IMPROVED CYCLIC CRF AGONISTS
    81.
    发明授权
    IMPROVED CYCLIC CRF AGONISTS 失效
    改进ZYCLISCHE CRF激动剂

    公开(公告)号:EP0800532B1

    公开(公告)日:2006-03-08

    申请号:EP95943747.6

    申请日:1995-12-12

    发明人: RIVIER, Jean E.F.

    IPC分类号: C07K14/575 G01N33/50

    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.

    OXYTOCIN ANTAGONIST
    86.
    发明公开
    OXYTOCIN ANTAGONIST 失效
    催产素防止早产

    公开(公告)号:EP0695309A1

    公开(公告)日:1996-02-07

    申请号:EP94915332.0

    申请日:1994-02-09

    IPC分类号: A61K38 A61P5 A61P13 A61P15 C07K7

    CPC分类号: C07K7/16 A61K38/00 Y10S930/26

    摘要: The oxytocin antagonist represented by formula (I) wherein (S-Pmp IS β,β-(3-thiapentamethylene)-β-mercaptopropionic acid, D-Trp is the D form of tryptophan, and Ile, Gln, Asn, Pen (Pen = penicillamine), Pro, and Arg are the L forms of isoleucine, glutamine, asparagine, proline and arginine, respectively. This compound can be administered to pregnant women to arrest premature labor while avoiding unwanted side effects due to antagonism of the antidiuretic hormone, vasopressin.