneously incorporate in to the plasma membranes of cells.
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公开(公告)号：US11760779B2
公开(公告)日：2023-09-19
申请号：US15734100
申请日：2018-06-04
CPC分类号： C07K9/001 , A61K47/545 , A61K47/549 , A61K47/64 , C07K1/1077 , C07K19/00
摘要： The preparation of water dispersible ceramide conjugates and derivatives of sphingolipid analogues is described. The conjugates and analogues are prepared by reacting a succinimidyl carbonate of a β-Ala derivative with the primary amine of a functionalised spacer. Despite their dispersibility in water, the ceramide conjugates and derivatives of sphingolipid analogues spontaneously incorporate into the plasma membranes of cells.
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公开(公告)号：US20180000929A1
公开(公告)日：2018-01-04
申请号：US15704977
申请日：2017-09-14
发明人： Carolyn R. Bertozzi , Mary Sloan Siegrist Palmore , John C. Jewett , Chelsea G. Gordon , Peyton Shieh
IPC分类号： A61K39/385 , A61K47/64 , C12Q1/18 , C12N1/20 , C07K14/47 , C07K9/00 , C07K14/195 , C12Q1/02 , A61K39/00
CPC分类号： A61K39/385 , A61K47/64 , A61K47/646 , A61K2039/6068 , C07K9/00 , C07K9/001 , C07K14/195 , C07K14/4725 , C12N1/20 , C12Q1/025 , C12Q1/18 , G01N2333/195
摘要： The present disclosure provides modified bacteria and modified peptidoglycan comprising modified D-amino acids; compositions comprising the modified bacteria or peptidoglycan; and methods of using the modified bacteria or peptidoglycan. The modified D-amino acids include a bioorthogonal functional group such as an azide, an alkyne or a norbornene group. Also provided are modified peptidoglycans conjugated to a molecule of interest via a linker.
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公开(公告)号：US20170283466A1
公开(公告)日：2017-10-05
申请号：US15444547
申请日：2017-02-28
发明人： Sylvie Bay , Claude Leclerc , Richard Lo-Man
CPC分类号： C07K9/00 , A61K47/55 , A61K47/645 , C07K9/001 , C07K14/70539
摘要： The present invention relates to a method for preparing carbohydrate T cell epitope conjugates of formula (I): M(T-B)n (I) wherein M, T, B and n ore as defined in claim 1.
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49.发明申请公开(公告)号：US20170216460A1
公开(公告)日：2017-08-03
申请号：US15169493
申请日：2016-05-31
发明人： Kwangmeyung KIM , Ju Hee RYU , Ick Chan KWON , Man Kyu SHIM , Hong Yeol YOON
IPC分类号： A61K49/00 , G01N33/58 , G01N33/574 , C07K9/00
CPC分类号： A61K49/0056 , A61K47/555 , A61K49/0032 , A61K49/0052 , C07K5/1016 , C07K5/1019 , C07K9/001 , G01N33/57496 , G01N33/581 , G01N2333/96466
摘要： The present disclosure relates to a glycopeptide targeting cancer cells and a contrast agent kit containing the same. The glycopeptide is one wherein an azide reporting monosaccharide is bound to a substrate peptide. As the substrate peptide is specifically cleaved by cathepsin B in cancer cells, an azide reporting monosaccharide is expressed onto the cell surface via metabolic glycoengineering, thereby providing a target for action as a contrast agent. Accordingly, because the azide is exposed to the cell surface only by cathepsin B, as it is specifically expressed in cancer cells, in particular in metastatic cancer cells, while it is limitedly expressed in normal cells and is hardly excreted out the cells, the cancer cells can be selectively imaged by an azide-specific contrast agent.
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公开(公告)号：US20160244495A1
公开(公告)日：2016-08-25
申请号：US15078885
申请日：2016-03-23
CPC分类号： C07K14/4725 , A61K38/00 , A61L27/227 , A61L27/24 , A61L27/3804 , A61L27/54 , A61L2300/25 , A61L2300/42 , C07K9/00 , C07K9/001 , C07K14/00 , C07K14/78
摘要： This invention relates to collagen-binding synthetic peptidoglycans and engineered collagen matrices comprising a collagen matrix and a collagen-binding synthetic peptidoglycan where the collagen-binding synthetic peptidoglycan can be aberrant or can have amino acid homology with a portion of the amino acid sequence of a protein or a proteoglycan that regulates collagen fibrillogenesis. The invention also relates to kits, compounds, compositions, and engineered graft constructs comprising such collagen-binding synthetic peptidoglycans or engineered collagen matrices and methods for their preparation and use.
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