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ANALOGUE GNRH DE NON-MAMMIFERES ET SON UTILISATION POUR LA REGULATION DE LA FERTILITE ET DE LA GROSSESSE
专利权人:
SILER-KHODR; THERESA M.
发明人:
申请号:
EP00966970.6
公开号:
EP1255555B1
申请日:
2000.09.26
申请国别(地区):
EP
年份:
2012
代理人:
摘要:
Specially designed non-mammalian GnRH analog decapeptides resistant to degradation by the placental enzyme, C-ase-1, or a post-proline peptidase, are disclosed. The GnRH analogs are further defined as analogs of Chicken II GnRH or Salmon GnRH. These non-mammalian analogs incorporate D-arginine, D-leucine, D-tBu-Serine or D-Trp at position 6 and ethylamide or aza-Gly-amide at position 10. The D-Arg (6)-Chicken II GnRH-ethylamide, D-Arg (6)-Chicken II GnRH-aza-Gly (10)-amide, the D-Arg (6)-Salmon GnRH ethylamide, and D-Arg (6)-Salmon GnRH-aza-Gly (10)-amide analogs are also provided, and demonstrate preferential binding to chorionic GnRH receptor that is greater relative to the biding of these analogs to pituitary GnRH receptor. These non-mammalian GnRH analogs may be used in pharmaceutical preparation, and specifically in various treatment methods as a contraceptive or post-coital contraceptive agent. The non-mammalian GnRH analogs are also provided in pharmaceutical preparations that may be used clinically for maintaining pregnancy when used in very low doses and administered in pulsatile fashion. In another aspect, the non-mammalian GnRH analogs may be used a luteolytic agents. The aza-Gly (10) amide non-mammalian analogs are yet other embodiments of the non-mammalian GnRH analogs provided as a part of the invention.L'invention concerne des décapeptides analogues GnRH de non-mammifères, spécialement conçus pour résister à la dégradation causée par l'enzyme placentaire, C-ase-1, ou une peptidase post-proline. Les analogues GnRH sont en outre définis comme analogues de GnRH de poulet II ou GnRH de saumon. Ces analogues de non-mammifères comprennent la D-arginine, la D-leucine, la D-tBu-Serine ou D-Trp en position 6 et l'éthylamide ou l'aza-Gly-amide en position 10. L'invention concerne également des analogues D-Arg (6) - GnRH poulet II - éthylamide, D-Arg (6) - GnRH-aza-Gly (10)-amide de poulet II, le D-Arg (6) - éthylamide GnRH de saumon, et D-Arg (6) - GnRH-aza-Gly
来源网站:
中国工程科技知识中心
来源网址:
http://www.ckcest.cn/home/
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