PEPTIDES AND PEPTIDE DERIVATIVES AS WELL AS PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME

    公开(公告)号:US20080039388A1

    公开(公告)日:2008-02-14

    申请号:US11678535

    申请日:2007-02-23

    摘要: Peptides and peptide derivatives of the following general Formula I: H2H-GHRPX1X2X3X4X5X6X7X8X9X10-(I) X11PX12PPPX13X14X15X16GYR-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.

    PEPTIDES AND PEPTIDE DERIVATIVES AS WELL AS PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME
    4.
    发明申请
    PEPTIDES AND PEPTIDE DERIVATIVES AS WELL AS PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME 审中-公开
    肽和肽衍生物作为含有其的药物组合物

    公开(公告)号:US20110098442A1

    公开(公告)日:2011-04-28

    申请号:US12280543

    申请日:2007-02-23

    IPC分类号: C07K14/00

    摘要: Peptides and peptide derivatives of the following general Formula (I): H2N-GHRPX1X2X3X4X5X6X7X8X9X10X11PX12PPPX13X14X15X16GYR—X17 (I), 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: 下列通式(I)的肽和肽衍生物:H2N-GHRPX1X2X3X4X5X6X7X8X9X10X11PX12PPPX13X14X15X16GYR-X17(I),其中:X1-X16表示20个遗传编码氨基酸之一,X17表示OR1,其中R1 =氢或(C1-C10 - 烷基)或NR 2 R 3,R 2和R 3相同或不同,表示氢,(C 1 -C 10) - 烷基或残基-PEG 5-60K,其中PEG残基通过间隔基与N原子相连,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的氨基酸,Z表示间隔基,通过其可以使用聚乙二醇(PEG) 可以连接残基,以及其生理上可接受的盐,或其中:X15或X16表示C或K基团的氨基酸,其通过侧面的杂原子与残基Z-PEG5-60K连接 链,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,表示氢 基或(C 1 -C 10) - 烷基,以及其生理上可接受的盐。

    Peptides and peptide derivatives as well as pharmaceutical compositions containing the same
    5.
    发明授权
    Peptides and peptide derivatives as well as pharmaceutical compositions containing the same 失效
    肽和肽衍生物以及含有它们的药物组合物

    公开(公告)号:US07799758B2

    公开(公告)日:2010-09-21

    申请号:US11678535

    申请日:2007-02-23

    IPC分类号: A61K38/16 C07K14/00

    摘要: Therapeutic compositions can include modified peptides which are derived from the chain of the Bbeta(15-42)-fibrin fragment and wherein one or several of the amino acids of the sequence have been substituted by genetically encoded or not genetically encoded amino acids or peptidomimetics. They may exist as free peptides or as C-terminal derivative and/or being linked to a polyethylene glycol (PEG)-polymer, and have anti-inflammatory and/or endothelium stabilizing effects. Esters or amides may for instance be taken into consideration as C-terminal derivatives. Processes for production of the peptides and derivatives thereof are also described.

    摘要翻译: 治疗组合物可以包括衍生自Bβ(15-42) - 纤维蛋白片段的链的修饰肽,并且其中序列的一个或几个氨基酸已被遗传编码的或未经遗传编码的氨基酸或肽模拟物取代。 它们可以作为游离肽或C末端衍生物存在和/或与聚乙二醇(PEG) - 聚合物连接,并具有抗炎和/或内皮稳定作用。 酯或酰胺可以例如被考虑为C末端衍生物。 还描述了肽及其衍生物的制备方法。

    Peptides and peptidomimetic compounds, the manufacturing thereof as well as their use for preparing a therapeutically and/or preventively active pharmaceutical composition
    7.
    发明授权
    Peptides and peptidomimetic compounds, the manufacturing thereof as well as their use for preparing a therapeutically and/or preventively active pharmaceutical composition 失效
    肽和拟肽化合物,其制备及其用于制备治疗和/或预防性活性药物组合物的用途

    公开(公告)号:US08088890B2

    公开(公告)日:2012-01-03

    申请号:US12239579

    申请日:2008-09-26

    CPC分类号: C07K14/75 A61K38/00

    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-Y-Z-PEG5-60K,其中Y表示化学键或来自S,C,K或R族的遗传编码氨基酸,和 Z表示可以连接聚乙二醇(PEG)残留物的间隔物及其生理学上可接受的盐, 表示在肽主链中诱导弯曲或转向的氨基酸或拟肽元件。

    PEPTIDES AND PEPTIDE DERIVATIVES AS WELL AS PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME
    9.
    发明申请
    PEPTIDES AND PEPTIDE DERIVATIVES AS WELL AS PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME 审中-公开
    肽和肽衍生物作为含有其的药物组合物

    公开(公告)号:US20100279924A1

    公开(公告)日:2010-11-04

    申请号:US12820804

    申请日:2010-06-22

    摘要: Therapeutic compositions can include modified peptides which are derived from the chain of the Bbeta(15-42)-fibrin fragment and wherein one or several of the amino acids of the sequence have been substituted by genetically encoded or not genetically encoded amino acids or peptidomimetics. They may exist as free peptides or as C-terminal derivative and/or being linked to a polyethylene glycol (PEG)-polymer, and have anti-inflammatory and/or endothelium stabilizing effects. Esters or amides may for instance be taken into consideration as C-terminal derivatives. Processes for production of the peptides and derivatives thereof are also described.

    摘要翻译: 治疗组合物可以包括衍生自Bβ(15-42) - 纤维蛋白片段的链的修饰肽,并且其中序列的一个或几个氨基酸已被遗传编码的或未经遗传编码的氨基酸或肽模拟物取代。 它们可以作为游离肽或C末端衍生物存在和/或与聚乙二醇(PEG) - 聚合物连接,并具有抗炎和/或内皮稳定作用。 酯或酰胺可以例如被考虑为C末端衍生物。 还描述了肽及其衍生物的制备方法。