申请人:Parke, Davis & Company
公开号:US04111923A1
公开(公告)日:1978-09-05
New octapeptides having the formula Prot Grp-R-Trp-Ser-Tyr-R.sub.2 -Leu-Arg-Pro-R.sub.3 ; salts thereof; wherein R is Gln, Gln (bzl), His (bzl), Ser (bzl), Pro, Leu, Tyr (bzl), Ile, Cys (bzl) or Phe, R.sub.2 is D-Phe, D-Ala, D-Leu, D-Trp, D-Tyr, D-Tyr (Me), D-Ser, D-Met, D-Arg, D-Val, D-His, D-Gln, D-Phs, D-Thr, D-Pro, D-Me.sub.5 Phe or D-Asn and R.sub.3 is NH.sub.2, NH(lower alkyl), N-(lower alkyl).sub.2, NH-benzyl, NHCH.sub.2 CH.sub.2 N-(lower alkyl).sub.2 or NH-CH.sub.2 CH.sub.2 SO.sub.2 NH-benzyl; methods for their production; certain peptide intermediates and their salts used in the production thereof; and the use of said octapeptides as luteinizing hormone releasing factor antagonists.
新的八肽具有公式Prot Grp-R-Trp-Ser-Tyr-R.sub.2 -Leu-Arg-Pro-R.sub.3;其盐;其中R为Gln,Gln(bzl),His(bzl),Ser(bzl),Pro,Leu,Tyr(bzl),Ile,Cys(bzl)或Phe,R.sub.2为D-Phe,D-Ala,D-Leu,D-Trp,D-Tyr,D-Tyr(Me),D-Ser,D-Met,D-Arg,D-Val,D-His,D-Gln,D-Phs,D-Thr,D-Pro,D-Me.sub.5 Phe或D-Asn,R.sub.3为NH.sub.2,NH(较低烷基),N-(较低烷基).sub.2,NH-benzyl,NHCH.sub.2 CH.sub.2 N-(较低烷基).sub.2或NH-CH.sub.2 CH.sub.2 SO.sub.2 NH-benzyl;其生产方法;用于生产的某些肽中间体及其盐;以及将所述八肽用作促黄体生成素释放因子拮抗剂的用途。