PEPTIDES AND DERIVATIVES THEREOF, THE MANUFACTURING THEREOF AS WELL AS THEIR USE FOR PREPARING A THERAPEUTICALLY AND/OR PREVENTIVELY ACTIVE PHARMACEUTICAL COMPOSITION
    3.
    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

    CPC分类号: C07K14/75 A61K38/00

    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。

    PEPTIDES AND DERIVATIVES THEREOF, THE MANUFACTURING THEREOF AS WELL AS THEIR USE FOR PREPARING A THERAPEUTICALLY AND/OR PREVENTIVELY ACTIVE PHARMACEUTICAL COMPOSITION
    5.
    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

    CPC分类号: C07K14/75 A61K38/00

    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。

    PEPTIDES, PEPTIDOMIMETICS AND DERIVATIVES THEREOF, THE MANUFACTURING THEREOF AS WELL AS THEIR USE FOR PREPARING A THERAPEUTICALLY AND/OR PREVENTIVELY ACTIVE PHARMACEUTICAL COMPOSITION

    公开(公告)号:US20090286739A1

    公开(公告)日:2009-11-19

    申请号:US12121526

    申请日:2008-05-15

    CPC分类号: C07K14/75 A61K38/00

    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.