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公开(公告)号：US20090081192A1
公开(公告)日：2009-03-26
申请号：US11860488
申请日：2007-09-24
CPC分类号： G01N33/5064 , G01N33/5088 , G01N2400/50 , G01N2800/328
摘要： A method screens compounds out of the group consisting of proteins, peptides, peptidomimetics, antibodies and small organic molecules that increase the activity of the protein Rac1 by virtue of their binding to the extracellular portion of this protein. The method includes the steps of: contacting a confluent layer of cultured endothelial cells with at least one of test compounds, lysing the endothelial cells with a lysation buffer, and measuring the amount of Rac1 activity.
摘要翻译： 一种方法筛选由蛋白质，肽，肽模拟物，抗体和小有机分子组成的组，其通过与蛋白质的细胞外部分结合而增加蛋白Rac1的活性。 所述方法包括以下步骤：使培养的内皮细胞的汇合层与至少一种测试化合物，裂解内皮细胞与裂解缓冲液和测量Rac1活性的量接触。
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2.发明申请PEPTIDES AND DERIVATIVES THEREOF, THE MANUFACTURING THEREOF AS WELL AS THEIR USE FOR PREPARING A THERAPEUTICALLY AND/OR PREVENTIVELY ACTIVE PHARMACEUTICAL COMPOSITION 审中-公开其制备方法及其衍生物，其制备方法及其用于制备治疗性和/或预防性活性药物组合物的用途公开(公告)号：US20090286725A1
公开(公告)日：2009-11-19
申请号：US12121544
申请日：2008-05-15
摘要： Peptides and peptide derivatives of the following general Formula I: (SEQ ID NO: 15) (I) H2N-GHRPX1X2X3X4X5X6X7X8PX9X10X11PX12PPPX13X14X15 X16GYR-X17, wherein: X1-X16 denote one of the 20 genetically encoded amino acids, X17 denotes OR1, with R1=hydrogen or (C1-C10-alkyl), or NR2R3, R2 and R3 being identical or different and denoting hydrogen, (C1-C10)-alkyl, or a residue -PEG5-60K, wherein the PEG-residue is linked to the N atom via a spacer, or a residue NH—Y-Z-PEG5-60K, wherein Y denotes a chemical bond or a genetically coded amino acid from among the group of S, C, K or R, and Z denotes a spacer by way of which a polyethylene glycol (PEG)-residue may be linked, as well as the physiologically acceptable salts thereof, or wherein: X15 or X16 denotes an amino acid from the group of C or K, which is linked to a residue Z-PEG5-60K via the heteroatom in the side chain, and wherein X17 denotes OR1, with R1=hydrogen or (C1-C10-alkyl), or NR2R3, R2 and R3 being identical or different and denoting hydrogen or (C1-C10)-alkyl, as well as the physiologically acceptable salts thereof.
摘要翻译： 以下通式I的肽和肽衍生物：（SEQ ID NO：15）（I）H 2 N-GHRPX1X2X3X4X5X6X7X8PX9X10X11PX12PPPX13X14X15 X16GYR-X17，其中：X1-X16表示20个遗传编码氨基酸之一，X17表示OR1，R1 = 氢或（C 1 -C 10 - 烷基）或NR 2 R 3，R 2和R 3相同或不同并且表示氢，（C 1 -C 10） - 烷基或残基-PEG 5 - 60K，其中所述PEG-残基连接到N 或者残基NH-YZ-PEG5-60K，其中Y表示S，C，K或R组中的化学键或遗传编码氨基酸，Z表示间隔基，通过其间隔， 可以连接聚乙二醇（PEG）残基以及其生理上可接受的盐，或其中：X 15或X 16表示与C或K基团相连的氨基酸，其与残基Z-PEG5-60K连接 并且其中X17表示OR1，其中R1 =氢或（C1-C10-烷基）或NR2R3，R2和R3相同或不同，并且de 注意氢或（C1-C10） - 烷基，以及其生理学上可接受的盐。
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公开(公告)号：US20090286739A1
公开(公告)日：2009-11-19
申请号：US12121526
申请日：2008-05-15
摘要： Peptides, peptidomimetics and derivatives thereof of the following general formula I: (SEQ ID NO: 1) (I)H2N-GHRPX1X2X3-β-X4X5X6X7X8X9X10-X11, in which X1-X10 denote one of the 20 genetically coded amino acids, wherein X8, X9 and X10 individually or jointly may also denote a single chemical bond X11 denotes OR1 in which R1 equals hydrogen or (C1-C10)alkyl NR2R3 with R2 and R3 are equal or different and denote hydrogen, (C1-C10)alkyl or a residue —W-PEG5-60K, in which the PEG residue is attached via a suitable spacer W to the N-atom, or a residue NH—Y-Z-PEG5-60K, in which Y denotes a single chemical bond or a genetically coded amino acids from the group S, C, K or R and in which Z denotes a spacer, via which a polyethylene glycol (PEG)-residue can be attached, as well as their physiologically acceptable salts, and in which additionally β denotes an amino acid, whether genetically coded or not, or a peptidomimetic element, which have the additional property of inducing a bend or turn in the peptide backbone. Such amino acids include without limitation L-proline, D-proline, L-hydroxyproline, D-hydroxyproline, L-(O-benzyl)-hydroxyproline, D-(O-benzyl)-hydroxyproline, L-(O-tert. butyl)-hydroxyproline, 4-(O-2-naphtyl)-hydroxyproline, 4-(O-2-naphtyl-methyl)-hydroxyproline, 4-(O-phenyl)-hydroxyproline, 4-(4-phenyl-benzyl)-proline, cis-3-phenyl-proline, cis-4-phenyl-proline, trans-4-phenyl-proline, cis-5-phenyl-proline, trans-5-phenyl-proline, 4-benzyl-proline, 4-bromobenzyl-proline, 4-cyclohexyl-proline, 4-fluor-proline, L-tetrahydroisoquinoline-2-carboxylic acid (L-Tic), all diastereomers of octahydro-indole-2-carboxylic acid (Oic), and all diastereomers of 1-aza-bicyclo[3,3,0]octane-2-carboxylic acid or a residue selected from a group of peptidomimetic residues.
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4.发明申请PEPTIDES AND DERIVATIVES THEREOF, THE MANUFACTURING THEREOF AS WELL AS THEIR USE FOR PREPARING A THERAPEUTICALLY AND/OR PREVENTIVELY ACTIVE PHARMACEUTICAL COMPOSITION 审中-公开其制备方法及其衍生物，其制备方法及其用于制备治疗性和/或预防性活性药物组合物的用途公开(公告)号：US20090286740A1
公开(公告)日：2009-11-19
申请号：US12121533
申请日：2008-05-15
摘要： Peptides and derivatives thereof of the following general formula I: (SEQ ID NO: 1) (I)H2N-GHRPX1X2PX3X4X5PX6PPPX7X8X9X10B(1)B(2)B(3)- X11, wherein: B(1) denotes either a chemical bond or the amino acid G B(2) denotes either a chemical bond or the amino acid Y B(3) denotes either a chemical bond or the amino acid R X1—X10 denote one of the 20 genetically encoded amino acids, X11 denotes OR1 with R1=hydrogen or (C1-C10-alkyl), or NR2R3, R2 and R3 being identical or different and denoting hydrogen, (C1-C10)-alkyl or a residue -PEG5-60K, wherein the PEG-residue is linked to the N atom via a spacer, or a residue NH—Y-Z-PEG5-60K, wherein Y denotes a chemical bond or a genetically coded amino acid from among the group of S, C, K or R, and Z denotes a spacer by way of which a polyethylene glycol (PEG)-residue may be linked, as well as the physiologically acceptable salts thereof.
摘要翻译： 下列通式I的肽及其衍生物：（1）（I）H2N-GHRPX1X2PX3X4X5PX6PPPX7X8X9X10B（1）B（2）B（3）-X11其中：B（1）表示化学键或 氨基酸GB（2）表示化学键或氨基酸YB（3）表示化学键或氨基酸R X1-X10表示20种遗传编码氨基酸之一，X11表示OR1，R1 =氢 或（C1-C10-烷基）或NR2R3，R2和R3相同或不同，表示氢，（C1-C10） - 烷基或残基-PEG5-60K，其中PEG-残基通过 间隔基或残基NH-YZ-PEG5-60K，其中Y表示S，C，K或R组中的化学键或遗传编码氨基酸，Z表示间隔基，通过该间隔物，聚乙烯 乙二醇（PEG）残基可以连接，以及其生理上可接受的盐。
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5.发明申请公开(公告)号：US20100081787A1
公开(公告)日：2010-04-01
申请号：US12239579
申请日：2008-09-26
IPC分类号： C07K14/00
摘要： Peptides, peptidomimetics and derivatives thereof of the general formula I: H2N-GHRPX1-β-X4X5X6X7X8X9X10-X11 (I), in which X1-X10 denote one of the 20 genetically coded amino acids, wherein X8, X9 and X10 may also denote a single chemical bond; X11 denotes OR1 in which R1 equals hydrogen or (C1-C10) alkyl NR2R3 with R2 and R3 are equal or different and denote hydrogen, (C1-C10) alkyl, or a residue —W-PEG5-60K, in which the PEG residue is attached via a suitable spacer W to the N-atom, or a residue NH—Y-Z-PEG5-60K, in which Y denotes a chemical bond or a genetically coded amino acids from the group S, C, K or R and Z denotes a spacer, via which a polyethylene glycol (PEG)-residue can be attached, and their physiologically acceptable salts, and β denotes an amino acid, or a peptidomimetic element, which induces a bend or turn in the peptide backbone.
摘要翻译： 通式I：H2N-GHRPX1-＆bgr; -X4X5X6X7X8X9X10-X11（I）的肽，肽模拟物及其衍生物，其中X 1 -X 10表示20个遗传编码氨基酸之一，其中X8，X9和X10也可以表示 单一化学键; X11表示其中R1等于氢的OR1或其中R2和R3相同或不同的（C1-C10）烷基NR2R3，表示氢，（C1-C10）烷基或残基-W-PEG5-60K，其中PEG残基 或者残基NH-YZ-PEG5-60K，其中Y表示化学键或来自S，C，K或R和Z的基因编码氨基酸，Z表示 可以连接聚乙二醇（PEG）残基的间隔物及其生理上可接受的盐， 表示在肽主链中诱导弯曲或转向的氨基酸或拟肽元件。
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6.发明申请PEPTIDES AND PEPTIDE DERIVATIVES, THE PRODUCTION THEREOF AS WELL AS THEIR USE FOR PREPARING A THERAPEUTICALLY AND/OR PREVENTIVELY ACTIVE PHARMACEUTICAL COMPOSITION 审中-公开肽和肽衍生物，其生产方式，因为它们用于制备治疗和/或预防性活性药物组合物公开(公告)号：US20100113740A1
公开(公告)日：2010-05-06
申请号：US12534716
申请日：2009-08-03
IPC分类号： C07K14/00
CPC分类号： C07K14/75
摘要： The invention relates to peptides and peptide derivatives of the following general Formulas Ia and Ib as well as in particular anti-inflammatory drugs containing these peptides.
摘要翻译： 本发明涉及以下通式Ia和Ib的肽和肽衍生物，特别是含有这些肽的抗炎药。
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