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    Neue Polypeptide mit blutgerinnungshemmender Wirkung, Verfahren zu deren Herstellung bzw. Gewinnung, deren Verwendung und diese enthaltende Mittel
    21.
    发明公开
    Neue Polypeptide mit blutgerinnungshemmender Wirkung, Verfahren zu deren Herstellung bzw. Gewinnung, deren Verwendung und diese enthaltende Mittel 失效
    具有抗凝血活性的新的多肽，它们的制备方法和恢复，其用途和含有它们的药剂。

    公开(公告)号：EP0158986A2

    公开(公告)日：1985-10-23

    申请号：EP85104445.3

    申请日：1985-04-12

    申请人： HOECHST AKTIENGESELLSCHAFT

    发明人： Tripier, Dominique, Dr.

    IPC分类号： C07K7/10 ,  A61K37/02

    CPC分类号： C07K14/815 ,  A61K38/00 ,  Y10S930/26

    摘要： Die Erfindung betrifft Polypeptide der Formel I
    In welcher m=0 - 50, n= 0 - 100 und R den phenolischen Wasserstoff oder eine Phenolestergruppe bedeuten, X für gleiche oder verschiedene Rest natürlich vorkommender a-Aminosäuren steht, Y Val, Ile, Thr, Leu oder Phe bedeu-tet und Z für gleiche oder verschiedene Reste natürlich vorkommender α-Aminosäuren steht und in der die Cys-Reste paarweise über Disulfid-Brücken verknüpft sind, Verfahren zu deren Herstellung bzw. Gewinnung und diese enthaltende Mittel.

    摘要翻译： 本发明涉及式I的多肽I 其中，m = 0 - 50，N = 0 - 100和R是酚氢或酚酯基，X天然存在的α氨基酸是相同的或不同的基团，Y是Val，异亮氨酸 ，苏氨酸，亮氨酸或苯丙氨酸所指-TET和Z表示的天然存在的α氨基酸相同或不同的基团是，并且其中所述Cys残基在对通过二硫键连接，它们的制备和回收和试剂的方法包含它们。

    CYCLIC CRF ANTAGONIST PEPTIDES
    25.
    发明公开
    CYCLIC CRF ANTAGONIST PEPTIDES 失效
    CRF环状多肽拮抗剂

    公开(公告)号：EP0994902A1

    公开(公告)日：2000-04-26

    申请号：EP98923720.1

    申请日：1998-05-26

    申请人： THE SALK INSTITUTE FOR BIOLOGICAL STUDIES

    发明人： RIVIER, Jean, E., F.

    IPC分类号： C07K14/575

    CPC分类号： G01N33/566 ,  A61K38/00 ,  C07K14/57509 ,  G01N33/74 ,  G01N2333/5751 ,  Y10S930/26 ,  Y10S930/27

    摘要： Novel cyclic CRF antagonist peptides are created by shortening the N-terminus of a CRF family peptide by 8 residues and adding an acyl group. CML is present in what would be the 27-position of the native CRF sequence, and a cyclizing bond is created between the side chains of the residues in positions 30 and 33. The side chain of Lys, preferably, in position 33 is linked to the side chain of Glu in position 30 by a lactam bridge. Disclosed CRF antagonists include: (cyclo 30-33)[Ac-Asp?9, D-Phe12, Nle21,38, CML27,40, Glu30, Lys33¿]r/hCRF(9-41); (cyclo 30-33) [Ac-Asp?9, D-Phe12, CML18,27, Nle21,38, Glu30, Lys33¿]r-hCRF(9-41); (cyclo 30-33)[Ac-Asp?9, D-Phe12, Nle21,38, CML27,37, Glu30, Lys33¿]r/hCRF(9-41); (cyclo 30-33)[Ac-Asp?9, D-Phe12, CML14,27, Nle21,38, Glu30, Lys33¿]r/hCRF(9-41); (cyclo 30-33)[Ac-Asp?9, D-Phe12, Nle21,38, CML27, Glu30, Lys33¿]r/hCRF(9-41); and (cyclo 30-33)[Ac-Asp?9, D-Phe12, Nle21,38, CML27,40, Glu30, Aib32, Lys33¿]r/hCRF(9-41).

    IMPROVED CYCLIC CRF AGONISTS
    26.
    发明公开
    IMPROVED CYCLIC CRF AGONISTS 失效
    改进ZYCLISCHE CRF激动剂

    公开(公告)号：EP0800532A1

    公开(公告)日：1997-10-15

    申请号：EP95943747.0

    申请日：1995-12-12

    申请人： THE SALK INSTITUTE FOR BIOLOGICAL STUDIES

    发明人： RIVIER, Jean E.F.

    IPC分类号： G01N33 ,  A61K38 ,  A61K45 ,  A61P25 ,  A61P29 ,  A61P35 ,  C07K14

    CPC分类号： G01N33/5008 ,  A61K38/00 ,  C07K14/57509 ,  G01N33/502 ,  G01N33/566 ,  G01N33/68 ,  G01N33/6842 ,  G01N33/74 ,  G01N2333/5751 ,  Y10S514/805 ,  Y10S930/26

    摘要： Novel cyclic CRF agonist peptides have the amino acid sequence: (cyclo 30-33)Ac-Pro-Pro-Ile-Ser-Leu-Asp-Leu-Thr-D-Phe-His-Leu-Leu-Arg-Glu-Val-Leu-Glu-Nle-Ala-Arg-Ala-Glu-Gln-Leu-Ala-Gln-R30-Ala-R32-R33-Asn-Arg-Lys-Leu-Nle-Glu-Ile-Ile-NH2 wherein R30 is Glu or Cys; R32 is His or a D-amino acid such as D-His, D-Arg or similar; R33 is Lys, Orn or Cys. The N-terminus may be extended by Ser-Glu-Glu. Lys may be substituted for Arg23, and its side chain connected by a lactam bridge to Glu20 to form a bicyclic peptide. Certain disclosed CRF agonists include: (cyclo 30-33)[Ac-Pro?4, D-Phe12, Nle21,38, D-His32, Glu30, Lys33¿]r/hCRF(4-41), (cyclo 30-33)[Ac-Pro?4, D-Phe12, Nle21,38, D-His32, Glu30, Orn33¿]r/hCRF(4-41), (cyclo 30-33)[Ac-Pro?4, D-Phe12, Nle21,38, Cys30,33, D-His32¿]r/hCRF(4-41), (bicyclo 20-23, 30-33)[Ac-Pro¿4?, D-Phe?12, Nle21,38, Lys23,33, Glu30, D-His32¿]-r/hCRF(4-41), (cyclo 30-33)[Ac-Pro¿4?, D-Phe?12, Nle21,38, CML27, Glu30¿, imBzlD-His?32, Lys33¿]r/hCRF(4-41) and (cyclo 30-33)[Ac-Pro?4, D-Phe12, Nle21,38, Glu30, D-Arg32, Lys33¿]r/hCRF(4-41). Labelled agonists such as (cyclo 30-33)[I?125Tyr0, D-Phe12, Nle21,38, Glu30, D-His32, Lys33¿]r/hCRF and (cyclo 30-33)[I?125D-Tyr3, D-Phe12, Nle21,38, Glu30, D-His32, Lys33¿]r/hCRF(3-41) are useful in screening for more potent agonists.

    CRF analogs
    28.
    发明公开
    CRF analogs 失效
    CRF模拟

    公开(公告)号：EP0516450A3

    公开(公告)日：1993-08-18

    申请号：EP92304911.8

    申请日：1992-05-29

    申请人： THE SALK INSTITUTE FOR BIOLOGICAL STUDIES

    发明人： Kornreich, Wayne D. ,  Hernandez, Jean-François ,  Rivier, Jean Edouard Frederic ,  Vale, Wylie Walker, Jr.

    IPC分类号： C07K7/10 ,  A61K37/43

    CPC分类号： C07K14/57509 ,  A61K38/00 ,  Y10S930/26

    摘要： Analogs of CRF, which are based upon hCRF, oCRF and alpha-helical CRF, are disclosed that can be administered to achieve a substantial elevation of ACTH, β-endorphin, β-lipotropin, other products of the pro-opiomelanocortin gene and corticosterone levels. Analogs include those having the formula (see SEQ ID NO:9): Y-Ser-Xaa₂-Glu-Pro-Pro-Ile-Ser-Leu-Asp-Leu-Thr-Phe-His-Leu-Leu-Arg-Glu-Val-Leu-Xaa₂₀-Xaa₂₁-Xaa₂₂-Xaa₂₃-Xaa₂₄-Xaa₂₅- Gln-Leu-Ala-Gln-Gln-Ala-Xaa₃₂-Ser-Asn-Arg-Lys-Leu-Xaa₃₈-Xaa₃₉-Ile-Xaa₄₁-NH₂, wherein Y is an acyl group having 7 or fewer carbon atoms or hydrogen; Xaa₂ is Glu or Gln; Xaa₂₀ is Ala or Glu; Xaa₂₁ is Met or Nle; Xaa₂₂ is Ala or Thr; Xaa₂₃ is Arg or Lys; Xaa₂₄ is D-Ala or Ala; Xaa₂₅ is Glu or Asp; Xaa₃₂ is D-His or His; Xaa₃₈ is Met, Nle or Leu; Xaa₃₉ is Ala, Glu or Asp; Xaa₄₁ is Ile or Ala; provided however that at least one of Xaa₂₀ and Xaa₃₉ is Ala and that the N-terminus may be shortened by a sequence of up to about 5 residues. One example is [Ala²⁰]-oCRF. These analogs or their pharmaceutically acceptable salts, dispersed in an acceptable liquid or solid carrier, can be administered to humans.